Monoamino propylamine derivatives

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Chapter: Medicinal Chemistry : Antihistamines

H1-antagonists with classical structure : Monoamino propylamine derivatives - Saturated analogues : 1. Pheniramine Maleate (Avil, Polarmine) 2. Chlorpheniramine HCl (Piriton, Alermine) - Synthesis and Drug Profile


SYNTHESIS AND DRUG PROFILE

 

H1-antagonists with classical structure

 
Monoamino propylamine derivatives

 

i. Saturated analogues

 

1. Pheniramine Maleate (Avil, Polarmine)


Properties and uses: Pheniramine maleate is a white crystalline powder, freely soluble in water, alcohol, methanol, and methylene chloride. This drug is the least potent member of the series and is marketed as the racemate.

Assay: Dissolve the sample in anhydrous acetic acid and titrate against 0.1 M perchloric acid. Determine the end point potentiometrically.

Dose: Usual dose is 25–30 mg per day in divided doses.

Synthesis

Route I. From: 2-Phenylacetonitrile


Route II. From: Picolinaldehyde


 

2. Chlorpheniramine HCl (Piriton, Alermine)


Synthesis

Route-I. From: 2-(4-Chlorophenyl)acetonitrile


Route-II. From: Picolinaldehyde


Properties and uses: Chlorpheniramine HCl is a white crystalline powder, soluble in water and in ethanol. Chlorination of pheniramine in the para position of the phenyl ring increases potency by almost 10-fold, with no appreciable change in toxicity. Most of the antihistaminic activity resides with the dextro isomer.

Assay: Dissolve the sample in anhydrous acetic acid and titrate against 0.1 M perchloric acid. Determine the end point potentiometrically.

Dose: Usual oral dose is 5 mg three or four times per day.

Dosage forms: Chlorpheniramine maleate injection I.P., B.P., Chlorpheniramine maleate tablets I.P., B.P., Chlorpheniramine oral solution B.P.

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