Walton T, Symes L R
Department of Pharmacy, Charleston Area Medical Center, WV 25326.
Clin Pharm. 1993 Apr;12(4):261-75.
The chemistry, pharmacology, pharmacokinetics, clinical uses, adverse effects, and dosage of felodipine and isradipine are reviewed. Felodipine and isradipine are new calcium-channel-blocking agents with FDA-approved labeling for use in the treatment of essential hypertension. Both agents are members of the dihydropyridine class of calcium antagonists, which also includes nifedipine and nicardipine. Like those agents, felodipine and isradipine affect blood pressure by producing peripheral vasodilation. Felodipine and isradipine undergo extensive first-pass metabolism; their bioavailabilities are approximately 15% and 17%, respectively. The drugs are highly protein bound but do not affect serum digoxin concentrations. Anticonvulsants may reduce the elimination half-life of felodipine. Felodipine and isradipine are effective antihypertensive agents when used alone or in combination with beta blockers or diuretics. Both agents have shown some benefit in the treatment of angina pectoris in limited studies. Clinical data do not support the use of either agent for the treatment of congestive heart failure or Raynaud's phenomenon. Felodipine and isradipine have similar adverse-effect profiles, and their adverse effects resemble those of other agents in the class. Common adverse effects are peripheral edema and increased heart rate. The initial dosage of isradipine for the treatment of hypertension is 2.5 mg twice daily. Felodipine should be started at a dosage of 5 mg once daily. Felodipine and isradipine are effective antihypertensive drugs but have not demonstrated clear advantages over other dihydropyridine calcium-channel blockers.
本文综述了非洛地平与伊拉地平的化学性质、药理学、药代动力学、临床应用、不良反应及剂量。非洛地平与伊拉地平是新型钙通道阻滞剂，其药品说明书已获美国食品药品监督管理局（FDA）批准，用于治疗原发性高血压。这两种药物均属于二氢吡啶类钙拮抗剂，该类还包括硝苯地平和尼卡地平。与这些药物一样，非洛地平与伊拉地平通过外周血管舒张来影响血压。非洛地平与伊拉地平均经历广泛的首过代谢；其生物利用度分别约为15%和17%。这些药物与蛋白质高度结合，但不影响血清地高辛浓度。抗惊厥药可能会缩短非洛地平的消除半衰期。非洛地平与伊拉地平单独使用或与β受体阻滞剂或利尿剂联合使用时均为有效的抗高血压药物。在有限的研究中，这两种药物在治疗心绞痛方面均显示出一定益处。临床数据不支持使用这两种药物治疗充血性心力衰竭或雷诺现象。非洛地平与伊拉地平的不良反应谱相似，且它们的不良反应与该类中的其他药物相似。常见的不良反应是外周水肿和心率加快。伊拉地平治疗高血压的初始剂量为每日两次，每次2.5mg。非洛地平应从每日一次，每次5mg开始服用。非洛地平与伊拉地平是有效的抗高血压药物，但尚未证明比其他二氢吡啶类钙通道阻滞剂有明显优势。
