Drugs used for the treatment of cough

Dr Aneela Khalid

LEARNING OBJECTIVES
Classification of drugs used for the non specific treatment of cough Define the term Expectorant and mucolytic Describe the mechanism of action, adverse effects and clinical uses of Expectorants Antitussives

Classification of drugs used for non specific treatment of cough

1. 2. 3. 4. Cough suppressants Centrally acting Antitussives Peripheral Antitussives Cough expectorants Antihistamines Bronchodilators

1) COUGH SUPPRESSANTS (Antitussives) 1- Centrally acting Antitussives Narcotic antitussive Opiates

Codeine Pholcodine Hydrocodone

Non narcotic antitussives Opiates

Dextromethorphan Levopropozyphene Noscapine

Non-Opiates Diphenhydramine Benzonatate

2- Peripheral Antitussives 1 Demulcents

Linctus Lozenges Liquorice

2 Inhalation
Water aerosol inhalation Benzoin Menthol

3 Local anaesthetics
Benzonatate Lignocaine (only in special circumstances)

2) Cough Expectorants 1 Drugs acting Reflexly

Ipecacuanha Ammonium chloride Potassium Iodide

2 Drugs Acting Directly

Potassium Iodide Guaiphenesin

3 Mucolytics

Acetylcysteine Bromhexine (Bisolvon) Carbocisteine Methylcysteine

Definition of Mucolytic and Expectorant

Mucolytic
A mucolytic is a drug that breaks down thick mucus, making it thinner and easier to cough out.

Expectorant
An expectorant is a drug which makes the cough more productive by loosening and liquefying bronchial secretions. Also known as Mucokinetics

Antitussives
Antitussives are substances that specifically inhibit or suppress the action of cough Depression of medullary centre or associated higher centers. Increases threshold of the cough centre. Interruption of tussal impulses peripherally in the respiratory tract. Inhibition of conduction along the motor pathways.

1)

2) 3) 4)

Narcotic Antitussives
Codeine and Pholcodeine
An opium alkaloid similar to morphine less potent then morphine as analgesic and respiratory depressant. 60% effective orally then parentrally as an analgesic and respiratory depressant. A standard antitussive A small fraction of administered codeine is metabolized to morphine which is responsible for analgesic effects of codeine.

MOA of Codeine:
Directly suppresses cough centre by binding to distinct receptors in Medulla. Suppresses cough for about 6 hrs. Dosage: 15 mg

Adverse effects of Codeine:

In therapeutic doses minimum side effects Sedations, nausea, constipation At higher doses respiratory depression and drowsiness can occur. Contraindicated in asthmatic patients and patients with diminished respiratory reserves.

 Pholcodeine has similar efficacy as codeine with longer duration of action of 12hrs It has no analgesic or addiction property

Non Narcotic Antitussives

Dextromethorphan Hydrobromide A synthetic compound. It is a dextrorotatory sterioisomer of a methylated derivative of levorphenol. Strong and partial agonist. As effective antitussive as codeine. MOA: 1. Controls cough spasm by depressing cough centre in medulla 2. Increase the threshold for coughing

Advantages of Dextromethorphan
No effect on ciliary activity No CNS depression No addiction potential No constipation Dosage: 15- 30mg three or four times daily.

Toxicity:
Toxic doses may cause. Stupor, ataxia, respiratory depression, convulsion in children and death with abuse of its purified powder.

 Contraindicated in children below 6 yrs of age and also in patients taking Monoamine oxidase inhibittors.

Levopropoxyphene
It is a sterioisomer of weak opioid agonist dextropropoxyphene. It is devoid of opioid effects Sedation is the only adverse effect

Dosage: 50-100mg 4hrly

Noscapine
An opium alkaloid No narcotic, analgesic or dependance inducing properties. Equally effective antitussive as codeine Useful for spasmodic cough. Headache and nausea are usual side effects Contraindicated in asthamatic patients.

Benzonatate
Chemically related to tetracaine. MOA: Reduces the cough reflex by anesthetizing the stretch receptors in the respiratory passages, Lungs and Pleura. It has some central effects also. Adverse effects: Headache, Dizziness, Pruritus Nasal Congestion, burning of eyes & tightness in chest.

EXPECTORANTS
These are the drugs which make the cough more productive by loosening and liquefying bronchial secretions. Also known as Mucokinetics.

Guaiphenesin
It is a derivative of Guaiacol Obtained from wood or synthetically prepared

MOA. Decrease sputum viscosity and increase

sputum volume thereby decreasing difficulty in expectoration only FDA Approved expectorant .

Adverse effects. Nausea, gastric disturbances

drowsiness and rash.

IPECACUANHA
Source: Natural alkaloid obtained from
roots of cephaelis acuminata contains:
Cephaeline Emetine

MOA.
Loosening & liquefying mucosa soothing irritated bronchial mucosa. It also has emetic & amoebicidal properties.

 Uses.

Mainly used for emesis in accidental poisoning.

Contraindications
Semiconscious, Unconscious or convulsing person
Corrosive poisoning or kerosine poisoning.

Mucolytics
MOA of Mucolytics:
Mucolytics open disulphide bonds in the mucoproteins present in the sputum making it less viscid.

Bromhexine: MOA: It depolymerizes the polysaccharides directly as well as by liberating lysosomal enzymes which breaks down the fiber network in the tenacious sputum. Particularly useful for mucous plugs. Adverse effects: Rhinorrhoea, lacrimation, and gastric irritation.

Antihistamines
Chlorphenaramine 2-5mg Diphenhydramine 5-25mg Promethazine 15-25mg Anti histamines provides relief in cough due to sedative and anticholinergic action. They lack selectivity for cough centres They have been promoted for treatment of cough in allergic states. No efficacy in Asthma

Bronchodilators
Bronchodilators by clearing secretions through increase in surface velocity of airflow during cough relieves . Should be used only when element of bronchoconstriction is present and not routinely Fixed dose combination of bronchodilators with anti tussives not preferred .

Special conditions
Cough may be useful or useless. No role of Antitussives Asthma young infants Congestive cardiac failure Bronchiactasis, COPD, Tuberculosis.

Antitussives may be prescribed For dry unproductive cough that is hazardous or is disturbing sleep. ( hernias, piles, after surgical procedures esp cataract surgery). Pholcodeine along with diphenhydramine is useful. In whooping cough or in pertusis. Bronchodilator along with Diphenhydramine is useful.