[Trypanocidal activity and plasma kinetics of cis-Pt(II) pentamidine in the parasitized sheep].
The trypanocidal activity of cis-Pt(II) pentamidine had been demonstrated during the first phase of Trypanosoma brucei brucei sheep experimental trypanosomiasis. But a subcutaneous treatment with 5 mg.kg-1 (+2 x 12 mg.kg-1) was not effective during the brain phase of trypanosomiasis. The blood pharmacokinetics of this compound had a plasmatic peak between 45 and 60 min, followed by a low decreasing phase along several days. The curve shape allowed an important interval before the following injection, and showed a compound storage in internal organs and extravascular sites. A model of cis-Pt(II) pentamidine metabolism had been studied: this product could be used as a chemoprophylactic medicine against African trypanosomiasis and American leishmaniasis.
Laboratoire de Parasitologie, Faculté de Pharmacie, Limoges.
G
G
Dreyfuss
B
B
Penicaut
E
E
Parrondo-Iglesias
D
D
Craciunescu
G
G
Dubost
J A
JA
Nicolas
D000818:Animals; D007700:Kinetics; D008297:Male; D009944:Organoplatinum Compounds / Q000097:blood / Q000493:pharmacokinetics* / Q000627:therapeutic use; D010419:Pentamidine / Q000031:analogs & derivatives* / Q000097:blood / Q000493:pharmacokinetics / Q000627:therapeutic use; D012756:Sheep / Q000469:parasitology; D014344:Trypanocidal Agents / Q000493:pharmacokinetics*; D014353:Trypanosomiasis, African / Q000097:blood / Q000188:drug therapy*
D009944:Organoplatinum Compounds; D014344:Trypanocidal Agents; C057919:platinum(II) pentamidine; D010419:Pentamidine
Activité trypanocide et cinétique plasmatique de la cis-Pt(II) pentamidine chez le mouton parasité.