Elliott H L, Meredith P A
Department of Medicine and Therapeutics, Stobhill General Hospital, Glasgow, UK.
Postgrad Med J. 1991;67 Suppl 3:S20-3.
By comparison with other calcium antagonist drugs, amlodipine has unique pharmacokinetic properties that are probably attributable to its chemical structure and positive ionic charge at physiological pH. Thus, amlodipine undergoes gradual absorption from the gastro-intestinal tract and is widely distributed throughout body tissues. It is cleared only slowly by metabolism in the liver and so has a long elimination half-life, which makes it suitable for single daily dosing. During steady-state administration there are only small peak-to-trough variations in plasma drug levels and in clinical use these pharmacokinetic properties appear to be associated with a smoother pharmacodynamic effect and a reduced incidence of (early) vasodilator side effects.
与其他钙拮抗剂药物相比，氨氯地平具有独特的药代动力学特性，这可能归因于其化学结构以及在生理pH值下的正离子电荷。因此，氨氯地平从胃肠道逐渐吸收，并广泛分布于全身组织。它仅通过肝脏代谢缓慢清除，因此消除半衰期长，这使其适合每日单次给药。在稳态给药期间，血浆药物水平仅存在小的峰谷波动，在临床应用中，这些药代动力学特性似乎与更平稳的药效学效应以及（早期）血管扩张剂副作用发生率降低相关。
