Urinary recovery and kinetics of sulphamethoxazole and its metabolites in HIV‐seropositive patients and healthy volunteers after a single oral dose of sulphamethoxazole.

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Abstract
1. The urinary excretion of sulphamethoxazole and its metabolites was compared between healthy volunteers and HIV‐seropositive patients in order to get a better understanding of why HIV seropositives are more predisposed to idiosyncratic toxicity of sulphonamides. 2. A single 800 mg oral dose of sulphamethoxazole was administered to seven healthy volunteers and seven asymptomatic HIV seropositives without previous use of sulphonamides. 3. Urine was collected for 4 days and drug analysis was by h.p.l.c. 4. No difference was observed between seropositive and seronegative individuals in the urinary recovery of sulphamethoxazole, N4‐acetyl‐, 5‐hydroxy‐, N4‐acetyl‐5‐hydroxy‐ sulphamethoxazole and the N1‐glucuronide conjugate. However the recovery of the hydroxylamine metabolite of sulphamethoxazole was significantly lower in the HIV seropositives (0.50 +/‐ 0.51 vs 2.23 +/‐ 0.85%; 95% CI on the difference, ‐0.90 to ‐2.55; P = 0.0006). 5. Sulphamethoxazole hydroxylamine may be a factor in the susceptibility of HIV infected individuals to sulphonamides.