Peripherally acting antitussives

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Chapter: Medicinal Chemistry : Expectorants and Antitussives

i. Benzonatate (Tessalon) ii. Carbetapentane (Toclase) iii. Caramiphen iv. Isoaminile - Synthesis and Drug Profile


SYNTHESIS AND DRUG PROFILE 

Peripherally acting antitussives

 

i. Benzonatate (Tessalon)


Synthesis


Properties and uses: It is a long-chain polyglycol derivative chemically related to tetracaine and benzocaine. It is a potent antitussive agent. It usually acts by inhibiting the transmission of impulses of the cough reflex in the vagal nuclei of the medulla and predominately depresses polysynaptic spinal reflexes. It is regarded as a cough suppressant acting both centrally and peripherally.

Dose: The usual dose is 100 mg three times daily.

 

ii. Carbetapentane (Toclase)


Synthesis


Properties and uses: It is a cough suppressant and is reported to reduce bronchial secretions. It is found to be effective in acute coughs associated with common upper respiratory infections.

Dose: The usual dose is 25–150 mg per day in divided doses.

 

iii. Caramiphen


Synthesis


Uses: It is a cough suppressant, less active than codeine, but with longer duration of action. It has little effect on respiration and no tolerance of dependence develops.

 

iv. Isoaminile


Uses: Used for control and management of cough, it is also a bronchodilator.

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