PHARMACOKINETIC PROPERTIES OF THE TRYPANOCIDAL DRUG MELARSOPROL

With a biological assay and atomic absorption spectrometry we determin ed the level of melarsoprol in the serum and cerebrospinal fluid of 19 patients treated with melarsoprol in Daloa, Ivory Coast. Most serum l evels were between 2 and 4 mug/ml 24 h after administration, and were still greater-than-or-equal-to 0.1 mug/ml after 120 h. Levels in the c erebrospinal fluid were between 0 and 0.1 mug/ml. Elimination was biph asic, with a pronounced beta1 phase. Mean terminal elimination half-li fe of melarsoprol was about 35 h, volume of distribution was about 100 1 and total clearance was about 50 ml/min. The results of these first pharmacokinetic studies on melarsoprol were used to simulate possible alternative therapy schemes which might avoid some of the problems tha t arise with melarsoprol use.