Booth Kemper, Clements Jennifer N
Presbyterian College School of Pharmacy, Clinton, SC, USA.
Department of Pharmacy Practice, Presbyterian College, Clinton, SC, USA.
J Pharm Technol. 2016 Jun;32(3):125-132. doi: 10.1177/8755122515624220. Epub 2016 Jan 11.
The pharmacology, pharmacokinetics, efficacy, and safety of bupropion plus naltrexone for weight loss were reviewed. A MEDLINE search (1970 to November 2015) was conducted for English-language articles using specific MESH terms. Published Phase 3 clinical trials with primary endpoints related to weight loss were included and critiqued in this review. Five trials were retrieved and reviewed regarding the efficacy and safety of bupropion plus naltrexone among obese and overweight patients. Bupropion is a dopamine/norepinephrine reuptake inhibitor, and naltrexone is an opioid receptor antagonist. The combination of these agents has led to increased weight loss, compared to placebo, among overweight and obese patients with a body mass index (BMI) at or above 30 or BMI at or above 27 with a comorbid condition. The combination of bupropion and naltrexone can produce an average placebo-subtracted weight loss of 4.25% over 56 weeks. Gastrointestinal (ie, nausea, vomiting, constipation) and central nervous system adverse events (ie, headache, dizziness) were commonly reported, and there was a high dropout rate among participants. Bupropion plus naltrexone has demonstrated effective weight loss, in conjunction with lifestyle modifications, among overweight and obese patients with and without comorbidities. Bupropion plus naltrexone has not been studied among special patient populations, such as those with sleep apnea, osteoarthritis, or extreme BMIs. Additional clinical trials and postmarketing data will provide a better understanding of this medication for weight loss.
对安非他酮加纳曲酮用于减肥的药理学、药代动力学、疗效和安全性进行了综述。使用特定医学主题词(MESH)对1970年至2015年11月期间的英文文章进行了MEDLINE检索。纳入了已发表的主要终点与减肥相关的3期临床试验并在本综述中进行了分析。检索并综述了五项关于安非他酮加纳曲酮在肥胖和超重患者中的疗效和安全性的试验。安非他酮是一种多巴胺/去甲肾上腺素再摄取抑制剂,纳曲酮是一种阿片受体拮抗剂。与安慰剂相比,对于体重指数(BMI)等于或高于30或BMI等于或高于27且伴有合并症的超重和肥胖患者,这些药物的组合导致体重减轻增加。安非他酮和纳曲酮的组合在56周内可产生平均比安慰剂多4.25%的体重减轻。常见的胃肠道不良事件(如恶心、呕吐、便秘)和中枢神经系统不良事件(如头痛、头晕)被报告,且参与者中有较高的退出率。安非他酮加纳曲酮在有或无合并症的超重和肥胖患者中,结合生活方式改变已证明能有效减轻体重。安非他酮加纳曲酮尚未在特殊患者群体中进行研究,如患有睡眠呼吸暂停、骨关节炎或极高BMI的患者。更多的临床试验和上市后数据将有助于更好地了解这种减肥药物。