i. Dapsone (DDS, Diaminodiphenyl sulphone) ii. Solapsone Sodium, Acedapsone
Sulphones
Synthesis
Route I. From: 4-chloro nitrobenzene
Route II. From: 4-Chloro nitrobenzene
Metabolism: The major metabolic product of Dapsone results from N-acetylation in the liver by N-acetyltransferase. It also undergoes N-hydroxylation to hydroxylamine
derivative. These metabolic reactions are catalyzed by CYP3A4 isoforms. Neither
of these compounds possesses significant leprostatic activity, although N-acetyldiamino-diphenyl sulphone may be
deacetylated back to Dapsone. Products found in the urine consist of small
amounts of Dapsone and the metabolites, that is, N-acetyldiamino-diphenyl sulphone and N-hydroxy-diamino-diphenyl sulfone, as well as glucuronide and
sulphate of each of these substances.
Properties and uses: Dapsone is a white or slightly yellowish-white
crystalline powder, very slightly soluble in water, soluble in acetone and
dilute mineral acids, but sparingly soluble in alcohol. It is a folic acid
synthesis inhibitor used in both lepromatous and tuberculoid leprosy.
Assay: Dissolve the sample in dilute hydrochloric acid and add
potassium bromide. Cool in ice and titrate against 0.1 N sodium nitrate.
Determine the end point electrometrically.
Dosage: The dose as tablets is 25 or 100 mg. For adults the dose
consumed is 50 mg per day orally. For lepromatous leprosy, 100 mg Dapsone + 600
mg Rifampin and/or clofazimine 100 mg daily for at least 2 years followed by
Dapsone monotherapy. For borderline tuberculoid disease, Dapsone 100 mg daily +
Rifampin 600 mg once monthly for 6 months.
Dose : Dapsone tablets I.P., B.P.
Synthesis
Synthesis
Route I: From Dapsone
Route II: From 4-Chloro nitrobenzene
Properties and uses: Acedapsone (prodrug of Dapsone) is used in the
treatment of both lepromatous and tuberculoid type of leprosy.
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