拉莫三嗪临床药物动力学。

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Rambeck B,狼P

拉莫三嗪临床药物动力学。

Pharmacokinet。1993; 12月25 (6):433 - 43。doi: 10.2165 / 00003088-199325060-00003。

PubMed ID

8119045 (在PubMed

]

文摘

拉莫三嗪是一种新型的抗癫痫剂化学无关任何建立药物使用。这种药物可以估计在生物体液通过高效液相色谱法和免疫测定。快速吸收,达到峰浓度postdose大约3小时内。口服生物利用度的形成大约是98%。血浆浓度时间曲线下的面积表示dose-linear药物动力学。血浆蛋白结合的程度是56%。唾液浓度46%的血浆浓度。拉莫三嗪的浓度在大脑中类似于等离子体的总浓度。拉莫三嗪展览一阶线性动力学长期执政期间。43 87%的剂量是尿液中恢复,主要是葡糖苷酸代谢物。 Mean half-lives of lamotrigine in healthy volunteers (single and multiple doses) as well as in epileptic patients receiving lamotrigine monotherapy range from 22.8 to 37.4 hours. Enzyme-inducing antiepileptic drugs such as phenytoin, phenobarbital (phenobarbitone) or carbamazepine reduce the half-life of lamotrigine (to mean values of 13.5 to 15 hours), whereas valproic acid increases the half-life of the drug (to mean values of 48.3 to 59 hours). Lamotrigine itself does not influence the plasma concentrations of concomitant antiepileptic drugs, except for causing an increase in concentrations of carbamazepine-10,11-epoxide, the main metabolite of carbamazepine. Other observations indicate that the interaction of carbamazepine and lamotrigine may be primarily pharmacodynamic rather than pharmacokinetic. Usual dosages of lamotrigine range from 50 to 400 mg/day depending on an enzyme-inducing or -inhibiting comedication. Therapeutic plasma concentrations of the drug are not known, but a putative therapeutic range of 1 to 4 mg/L has been proposed. Some patients have tolerated concentrations > 10 mg/L with benefit and without clinical toxicity. The value of measuring the concentrations of lamotrigine in helping to optimise the dosage or reduce the likelihood of adverse effects has not been established. Safety data from several large studies indicate that the incidence of adverse effects of the drug is low and that unwanted effects are reversible.

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药物

拉莫三嗪