Clissold S P, Lynch S, Sorkin E M
Drugs. 1987 May;33(5):430-60. doi: 10.2165/00003495-198733050-00002.
Buflomedil hydrochloride is a vasoactive drug with a variety of pharmacodynamic properties. Importantly, it seems to improve nutritional blood flow in ischaemic tissue of patients with peripheral and/or cerebral vascular disease by a combination of pharmacological effects: inhibition of alpha-adrenoceptors, inhibition of platelet aggregation, improved erythrocyte deformability, nonspecific and weak calcium antagonistic effects, and oxygen sparing activity. Therapeutic trials with buflomedil in patients with peripheral vascular diseases have shown that it increases walking distances in those with intermittent claudication and heals trophic lesions and reduces rest pain in many patients with more severe vasculopathies. In open clinical trials a good to very good clinical response was achieved in 57 to 87% of those treated. In comparative studies buflomedil 600 mg/day orally was shown to be significantly superior to placebo and comparable in efficacy to pentoxifylline (oxpentifylline) and naftidrofuryl. In patients with symptoms presumed to be due to cerebrovascular insufficiencies and elderly patients with senile dementia, buflomedil 450 to 600 mg/day alleviated symptoms associated with impairment of cognitive and psychometric function and was significantly superior to placebo and slightly more effective than drugs such as cinnarizine, flunarizine and co-dergocrine mesylate. Overall, buflomedil at dosages of up to 600 mg/day has been very well tolerated and discontinuation of therapy has rarely been necessary. Thus, buflomedil would seem to be a useful adjunct to conservative treatment in patients with mild-to-moderate peripheral vascular disease and/or cerebrovascular insufficiency, and well worth a try in patients with more severe peripheral disease unable to undergo surgery. However, a few well-designed long term studies are needed to fully define its overall place in therapy.
盐酸丁咯地尔是一种具有多种药效学特性的血管活性药物。重要的是,它似乎通过多种药理作用的组合来改善外周和/或脑血管疾病患者缺血组织中的营养性血流:抑制α-肾上腺素能受体、抑制血小板聚集、改善红细胞变形能力、非特异性和微弱的钙拮抗作用以及氧储备活性。在周围血管疾病患者中进行的丁咯地尔治疗试验表明,它能增加间歇性跛行患者的行走距离,治愈营养性病变,并减轻许多患有更严重血管病变患者的静息痛。在开放临床试验中,57%至87%的治疗患者获得了良好至非常好的临床反应。在比较研究中,口服丁咯地尔600毫克/天被证明明显优于安慰剂,疗效与己酮可可碱(氧甲吡嗪)和萘呋胺酯相当。在疑似脑血管供血不足症状的患者和老年痴呆患者中,丁咯地尔450至600毫克/天可缓解与认知和心理测量功能受损相关的症状,明显优于安慰剂,且比桂利嗪、氟桂利嗪和甲磺酸双氢麦角毒碱等药物稍有效。总体而言,丁咯地尔剂量高达600毫克/天耐受性良好,很少需要停药。因此,丁咯地尔似乎是轻度至中度外周血管疾病和/或脑血管供血不足患者保守治疗的有用辅助药物,对于无法接受手术的更严重外周疾病患者也值得一试。然而,需要一些精心设计的长期研究来全面确定其在治疗中的总体地位。