临床唑吡坦的药代学和药效学。治疗的影响。

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萨尔瓦•P,科斯塔J

临床唑吡坦的药代学和药效学。治疗的影响。

Pharmacokinet。1995年9月,29 (3):142 - 53。doi: 10.2165 / 00003088-199529030-00002。

PubMed ID

8521677 (在PubMed

]

文摘

唑吡坦是一个imidazopyridine,不同结构的苯二氮卓类和zopiclone。这是一个强大的镇静剂只有较小的抗焦虑药,myorelaxant和抗惊厥的属性,已被证明是有效的诱导和维持睡眠在成人。现有证据表明,唑吡坦生产没有反弹或咖啡因脱瘾症状,和病人经历了好白天警觉性。唑吡坦10毫克的费用和减少了5毫克的剂量老年人是临床上有效的。在人类中,主要的代谢途径包括氧化、羟基化;所有的代谢物似乎药物活性。唑吡坦的药理作用选择性的结果绑定到中央ω1苯二氮受体亚型。唑吡坦是大约92%与血浆蛋白;唑吡坦的绝对bio-availability约为70%。单20毫克口服剂量后,人类唑吡坦的药代动力学变量的典型值是:血浆浓度峰值的192 - 324微克/ L postdose发生0.75到2.6小时; a terminal elimination half-line of 1.5 to 3.2 hours; and total clearance of 0.24 to 0.27 ml/min/kg. Zolpidem pharmacokinetics are unchanged during multiple-dose treatment. Zolpidem pharmacokinetics are not significantly influenced by gender. Clearance of zolpidem in children is 3 times higher than in young adults, and is lower in very elderly people. There are no significant differences in the pharmacokinetic parameters between various racial groups. Dosage reduction appears to be prudent in patients with renal disease, and caution should be exercised when prescribing zolpidem to elderly patients with hepatic impairment. Coadministration of haloperidol, cimetidine, ranitidine, chlorpromazine, warfarin, digoxin or flumazenil do not alter the pharmacokinetics of zolpidem; flumazenil predictably antagonises the hypnotic effects of zolpidem. Alertness tends to be reduced when cimetidine is combined with zolpidem. Volunteers treated with imipramine plus zolpidem developed anterograde amnesia.

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药物

唑吡坦