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西沙必利(Cisapride,商品名普瑞博思)是新一代全胃肠道促动力药。现就其临床应用情况作一概述如下。 1 药代动力学及作用机理 1.1 药代动力学:西沙必利口服吸收迅速彻底,1～2小时内血药浓度达峰值,半衰期为10小时左右,在肝病患者及一些老年人,半衰期可能延长。经氧化脱烃基和芳香族的羟基化作用代谢,几乎全部的代谢产物近似均等地经粪便、尿排泄。在肾功能不全时,其排出无明显改变。口服给药的绝对生物利用度约40％,广泛地与血浆蛋白结合(97.5％),其血药浓度随口服剂量(5～20mg)成比例增加。药代动力学和稳定血浆浓度与治疗持续时间无关。
Cisapride (brand name Puri Booz) is a new generation of total gastrointestinal motility drug. Now the clinical application of a summary is as follows. 1 Pharmacokinetics and mechanism of action 1.1 Pharmacokinetics: cisapride oral absorption quickly and thoroughly, within 1 to 2 hours of peak plasma concentration, half-life of 10 hours or so, in patients with liver disease and some elderly, the half-life may be extended . Metabolized by oxidative dehydroxylation and aromatic hydroxylation, almost all of the metabolites are excreted approximately excreta and urine approximately equally. In renal insufficiency, its discharge no significant change. The absolute bioavailability of oral administration is about 40%, broadly associated with plasma proteins (97.5%) and its plasma concentration increases proportionally with oral dose (5-20 mg). Pharmacokinetics and stable plasma concentrations have nothing to do with the duration of treatment.