临床药物动力学H1-receptor拮抗剂(抗组胺药)。
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Paton DM,韦伯斯特博士
临床药物动力学H1-receptor拮抗剂(抗组胺药)。
Pharmacokinet。1985; 11 - 12月10 (6):477 - 97。
- PubMed ID
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2866055 (在PubMed]
- 文摘
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本文综述临床药代动力学数据H1-receptor拮抗剂,通常被称为抗组胺药。尽管被广泛使用在较长时间内,相对较少的药代动力学数据可用于许多这样的药物。许多H1-receptor拮抗剂已经化验主要使用等方法。这些也通常代谢物大或小的程度来衡量。因此,这些数据的解释是复杂的。口服后H1-receptor拮抗剂糖浆或平板配方,血浆浓度峰值通常2到3小时后观察。生物利用度并没有被广泛研究,但大约是0.34扑尔敏、苯海拉明0.40到0.60,0.25异丙嗪。beplayapp这些药物在肝脏代谢,这是非常广泛的在某些情况下(例如,赛庚啶和terfenadine)。全身间隙成年人一般在5到12毫升/分钟/公斤(阿司咪唑、溴苯那敏、扑尔敏、苯海拉明、羟嗪、异丙嗪和曲普立啶),而他们的消除半衰期从约3小时到18天左右(桂利嗪约3小时;beplayapp苯海拉明约4小时;beplayapp 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.