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