盐酸安非他酮缓释片戒除烟瘾的初步临床试验

目的:初步评价国产盐酸安非他酮缓释片戒除烟瘾的有效性及安全性。方法:采用随机、双盲、安慰剂平行对照研究。受试者随机分为2组,分别口服盐酸安非他酮缓释片150-300 mg.d-1或安慰剂,疗程4周,观察12周。结果:共入组自愿戒烟者48例,其中盐酸安非他酮组24例,安慰剂组24例。自治疗后1周起,盐酸安非他酮组日吸烟量的减少值均大于安慰剂组(P<0.01)。治疗后4周盐酸安非他酮组戒烟率为29.2%,高于安慰剂组(P<0.05)。盐酸安非他酮组常见的不良反应为:困倦、口干、注意力不集中、腹部不适和乏力。结论:国产盐酸安非他酮缓释片是一种安全有效的戒烟药物,不良反应轻。     

丹栀逍遥丸与安非他酮缓释片戒烟治疗的临床对照研究

目的比较丹栀逍遥丸与安非他酮缓释片戒烟治疗的疗效和安全性。方法自愿戒烟者77例，随机分为丹栀逍遥丸治疗组37例、安非他酮缓释片治疗组40例，在治疗1周后设定目标戒烟日，然后治疗4周，在治疗前及戒烟治疗第4周进行烟草依赖程度评估、呼出气120检测，并评估治疗不良反应，电话随访至24周。结果治疗4周和随访24周时安非他酮缓释片组戒烟率分别为59％、40％，高于丹栀逍遥丸组戒烟率的32％和16％，差异有显著意义（P〈0．05），2组未发现严重的不良反应。结论安非他酮缓释片戒烟治疗的效果优于丹栀逍遥丸，丹栀逍遥丸在戒烟治疗中的作用有待进一步探索。     

盐酸安非他酮缓释片治疗抑郁症的临床试验

目的:评价国产盐酸安非他酮缓释片治疗抑郁症的有效性和安全性。方法:采用随机、双盲、双模拟、阳性药平行对照研究。48例抑郁症患者随机分为试验组24例与对照组24例,分别口服盐酸安非他酮缓释片300mg·d~(-1)或氟西汀20mg·d~(-1),疗程42d,观察汉密尔顿抑郁量表与临床总体印象量表总分变化及药物不良反应等。结果:两组汉密尔顿抑郁量表评分在治疗结束时较基线均显著减少(P＜0．01);试验组与对照组有效率分别为86．4%与73．9%,差异无显著性(P＞0．05)。试验组常见的不良反应为:恶心呕吐、头昏、口干、食欲减退。结论:盐酸安非他酮缓释片治疗抑郁症安全而有效。     

盐酸安非他酮缓释片治疗抑郁症的Ⅱ期临床研究

目的 评价盐酸安非他酮缓释片治疗轻中度抑郁症的临床疗效和安全性。方法 对符合《CCMD》勘抑郁症诊断标准的66例抑郁症患者进行盐酸安非他酮缓释片和氟西汀的对照研究，其中盐酸安非他酮缓释片组34例（300mg／d），氟西汀组32例（20mg／d），共治疗6周。采用汉密尔顿抑郁量表（HAMD），汉密尔顿焦虑量表（HAMA），临床总体评定量表（CGI）评定临床疗效，副反应量表（Tess）评定不良反应。结果经6w治疗后，盐酸安非他酮缓释片治疗总有效率为76．47％，氟西汀组为75．00％，两组比较。差异无显著性（P〉0．05）。两组的HAMD，HAMA评分治疗前后相比较差异有高度显著性（P〈0．01）。不良反应分析，两组药物不良反应的发生率无显著性差异（P〉0．05），常见的不良反应有恶心、口干、头昏、失眠、出汗、食欲减退、便秘等。结论 盐酸安非他酮缓释片治疗抑郁症安全有效。     

国产安非他酮缓释片治疗抑郁症的Ⅱ期临床研究

目的:评价安非他酮治疗抑郁症的疗效和安全性。方法:采用随机、双盲、多中心、平行对照研究。共入组抑郁症患者237例,其中试验组119例,对照组118例,分别口服安非他酮150～450 mg·d-1,氟西汀10～30 mg·d-1。疗程均为6周。用汉密尔顿抑郁量表(HAMD)和临床总体印象量表(CGI)评定疗效,药物不良反应量表(TESS)评定安全性。结果:治疗6周后两组患者HAMD评分较基线均显著降低(P<0．05),总有效率安非他酮组70．69％,氟西汀组74．14％。组间差异无显著性(P>0．05)。不良反应发生率安非他酮组41．4％,氟西汀组44．8％,组间差异无显著性(P>0．05)。结论:安非他酮治疗抑郁症安全有效。     

安非他酮缓释片治疗抑郁症的随机双盲多中心临床试验

目的评价安非他酮缓释片治疗抑郁症的疗效和安全性。方法采用随机、双盲双模拟、多中心、平行对照(氟西汀),为期6 wk。共入组237例,完成232例,其中安非他酮组117例,氟西汀组115例。2组分别服用安非他酮缓释片300 mg.d-1和氟西汀20 mg.d-1治疗。结果治疗6 wk后,安非他酮组和氟西汀组的汉密尔顿抑郁量表(HAMD)总分减分值分别为(12.45±6.85)与(12.63±6.10)分,有效率分别为69.23%与67.83%,临床痊愈率分别为35.04%和45.22%,2组相比差异均无统计学意义(P>0.05)。非劣效性检验显示,安非他酮组疗效非劣于氟西汀组。2组的不良反应发生率分别为52.14%和52.17%,差异无统计学意义(P>0.05)。结论安非他酮缓释片是一种安全有效的抗抑郁药。     

安非他酮缓释片治疗抑郁症72例的随机双盲双模拟多中心临床研究

目的:评价安非他酮缓释片治疗抑郁症的有效性和安全性。方法:采用随机双盲双模拟多中心平行对照研究。氟西汀为对照药。试验组和对照组各入组72例,完成6wk治疗的病人共125例,其中试验组61例,对照组64例。试验组用安非他酮缓释片300mg·d-1,对照组用氟西汀20mg·d-1。结果:治疗6wk后,试验组和对照组HAMD的减分值分别为(12±s6)分和(12±6)分,2组的有效率分别为74%和62%,2组相比差异均无统计学意义(P>0.05)。试验组总不良反应发生率为53%,对照组为54%,2组相比差异无统计学意义(P>0.05)。结论:安非他酮缓释片是一种安全、有效的抗抑郁新药。     

戒烟药物研究进展

烟草依赖为一种慢性尼古丁成瘾性疾病.尼古丁强化效应是吸烟者戒烟失败的主要原因.吸烟者成功戒烟往往需戒烟药物的辅助治疗,常用戒烟药物有一线戒烟药物(如尼古丁替代、安非他酮及伐尼克兰)和二线戒烟药物(如可乐定和去甲替林等),以及其他戒烟药物.     

尼古丁依赖的药物治疗:指南与经验

吸烟是许多疾病的患病危险因素,戒烟可减少很多疾病的发病率及病死率,戒烟困难的原因在于尼古丁的成瘾性。尼古丁依赖是一种慢性高复发性疾病,属于精神神经疾病。有关戒烟指南指出针对戒烟者的尼古丁依赖鼓励使用戒烟药物。戒烟药物包括尼古丁替代药物,安非他酮及尼古丁乙酰胆碱受体α4β2亚型的选择性部分激动药(伐尼克兰),三类药物各有特点。伐尼克兰作为一种新型的戒烟药物,与尼古丁替代疗法(nicotine replacement therapy,NRT)存在不同的特点。我们比较了两者用于临床戒烟的有效性和不良反应,以期指导临床中不同特点戒烟者的尼古丁依赖的治疗。结果显示伐尼克兰应用和NRT都是安全有效的戒烟疗法,药物不良反应各有不同,临床工作中可根据戒烟者自身的不同特点进行相应的选择。     

安非他酮与舍曲林治疗抑郁症疗效比较

目的比较安非他酮与舍曲林对抑郁症的疗效及其安全性。方法125例抑郁症分为2组。安非他酮组63例[男性30例,女性33例,年龄(36±s 13)岁,本次抑郁病期(3±5)mo]予安非他酮300～450 mg·d~(-1),po,bid;舍曲林组62例[男性28例,女性34例,年龄(40±11)岁,本次抑郁病期(3±4)mo]予舍曲林50～100 mg,po,qd;均6 wk为一个疗程。结果对抑郁症状的治疗,安非他酮组显效率71%,舍曲林组显效率74%,2组疗效比较差异无显著意义(P>0.05);对伴随焦虑症状的治疗,安非他酮组显效率48%,舍曲林组显效率45%,2组疗效比较差异无显著意义(P>0.05)。整体药物不良反应发生率2组相当。结论安非他酮与舍曲林疗效相当,能有效治疗抑郁症及伴随焦虑症状,不良反应轻微。     

A preliminary study of bupropion sustained-release for smoking cessation in patients with chronic posttraumatic stress disorder

This study was conducted to evaluate the effect of bupropion sustained-release (SR) on smoking cessation in patients with chronic posttraumatic stress disorder (PTSD). Fifteen veterans with chronic PTSD who desired to stop smoking enrolled in a 12-week double-blind evaluation of bupropion SR and placebo. Patients were randomly assigned in a 2:1 ratio to receive either bupropion SR or placebo. Bupropion SR was initiated at 150 mg daily for 3 or 4 days and increased to a final dose of 150 mg twice daily (300 mg daily total). Ten patients received bupropion SR and five received placebo. Nine of the patients who received bupropion SR were already being treated with at least one other psychotropic medication. One of the ten patients did not complete the study because of medication side effects. Eighty percent of patients receiving bupropion SR successfully stopped smoking by the end of week 2, and 6 (60%) of these 10 maintained smoking cessation at the study endpoint (week 12). At the 6-month follow-up, 40% of the patients (4 of 10) who received bupropion SR maintained smoking cessation. One (20%) of the five patients who received placebo stopped smoking and maintained smoking cessation at the 6-month follow-up. Bupropion SR was generally well-tolerated in combination with other psychotropic medications. Bupropion SR may be effective in helping patients who desire to quit smoking and who also have a concomitant anxiety disorder, such as PTSD.     

A 12-week double-blind, placebo-controlled study of bupropion sr added to high-dose dual nicotine replacement therapy for smoking cessation or reduction in schizophrenia

The objective of this study was to examine whether there is a benefit of adding bupropion SR to high-dose combination nicotine replacement therapy (NRT) and weekly group cognitive behavioral therapy (CBT) for smoking reduction or cessation in schizophrenia. Fifty-one adult smokers with schizophrenia were randomly assigned to a 12-week trial of bupropion SR 300 mg/d or placebo added to transdermal nicotine patch, nicotine polacrilex gum, and CBT. The treatment goal was smoking cessation. The primary outcome measure was biochemically confirmed 7-day point-prevalence of 50% to 100% smoking reduction at week 12. Secondary outcomes were biochemically confirmed tobacco abstinence and change from baseline in expired air carbon monoxide (CO) and psychiatric symptoms. Subjects on bupropion + NRT had a greater rate of 50% to 100% smoking reduction at weeks 12 (60% vs. 31%; P = 0.036) and 24, a lower expired air CO in the treatment and follow-up periods, (F = 13.8; P < 0.001) and a greater continuous abstinence rate at week 8, before NRT taper, (52% vs. 19%; P = 0.014). However, relapse rates in subjects on bupropion + dual NRT were 31% during NRT taper (weeks 8-12) and 77% at the 12-month follow-up. Abstinence rates did not differ by treatment group at weeks 12 (36% vs. 19%), 24 (20% vs. 8%), or 52 (12% vs. 8%). Because abstinence rates were high during treatment with combination pharmacotherapy and relapse rates were very high during taper and after discontinuation of treatment, study of longer term treatment with combination pharmacotherapy and CBT for sustained abstinence is warranted in those who attain initial abstinence with this intervention.     

A preliminary investigation of naltrexone augmentation of bupropion to stop smoking with less weight gain

Certain barriers prevent some cigarette smokers from attempting to quit, particularly the fear of post-cessation weight gain. This investigation was an open label study of naltrexone hydrochloride (25 mg/day) in combination with sustained-release (SR) bupropion hydrochloride (300 mg/day) for smoking cessation and minimization of post-quit weight gain in weight-concerned smokers. The study sample (n=20) was compared to matched controls (n=20) who received an identical psychosocial intervention and bupropion SR treatment regimen. The primary outcomes analyzed were: (a) biochemically verified continuous abstinence from smoking over the 6-week treatment, (b) point prevalence abstinence in the last 7 days of treatment, and (c) weight gain from baseline. Neither adherence to the combination pharmacotherapy nor the percentage of patients reporting adverse events differed significantly between the two groups nor were there differences in either continuous or point prevalence abstinence from smoking. Although not statistically significant in this small sample, continuously abstinent participants in the naltrexone+bupropion group gained less weight (mean=1.67 lb) than those in the bupropion only group (mean=3.17 lb; p=.35; Cohen's d=0.56). The results of this preliminary study suggest that combining naltrexone and bupropion may help minimize post-cessation weight gain, but does not result in higher smoking cessation rates compared to bupropion alone. The effect size for the difference in weight gain among continuously abstinent participants was in the moderate range, suggesting that this treatment deserves further study in an appropriately powered clinical trial as an adjunct for weight-concerned smokers, who may value the weight-suppressant effect of naltrexone.     

Use of sustained-release bupropion in specific patient populations for smoking cessation

Smoking cessation trials of sustained-release bupropion (bupropion SR) were initially conducted in a general population of smokers who were motivated to quit smoking. Bupropion SR has also been found to be a useful treatment of tobacco dependence in various special populations of smokers who often experience difficulty in overcoming tobacco addiction. Point-prevalence quit rates at 6 months were higher in those treated with bupropion SR than in those receiving placebo in studies on smokers with chronic obstructive pulmonary disease (23% vs 16%) and in those with cardiovascular disease (34% vs 12%). Abstinence from smoking after treatment with bupropion SR was not affected by a history of major depression or alcoholism. Women treated with bupropion SR were just as likely as men to abstain from smoking. Approximately one-third of a study population who were initially unwilling or unable to quit smoking were able to reduce their smoking by 50% or more during therapy with bupropion SR; 14% of these went on to achieve abstinence. Bupropion SR was well tolerated in these trials; importantly, it had no clinically significant effect on mean blood pressure in smokers, including those with hypertension, and attenuated the weight gain associated with smoking cessation, particularly in women.     

Predictors of 12-month outcome in smokers who received bupropion sustained-release for smoking cessation

AIM: To examine heterogeneity in outcome at 12 months following 8 weeks of treatment for smoking cessation with bupropion sustained-release (SR) 150 or 300 mg/day combined with behavioural counselling. DESIGN, SETTING, PARTICIPANTS: Smokers were recruited from a large healthcare system and then randomized to receive either bupropion SR 150 mg/day (n = 763) or 300 mg/day (n = 761) taken for 8 weeks in combination with either proactive telephone counselling or a tailored mail approach. MEASUREMENTS AND FINDINGS: A comprehensive set of relevant individual pretreatment and treatment characteristics was included in the analysis. Smoking outcome at 12 months was defined as point-prevalence of any regular self-reported smoking within the 7 days prior to follow-up contact. Classification and regression tree analysis identified subgroups that varied with respect to likelihood of being nonsmokers at 12 months. Seven subgroups were identified among those receiving bupropion SR 150 mg/day (proportion of nonsmokers at 12 months ranged from 13.7% to 43.5%) and eight subgroups among those receiving bupropion SR 300 mg/day (proportion of nonsmokers at 12 months ranged from 9.6% to 51.7%). In the 150-mg/day group, those with the lowest rate reported no previous quit attempt of 1 month or more in duration while those with the highest rate all reported previous quit attempts of 1 month or longer. In the 300 mg/day group, those with the lowest rate had very high levels of dependence while those with the highest rate were more highly educated and smoked at a lower level. Across all subgroups, cost per 12-month quitter ranged from a low of USD302 to a high of USD2,502. CONCLUSIONS: These results indicate the presence of a substantial amount of variation in outcome following treatment with both dosages of bupropion SR, with substantial cost consequences. Variation in outcome could be reduced by providing treatments tailored to subgroups of individuals who are at exceptionally high risk for smoking following a quit attempt.     

Clinical efficacy of bupropion in the management of smoking cessation

Nicotine addiction is a chronic relapsing condition that can be difficult to treat. Until recently, pharmacological options for the treatment of tobacco dependence were primarily limited to nicotine replacement therapy (NRT). Sustained-release bupropion (bupropion SR) is the first non-nicotine pharmacological treatment approved for smoking cessation. Bupropion SR is recommended for first-line pharmacotherapy alongside NRT in the updated US Clinical Practice Guidelines and the UK Health Education Authority Guidelines. The UK National Institute of Clinical Excellence recommends NRT and bupropion SR for smokers who have expressed a desire to quit smoking. This review presents evidence that bupropion SR is an effective first-line therapy for smoking cessation in a wide range of patient populations. It is associated with significantly higher smoking cessation rates compared with placebo in patients with or without a history of prior bupropion SR or NRT use, and its effect is independent of gender. Bupropion SR treatment is effective in the prevention of relapse to smoking in those patients who have successfully quit, and re-treatment is effective in smokers who recommence smoking after a previous course of bupropion SR. Bupropion SR treatment relieves the symptoms of craving and nicotine withdrawal, and attenuates the weight gain that often occurs after smoking cessation. Data collected from motivational support programmes and employer-based studies provide strong evidence of the effectiveness of bupropion SR as an aid to smoking cessation in 'real life' situations, and confirm the efficacy seen in clinical trials.     

地尔硫缓释片与倍他洛尔治疗轻中度高血压病的疗效比较

目的 :比较地尔硫缓释片与倍他洛尔治疗轻、中度高血压病的疗效与安全性。方法 :随机开放对照试验 ,经 2wk安慰剂导入期 ,4 0例轻、中度高血压病人分成 2组 ,各 2 0例 ,进入 6wk治疗期。2组病人分别服地尔硫缓释片 2 0 0mg或倍他洛尔 10mg ,qd ,2wk后如舒张压≥ 12kPa ,则增量至地尔硫缓释片 30 0mg或倍他洛尔 2 0mg至疗程结束。结果 :2组药物均能明显降低血压 (P <0 .0 1) ,有效率分别为 79%及 84 % (P >0 .0 5)。同时 2种药物均有降低心率的作用。动态血压显示 2药持续降压作用达 2 4h。结论 :地尔硫缓释片每日 1次能有效降低轻、中度高血压病病人的血压     

Bupropion SR and contingency management for adolescent smoking cessation

There is a significant need for evidence-based treatments for adolescent smoking cessation. Prior research, although limited, has suggested potential roles for bupropion sustained-release (SR) and contingency management (CM), but no previous studies have assessed their combined effect. In a double-blind, placebo-controlled design, 134 adolescent smokers were randomized to receive a 6-week course of bupropion SR + CM, bupropion SR + non-CM, placebo + CM, or placebo + non-CM, with final follow-up at 12 weeks. The primary outcome was 7-day cotinine-verified point prevalence abstinence, allowing for a 2-week grace period. Combined bupropion SR + CM treatment yielded significantly superior abstinence rates during active treatment when compared with placebo + non-CM treatment. In addition, combined treatment showed greater efficacy at multiple time points than did either bupropion SR + non-CM or placebo + CM treatment. Combined bupropion SR and CM appears efficacious, at least in the short-term, for adolescent smoking cessation and may be superior to either intervention alone.     

Partial agonism at nicotinic receptors with varenicline – a new approach to smoking cessation

Cigarette smoking is the leading preventable cause of death. Varenicline is a partial agonist at nicotinic α₄β₂ receptors being tested for smoking cessation. During a trial in which the drugs were administered for 12 weeks, the continuous abstinence rate was 17.7% in the placebo group, which improved to 29.5% with bupropion SR and to 44.0% with varenicline 1 mg b.i.d. Abstinence rates for weeks 9 through 52 were 8.4, 16.1 and 21.9% for placebo, bupropion and varenicline, respectively. Prolonging the treatment with varenicline may give better quit rates. In this trial, after 12 weeks of open-label varenicline, the abstainers received either another 12 weeks of varenicline or placebo. At week 24, more of the participants in the varenicline group (70.5%) were abstinent than in the placebo group (49.6%). The most common adverse effect in both these trials with varenicline was nausea. This prompted a trial comparing the efficacy and safety of four varenicline dosing regimens, to determine whether a lower dose was effective and with reduced adverse effects. After 52 weeks, the abstinence rates were 3.9% in the placebo group, and higher in the varenicline 0.5 mg b.i.d. (18.5%) and 1 mg b.i.d. groups (22.4%). The rates of nausea were not significantly increased by varenicline 0.5 mg b.i.d., but were by varenicline 1 mg b.i.d. In summary, varenicline may give slightly higher smoking cessation rates than bupropion, but the smoking cessation rates, especially at 52 weeks, remain low.