Mahony C, Cox J L, Bjornsson T D
J Clin Pharmacol. 1983 Feb-Mar;23(2-3):123-6. doi: 10.1002/j.1552-4604.1983.tb02714.x.
Twenty patients received dipyridamole by two different dosage regimens yielding a total daily dose of 150 mg, either as 50 mg three times a day or 75 mg twice a day. The rationale for comparing these two regimens is that dipyridamole is usually given three times a day, but recent studies have revealed a final elimination half-life of the drug of about half a day. Based on drug cumulation during chronic dosing, the final half-life of dipyridamole observed in this study also averaged about half a day. The 75 mg b.i.d. regimen did not result in lower trough concentrations than the 50 mg t.i.d. regimen. There was wide interpatient variability in observed plasma dipyridamole concentrations for both regimens, averaging about 10-fold. These results suggest that dipyridamole could be administered twice a day and that dipyridamole levels should be monitored in clinical studies on the antithrombotic effect of the drug.
20名患者接受了双嘧达莫治疗,采用两种不同的给药方案,每日总剂量为150mg,即每日3次,每次50mg,或每日2次,每次75mg。比较这两种方案的基本原理是,双嘧达莫通常每日给药3次,但最近的研究表明该药物的最终消除半衰期约为半天。基于长期给药期间的药物蓄积情况,本研究中观察到的双嘧达莫最终半衰期平均也约为半天。每日2次,每次75mg的方案所导致的谷浓度并不低于每日3次,每次50mg的方案。两种方案观察到的血浆双嘧达莫浓度在患者间存在很大差异,平均约为10倍。这些结果表明,双嘧达莫可以每日给药2次,并且在该药物抗血栓作用的临床研究中应监测双嘧达莫水平。