Erratic zidovudine bioavailability in HIV seropositive patients.

The bioavailability of zidovudine was evaluated in 16 HIV seropositive patients using a prospective standardized study. Symptomatology, D-xylose absorption and immune status were also measured to determine indicators of poor bioavailability. Zidovudine was rapidly absorbed (Tmax: 0.82 +/- 0.39 h) with a large variation in peak serum concentrations (Cmax: 1.21 +/- 0.64 mg/L). The mean elimination half-lives after intravenous and oral administration were 1.5 +/- 0.4 h and 1.3 +/- 0.2 h, respectively. Mean zidovudine bioavailability was 64.0 +/- 21.3% and was not associated with D-xylose absorption values. Five h urine D-xylose excretion was abnormal in seven patients but only three (43%) had zidovudine bioavailabilities below the mean for the group. Conversely, only five of nine patients (56%) with normal D-xylose absorption tests had zidovudine absorption values below the mean. The presence of a mild alteration in bowel habits, defined as up to four unformed or semi-solid stools per day, showed a highly significant relationship to low bioavailability (P < 0.0001, Student's t-test). Lower CD4 lymphocyte counts were also associated with a low bioavailability (R-squared, 0.36, P = 0.0143). Patients with lower CD4 lymphocyte counts or with mild diarrhoea may be at risk for erratic zidovudine absorption.