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    Hipertensi

    Uploaded by

    Irna Purwanti Rahayu
    1. This document discusses various classes of antihypertensive drugs, including their mechanisms of action, hemodynamic effects, indications, and side effects. 2. The main classes covered are diuretics, sympatholytic drugs like alpha and beta blockers, vasodilators, ACE inhibitors, angiotensin receptor blockers, and calcium channel blockers. 3. Combination drug therapy is often recommended to control blood pressure, with choices based on the severity of hypertension and any compelling patient indications. The goal is to safely lower blood pressure to below 140/90 mmHg or 130/80 mmHg for those with diabetes or chronic kidney disease.

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    Hipertensi

    Uploaded by

    Irna Purwanti Rahayu
    107 views37 pages
    1. This document discusses various classes of antihypertensive drugs, including their mechanisms of action, hemodynamic effects, indications, and side effects. 2. The main classes covered are diuretics, sympatholytic drugs like alpha and beta blockers, vasodilators, ACE inhibitors, angiotensin receptor blockers, and calcium channel blockers. 3. Combination drug therapy is often recommended to control blood pressure, with choices based on the severity of hypertension and any compelling patient indications. The goal is to safely lower blood pressure to below 140/90 mmHg or 130/80 mmHg for those with diabetes or chronic kidney disease.

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    1. This document discusses various classes of antihypertensive drugs, including their mechanisms of action, hemodynamic effects, indications, and side effects. 2. The main classes covered are diuretics, sympatholytic drugs like alpha and beta blockers, vasodilators, ACE inhibitors, angiotensin receptor blockers, and calcium channel blockers. 3. Combination drug therapy is often recommended to control blood pressure, with choices based on the severity of hypertension and any compelling patient indications. The goal is to safely lower blood pressure to below 140/90 mmHg or 130/80 mmHg for those with diabetes or chronic kidney disease.

    Copyright:

    Attribution Non-Commercial (BY-NC)
    Download as PPT, PDF, TXT or read online from Scribd
    Download as ppt, pdf, or txt
    107 views37 pages

    Hipertensi

    Uploaded by

    Irna Purwanti Rahayu
    1. This document discusses various classes of antihypertensive drugs, including their mechanisms of action, hemodynamic effects, indications, and side effects. 2. The main classes covered are diuretics, sympatholytic drugs like alpha and beta blockers, vasodilators, ACE inhibitors, angiotensin receptor blockers, and calcium channel blockers. 3. Combination drug therapy is often recommended to control blood pressure, with choices based on the severity of hypertension and any compelling patient indications. The goal is to safely lower blood pressure to below 140/90 mmHg or 130/80 mmHg for those with diabetes or chronic kidney disease.

    Copyright:

    Attribution Non-Commercial (BY-NC)
    Download as PPT, PDF, TXT or read online from Scribd
    Download as ppt, pdf, or txt
    of 37

    ANTIHYPERTENSIVE DRUGS

    Principles of blood pressure regulation:


    1. BP is regulated by: a. CO b. PVR c. Vol. of intravasc fluid (controlled at the kidney)

    2. Baroreflexes adjust moment-tomoment blood pressure: Carotid baroreceptors 3. Reduction in renal perfusion pressure

    Hemodynamic effect:
    1.

    CO: syst. BP a. SV Sirc. Vol : diuretics inotropic (-) : -blockers b. HR : -blockers PVR : Dyast. BP syst. BP vasodilator Combination : Main effect!

    2.

    3.

    ANTIHYPERTENSIVE DRUGS
    DIURETICS 2. SYMPATHOLYTIC DRUGS 3. VASODILATORS 4. ACE INHIBITORS AND ANGIOTENSIN II RECEPTOR ANTAGONISTS 5. CALSIUM CHANNEL BLOCKERS
    1.

    1. DIURETICS

    Mech. of ACTION & hemodynamic EFFECT : - Depleting Na+ BV & CO, PR may . (adaptation) - 6-8 weeks : CO normal ; PR BP

    Figure 3.Actions of thiazide Diuretics


    Thiazide Na+, water retention Blood Vol

    PR

    CO

    BP

    INDICATION :

    THIAZIDE DIURETICS : Mild or moderate essential HT (normal renal & cardiac function)

    TOXICITY/ADVERSE REACTION :

    Hypokalemia, precaution :

    a. Persons taking digitalis b. Chronic arrhythmias c. AMI

    Hypomagnesia

    TOXICITY/ADVERSE REACTION :
    Metabolic

    dose): a.Glucose intolerance b.Serum lipid c.Uric acid , precipitate gout

    effect (especially at

    2. SYMPATHOLYTIC DRUGS
    2A. BLOCKERS DRUGS:Prazosin, terazosin, doxazosin Action: A. & V Relax PR and arterial BP CO, RBF, GFR min. (tachycardia and increased renin release do not occur)

    SIDE EFFECT & TOXICITY

    1 blockers: postural hypotension syncope after the 1st dose (1st pass effect) the 1st dose should be small and should be administered at bedtime

    INDICATION BLOCKERS :

    Mild to moderate HT. In combination with propranolol or a diuretic for additive effect.

    2B. Blockers

    Activation of 1 on heart

    CO
    PR

    -Adrenoceptor blockers Renin

    BP

    Angiotensin II

    Aldosteron Sodium, water retention


    Blood volume

    DRUGS: Non selective: propranolol, nadolol, carteolol 1 blockers (cardioselective): atenolol, metoprolol (relative), betaxolol, bisoprolol Partial agonist (-blockers with ISA): acebutolol (cardioselective), pindolol, penbutolol, bopindolol. -blockers with -blocking effect: labetalol & carvedilol

    PHARMACOKINETICS & DOSAGE: Propanolol: Oral doses >> IV doses (1st-pass hepatic metabolism) T 3-6 hrs.

    INDICATION Propanolol:
    -

    HT with tachyarrhythmia, previous MI, A. pectoris, glaucoma, migraine headache.

    - It more effective : young patient > elderly

    3. VASODILATORS

    A. Hidralazine & minoxidil (p.o): long term outpatient Th/ B. Nitroprusside & diazoxide Hypertensive Emergencies. C. Calcium channel blockers

    3A1. Hydralazine Dilates arteries and arteriole (not veins)

    PR and reflex HR & CO.

    Pharmacokinetics : Bioavailability (25%) Metabolism : rapid & slow acetylators

    Hydralazine Toxicity: headache, anorexia, palpitations, Sweating and flushing Usage: Th/ moderately severe HT It is almost always as combination with a -blockers and diuretics (see figure 5)

    3B. HYPERTENSI EMERGENCY

    Diastolic BP > 150 mmHg or >130 mmHg with complications : - Encephalopathy


    - Cerebral hemorrhage - Left ventricular failure - Aortic stenosis

    Goal Th/ : rapidly reduce blood pressure

    3B2. Diazoxide

    Direct-acting arteriolar vasodilator. Vascular effect hydralazine. For coronary insuff. patients : diazoxide IV

    USAGE: Th/ HT emergency, esp.: - Malignant HT - HT encephalopathy - Eclampsia TOXICITY: Excessive hypotension

    3C. Calcium Channel Blockers

    ACTION : - Inhibit Ca++ influx into vasc. smooth muscle cells vasodilatation PR BP - Intrinsic natriuretic effect - Useful in HT with asthma, diabetes, angina and peripheral vascular disease

    DRUGS :

    A. Dihydropyridine family:
    - Nifedipine - Isradipine - Nicardipine - Nisoldipine - Amlodipine - Felodipine - Nimodipine (cerebral vasodilator)

    Pharmacological effect of Dihydropyridine family :


    - Vasculoselective - Cardiac depr. <<< verapamil/diltiazem - Reflex sympathetic activation: slight tachycardia and slight increases CO

    B. Verapamil

    It has the greatest effect on the heart: Slows cardiac cond. HR , balanced by reflex activation Contraindicated in patient with preexisting depressed cardiac function or AV conduction abnormalities !!!

    Weak vasodilator

    C. Diltiazem

    It reduces HR (lesser than verapamil), BP .

    SIDE EFFECT AND TOXICITY :


    Excessive inhibition of Ca++ influx serious cardiac depression SIDE EFFECT : - Flushing - Headache - Hypotention - Peripheral edema - Constipation - Fatigue

    4. INHIBITORS OF ANGIOTENSIN
    A. ACE-INHIBITOR
    Captopril Enalapril Lisinopril Benazepril Fesinopril Moexipril Quinopril Ramipril (long acting)

    B. ANGIOTENSIN RECEPTORBLOCKING AGENTS B1. Angiotensin Type 1 (AT1) Receptor Blocking Agents - Losartan - Valsartan B2. Analog and competitive Inhibitor of Angiotensin II : Saralasin

    4A. ACE INHIBITOR

    Pharmacological effect:
    Captopril:
    - VR BP - Aldosteron secretion Na+ & water retention K+ retention - Bradikinin vasodilation - Vasodilator preload CO

    Toxicity/side effect:

    ARF (particularly in renal stenosis) Hyperkalemia Dry cough Angioedema Altered sense of taste Allergic skin rashes, Drug fever

    Contraindication: 2nd and 3rd trimesters of pregnancy

    USAGE:

    - Mild-moderate hypertension
    - Hypertension who were refractory to standard multidrug antihypertensive regimens - Hypertension with chronic congestive heart failure

    Recommended combinations

    Diuretic + -blocker/centrally acting drug

    Diuretic + Vasodilator (ca-channel blocker, ACE inhibitor, analog and competitive AT II) Diuretic + adrenergic antagonist + Vasodilator
    -blocker + Vasodilator ACE inhibitor + ca-channel blocker

    Combinations should be avoided

    2 same class drugs -blocker + centrally acting drug

    -blocker + diltiazem/verapamil (AV nodes depression )

    Algorithm for Treatment of Hypertension


    Lifestyle Modifications Not at Goal Blood Pressure (<140/90 mmHg) (<130/80 mmHg for those with diabetes or chronic kidney disease)

    Initial Drug Choices

    Without Compelling Indications

    With Compelling Indications

    Stage 1 Hypertension
    (SBP 140159 or DBP 9099 mmHg) Thiazide-type diuretics for most. May consider ACEI, ARB, BB, CCB, or combination.

    Stage 2 Hypertension
    (SBP >160 or DBP >100 mmHg) 2-drug combination for most (usually thiazide-type diuretic and ACEI, or ARB, or BB, or CCB)

    Drug(s) for the compelling indications


    Other antihypertensive drugs (diuretics, ACEI, ARB, BB, CCB) as needed.

    Not at Goal Blood Pressure Optimize dosages or add additional drugs until goal blood pressure is achieved. Consider consultation with hypertension specialist.

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