Anasthetic Drugs

NOREPINEPHRINE Indication & Dosage Intravenous Acute hypotensive states Adult: Initially, 8-12 mcg/minute, up to 8-30 mcg/minute in refractory
shock. Infuse using a solution of 4 mcg/ml in glucose 5%, or sodium chloride 0.9% and glucose 5% at a rate of 2-3 ml/minute. Adjust according to BP response. Average maintenance dose: 0.5-1 ml/minute (24 mcg/minute). Infuse via a central venous catheter or into a large vein. 2 Child: Administer at a rate of 2 mcg/minute. Alternatively, 2 mcg/m /minute. Adjust rate according to BP response and perfusion. Elderly: Initial dose should be at low end of dose range. Injection Upper gastrointestinal haemorrhage Adult: Intraperitoneal admin: 8 mg in 250 ml of 0.9% sodium chloride inj. Alternatively, instill 8 mg in 100 ml of 0.9% sodium chloride solution through a nasogastric tube every hr for 68 hr, then every 2 hr for 46 hr. Withdraw drug gradually. Reconstitution: Dilute with 5% glucose inj, with or without sodium chloride; dilution with sodium chloride inj alone is not recommended. Incompatibility: Incompatible with alkali and oxidising agents, barbiturates, chlorphenamine, chlorothiazide, nitrofurantoin, novobiocin, phenytoin, sodium bicarbonate, sodium iodide, streptomycin, insulin. Overdosage Contraindications Symptoms: Hypertension, sweating, cerebral haemorrhage, convulsions. Hypertension. Pregnancy. Patients with peripheral or mesenteric vascular thrombosis unless necessary as a life-saving procedure. Not a substitute for replacement of blood, plasma, fluids, and/or electrolytes; correct volume depletion prior to admin. Identify and correct hypoxia, hypercapnia and acidosis prior to or during admin. Avoid extravasation as tissue necrosis may occur. Avoid inj into leg veins, especially in elderly or those with occlusive vascular diseases, arteriosclerosis, DM or Buerger's disease. Hypertensive or hyperthyroid patients. In conjunction with local anaesthetics, do not use in fingers, toes, ears, nose or genitalia. Lactation. Hypertension, headache, peripheral ischaemia, bradycardia, arrhythmias, anxiety, skin necrosis (with extravasation), dyspnoea, respiratory difficulty. Guanethidine, methyldopa, reserpine, TCAs may increase pressor response to norepinephrine. Potentially Fatal: Increased risk of arrhythmias with cocaine, cyclopropane or halogenated hydrocarbon anaesthetics. Hypertensive crisis may occur with MAOIs. Hypertensive effects may be increased by nonselective -blockers. Click to view more norepinephrine Drug Interactions Pregnancy Category (US FDA) Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.
Special Precautions
Adverse Drug Reactions Drug Interactions
Storage
Intravenous: Store at room temperature (25C) and protect from light. Store in tight, lightresistant containers as norepinephrine is readily oxidised. Do not use if discoloured (e.g. pink, dark yellow, brown) or if there is a precipitate.
Mechanism of Action
Norepinephrine is a direct-acting sympathomimetic which stimulates 1- and -adrenergic receptors. Its -agonist effects cause vasoconstriction, thereby raising systolic and diastolic BP with reflex slowing of heart rate. Onset: Rapid. Duration: Short; stops within 1-2 min after discontinuing the infusion. Absorption: Oral: Destroyed in the GI tract; SC: Poorly absorbed. Distribution: Mainly localises in sympathetic nervous tissue; crosses the placenta but not the blood-brain barrier. Metabolism: Metabolised in the liver and in other tissues by the enzymes catechol-Omethyltransferase (COMT) and monoamine oxidase (MAO). Excretion: Via urine (mainly as metabolites).
MIMS Class ATC Classification
Vasoconstrictors C01CA03 - norepinephrine ; Belongs to the class of adrenergic and dopaminergic cardiac stimulants excluding glycosides. Used in the treatment of heart failure.
EPINEPHRINE Indication & Dosage Inhalation Acute asthma Adult: Spray: Aqueous solution with an adrenaline content equivalent to 1:100. Pressurised aerosols delivering metered doses equivalent to approximately 160-275 mcg: 1-2 inhalations, may repeat after 3 hr if necessary. Parenteral Acute asthma Adult: As 1:1,000 aqueous solution: 0.3-0.5 ml (300-500 mcg). Dose may be given via IM or SC inj. Child: As 1:1,000 aqueous solution: 0.01 ml/kg (10 mcg/kg). Max: 0.5 ml (500 mcg). Dose may be given via IM or SC inj. Intravenous Advanced cardiac life support Adult: Initially, 1 mg (10 mL of a 1:10,000 solution), may repeat as often as every 2-3 minutes throughout the resuscitation process. May also be given via intraosseous route at the same dosage. For endotracheal doses: 2-3 times of the IV dose. Child: Initially, 10 mcg/kg, may repeat as often as every 2-3 minutes throughout the resuscitation process. Endotracheal doses: 100 mcg/kg. Intraosseous doses are the same as IV doses. Max Dosage: Intraosseous doses for adults and children are the same as IV doses. Intravenous Anaphylactic shock Adult: 0.5 mg (5 mL of a 1:10,000 solution) given at a slow rate of 100 mcg/minute, stopping when a response is achieved. Child: 10 mcg/kg. If autoinjectors are used, doses are based on body wt: 15-30 kg: 150 mcg and >30 kg: 300 mcg. Intramuscular Anaphylactic shock Adult: As 1:1,000 solution: 500 mcg (0.5 ml), repeat every 5 minutes as needed until improvement occurs. For emergency self-admin (e.g. via autoinjector): A dose of 300 mcg (0.3 ml) may be used. Child: Dose depends on age and weight. Usual dose: 10 mcg/kg. Ophthalmic Ocular hypertension Adult: Instill 0.5%, 1% or 2% eye drops once or twice daily. Ophthalmic Open-angle glaucoma Adult: Instill 0.5%, 1% or 2% eye drops once or twice daily. Overdosage Overdosage intravascular inj of epinephrine may cause cerebral haemorrhage due to a sharp rise in BP. Fatalities may also result from pulmonary oedema because of peripheral vascular constriction together with cardiac stimulation. Preexisting hypertension; occlusive vascular disease; angle-closure glaucoma (eye drops); hypersensitivity; cardiac arrhythmias or tachycardia. When used in addition to local anaesthetics: Procedures involving digits, ears, nose, penis or scrotum. CV diseases; hyperthyroidism; DM; Parkinson's disease; elderly; pregnancy, lactation.
Contraindications
Special Precautions
Adverse Drug Reactions
CNS effects; GI disturbances; epigastric pain; CV disorders; difficulty in micturition with urinary retention; dyspnoea; hyperglycaemia; sweating; hypersalivation; weakness, tremors; coldness of extremities; hypokalaemia. Gangrene, tissue necrosis and sloughing (extravasation) when used in addition to local anaesthetics. Eye drops: Severe smarting, blurred vision, photophobia; naso-lachrymal ducts obstruction. Oedema, hyperaemia and inflammation of the eyes with repeated administration. Halogenated inhalation anaesthetics; - or -blocking agents; methyldopa, guanethidine; drugs with vasoconstrictor and pressor effects; antihypertensives; adrenergic neuron blockers; potassium-depleting drugs; cardiac glycosides; ephedra, yohimbe. TCAs may induce hypertension and arrhythmia. Click to view more epinephrine Drug Interactions Increase in bilirubin, catecholamines, glucose, uric acid.
Drug Interactions
Lab Interference Pregnancy Category (US FDA)
Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus. Storage Inhalation: Store at 25C. Intramuscular: Store at 25C. Intravenous: Store at 25C. Ophthalmic: Store at 25C.Parenteral: Store at 25C. Epinephrine, an active principle of the adrenal medulla, is a direct-acting sympathomimetic. It stimulates - and -adrenergic receptors resulting in relaxation of smooth muscle of the bronchial tree, cardiac stimulation and dilation of skeletal muscle vasculature. It is frequently added to local anaesthetics to retard diffusion and limit absorption, to prolong the duration of effect and to lessen the danger of toxicity. Onset: SC: approx 5-10 min; inhalation: approx 1 min; conjunctival instillation: IOP declines approx 1 hr. Duration: Ocular effect: 12-24 hrs. MIMS Class ATC Classification Cardiac Drugs / Antiasthmatic & COPD Preparations / Antiglaucoma Preparations A01AD01 - epinephrine ; Belongs to the class of other agents for local oral treatment. S01EA01 - epinephrine ; Belongs to the class of sympathomimetics used in the treatment of glaucoma. C01CA24 - epinephrine ; Belongs to the class of adrenergic and dopaminergic cardiac stimulants excluding glycosides. Used in the treatment of heart failure. R01AA14 - epinephrine ; Belongs to the class of topical sympathomimetic agents used as nasal decongestants. B02BC09 - epinephrine ; Belongs to the class of local hemostatics. Used in the treatment of hemorrhage. R03AA01 - epinephrine ; Belongs to the class of adrenergic inhalants, alpha- and betaadrenoreceptor agonists. Used in the treatment of obstructive airway diseases.
Mechanism of Action
DOPAMINE Indication & Dosage Intravenous Acute heart failure Adult: As hydrochloride: Initially, 1-5 mcg/kg/min increased gradually by up to 5-10 mcg/kg/min according to the patient's BP, cardiac output and urine output. Up to 20-50 mcg/kg/min may be required in seriously ill patients. Overdosage Symptoms include excessive BP elevation. Treatment includes reducing rate of admin or temporarily discontinuing therapy until patient's condition stabilises. Usually, no additional remedial measures are needed as dopamine has short duration of action. In severe cases, short-acting -adrenergic blocking agent, phentolamine, may be used. Pheochromocytoma, uncorrected tachyarrhythmias, ventricular fibrillation. Hypersensitivity. Shock secondary to MI, history of peripheral vascular disease. Correct hypovolaemia before infusion. History of occlusive vascular disease e.g, atherosclerosis, Raynaud's disease, Buerger's disease, diabetic endarteritis; disproportionate increase in diastolic pressure. Pregnancy. Nausea, vomiting, tachycardia, ectopic beats, palpitation, anginal pain, hypotension, vasoconstriction, bradycardia, hypertension, dyspnoea, headache, widened QRS complexes, azotaemia. Cyclopropane and halogenated hydrocarbon anaesthetics may sensitise myocardium to dopamine and precipitate ventricular arrhythmias. MAO inhibitors prolong and increase dopamine effects. Ergots potentiate vasoconstriction action of dopamine. Alpha-blockers unmask dopamine's beta action. Click to view more dopamine Drug Interactions Suppresses pituitary secretion of thyroid-stimulating hormone, growth hormone and prolactin.
Contraindications Special Precautions
Drug Interactions
Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus. Storage Mechanism of Action Intravenous: Store below 30C. Dopamine stimulates dopaminergic receptors at lower doses producing renal and mesenteric vasodilation while at higher doses stimulate both dopaminergic and -adrenergic receptors producing cardiac stimulation and renal vasodilation. It increases heart rate and force of contraction. At low infusion rates vasodilatation occurs in the renal, mesenteric, coronary and cerebral beds. At higher rates vasoconstriction in skeletal muscles and a rise in BP. Absorption: Inactivated in the GI tract and body (oral). Metabolism: Into dopamine-related products; converted to noradrenaline. Excretion: Eliminated as metabolic products of noradrenaline; 2 min (elimination half-life). Cardiac Drugs C01CA04 - dopamine ; Belongs to the class of adrenergic and dopaminergic cardiac stimulants excluding glycosides. Used in the treatment of heart failure.
PHENYLEPHRINE Indication & Dosage Oral Nasal congestion Adult: As hydrochloride: 10 mg every 4 hr, max 60 mg daily; or 12 mg up to 4 times daily. Child: Child: 2-6 yr: As tannate salt: 1.87-3.75 mg every 12 hr. 6-12 yr: As hydrochloride salt: 10 mg every 4 hr; as tannate salt: 3.75-7.5 mg every 12 hr. >12 yr: As hydrochloride salt: 1020 mg every 4 hr; as tannate salt: 7.5-15 mg every 12 hr. Nasal Nasal congestion Adult: 0.25 to 1% solution: Instill as nasal drops or a spray into each nostril every 4 hr as needed. Child: 2-6 yr: 0.125% or 0.16% solution: 2-3 drops into each nostril every 4 hr as needed; 612 yr: 0.25% solution: 2-3 drops, or 1-2 sprays, into each nostril every 4 hr as needed. Parenteral Hypotensive states Adult: As hydrochloride: Hypotension: Initially, 2-5 mg as a 1% solution via SC/IM admin with further doses of 1-10 mg if necessary; or 100-500 mcg by slow IV inj as a 0.1% solution, repeat as necessary after at least 15 min. Severe hypotension: 10 mg in 500 ml of glucose 5% or sodium chloride 0.9% infused IV at initial rate of up to 180 mcg/min reduce to 30-60 mcg/min according to response. Child: Acute hypotension: Subcutaneous/IM: 1-12 yr: 100 mcg/kg every 1-2 hr as needed (max: 5 mg); 12-18 yr: 2-5 mg, followed by further doses of 1-10 mg (max initial dose 5 mg) if necessary. IV injection: 1-12 yr: 5 to 20 mcg/kg (max 500 mcg), repeated as needed after at least 15 min; 12-18 yr: 100-500 mcg, repeated as needed after at least 15 min. IV infusion: Solution is diluted with glucose 5% or sodium chloride 0.9% to a concentration of 20 mcg/ml and given via a central venous catheter. 1-16 yr: 100-500 nanograms/kg/min, adjusted according to response; 16-18 yr: initially up to 180 mcg/min, reduced to 30-60 mcg/min according to response. Injection Paroxysmal supraventricular tachycardia Adult: As hydrochloride: Initially, max of 500 mcg as a 0.1% solution, subsequent doses gradually increase by 100-200 mcg, up to 1 mg, if necessary. Ophthalmic Mydriasis Adult: As hydrochloride: Up to 10%. Instill 1 drop, may repeat in 10-60 minutes as needed. May cause intense irritation and a local anaesthetic other than butacaine (incompatible) should be instilled into the eye a few minutes beforehand. Child: 2.5% solution: <1 yr: Instill 1 drop 15-30 min before procedure. 1 yr: Instill 1 drop, may repeat in 10-60 min as needed. Ophthalmic Conjunctival decongestant Adult: As hydrochloride: Usually 0.12%. Instill 1-2 drops into affected eye, up to 4 times daily; do not use for >72 hr. Rectal Haemorrhoids Adult: Cream/ointment: Apply to clean dry area, up to 4 times daily; may be used externally or inserted rectally using applicator. Suppository: Insert 1 suppository, up to 4 times daily.
Child: 12 yr: Cream/ointment: Apply to clean dry area, up to 4 times daily; may be used externally or inserted rectally using applicator. Suppository: Insert 1 suppository, up to 4 times daily. Administration Overdosage Should be taken with food. Vomiting, hypertension, palpitations, paresthesia, ventricular extrasystoles. Treatment is supportive; in extreme cases, IV phentolamine may be used. Hypertension, ventricular tachycardia. Oral: use with or within 14 days of MAOI therapy. Ophthalmic: narrow-angle glaucoma. Severe hyperthyroidism, severe ischaemic heart disease, DM, prostatic hyperplasia. Rebound congestion in prolonged or excessive use of nasal drops. Use 10% eye drops in extreme caution in infants, elderly, cardiac disease, significant hypertension, advanced arteriosclerosis. Pregnancy and lactation. Over-the-counter cough and cold medications should not be used in infants and children <2 yr. Anxiety, reflex bradycardia, tachycardia, arrhythmias, headache, cold extremities/gangrene, hypertension, nausea, vomiting, sweating, weakness, fear, restlessness, insomnia, confusion, irritability, psychotic states, dyspnoea, anorexia, palpitations, extravasation causing tissue necrosis and sloughing, mydriasis, difficulty in micturition and urinary retention, piloerection, increased salivation, hyperglycaemia, lactic acidosis. Ophthalmic solutions may liberate pigment granules from the iris, corneal clouding/damage. Potentially Fatal: Increase in cardiac contractility, which may lead to angina or cardiac arrest; severe hypertension leading to cerebral haemorrhage or pulmonary oedema. Drug Interactions May increase hypertensive effect of beta-blockers (nonselective); MAOI potentiate hypertension; methyldopa and TCA can increase the pressor response. Click to view more phenylephrine Drug Interactions Ephedra and yohimbe may cause CNS stimulation.
Contraindications
Special Precautions
Food Interaction Pregnancy Category (US FDA)
Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus. Storage Injection: Solution for injection: Store vials at 15-30C. Protect from light. Do not use solution if discolored or contains a precipitate. Ophthalmic: Ophthalmic solution: 0.12%: Store at controlled room temperature. Protect from light and excessive heat. 2.5% and 10%: Refer to product labeling. Some products are stored at room temperature, others under refrigeration at 2-8C. Do not use solution if discolored or contains a precipitate.Parenteral: Solution for injection: Store vials at 15-30C. Protect from light. Do not use solution if discoloured or contains a precipitate. Mechanism of Action Phenylephrine is a sympathomimetic with mainly direct effects on alpha-adrenergic receptors and weak beta-adrenergic activity. It causes vasoconstriction of the arterioles of the nasal mucosa and conjunctiva; activates the dilator muscle of the pupil to cause contraction; produces vasoconstriction of arterioles in the body and produces systemic arterial vasoconstriction. Onset: Subcutaneous/IM/Ophthalmic: 10-15 min. IV: immediate.
Duration: Subcutaneous: 1 hr; IM: Up to about 2 hr; IV: 15-30 min; Ophthalmic: maximal mydriasis: 1 hr, recover time: 3-6 hr. Absorption: Systemic absorption follows topical application. Metabolism: Via intestinal monoamine oxidase to phenolic conjugates in the liver. Excretion: Via urine (90%). MIMS Class Mydriatic Drugs / Cough & Cold Preparations / Nasal Decongestants & Other Nasal Preparations / Ophthalmic Decongestants, Anesthetics, AntiInflammatories / Vasoconstrictors / Anorectal Preparations R01AB01 - phenylephrine ; Belongs to the class of topical sympathomimetic combination preparations, excluding corticosteroids. Used as nasal decongestants. C01CA06 - phenylephrine ; Belongs to the class of adrenergic and dopaminergic cardiac stimulants excluding glycosides. Used in the treatment of heart failure. S01FB01 - phenylephrine ; Belongs to the class of sympathomimetics used as mydriatics and cycloplegics. S01GA05 - phenylephrine ; Belongs to the class of sympathomimetics used as ophthalmologic decongestants. R01AA04 - phenylephrine ; Belongs to the class of topical sympathomimetic agents used as nasal decongestants. R01BA03 - phenylephrine ; Belongs to the class of systemic sympathomimetic preparations used as nasal decongestants.
ATC Classification
VASOPRESSINE ndication & Dosage Parenteral Cranial diabetes insipidus Adult: As argipressin: 5-20 units SC/IM every 4 hr. Intravenous Initial control of variceal bleeding Adult: As argipressin: 20 units in 100 ml of glucose 5% infused over 15 min. Contraindications Hypersensitivity. Vascular disease especially coronary artery disease; chronic nephritis (until reasonable blood-nitrogen conc attained). Heart failure; migraine; epilepsy; asthma or other conditions which might be exacerbated by fluid retention; renal impairment; hypertension or other conditions that may worse with BP increase. Adjust fluid intake to avoid fluid overload. Lactation, pregnancy (especially 3rd trimester as it may have oxytocic effect). Pallor, vomiting, nausea, belching, abdominal cramps, tremour, pounding headache, vertigo, fluid retention, hyponatraemia, hypersensitivity reaction, sweating, urticaria, gangrene, desire to defecate, arrhythmias, bradycardia, angina, MI and bronchoconstriction. Potentially Fatal: Anaphylaxis; cardiac arrest or shock. Carbamazepine, chlorpropamide, clofibrate, urea, fludrocortisone and tricyclic antidepressants may potentiate the antidiuretic action of vasopressin. Demeclocycline, noradrenaline, lithium, heparin and alcohol may decrease antidiuretic action of vasopressin. Ganglionic blockers may increase sensitivity to the pressor effect of vasopressin. Increased risk of QT prolongation with dolasetron. Click to view more vasopressin Drug Interactions
Special Precautions
Drug Interactions
Pregnancy Category (US FDA) Category B: Either animal-reproduction studies have not demonstrated a foetal risk but there are no controlled studies in pregnant women or animal-reproduction studies have shown an adverse effect (other than a decrease in fertility) that was not confirmed in controlled studies st in women in the 1 trimester (and there is no evidence of a risk in later trimesters). Storage Intravenous: Store between 15-25C (59-77F). Parenteral: Store between 15-25C (5977F). Mechanism of Action Vasopressin is a posterior pituitary hormone which may be synthetically prepared or extracted from animals. It exerts direct antidiuretic action on the kidneys by increasing tubular reabsorption of water. Vasopressin also acts by constricting the peripheral blood vessels and causes the smooth muscle of the intestine, gall bladder and urinary bladder to contract. Vasopressin is given parenterally or intranasally in the form of argipressin or lypressin. Argipressin is a synthetic type of vasopressin derived from most mammals (including man but excluding pig) while lypressin is vasopressin from pig. Haemostatics / Antidiuretics H01BA01 - vasopressin ; Belongs to the class of vasopressin and analogues. Used in posterior pituitary lobe hormone preparations.
DOBUTAMINE Indication & Dosage Intravenous Acute heart failure Adult: 2.5-10 mcg/kg, up to 0.5-40 mcg/kg according to patient's heart rate, cardiac output, BP and urine output. Intravenous Cardiac stress test Adult: 5 mcg/kg/min for 8 min using a 1 mg/ml solution, dose is then increased at 5 mcg/kg/min until 20 mcg/kg/min, with each dose being infused for 8 min before the next increase. Monitor ECG and stop infusion ifarrhythmias, marked ST segment depression or other adverse effects occur. Overdosage Symptoms may include anorexia, nausea, vomiting, tremor, anxiety, palpitations, headache, shortness of breath, and anginal and nonspecific chest pain. Treatment includes discontinuing drug admin, establishing an airway, ensuring oxygenation and ventilation. Initiate resuscitative measures immediately. Severe ventricular tachyarrhythmias may be treated with propranolol or lidocaine. Hypertension usually responds to dose reduction or therapy discontinuation. Hypersensitivity; idiopathic hypertrophic subaortic stenosis (IHSS). Correct hypovolaemia prior to treatment. Increased risk of rapid ventricular response in patients with atrial fibrillation. Insufficient data to determine the safety and efficacy of dobutamine use after acute MI. Elderly. Neonates. Pregnancy. Increased heart rate and BP, ectopic beats, palpitation. Nausea, headache, chest pain, palpitation, dyspnoea, paraesthesia, leg cramps. Tissue necrosis at site of extravasation. Potentially Fatal: Cardiac arrhythmias, allergy (rare), MI and hypotension. Increased cardiac output when used with nitroprusside. Increased vasopressor effect of dobutamine when used with bretylium, guanethidine, oxytocic drugs or TCAs. Click to view more dobutamine Drug Interactions
Drug Interactions
Pregnancy Category (US FDA) Category B: Either animal-reproduction studies have not demonstrated a foetal risk but there are no controlled studies in pregnant women or animal-reproduction studies have shown an adverse effect (other than a decrease in fertility) that was not confirmed in controlled studies st in women in the 1 trimester (and there is no evidence of a risk in later trimesters). Storage Mechanism of Action Intravenous: Store at 15-30C. Dobutamine increases contractility and heart rate by stimulating -adrenergic receptors in the cardiac tissues. Absorption: Inactivated in the GI tract (oral). Metabolism: Converted to 3-O-methyldobutamine. Excretion: Mainly via urine, via faeces (small amounts); 2 min (elimination half-life). Cardiac Drugs C01CA07 - dobutamine ; Belongs to the class of adrenergic and dopaminergic cardiac stimulants excluding glycosides. Used in the treatment of heart failure.
ATROPINE SULPHATE Indication & Dosage Parenteral Premedication in balanced anaesthesia Adult: 300-600 mcg IM/SC 30-60 minutes before anaesthesia. Alternatively, 300-600 mcg IV immediately before induction of anaesthesia. Child: >20 kg: 300-600 mcg; 12-16 kg: 300 mcg; 7-9 kg: 200 mcg; >3 kg: 100 mcg. Doses to be given via IM/SC admin 30-60 minutes before anaesthesia. Parenteral Organophosphorus poisoning Adult: 2 mg IV/IM, every 10-30 minutes until muscarinic effects disappear or atropine toxicity appears. In severe cases, dose can be given as often as every 5 minutes. In moderate to severe poisoning, a state of atropinisation is maintained for at least 2 days and continued for as long as symptoms are present. Child: 20 mcg/kg given every 5-10 minutes. Parenteral Poisoning or overdosage with compounds having muscarinic actions Adult: 0.6-1 mg IV/IM/SC, repeated every 2 hr. Intravenous Bradycardia Adult: 500 mcg every 3-5 minutes. Total: 3 mg. Max Dosage: 0.04 mg/kg body weight. Ophthalmic Inflammatory eye disorders Adult: Instill 1-2 drops of a 0.5-1% solution up to 4 times daily. Child: As sulfate: Instill 1-2 drops of a 0.5% soln (or 1 drop of a 1% solution) up to tid. Ophthalmic Eye refraction Adult: Instill 1 drop of a 1% solution bid for 1-2 days before the procedure, or on a single occasion 1 hr before the procedure. Child: As sulfate: Instill 1 or 2 drops of a 0.5% soln (or 1 drop of a 1% solution) bid for 1-3 days before the procedure, with a further dose given 1 hr before the procedure. Incompatibility: Incompatible with hydroxybenzoate preservatives. Administration Overdosage May be taken with or without food. Take w/ food or water. May cause hyperthermia, hypertension, increased respiratory rate, nausea and vomiting. May also lead to CNS stimulation. Severe intoxication may lead to CNS depression, coma, respiratory failure and death. Glaucoma, chronic respiratory disease, sick sinus syndrome, thyrotoxicosis, cardiac failure, pyloric stenosis, prostatic hypertrophy. Reflux oesophagitis, elderly, infants and children. Pregnancy. Dry mouth, dysphagia, constipation, flushing and dryness of skin, tachycardia, palpitations, arrhythmias, mydriasis, photophobia, cycloplegia, raised intraocular pressure. Toxic doses cause tachycardia, hyperpyrexia, restlessness, confusion, excitement, hallucinations, delirium and may progress to circulatory failure and resp depression. Eye drops: Systemic toxicity esp in children, on prolonged use may lead to irritation, hyperaemia, oedema and
Contraindications
Special Precautions Adverse Drug Reactions
conjunctivitis. Increased intraocular pressure. Inhalation: Dryness of mouth, throat. Potentially Fatal: Atrial arrhythmias, AV dissociation, multiple ventricular ectopics. Drug Interactions Additive anticholinergic effects with quinidine, antidepressants and some antihistamines. Click to view more atropine Drug Interactions
Pregnancy Category (US FDA) Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus. Storage Intravenous: Store at 15-30C. Ophthalmic: Store at 15-30C. Parenteral: Store at 1530C. Mechanism of Action Atropine is an anticholinergic agent which competitively blocks the muscarinic receptors in peripheral tissues such as the heart, intestines, bronchial muscles, iris and secretory glands. Some central stimulation may occur. Atropine abolishes bradycardia and reduces heart block due to vagal activity. Smooth muscles in the bronchi and gut are relaxed while glandular secretions are reduced. It also has mydriatic and cycloplegic effect. Absorption: Readily absorbed from the GI tract; also absorbed from mucous membranes, eye, and through intact skin. Distribution: Distributes throughout the body and crosses the blood-brain barrier and placenta. Metabolism: Incomplete metabolism in the liver. Excretion: Excreted in urine as unchanged drug and metabolites. Half-life reported to be 4 hr. MIMS Class Mydriatic Drugs / Antidotes, Detoxifying Agents & Drugs Used in Substance Dependence / Other Cardiovascular Drugs / Antidotes, Detoxifying Agents & Drugs Used in Substance Dependence S01FA01 - atropine ; Belongs to the class of anticholinergics used as mydriatics and cycloplegics. A03BA01 - atropine ; Belongs to the class of belladonna alkaloids, tertiary amines. Used in the treatment of functional gastrointestinal disorders.
ATC Classification
EPHEDRINE Indication & Dosage Oral Diabetic neuropathic oedema Adult: 30-60 mg tid. Child: Intravenous Reversal of spinal or epidural anaesthesia-induced hypotension Adult: 3-6 mg or up to 9 mg in a 3 mg/mL soln given as slow Inj repeated every 3-4 min, as needed. Max Dosage: 30 mg. Administration Contraindications Special Precautions May be taken with or without food. Hypersensitivity. Hypertension, thyrotoxicosis, BPH. Lactation. Ischaemic heart disease, hyperthyroidism, diabetes mellitus, hypertension, angle-closure glaucoma, renal impairment; prostatic enlargement; pregnancy, elderly. Anxiety, tachycardia, tremor, dry mouth, hypertension, cardiac arrhythmias, impaired circulation to the extremities, nervousness, insomnia, palpitations. Difficulty in micturition in patients with prostatic enlargement. Nasal drops: Local irritation, rebound nasal congestion and drug-induced rhinitis on prolonged use. Potentially Fatal: Delusions, hallucinations. Seen with hypersensitivity and overdosage. Acute CNS and CVS stimulation presenting as vomiting, fever, hypertension, psychosis. Cardiac arrhythmias. Drug Interactions Reduces antihypertensive effect of bethanidine and guanethidine. May increase clearance of dexamethasone. Increased incidence of adverse effects when used with theophylline. Potentially Fatal: Severe HTN when combined with MAOIs or withi 2 wk of discontinuance of MAOI treatment. Increased risk of arrhythmias with cardiac glycosides, quinidine or tricyclic antidepressants. Increased vasoconstriction or pressor effects with ergot alkaloids or oxytocin. Click to view more ephedrine Drug Interactions Pregnancy Category (US FDA) Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus. Storage Mechanism of Action Intravenous: Store at 15-25C. Oral: Store at 15-25C. Ephedrine has both - and -adrenergic acitivity with pronounced stimulating effects on the CNS. It increases cardiac output, induces peripheral vasoconstriction, bronchodilation, reduces intestinal tone and motility, and relaxes the bladder while contracting the sphincter muscle. It also has stimulant action on the resp center and dilates the pupil witho affecting light reflexes. Absorption: Readily and completely absorbed form the GIT (oral). Metabolism: Hepatic. Excretion: Via urine (largely as unchanged, small amounts of metabolites); 3-6 hrs (elimination half-life).
Vasoconstrictors C01CA26 - ephedrine ; Belongs to the class of adrenergic and dopaminergic cardiac stimulants excluding glycosides. Used in the treatment of heart failure. R01AB05 - ephedrine ; Belongs to the class of topical sympathomimetic combination preparations, excluding corticosteroids. Used as nasal decongestants. S01FB02 - ephedrine ; Belongs to the class of sympathomimetics used as mydriatics and cycloplegics. R03CA02 - ephedrine ; Belongs to the class of adrenergics for systemic use, alpha- and beta-adrenoreceptor agonists. Used in the treatment of obstructive airway diseases. R01AA03 - ephedrine ; Belongs to the class of topical sympathomimetic agents used as nasal decongestants.
LIDOCAINE Indication & Dosage Intravenous Pulseless ventricular fibrillation or ventricular tachycardia Adult: As hydrochloride: 1-1.5 mg/kg repeated as necessary. Max total: 3 mg/kg. For ventricular arrhythmias in more stable patients: Usual loading dose: 50-100 mg as an IV inj at 25-50 mg/minute, may repeat once or twice up to a max of 200-300 mg in 1 hr, followed by 1-4 mg/minute via continuous IV infusion. May need to reduce dose if the infusion is longer than 24 hr. Hepatic impairment: Reduce dose by 50% in acute hepatitis and decompensated cirrhosis. Parenteral Sympathetic nerve block Adult: As hydrochloride: 50 mg (5 ml) of a 1% solution for cervical block or 50-100 mg (5-10 ml) of a 1% solution for lumbar block. Hepatic impairment: Reduce dose by 50% in acute hepatitis and decompensated cirrhosis. Epidural Epidural anaesthesia Adult: As hydrochloride: 2-3 ml solution administered for each dermatome to be anaesthesized. Recommended doses are: lumbar epidural 250-300 mg (25-30 ml of a 1% solution) for analgesia and 225-300 mg (15-20 ml of a 1.5% solution) or 200-300 mg (10-15 ml of a 2% solution) for anaesthesia; for thoracic epidural: 200-300 mg of a 1% solution. For obstetric caudal analgesia, up to 300 mg (30 ml of a 0.5% or 1% solution); for surgical caudal analgesia: 225-300 mg (15-20 ml of a 1.5% solution). For continuous epidural anaesthesia, not to repeat max doses more frequently than 1.5 hrly. Hepatic impairment: Reduce dose by 50% in acute hepatitis and decompensated cirrhosis. Intraspinal Spinal anaesthesia Adult: As hyperbaric solution of 1.5% or 5% lidocaine in 7.5% glucose solution. Normal vaginal delivery: 50 mg (1 ml) of a 5% solution or 9-15 mg (0.6-1 ml) of a 1.5% solution. Caesarian operation: Up to 75 mg (1.5 ml) of a 5% solution. Other surgical procedures: 75100 mg (1.5-2 ml). Hepatic impairment: Reduce dose by 50% in acute hepatitis and decompensated cirrhosis. Intravenous Intravenous regional anaesthesia Adult: 50-300 mg (10-60 ml) of a 0.5% solution without adrenaline; max dose: 4 mg/kg. Hepatic impairment: Reduce dose by 50% in acute hepatitis and decompensated cirrhosis. Urethral Surface anaesthesia Adult: As 2% gel: Female: 60-100 mg inserted into the urethra several minutes before examination. Male: 100-200 mg before catheterisation and 600 mg before sounding or cystoscopy. Hepatic impairment: Reduce dose by 50% in acute hepatitis and decompensated cirrhosis. Intramuscular Emergency treatment of ventricular arrhythmias Adult: As hydrochloride: 300 mg injected into the deltoid muscle, repeat after 60-90 minutes if necessary. Hepatic impairment: Reduce dose by 50% in acute hepatitis and decompensated cirrhosis. Parenteral
Percutaneous infiltration anaesthesia Adult: As hydrochloride: 5-300 mg (1-60 ml of a 0.5% solution or 0.5-30 ml of a 1% solution). Hepatic impairment: Reduce dose by 50% in acute hepatitis and decompensated cirrhosis. Parenteral Peripheral nerve block Adult: As hydrochloride: For brachial plexus block: 225-300 mg (15-20 ml) of a 1.5% solution; for intercostal nerve block: 30 mg (3 ml) of a 1% solution; for paracervical block: 100 mg (10 ml) of a 1% solution on each side, repeated not more frequently than every 90 minutes; for paravertebral block: 30-50 mg (3-5 ml) of a 1% solution; for pudendal block: 100 mg (10 ml) as a 1% solution on each side; for retrobulbar block: 120-200 mg (3-5 ml) of a 4% solution. Hepatic impairment: Reduce dose by 50% in acute hepatitis and decompensated cirrhosis. Injection Pupil dilatation during phacoemulsification cataract surgery Adult: As a 1% ophthalmic preservative-free solution (often used in combination with phenylephrine and cyclopentolate). To be injected into the anterior chamber of the eye at the beginning of the procedure. Mouth/Throat Surface anaesthesia Adult: For pain: 300 mg (15 ml) of 2% solution rinsed and ejected for mouth and throat pain; or gargled and swallowed if necessary for pharyngeal pain. Not to be used more frequently than every 3 hr. Max (topical oral solution): 2.4 g/day. Before bronchoscopy, bronchography, laryngoscopy, oesophagoscopy, endotracheal intubation, and biopsy in the mouth and throat: 40-300 mg (1-7.5 ml) of 4% solution. For dentistry and otorhinolaryngology procedures: 1050 mg of 10% solution sprayed to mucous membrane. For laryngotracheal anaesthesia: 160 mg of 4% solution sprayed or instilled as a single dose into the lumen of the larynx and trachea. Hepatic impairment: Reduce dose by 50% in acute hepatitis and decompensated cirrhosis. Ophthalmic Surface anaesthesia Adult: As hydrochloride 4 % with fluorescein: 1 or more drops as required. Child: As hydrochloride 4 % with fluorescein : As directed by physician. Topical/Cutaneous Surface anaesthesia Adult: As eutectic mixture containing lidocaine base 2.5% and prilocaine base 2.5%: Apply cream to skin under an occlusive dressing before procedure. Use without an occlusive dressing for genital warts. Hepatic impairment: Reduce dose by 50% in acute hepatitis and decompensated cirrhosis. Rectal Haemorrhoids Adult: Apply topically to clean, dry area or using applicator, insert rectally, up to 6 times/day. Child: 12 yr: Apply topically to clean, dry area or using applicator, insert rectally, up to 6 times/day. Hepatic impairment: Reduce dose by 50% in acute hepatitis and decompensated cirrhosis. Rectal Perianal pain and itching Adult: Apply topically to clean, dry area or using applicator, insert rectally, up to 6 times/day.
Child: 12 yr: Apply topically to clean, dry area or using applicator, insert rectally, up to 6 times/day. Hepatic impairment: Reduce dose by 50% in acute hepatitis and decompensated cirrhosis. Reconstitution: Standard diluent: 2 g/250 ml dextrose 5%. Incompatibility: Y-site incompatibility: Amphotericin B cholesteryl sulfate complex, thiopental. Syringe incompatibility: Cefazolin. Admixture incompatibility: Phenytoin, amphotericin B, dacarbazine, methohexital. Overdosage Severe hypotension, asystole, bradycardia, apnoea, seizures, coma, cardiac arrest, respiratory arrest, and death. Hypovolaemia; heart block or other conduction disturbances. Hepatic or renal impairment; CHF and following cardiac surgery; bradycardia; respiratory depression; porphyria; elderly or debilitated patients; pregnancy. Dizziness, paraesthesia, drowsiness, confusion, respiratory depression and convulsions. Potentially Fatal: Hypotension and bradycardia leading to cardiac arrest; anaphylaxis. Additive cardiac effects with IV phenytoin. Effects antagonized by hypokalaemia caused by acetazolamide, loop diuretics and thiazides. Dose requirements may be increased with longterm use of phenytoin and other enzyme-inducers. Potentially Fatal: Cimetidine and propranolol increase plasma concentration and toxicity. Increased risk of myocardial depression with beta blockers and other antiarrhythmics. Click to view more lidocaine Drug Interactions Food Interaction Lab Interference Decreased levels with St John's wort. IM admin of lidocaine increases creatine phosphokinase levels interfering with diagnosis of MI. ROUTE(S) : Intradermal / Topical/Cutaneous
Pregnancy Category (US FDA)
Category B: Either animal-reproduction studies have not demonstrated a foetal risk but there are no controlled studies in pregnant women or animal-reproduction studies have shown an adverse effect (other than a decrease in fertility) that was not confirmed in controlled studies st in women in the 1 trimester (and there is no evidence of a risk in later trimesters). ROUTE(S) : Parenteral
As LA & cardiac drug. Category B: Either animal-reproduction studies have not demonstrated a foetal risk but there are no controlled studies in pregnant women or animal-reproduction studies have shown an adverse effect (other than a decrease in fertility) that was not confirmed in controlled studies st in women in the 1 trimester (and there is no evidence of a risk in later trimesters). Storage Epidural: Stable at room temperature. Intramuscular: Stable at room temperature. Intraspinal: Stable at room temperature. Intravenous: Stable at room temperature. Mouth/Throat: Stable at room temperature. Ophthalmic:Store at 15-25C. Protect from light. Discard after use. Parenteral: Stable at room temperature. Rectal: Stable at room temperature. Topical/Cutaneous: Stable at room temperature. Urethral: Stable at
room temperature. Mechanism of Action Lidocaine is an amide type local anaesthetic. It stabilises the neuronal membrane and inhibits sodium ion movements, which are necessary for conduction of impulses. In the heart, lidocaine reduces phase 4 depolarisation and automaticity. Duration of action potential and effective refractory period are also reduced. Onset: 45-90 sec. Duration: 10-20 min. Absorption: Readily absorbed from the GI tract, mucous membranes, damaged skin, inj sites, including muscle; poor through intact skin. Distribution: Crosses the placenta, blood-brain barrier and enters breast milk. Proteinbinding: 66% (1-acid glycoprotein). Metabolism: 90% hepatic; converted to monoethylglycinexylidide and glycinexylidide. Firstpass metabolism is extensive, bioavailability after oral dose is approx 35%. Excretion: Via urine (<10% unchanged). Elimination half-life: biphasic; initial: 7-30 min; terminal: 1.5-2 hr (adults), 3.2 hr (infants, premature infants). MIMS Class ATC Classification Anaesthetics - Local & General / Cardiac Drugs / Anaesthetics - Local & General C01BB01 - lidocaine ; Belongs to class Ib antiarrhythmics. N01BB02 - lidocaine ; Belongs to the class of amides. Used as local anesthetics. S01HA07 - lidocaine ; Belongs to the class of local ophthalmologic anesthetics. S02DA01 - lidocaine ; Belongs to the class of analgesic and anesthetic agents used as otologicals. C05AD01 - lidocaine ; Belongs to the class of local anesthetics. Used in the topical treatment of hemorrhoids and anal fissures. D04AB01 - lidocaine ; Belongs to the class of topical anesthetics used in the treatment of pruritus. R02AD02 - lidocaine ; Belongs to the class of local anesthetics used in throat preparations.
DEXAMETHASONE Indication & Dosage Oral Anti-inflammatory Adult: 0.75-9 mg daily in 2-4 divided doses; may also be given via IM/IV admin. Child: 1 mth-18 yr: 10-100 mcg/kg daily in 1-2 divided doses via oral admin, adjusted according to response; up to 300 micrograms/kg daily may be used in emergency situations. Oral As a screening test for Cushing's syndrome Adult: 0.5 mg every 6 hr for 48 hr after determining baseline 24-hr urinary 17hydroxycorticosteroid (17-OHCS) concentrations. During the second 24 hr of dexamethasone admin, urine is collected and analysed for 17-OHCS. Alternatively, after a baseline plasma cortisol determination, 1 mg may be given at 11 pm and plasma cortisol determined at 8 am the next morning. Plasma cortisol and urinary output of 17-OHCS are depressed after dexamethasone admin in normal individuals but remain at basal levels in patients with Cushing's syndrome. Oral Acute exacerbations in multiple sclerosis Adult: 30 mg daily for 1 wk followed by 4-12 mg daily for 1 mth. Child: 1 mth-12 yr: 100-400 mcg/kg daily in 1-2 divided doses; 12-18 yr: Initially 0.5-24 mg daily. Max. 24 mg daily. Parenteral Cerebral oedema caused by malignancy Adult: As phosphate: 10 mg IV followed by 4 mg IM every 6 hr until response is achieved, usually after 12-24 hr. May reduce dosage after 2-4 days then gradually discontinued over 57 days. In severe cases, an initial dose of 50 mg IV may be given on day 1, with 8 mg every 2 hr, reduced gradually over 7-13 days. Maintenance dose: 2 mg 2-3 times daily. Child: As phosphate: <35 kg: Initially 20 mg, then 4 mg every 3 hr for 3 days, then 4 mg every 6 hr for 1 day, then 2 mg every 6 hr for 4 days, then decrease by 1 mg daily. >35 kg: Initially 25 mg, then 4 mg every 2 hr for 3 days, then 4 mg every 4 hr for 1 day, then 4 mg every 6 hr for 4 days, then decrease by 2 mg daily. Doses are given via IV inj. Intra-articular Inflammatory joint diseases Adult: 0.8-4 mg depending on the size of the affected joint. For soft-tissue inj, 2-6 mg may be used. May repeat inj every 3-5 days to every 2-3 wk. Intravenous Unresponsive shock Adult: As phosphate: Initially, 40 mg or 1-6 mg/kg as a single IV inj, may repeat every 2-6 hr. Continue high-dose treatment only until patient's condition has stabilised and not to be continued beyond 48-72 hr. Intravenous Bacterial meningitis Adult: 0.15 mg/kg 4 times daily, to be given 10-20 min before or with the 1st dose of antiinfective treatment. Treatment should be given for the first 2-4 days of the anti-infective treatment. Child: As phosphate: 2 mth-18 yr: 150 mcg/kg every 6 hr for 4 days, starting before or with 1st dose of antibacterial treatment. Intravenous
Prophylaxis of nausea and vomiting associated with cytotoxic therapy Adult: Prevention: 10-20 mg 15-30 minutes before admin of chemotherapy on each treatment day. For continuous infusion regimen: 10 mg every 12 hr on each treatment day. For midly emetogenic regimen: 4 mg every 4-6 hr. Ophthalmic Ocular inflammation Adult: As 0.1% suspension: Apply 1-2 drops into the affected eye/s 4-6 times daily in mild disease, up to hrly admin in more severe disease. As 0.05% ointment: Apply 0.5-1 inch ribbon of ointment into the conjunctival sac(s) up to 4 times daily. Reduce to once daily dosing once conditon has improved. Administration Overdosage Should be taken with food. Treatment is supportive and symptomatic. In acute overdosage, gastric lavage or emesis may be used. Hypersensitivity; active untreated infections; ophthalmic use in viral, fungal disease of the eye. Patients with hypothyroidism; cirrhosis, hypertension, CHF, ulcerative colitis, thromboembolic disorders, osteoporosis, glaucoma, cataracts or TB of the eye, diabetes, peptic ulcer. Monitor blood glucose levels in diabetics and coagulation indices in patients on warfarin. Elderly, children and adolescent; pregnancy and lactation. Growth retardation, osteoporosis, peptic ulcer, glaucoma and subcapsular cataracts, vertebral compression fractures. Cushing-like features, pancreatic dysfunction and pancreatitis, GI upsets, increased appetite, increased fragility of the skin. Increased susceptibility to infection. Topical application: Dermal atrophy, local irritation, folliculitis, delayed wound healing, systemic absorption and toxicity with occlusive dressing on application to large areas of the body and broken skin. Topical application to eye: Corneal ulcers, glaucoma and reduced visual ability. Inhalation: Hoarseness, candidiasis of mouth and throat. Intra-articular inj: Aseptic necrosis of bone and joint damage. Potentially Fatal: HPA supression; CV collapse on rapid IV admin. Increased risk of hypokalaemia when used concurrently with potassium-depleting drugs such as amphotericin B and loop diuretics. Reduces efficacy of isoniazid, salicylates, vaccines and toxoids. Increased activity of dexamethasone and cyclosporin when used together. Concurrent use with aspirin or ethanol may lead to increased GI side effects. Potentially Fatal: Reduced efficacy in combination with ephedrine, cholestyramine, phenytoin, phenobarbital andrifampicin. Click to view more dexamethasone Drug Interactions Food Interaction Pregnancy Category (US FDA) Dexamethasone interferes with calcium absorption. Limit caffeine. ROUTE(S) : Ophthalmic
Contraindications
Special Precautions
Drug Interactions
Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus. ROUTE(S) : Oral / Parenteral
D in 1st trimester. Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus. Storage Intra-articular: Store at 15-30C. Intravenous: Store at 15-30C. Ophthalmic: Store at 1530C. Oral: Store at 15-30C. Parenteral: Store at 15-30C. Dexamethasone is a synthetic glucocorticoid which decreases inflammation by inhibiting the migration of leukocytes and reversal of increased capillary permeability. It suppresses normal immune response. Onset: As acetate: Prompt. Duration: 72 hr. Absorption: Readily absorbed from the GI tract (Oral). Distribution: Readily crosses the placenta. Protein binding: About 77%. Metabolism: Hepatic. Excretion: Via urine (65% of the dose within 24 hr). Half-life: About 190 min. Corticosteroid Hormones / Eye Corticosteroids / Topical Corticosteroids D10AA03 - dexamethasone ; Belongs to the class of topical corticosteroids used in the treatment of acne. S02BA06 - dexamethasone ; Belongs to the class of corticosteroids used in the treatment of inflammation of the ear. D07XB05 - dexamethasone ; Belongs to the class of moderately potent (group II) corticosteroids in other combinations. Used in the treatment of dermatological diseases. A01AC02 - dexamethasone ; Belongs to the class of local corticosteroid preparations. Used in the treatment of diseases of the mouth. S03BA01 - dexamethasone ; Belongs to the class of corticosteroids used in ophthalmologic and otologic preparations. R01AD03 - dexamethasone ; Belongs to the class of topical corticosteroids used for prophylaxis and treatment of allergic rhinitis. S01CB01 - dexamethasone ; Belongs to the class of corticosteroids/antiinfectives/mydriatics combinations. Used in the treatment of eye diseases. D07AB19 - dexamethasone ; Belongs to the class of moderately potent (group II) corticosteroids. Used in the treatment of dermatological diseases. S01BA01 - dexamethasone ; Belongs to the class of corticosteroids. Used in the treatment of inflammation of the eye. H02AB02 - dexamethasone ; Belongs to the class of glucocorticoids. Used in systemic corticosteroid preparations. C05AA09 - dexamethasone ; Belongs to the class of products containing corticosteroids for topical use. Used in the treatment of hemorrhoids and anal fissures.
Mechanism of Action
RANITIDINE Indication & Dosage Oral Benign gastric and duodenal ulceration Adult: Initially, 300 mg as a single daily dose at bedtime or 150 mg bid; 300 mg bid for 4 wk may be used induodenal ulcer to improve healing). Treatment duration: 4-8 wk for benign gastric and duodenal ulceration; up to 8 wk in NSAID-associated ulceration. For prevention of NSAID-associated ulceration: 150 mg bid. Child: 3-12 yr: 2-4 mg/kg (max: 150 mg) bid for 4-8 wk. Renal impairment: Dosage reduction is required in severe renal impairment. CrCl (ml/min) Dosage Recommendation 20 Dosage should be halved.
Oral H.pylori infection Adult: 300 mg once daily or 150 mg bid in combination with amoxicillin 750 mg tid and metronidazole 500 mg tid given for 2 wk. Treatment with ranitidine may be continued for a further 2 wk. Renal impairment: Dosage reduction is required in severe renal impairment. CrCl (ml/min) Dosage Recommendation 20 Dosage should be halved.
Oral Gastro-oesophageal reflux disease Adult: 150 mg bid or 300 mg at bedtime for up to 8 wk, may increase to 150 mg four times daily for 12 wk in severe cases. Child: 5-10 mg/kg daily, given in 2 divided doses. Renal impairment: Dosage reduction is required in severe renal impairment. CrCl (ml/min) Dosage Recommendation 20 Dosage should be halved.
Oral Hypersecretory conditions Adult: Initially, 150 mg bid/tid increased to 6 g daily if necessary. Renal impairment: Dosage reduction is required in severe renal impairment. CrCl (ml/min) Dosage Recommendation 20 Dosage should be halved.
Oral Acid aspiration during general anaesthesia Adult: 150 mg given 2 hr before induction of anaesthesia and preferably, an additional dose on the previous evening. Renal impairment: Dosage reduction is required in severe renal impairment. CrCl (ml/min) Dosage Recommendation 20 Dosage should be halved.
Oral Dyspepsia Adult: 75 mg repeated if necessary up to 4 doses daily. Max: 2 wk of continuous use at each time. For chronic episodic dyspepsia: 150 mg bid for up to 6 wk. Renal impairment: Dosage reduction is required in severe renal impairment. CrCl (ml/min) Dosage Recommendation 20 Dosage should be halved.
Parenteral Prophylaxis of acid aspiration during general anaesthesia Adult: 50 mg IV/IM given 45-60 minutes before the induction of anaesthesia. Renal impairment: Dosage reduction is required in severe renal impairment. CrCl (ml/min) Dosage Recommendation 20 Doses should be halved.
Intravenous Hypersecretory conditions Adult: Initially, 1 mg/kg/hr IV infusion, may increase by increments of 0.5 mg/kg/hr starting after 4 hr if necessary. Renal impairment: Dosage reduction is required in severe renal impairment. CrCl (ml/min) Dosage Recommendation 20 Dosage should be halved.
Intravenous Stress ulceration of upper gastrointestinal tract Adult: 50 mg by slow IV Inj as priming dose followed by 125-250 mcg/kg/hr as continuous IV infusion then transfer to oral dose of 150 mg bid once oral feeding is resumed. Renal impairment: Dosage reduction is required in severe renal impairment. CrCl (ml/min) Dosage Recommendation 20 Administration Overdosage Contraindications Special Precautions Dosage should be halved.
May be taken with or without food. May lead to muscular tremors, vomiting and rapid respiration. Porphyria. Exclude malignancy before treating gastric ulcer. Renal and hepatic impairment. Infants, pregnancy and lactation. Headache, dizziness. Rarely hepatitis, thrombocytopaenia, leucopaenia, hypersensitivity, confusion, gynaecomastia, impotence, somnolence, vertigo, hallucinations. Potentially Fatal: Anaphylaxis, hypersensitivity reactions. Antacids may interfere with absorption. May decrease the GI absorption of ketoconazole. Smoking may decrease the plasma levels of ranitidine. May cause an increase in the bioavailability of furosemide. Click to view more ranitidine Drug Interactions
Drug Interactions
Pregnancy Category
(US FDA) Category B: Either animal-reproduction studies have not demonstrated a foetal risk but there are no controlled studies in pregnant women or animal-reproduction studies have shown an adverse effect (other than a decrease in fertility) that was not confirmed in controlled studies st in women in the 1 trimester (and there is no evidence of a risk in later trimesters). Mechanism of Action Ranitidine blocks histamine H2-receptors in the stomach and prevents histamine-mediated gastric acid secretion. It does not affect pepsin secretion, pentagastrin-stimulated factor secretion or serum gastrin. Absorption: 50% with peak plasma concentrations after 2-3 hr (oral); rapid with peak plasma concentrations after 15 min (IM). Distribution: Widely distributed. Crosses the placental barrier and enters breast milk. Protein-binding: 20% Metabolism: Hepatic; converted to N-oxide, S-oxide and desmethylranitidine. Excretion: Urine (as unchanged drug) within 24 hr; faeces; 2-3 hr (elimination half-life). MIMS Class ATC Classification Antacids, Antireflux Agents & Antiulcerants A02BA02 - ranitidine ; Belongs to the class of H2-receptor antagonists. Used in the treatment of peptic ulcer and gastro-oesophageal reflux disease (GERD).
ONDANSENTRON Indication & Dosage Oral Prophylaxis of postoperative nausea and vomiting Adult: 16 mg taken 1 hr before anaesthesia; or 8 mg taken 1 hr before anaesthesia followed by 2 more doses of 8 mg at 8-hr intervals. Hepatic impairment: Moderate or severe hepatic impairment: Max: 8 mg daily. Oral Nausea and vomiting associated with cancer chemotherapy Adult: 24 mg, as a single dose, 30 minutes before the start of single-day chemotherapy. Child: 4-11 yr: 4 mg 30 minutes before chemotherapy; repeat dose at 4 and 8 hr after initial dose, then 4 mg every 8 hr for 1-2 days after completion of chemotherapy. Hepatic impairment: Moderate or severe hepatic impairment: Max: 8 mg daily. Oral Nausea and vomiting associated with cancer chemotherapy or radiotherapy Adult: For less emetogenic chemotherapy and/or radiotherapy: 8 mg 2 hr before treatment followed by 8 mg 8-12 hr later. Hepatic impairment: Moderate or severe hepatic impairment: Max: 8 mg daily. Oral Prevent delayed emesis following chemotherapy Adult: 8 mg bid, for up to 5 days after the end of a course of chemotherapy. Hepatic impairment: Moderate or severe hepatic impairment: Max: 8 mg daily. Parenteral Nausea and vomiting associated with cancer chemotherapy Adult: For highly emetogenic chemotherapy: 8 mg as a single dose, given via IM or slow IV inj immediately before treatment; or 8 mg IM or slow IV inj given immediately before treatment followed by either continuous IV infusion of 1 mg/hr for up to 24 hr or by a further 2 doses of 8 mg 2-4 hr apart; or 32 mg as a single dose via IV infusion over 15 minutes immediately before treatment; or 150 mcg/kg via IV infusion over 15 minutes (beginning 30 minutes before chemotherapy) and repeated 4 and 8 hr after the 1st dose. Anti-emetic efficacy can be enhanced by giving 20 mg dexamethasone sodium phosphate via IV admin before chemotherapy. Child: 6 mth: 150 mcg/kg via IV infusion 30 minutes before the start of chemotherapy, repeat dose at 4 and 8 hr after the first dose; or 0.45 mg/kg/day as a single dose. Hepatic impairment: Moderate or severe hepatic impairment: Max: 8 mg daily. Parenteral Prophylaxis of postoperative nausea and vomiting Adult: 4 mg as a single dose via IM or slow IV inj at induction of anaesthesia. Child: 1 mth: 40 kg: 100 mcg/kg as a single dose; >40 kg: 4 mg as a single dose. Max Dosage: Child: 4 mg. Hepatic impairment: Moderate or severe hepatic impairment: Max: 8 mg daily. Parenteral Postoperative nausea and vomiting Adult: 4 mg IM or slow IV inj as a single dose. Child: 1 mth: 100 mcg/kg slow IV injection, up to a maximum of 4 mg. Hepatic impairment: Moderate or severe hepatic impairment: Max: 8 mg daily. Rectal Nausea and vomiting associated with cancer chemotherapy
Adult: As suppository: 16 mg given 1-2 hr before treatment. Hepatic impairment: Moderate or severe hepatic impairment: Max: 8 mg daily. Rectal Prevent delayed emesis following chemotherapy Adult: As suppository: 16 mg once daily, for up to 5 days after the end of a course of chemotherapy. Hepatic impairment: Moderate or severe hepatic impairment: Max: 8 mg daily. Reconstitution: Prior to IV infusion, dilute in 50 ml D5W or normal saline. Incompatibility: Y-site incompatibility: Acyclovir, allopurinol, aminophylline, furosemide, ganciclovir, lorazepam, amphotericin B, amphotericin B cholesteryl sulfate complex, ampicillin, ampicillin/sulbactam, piperacillin, sargramostim, sodium bicarbonate, amsacrine, cefepime, cefoperazone, methylprednisolone sodium succinate. Administration Overdosage May be taken with or without food. Sudden transient blindness, severe constipation, hypotension, and vasovagal episode with transient secondary heart block. Treatment is supportive. Use with apomorphine (profound hypotension). May cause QT prolongation; caution when used in cardiac diseases, patients who are on medications that can prolong QT or patients with electrolyte abnormalities. Severe hepatic impairment. May mask progressive ileus and/or gastric distension. Pregnancy, lactation. Headache, malaise/fatigue, constipation; drowsiness, fever, dizziness, anxiety, cold sensation; pruritus, rash; diarrhoea; gynaecological disorder, urinary retention; elevated transaminase; local inj site reaction (pain, redness, burning); paresthesia; hypoxia. Rarely: Anaphylaxis, angina, bronchospasm, ECG changes, extrapyramidal symptoms, grand mal seizure, hypokalaemia, tachycardia, vascular occlusive events. Rifampicin and other CYP3A4 inducers reduce levels/effects of ondansetron. Potentially Fatal: Concurrent use may increase the hypotensive effect of apomorphine; avoid concurrent use. Click to view more ondansetron Drug Interactions Food Interaction Extent of absorption increased with food. St John's wort may reduce serum levels of ondansetron.
Drug Interactions
Pregnancy Category (US FDA) Category B: Either animal-reproduction studies have not demonstrated a foetal risk but there are no controlled studies in pregnant women or animal-reproduction studies have shown an adverse effect (other than a decrease in fertility) that was not confirmed in controlled studies st in women in the 1 trimester (and there is no evidence of a risk in later trimesters). Storage Oral: Oral solution: Store at 15-30 C. Protect from light. Tablet: Store at 230C. Parenteral: Vial: Store at 2-30C. Protect from light. Stable with D5W or normal saline for 48 hr at room temperature. Mechanism of Action Ondansetron antagonises 5-HT3 receptor, blocking serotonin, both peripherally on vagal nerve terminals and centrally in the chemoreceptor trigger zone. Onset: Approx 30 minutes. Absorption: Peak plasma concentrations: Oral: 1.5 hr; rectal: 6 hr.
Distribution: Extensively distributed. Protein-binding: 70-75%. Metabolism: Hepatic via multiple enzymatic pathways. Excretion: Via urine (44-60% as metabolites, 5-10% as unchanged), faeces (approx 25%). Terminal elimination half-life: Oral/parenteral: 3 hr; rectal: 6 hr; elderly/renal impairment: prolonged, approx 5 hr; severe hepatic impairment: 15-32 hr. MIMS Class ATC Classification Supportive Care Therapy / Antiemetics A04AA01 - ondansetron ; Belongs to the class of serotonin (5HT3) antagonists. Used for the prevention of nausea and vomiting.
KETOROLAC Indication & Dosage Oral Moderate to severe pain Adult: 10 mg every 4-6 hr. Max: 40 mg/day. Max duration: 7 days. Elderly: 10 mg every 6-8 hr. Max duration: 7 days. Renal impairment: Contraindicated in moderate to severe impairment. Parenteral Moderate to severe pain Adult: 60 mg as a single dose via IM inj or 30 mg as a single IV dose. Alternatively, 30 mg every 6 hr via IM or IV admin up to a max of 120 mg daily. Halve the doses in patients weighing <50 kg. Max duration: 2 days; patient should be transferred to oral therapy as soon as possible. Elderly: 30 mg as a single dose via IM inj or 15 mg as a single IV dose. Alternatively, 15 mg every 6 hr via IM or IV admin up to a max of 60 mg daily. Renal impairment: 30 mg as a single dose via IM inj or 15 mg as a single IV dose. Alternatively, 15 mg every 6 hr via IM or IV admin up to a max of 60 mg daily. Contraindicated in moderate to severe impairment. Ophthalmic Ocular itching associated with seasonal allergic conjunctivitis Adult: As trometamol: Instil 1 drop of a 0.5% solution into the affected eye(s) 4 times daily. Renal impairment: Contraindicated in moderate to severe impairment. Ophthalmic Prophylaxis and reduction of postoperative ocular inflammation Adult: As trometamol: Instil 1 drop of a 0.5% solution into the appropriate eye(s) 4 times daily starting 24 hr after surgery. Continue for 2 wk. Renal impairment: Contraindicated in moderate to severe impairment. Ophthalmic Cystoid macular oedema Adult: As trometamol: Instil 1-2 drops of a 0.5% solution into the appropriate eye(s) every 68 hr starting 24 hr before surgery and continue for 3-4 wk after surgery. Renal impairment: Contraindicated in moderate to severe impairment. Ophthalmic Pain and photophobia after incisional refractive surgery Adult: As trometamol: Instil 1 drop of a 0.5% solution 4 times daily into the operated eye for up to 3 days after surgery. Renal impairment: Contraindicated in moderate to severe impairment. Incompatibility: Y-site incompatibility: Fenoldopam, azithromycin. Syringe incompatibility: Promethazine, hydroxyzine, nalbuphine, haloperidol, prochorperazine edisylate, triethylperazine. Admixture incompatibility: Promethazine, morphine, hydroxyzine, meperidine. Overdosage Symptoms: Abdominal pain, nausea, vomiting, hyperventilation, peptic ulceration, erosive gastritis and renal dysfunction. Management: Supportive and symptomatic. Hypersensitivity to aspirin or other NSAIDs, asthma. Hypovolaemia or dehydration. Do not give postoperatively to patients with high risk of haemorrhage. History of peptic ulcer or coagulation disorders. Nasal polyps, angioedema, bronchospasm. Labour. Moderate to
Contraindications
severe renal impairment. GI bleeding, cerebrovascular bleeding. As prophylactic analgesic before surgery. Pregnancy, lactation. Special Precautions Elderly, patients weighing <50 kg, hepatic dysfunction, heart failure, predisposition to reduced blood volume or renal blood flow. Mild renal impairment; monitor renal function closely. GI ulcer, bleeding and perforation, drowsiness, rash, bronchospasm, hypotension, psychosis, dry mouth, fever, bradycardia, chest pain, dizziness, headache, sweating, oedema, pallor, liver function changes. Transient stinging and local irritation (ophthalmic). Potentially Fatal: Anaphylaxis. Severe skin reactions. MI, stroke, GI bleeding. Drug Interactions May reduce effects of antihypertensives eg ACE inhibitors or angiotensin II receptor antagonists (AIIA). Increased risk of renal toxicity with ACE inhibitors, diuretics. Increased adverse effects with aspirin or other NSAIDs. Hallucinations may occur when used with fluoxetine, thiothixene, alprazolam. Potentially Fatal: Increased risk of GI bleeding with warfarin. May increase toxicity of methotrexate (MTX) and lithium. Increased plasma concentrations with probenecid. Click to view more ketorolac Drug Interactions Pregnancy Category (US FDA) Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.
in 3rd trimester or near delivery. Category D: There is positive evidence of human foetal risk, but the benefits from use in pregnant women may be acceptable despite the risk (e.g., if the drug is needed in a lifethreatening situation or for a serious disease for which safer drugs cannot be used or are ineffective). Storage Ophthalmic: Store at 15-25C (59-77F). Oral: Store at 15-30C (5986F). Parenteral: Store at 15-30C (59-86F). Protect from light. Ketorolac inhibits prostaglandin synthesis by decreasing the activity of the cyclooxygenase enzyme. Onset: 30-60 min (oral); 10 min (IM). Duration: 6-8 hr (oral/IM). Absorption: Well absorbed (oral/IM); peak plasma concentrations after 30-60 min. Distribution: Protein-binding: 99%. Crosses the placenta; enters breast milk; poorly penetrates into CSF. Metabolism: Hepatic via glucuronic acid conjugation. Excretion: Via urine (90%, as unchanged drug and metabolites); via faeces (remaining dose). Terminal elimination half-life: 4-6 hr; 6-7 hr (elderly); 9-10 hr (renal impairment). MIMS Class Nonsteroidal Anti-Inflammatory Drugs (NSAIDs) / Ophthalmic Decongestants, Anesthetics, Anti-Inflammatories M01AB15 - ketorolac ; Belongs to the class of acetic acid derivatives and related substances
Mechanism of Action
ATC Classification
of non-steroidal antiinflammatory and antirheumatic products. S01BC05 - ketorolac ; Belongs to the class of non-steroidal antiinflammatory agents. Used in the treatment of inflammation of the eye.
METOCLOROPAMIDE Indication & Dosage Oral Diabetic gastric stasis Adult: 10 mg 4 times/day. To be given 30 minutes before meals and at bedtime. Usual treatment duration: 2-8 wk. Renal impairment: Moderate to severe: Reduce dose by at least 50% CrCl (ml/min) Dosage Recommendation <40 Reduce dose by at least 50%.
Hepatic impairment: Dose reduction may be necessary. Oral Nausea and vomiting associated with cancer chemotherapy or radiotherapy Adult: 2 mg/kg/dose, given 1 hr before start of treatment. Repeat dose 3 times at 2-hrly intervals. May repeat 2 additional doses at 3-hrly intervals if needed. Max: 12 mg/kg/day. Child: Neonate: 100 mcg/kg every 6-8 hr; 1 mth-1 yr (up to 10 kg): 100 mcg/kg (max 1 mg) bid; 1-3 yr (10-14 kg): 1 mg bid-tid; 3-5 yr (15-19 kg): 2 mg bid-tid; 5-9 yr (20-29 kg): 2.5 mg tid; 9-14 yr (30 kg): 5 mg tid; 15-19 yr (30-59 kg): 5 mg tid; 15-19 yr (60 kg): 10 mg tid. Where wt is less than that specified for a given age group, use the dose corresponding to the wt rather than the age, so that a lower dose is given. Max: 500 mcg/kg. Renal impairment: Moderate to severe: Reduce dose by at least 50%. CrCl (ml/min) Dosage Recommendation <40 Reduce dose by at least 50%.
Hepatic impairment: Dose reduction may be necessary. Oral Gastro-oesophageal reflux disease Adult: 10-15 mg up to 4 times/day, given 30 minutes before meals and at bedtime, depending on severity of symptoms. If symptoms are intermittent, may give single doses of 20 mg prior to the provoking situation. Max Dosage: 500 mcg/kg Renal impairment: Moderate to severe: Reduce dose by at least 50% CrCl (ml/min) Dosage Recommendation <40 Reduce dose by at least 50%
Hepatic impairment: Dose reduction may be necessary. Oral Prevent delayed emesis following chemotherapy Adult: 20-40 mg 2-4 times/day for 3-4 days. Oral Premedication in diagnostic procedures Adult: Child: 1 mth-3 yr and up to 14 kg: 100 mcg/kg (max 1 mg); 3-5 yr and 15-19 kg: 2 mg; 5-9 yr and 20-29 kg: 2.5 mg; 9-15 yr and 30-60 kg: 5 mg; 15-18 yr and >60 kg: 10 mg. To be given as a single dose 5-10 minutes before examination. Parenteral Diabetic gastric stasis Adult: 10 mg 4 times/day via IM/IV admin; to be given 30 minutes before meals and at bedtime. Convert to oral admin when symptoms have subsided sufficiently. Usual treatment
duration: 2-8 wk. Max Dosage: 500 mcg/kg Renal impairment: Moderate to severe: Reduce dose by at least 50% CrCl (ml/min) Dosage Recommendation <40 Reduce dose by at least 50%
Hepatic impairment: Dose reduction may be necessary. Intravenous Nausea and vomiting associated with cancer chemotherapy Adult: For highly emetogenic drugs/regimens: 2 mg/kg as IV infusion to be given 30 minutes before start of treatment. Repeat twice at 2-hrly intervals after the 1st dose. For less emetogenic drugs/regimens: 1 mg/kg may be used. If vomiting is not well-controlled, may continue with 3 additional doses at 2 mg/kg/dose at 3-hrly intervals; if vomiting is wellcontrolled with the 1st 3 doses, may reduce dose to 1 mg/kg given at 3-hrly intervals for 3 additional doses. Child: Neonate: 100 mcg/kg every 6-8 hr; 1 mth-1 yr (up to 10 kg): 100 mcg/kg (max 1 mg) bid; 1-3 yr (10-14 kg): 1 mg bid-tid; 3-5 yr (15-19 kg): 2 mg bid-tid; 5-9 yr (20-29 kg): 2.5 mg tid; 9-14 yr (30 kg): 5 mg tid; 15-19 yr (30-59 kg): 5 mg tid; 15-19 yr (60 kg): 10 mg tid. Where wt is less than that specified for a given age group, use the dose corresponding to the wt rather than the age, so that a lower dose is given. Max: 500 mcg/kg. Renal impairment: Moderate to severe: Reduce dose by at least 50% CrCl (ml/min) Dosage Recommendation <40 Reduce dose by at least 50%
Hepatic impairment: Dose reduction may be necessary. Intravenous Premedication for radiologic examination of the upper gastrointestinal tract Adult: 10 mg. To be given as a single direct IV inj. Child: <6 yr: 100 mcg/kg; 6-14 yr: 2.5-5 mg. To be given as a single direct IV inj. Renal impairment: Moderate to severe: Reduce dose by at least 50%. CrCl (ml/min) Dosage Recommendation <40 Reduce dose by at least 50%.
Hepatic impairment: Dose reduction may be necessary Intravenous Intubation of the small intestine Adult: 10 mg. To be given as a single direct IV inj. Child: <6 yr: 100 mcg/kg; 6-14 yr: 2.5-5 mg. To be given as a single direct IV inj. Renal impairment: Moderate to severe: Reduce dose by at least 50%. CrCl (ml/min) Dosage Recommendation <40 Reduce dose by at least 50%.
Hepatic impairment: Dose reduction may be necessary Intramuscular Postoperative nausea and vomiting Adult: 10 mg, given near the end of the procedure. May repeat every 4-6 hr when necessary. Incompatibility: Incompatible with cephalothin sodium, chloramphenicol sodium, and sodium bicarbonate.
Administration Overdosage Contraindications
Should be taken on an empty stomach. Take hr before meals. Drowsiness, ataxia, extrapyramidal symptoms, seizures, methemoglobinaemia (in infants). GI haemorrhage, mechanical obstruction and perforation; phaeochromocytoma; history of seizures. Children, elderly. Renal or hepatic impairment, porphyria, epilepsy, Parkinson's disease, history of depression. Ability to drive or operate machineries may be impaired. Pregnancy and lactation. Monitor patients on prolonged therapy. Increased risk of tardive dyskinesia in patients on prolonged or high-dose treatment. Extrapyramidal symptoms, restlessness, drowsiness, anxiety, diarrhoea, hypotension, hypertension, headache, depression, blood disorders (e.g. aganulocytosis, methaemoglobinaemia), hypersensitivity reactions (e.g. bronchospasm, rash), galactorrhoea or related disorders, transient increase in plasma aldosterone levels. Potentially Fatal: Neuroleptic malignant syndrome; cardiac conduction disorders may occur with IV dosage form.
Special Precautions
Drug Interactions
Increased sedative effects with CNS depressants. GI effects antagonised by antimuscarinics and opioids. Reduces absorption of digoxin. Increases absorption of ciclosporin, levodopa, aspirin, paracetamol. Interferes with hypoprolactinaemic effect of bromocriptine. Inhibits serum cholinesterase and prolongs neuromuscular blockade produced by suxamethonium and mivacurium. Potentially Fatal: Serotonin syndrome with sertraline (SSRI). Click to view more metoclopramide Drug Interactions
Food Interaction Lab Interference Pregnancy Category (US FDA)
Avoid ethanol (may increase CNS depression). Increased aminotransferase, increased amylase.
Category B: Either animal-reproduction studies have not demonstrated a foetal risk but there are no controlled studies in pregnant women or animal-reproduction studies have shown an adverse effect (other than a decrease in fertility) that was not confirmed in controlled studies st in women in the 1 trimester (and there is no evidence of a risk in later trimesters). Storage Intramuscular: Store intact vial at 20-25C (68-77F). Protect from light. Intravenous: Store intact vial at 20-25C (68-77F). Protect from light. Dilutions with D5W or normal saline are stable for at least 24 hr and do not require light protection if used within 24 hours. Oral: Store tablets at 20-25C (68-77F). Parenteral: Store intact vial at 20-25C (68-77F). Protect from light. Dilutions with D5W or normal saline are stable for at least 24 hr and do not require light protection if used within 24 hr. Mechanism of Action Metoclopramide enhances the motility of the upper GI tract and increases gastric emptying without affecting gastric, biliary or pancreatic secretions. It increases duodenal peristalsis which decreases intestinal transit time, and increases lower oesophageal sphincter tone. It is also a potent central dopamine-receptor antagonist and may also have serotonin-receptor (5HT3) antagonist properties. Absorption: Rapidly and almost completely absorbed from the GI tract (oral); peak plasma concentrations after 1-2 hr. Distribution: Widely distributed; crosses the blood-brain barrier and placenta; enters breast milk.
Metabolism: Extensively hepatic. Excretion: Via urine (as unchanged drug, sulfate or glucuronide conjugates and metabolites), faeces; 4-6 hr (terminal elimination half-life). MIMS Class ATC Classification Antiemetics / GIT Regulators, Antiflatulents & Anti-Inflammatories A03FA01 - metoclopramide ; Belongs to the class of propulsives. Used in the treatment of functional gastrointestinal disorders.
PETHIDINE Indication & Dosage Oral Moderate to severe acute pain Adult: As hydrochloride: 50-150 mg every 4 hr if needed. Child: As hydrochloride: Children 2 mth to 12 yr: 0.5-2 mg/kg; 12-18 yr: 50-100 mg. Repeat dose every 4-6 hr if necessary. Elderly: As hydrochloride: 50 mg every 4 hr. Renal impairment: Dose reductions may be necessary. Hepatic impairment: Dose reductions may be necessary. Parenteral Moderate to severe acute pain Adult: As hydrochloride: 25-100 mg IM/SC inj or 25-50 mg by slow IV inj repeated after 4 hr. Child: As hydrochloride: SC/IM: 2 mth to 12 yr: 0.5-2 mg/kg; 12-18 yr: 20-100 mg. Repeat dose every 4-6 hr if needed. IV inj: Neonates and children 12 yr: 0.5 -1 mg/kg IV inj every 10-12 hr if needed in those up to 2 mth and every 4-6 hr if needed in older children. 12-18 yr: 25-50 mg every 4-6 hr if needed. Alternatively, 1 mth: Loading dose: 1 m g/kg by IV inj followed by 100-400 mcg/kg/hr via continuous IV infusion adjusted according to response. Elderly: 25 mg every 4 hr. Renal impairment: Dose reductions may be necessary. Hepatic impairment: Dose reductions may be necessary. Parenteral Obstetric analgesia Adult: As hydrochloride: 50-100 mg by IM/SC inj as soon as contractions occur at regular intervals; repeat after 1-3 hr if needed. Max: 400 mg in 24 hr. Renal impairment: Dose reductions may be necessary. Hepatic impairment: Dose reductions may be necessary. Parenteral Preoperative medication Adult: As hydrochloride: 25-100 mg IM/SC given 1 hr before surgery. Child: As hydrochloride: 1-2 mg/kg given IM 1 hr before surgery. Renal impairment: Dose reductions may be necessary. Hepatic impairment: Dose reductions may be necessary. Parenteral Postoperative pain Adult: As hydrochloride: 25-100 mg IM/SC inj every 2-3 hr if necessary. Child: As hydrochloride: 0.5-2 mg/kg IM every 2-3 hr if necessary. Renal impairment: Dose reductions may be necessary. Hepatic impairment: Dose reductions may be necessary. Intravenous Adjunct to anaesthesia Adult: As hydrochloride: 10-25 mg by slow IV inj. Renal impairment: Dose reductions may be necessary. Hepatic impairment: Dose reductions may be necessary. Reconstitution: IV infusion: Dilute with glucose 5% or sodium chloride 0.9% to required volume. IV inj: Dilute with water for inj to a concentration of 5-10 mg/ml. Incompatibility: Y-site incompatible with idarubicin, imipenem/cilastatin, minocycline,
allopurinol, amphotericin B cholesteryl sulfate complex, cefepime, cefoperazone, doxorubicin liposome. Admixture incompatibility: Aminophylline, amobarbital, floxacillin, furosemide, heparin, morphine, phenobarbital, phenytoin, thiopental, pentobarbital. Syringe incompatibility: Pentobarbital, heparin, morphine. Overdosage Symptoms: CNS/respiratory depression, mydriasis, bradycardia, pulmonary oedema, chronic tremor, CNS excitability, seizures. Treatment: Symptomatic. Naloxone can be used to reverse opioid effects. Do not use naloxone for pethidine-induced seizures. May impair ability to drive or operate machinery. Hypovolaemia, CV disease; adrenal insufficiency; biliary tract disorder; CNS depression or coma; history of drug abuse or acute alcoholism; head injury, intracranial lesions, elevated intracranial pressure; hepatic or renal impairment; morbidly obese; prostatic hyperplasia; toxic psychoses; pre-existing respiratory compromise (hypoxia and/or hypercapnia), COPD or other obstructive airway disease; sickle-cell disease; supraventricular tachycardia; thyroid dysfunction. Elderly and debilitated patients. Withdraw gradually. Pregnancy (avoid prolonged use or high doses at term) and lactation. Hypotension; fatigue, drowsiness, dizziness, nervousness, headache, restlessness, malaise, confusion, depression, hallucinations, tremors, muscle twitches, increased intracranial pressure, seizure, serotonin syndrome; rash, urticaria; nausea, vomiting, constipation, anorexia, stomach cramps, xerostomia, biliary spasm, paralytic ileus, sphincter of Oddi spasm; ureteral spasms, decreased urination; pain at inj site; weakness; dyspnoea; histamine release, physical and psychological dependence. Increased pethidine metabolite levels with aciclovir, cimetidine, ritonavir. Reduced analgesic effects withphenytoin, barbiturates. Additive sedative and/or respiratory depressive effects with alcohol, barbiturates, benzodiazepines, phenothiazines, TCAs, other CNS depressants. Potentially Fatal: Increased risk of serotonin syndrome with MAOIs (not be given concurrently or within 14 days of their discontinuation), serotonin agonists, serotonin reuptake inhibitors, sibutramine, TCAs. Click to view more pethidine Drug Interactions Food Interaction Pregnancy Category (US FDA) Category B: Either animal-reproduction studies have not demonstrated a foetal risk but there are no controlled studies in pregnant women or animal-reproduction studies have shown an adverse effect (other than a decrease in fertility) that was not confirmed in controlled studies st in women in the 1 trimester (and there is no evidence of a risk in later trimesters). Increased CNS depression with valerian, St John's wort, kava kava, gotu kola.
Special Precautions
Drug Interactions
if prolonged use/high doses at term. Category D: There is positive evidence of human foetal risk, but the benefits from use in pregnant women may be acceptable despite the risk (e.g., if the drug is needed in a lifethreatening situation or for a serious disease for which safer drugs cannot be used or are ineffective). Storage Intravenous: Store at room temperature. Do not freeze and protect from light. Oral: Protect from light. Store at room temperature. Parenteral: Store at room temperature. Do not freeze and protect from light.
Mechanism of Action
Pethidine is a phenylpiperidine derivative opioid analgesic. It acts mainly as mu-receptor agonist. Like most, opioid analgesics, it mimics endogenous opioids by activating opioid receptors in the central and peripheral nervous system. It reduces the release of neurotransmitter substances and also reduces the activity of postsynaptic neurons in the spinal cord thus preventing transmission of pain impulse. Absorption: Absorbed from the GI tract; only 50% reaches the circulation due to 1st-pass effect. Peak plasma concentrations after 1-2 hr (oral). Variable absorption (IM). Distribution: Crosses the placenta; enters breast milk; appears in CSF. Protein-binding: 6080%. Metabolism: Extensively hepatic via hydrolysis to pethidinic acid and norpethidinic acid and via demethylation to norpethidine. Excretion: Via urine (small amounts as unchanged drug); elimination half-life: 3-5 hr (unchanged drug), 20 hr (norpethidine).
Analgesics (Opioid) N02AB02 - pethidine ; Belongs to the class of phenylpiperidine derivative opioids. Used to relieve pain.
FENTANYL Indication & Dosage Oral Breakthrough cancer pain Adult: For patients who are already receiving and tolerant to opioid treatment: As a loz: Initially, 200 mcg over 15 minutes for an episode of breakthrough pain; may repeat once after 15 minutes if needed. Titrate subsequent doses based on response up to 1.6 mg per dose. Once the effective dose has been identified, no more than 4 unit doses should be taken daily. Elderly: and debilitated patients: Dose reduction may be needed. Intravenous Adjunct to general anaesthesia Adult: For patients with spontaneous respiration: Initially, 50-200 mcg followed by supplements of 50 mcg. To be injected over 3-5 minutes. Possible increased risk of resp depression following doses >200 mcg. For patients with assisted ventilation: Initially, 300-3,500 mcg (up to 50 mcg/kg) followed by supplements of 100-200 mcg depending on the patient's response. To be injected over 3-5 minutes. Child: For patients with spontaneous respiration: >2 yr: 3-5 mcg/kg IV, supplements of 1 mcg/kg may be given. For patients with assisted ventilation: >2 yr: Initially, 15 mcg/kg with supplements of 1-3 mcg/kg. Elderly: and debilitated patients: Dose reduction may be needed. Transdermal Intractable chronic pain Adult: Patches deliver fentanyl in doses that range from 12-100 mcg/hr. Doses should be individually titrated based on previous use of opioids. For opioid-naive patients: Initiate with patches that deliver not more than 25 mcg/hr of fentanyl. Recommended for opioid-naive patients to start with low doses of short-acting opioids before starting on fentanyl patches. For patients who have been receiving a strong opioid, the initial dose should be based on the previous 24-hr opioid requirement. During transfer to fentanyl patches, previous opioid treatment should be phased out gradually. If patient requires doses >100 mcg/hr, >1 patch may be used; consider alternative or additional therapy if doses >300 mcg/hr are required. Replace patch every 72 hr and apply the new patch to a different site; avoid using the same area of skin for a few days. Elderly: and debilitated patients: Dose reduction may be needed. Intramuscular Premedication before anaesthesia Adult: 50-100 mcg, to be given 30-60 minutes before induction of anaesthesia. Elderly: and debilitated patients: Dose reduction may be needed. Incompatibility: Thiopental sodium and methohexital sodium. Contraindications Special Precautions Hypersensitivity. Myasthaenia gravis. Head injury; increased intracranial pressure; intracranial lesions; renal or hepatic impairment; neonates; opioid-nontolerant patients. Increased risk of respiratory depression in elderly, debilitated patients, patient with hypoxia or hypercapnia. Hypothyroidism, prostatic hyperplasia, inflammatory bowel disorders, bradycardia or bradyarrhythmias. Rapid IV infusion may cause skeletal muscle and chest wall rigidity, impaired ventilation or respiratory distress/arrest. Prolonged use may cause tolerance, psychological and physical dependence. Abrupt withdrawal after prolonged admin may lead
to withdrawal symptoms. Lactation. Pregnancy (avoid high doses or prolonged usage). Adverse Drug Reactions Nausea, vomiting; bradycardia, oedema, CNS depression, confusion, dizziness,drowsiness, headache, sedation, transient hypotension, peripheral vasodilation; increased intracranial pressure. High IV dose may cause chest wall rigidity. Transdermal: Rash, erythema and itching. Potentially Fatal: Respiratory depression, trunk rigidity, laryngospasm, bronchoconstriction. Depressant effects may be enhanced by other CNS depressants e.g. alcohol, anaesthetics, anxiolytics, hypnotics, TCAs and antipsychotics. Ammonium chloride may increase excretion of fentanyl. Phenothiazines may increase hypotensive effect of opioid analgesics. Serum levels may be increased by CYP3A4 inhibitors (e.g. azole antifungals, clarithromycin, diclofenac, doxycycline, erythromycin, imatinib, isoniazid, nefazodone, nicardipine,propofol, protease inhibitors, quinidine, telithromycin and verapamil). May reduce the efficacy of pegvisomant. Serum levels may be reduced by rifamycin derivatives. May increase serotonergic effect of SSRIs andsibutramine. Click to view more fentanyl Drug Interactions Avoid valerian, kava-kava and gotu kola. Serum levels may be reduced by St John's wort.
Drug Interactions
Food Interaction Pregnancy Category (US FDA)
Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.
if prolonged use/high doses at term. Category D: There is positive evidence of human foetal risk, but the benefits from use in pregnant women may be acceptable despite the risk (e.g., if the drug is needed in a lifethreatening situation or for a serious disease for which safer drugs cannot be used or are ineffective). Storage Intramuscular: Store between 20-25C. Intravenous: Store between 20-25C. Oral: Store between 20-25C.Transdermal: Store between 20-25C. Fentanyl is a potent opioid analgesic that increases pain threshold, alters pain reception and inhibits ascending pain pathways by binding to stereospecific receptors within the CNS. Onset: Rapid. Duration: Short. Distribution: Rapidly into tissues; appears in the CSF, crosses the placenta and small amounts enter the breast milk. Protein-binding: 80% Metabolism: Hepatic via N-dealkylation and hydroxylation. Excretion: Urine (as metabolites and unchanged drug); 4 hrs (elimination half-life). MIMS Class ATC Classification Analgesics (Opioid) N02AB03 - fentanyl ; Belongs to the class of phenylpiperidine derivative opioids. Used to relieve pain. N01AH01 - fentanyl ; Belongs to the class of opioid anesthetics. Used as general anesthetics.
Mechanism of Action
MORPHINE Indication & Dosage Oral Pain relief Adult: Initially, 5-20 mg every 4 hr (or equivalent for modified release formulations). Start with low dose and adjust according to response. Elderly: Dosage may need to be reduced. Renal impairment: Dosage may need to be reduced. Hepatic impairment: Dosage may need to be reduced. Oral Intractable cough associated with lung cancer Adult: Initially, 5 mg oral solution given every 4 hr. Adjust according to response. Intravenous Pain associated with myocardial infarction Adult: 10 mg at a rate of 2 mg/minute followed by a further dose of 5-10 mg if necessary. Elderly: 5 mg at a rate of 2 mg/min followed by a further dose of 2.5-5 mg if necessary. Renal impairment: Dosage may need to be reduced. Hepatic impairment: Dosage may need to be reduced. Intravenous Acute pulmonary oedema Adult: 5-10 mg via slow inj at a rate of 2 mg/minute. Elderly: Dosage may need to be reduced. Renal impairment: Dosage may need to be reduced. Hepatic impairment: Dosage may need to be reduced. Parenteral Acute pain Adult: IM or SC admin:: 10 mg every 4 hr (or more frequently during titration); adjust according to response. IV admin: Initially, 2.5 mg every 4 hr (or more frequently during titration), adjust according to response Child: By IM or SC inj: <1 mth: 150 mcg/kg 6 hrly; 1-12 mth: 200 mcg/kg 6 hrly; 1-5 yr: 2.5-5 mg 4 hrly; 5-12 yr: 5-10 mg 4 hrly. Repeat doses should only be given when necessary. Adjust according to response. Elderly: Dosage may need to be reduced. Renal impairment: Dosage may need to be reduced. Hepatic impairment: Dosage may need to be reduced. Intraspinal Moderate to severe pain Adult: Initially, 5 mg epidural inj; after 1 hr, additional doses of 1-2 mg may be given if pain relief is unsatisfactory up to a total dose of 10 mg/24 hr. Alternatively, 2-4 mg/24 hr continuous infusion, increased by further 1-2 mg increments if necessary. Elderly: Dosage may need to be reduced. Renal impairment: Dosage may need to be reduced. Hepatic impairment: Dosage may need to be reduced. Intrathecal Moderate to severe pain Adult: 0.2-1 mg, to be injected on a single occasion. Parenteral Premedication in surgery
Adult: IM/SC inj: Up to 10 mg 60-90 minutes before operation. Child: IM inj: 150 mcg/kg before operation. Elderly: Lower dose may be required. Renal impairment: Dosage may need to be reduced. Hepatic impairment: Dosage may need to be reduced. Intravenous Unstable angina not responsive to anti-ischaemic therapy Adult: 2-5 mg repeated every 5-30 minutes as needed for symptom relief. Parenteral Analgesia during labour Adult: 10 mg by IM or SC inj. Rectal Chronic pain Adult: Initially, 15-30 mg suppository every 4 hr, adjusted according to response. Administration Overdosage May be taken with or without food. May be taken w/ meals to reduce GI discomfort. Characterised by respiratory depression and sometimes CNS depression. Maintain adequate respiratory function. Naloxone may be used as an antidote (repeated admin may be necessary following intrathecal or epidural overdosage). Respiratory depression, acute or severe asthma; paralytic ileus; obstructive airway disease; acute liver disease; comatose patients; increased intracranial pressure; acute alcoholism. Pulmonary oedema resulting from a chemical respiratory irritant. Elderly; hypothyroidism; renal and liver disease; head injury, intracranial lesions; hypotension, circulatory shock; adrenocortical insufficiency; asthma; prostatic hyperplasia; inflammatory or obstructive bowel disease; myasthaenia gravis; infants <3 mth; pregnancy, lactation; hypovolaemia, biliary tract disorders. Convulsions; nausea, vomiting, dry mouth, constipation; urinary retention; headache, vertigo; palpitations; hypothermia; pruritus, urticaria; tachycardia, bradycardia; blurred vision; miosis; dependency; drowsiness; lightheadedness; dizziness; sweating; dysphoria; euphoria. Potentially Fatal: Respiratory depression; circulatory failure; hypotension; deepening coma; anaphylactic reactions. Drug Interactions May potentiate effects of TCAs; increased risk of serotonin syndrome with serotonergic drugs; risk of cardiac arrythmias with QT prolonging drugs; sedative effects may be increased by metoclopramide; antagonises efficacy of diuretics; morphine levels decreased by rifampicin. Potentially Fatal: Increased CNS depression with other CNS depressants (e.g. other opioids, general anaesthetics, benzodiazepines, barbiturates), alcohol. Risk of severe hypotension with MAOIs. Click to view more morphine Drug Interactions Pregnancy Category (US FDA) Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.
Contraindications
Special Precautions
if prolonged use/high doses at term. Category D: There is positive evidence of human foetal risk, but the benefits from use in pregnant women may be acceptable despite the risk (e.g., if the drug is needed in a lifethreatening situation or for a serious disease for which safer drugs cannot be used or are ineffective). Storage Mechanism of Action Intravenous: Store at 20-25C. Morphine is a phenanthrene derivative which acts mainly on the CNS and smooth muscles. It binds to opiate receptors in the CNS altering pain perception and response. Analgesia, euphoria and dependence are thought to be due to its action at the mu-1 receptors while respiratory depression and inhibition of intestinal movements are due to action at the mu-2 receptors. Spinal analgesia is mediated by morphine agonist action at the K receptor. Cough is suppressed by direct action on cough centre. Onset: 1 hr (oral); 5-10 minutes (IV); 20-60 minutes (rectal); 50-90 minutes (SC); 30-60 minutes (IM). Duration: 4 hr. Absorption: Variably absorbed from the GI tract (oral); readily absorbed into blood (IM/SC). Distribution: Kidneys, liver, lungs, spleen, brain and muscles (low concentrations); crosses the blood-brain barrier and placenta; enters breast milk. Protein-binding: 20-35%. Metabolism: Hepatic and gut by glucuronidation; extensive first-pass metabolism. Excretion: Faeces, urine (as metabolites and unchanged drug) Elimination half-life of around 2 hr but varies between individuals. MIMS Class ATC Classification Cough & Cold Preparations / Analgesics (Opioid) N02AA01 - morphine ; Belongs to the class of natural opium alkaloids. Used to relieve pain.
BUPIVACAINE Indication & Dosage Injection Percutaneous infiltration anaesthesia Adult: 0.25% solution is typically used. For prolonged action: 9 mg (1.8 ml) of a 0.5% solution with adrenaline(1:200,000) can be admin, repeated once after 2-10 min if necessary. Max total: 90 mg/dental sitting. Max single dose: 150 mg with or without adrenaline, followed by 50 mg every 2 hr if needed. Injection Peripheral nerve block Adult: 12.5 mg (5 ml) of a 0.25% solution or 25 mg (5 ml) of a 0.5% solution. Max single dose: 150 mg with or without adrenaline, followed by 50 mg every 2 hr if needed. Injection Sympathetic nerve block Adult: 50-125 mg (20-50 ml) of a 0.25% solution. Injection Retrobulbar block Adult: 15-30 mg (2-4 ml) of a 0.75% solution. Injection Caudal block Adult: In surgery: 37.5-75 mg (15-30 ml) of a 0.25% solution or 75-150 mg (15-30 ml) of a 0.5% solution. With analgesia during labour: 25-50 mg (10-20 ml) of a 0.25% solution or 50100 mg (10-20 ml) of a 0.5% solution. Injection Lumbar epidural block Adult: In surgery: 25-50 mg (10-20 ml) of a 0.25% solution or 50-100 mg (10-20 ml) of a 0.5% solution. With analgesia during labour: 15-30 mg (6-12 ml) of a 0.25% solution or 30-60 mg (6-12 ml) of a 0.5% solution. In non-obstetric surgery: 75-150 mg (10-20 ml) of a 0.75% solution. Overdosage Management includes careful and constant monitoring of CV and respiratory vital signs and the patient's state of consciousness after each local anaesthetic inj. Establish and maintain a patent airway, oxygen may be needed. If necessary, drugs may be used to control convulsions. Hypotension may also be managed by giving IV fluids such as sodium chloride inj. Hypersensitivity to local anaesthetics of amide type. IV regional anaesthesia; paracervical block in obstetrics; spinal anaesthesia <18 yr. Lactation. Solutions containing preservatives for caudal or epidural block. Hepatic disease; CV disease; children <12 yr; pregnancy. Elderly and debilitated patients. CNS excitation may be followed by depression. Hypotension, bradycardia, arrhythmias and cardiac arrest; methaemoglobinaemia; seizures, restlessness, dizziness. Hypersensitivity. Prolonged block. Potentially Fatal: Cardiac and sudden respiratory arrest. Decreased duration with hyaluronidase. Decreased clearance with cimetidine and ranitidine. Potentiates lidocaine and mepivacaine. Allergic-type reactions with formulations containing sodium metabisulfite. Potentially Fatal: May potentiate systemic toxicity of other local amide anaesthetics.
Contraindications
Special Precautions Adverse Drug Reactions
Drug Interactions
Increased risk of myocardial depression with antiarrhythmics. Click to view more bupivacaine Drug Interactions Pregnancy Category (US FDA) Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus. Mechanism of Action Bupivacaine blocks both the initiation and conduction of nerve impulses reducing the permeability of neuronal membranes to Na ions resulting in inhibition of depolarization with resultant blockade of conduction. Onset: 4-10 min. Duration: 1.5-8.5 hr. Distribution: Crosses the placenta, diffuses into CSF, enters breast milk (small amounts). Protein-binding: 95%. Metabolism: Hepatic. Excretion: Urine (as metabolites); 1.5-5.5 hr (elimination half-life). MIMS Class ATC Classification Anaesthetics - Local & General / Anaesthetics - Local & General N01BB01 - bupivacaine ; Belongs to the class of amides. Used as local anesthetics.
LEVOBUPIVACAINE Indication & Dosage Injection Surgical anaesthesia Adult: Epidural block: 50-100 mg (10-20 ml) of a 0.5% solution or 75-150 mg (10-20 ml) of a 0.75% solution. Caesarean section: 75-150 mg (15-30 ml) of a 0.5% solution. Spinal block: 15 mg (3 ml) of a 0.5% solution. Max: 150 mg/dose; 400 mg/day. Injection Peripheral nerve block Adult: 2.5-150 mg or 1-2 mg/kg (0.4 ml/kg) of a 0.25 or 0.5% solution. Not to exceed 40 ml. Max: 150 mg/dose; 400 mg/day. Injection Infiltration anaesthesia Adult: Up to 150 mg (60 ml) of a 0.25% solution. For peribulbar block in ophth procedures: 37.5-112.5 mg (5-15 ml) of a 0.75% solution. Max: 150 mg/dose; 400 mg/day. Child: For ilioinguinal or iliohypogastric blocks in children <12 yr: 0.625-2.5 mg/kg (0.25-0.5 ml/kg) of a 0.25 or 0.5% solution. Injection Acute pain Adult: Pain relief during labour: 15-50 mg (6-20 ml) of a 0.25% solution, to be given as a bolus dose; alternatively, dose may be given via continuous infusion at 5-12.5 mg (4-10 ml) per hr using 0.125% solution or 5-12.5 mg (8-20 ml) per hr using 0.0625% solution. Postoperative pain: 10-25 mg (4-10 ml) per hr of a 0.25% solution, 12.5-18.75 mg (10-15 ml) per hr of a 0.125% solution or 12.5-18.75 mg (20-30 ml) per hr of a 0.0625% solution; dose may be given as an epidural infusion. Max: 150 mg/dose; 400 mg/day. Reconstitution: When needed, dilutions should be made with normal saline. Contraindications Not to be used in IV regional anesth (Bier's block) and paracervical block in obstetrics. Do not use 0.75% solution for epidural block in obstetrics. Hypovolaemia, complete heart block. Epilepsy, respiratory impairment, impaired cardiac conduction, bradycardia, severe shock, acute porphyria, myasthenia gravis, renal or hepatic impairment. Pregnancy, lactation. Reduce dose in elderly or debilitated patients. Resuscitative equipment should be available. Do not use solutions containing adrenaline for anesth in appendages. Do not use solutions containing preservatives for caudal or epidural block. CNS effects such as restlessness, anxiety, dizziness, confusion, respiratory depression and convulsions. Neuromuscular and skeletal weakness, blurred vision, pupillary constriction, tinnitus. Hypotension, bradycardia and CV collapse which may lead to cardiac arrest. Rarely, hypersensitivity reactions. Plasma levels may be reduced when used with enzyme-inducing drugs such as rifampicin. Substrates for or inhibitors of CYP3A4 and CYP1A2 may affect the plasma levels of levobupivacaine. Click to view more levobupivacaine Drug Interactions
Special Precautions
Drug Interactions
Pregnancy Category (US FDA) Category B: Either animal-reproduction studies have not demonstrated a foetal risk but there are no controlled studies in pregnant women or animal-reproduction studies have shown an
adverse effect (other than a decrease in fertility) that was not confirmed in controlled studies st in women in the 1 trimester (and there is no evidence of a risk in later trimesters). Storage Injection: To be used immediately after opening. After dilution in normal saline: Chemical and physical in-use stability at 20-22C for 7 days. Mechanism of Action Levobupivacaine is a long acting local anaesthetic of the amide type. It is the S-enantiomer of bupivacaine. It blocks nerve conduction in sensory and motor nerves mainly by interacting with voltage sensitive sodium channels on the cell membrane. It also interferes with impulse transmission and conduction in other tissues. Levobupivacaine is given as the hydrochloride for infiltration anaesthesia and regional nerve blocks including epidural block. It is contraindicated in obstetric paracervical block and IV regional anaesthesia (Bier's block). The 0.75% solution is also contraindicated for epidural blocks in obstetrics. Distribution: Protein binding: At least 97%. Volume of distribution after IV admin: 67 litres. Metabolism: Extensively metabolised in liver. Major metabolite: 3-Hydroxylevobupivacaine. Excretion: Mean half-life after IV admin: About 80 min. Excreted as its metabolites largely in the urine, with some in faeces. MIMS Class ATC Classification Anaesthetics - Local & General / Anaesthetics - Local & General N01BB10 - levobupivacaine ; Belongs to the class of amides. Used as local anesthetics.
MIDAZOLAM Indication & Dosage Oral Short-term management of insomnia Adult: 7.5-15 mg given at night. Oral Sedation for dental and minor surgical procedures Child: 6 mth: Single dose of 250-500 mcg/kg, up to a max of 20 mg. Younger patients (6 mth<6 yr) may require up to 1 mg/kg. Oral Premedication in surgery Child: 6 mth: Single dose of 250-500 mcg/kg, up to a max of 20 mg. Younger patients (6 mth<6 yr) may require up to 1 mg/kg. Intramuscular Premedication in surgery Adult: 70-100 mcg/kg (usual dose: 5 mg) given 20-60 minutes before surgery by deep IM inj. Child: 1 yr: 80-200 mcg/kg given 20-60 minutes before surgery by deep IM inj. Elderly: 20-50 mcg/kg given 20-60 minutes before surgery by deep IM inj. Parenteral Sedation for dental and minor surgical procedures Adult: IV admin: Initially, up to 2.5 mg given over at least 2-5 minutes, 5-10 minutes before procedure. Repeat after at least 2 minutes if necessary. Usual total: 3.5-5 mg. Max total: 7.5 mg. Child: IV admin: 6 mth-5 yr: Initial: 50-100 mcg/kg given over 2 minutes, increase slowly at 2minute intervals up to a total of 600 mcg/kg, max total dose: 6 mg. 6-12 yr: 25-50 mcg/kg given over 2 minutes and increase slowly at 2-minute intervals up to a total of 400 mcg/kg; max total dose: 10 mg. IM admin (used only in exceptional cases): 1-15 yr: 50-150 mcg/kg; max: 10 mg. Elderly: Initially 1-1.5 mg given over 2 min, increased by increments of 0.5-1 mg at 2 min intervals as needed. Intravenous Induction of anaesthesia Adult: 150-200 mcg/kg by slow inj in premedicated patients and at least 300 mcg/kg for those who have not received a premedicant. Additional doses may be required to complete induction, up to 600 mcg/kg in resistant cases. Child: >7 yr: 150 mcg/kg. Max total: 500 mcg/kg (not >25 mg). Elderly: 100-200 mcg/kg in divided doses at 2-minute intervals. Intravenous Sedation in critical care Adult: Loading dose: 30-300 mcg/kg given as infusion over 5 minutes to induce sedation. Maintenance dose: 20-200 mcg/kg/hr. For patients with hypothermia, hypovolaemia or vasoconstriction: Reduce or omit loading dose, and reduce maintenance dose. Child: Neonates with gestational age <32 wk: 30 mcg/kg/hr by continuous IV infusion. Neonates with gestational age >32 wk and who are <6 mth: 60 mcg/kg/hr. 6 mth: Initial loading dose of 50-200 mcg/kg given by slow IV inj; maintenance dose of 60-120 mcg/kg/hr given as IV infusion. In obese paediatric patients, calculate dose based on ideal wt. Elderly: Dosage may need to be reduced. Rectal Sedation for dental and minor surgical procedures
Child: >6 mth: 300-500 mcg/kg as a single dose. May dilute with water for inj up to a total volume of 10 mL if the volume is too small. Rectal Premedication in surgery Child: >6 mth: 300-500 mcg/kg as a single dose. May dilute with water for inj up to a total volume of 10 mL if the volume is too small. Special Populations: Dosage in intensive care may need to be reduced in patients with hypovolaemia, vasoconstriction or hypothermia. Reconstitution: Midazolam solution for injection may be administered rectally. The inj solution may be diluted with Water for Injections up to a total volume of 10 ml if the volume is too small. Administration Overdosage May be taken with or without food. Symptoms of overdose include sedation, confusion, impaired coordination, muscle relaxation or paradoxical excitation. More serious symptoms would be areflexia, hypotension, cardiorespiratory depression, apnoea and coma. Treatment is generally supportive and symptomatic. The benzodiazepine antagonist flumazenil is indicated in cases of severe intoxication accompanied with coma or respiratory depression. Caution should be observed in the use of flumazenil in case of mixed drug overdosage and in patients with epilepsy already treated with benzodiazepines. Acute narrow-angle glaucoma; coma or patients in shock; acute alcohol intoxication; intrathecal and epidural admin. Acute pulmonary insufficiency or marked neuromuscular respiratory weakness including unstable myasthenia gravis; severe respiratory depression.
Contraindications
Special Precautions Paediatric patients with cardiovascular instability; chronic renal failure; open-angle glaucoma; cardiac disease; respiratory disease; myasthenia gravis; neonates; history of drug or alcohol abuse; elderly and debilitated (reduce dose); avoid prolonged use or abrupt withdrawal; hepatic impairment; severe fluid or electrolyte disturbances. May impair ability to drive or operate machinery; titrate dose carefully; monitor for early signs of hypoventilation, airway obstruction, or apnea. Pregnancy, lactation Adverse Drug Reactions Physical and psychological dependence with withdrawal symptoms; decreased tidal volume and respiration rate; apnoea; headache; hiccup; nausea, increased appetite, vomiting; cough; oversedation; seizure-like activity (paediatrics); paradoxical reactions; kernicterus; nystagmus; skin rash, pruritus; reduced alertness, confusion, euphoria, hallucinations, fatigue, dizziness, ataxia, post-operative sedation, anterograde amnesia; jaundice; cardiac arrest, heart rate changes, thrombosis; anaphylaxis; laryngospasm, bronchospasm. Potentially Fatal: Respiratory depression, respiratory arrest; hypotension. Increased CNS depression with alcohol, opioids, barbiturates, other sedatives and anaesthetics. Increased respiratory depression with opiates, phenobarbital, other benzodiazepines. Plasma concentrations increased by CYP3A4 inhibitors such as cimetidine, erythromycin, clarithromycin, diltiazem, verapamil, ketoconazole anditraconazole, antiretroviral agents, quinupristin with dalfopristin. Midazolam concentration decreased byphenytoin, carbamazepine, phenobarbital, rifampicin. Halothane, thiopental requirements may be reduced during concurrent use. Click to view more midazolam Drug Interactions Bioavailability of oral midazolam increased by grapefuit juice. Avoid concomittant use.
Drug Interactions
Food Interaction
Pregnancy Category (US FDA) Category D: There is positive evidence of human foetal risk, but the benefits from use in pregnant women may be acceptable despite the risk (e.g., if the drug is needed in a lifethreatening situation or for a serious disease for which safer drugs cannot be used or are ineffective). Storage Intramuscular: Store at 20-25C. At a final concentration of 0.5 mg/ml, midazolam is stable for up to 24 hr when diluted with 0.9% sodium chloride or 5% dextrose in water. Intravenous: Store at 20-25C. At a final concentration of 0.5 mg/ml, midazolam is stable for up to 24 hr when diluted with 0.9% sodium chloride or 5% dextrose in water. Parenteral: Store at 20-25C. At a final concentration of 0.5 mg/ml, midazolam is stable for up to 24 hr when diluted with 0.9% sodium chloride or 5% dextrose in water. Rectal: Store at 20-25C. Mechanism of Action Midazolam is a short-acting benzodiazepine. It exerts sedative and hypnotic, muscle relaxant, anxiolytic and anticonvulsant actions. While the probable anxiolytic action might be as a result of the drug's ability to increase glycine inhibitory neurotransmitter level, the hypnotic/anaesthetic action may be due to the occupation of the benzodiazepine and GABA receptors leading to membrane hyperpolarisation and neuronal inhibition, and further interfering with the re-uptake of GABA at the synapses. Absorption: Rapidly absorbed (any route); peak plasma concentrations after 20-60 min (depending on route). Distribution: Crosses the placenta; enters breast milk. Protein-binding: 96% Metabolism: Extensively hepatic via CYP3A4 isoenzyme; converted to hydroxymethylmidazolam. Excretion: Urine (as glucuronide conjugates); 2 hr (elimination half-life), prolonged in neonates, elderly and hepatic impairment. MIMS Class ATC Classification Anxiolytics / Anticonvulsants / Hypnotics & Sedatives N05CD08 - midazolam ; Belongs to the class of benzodiazepine derivatives. Used as hypnotics and sedatives.
KETAMINE Indication & Dosage Intravenous Induction of anaesthesia Adult: 1-4.5 mg/kg as IV inj. Surgical anaesthesia is produced within 30 sec of the end of inj. Usual dose to produce 5-10 minutes of anaesthesia: 2 mg/kg over 60 seconds. Alternatively, 1-2 mg/kg infused at 0.5 mg/kg/minute; may use with diazepam to prevent emergence reactions. Child: 1-4.5 mg/kg as IV Inj. Surgical anaesthesia is produced within 30 sec of the end of inj and lasts for 5-10 min if 2 mg/kg is given over 60 sec. Alternatively, 0.5-2 mg/kg as IV infusion. Maintenance: Achieve with 10-45 mcg/kg/min; titrate infusion rate according to response. Intramuscular Induction of anaesthesia Adult: 6.5-13 mg/kg. Usual dose to produce 12-25 minutes of anesthesia: 10 mg/kg. Incompatibility: May form precipitates with barbiturates; do not inject in the same syringe. Contraindications Hypertension, history of cerebrovascular accident. Eye injury, raised ocular and intracranial pressure. Psychotic disorders. Minimise verbal and tactile stimulation during recovery period. Chronic alcoholic and alcoholintoxicated patients. Preanaesthetic elevated CSF pressure. Dependence and tolerance may develop. May impair ability to drive or operate machinery. Monitor cardiac function in patients with hypertension or cardiac decompensation. Pregnancy and lactation. Emergence reactions e.g. vivid dreams, hallucinations, confusion, irrational behaviour. Increased muscle tone sometimes resembling seizures. Temporary hypertension and tachycardia. Hypotension, bradycardia, arrhythmias. Respiratory depression, apnoea, laryngospasm, diplopia, nystagmus, nausea, vomiting, lachrymation, hypersalivation, raised intraocular and CSF pressure, skin rash and pain at inj site. May increase effects of nondepolarising muscle relaxants. May reduce hypnotic effect of thiopental. Prolonged recovery time with barbiturates/narcotics. Reduced cardiac output, BP and pulse rate with halothane. Increased risk of hypertension and tachycardia with thyroid hormones. Seizures and tachycardia may occur when used with theophyllines. Click to view more ketamine Drug Interactions
Special Precautions
Drug Interactions
Pregnancy Category (US FDA) Category B: Either animal-reproduction studies have not demonstrated a foetal risk but there are no controlled studies in pregnant women or animal-reproduction studies have shown an adverse effect (other than a decrease in fertility) that was not confirmed in controlled studies st in women in the 1 trimester (and there is no evidence of a risk in later trimesters). Storage Mechanism of Action Intramuscular: Store at 15-30C (59-86F). Intravenous: Store at 15-30C (59-86F). Ketamine has a direct action on the cortex and limbic system. It produces a cataleptic-like state wherein the patient is withdrawn from the surrounding environment. Distribution: Crosses the placenta. Metabolism: Hepatic biotransformation to norketamine. Other metabolic pathways include hydroxylation of the cyclohexone ring and conjugation with glucuronic acid.
Excretion: Via urine (as metabolites); 2.5 hr (beta phase half-life). MIMS Class ATC Classification Anaesthetics - Local & General / Anaesthetics - Local & General N01AX03 - ketamine ; Belongs to the class of other general anesthetics.
PROPOFOL Indication & Dosage Intravenous Induction and maintenance of general anaesthesia Adult: Induction: 40 mg by inj or infusion every 10 sec. Usual dose: 1.5-2.5 mg/kg. Maintenance: 4-12 mg/kg/hr or intermittent bolus inj of 20-50 mg. Child: >8 yr: Induction dose of 2.5 mg/kg. Maintenance dose: 9-15 mg/kg/hr by IV infusion or intermittent bolus inj. Elderly: Including neurosurgical and debilitated patients: Infuse at a rate of 20 mg every 10 sec. Maintenance: 3-6 mg/kg/hr. Usual dose needed: 1-1.5 mg/kg. Intravenous Sedation Adult: In diagnostic and surgical procedures: Initially, 6-9 mg/kg/hr by infusion given for 3-5 minutes or an alternative dose of 0.5-1 mg/kg by slow inj over 1-5 minutes. Maintenance: 1.5-4.5 mg/kg/hr infusion. Reduce maintenance dose by 20% for high-risk patients needing sedation. For ventilated patients: 0.3-4 mg/kg/hr by infusion. Monitor lipid concentrations if duration of sedation lasts >3 days. Contraindications Special Precautions Electroconvulsive therapy, obstetrics. Sedation in children 16 yr. Pregnancy, lactation. Paediatrics, elderly, hypovolaemia, epilepsy, lipid disorders, patients with increased intracranial pressure. Avoid rapid bolus doses in high risk patients. Emulsion formulation of propofol 2% should only be used in children >3 yr. Involuntary muscle movements; nausea, vomiting, headache, fever; pain, burning or stinging at inj site. Potentially Fatal: Apnoea, bradycardia, hypotension, convulsions; anaphylaxis. Reduce dose if given with nitrous oxide or halogenated anaesthetics. Increased sedative, anaesthetic and cardiorespiratory effects when used with other CNS depressants. Click to view more propofol Drug Interactions
Drug Interactions
Pregnancy Category (US FDA) Category B: Either animal-reproduction studies have not demonstrated a foetal risk but there are no controlled studies in pregnant women or animal-reproduction studies have shown an adverse effect (other than a decrease in fertility) that was not confirmed in controlled studies st in women in the 1 trimester (and there is no evidence of a risk in later trimesters). Mechanism of Action Propofol is a short-acting anaesthetic given for induction and maintenance of general anaesthesia. Onset: 30 sec. Duration: 3-10 min. Distribution: Extensively redistributed from brain to other tissues; crosses the placenta and enters breast milk. Protein-binding: 95% Metabolism: Extensively hepatic; converted to water-soluble sulfate and glucuronide conjugates. Excretion: Urine (as metabolites); faeces. Elimination half-life:40 min (initial); 4-7 hr (terminal). MIMS Class ATC Classification Anaesthetics - Local & General / Anaesthetics - Local & General N01AX10 - propofol ; Belongs to the class of other general anesthetics.
ISOFLURANE Indication & Dosage Inhalation Induction and maintenance of general anaesthesia Adult: Induction: Initially, 0.5% v/v with oxygen or oxygen and nitrous oxide, increased to 1.5-3% v/v. Surgicalanaesthesia is usually produced within 10 minutes. Maintenance: 1-2.5% v/v with oxygen and nitrous oxide mixtures or 1.5-3.5% v/v with oxygen only. For maintenance of anesth during caesarean section: 0.5-0.75% v/v with oxygen and nitrous oxide mixtures. Contraindications Special Precautions Known or suspected susceptibility to malignant hyperthermia. Porphyria. Perioperative hyperkalaemia; raised intracranial pressure. May impair ability to drive or operate machinery. Pregnancy and lactation. Do not allow carbon dioxide absorbents in anaesthetic apparatus to dry out when delivering isoflurane to minimise the risk of developing elevated carboxyhaemoglobin levels. Respiratory depression, hypotension, arrhythmias, malignant hyperthermia. Shivering, nausea, vomiting, ileus. Breath holding, coughing and laryngospasm. Rarely, postoperative hepatic dysfunction and hepatitis. Hypersensitivity reactions. Transient WBC elevation. Enhances effects of neuromuscular blockers. May sensitise the myocardium to adrenaline and other sympathomimetics. Enhances hypotensive effects of ACE inhibitors, TCAs, MAOIs, antihypertensives, antipsychotics or -blockers. May have synergistic effects with CNS depressants. Click to view more isoflurane Drug Interactions
Drug Interactions
Pregnancy Category (US FDA) Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus. Storage Mechanism of Action Inhalation: Store at 20-25C (68-77F). Isoflurane, a volatile halogenated anaesthetic, causes a reversible loss of consciousness and pain sensations, suppression of voluntary motor activity, modification of autonomic reflexes, and depression of the respiratory and the CV system. Anaesthetics - Local & General / Anaesthetics - Local & General N01AB06 - isoflurane ; Belongs to the class of halogenated hydrocarbons. Used as general anesthetics.
HALOTHANE Indication & Dosage Inhalation Induction and maintenance of general anaesthesia Adult: Induction: 2-4% v/v of halothane in O2 or mixtures of nitrous oxide and O2. Alternatively, 0.5% v/v of halothane may be used for induction and gradually increased to the required level for maintenance ofanaesthesia. Maintain anesthesia at 0.5-2% v/v depending on the flow rate used. Child: Induction: 1.5-2% v/v. Maintenance of anaesthesia: 0.5-2% v/v depending on the flow rate used. Incompatibility: Reacts with many metals when in contact with moisture. Rubber and some plastics deteriorate when in contact with halothane vapour or liquid. Overdosage Contraindications Special Precautions Bradycardia and profound hypotension. Obstetrics; malignant hyperthermia; porphyria. Phaeochromocytoma; poor cardiac/liver function, early pregnancy. Premedication with atropine is recommended to decrease vagal tone and prevent bradycardia and severe hypotension. May trigger malignant hyperthermia and increase intracranial pressure. Increased risk of hyperkalaemia in paediatrics with underlying neuromuscular disorders. May reduce hepatic, renal and splenic blood flow. Bradycardia, hypotension, cardiac arrhythmias, respiratory depression, shivering during recovery (occasional), hepatitis (multiple exposure). Potentially Fatal: Fulminant hepatic failure, malignant hyperpyrexia and pulmonary oedema. Adrenaline, other sympathomimetics, and theophylline can produce cardiac arrhythmias. Morphine andchlorpromazine may increase depressant effects of halothane on respiration. Increased risk of phenytoinintoxication when used together. Midazolam may potentiate the anaesthetic action of halothane. Potentially Fatal: Dopaminergics increase the risk of ventricular arrhythmias. Neuromuscular blocking drugs are potentiated by halothane. Click to view more halothane Drug Interactions Pregnancy Category (US FDA) Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus. Storage Mechanism of Action Inhalation: Store at 15-25C. Halothane causes reversible CNS depression; sympathetic system is more depressed than the parasympathetic. Respiration is progressively depressed. BP, heart rate, cardiac output and coronary blood flow are reduced. Absorption: Well absorbed (inhalation). Distribution: Soluble in the neutral fats of adipose tissue. Crosses the placenta and enters breast milk. Metabolism: Hepatic; converted to trifluoroacetic acid, bromide and chloride salts (oxidative pathway) and fluoride salts (reductive pathway).
Drug Interactions
Excretion: Lungs (as unchanged drug). MIMS Class ATC Classification Anaesthetics - Local & General / Anaesthetics - Local & General N01AB01 - halothane ; Belongs to the class of halogenated hydrocarbons. Used as general anesthetics.
SEVOFLURANE Indication & Dosage Inhalation Induction and maintenance of general anaesthesia Adult: Given via a calibrated vaporiser: Induction: Up to 5% v/v with oxygen or a mixture of oxygen and nitrous oxide. Maintenance: 0.5-3% v/v with or without nitrous oxide. Child: Given via a calibrated vaporiser: Induction: Up to 7% v/v. Maintenance: 0.5-3% v/v with or without nitrous oxide. Overdosage Discontinue admin, maintain a patent airway and adequate CV function. Initiate assisted/controlled ventilation with oxygen. Known or suspected susceptibility to malignant hyperthermia. Previous hypersensitivity. Raised intracranial pressure; cardiac, respiratory, renal, or hepatic impairment, elderly or obese patients. Maintenance of haemodynamic stability is important in patients with coronary artery disease. Concomitant use with adrenaline or other sympathomimetics. Pregnancy and lactation. May increase serum potassium levels. Cardiorespiratory depression, hypotension, malignant hyperthermia, agitation, laryngospasm, increased cough, salivation, acute renal failure, shivering, nausea, vomiting; rarely, dystonic movements in children, postoperative hepatitis, and seizure-like activity. May enhance effect and duration of competitive neuromuscular blockers. Metabolism and toxicity increased by cytochrome P450 isoenzyme CYP2E1 inducers including isoniazid and alcohol. Increased risk of cardiac arrhythmias when used with epinephrine or norepinephrine. Click to view more sevoflurane Drug Interactions Transient elevations in plasma glucose, WBC count and LFTs.
Drug Interactions
Category B: Either animal-reproduction studies have not demonstrated a foetal risk but there are no controlled studies in pregnant women or animal-reproduction studies have shown an adverse effect (other than a decrease in fertility) that was not confirmed in controlled studies st in women in the 1 trimester (and there is no evidence of a risk in later trimesters). Storage Mechanism of Action Inhalation: Store at 15-30C. Sevoflurane is a volatile halogenated general anaesthetic which causes a reversible loss of consciousness and pain sensation, suppression of voluntary motor activity, modification of autonomic reflexes, depression of the respiratory and CV systems. It also has muscle relaxant properties. Onset: Within 2 minutes. Duration: 4-14 minutes. Absorption: Absorbed on inhalation. Blood/gas partition coefficient is low. Distribution: Crosses placenta. Metabolism: Up to 5% of the absorbed dose is metabolised by the hepatic CYP2E1 isoenzyme. Excretion: Eliminated in the urine as metabolites. MIMS Class ATC Classification Anaesthetics - Local & General / Anaesthetics - Local & General N01AB08 - sevoflurane ; Belongs to the class of halogenated hydrocarbons. Used as general anesthetics.
ATRACURIUM Indication & Dosage Intravenous Muscle relaxant in general anaesthesia, Endotracheal intubation, Aid controlled ventilation Adult: Initially, 300-600 mcg/kg as inj. Subsequently, 100-200 mcg/kg when necessary or every 15-25 minutes for maintenance in prolonged procedures. Alternatively, maintenance can also be achieved by continuous infusion at 5-10 mcg/kg/minute. Initial dose should be given over 60 seconds in patients with CV disease. Dose should be calculated based on ideal body-weight in obese patients. Child: 2 mth: Initially, 400-500 mcg/kg as inj. Maintenance dose: 80-100 mcg/kg; first maintenance dose may be given 20-45 min after the initial dose, subsequently, may be repeated every 15-25 min. For children 1 mth-2 yr: 300-400 mcg/kg may be used as initial dose in those who are under halothane anaesthesia. Maintenance doses may be admin more frequently in infant and children than adults. Special Populations: For patients with significant CV disease or any history (e.g. severe anaphylactoid reactions or asthma) suggesting a greater risk of histamine release, an initial dose of 0.3-0.4 mg/kg should be given slowly or in divided doses over 1 min. For adults receiving atracurium following the use of succinylcholine for intubation under balanced anesthesia, an initial dose of 0.3-0.4 mg/kg is recommended. Dosage reductions may be necessary in patients with neuromuscular disease, severe electrolyte disorders or carcinomatosis in which potentiation of neuromuscular block or difficulties with reversal have been demonstrated. Reconstitution: May be diluted in normal saline, dextrose 5% in water or dextrose 5% in normal saline. Incompatibility: Incompatible with alkaline solutions and lactated Ringer's solution. Y-site incompatibility: Diazepam, thiopental, propofol. Admixture incompatibility: Ranitidine, sodium nitroprusside, heparin, cefazolin, aminophylline, quinidine gluconate. Overdosage Contraindications Special Precautions May lead to prolonged apnoea with CV collapse and the effects of histamine release. Hypersensitivity. Neonates; severe CVS disorders; renal or hepatic dysfunction; myasthenia gravis and other neuromuscular disorders; severe electrolyte imbalances; respiratory insufficiency or pulmonary disease, asthma; burns; cardiopulmonary bypass; smoking; pregnancy and lactation. Dosage for obese patients should be based on ideal body-weight to prevent overdosing. Cutaneous reactions; bradycardia, transient hypotension in patients with CVS disorders; dyspnoea, bronchospasm; rash and urticaria. Mixed block with suxamethonium which is difficult to reverse with anticholinergic drugs. Ketamine may potentiate the effects of atracurium. Concurrent use with tamoxifen or danazol may prolong effects of atracurium. Potentially Fatal: Neuromuscular blockade potentiated by parenteral Mg salts, anaesthetics, aminoglycosides and polypeptide antibiotics, botulinum A toxin. Malignant hyperthermia with halogenated anaesthetics and succinylcholine. MAOIs. Click to view more atracurium besilate Drug Interactions
Pregnancy Category (US FDA) Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus. Storage Intravenous: Intact vials: Refrigerate at 2-8C. Do not freeze. Dilutions of 0.2 mg/ml or 0.5 mg/ml are stable for up to 24 hr at room temperature or under refrigeration. Mechanism of Action Atracurium besilate blocks neural transmission at the neuromuscular junction by competitive binding at the cholinergic receptor sites on the motor end plate. Distribution: Protein binding: 80%. Excretion: Excretion in urine and bile, mostly as metabolites. Elimination half-life: about 20 min. MIMS Class Muscle Relaxants
ROCURONIUM Indication & Dosage Intravenous Muscle relaxant in general anaesthesia, Endotracheal intubation, Aid controlled ventilation Adult: Initially, 600 mcg/kg by inj. Higher doses of 1 mg/kg may be used for intubation during rapid sequence induction of anaesthesia. Maintenance: 150 mcg/kg by inj (may reduce to 75100 mcg/kg if inhalationalanaesthesia is used) or by infusion at a rate of 300-600 mcg/kg/hr. Doses should be based on lean body weight for obese patients weighing >30% above the ideal body weight. Child: Infants and children >1 mth: Initially, 600 mcg/kg by inj. Maintenance: 150 mcg/kg by inj or by infusion at a rate of 300-600 mcg/kg/hr, maintenance doses may be required more frequently than in adult patients. Elderly: Reduced maintenance doses: 75-100 mcg/kg. Renal impairment: Initially, 600 mcg/kg by inj. Maintenance: 75-100 mcg/kg. Hepatic impairment: or biliary tract disease: Initially, 600 mcg/kg by inj. Maintenance: 75100 mcg/kg. Overdosage May lead to prolonged apnoea due to paralysis of the diaphragm and the intercostal muscles. Hypersensitivity. Pulmonary disease, hepatic, renal impairment, biliary disease, electrolyte/acid-base abnormalities, neuromuscular diseases, DM, dehydrated or severely-ill patients, patients with >40% burns. Ventilation must be supported during neuromuscular blockade. Pregnancy and lactation. Doses >900 mcg/kg may have vagolytic activity. Itching and erythematous reactions at the inj site and/or generalised histaminoid reactions. CV changes. Tachycardia and increase in BP. Potentially Fatal: Abnormal ECG, arrhythmia, bronchospasm, anaphylaxis and malignant hyperthermia. Drug Interactions May cause enhanced block when used with lidocaine, procainamide, quinidine, verapamil, aminoglycosides, inhalational anaesthetics and vancomycin. May cause prolonged paralysis when used with clindamycin. Anticholinesterases such as pyridostigmine and galantamine may antagonise the effect of rocuronium. Chronic use of carbamazepine or phenytoin may lead to resistance to rocuronium. Click to view more rocuronium bromide Drug Interactions
Pregnancy Category (US FDA) Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus. Storage Mechanism of Action Intravenous: Store at 2-8C. Rocuronium is a competitive neuromuscular blocker that acts by blocking the binding of acetylcholine to receptors on the motor endplate, inhibiting depolarisation. Onset: 1-2 min. Max: 4 min. Duration: 30 min.
Distribution: 30% bound to plasma proteins. Excretion: Elimination half-life: about 1.2-1.4 hr. Up to 40% of a dose is excreted in the urine within 24 hr. Also excreted in the bile. MIMS Class ATC Classification Muscle Relaxants M03AC09 - rocuronium bromide ; Belongs to the class of other quaternary ammoniumcontaining agents used as peripherally-acting muscle relaxants.
VECURONIUM Indication & Dosage Intravenous Muscle relaxant in general anaesthesia, Facilitate endotracheal intubation Adult: Initially, 80-100 mcg/kg given as inj (reduced doses at 30-50 mcg/kg have been suggested after use of suxamethonium; not to exceed 100 mcg/kg in caesarean and neonatal surgery). Maintenance in prolonged procedure: 20-30 mcg/kg, adjust according to response. Alternatively, as continuous infusion: 0.8-1.4 mcg/kg/minute after initial IV dose of 40-100 mcg/kg. Child: < 5 mth: Initially, 10-20 mcg/kg, increased if necessary according to response. > 5 mth: initially, 80-100 mcg/kg given as inj; alternatively, 30-50 mcg/kg after clinical recovery from neuromuscular blockade of suxamethonium. Max in caesarean and neonatal surgery: 100 mcg/kg. Maintenance in prolonged procedure: 10-15 mcg/kg. Elderly: Dose reduction may be needed. Renal impairment: Dose adjustments may be needed. Hepatic impairment: Dose adjustments may be needed. Incompatibility: Incompatible with furosemide, alkaline solution e.g. thiopental sodium. Overdosage Symptoms: Mainly extensions of the usual pharmacologic effects of the drug. Skeletal muscle weakness, decreased respiratory reserve, low tidal volume, or apnea. A peripheral nerve stimulator may be used to monitor recovery from blockade and to differentiate between prolonged neuromuscular blockade from other causes of diminished respiratory reserve. Management: Treatment is supportive and symptomatic. Maintain an adequate, patent airway using assisted or controlled respiration. Neuromuscular blockade may be reversed by admin of a cholinesterase inhibitor such as neostigmine, pyridostigmine or edrophonium. Hypersensitivity to vecuronium or bromide. Pregnancy, lactation, elderly. Renal and hepatic impairment. Increase in onset time in conditions associated with prolonged circulation time (e.g. CV disease, oedema). Neuromuscular disease e.g. myasthenia gravis, Eaton-Lambert syndrome or after poliomyelitis. Hypothermia, burns patients. Decrease dose in obese patients, taking into account lean body-mass. Correct severe electrolyte disturbances, altered blood pH, dehydration where possible before vecuronium admin. Do not use potentially dangerous machinery or drive a car within 24 hr after full recovery from the neuromuscular blocking action of vecuronium. Do not admin vecuronium unless facilities for intubation, artificial respiration, oxygen therapy and agents for neuromuscular reversal are immediately available. Muscle weakness, paralysis, muscle atrophy (after long term use), hypersensitivity reactions e.g urticaria and erythema. Potentially Fatal: Anaphylaxis, respiratory failure, apnoea. Increases neuromuscular blockade with volatile anaesthetic agents (halothane, ether, enflurane, isoflurane,methoxyflurane, propofol and cyclopropane), fentanyl, other non-depolarising muscle relaxants, prior admin of succinylcholine, tetracyclines, polymyxins, diuretics, thiamine, MAOIs, bacitracin, colistin, sodium colistimethate, acylaminopenicillins, aminoglycoside antibiotics, high dose metronidazole, protamine, -adrenergic blocking agents, calcium antagonists e.g. verapamil, and Mg. Decreased neuromuscular blockade with anticholinesterases, prior chronic admin of
Drug Interactions
corticosteroids, phenytoin, carbamazepine, noradrenaline, azathioprine, theophylline, calcium chloride. Click to view more vecuronium bromide Drug Interactions Pregnancy Category (US FDA) Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus. Mechanism of Action Vecuronium bromide inhibits depolarisation by blocking acetylcholine from binding to receptors on motor endplate. Onset: 1.5-2 min. Duration: 20-30 min. Metabolism: Hepatic; yielding metabolites also possessing neuromuscular blocking activity. Excretion: Via bile (as unchanged drug and metabolites), via urine (trace amounts); 30-80 min (elimination half-life). MIMS Class Muscle Relaxants

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NOREPINEPHRINE Indication & Dosage Intravenous Acute hypotensive states Adult: Initially, 8-12 mcg/minute, up to 8-30 mcg/minute in refractory

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