The sulfones are derivatives of 4,4'-diaminodiphenylsulfone (dapsone), all of which share certain pharmacological properties. Only dapsone and sulfoxone are considered here.
ANTIBACTERIAL ACTIVITY, MECHANISM OF ACTION, AND RESISTANCE
Because Mycobacterium leprae does not grow on artificial media, in vivo assays with rat footpads have been used to test potential therapeutic agents. Dapsone is bacteriostatic for M. leprae due to competitive inhibiton of dihydropteroate synthase, which prevents bacterial utilization of para-aminobenzoic acid.
M. leprae may develop drug resistance during therapy, which is termed secondary resistance; this typically occurs in lepromatous (multibacillary) patients treated with a single drug. The incidence is as high as 19%. Partial-to-complete primary resistance in previously untreated patients has been described in 2.5-40% of patients, depending on geographical location.
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