Pain - Opioids Combined PDF
Pain - Opioids Combined PDF
Pain - Opioids Combined PDF
An unpleasant sensory & emotional experience associated with actual or potential tissue damaged, or described in terms of such damage
CV Thrombosis
15 – 30 mg q 6 hrs Reduce Dose to 15mg to those with renal impairment, > 65 yo, or low
GI Bleeding
Ketorolac Max: 5 days body weight < 50 kg
Renal Impairment
Toradol
NSAIDs
Platelet
15mg just as effective Can be given IV
Dysfunction
Dicyclomine 20 mg PO/IM
X: Elderly Alleviates smooth muscle spasms in GI tract – great for abdominal pain
Anti-Spasmodic / Anticholinergic Not IV: thrombosis
Neuropathic Pain
- Burning, tingling, electric-shock like sensations
Lyrica
Carbamazepine
Amitriptyline analgesia
Sleeplessness
SNRI
60 mg QD Headache / Dizziness
Duloxetine 120 mg no more effective Dry Mouth
Constipation
Ketamine /
Lidocaine
Tizanidine Sedating Helpful in many OUD symptoms
Skeletal Muscle
Sedating
Cyclobenzaprine Serotonin Syndrome Risk
Short-Term Only
Dependence Risk
Carisoprodol Withdrawal
Benzodiazepines High overdose risk with opioids
IR: 5-15 mg Q4H Itching can add hydroxyzine ½ life: 150 minutes
Morphine ER: 15-30 mg Q12H or or diphenhydramine
Base > 60 mg / day Low Lipid Sol. = slow to enter BBB
ER: MS Contin 24H
X: Severe Renal Impairment Renal Adjustment Needed
IV: 1-2 mg Q4H
Hydrocodone IR: 5 – 10 mg Q 4 H
= > 60 mg / day Itching
Norco / Vicodin ER: 10-20 mg Q12 or 24 H
Semi-Synthetic
1.5 x
Oxycodone IR: 5-15 mg Q4H Metabolized through CYP34A
More > 30 mg / day
Potent Percocet / OxyContin ER: 10-20 mg Q12H Renal Adjustment Needed
Anxiety / Dysphoria
Hydroxyzine - 25 – 50 mg TID PRN Diphenhydramine 25mg Q6H PRN Can be sedating
Lacrimation / Rhinorrhea
Topical Medications
Myalgias NSAIDS or Acetaminophen 650 mg Q6H PRN Less systemic effects
Menthol / Lidocaine
Sleep Disturbances Trazodone - 25 – 300 mg HS
Prochlorperazine 5-10mg Q4H PRN
Nausea Ondansetron 4mg Q6H PRN
Promethazine 25 mg Q6H PRN
ALTO Pathways
Immediate / 1st Line Alternatives Discharge Medications
APAP 1000mg PO + Cyclobenzaprine 5mg OR Diazepam 5mg APAP 1000 mg Q6H PRN + NSAID
Opioid-Naïve Ibu 600 mg or Ketorolac 15mg IV/IM Ketamine 0.1-0.3 mg/kg IVPB Cyclobenzaprine 5-10 mg Q8HPRN
Musculoskeletal Pain Lidocaine 1% Trigger Point Injection Lidoderm 5% Patch
Lidoderm Patch 4 or 5% (max 3 patches) Gabapentin 300-600mg Gabapentin 300mg HS
BR is on morphine solution 15mg PO Q6H. You recommend switching him to MS Contin (ER) tablets because
Changing
BR is on morphine solution 15mg PO Q6H. You recommend switching him to Oxycontin (ER) because his TDD: 15 x 4 (Q6H) = 60 mg MME
Changing
Opioid
BR begins Oxycontin 15mg Q12H with good relief… except when he goes out for a long walk with his dog
Only)
sparky. He notices towards the end of his walk he has more pain in his leg than normal.
Pain
60 mg MME
Fentanyl Patch comes in 12, 25, 50, 75, 100 mcg/hr
Patch
60/2 = 30
Frequency: Q72H Give 25 mcg Patch
or
Acidic pKa 10 Leucine (Leu) Neutral
O Glycine O
H H
N-Terminus N N O C-Terminus
H 3N N N
H H
O Glycine O O
Dorsal Horn
Phenylalanine (Phe) of
Neutral Spinal Cord
Add 14-OH
3-OH and 6-OH à Esters
á Binding Potency
á potency
Enters CNS Faster and
in á concentration Remove 7-8 Double Bond
á Potency
6-OH
3-OH 2 Alcohol – Neutral
Phenol – Ionized – Acidic
Quaternary Carbon
linked to phenyl ring
Binding
H
N
CH3 CH3
N N N-Demethylation
Oxidative-O-Dealkylation
O-Demethylation CYP CH3 O
CYP2D6 N HO Normorphine OH
Conjugation Less Active
Glucuronidation
O O
H3CO OH HO OH
Codeine Morphine O
Less Active Active Metabolite ConjO OGluc
More Polar - hard to get into CNS
Phenol = Shorter Duration More H20 Soluble - easily excreeted
Easily inactivated
Morphine Analogs
Binding Affinity
Morphinan - μ receptor agonist Morphinan Derivatives
(-)-3-hydroxy-N-methylmorphinian (+)-3-hydroxy-N-methylmorphinian
Antagonist
3-OH à
Analgesic Methyl mixed acting
6x more μ antagonist / k agonist
â analgesic
potent than á antitussive
Mild – Moderate Pain
morphine
á Potency
Antagonist
Mild – Moderate Pain
4-Phenylpiperidine - μ receptor agonist Meperidine μ agonism in the gut -- Treats Diarrhea - â GI motility
CH3
N
O CH3
Open Chain Derivatives - μ receptor agonist Methadone – Dolophine Tramadol - Ultram Nucynta – Tapentadol
Antagonist
Opioid Analgesics
Opiate: naturally derived from poppy opium – Codeine, Morphine, Heroin
Opioid: any drug with effect at opioid receptor
MOR / KOR
MOR Antagonist Moderate Pain Weakness / Floaty Feeling /
Stadol
Mixed Psychomimetic
Pentazocine X: CHF
Mild – Moderate Pain IV Injection
Weak
Codeine
Opiates
Natural
Dilaudid
Fentanyl Severe Pain Rapid Onset / Shorter
Sublimaze Postoperative Labor Analgesia Duration Nausea / Confusion
Sufentanil – Sufenta Sedation / Constipation
Severe Pain Respiratory Depression
Alfentanil – Alfenta Fentanyl Analogs
s–anesthetic adjuvant
Remifentanil – Ultiva
Meiosis / Seizures / Sedation
Meperidine Analgesia
t½: 15-20 hours Respiratory Depression
Demerol Post-Anesthesia Shivering Muscle Twitches / CNS Excitation
Methadone Anticholinergic Effects
Long QT Syndrome
Dolophine Long Acting - t ½: 27 hours
Analgesia
CYP3A4 Metabolism Sedation / Nausea / Vomiting
Partial
Methylnaltrexone
Reliston Diarrhea / Gas / Nausea / Headache
Stomach Pain / Chills
MOR / DOR / KOR Antagonist
Poor nutrition
Could happen with first or second dose when taking APAP for the first time
Warfarin
Drug Interaction
APAP is safest choice for pain/fever only if used appropriately and monitored
Dose: <2g / day for shortest possible duration and monitor if using > 3 consecutive days
X May enhance anticoagulant effect when taken at doses >1.3 or 2 g / day for consec. days
X May increase INR / bleeding risk
P Monitor and Educate
Ibuprofen / Naproxen
Non-Steroidal Anti-Inflammatory Drugs – NSAIDS
Effective analgesic & antipyretic & anti-inflammatory
Inhibits prostaglandin synthesis by peripheral & reversible inhibition of COX1 / COX2
MOA
Kidney: NA/Water retention, hypertension, hemodynamic acute kidney injury – COX 1 & 2
Cardiovascular: stroke, myocardial infarction – COX 1 & 2 / Aspirin
COX 2 > COX 1 inhibition
Large doses or longer duration of treatment with NSAIDs Concurrent use increases risk:
GI Risks / IXNs
Pain: unpleasant sensory and emotional experience associated with actual or potential tissue damage
Chronic Pain: pain lasting at least 3 months
Approx. 80% use (often inappropriately) an OTC pain relieve at least 1x/week
Common Medications
Assessing and Evaluating for Self-Care
Poor nutrition
Could happen with first or second dose when taking APAP for the first time
Warfarin
Drug Interaction
APAP is safest choice for pain/fever only if used appropriately and monitored
Dose: <2g / day for shortest possible duration and monitor if using > 3 consecutive days
X May enhance anticoagulant effect when taken at doses >1.3 or 2 g / day for consec. days
X May increase INR / bleeding risk
P Monitor and Educate
Ibuprofen / Naproxen
Non-Steroidal Anti-Inflammatory Drugs – NSAIDS
Effective analgesic & antipyretic & anti-inflammatory
Inhibits prostaglandin synthesis by peripheral & reversible inhibition of COX1 / COX2
MOA
Kidney: NA/Water retention, hypertension, hemodynamic acute kidney injury – COX 1 & 2
Cardiovascular: stroke, myocardial infarction – COX 1 & 2 / Aspirin
COX 2 > COX 1 inhibition
Large doses or longer duration of treatment with NSAIDs Concurrent use increases risk:
GI Risks / IXNs
MJ asks if there are any serious complications with NSAID use. What would you tell her?
MJ asks how she can minimize her risks for these serious ADRs. What would you tell her?
Screen her for risks / concurrent meds – ASA > Naproxen > Ibuprofen
Case 2: Mr. AB is 70-year-old male picking up diabetes medications and a diuretic that helps him with his leg
swelling. He also wants to pay for OTC ibuprofen
Yes
What are some other risk factors that may increase NSAID associated renal toxicity?
See above -- avoid use with history of impaired renal function, congestive heart failure, disease that
compromises renal hemodynamics
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ADD IN LECTURE TIME STAMP 1:01 SLIDES 39 – 41
650 mg Q 4 H or 1000 mg Q 6 H
Not recommended < 12 years old
MAX: 4000 mg / day
Reye’s Syndrome
- Acute, potentially fatal illness exclusive to children < 19 years old
- Leads to progressive neurologic damage, hepatic injury, hypoglycemia
- Onset follows a viral infection with influenza or chickenpox
- Vomiting, lethargy, rigidity, fixed pupils, seizures, respiratory arrest
- Salicylates increase risk x 35 fold
- Avoid in children < 19 years old who have or are recovering from flu/chickenpox
Toxicity:
- Associated with risk of 90-100mg/kg/dose x 2 days
- Risk factors:
o Renal/hepatic impairment
o Metabolic disorders
o Unstable disease
o Multiple cormorbidities
- Symptoms: dizziness, tinnitus, ….
Avoid in patients with history of gout or hyperuricemia
Intolernace within 3 hours, High cross reaction with other NSAIDS, APAP preferred alternative
Case: AB is 70-year-old male who reports taking “baby” Aspirin daily
325 mg
Topical analgesics
Cannabis1
Derived from hemp and marijuana plants
Mostly used for Chronic Neuropathic Pain
ADR’s
- CBD: decreased appetite, weight loss, diarrhea, dizziness, drowsiness, and fatigue
- THC: psychoactive effects such as feeling drunk, disturbance in attention, dizziness, sedation,
disorientation, dissociation, paranoia, and euphoric mood
Withdrawal Symptoms: anxiety, headache, hypersomnia, restlessness, depression, irritability, insomnia / odd
dreams, tremors, decreased appetite
Drug Interactions; THC and CBD are primarily metabolized by CYP P450 enzymes
- Severity based on route of administration (sublingual > topical)
1
file:///Users/jennadant/Desktop/Thera/CBD vs THC (1).pdf
Acute Musculoskeletal Pain – Lower Back Pain / Sprain
APAP or NSAIDs recommended in doses/intervals
Topical counterirritants can be used as an adjunct to systemic analgesics
Self-Care Exclusions
Common Causes
Lumbar sprain or strain
Sciatica (warrants medical reference)
Heat Therapy
Non-Inflammatory Pain or Lower Back Pain
Never in acute phase (<48 hours)
Non-Pharmacologic Measures
ICE/HEAT Therapy: may provide temporary relief and some benefit from alternating
Pharmacologic Measures
APAP
- Start with non-pharmacologic measures / use in conjunction
- Titrate up to appropriate max dose prior to initiating NSAIDs
- Use in conjunction with topical analgesic
NSAID’s
- If no relief from APAP and no counterindications
Glucosamine + Chondroitin
- Herbal supplement that works slowly (up to 2 months before improvement)
- Building blocks of articular cartilage
- Use in combination with methylsulfonylmethane (MSM)
- Dosing: Glucosamine 1500mg/day and Chondroitin 1200mg/day
- ADRs: nausea, stomach upset, constipation, diarrhea
- Drug Interaction: Warfarin
Headaches (HA)
Primary Secondary
Self-Care Exclusions
MOA: smooth muscle relaxant activity on vascular walls in cerebral blood vessels
Dosing:
- Adult: 50-75 mg po bid up to 4 months
- Child: 25-50 mg bid up to 4 months
ADRs: GI distress, burping, itching, rash, hot flushes, headaches, skin discoloration