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西咪替丁给药方案综述。多次口服给药后可能的药物蓄积。

Dosage regimen of cimetidine reviewed. Possible drug accumulation after multiple oral doses.

作者信息

Prandota J, Smith I J, Wilson J T

机构信息

J. Korczak Memorial Children's Hospital, Wrocław, Poland.

出版信息

Eur J Clin Pharmacol. 1988;34(6):539-42. doi: 10.1007/BF00615214.

Abstract

The doses of cimetidine recommended differ in children, especially those with cystic fibrosis. These dosage regimens were derived from single-dose pharmacokinetic studies of the drug. Some authors showed, however, that after administration of repeated oral doses of cimetidine in healthy adults and children with cystic fibrosis, the elimination half-life of the drug was markedly prolonged. In view of the ability of cimetidine to inhibit metabolism of other drugs, it is suggested that the parent compound and/or it is metabolite(s) may inhibit its own metabolism during a prolonged course of treatment. Enterohepatic recirculation of the drug and/or its metabolite(s) may also contribute to prolongation of its elimination. One should therefore be cautious in using single-dose pharmacokinetic parameters to calculate repeated dose regimens and expected plasma steady-state concentrations.

摘要

西咪替丁的推荐剂量在儿童中有所不同,尤其是患有囊性纤维化的儿童。这些给药方案源自该药物的单剂量药代动力学研究。然而,一些作者表明,在健康成年人和患有囊性纤维化的儿童中多次口服西咪替丁后,该药物的消除半衰期显著延长。鉴于西咪替丁具有抑制其他药物代谢的能力,有人提出母体化合物和/或其代谢物可能在长期治疗过程中抑制自身代谢。该药物和/或其代谢物的肠肝循环也可能导致其消除时间延长。因此,在使用单剂量药代动力学参数来计算重复给药方案和预期的血浆稳态浓度时应谨慎。

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