Dreyfuss G, Penicaut B, Parrondo-Iglesias E, Craciunescu D, Dubost G, Nicolas J A
Laboratoire de Parasitologie, Faculté de Pharmacie, Limoges.
Bull Soc Pathol Exot. 1990;83(3):367-75.
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.
顺铂（II）喷他脒的杀锥虫活性已在布氏布氏锥虫绵羊实验性锥虫病的第一阶段得到证实。但在锥虫病的脑期，5mg.kg-1（+2×12mg.kg-1）的皮下治疗无效。该化合物的血液药代动力学在45至60分钟之间出现血浆峰值，随后在数天内呈低水平下降阶段。曲线形状允许在下一次注射前有一个重要的间隔时间，并显示该化合物在内部器官和血管外部位有储存。已研究了顺铂（II）喷他脒的代谢模型：该产品可作为预防非洲锥虫病和美洲利什曼病的化学预防药物。
