Differential effect of isoniazid on triazolam oxidation and oxazepam conjugation.
Differential effect of isoniazid on triazolam oxidation and oxazepam conjugation.
复制标题
异烟肼对三唑仑氧化和奥沙西泮结合的不同影响。
DOI：
10.1111/j.1365-2125.1983.tb02256.x
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发表时间：
1983
影响因子：
3.4
通讯作者：
Knüchel,M
中科院分区：
文献类型：
--
作者：
Ochs,HR;Greenblatt,DJ;Knüchel,M
健康受试者单次服用三唑仑(0.5 mg)或奥沙西潘(30 Mg)两次，一次在对照组，另一次在异烟肼(INH)碱联合给药期间，每天180 mg。INH合用延长了三唑仑的半衰期(3.3vs2.5h，P<0.05)，增加了曲线下总面积(38.6vs26.5ngml-1h，P<0.01)，与降低口腔表观清除率(3.9vs6.8mlmin-1 kg-1，比P<0.1减少0.05)一致。异烟肼合用对奥沙西潘的药动学无影响。异丙肾上腺素损害三唑仑的肝微体氧化，导致首过肝抽提物减少，半衰期延长。但异烟肼对奥沙西潘的结合无影响。
Healthy volunteers received a single dose of triazolam (0.5 mg) or oxazepam (30 mg) on two occasions, once in the control state and again during coadministration of isoniazid (INH) base, 180 mg day. INH coadministration prolonged triazolam half‐life (3.3 vs 2.5 h, P less than 0.05) and increased total area under the curve (38.6 vs 26.5 ng ml‐ 1 h, P less than 0.01) consistent with a reduction of apparent oral clearance (3.9 vs 6.8 ml min‐1 kg‐1, 0.05 less than P less than 0.1). INH coadministration had no influence on the kinetics of oxazepam. INH impairs hepatic microsomal oxidation of triazolam, leading to reduced first‐pass hepatic extraction as well as prolonged half‐life. However INH had no influence on oxazepam conjugation.