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    Anti-Tussives-Mucolytics-Expectorants-Feb 2015

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    This document discusses antitussives, mucolytics, and expectorants which are drugs used to manage cough. It describes cough as a protective reflex and the cough reflex pathway. It then explains the mechanisms and examples of three classes of cough preparations: [1] Antitussives suppress cough through the cough center, such as codeine, dextromethorphan, and diphenhydramine. [2] Expectorants liquefy mucus making it easier to cough up, such as guaifenesin, sodium citrate, and ammonium chloride. [3] Mucolytics directly alter mucus viscosity, such as acetylcysteine, carbocysteine, and bromhexine

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    Anti-Tussives-Mucolytics-Expectorants-Feb 2015

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    This document discusses antitussives, mucolytics, and expectorants which are drugs used to manage cough. It describes cough as a protective reflex and the cough reflex pathway. It then explains the mechanisms and examples of three classes of cough preparations: [1] Antitussives suppress cough through the cough center, such as codeine, dextromethorphan, and diphenhydramine. [2] Expectorants liquefy mucus making it easier to cough up, such as guaifenesin, sodium citrate, and ammonium chloride. [3] Mucolytics directly alter mucus viscosity, such as acetylcysteine, carbocysteine, and bromhexine

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    ANTI-TUSSIVES-MUCOLYTICS-EXPECTORANTS-FEB 2015

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    This document discusses antitussives, mucolytics, and expectorants which are drugs used to manage cough. It describes cough as a protective reflex and the cough reflex pathway. It then explains the mechanisms and examples of three classes of cough preparations: [1] Antitussives suppress cough through the cough center, such as codeine, dextromethorphan, and diphenhydramine. [2] Expectorants liquefy mucus making it easier to cough up, such as guaifenesin, sodium citrate, and ammonium chloride. [3] Mucolytics directly alter mucus viscosity, such as acetylcysteine, carbocysteine, and bromhexine

    Copyright:

    © All Rights Reserved
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    Download as pptx, pdf, or txt
    29 views10 pages

    Anti-Tussives-Mucolytics-Expectorants-Feb 2015

    Uploaded by

    Homeground entertainment
    This document discusses antitussives, mucolytics, and expectorants which are drugs used to manage cough. It describes cough as a protective reflex and the cough reflex pathway. It then explains the mechanisms and examples of three classes of cough preparations: [1] Antitussives suppress cough through the cough center, such as codeine, dextromethorphan, and diphenhydramine. [2] Expectorants liquefy mucus making it easier to cough up, such as guaifenesin, sodium citrate, and ammonium chloride. [3] Mucolytics directly alter mucus viscosity, such as acetylcysteine, carbocysteine, and bromhexine

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    © All Rights Reserved
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    of 10

    ANTI-TUSSIVES, MUCOLYTICS AND

    EXPECTORANTS

    Copperbelt University School of Medicine


    MBChB Pharmacology
    February 2015
    (Dr Sindwa Kanyimba)

    1
    Introduction

    • Antitussives, mucolytics and expectorants are drugs that are used in the
    management of cough
    • Cough is the sudden and forceful release of air from lungs. It is often an
    involuntary (protective) reflex
    • Cough is a useful physiological mechanism that serves to clear the
    respiratory passages of foreign material and excess secretions
    • Cough is produced by the cough reflex, which is integrated in the cough
    centre in the medulla
    • The initial stimulus for cough arises in the bronchial mucosa, where
    irritation results in bronchoconstriction
    • Cough receptors (specialised stretch receptors) in the trachea and
    bronchial tree, send vagal afferents to the cough center and trigger the
    cough reflex

    2
    Mechanism of cough

    Stimulation of mechano- or chemoreceptors (throat, respiratory


    passages or stretch receptors in lungs)

    Afferent impulses to cough centre (medulla)

    Efferent impulses via parasympathetic & motor nerves to


    diaphragm, intercostal muscles & lung

    Increased contraction of diaghramatic, abdominal & intercostal


    (ribs) muscles  noisy expiration (cough)

    3
    Drug management of cough

    • Cough should not be suppressed indiscriminately because it is


    a major defensive mechanism in the respiratory tract
    • There are, however, many situations in which cough does not
    serve any useful purpose but may, instead only annoy the
    patient or prevent rest and sleep
    • There are three classes of cough preparations:
    – Antitussives
    – Expectorants
    – Mucolytics

    4
    Antitussives

    • Antitussives are drugs that suppress cough and produces symptomatic relief
    • Mechanism of action of antitussives: Decrease sensitivity of the cough centre to
    peripheral stimuli and decrease mucosal secretions
    • Use of antitussives: cough suppression for non-productive irritating coughs
    • Drugs with anti-tussive effect include opiates and diphenhydramine
    • Examples of opiates that are used for cough suppression include: codeine, hydrocodone,
    hydromorphone, pholcodeine, noscapine and dextromethorphan
    • Antitussive actions of codeine, hydromorphone and hydrocodone occur at doses lower
    than those required for analgesia. However, they produce constipation, nausea and
    respiratory depression.
    • Dextromethorphan, noscapine and pholcodeine do not have analgesic properties and are
    not addictive and are less constipating
    • Diphenhydramine is an H1 receptor antagonist that acts centrally to decrease the
    sensitivity of the cough centre to afferents

    5
    Expectorants
    Expectorants are agents given orally to liquefy respiratory secretions
    and allow for their easier removal
    Expectorants stimulate the production of a watery, less viscous
    mucus
    Guaifenesin (glyceryl guiacolate)
    • Increases the volume and reduce the viscosity of secretion in
    trachea and bronchi by increasing respiratory tract fluid
    • Acts directly via the GIT to stimulate the vagal reflex
    • Near emetic doses are required for beneficial effect
    • Taken by mouth
    • Available as single drug and in combinations with other drugs
    6
    Expectorants …. cont’d

    Sodium and potassium citrate or acetate


    Increase bronchial secretions by salt action
    Ammonium salts (e.g. ammonium chloride)
    Gastric irritants that reflexly increase bronchial secretions

    7
    Mucolytics
    • Mucolytics liquefy the viscous tracheobronchial secretions. They designed to
    alter the viscosity of bronchial secretions, thereby making them easier to clear
    by cough or ciliary transport.
    • Mucolytics react directly with mucus to make it more watery resulting in the
    cough becoming more productive
    • Mucolytics include bromhexine, acetyl cysteine, carbocisteine, mecysteine
    • Uses of mucolytics: to facilitate expectoration of sputum in conditions such as
    cystic fibrosis and chronic obstructive pulmonary disease
    Acetylcysteine, carbocisteine and mecysteine
    • MOA: reduce the viscosity of mucus and sputum by cleaving disulfide bonds in
    the mucoproteins contained in them
    • Aceytylcysteine is given by inhalation while carbocisteine and mecysteine are
    given orally
    Bromhexine
    • MOA: thinning & fragmentation of mucopolysaccaride fibers

    8
    Antihistamines

    • Added to antitussives/expectorant formulations


    • Due to sedative & anticholinergic actions they produce relief
    in cough but lack selectivity for cough centre
    • They do no have expectorant action (anticholinergic effect
    results in thickening of secretions)
    • Suitable for allergic cough (not for asthma)
    • Examples: chlorpheniramine, diphenhydramine,
    promethazine

    9
    ENDE

    10

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