The metabolism and toxicity of dapsone was compared in vitro and in vivo in rat, mouse and man. Metabolism was assessed by high-pressure liquid chromatography-mass spectrometry and methemoglobin formation has been used as a toxic endpoint. The greatest toxicity in vitro was seen in microsomes prepared from male Wistar rats (36.6 +/- 1.5% methemoglobin), although toxicity was also seen in micros...

In order to address the question whether hypersensitivity reactions to dapsone are becoming more frequent, the clinical data of 7300 leprosy patients treated between 1949 and September 1988 at the McKean Rehabilitation Centre in Thailand were reviewed. Information from the period 1949 to 1969 was too incomplete to allow conclusions. The incidence of hypersensitivity reactions to dapsone between...

BACKGROUND Topical administration of dapsone can be an alternative route for treatment of leprosy and can also provide new therapeutic applications for an established drug. However, the physicochemical properties of dapsone make it difficult to incorporate into conventional formulations. The current study was directed toward developing a stable nanoemulsion that contains dapsone which can be ad...

Dapsone activates CYP2C9-mediated metabolism in various expression systems and is itself metabolized by CYP2C9 to its hydroxylamine metabolite. Studies were conducted with expressed CYP2C9 to characterize the kinetic effects of dapsone (0-100 microM) on (S)-flurbiprofen (2-300 microM), (S)-naproxen (10-1800 microM), and piroxicam (5-900 microM) metabolism in 6 x 6 matrix design experiments. The...

Dapsone-induced agranulocytosis is a rare adverse effect. There are various reports of agranulocytosis in patients treated with dapsone for malaria prophylaxis and other dermatological diseases. However, this adverse reaction in leprosy is not often encountered. We describe agranulocytosis in a young patient who was taking dapsone (100 mg) for borderline-tuberculoid leprosy in a rural environment.

OBJECTIVE To evaluate the risk of hemolysis in subjects with glucose-6-phosphate dehydrogenase (G6PD) deficiency who were treated for acne vulgaris with either dapsone gel, 5% (dapsone gel), or vehicle gel. DESIGN Double-blind, randomized, vehicle-controlled, crossover study. SETTING Referral centers and private practice. PARTICIPANTS Sixty-four subjects 12 years or older with G6PD defici...

Ninety-seven strains of Mycobacterium leprae recovered from patients with previously untreated multibacillary leprosy were tested for dapsone susceptibility. The specimens originated from Shanghai Municipality, Jiang-su Province and Fu-jian Province. Approximately 28% of the strains either did not infect the mice or the results of susceptibility were inconclusive due to the low proportion of vi...

Methaemoglobinaemia and haemolytic anaemia were the principal side-effects observed in 30 leprosy patients undergoing long-term treatment with dapsone as a single drug or as part of multidrug therapy. Hepatic, pancreatic and renal evaluations showed no relevant clinical changes. Since N-acetylation is a major metabolic pathway for dapsone, slow acetylation phenotype may be a risk factor for the...

Current treatment for leprosy is based on standard MDT which consists of dapsone, rifampicin, and clofazamine (WHO 1982). However, other antibiotics like ofloxacin, minocycline are also administered to patients, if required. Prior to the introduction of MDT, dapsone monotherapy was used for treatment. Long term monotherapy with dapsone resulted in poor compliance, treatment failures and emergen...