英文药名: Wellbutrin XL (Bupropion Extended Release Tablets) 中文药名: 安非他酮缓释片 生产厂家: Glaxo Smith Kline 药品名称 通用名：盐酸安非他酮缓释片 英文名：Bupropion　Hydrochloride　Sustained-Release　Tablets 药理毒理 安非他酮是去甲肾上腺素、5-羟色胺、多巴胺再摄取的弱抑制剂，对单胺氧化酶没有抑制作用。本品抗抑郁作用机制尚不清楚，可能与其抑制去甲肾上腺素和/或多巴胺的作用有关。 药代动力学 安非他酮是一种消旋混合物。尚未研究单个对映体的药理活性和药代动力学。安非他酮的药代动力学曲线呈二室模型。终末相平均半衰期为 21小时（±20%），分布相平均半衰期为3-4小时。 适应症　　 用于治疗抑郁症。用于辅助戒烟。 用法用量 抑郁症: 口服。用药时从小剂量开始，起始剂量为一次75mg（1片），一日2次；服用3天后，逐渐增大剂量到一次75mg（1片），一日3次；以后逐渐增加至每日300mg的维持剂量。3日内剂量增加不超过一日100mg。最大剂量不超过一次150mg（2片），一日3次，用药间隔不得少于6小时。 戒烟: 用药开始第 1 ～ 3 天为一次 150mg （一片），每日 1 次，连续使用 3 天，随后第 4 ～ 7 天改为一次 150 mg （一片），每日 2 次。两次用药间隔时间大于 8 小时，第 8 天开始为一次 150 mg （一片），每日 1 次或 2 次。疗程 7-12 周或更长，可同时使用尼古丁代用品。本品的最大推荐剂量为一日 300mg （ 2 片），分两次服用。由于连续服药 1 周安非他酮的血药浓度才能达到稳态，所以应该在患者仍然吸烟时就开始给药。在服药的第二周设定一个目标戒烟日（通常是服药第 8 天）。若治疗 7 周后仍不见效则停止使用，停药时无需逐渐减量。在用药期间和停药后对患者进行戒烟的指导和帮助是非常必要的。谨遵医嘱！ 不良反应　　 常见口干、失眠、头晕、头痛/偏头痛、易怒、恶心/呕吐、便秘、水肿、皮疹、尿频等不良反应。偶见肝功能异常、胃炎、幻觉、食欲减退和体重改变等。贫血、共济失调等罕见。 禁忌症 1．癫痫发作患者。 2．使用其他含有安非他酮成分药物的患者。 3．贪食症或厌食症的患者。 4．对安非他酮或本品所含任一成份过敏者。 注意事项 1．盐酸安非他酮有诱发癫痫的可能性。以下措施可以使癫痫发作的风险减至最低：每日最大给药量不超过450mg；每日三次给药，单次给药量不超过150mg；逐渐增加给药量。 2．有癫痫病史、颅脑肿瘤或其它有癫痫倾向、正在服用其它降低癫痫发作阈的药物（如抗精神病药、抗抑郁药、甾体化合物）的患者慎用。 3．与单胺氧化酶（MAO）抑制剂不能合并使用。MAO抑制剂与安非他酮的服用间隔至少应为14天。 4．严重肝硬化患者慎用。这部分患者服用本品时，最大剂量不超过75mg，每日服用一次。 药物相互作用 1．细胞色素P450IID6代谢的药物：体外试验表明安非他酮和羟安非他酮是CYPIID6酶的抑制剂，因此正在使用CYPIID6酶代谢药物治疗的患者服用安非他酮时，应当考虑减少原来药物的剂量，特别是那些治疗指数窄的药物。这些药物包括某些抗抑郁药物（如：去甲替林，米帕明，地昔帕明，帕罗西汀，氟西汀，舍曲林），抗精神病药（如：氟哌啶醇，利培酮，甲硫达嗪），b-阻断剂（如：美托洛尔），抗心律失常药物（如：普罗帕酮，哌氟酰胺），同时在合并治疗开始时应当使用最小剂量。 2. MAO抑制剂：动物研究显单胺氧化酶抑制剂（MAOI）苯乙胼可以增加安非他酮的急性毒性。 3. 左旋多巴：临床资料表明同时使用安非他酮和左旋多巴后，副作用发生率可能升高。服用左旋多巴的患者同时服用本品时应谨慎，从最小剂量开始使用，然后逐渐加量。 4. 降低癫痫发作阈值的药物：本品与降低癫痫发作阈值的药物（如：抗精神病药物，抗抑郁药物，茶碱，类固醇化合物等）合用或突然中断苯二氮卓类药物治疗后使用本品时应减少剂量，剂量的增加应缓慢。 WELLBUTRIN XL WELLBUTRIN XL is indicated for the treatment of major depressive disorder, as well as the prevention of seasonal major depressive episodes in patients with a diagnosis of seasonal affective disorder.  INDICATIONS AND USAGE  Major Depressive Disorder: WELLBUTRIN XL is indicated for the treatment of major depressive disorder.  The efficacy of bupropion in the treatment of a major depressive episode was established in two 4-week controlled trials of inpatients and in one 6-week controlled trial of outpatients whose diagnoses corresponded most closely to the Major Depression category of the APA Diagnostic and Statistical Manual (DSM).  A major depressive episode (DSM-IV) implies the presence of 1) depressed mood or 2) loss of interest or pleasure; in addition, at least 5 of the following symptoms have been present during the same 2-week period and represent a change from previous functioning: depressed mood, markedly diminished interest or pleasure in usual activities, significant change in weight and/or appetite, insomnia or hypersomnia, psychomotor agitation or retardation, increased fatigue, feelings of guilt or worthlessness, slowed thinking or impaired concentration, a suicide attempt, or suicidal ideation.  The efficacy of bupropion in maintaining an antidepressant response for up to 44 weeks following 8 weeks of acute treatment was demonstrated in a placebo-controlled trial with the sustained-release formulation of bupropion. Nevertheless, the physician who elects to use WELLBUTRIN XL for extended periods should periodically reevaluate the long-term usefulness of the drug for the individual patient.  Seasonal Affective Disorder: WELLBUTRIN XLisindicatedforthepreventionofseasonal majordepressive episodes in patients with a diagnosis of seasonal affective disorder. The efficacy of WELLBUTRIN XL for the prevention of seasonal major depressive episodes was established in 3 controlled trials of adult outpatients with a history of major depressive disorder with an autumn-winter seasonal pattern as defined by Diagnostic and Statistical Manual of Mental Disorders, 4th edition (DSM-IV) criteria.  Seasonal affective disorder is characterized by recurrent major depressive episodes, most commonly occurring during the autumn and/or winter months. Episodes may last up to 6 months in duration, typically beginning in the autumn and remitting in the springtime. Although patients with seasonal affective disorder may have depressive episodes during other times of the year, the diagnosis of seasonal affective disorder requires that the number of seasonal episodes substantially outnumber the number of non-seasonal episodes during the individual's lifetime.  CONTRAINDICATIONS  WELLBUTRIN XL is contraindicated in patients with a seizure disorder.  WELLBUTRIN XL is contraindicated in patients treated with ZYBAN® (bupropion hydrochloride) Sustained-Release Tablets; WELLBUTRIN® (bupropion hydrochloride), the immediate-release formulation; WELLBUTRIN SR® (bupropion hydrochloride), the sustained- release formulation; or any other medications that contain bupropion because the incidence of seizure is dose dependent.   WELLBUTRIN XL is contraindicated in patients with a current or prior diagnosis of bulimia or anorexia nervosa because of a higher incidence of seizures noted in patients treated for bulimia with the immediate-release formulation of bupropion.  WELLBUTRIN XL is contraindicated in patients undergoing abrupt discontinuation of alcohol or sedatives (including benzodiazepines).  The concurrent administration of WELLBUTRIN XL Tablets and a monoamine oxidase (MAO) inhibitor is contraindicated. At least 14 days should elapse between discontinuation of an MAO inhibitor and initiation of treatment with WELLBUTRIN XL Tablets.  WELLBUTRIN XL is contraindicated in patients who have shown an allergic response to bupropion or the other ingredients that make up WELLBUTRIN XL Tablets.  WARNINGS  Clinical Worsening and Suicide Risk: Patients with major depressive disorder (MDD), both adult and pediatric, may experience worsening of their depression and/or the emergence of suicidal ideation and behavior (suicidality) or unusual changes in behavior, whether or not they are taking antidepressant medications, and this risk may persist until significant remission occurs. Suicide is a known risk of depression and certain other psychiatric disorders, and these disorders themselves are the strongest predictors of suicide. There has been a long-standing concern, however, that antidepressants may have a role in inducing worsening of depression and the emergence of suicidality in certain patients during the early phases of treatment. Pooled analyses of short-term placebo-controlled trials of antidepressant drugs (SSRIs and others) showed that these drugs increase the risk of suicidal thinking and behavior (suicidality) in  children, adolescents, and young adults (ages 18-24) with major depressive disorder (MDD) and other psychiatric disorders. Short-term studies did not show an increase in the risk of suicidality with antidepressants compared to placebo in adults beyond age 24; there was a reduction with antidepressants compared to placebo in adults aged 65 and older.