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    Chapter 10 Adrenoceptor Antagonist Drugs

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    Christine Annmarie Tapawan
    This document summarizes adrenoceptor antagonist drugs, including alpha and beta blockers. It describes their classification, mechanisms of action, effects, and clinical uses. Alpha blockers are classified as irreversible long-acting, reversible short-acting, alpha1 selective, or alpha2 selective. Nonselective alpha blockers reduce cardiovascular tone and blood pressure, while selective alpha1 blockers cause less tachycardia. Beta blockers are classified based on receptor selectivity and other properties. They are used to treat hypertension, angina, heart failure, glaucoma and other conditions, and can cause side effects affecting the cardiovascular, respiratory, and central nervous systems.

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    Chapter 10 Adrenoceptor Antagonist Drugs

    Uploaded by

    Christine Annmarie Tapawan
    75 views7 pages
    This document summarizes adrenoceptor antagonist drugs, including alpha and beta blockers. It describes their classification, mechanisms of action, effects, and clinical uses. Alpha blockers are classified as irreversible long-acting, reversible short-acting, alpha1 selective, or alpha2 selective. Nonselective alpha blockers reduce cardiovascular tone and blood pressure, while selective alpha1 blockers cause less tachycardia. Beta blockers are classified based on receptor selectivity and other properties. They are used to treat hypertension, angina, heart failure, glaucoma and other conditions, and can cause side effects affecting the cardiovascular, respiratory, and central nervous systems.

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    CHAPTER 10 ADRENOCEPTOR ANTAGONIST DRUGS(1)

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    This document summarizes adrenoceptor antagonist drugs, including alpha and beta blockers. It describes their classification, mechanisms of action, effects, and clinical uses. Alpha blockers are classified as irreversible long-acting, reversible short-acting, alpha1 selective, or alpha2 selective. Nonselective alpha blockers reduce cardiovascular tone and blood pressure, while selective alpha1 blockers cause less tachycardia. Beta blockers are classified based on receptor selectivity and other properties. They are used to treat hypertension, angina, heart failure, glaucoma and other conditions, and can cause side effects affecting the cardiovascular, respiratory, and central nervous systems.

    Copyright:

    © All Rights Reserved
    Download as PDF, TXT or read online from Scribd
    Download as pdf or txt
    75 views7 pages

    Chapter 10 Adrenoceptor Antagonist Drugs

    Uploaded by

    Christine Annmarie Tapawan
    This document summarizes adrenoceptor antagonist drugs, including alpha and beta blockers. It describes their classification, mechanisms of action, effects, and clinical uses. Alpha blockers are classified as irreversible long-acting, reversible short-acting, alpha1 selective, or alpha2 selective. Nonselective alpha blockers reduce cardiovascular tone and blood pressure, while selective alpha1 blockers cause less tachycardia. Beta blockers are classified based on receptor selectivity and other properties. They are used to treat hypertension, angina, heart failure, glaucoma and other conditions, and can cause side effects affecting the cardiovascular, respiratory, and central nervous systems.

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    © All Rights Reserved
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    of 7

    Basic and Clinical Pharmacology

    C10 ADRENOCEPTOR ANTAGONIST DRUGS


    A. Q. Sangalang, MD, MHPEd, FPOGS
    FACULTY OF PHARMACY
    UNIVERSITY OF SANTO TOMAS

    • Alpha and beta blockers


    • Differ in their effects and clinical application
    • Pharmacologic antagonists
    • Divided into primary subgroups based on the receptor selectivity

    ADRENOCEPTOR ANTAGONISTS
    Alpha-blockers Beta-blockers
    Alpha2-selective Beta2-selective
    Alpha1-selective Beta1-selective
    Nonselective Nonselective
    Reversible
    Irreversible

    ALPHA BLOCKING DRUGS


    • All active by
    Ø Oral route
    Ø Parenteral route

    CLASSIFICATION/PHARMACOKINETICS/MOA
    IRREVERSIBLE LONG-ACTING
    • PHENOXYBENZAMINE
    o Prototype
    o Only slightly alpha1 selective
    o Short elimination half life
    o Long duration of action (48 hours)
    o Binds covalently to the alpha receptors
    REVERSIBLE SHORT-ACTING
    • PHENTOLAMINE
    o Prototype
    o Nonselective (alpha1=alpha2)
    o Duration of action
    Ø Oral (2-4 hours)
    Ø IV (20-40 minutes)
    ALPHA1 SELECTIVE
    • PRAZOSIN
    o Prototype
    o Selective reversible alpha1 blocker
    o Duration of action 8-24 hours
    o Doxasozin, terazosin and tamsulosin
    ALPHA2 SELECTIVE
    • YOHIMBINE, RAUWOLSCINE
    o Prototype
    o Selective alpha2 competitive blockers
    o Used primarily in research application
    • •YOHIMBINE
    o Treatment of orthostatic hypotension

    1
    o Promotes norepinephrine release through blockade of α2 receptors in both
    the CNS and the periphery

    EFFECTS
    NONSELECTIVE BLOCKERS
    • Most important effects are on the CVS system
    o Reduction in cardiovascular tone
    o Reduction of both arterial and venous pressure
    Ø Decrease in BP
    • Cause baroreceptor reflex-mediated tachycardia as a result of the drop
    in mean arterial pressure (MAP)
    o Tachycardia maybe exaggerated-
    o Alpha2 receptors on adrenergic terminals in the heart that normally
    reduce the release of NE are also blocked

    • EPINEPHRINE REVERSAL
    o Predictable result of the use of an agonist in a patient who has received
    an alpha-blocker
    o Reversal in the BP effect of large doses of epinephrine
    o From pressor response (alpha receptors) to a depressor response
    (beta receptors)
    o Not observed with phenylephrine or NE because they lack sufficient
    beta2 effects

    SELECTIVE ALPHA1 BLOCKERS


    • Block alpha1 receptors much more effectively
    • Cause much less tachycardia than the nonselective blockers when reducing
    BP
    • Limited clinical application
    Ø Presurgical treatment of pheochromocytoma
    • Tumor that secretes cathecolamines
    • Phenoxybenzamine is used during the preparatory phase
    • Phentolamine during surgery

    NONSELECTIVE ALPHA BLOCKERS


    • Severe hypertension caused by overdose with drugs of abuse such as
    amphetamine, cocaine, or phenylpropanolamine

    SELECTIVE ALPHA BLOCKERS


    • Prazosin, doxazosin, and terazosin are used in hypertension
    • Used together with tamsulosin for urinary hesitancy and prevention of urinary
    retention with benign prostatic hyperplasia

    TOXICITY
    • Main manifestation is orthostatic hypotension
    • For nonselective agents, marked reflex tachycardia
    • Nausea and vomiting when taken orally
    • Exaggerated orthostatic hypotensive response to the first dose of alpha1-
    selective agents

    2
    BETA BLOCKING DRUGS
    • Competitive pharmacologic antagonists
    • Propranolol is the prototype
    • Developed for chronic oral use
    • Bioavailability and duration of action vary widely
    • Usually classified into subgroups (Table in Katzung)

    CLASSIFICATION/SUBGROUPS/MECHANISMS

    • RECEPTOR SELECTIVITY
    o Beta1 receptor selectivity
    o Beta1 block>beta2 block
    o Advantage when treating patients with asthma
    • Beta1 receptor selectivity
    o Acebutolol
    o Atenolol
    o Esmolol
    o Metoprolol
    • Nonselective beta-blockers
    o Nadolol
    o Propranolol
    o Timolol
    o Pindolol
    • Combined alpha and beta-blockers
    o Optically active
    Ø Labetalol
    Ø Carvedilol
    • PARTIAL AGONIST ACTIVITY
    o ” Intrinsic sympathomimetic activity”
    o Pindolol
    o Acebutolol
    o Labetalol

    3
    o May be an advantage in treating patients with asthma
    o At maximum dose, can cause some bronchodilatation
    • LOCAL ANESTHETIC ACTIVITY
    o ”Membrane stabilizing ability”
    o Disadvantage when a beta-blocker is used topically in the eye because
    it decreases protective reflexes and increases the risk of corneal
    ulceration
    o Acebutolol
    o Labetalol
    o Metoprolol
    o Propranolol
    o Pindolol

    ESMOLOL
    • Short-acting ester
    • Used only parenterally

    NADOLOL
    • Longest acting beta-blocker
    ACEBUTOLOL, ATENOLOL and NADOLOL
    • Less lipid soluble
    • Enter the CNS to a lesser extent

    4
    EFFECTS
    CVS
    • Decrease BP
    • Antagonize renin secretion
    • (-) inotropic effect
    • (-) chronotropic effect
    RESPIRATORY
    • Bronchoconstriction
    • Increase airway resistance
    EYE
    • Decrease intraocular pressure
    • Decrease production of aqueous humor
    METABOLIC AND ENDOCRINE
    • Reduce insulin secretion
    • Caution for insulin dependent DM

    CLINICAL USES
    • Open-angle glaucoma
    • Hypertension
    • Angina
    • Arrhythmias
    • Chronic heart failure
    • Pheochromocytoma

    TOXICITY
    CVS
    • Bradycardia

    5
    • AV blockade
    • Heart failure
    RESPIRATORY
    • Worsen the asthma
    CNS
    • Sedation
    • Fatigue
    • Sleep alteration
    • Depression
    • Psychosis

    6
    7

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