Zwar Nicholas, Richmond Robyn
University of New South Wales.
Aust Fam Physician. 2002 May;31(5):443-7.
Originally developed as an antidepressant, bupropion hydrochloride is a selective re-uptake inhibitor of dopamine and noradrenalin which was found to reduce nicotine withdrawal symptoms and the urge to smoke. Bupropion came onto the Australian market in November 2000 as a 150 mg sustained release preparation to be used as an aid to smoking cessation in combination with counselling. Following the PBS listing in February 2001, there was a dramatic increase in prescribing, and considerable public and professional attention focused on this drug.
This review summarises the evidence on how bupropion sustained release (SR) works, its contraindications and risks, adverse effects, studies on efficacy and place in smoking cessation pharmacotherapy.
Bupropion SR is a useful oral and non-nicotine form of pharmacotherapy for smoking cessation. Efficacy has been demonstrated in two key published trials. In one of these trials efficacy was superior to nicotine patch. There is also evidence of efficacy in patients with mild to moderate chronic obstructive pulmonary disease. Bupropion SR is contraindicated in a number of conditions where there is an increased risk of seizures. This includes patients with a current seizure disorder or any history of seizures. It must not be used concurrently with monoamine oxidase inhibitors and interacts with medications which can lower the seizure threshold. Minor adverse effects such as insomnia, headache, dry mouth and nausea are common. Serious adverse effects are rare but include seizures (risk of 1/1000) and hypersensitivity reactions. The latter can manifest as skin rash and a serum sickness-like reaction.
盐酸安非他酮最初作为一种抗抑郁药开发，是一种多巴胺和去甲肾上腺素的选择性再摄取抑制剂，后来发现它可减轻尼古丁戒断症状和吸烟欲望。安非他酮于2000年11月以150毫克缓释制剂的形式进入澳大利亚市场，用于辅助戒烟并结合咨询服务。在2001年2月被列入澳大利亚药品福利计划（PBS）之后，其处方量急剧增加，引起了公众和专业人士的广泛关注。
本综述总结了关于安非他酮缓释剂（SR）的作用机制、禁忌证和风险、不良反应、疗效研究以及在戒烟药物治疗中的地位的证据。
安非他酮SR是一种用于戒烟的有用的口服非尼古丁药物疗法。在两项关键的已发表试验中已证明其疗效。在其中一项试验中，其疗效优于尼古丁贴片。也有证据表明其对轻度至中度慢性阻塞性肺疾病患者有效。安非他酮SR在一些癫痫发作风险增加的情况下是禁忌的。这包括目前患有癫痫症或有任何癫痫病史的患者。它绝不能与单胺氧化酶抑制剂同时使用，并且会与可降低癫痫阈值的药物相互作用。常见的轻微不良反应如失眠、头痛、口干和恶心。严重不良反应很少见，但包括癫痫发作（风险为1/1000）和过敏反应。后者可表现为皮疹和血清病样反应。
