Benzpyrazine derivatives

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Chapter: Medicinal Chemistry : Antileprotic Drugs

Benzpyrazine derivatives: Clofazimine (Lamprene), Thalidomide (Thaloda, Thycad, Thalomid)


Antileprotic Drugs - SYNTHESIS AND DRUG PROFILE

Benzpyrazine derivatives

 

Clofazimine (Lamprene)


Synthesis


Metabolism: It is thought to undergo hydroxylic dehalogenation on the 4-chloroaniline, followed by sulphate conjugation. It also undergoes glucuronic acid conjugation.


Properties and uses: Clofazimine is a reddish-brown fine powder, practically insoluble in water, soluble in methylene chloride, and very slightly soluble in ethanol. It is used as antileprotic drug.

Assay: Dissolve the sample in methylene chloride, add acetone and anhydrous acetic acid and titrate with

0.1 M perchloric acid. Determine the end point potentiometrically.

Dose: The dose orally is 100 mg daily.

Dosage forms : Clofazimine capsules I.P., B.P.

 

Thalidomide (Thaloda, Thycad, Thalomid)


Synthesis


Properties and uses: It is the drug of choice for Erythema nodosum leprosum. It must not be used in women during pregnancy because of its teratogenic activity.

Dose: Doses of 100–300 mg per day are effective.

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