acamprosate的临床药物动力学。

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洛Saivin年代,T, Chabac年代,波特,杜宾P, Houin G

acamprosate的临床药物动力学。

Pharmacokinet。1998年11月,35 (5):331 - 45。doi: 10.2165 / 00003088-199835050-00001。

PubMed ID

9839087 (在PubMed

]

文摘

Acamprosate是一种新的精神药物用于治疗酒精(乙醇)的依赖。最近的研究表明,acamprosate能抑制与兴奋性氨基酸的神经兴奋过度。可用333毫克肠衣的平板电脑,推荐剂量为1.3克/天患者体重< 60公斤,2 g /天患者体重>或= 60公斤。治疗高剂量强度平板电脑2 x 500毫克每日两次是bioequivalent治疗2 x 333毫克每天3次给药方案。通过paracellular Acamprosate吸收胃肠道的路线。口服后吸收迅速,但有限。在稳态,acamprosate中等体积分布的约20 l。beplayappAcamprosate不是蛋白质绑定或代谢。一半的消除acamprosate发生不变acetyl-homotaurine尿液,另一半可能消除胆汁排泄。肠溶平板电脑的管理与终端显示一个触发器机制消除半衰期10倍高于静脉输液后3小时半衰期报道。 During repeated oral administration of 666 mg 3 times daily, steady-state is reached after 5 to 7 days and leads to plasma concentrations ranging from 370 to 650 micrograms/L. The pharmacokinetics of acamprosate administered as an enteric-coated tablets are time- and dose-independent, and its accumulation ratio is about 2.4 at steady-state. Acamprosate disposition does not differ between males and females. The pharmacokinetics of acamprosate are not modified in patients with hepatic insufficiency or chronic alcoholism. In contrast, renal insufficiency influences the elimination of acamprosate and it is, therefore, contraindicated under such circumstances. Interaction studies have confirmed that when acamprosate is concomitantly administered with food, the amount absorbed is decreased. When combined with diazepam, disulfiram or alcohol, the pharmacokinetic disposition of acamprosate is not modified. Acamprosate does not influence the kinetics of diazepam, alcohol or imipramine and its metabolite desipramine.

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药物

Acamprosate