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    Pharma Unit 1-2 Anti - Adrenergic Drugs

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    MIbrahim
    This document summarizes different types of anti-adrenergic drugs. It discusses alpha and beta adrenergic blockers, describing their mechanisms of action, classifications, effects and uses. Alpha blockers are used to treat conditions like hypertension and benign prostatic hyperplasia, while beta blockers are commonly used for hypertension, angina, arrhythmias and migraine prevention. The document provides details on selective and non-selective alpha and beta blockers as well as drugs that block both receptor types.

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    Pharma Unit 1-2 Anti - Adrenergic Drugs

    Uploaded by

    MIbrahim
    88 views21 pages
    This document summarizes different types of anti-adrenergic drugs. It discusses alpha and beta adrenergic blockers, describing their mechanisms of action, classifications, effects and uses. Alpha blockers are used to treat conditions like hypertension and benign prostatic hyperplasia, while beta blockers are commonly used for hypertension, angina, arrhythmias and migraine prevention. The document provides details on selective and non-selective alpha and beta blockers as well as drugs that block both receptor types.

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    Adrenergic drugs

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    Pharma Unit 1-2 Anti- Adrenergic drugs

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    This document summarizes different types of anti-adrenergic drugs. It discusses alpha and beta adrenergic blockers, describing their mechanisms of action, classifications, effects and uses. Alpha blockers are used to treat conditions like hypertension and benign prostatic hyperplasia, while beta blockers are commonly used for hypertension, angina, arrhythmias and migraine prevention. The document provides details on selective and non-selective alpha and beta blockers as well as drugs that block both receptor types.

    Copyright:

    © All Rights Reserved
    Download as PDF, TXT or read online from Scribd
    Download as pdf or txt
    88 views21 pages

    Pharma Unit 1-2 Anti - Adrenergic Drugs

    Uploaded by

    MIbrahim
    This document summarizes different types of anti-adrenergic drugs. It discusses alpha and beta adrenergic blockers, describing their mechanisms of action, classifications, effects and uses. Alpha blockers are used to treat conditions like hypertension and benign prostatic hyperplasia, while beta blockers are commonly used for hypertension, angina, arrhythmias and migraine prevention. The document provides details on selective and non-selective alpha and beta blockers as well as drugs that block both receptor types.

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    © All Rights Reserved
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    of 21

    Anti Adrenergic

    Drugs
    Introduction

    • Antagonise the receptor action of adrenaline


    and related drugs
    • Classified on the basis of receptors they
    block primarily
    • Alpha, Beta, Both
    • Each has their own sub types
    • Anti-adrenergics vs Adrenergic neurone
    blockers
    AntiAdrenergic Drugs

    Antiadrenergic agents inhibit the activity of the


    sympathetic nervous system. They act by
    blocking adrenergic receptors in target organs or by
    inhibiting the synthesis, storage, or release of
    endogenous catecholamines (mainly norepinephrine)
    Alpha adrenergic blocking Drugs
    • Non-equilibrium type (Non competitive):
    • Beta-haloalkylamines: Phenoxybenzamines
    • Equilibrium type (Competitive)
    • Non-selective
    • Ergot alkaloids: Ergotamine, Ergotoxin
    • Hydrogenated ergot alkaloids: Dihydroergotamine (DHE),
    Dihydroergotoxin
    • Imidazoline: Phentolamine
    • Miscellaneous: Chlorpromazine (Neuroleptics)
    • Alpha1 selective: Prazosin, Terazosin, Doxazosin,
    Alfuzosin, Tamsulosin
    • Alpha2 selective: Yohimbine
    General effects of alpha blockers
    • Fall in BP
    • Postural reflex interfered: marked hypotension 
    dizziness, syncope
    • Vasomotor reversal of Dale

    • Reflex tachycardia

    • Na+ retention and expansion of blood volume


    General effects of alpha blockers

    • Nasal stuffiness and miosis

    • Increased intestinal motility

    • Reduced tone of bladder trigone, sphincter and


    prostate

    • Inhibits ejaculation (relaxation of vas deferens and


    related)
    Alpha adrenergic blocking Drugs
    • Uses:
    • Pheochromocytoma
    • Hypertension
    (phenoxybenzamine/phentolamine)
    • HTN d/t clonidine withdrawal, cheese reaction
    • Benign hypertrophy of prostate
    • Secondary shock
    • Peripheral vascular disease (Raynaud’s,
    acrocyanosis)
    • Congestive heart failure
    Alpha adrenergic blocking Drugs
    • Side effects:
    • Phenoxybenzamine: Postural hypotension,
    palpitation, nasal blockade, miosis, inhibition of
    ejaculation

    • Ergot alkaloids: peripheral vascular insufficiency


    and gangrene of toes and fingers (ergotism)

    • Prazosin and alike : postural hypotension


    Beta adrenergic blocking drugs
    • Nonselective (beta-1 and beta -2)
    • Without intrinsic sympathomimetic activity:
    propranolol, sotalol, timolol
    • With intrinsic sympathomimetic activity: pindolol
    • With additional alpha blocking property:
    labetolol, carvedilol
    • Cardioselective (beta- 1)
    • Metoprolol, Atenolol, Acebutolol, Bisoprolol,
    Esmolol, Betaxolol, Celiprolol, Nebivolol
    Beta adrenergic blocking drugs
    First Second Third Generation (with
    Generation Generation additional alpha blocking
    (Older, (β1 and/or vasodilator property)
    nonselective) selective)
    Propanolol Metoprolol Labetalol
    Timolol Atenolol Carvedilol
    Sotalol Acebutolol Celiprolol
    Pindolol Bisoprolol Nebivolol
    Esmolol Betaxolol
    General Effects of beta blockers

    • Heart:
    • Decreases heart rate, force of contraction (high
    dose) and cardiac output

    • Reduced cardiac work and oxygen consumption

    • Blood supply to sub-endocardial region not


    impaired: improved oxygen supply/demand
    status in angina patients
    General Effects of beta blockers
    • Blood vessels:
    • Blocks fall in BP evoked by Isoprenaline; Enhanced
    rise in BP by Adr

    • Re-reversal of vasomotor reversal of Dale


    • Gradual fall in BP on prolonged
    administration in hypertensives
    • Adaptation of resistance vessels to reduced C.O.  fall
    in total peripheral resistance
    eneral Effects of beta blockers
    stem Effects
    spiratory Increase bronchial resistance (β2 blockade)
    S Subtle behaviour changes, forgetfulness, increased
    dreaming and nightmares
    Anti-anxiety effect (peripheral action of propranolol)
    tabolic Blocks adrenergically mediated lipolysis
    Inhibits glygenolysis in heart, skeletal muscles, liver
    May reduce carbohydrate tolerance (decreased insulin
    release)
    elet Inhibits adrenergically provoked tremor (β2
    blockade) Attenuate exercise capacity
    scl

    e Reduced secretion of aqueous humour and intra ocular


    Cardio-selective beta blockers
    Metoprolol, Atenolol, Acebutolol, Bisoprolol,
    Nebivolol
    • More potent β1 blocking action (lost at high doses)
    • Low propensity to cause bronchoconstriction
    • Less interference with carbohydrate metabolism
    • Lower incidence of colder hands and feet
    • Less effect on lipid profile
    • Less liable to impair exercise capacity
    Partial agonistic beta blockers
    Pindolol, Celiprolol, Acebutolol
    • Activates β1 and/or β2 receptors sub-
    maximally
    • Bradycardia and depression of contractility:
    • Not prominent at rest
    • Exercise tachycardia blocked
    • Prevents development of super-sensitivity
    • No/less effect on plasma lipid profile
    • Not suitable for prophylaxis in MI, migraine
    Beta blockers: Additional Properties
    Membrane stabilizing activity of
    beta blockers Lipid insoluble beta blockers
    Propanolol, Atenolol, Celiprolol,
    Oxprenolol, Bisoprolol, Sotalol
    acebutolol • Less likely to produce
    • Contributes to the sleep disturbances and
    nightmares
    anti arrhythmic
    action • Incomplete absorption, no
    first pass metabolism,
    • Significant only at high excreted unchanged in
    doses urine
    • Longer acting (6-20 hrs)
    • Effective in narrow dose
    range
    Beta adrenergic blocking drugs:Uses
    • Hypertension • Dissecting aortic
    • Stable Angina aneurysm
    • Cardiac arrhythmias • Pheochromocytoma
    • Myocardial infarction • Thyrotoxicosis
    • Congestive heart • Migraine
    failure • Anxiety
    • Hypertrophic • Essential tremor
    obstructive • Glaucoma
    cardiomyopathy
    Beta blockers: Adverse effects

    Can accentuate myocardial insufficiency and precipitate


    CHF/edema
    Bradycardia
    Exacerbates variant angina
    mpaired Carbohydrate tolerance
    Altered plasma lipid profile
    Tiredness and reduced exercise capacity
    Cold hands and feet
    Others: G.I. upset, lack of drive, nightmares,
    orgetfulness, hallucinations, sexual distress in male
    Beta blockers: Warnings and
    Contraindications

    • Sudden withdrawal : rebound hypertension,


    worsening of angina, sudden death
    • Worsens COPD; can produce acute Bronchial
    asthma: Contraindicated
    • Partial or complete heart block: Contraindicated
    α + β adrenergicblockers
    Labetalol, Carvedilol
    • β1+ β2 + α1 blocking property; weak β2 agonistic
    activity
    • 5 times more potent in blocking β receptors
    •• Fall
    Uses:in BP • Side
    • Pheochromocytoma •effects:
    Postural
    • Clonidine withdrawal Hypotension
    • Essential
    • Rashes, liver
    Hypertension
    damage
    That would be all for thistopic.

    Thank you!!!

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