Singlas E, Martre H
Ann Cardiol Angeiol (Paris). 1983 Dec;32(8):503-9.
Molsidomine is well absorbed by the gastro-intestinal tract and is taken up by the liver during the first passage. Its bioavailability is 60 per cent. Digestive or sublingual absorption is rapid: maximal plasma concentrations are obtained 0.5 to 1.0 hours after administration. Molsidomine is minimally bound by plasma proteins and is distributed in a volume of 1 litre/kg. The excretion is essentially extrarenal: less than 2 per cent of the administered dose is excreted in the form of unchanged molsidomine. Molsidomine is metabolized in the liver to two pharmacologically active metabolites which spontaneously and rapidly breakdown into inactive metabolites which are excreted by the kidneys. The plasma half-life of molsidomine is 1 to 2 hours: it is not modified in patients with renal failure, but it is prolonged in patients with hepatic failure. The kinetics are linear and independent of the route of administration and the dose. There is a correlation between the plasma concentration and the pharmacological effect: the minimal effective concentration is about 5 ng/ml. At the usual dose of 2 mg three times a day, there is no accumulation of the drug.
莫西多明经胃肠道吸收良好，首次通过肝脏时被摄取。其生物利用度为60%。消化或舌下吸收迅速：给药后0.5至1.0小时达到血浆最大浓度。莫西多明与血浆蛋白的结合极少，分布容积为1升/千克。排泄主要通过肾外途径：给药剂量中不到2%以原形莫西多明的形式排泄。莫西多明在肝脏中代谢为两种具有药理活性的代谢产物，这些代谢产物会自发且迅速分解为无活性的代谢产物，经肾脏排泄。莫西多明的血浆半衰期为1至2小时：在肾衰竭患者中不变，但在肝功能衰竭患者中会延长。其动力学呈线性，与给药途径和剂量无关。血浆浓度与药理效应之间存在相关性：最小有效浓度约为5纳克/毫升。在通常每日三次、每次2毫克的剂量下，该药物无蓄积现象。
