h1受体拮抗剂(抗组胺药)的临床药代动力学。
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佩顿DM，韦伯斯特DR
h1受体拮抗剂(抗组胺药)的临床药代动力学。
临床药物通讯。1985 11 - 12;10(6):477-97。
- PubMed ID
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2866055 (查看PubMed］
- 摘要
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本文综述了h1受体拮抗剂(通常称为抗组胺药)的临床药代动力学数据。尽管这些药物在较长时期内被广泛使用，但其中许多药物的药代动力学数据相对较少。许多h1受体拮抗剂已主要使用放射免疫分析法进行测定。这些方法通常也可以或多或少地测量代谢物。因此，对这些数据的解释是复杂的。口服糖浆或片剂等h1受体拮抗剂后，通常在2 - 3小时后观察到血药浓度峰值。生物利用度尚未得到广泛研究，但氯苯那敏约为0.34，苯海拉明约为0.40 - 0.60，异丙嗪约为0.25。这些药物中的大多数在肝脏中代谢，在某些情况下代谢非常广泛(如赛庚啶和特非那定)。成人的全身清除率一般在5至12毫升/分钟/公斤之间(阿司美唑、溴苯那敏、氯苯那敏、苯海拉明、羟嗪、异丙嗪和三丙啶)，而它们的消除半衰期约为3小时至18天[朱纳嗪约为3小时;苯海拉明约4小时; promethazine 10 to 14 hours; chlorpheniramine 14 to 25 hours; hydroxyzine about 20 hours; brompheniramine about 25 hours; astemizole and its active metabolites about 7 to 20 days (after long term administration); flunarizine about 18 to 20 days]. They also have relatively large apparent volumes of distribution in excess of 4 L/kg. In children, the elimination half-lives of chlorpheniramine and hydroxyzine are shorter than in adults. In patients with alcohol-related liver disease, the elimination half-life of diphenhydramine was increased from 9 to 15 hours, while in patients with chronic renal disease that of chlorpheniramine was very greatly prolonged. Little, if any, published information is available on the pharmacokinetics of these drugs in neonates, pregnancy or during lactation. The relatively long half-lives of a number of the older H1-receptor antagonists such as brompheniramine, chlorpheniramine and hydroxyzine suggest that they can be administered to adults once daily.