Todd P A, Faulds D
Adis International Limited, Auckland, New Zealand.
Drugs. 1992 Aug;44(2):251-77. doi: 10.2165/00003495-199244020-00008.
Felodipine is a vascular-selective, dihydropyridine calcium antagonist previously investigated as a conventional tablet formulation administered twice daily. More recently considerable experience has been gained with an extended release (ER) formulation which has the convenience of once daily administration. Felodipine ER has been well studied in patients with essential hypertension. As monotherapy in mild to moderate essential hypertension, felodipine ER is at least as effective in reducing blood pressure as other calcium antagonists, beta-blockers, diuretics and ACE inhibitors, with some results favouring felodipine ER at a statistically significant level at the dosages used. It is also effective combined with controlled release metoprolol or enalapril in patients with mild to moderate essential hypertension. In patients with more severe forms of essential hypertension uncontrolled by beta-blocker and/or diuretic therapy, felodipine ER was effective as an 'add-on' therapy in placebo-controlled trials, and, at the dosages used, more effective than either sustained release nifedipine or nitrendipine. Felodipine produces effective control of blood pressure without negative effects on cardiac performance. In addition to its antihypertensive action, results suggest that felodipine therapy is associated with significant regression of left ventricular hypertrophy. Furthermore, it appears suitable for use in patients with concomitant diabetes, renal dysfunction or asthma, and is also being investigated for use in patients with congestive heart failure or angina pectoris. Felodipine ER is an effective drug for the treatment of all grades of essential hypertension, and can be used both as monotherapy and in combination with other antihypertensive agents. Further clinical experience should fully establish the long term tolerability of felodipine ER and consequently its place in therapy relative to other accepted antihypertensive drugs. However, with the convenience of once daily administration, felodipine ER is a worthwhile innovation in the treatment of hypertension.
非洛地平是一种血管选择性二氢吡啶类钙拮抗剂，此前曾作为每日服用两次的传统片剂剂型进行研究。最近，一种缓释（ER）剂型积累了大量经验，该剂型方便每日服用一次。非洛地平缓释片已在原发性高血压患者中得到充分研究。作为轻度至中度原发性高血压的单一疗法，非洛地平缓释片在降低血压方面至少与其他钙拮抗剂、β受体阻滞剂、利尿剂和血管紧张素转换酶抑制剂一样有效，在所用剂量下，一些结果在统计学上显著有利于非洛地平缓释片。在轻度至中度原发性高血压患者中，它与控释美托洛尔或依那普利联合使用也有效。在β受体阻滞剂和/或利尿剂治疗无法控制的更严重原发性高血压患者中，在安慰剂对照试验中，非洛地平缓释片作为“附加”疗法有效，并且在所用剂量下，比缓释硝苯地平或尼群地平更有效。非洛地平能有效控制血压，且对心脏功能无负面影响。除了其降压作用外，结果表明非洛地平治疗与左心室肥厚的显著消退有关。此外，它似乎适用于伴有糖尿病、肾功能不全或哮喘的患者，也正在对充血性心力衰竭或心绞痛患者进行研究。非洛地平缓释片是治疗各级原发性高血压的有效药物，可作为单一疗法使用，也可与其他抗高血压药物联合使用。进一步的临床经验应能充分确定非洛地平缓释片的长期耐受性，从而确定其相对于其他公认抗高血压药物在治疗中的地位。然而，由于每日服用一次的便利性，非洛地平缓释片是高血压治疗中一项有价值的创新。
