succimer and anthiolimine

The currently available anti-leishmanial antimonial drugs, together with other antimony compounds were individually tested, in combination with difluoromethylornithine (DFMO), against experimental murine trypanosomiasis with central nervous system involvement. Satisfactory cure rates could be achieved using a combination treatment of DFMO with most of these anti-leishmanial drugs, but in general, only when they were administered at least twice daily. Of the compounds tested, the most effective was antimony dimercaptosuccinate (Astiban).

Topics: Animals; Antimony; Antimony Sodium Gluconate; Drug Synergism; Drug Therapy, Combination; Eflornithine; Female; Meglumine; Meglumine Antimoniate; Mice; Organometallic Compounds; Succimer; Tartrates; Trypanocidal Agents; Trypanosoma brucei brucei; Trypanosomiasis, African

The SbIII preparations available for clinical use were compared in vitro for their concentration/time/effect curves on Trypanosoma venezuelense (T. evansi), measuring decrease of motility and of parasite numbers. With these two criteria leading to similar relative results, the drugs are classified into a rapidly acting group, led by sodium emetic (AST), followed by its dimethylcysteine chelate (NAP) and Anthiomaline, and a less and more slowly acting one: Triostam, Astiban and Stibophen. The relative activity of these drugs in vitro is parallel to that encountered against Schistosoma mansoni, attributed to a similar pattern of intracellular absorption. In vivo effectiveness may depend on bioavailability of Sb in the host and the direct action on the parasite, reflected by its in vitro activity. The interplay of these two factors leads to a different in vitro/in vivo activity relationship of the antimonials even in the same host (mouse) and to its variation in other host species.

Topics: Antimony; Antimony Sodium Gluconate; Benzenesulfonates; Cysteine; In Vitro Techniques; Organometallic Compounds; Succimer; Succinates; Tartrates; Trypanocidal Agents; Trypanosoma

Topics: Animals; Antimony; Antimony Sodium Gluconate; Benzenesulfonates; Drug Administration Schedule; Mice; Organometallic Compounds; Succimer; Succinates; Time Factors; Trypanosomiasis