The pharmacokinetics of thiacetazone, a bacteriostatic drug with both antituberculosis and antileprosy activity, have been studied in healthy volunteers and tuberculosis patients using a high pressure liquid chromatographic method. Urinary excretion of thiacetazone was measured over a period of7 days fo llowing the ingestion of a single oral dose of 150 mg of the drug. Peak plasma concentrations of thiacetazone during supervised daily treatment averaged 1•8 Ilg/ml. From the rate of decline of thiacetazone plasma concentrations and urinary excretion, it was calculated that thiacetazone concentrations capable of inhibiting the multiplication of Mycobacterium /eprae would only be maintained for about 3 days in the event of patients discontinuing to take the drug. It was concluded that thiacetazone cannot be recommended for use in the multi-drug treatment of lepromatous leprosy.
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