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    Beta Adrenergic Blockers: Sympatholytic

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    Abdullah asad
    Beta adrenergic blockers work by competitively blocking beta-adrenergic receptors, which prevents the "fight or flight" response and lowers heart rate, blood pressure, and myocardial contractility. There are selective and non-selective beta blockers that are well-absorbed orally and have half-lives of 3-10 hours. They are used to treat hypertension, ischemic heart disease, arrhythmias, hyperthyroidism, migraines, tremors, and anxiety. Potential adverse effects include bradycardia and CNS effects like sedation.

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    Beta Adrenergic Blockers: Sympatholytic

    Uploaded by

    Abdullah asad
    70 views12 pages
    Beta adrenergic blockers work by competitively blocking beta-adrenergic receptors, which prevents the "fight or flight" response and lowers heart rate, blood pressure, and myocardial contractility. There are selective and non-selective beta blockers that are well-absorbed orally and have half-lives of 3-10 hours. They are used to treat hypertension, ischemic heart disease, arrhythmias, hyperthyroidism, migraines, tremors, and anxiety. Potential adverse effects include bradycardia and CNS effects like sedation.

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    Beta Blockers

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    Beta adrenergic blockers work by competitively blocking beta-adrenergic receptors, which prevents the "fight or flight" response and lowers heart rate, blood pressure, and myocardial contractility. There are selective and non-selective beta blockers that are well-absorbed orally and have half-lives of 3-10 hours. They are used to treat hypertension, ischemic heart disease, arrhythmias, hyperthyroidism, migraines, tremors, and anxiety. Potential adverse effects include bradycardia and CNS effects like sedation.

    Copyright:

    © All Rights Reserved
    Download as PPTX, PDF, TXT or read online from Scribd
    Download as pptx, pdf, or txt
    70 views12 pages

    Beta Adrenergic Blockers: Sympatholytic

    Uploaded by

    Abdullah asad
    Beta adrenergic blockers work by competitively blocking beta-adrenergic receptors, which prevents the "fight or flight" response and lowers heart rate, blood pressure, and myocardial contractility. There are selective and non-selective beta blockers that are well-absorbed orally and have half-lives of 3-10 hours. They are used to treat hypertension, ischemic heart disease, arrhythmias, hyperthyroidism, migraines, tremors, and anxiety. Potential adverse effects include bradycardia and CNS effects like sedation.

    Copyright:

    © All Rights Reserved
    Download as PPTX, PDF, TXT or read online from Scribd
    Download as pptx, pdf, or txt
    of 12

    Beta Adrenergic Blockers

    Also known as sympatholytic drugs. They produce competitive antagonism


    of beta-adrenoceptors in the autonomic nervous system. This prevents the
    “flight or fight” response induced by adrenaline and noradrenaline.

    MODE OF ACTION:
    LOWERS MYOCARDIAL OXYGEN DEMAND BY

    A. REDUCING HEART RATE


    B. REDUCING BLOOD PRESSURE
    C. REDUCING MYOCARDIAL CONTRACTILITY
    Types

    • There are three main sub-types of beta-adrenoceptors:

    • Beta1-adrenoceptors (75%) are located in the heart (selective)


    • Beta 2-adrenoceptors are located in vascular and bronchial smooth
    muscle
    • Beta 3-adrenoceptors are located on adipocytes and are thought to be
    involved with fatty acid metabolism
    Classification
    Non Selective act both on beta 1 and beta 2 adrenergic receptors.
    • Propranolol, sotalol, timolol, pindolol, labetalol,carvedolol (1st
    generation)
    Selective that act only on Beta 1
     Metoprolol, atenolol, bisoprolol, acebutolol (2nd generation)
     3rd generation having alpha blocking activity
    Pharmacokinetics
    • Absorption
    • Most of the drugs in this class are well absorbed after oral
    administration; peak concentrations occur 1–3 hours after ingestion.
    • Sustained-release preparations of propranolol and metoprolol are
    available
    • Distribution and Clearance
    • The β antagonists are rapidly distributed and have large volumes of
    distribution. Propranolol and penbutolol are quite lipophilic and readily
    cross the blood-brain barrier. Most β antagonists have half-lives in the
    range of 3–10 hours.
    Pharmacodynamics of the Beta-Receptor
    Antagonist Drugs
    • Effects on the Cardiovascular System
    • Beta-blocking drugs given chronically lower blood pressure in patients
    with hypertension. The mechanisms involved are not fully understood
    but probably include suppression of renin release and effects in the
    CNS. These drugs do not usually cause hypotension in healthy
    individuals with normal blood pressure. So it is useful
    • Angina
    • Myocardial infarction
    • chronic heart failure
    Effects on the Respiratory Tract
    • Blockade of the β2 receptors in bronchial smooth muscle may lead to
    an increase in airway resistance, particularly in patients with asthma.
    Consequently, these drugs should generally be avoided in patients with
    asthma.
    Effects on the Eye
    • Beta-blocking agents reduce intraocular pressure, especially in
    glaucoma. The mechanism usually reported is decreased aqueous
    humor production
    Metabolic and Endocrine Effects

    • Beta-receptor antagonists such as propranolol inhibit sympathetic


    nervous system stimulation of lipolysis.

    • glycogenolysis in the human liver is at least partially inhibited after


    β2-receptor blockade. Glucagon is the primary hormone used to
    combat hypoglycemia so they should be used with caution in insulin-
    dependent diabetic patients.
    • The chronic use of β-adrenoceptor antagonists has been associated with
    increased plasma concentrations of very-low-density lipoproteins (VLDL)
    and decreased concentrations of HDL cholesterol. Both of these changes
    are potentially unfavorable in terms of risk of cardiovascular disease

    • Effects Not Related to Beta-Blockade

    • Local anesthetic action, also known as “membrane-stabilizing” action, is a


    prominent effect of several β blockers. This action is the result of typical
    local anesthetic blockade of sodium channels.
    CLINICAL PHARMACOLOGY OF THE BETA-
    RECEPTOR–BLOCKING DRUGS
    • Hypertension
    • The β-adrenoceptor–blocking drugs have proved to be effective and
    well tolerated in hypertension
    • Ischemic Heart Disease
    • Beta-adrenoceptor blockers reduce the frequency of anginal episodes
    and improve exercise tolerance in many patients with angina These
    actions are due to blockade of cardiac β receptors, resulting in
    decreased cardiac work and reduction in oxygen demand.
    • Cardiac Arrhythmias
    • Beta antagonists are often effective in the treatment of both
    supraventricular and ventricular arrhythmias

    • Hyperthyroidism
    • Excessive catecholamine action is an important aspect of the
    pathophysiology of hyperthyroidism, especially in relation to the
    heart. The β antagonists are beneficial in this condition. Propranolol
    has been used extensively in patients with thyroid storm (severe
    hyperthyroidism
    Neurologic Diseases
    • Propranolol reduces the frequency and intensity of migraine
    headache. Other β-receptor antagonists with preventive efficacy
    include metoprolol and probably also atenolol, timolol, and nadolol.
    The mechanism is not known.
    • Since sympathetic activity may enhance skeletal muscle tremor, so β
    antagonists have been found to reduce certain tremors
    • The somatic manifestations of anxiety may respond dramatically to
    low doses of propranolol, particularly when taken prophylactically.
    For example, benefit has been found in musicians with performance
    anxiety (“stage fright”).
    • Propranolol may contribute to the symptomatic treatment of alcohol
    withdrawal in some patients.
    Adverse effects
    • Bradycardia
    • CNS effects include mild sedation, vivid dreams, and rarely,
    depression
    • Discontinuing the use of β blockers in any patient who develops
    psychiatric depression should be seriously considered if clinically
    feasible.

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