Flores-Runk P, Raasch R H
School of Pharmacy, University of North Carolina, Chapel Hill 27599.
Ann Pharmacother. 1993 Sep;27(9):1090-8. doi: 10.1177/106002809302700915.
To review the pharmacology, pharmacokinetics, clinical efficacy, and toxicity of ticlopidine. Comparisons with other antiplatelet agents are presented, with an emphasis on efficacy, and a recommendation is provided regarding ticlopidine's place in therapy.
A MEDLINE literature retrieval of English-language journal articles from 1987 to January 1993 and references identified from bibliographies of review articles and clinical trials.
Randomized, blind, controlled studies of ticlopidine and other antiplatelet agents were preferentially selected.
Clinical trials were reviewed in terms of study design, efficacy results, and toxicity.
Ticlopidine is a new antiplatelet agent with a distinct mechanism of action. In the largest trial of the drug for the prevention of stroke, it was found to be more effective than aspirin in reducing the risk of stroke or death. Clinical trials have also shown ticlopidine to decrease the rate of vascular death and myocardial infarction in patients with unstable angina, and to maintain venous graft patency after coronary artery bypass grafting. The use of ticlopidine in diabetic microangiopathy and peripheral vascular disease appears promising, but further studies are needed. Adverse reactions most commonly reported with ticlopidine are gastrointestinal complaints; the most severe reaction is transient neutropenia, which is seen in approximately 2.3 percent of patients and is severe in nearly 1 percent.
Ticlopidine is a reasonable alternative for use in preventing stroke among patients unable to take aspirin or those who do not benefit from aspirin therapy. Its use as first-line therapy is limited by its high cost and the occurrence of hematologic adverse effects.
综述噻氯匹定的药理学、药代动力学、临床疗效及毒性。与其他抗血小板药物进行比较,重点在于疗效,并就噻氯匹定在治疗中的地位提出建议。
检索1987年至1993年1月的英文期刊文章的MEDLINE文献,并从综述文章和临床试验的参考文献中确定相关文献。
优先选择噻氯匹定和其他抗血小板药物的随机、盲法、对照研究。
根据研究设计、疗效结果和毒性对临床试验进行综述。
噻氯匹定是一种作用机制独特的新型抗血小板药物。在该药物预防中风的最大规模试验中,发现其在降低中风或死亡风险方面比阿司匹林更有效。临床试验还表明,噻氯匹定可降低不稳定型心绞痛患者的血管性死亡和心肌梗死发生率,并在冠状动脉搭桥术后维持静脉移植物通畅。噻氯匹定用于糖尿病微血管病变和周围血管疾病似乎很有前景,但还需要进一步研究。噻氯匹定最常报告的不良反应是胃肠道不适;最严重的反应是短暂性中性粒细胞减少,约2.3%的患者会出现,近1%的患者症状严重。
对于不能服用阿司匹林或从阿司匹林治疗中未获益的患者,噻氯匹定是预防中风的合理替代药物。其作为一线治疗的应用受到高成本和血液学不良反应发生的限制。