Amlodipine is a dihydropyridine calcium antagonist drug with distinctive pharmacokinetic characteristics which appear to be attributable to a high degree of ionisation. Following oral administration, bioavailability is 60 to 65% and plasma concentrations rise gradually to peak 6 to 8h after administration. Amlodipine is extensively metabolised in the liver (but there is no significant presystemic or first-pass metabolism) and is slowly cleared with a terminal elimination half-life of 40 to 50h. Volume of distribution is large (21 L/kg) and there is a high degree of protein binding (98%). There is some evidence that age, severe hepatic impairment and severe renal impairment influence the pharmacokinetic profile leading to higher plasma concentrations and longer half-lives. There is no evidence of pharmacokinetic drug interactions. Amlodipine shows linear dose-related pharmacokinetic characteristics and, at steady-state, there are relatively small fluctuations in plasma concentrations across a dosage interval. Thus, although structurally related to other dihydropyridine derivatives, amlodipine displays significantly different pharmacokinetic characteristics and is suitable for administration in a single daily dose.

译文

氨氯地平是一种二氢吡啶类钙拮抗剂药物,具有独特的药代动力学特征,似乎归因于高度电离。口服给药后,生物利用度为60至65%,血浆浓度在给药后6至8小时逐渐升高至峰值。氨氯地平在肝脏中广泛代谢 (但没有明显的前代谢或首过代谢),并缓慢清除,最终消除半衰期为40至50小时。分布的体积很大 (21 l/kg) 并且存在高度的蛋白质结合 (98%)。有一些证据表明,年龄,严重的肝损害和严重的肾损害会影响药代动力学特征,从而导致更高的血浆浓度和更长的半衰期。没有药代动力学药物相互作用的证据。氨氯地平显示出线性剂量相关的药代动力学特征,并且在稳态下,在整个剂量间隔内血浆浓度的波动相对较小。因此,尽管与其他二氢吡啶衍生物在结构上相关,但氨氯地平显示出明显不同的药代动力学特征,并且适合以每日单一剂量给药。

+1
+2
100研值 100研值 ¥99课程
检索文献一次
下载文献一次

去下载>

成功解锁2个技能,为你点赞

《SCI写作十大必备语法》
解决你的SCI语法难题!

技能熟练度+1

视频课《玩转文献检索》
让你成为检索达人!

恭喜完成新手挑战

手机微信扫一扫,添加好友领取

免费领《Endnote文献管理工具+教程》

微信扫码, 免费领取

手机登录

获取验证码
登录