Expectorants & Antitussives

5-Oct-19 1
 Expectorants : Introduction

Definition: “Expectorants are oral drugs that are increase

bronchial secretion or reduce its viscosity, facilitating its
removal by coughing simply they enhance the clearance of
mucus.”.

Also called as Mucokinetics.

FDA has removed most expectorants from the market in a

review of over the-counter drugs; only guaifenesin is approved
as expectorants in the U.S.

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 Classification of
TheExpectorants
drugs used as expectorants are classified as follows;
1. Bronchial secretion enhancers:
Ex- Sodium or Potassium citrate,
Potassium iodide,
Guaiphenesin
(Glyceryl guaiacolate),
balsum of Tolu &
Vasaka,
Ammonium chloride.
2. Mucolytics:
Ex- Bromhexine,
Ambroxol,
Acetyl cysteine,
Carbocisteine
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1. Bronchial secretion
enhancers:
Potassium iodide secreted by bronchial glands and can irritate the
airway mucosa are considered to increase bronchial secretion by
salt action If potassium iodide given externally for prolong use
can affect thyroid function and produce iodism.

Guaiphenesin, vasaka, tolu balsum are plant products

enhance bronchial secretion and mucociliary function.

Ammonium salts are nauseating—reflexly increase respiratory

secretions so US-FDA has stopped marketing of all expectorants,
except guaiphenesin.

Now a days steam inhalation and proper hydration may be

more helpful in clearing airway mucus 5-Oct-19 4
2. Mucolytics:
Several agents can reduce the viscosity of sputum in vitro but
clinical studies in chronic bronchitis, asthma, and bronchiectasis
not showing much activity.

Mucolytic drugs (ex-derivatives of cysteine) reduce the disulfide

bridges that bind glycoproteins to other proteins such as
albumin and secretory IgA.

These drugs also act as antioxidants and may therefore

reduce airway inflammation.

Only N-acetylcysteine (MUCOMYST, others) is available

in the U.S.; carbocysteine, methylcysteine, erdosteine,
and bromhexine are available elsewhere.
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COPD patients if not treated with inhaled corticosteroids or
other medications shows symptomatic relief after treatment with
carbocysteine .

But N-acetylcysteine is not currently recommended for

COPD management.

Various triggers like oxidative stress, cigarette smoke,

inflammatory cytokines, and activated TLRs(Toll-like receptors)
stimulates the epidermal growth factor receptor (EGFR) which
plays a critical role in airway mucus secretion from goblet cells
and submucosal Glands.

Small molecule inhibitors of EGFR kinase, such as gefitinib

and erlotinib (anticancer drugs) are currently used for
treatments of mucus hypersecretion in COPD patient s .
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Sr Drug Name Use Dose
No
1 Bromhexine A derivative of the alkaloid vasicine Adults 8 mg TDS,
obtained from Adhatoda vasica (Vasaka). It children
is particularly useful if mucus plugs are 1–5 years 4 mg BD,
present. 5–10 years 4 mg TDS.
Potent mucolytic and mucokinetic. Side effects :
It depolymerises mucopolysacchrides Rhinorrhoea and
directly as well as by liberating lysosomal lacrimation, nausea,
enzymes network of fibres in tenacious gastricirritation,
sputum is broken hypersensitivity.

2 Ambroxol Metabolite of bromhexine having 15–30 mg TDS.

similar mucolytic action, uses and side AMBRIL, AMBROLITE,
effects. AMBRODIL, MUCOLITE

3 Acetylcysteine It opens disulfide bonds in mucoproteins MUCOMIX 200 mg/ml inj in

present in sputum—makes it less viscid, but 1,2,5 ml amps; injectable
has to be solution may be
administered directly into the respiratory nebulized/instilled through
tract. trachiostomy tube.

4 Carbocisteine It liquefies viscid sputum in the MUCODYNE 375 mg cap,

same way as acetylcysteine. 250 mg/5 ml.
Some patients of chronic bronchitis have
been shown to benefit.
It may break gastric mucosal barrier; is
contraindicated in peptic ulcer patients.
Side effects are gastric discomfo5r-tOactn- 7
1d9 rashes.
 Antitussives: Introduction
Definition: “ These are drugs that act in the CNS to raise the
threshold of cough centre or act peripherally in the respiratory tract
to reduce tussal impulses, or both these actions.”

Actually cough is a common symptom of airway disease, but its

mechanisms are poorly understood. Viral infections of the
upper respiratory tract are the most common cause of cough;
postviral cough is usually self-limiting and commonly patient-
medicated.

Antitussives should be used only for dry nonproductive cough or

if cough is unduly tiring, disturbs sleep or is hazardous (hernia,
piles, cardiac disease, ocular surgery).
Before treatment with antitussives, it is important to
identify underlying causal mechanisms that may r e q u i re
5 -O ct 8
-1 9

therapy.
 Classification of
Antitussives
1. Opioids: Ex- Codeine,
Ethylmorphine,
Pholcodeine.
2. Nonopioids: Ex-
Noscapine,
Dextromethorphan,
Chlophedianol.
3. Antihistamines: Ex-
Chlorpheniramine,
Diphenhydramine,
Promethazine.
4. Peripherally acting: Ex-
Prenoxdiazine.
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5. Adjuvant antitussives/
1. Opioids derivatives:
Definition: “Opiates have a central mechanism of action on μ
opioid receptors in the medullary cough center, they may have
additional peripheral action on cough receptors in the proximal
airways.”

Codeine and pholcodine are commonly used derivatives in

postviral cough but they produces side effects like sedation
and constipation.

Morphine and methadone are effective but indicated only

for intractable cough (lasts more than 8 weeks) associated
with bronchial carcinoma.

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Sr Drug Name Use Dose
No

1 Codeine An opium alkaloid, less potent than morphine, 10–30 mg;

but is more selective for cough centre. children
Codeine is standard antitussive; suppresses 2–6 years
cough for about 6 hours. 2.5–5 mg,
The antitussive action is blocked by naloxone 6–12 years
indicating that it is exerted through opioid 5–10 mg,
receptors in the brain. used as syrup
Side effect: Low Abuse liability and codeine phos.
constipation. 4–8 ml.
At higher doses specially in children CODINE 15
respiratory depression and drowsiness can
occur.

2 Ethylmorphine It is closely related to codeine DIONINDO

which is methylmorphine, and has antitussive, N 16 mg tab
respiratory depressant properties like it, but is
believed to be less constipating.

3 Pholcodeine It has practically no analgesic or addicting dose: 10–15

property, but is similar in efficacy as antitussive mg.
to codeine and is longer acting—acts
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for 12 11

hours.
2. Nonopioids derivatives:
Definition:“ These are the agents used in reducing cough
without causing any hallucinations or narcotic action it less
abuse potential .”
Sr No Drug Name Use Dose

1. Noscapine An opium alkaloid of the Dose: 15–30 mg,

(Narcotine) benzoisoquinoline series. children 2–6 years
It depresses cough but has no 7.5 mg, 6–12
narcotic, analgesic or dependence years 15 mg.
inducing properties. It is nearly COSCOPIN 7
equipotent antitussive as codeine, mg/5 ml syrup,
especially useful in spasmodic COSCOTABS 25
cough. mg tab.
Side effect: Headache and
nausea. It can release histamine
produce bronchoconstriction in
asthmatics.
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Sr Drug Name Use Dose
No

2 Dextro- A synthetic central NMDA Dose: 10–20

methorphan (N-methyl D-aspartate) receptor antagonist; mg,
also antagonize opioid receptors; children 2–6
The d-isomer – antitussive action years 2.5–5
l-isomer - analgesic. mg,
Non-addicting. The antitussive action of 6–12 years
dextromethorphan has been rated equivalent to 5–10 mg.
codeine.
Side effect: Dizziness, nausea, drowsiness; at
high doses hallucinations and ataxia ( without
coordination) may occur.

3 Chlophedianol It is a centrally acting antitussive Dose: 20–40

with slow onset and longer duration of mg;
action.
Side effect: Dryness of mouth, vertigo,
irritability. 5-Oct-19 13
 3.Antihistamines:
Many H1 antihistamines have been conventionally added
to antitussive/ expectorant formulations .

They relieves cough due to their sedative and anticholinergic

actions, but lack selectivity for the cough centre.

They have no expectorant property, may even reduce secretions

by anticholinergic action. They have been specially promoted for
cough in respiratory allergic states, though their lack of efficacy
in asthmatic conditions.
Chlorpheniramine (2–5 mg),
Diphenhydramine (15–25 mg) and
Promethazine (15–25 mg; PHENERGAN 5 mg/5 ml elixir)
Second generation antihistamines like fexofenadine, loratadine,
are ineffective.
etc. 5-Oct-19 14
4. Peripherally acting
antitussives:
Prenoxdiazine In contrast to other antitussives, it acts
peripherally; desensitizes the pulmonary stretch receptors
and reduces tussal impulses originating in the lungs.

It is indicated in cough of bronchial

origin. Efficacy, however, is not

impressive.

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5. Bronchodilators:
Bronchospasm can induce or aggravate cough. Stimulation of
pulmonary receptors can trigger both cough and
bronchoconstriction, especially in individuals with bronchial
hyperreactivity.

Bronchodilators relieve cough in such individuals and improve

the effectiveness of cough in clearing secretions by increasing
surface velocity of airflow during the act of coughing.

Fixed dose combinations of a centrally acting antitussive with

a bronchodilator or with an antihistaminic having high
atropinic activitivity.

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 SOME ANTITUSSIVE-EXPECTORANT COMBINATIONS

Sr. Brand Name Drugs Dosage

No form
1 ASTHALIN Salbutamol 2 + guaiphenesin 100 mg /10ml syrup
EXPECTORANT
2 ASCORIL-C Codeine 10mg+chlorpheniramine 4 mg/5ml
3 AXALIN Ambroxol 15 mg+guaiphenesin 50
mg+salbutamol 1 mg+ menthol 1 mg / 5 ml
4 BRONCHOSOLVIN Guaiphenesin 100 mg+ terbutalin 2.5mg + suspension
bromhexine 8 mg /10 ml
5 CADICOFF, Dextromethorphan 5 mg+ chlorpheniramine 2.5
GRILINCTUS mg+ guaiphenesin 50 mg+ Amm.chloride
60 mg/ 5 ml
6 BENADRYL Diphenhydramine 14 mg+ amm. chlor. 138 mg syrup
+ sod. citrate 57 mg+ menthol 1.1 mg/ 5 ml

7 BRO-ZEDEX Bromhexine 8 mg+ guaiphenesin 100 mg+ syrup

terbutaline 2.5 mg+ menthol 5 mg /10 ml
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 Sr. Brand Name Drugs Dosage
No form
8 CADISTIN Chlorpheniramine 2 mg+ glyceryl guaiacolate 80 syrup
EXPECTORA mg+ amm. chlor. 100 mg+ sod. citrate
NT 44 mg+ menthol 0.8 mg+ terpin hydrate 4 mg+
tolu
balsum 6 mg+ Vasaka syrup 0.13 ml.
9 CHERICOF Dextromethorphan 10 mg+ chlorpheniramine 2 Monophasic
mg, phenylpropanolamine 12.5 mg/ 5 ml. liquid
10 CLISTIN Carbinoxamine 4 mg+ amm. chlor. 240 mg+ sod. Syrup
citrate 240 mg/ 10 ml
11 COREX Chlorpheniramine 4 mg+ codeine phos. 10 mg+ syrup
menthol 0.1 mg/ 5 ml
12 COSCOPIN Noscapine 7 mg+ chlorpheniramine 2 mg+ citric syrup
LINCTUS acid 29 mg+ sod. citrate 3 mg+ amm. chlor. 28 mg/5
ml;
13 COSOME Dextromethorphan 10 mg+ phenylpropanolamine
25 mg+ chlorpheniramine 4 mg /10 ml
14 GRILINCTUS Dextromethorphan 5 mg, chlorpheniramine 2.5
mg, guaiphenesin 50 mg, ammon. chlor. 60 mg/5 ml
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Sr. No Brand Name Drugs Dosage
form
15 GRILINCTUS Dextromethorphan 10 mg+ Softcapsule
SOFTCAPS: chlorpheniramine 2 mg+
phenylpropanolamine 12.5 mg.
16 SOLVIN Bromhexine 4 mg+ pseudoephedrine 30 Tablet
EXPECTORANT mg
17 SOLVIN Bromhexine 4 mg+ pseudoephedrine Tablet &
EXPECTORANT: 30 mg Liquid
18 TOSSEX: Codeine phos 10 mg+ chlorpheniramine Liquid
4 mg.+menthol 1.5 mg+sod. citrate 75
19 VENTORLIN Salbutamol 2 mg+guaiphenesin syrup
EXPECTORANT 100 mg
20 ZEET LINCTUS: Dextromethorphan 10 mg+ guaiphenesin
50 mg+ phenylpropanolamine 25 mg

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Reference:
⚫ Rang H.P. and Dale M.M.: Pharmacology, Churchill
Livingstone, Edinbergh.
⚫ Katzung B.G.: Basic and Clinical Pharmacology, Lange
Medical Publications, California.
⚫ Craig C.R. and Stitzel R.E.: Modern Pharmacology,
Little Brown and Co., Boston.
⚫ Bowman W.C. and Rand M.J.: Textbook of
Pharmacology, Blackwell Scientific Publications,
Oxford.
⚫ P.N Bennett & M J Brown: Clinical Pharmacology,
Churchill Livingstone, Edinburgh.
⚫ Tripathi K.D.: Essentials of Medical Pharmacology,
Jaypee Brothers, Medical Publishers, New Delhi.
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