Soto J, Sacristan J A, Alsar M J
Clinical Pharmacology Unit, Hospital Santa Cruz, Liencres-Cantabria, Spain.
Ther Drug Monit. 1994 Feb;16(1):49-52. doi: 10.1097/00007691-199402000-00008.
On the basis of reports that diltiazem may bind to the hepatic microsomal enzymes and inhibits the metabolism of some co-administered drugs, and to determine the effects of diltiazem on theophylline pharmacokinetics in patients with bronchospastic airway disease, we have investigated the effect of a 180-mg daily dose of oral diltiazem during 5 days on theophylline clearance in eight patients with that disease. Theophylline half-life increased 24%, from 5.7 +/- 1 to 7.5 +/- 1.8 h (p < 0.05), and total body theophylline clearance showed a decrease of 22%, from 87.3 +/- 20 to 68.3 +/- 18.6 ml/min (p < 0.05) after diltiazem therapy. The apparent volume of distribution was unchanged. This reduction in theophylline clearance is likely produced by inhibition of its metabolism by diltiazem. A clinically important drug interaction may occur with theophylline when diltiazem therapy is given concurrently in patients with bronchospastic airway disease.
基于地尔硫䓬可能与肝微粒体酶结合并抑制某些合用药物代谢的报道，为确定地尔硫䓬对支气管痉挛性气道疾病患者茶碱药代动力学的影响，我们研究了8例该疾病患者连续5天每日口服180 mg地尔硫䓬对茶碱清除率的影响。地尔硫䓬治疗后，茶碱半衰期增加了24%，从5.7±1小时增至7.5±1.8小时（p<0.05），全身茶碱清除率降低了22%，从87.3±20降至68.3±18.6 ml/分钟（p<0.05）。分布容积未发生变化。茶碱清除率的降低可能是由于地尔硫䓬抑制了其代谢。在支气管痉挛性气道疾病患者中同时给予地尔硫䓬治疗时，可能会与茶碱发生具有临床意义的药物相互作用。
