Vinyl pyrimidines

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Chapter: Medicinal Chemistry : Anthelmintics

Vinyl pyrimidines: Pyrantel (Antiminth, Combantrin) - Synthesis and Drug Profile


Anthelmintics - Synthesis and Drug Profile

Vinyl pyrimidines

 

Pyrantel (Antiminth, Combantrin)


Synthesis


Mode of action: Pyrantel is a depolarizing neuromuscular blocking agent. It induces marked persistent activation of the nicotinic receptors, which result in spastic paralysis of the worm. It is an alternative to mebendazole in the treatment of ascariasis and enterobiasis.

Properties and uses: It is a pale yellow or yellow powder, practically insoluble in water and in methanol, soluble in dimethyl sulphoxide. It is also as investigational drug for the treatment of hookworms, moniliformis, and trichostrongylus infections.

Assay: To the sample add acetic anhydride and glacial acetic acid, heat and stir. Allow to cool and titrate with 0.1 M perchloric acid. Determine the end point potentiometrically.

Doses: The dose for oral suspension or liquid is 50 mg/ml. A single dose of 11 mg/kg for ascarasis and enterobiasis.

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