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Dapsone Pharmacology, Pharmacokinetics, Studies, Metabolism - Dapsone

Dapsone Pharmacology, Pharmacokinetics, Studies, Metabolism - Dapsone

CLINICAL PHARMACOLOGY

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The mechanism of action in Dermatitis herpetiformis has not been established. By the kinetic method in mice, Dapsone is bactericidal as well as bacteriostatic against Mycobacterium leprae.

Absorption and Excretion

Dapsone, when given orally, is rapidly and almost completely absorbed. About 85 percent of the daily intake is recoverable from the urine mainly in the form of water-soluble metabolites. Excretion of the drug is slow and a constant blood level can be maintained with the usual dosage.

Blood Levels

Detected a few minutes after ingestion, the drug reaches peak concentration in 4-8 hours. Daily administration for at least eight days is necessary to achieve a plateau level. With doses of 200 mg daily, this level averaged 2.3 mg/ml with a range of 0.1-7.0 mg/ml. The half-life in the plasma in different individuals varies from ten hours to fifty hours and averages twenty-eight hours. Repeat tests in the same individual are constant. Daily administration (50 - 100 mg) in leprosy patients will provide blood levels in excess of the usual minimum inhibitory concentration even for patients with a short Dapsone half-life.

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