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噻氯匹定(Tichopidine,T)为一抑制血小板聚集的新药,能减少各种血栓栓塞发作的危险性,并认为相对安全,但能显著抑制被肝细胞微粒体色素P_(450)酶系统(CYP)代谢的几种药物,如安替比林和茶硷,能降低后者的全身清除约36%.最近治疗缺血性心脏病与脑血管病病人趋向于伍用抗凝血药和抗血小板聚集药.华法令(Warfarin,W)是R与S两种对映异构体的消旋化合物,主要由CYP450代谢,临床效应主要由S-W起作用,因其活性是R-W的5~8倍.方法:9例男病人年龄为65~76岁,因患慢性房颤、复发性房扑、机械的人工心脏瓣膜,保持合成移植物通畅和中园,而长期服W12~48月,平均6±1.5mg/ d.均经筛选,即肝、肾功能、全血细胞包括白细胞分类和血小板计数均正常.试验前3月凝血酶元时间(PT)的变异系数≤5%.试验期戒烟酒、用原有的饮食和药物.伍用前和口服T250mg,2次/d的第13、14 d检验血清R-W和S-W的稳态血浓,用HPLC法经比率(INRs),用MLA1000C光学密度测定法,资料经统计学处理.结果与讨论:伍用T前后S-W平均血浓度从359.7至362.8ng/mL(升高
Tichopidine (T), a new drug that inhibits platelet aggregation, reduces the risk of various thromboembolic events and is believed to be relatively safe but significantly inhibits the hepatotoxicity caused by hepatocyte microsome P_ (450) enzyme system CYP) metabolites such as antipyrine and theophylline can reduce the systemic clearance of the latter about 36% .The recent treatment of patients with ischemic heart disease and cerebrovascular disease tended to use anti-coagulant and anti-drug Warfarin (W) is a racemic compound of two enantiomers of R and S. It is mainly metabolized by CYP450 and its clinical effect is mainly played by SW, because its activity is 5-8 times that of RW Methods: Nine male patients aged 65-76 years old, suffering from chronic atrial fibrillation, recurrent atrial flutter, mechanical prosthetic heart valves, keeping the synthetic graft patency and Park, and long-term service W12 ~ 48 months, an average of 6 ± 1.5mg / d were screened, that is, liver and kidney function, whole blood cells, including white blood cell classification and platelet count were normal .Three months before the test the coefficient of variation (PT) coefficient of variation (PT) With the original diet and drugs. Wu pre-and oral T250mg, 2 times / d on the 13th and 14th days to test serum RW and SW stable Blood concentration, ratio by HPLC method (INRs), with an optical density MLA1000C assays, data were statistically Results and discussion: combined with the longitudinal T S-W mean plasma concentration from 359.7 to 362.8ng / mL (increased