PYRIMETHAMINE

PYRIMETHAMINE

Brand Names : RP 4753; Daraprim; Chloridin; Darapram, Malocide; Tindurin; BW-50-63; Pirimetamina.
Pyrimethamine is a fully sub-stituted pyrimidine. It can be prepared  from open-chain compounds by cyclization reactions. In one method,it is synthesized from   α -propionyl-p- chlorophenylacetonitrile, which is converted into the ethyl ether by the action of ethyl orthopropionate. This ether reacts with guanidine to give a product which cyclizes to form pyrimethamine.

Pyrimethamine is a white, odourless, crystalline powder, m.p. 240-242°. It is practically insoluble in water, slightly soluble in ethanol and in dilute hydrochloric acid; soluble in boiling ethanol; very sparingly soluble in propylene glycol and dimethylacetamide at 70°; stored in airtight containers and protected from light. It is slowly but completely absorbed from the gastro-intestinal tract. It is present in the liver, lungs, kidney and spleen and is excreted through the urine.


Uses: Pyrimethamine is an antimalarial drug which is effective erythrocytic schizontocide againstall human malaria especially in most infections due to P. vivax and P. falciparum.

Side Effect
Pyrimethamine with sulphadoxine is usually well-tolerated but severe and sometimes fatal reactions have been reported. Severe cutaneous reactions include erythema, multiforme, Stevens-Johnson syndrome, and toxic epidermal necrolysis.


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