ANTI-TUSSIVES, MUCOLYTICS AND

EXPECTORANTS

Copperbelt University School of Medicine

MBChB Pharmacology
February 2015
(Dr Sindwa Kanyimba)

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 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

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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)

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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

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 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

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 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
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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

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 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

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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

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ENDE

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