Holmes B, Brogden R N, Heel R C, Speight T M, Avery G S
Drugs. 1984 Jan;27(1):6-44. doi: 10.2165/00003495-198427010-00002.
Flunarizine is a 'selective' calcium entry blocker with a similar chemical structure and pharmacological profile to the related compound, cinnarizine. However, in contrast to cinnarizine it has a long plasma half-life and need only be given once a day. The majority of therapeutic trials in the prophylaxis of migraine, occlusive peripheral vascular disease and vertigo of central or peripheral origin have been placebo-controlled, and have shown that the drug produces significantly greater beneficial effects than placebo as evaluated by subjective and objective criteria. A small number of comparative studies have shown flunarizine to be at least as effective as pizotifen in migraine prophylaxis, and in a longer term study as effective as cinnarizine in vertigo of central origin. However, it has not been compared with other drugs which may be useful in these areas, such as methysergide in migraine prophylaxis, some antihistamines or phenothiazines in vertigo, or (understandably at this stage of its evolution) with surgical revascularisation in severe occlusive peripheral vascular disease. In preliminary placebo-controlled studies there was some evidence that flunarizine may improve impaired cognitive function in patients with cerebrovascular disorders, but such findings need further confirmation in additional carefully conducted studies. With a very long half-life, flunarizine may be given once daily; and drowsiness, the main side effect, can be minimised by taking the daily dose in the evening. Thus, it appears that flunarizine will offer a useful alternative in some therapeutic areas that can be difficult to manage with previously available therapy. However, a definitive statement on its relative place in therapy of such conditions must await a few well-controlled comparative studies.
氟桂利嗪是一种“选择性”钙通道阻滞剂，其化学结构和药理特性与相关化合物桂利嗪相似。然而，与桂利嗪不同的是，它的血浆半衰期长，每天只需给药一次。在偏头痛、闭塞性外周血管疾病以及中枢性或外周性眩晕预防的大多数治疗试验中，均以安慰剂作为对照，结果表明，根据主观和客观标准评估，该药物产生的有益效果明显优于安慰剂。少数比较研究表明，在偏头痛预防方面，氟桂利嗪至少与苯噻啶一样有效；在一项长期研究中，在中枢性眩晕治疗方面，其效果与桂利嗪相当。然而，尚未将其与这些领域可能有用的其他药物进行比较，如偏头痛预防中的麦角新碱、眩晕治疗中的一些抗组胺药或吩噻嗪类药物，或者（在其发展的现阶段可以理解）与严重闭塞性外周血管疾病的手术血管重建术进行比较。在初步的安慰剂对照研究中，有证据表明氟桂利嗪可能改善脑血管疾病患者受损的认知功能，但这些发现需要在更多精心开展的研究中进一步证实。由于半衰期很长，氟桂利嗪可以每天给药一次；嗜睡是主要的副作用，通过在晚上服用每日剂量可以将其降至最低。因此，在一些用先前可用疗法难以处理的治疗领域，氟桂利嗪似乎将提供一种有用的替代药物。然而，关于其在这些病症治疗中相对地位的确切结论必须等待一些严格对照的比较研究。
