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Bepridil 盐酸盐是一种钙离子拮抗剂,首先在法国制成并用于治疗心绞痛患者。该药与其它钙离子拮抗剂在结构上及药物动力学特征上均不同。Bepridil 与其它三种钙离子拮抗剂(异搏停、硝苯吡啶及地尔硫(艹卓))的重要不同点有:(1)Bepridil 的半衰期接近两天,为其它药的5~6倍时间;(2)它的蛋白结合程度(游离部份仅为0.23%)远远超过其它药;致使(3)其血浆清除率亦显著低于其它三种药。因此该药有最高的口服利用度。化学结构Bepridil Hcl,β-[(2-methylpropoxy)-methyl]-N-phenyl-N-(phenylmethyl)-1-
Bepridil hydrochloride is a calcium ion antagonist, first made in France and used to treat angina patients. The drug differs from other calcium antagonists in both structural and pharmacokinetic characteristics. The important differences between Bepridil and the other three calcium antagonists (Verapamil, Nifedipine and Diltiazem) are: (1) Bepridil has a half-life of nearly two to six days, which is five to six times that of other drugs Time; (2) its degree of protein binding (only 0.23% of the free fraction) far exceeds that of other drugs; resulting in (3) its plasma clearance rate is also significantly lower than the other three drugs. Therefore, the drug has the highest oral availability. Chemical Structure Bepridil Hcl, β - [(2-methylpropoxy) -methyl] -N-phenyl-N- (phenylmethyl) -1-