Nakashima M, Yamamoto J, Shibata M, Uematsu T, Shinjo H, Akahori T, Shioya H, Sugiyama K, Kawahara Y
Department of Pharmacology, Hamamatsu University School of Medicine, Japan.
Eur J Clin Pharmacol. 1992;43(6):657-9. doi: 10.1007/BF02284968.
The pharmacokinetics of temocapril hydrochloride, a novel prodrug-type angiotensin-I converting enzyme (ACE) inhibitor, has been studied in patients with mild (Group II) to severe (Group III) renal insufficiency in comparison with subjects with normal renal function (Group I). The pharmacokinetic parameters of the active diacid metabolite, including Cmax, AUC and half-life (t1/2), showed only slight changes between the three groups: AUC (0-inaffinity) was significantly larger in Group III than Group I, and t1/2 tended to be prolonged in Group III, but the change was not significant. The urinary recovery of the diacid was significantly decreased in Group III. (Group I, 28.1%, Group II, 21.6%, Group III, 12.8%). Compared with other ACE inhibitors, which are mainly excreted through the kidney, the plasma concentration of the active diacid metabolite was hardly influenced by renal function. It was speculated that lowering of the dose of temocapril might be recommended only in patients with severe renal insufficiency.
已对新型前体药物型血管紧张素I转换酶（ACE）抑制剂盐酸替莫卡普利在轻度（II组）至重度（III组）肾功能不全患者中的药代动力学进行了研究，并与肾功能正常的受试者（I组）进行了比较。活性二酸代谢物的药代动力学参数，包括Cmax、AUC和半衰期（t1/2），在三组之间仅显示出轻微变化：III组的AUC（0-亲和力）显著大于I组，III组的t1/2有延长趋势，但变化不显著。III组二酸的尿回收率显著降低。（I组为28.1%，II组为21.6%，III组为12.8%）。与主要通过肾脏排泄的其他ACE抑制剂相比，活性二酸代谢物的血浆浓度几乎不受肾功能的影响。据推测，仅在重度肾功能不全患者中可能建议降低替莫卡普利的剂量。
