口服维拉帕米疗法对安替比林清除率的影响。
The effect of oral verapamil therapy on antipyrine clearance.
作者信息
Rumiantsev D O, Piotrovskii V K, Riabokon O S, Slastnikova I D, Kokurina E V, Metelitsa V I
出版信息
Br J Clin Pharmacol. 1986 Nov;22(5):606-9. doi: 10.1111/j.1365-2125.1986.tb02942.x.
Abstract
The influence of chronic verapamil treatment on antipyrine elimination was studied in eight angina patients. Antipyrine half-life (mean +/- s.d.) was 13.1 +/- 1.15 h at the start of therapy and 16.6 +/- 3.05 h (P less than 0.05) during chronic oral administration of verapamil (80-120 mg four or three times daily for 4 to 7 months). There was a significant decrease in antipyrine clearance (mean +/- s.d, 43.2 +/- 16.8 ml min-1 vs 28.7 +/- 16.6 ml min-1, P less than 0.01) while the change of distribution volume was insignificant. Verapamil elimination was also found to be impaired after chronic dosing as compared to single administration. Half-lives measured from the concentration vs time and urinary excretion rate vs time curves were both prolonged and oral clearance was decreased. Our results suggest that the inhibition of drug-metabolizing enzymes accounts for the impairment of verapamil elimination on chronic administration.
摘要
研究了八名心绞痛患者长期服用维拉帕米对安替比林消除的影响。治疗开始时安替比林半衰期（均值±标准差）为13.1±1.15小时，在长期口服维拉帕米（80 - 120毫克，每日三或四次，共4至7个月）期间为16.6±3.05小时（P<0.05）。安替比林清除率显著降低（均值±标准差，43.2±16.8毫升/分钟对28.7±16.6毫升/分钟，P<0.01），而分布容积变化不显著。与单次给药相比，长期给药后维拉帕米的消除也受到损害。从浓度对时间曲线和尿排泄率对时间曲线测得的半衰期均延长，口服清除率降低。我们的结果表明，药物代谢酶的抑制是长期给药时维拉帕米消除受损的原因。
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