Respiratory system pharmacology

By

Mworozi Peter (BSc MSc)

COUGH
 Cough
Dfn:
Cough is a reflex triggered by a
mechanical or chemical stimulation of
upper respiratory tract or by a central
stimuli
Cough is a protective reflex mechanism
that removes foreign material and
secretions from the bronchi and
bronchioles.
Cough can be inappropriately stimulated by
respiratory conditions such as those
associated with inflammation (e.g. in asthma,
rhinitis) or with bronchial carcinoma (dry
painful cough).
However, sometimes cough occurs without a
known cause or persists despite treatment of
the primary condition ;which requires
specific antitussive therapy
 As a reflex, cough involves a reflex arc with sensor,
central and efferent component.
 The sensors and the central components of the reflex arc
are targets of drugs used to suppress cough.

 Drugs to suppress cough reduce either:

a. Receptor activation and therefore activity in the
afferent nerves. i.e. Peripherally acting antitussives
b. The sensitivity of the “cough center”. i.e. Centrally
acting antitussives
 Centrally acting antitussives
The narcotic analgesics:
 Have effective antitussive action in doses below those required for
pain relief, and various derivatives of these agents, which are
neither analgesic nor addictive, are also effective against cough.

Codeine
 Codeine, or methylmorphine, is an opiate that has considerably less
addiction liability than the main opioid analgesics.
 It possesses central antitussive actions by virtue of it’s agonist
action on opiate receptors in cough centers. This action can be
separated from other opioid effects.
 Codeine is usually used therapeutically in ‘cough mixtures’ in some
countries.
Adverse effects
 It decreases secretions in the bronchioles, which thickens sputum and
inhibits ciliary activity; this reduces clearance of the thickened sputum.
 Constipation also occurs because of the well-known action of opiates on the
GIT

Dextromethorphan
 It’s a derivative of the methyl ether opiate, levorphanol and is devoid of
analgesic properties.
 Its antitussive potency is equivalent to that of codeine.
 It produces only marginally less constipation and inhibition of mucociliary
clearance. but very high doses can cause CNS depression.

 PHOLCODINE
 Pholcodine is a non-analgesic opiate of the same chemical class as
papaverine; it is also used as a cough suppressant.
NOTE
 It should be understood that these drugs merely suppress the
symptom without influencing the underlying condition.

 These agents shouldn’t be given to patients presenting with

cough associated with bronchiectasis (suppurating bronchial
inflammation) or chronic bronchitis;
 Antitussive drugs can cause harmful sputum thickening and
retention.
 They should not be used for the cough associated with asthma.
 Peripherally acting antitussives
 These drugs act directly in some way to reduce the sensitivity of
“cough receptors” to substances such as irritant chemicals and
autacoids which activate these receptors.
Menthol
 Inhalation of menthol vapor reduces the sensitivity of peripheral cough
receptors.
 Drugs impregnated with menthol or eucalyptus oil will also reduce the
tendency to cough.
Topical local anaesthetics
 Such as benzocaine, bupivacaine or lidocaine applied to the pharynx
and larynx can reduce the sensitivity of the ‘cough receptors’ in these
areas to irritant chemical and physical stimuli.
 These are typically used to treat cough in patients who are resistant to
other cough therapies.
 Assignment
• Read and make a write up on
the; Antibacterial agents used
in the management of cough
• Commonly used herbal
remedies in the management
of cough
 Rhinitis
 This is an inflammation of the mucus membranes
of the nose.
 It is characterised by sneezing, nasal itching,
watery rhinorrhoea and congestion
 It may be caused by allergens like dust, pollen or
animal hair which interact with mast cells.
 Combination of oral antihistamines and
decongestants are the first line therapy for allergic
rhinitis
 ANTIHISTAMINES (H1-RECEPTOR
BLOCKERS)
 These are the most frequently used drugs in treatment of
sneezing and watery rhinorrhoea associated with allergic
rhinitis
 Eg diphenylhydramine, chlopheniramine, loratadine,
terfenadine and astamizole

 These drugs are useful in treating symptoms of allergic

rhinitis caused by histamine release.
 A combination of antihistamines and decongestants are
useful in treating rhinitis
 The two drug classes only differ in their duration of action
 ALPHA ADRENERGIC AGONISTS (NASAL
DECONGESTANTS )
 Phenylephrine and oxymetazoline

 These drugs constrict dilated arterioles in the nasal

mucosa and reduce air way resistance
 When administered as aerosols, they have a rapid onset of
action and show fewer systemic effects
 A combination of antihistamines and alpha adrenergic
agonists should not be used for long because rebound
nasal congestion can occur upon discontinuation of these
drugs
 Corticosteroids
 Beclomethasone , fluticasone, flunisolide and triamcinolone are
effective when administered as nasal sprays
 Topical steroids may be more effective than systemic
antihistamines in reliving the nasal symptoms of both allergic and
non allergic rhinitis
 Treatment of chronic rhinitis may not result in improvement until 1
to two weeks after the start of therapy
 Cromolyn -This drug may be used before contact with the allergen
 Chronic Obstructive Lung disease (COPD)
 This is a chronic irreversible obstruction of air flow
 Smoking is the greatest risk factor of COPD

 Bronchodilators like anticolinergic agents, beta adrenergic

agonists and theophyline are use to treat COPD
 Treatment does not cure the disease but only reduces the
symptoms
 End
“Success is for hard
workers not for comfert
seekers”