Rimmer E M, Routledge P A, Tsanaclis L M, Richens A
Br J Clin Pharmacol. 1986 May;21(5):511-4. doi: 10.1111/j.1365-2125.1986.tb02833.x.
The pharmacokinetics of antipyrine were examined after oral and intravenous administration to 20 epileptic subjects receiving antiepileptic drug therapy. Bioavailability was essentially complete (mean bioavailability 101.2% +/- 14.4 (s.d.] indicating that even in enzyme induced subjects, antipyrine behaves as a restrictively eliminated compound with negligible presystemic elimination in the gut or liver. Of the generally used measures of enzyme induction (oral clearance, oral half-life and intravenous half-life) oral clearance was the most closely related to the intravenous clearance of antipyrine (r = 0.919, P less than 0.001). Oral antipyrine administration is an alternative to intravenous administration in epileptic subjects who are enzyme-induced.
对20名接受抗癫痫药物治疗的癫痫患者进行口服和静脉注射安替比林后的药代动力学研究。生物利用度基本完全(平均生物利用度101.2%±14.4(标准差)),表明即使在酶诱导的患者中,安替比林也表现为一种消除受限的化合物,在肠道或肝脏中的首过消除可忽略不计。在常用的酶诱导指标(口服清除率、口服半衰期和静脉半衰期)中,口服清除率与安替比林的静脉清除率相关性最强(r = 0.919,P<0.001)。对于酶诱导的癫痫患者,口服安替比林是静脉注射的一种替代方法。