DRUG CLASS AND MECHANISM:
Bupropion is an antidepressant medication that affects chemicals within the brain that nerves use to send messages to each other. These chemical messengers are called neurotransmitters. Many experts believe that depression is caused by an imbalance among the amounts of neurotransmitters that are released. Nerves, in a process referred to as reuptake, may recycle released neurotransmitters. Bupropion works by inhibiting the reuptake of dopamine, serotonin, and norepinephrine; an action that results in more dopamine, serotonin, and norepinephrine to transmit messages to other nerves. Bupropion is unique and unlike other antidepressants in that its major effect is on dopamine, an effect that is not shared by the selective serotonin reuptake inhibitors or SSRIs [for example, paroxetine (Paxil), fluoxetine (Prozac), sertraline (Zoloft)] or the tricyclic antidepressants or TCAs [for example, amitriptyline (Elavil), imipramine (Tofranil), desipramine (Norpramin)]. The FDA approved bupropion in December 1985.

STORAGE:
Tablets should be kept at room temperature, 15-25°C (59-77°F).

PRESCRIBED FOR:
Bupropion is used for the management of major depression and seasonal affective disorder(depression that occurs primarily during the fall and winter). It is also prescribed for smoking cessation.

DOSING:
Bupropion usually is given in one, two or three daily doses. For immediate-release tablets, no single dose should exceed 150 mg and each dose should be separated by 6 hours. For depression the recommended dose of immediate-release tablets is 100 mg 3 times daily (300 mg/day); maximum dose is 450 mg daily. The initial dose is 100 mg twice daily. The dose may be increased to 100 mg 3 times daily after three days. The initial dose of sustained-release tablets is 150 mg daily; target dose is 150 mg twice daily; maximum dose is 200 mg twice daily. The initial dose of extended-release tablets is 150 mg daily; target dose is 300 mg daily; maximum dose is 450 mg daily. Extended release tablets are administered once daily. When used for smoking cessation, bupropion usually is started as 150 mg once daily for three days, and then the dose is increased if the patient tolerates the starting dose. Smoking is discontinued two weeks after starting bupropion therapy.

DRUG INTERACTIONS:
Bupropion should be used cautiously in patients receiving drugs that reduce the threshold for seizures. Such drugs include prochlorperazine (Compazine), chlorpromazine (Thorazine), and other antipsychotic medications of the phenothiazine class. Additionally, persons who are withdrawing from benzodiazepines [for example, diazepam (Valium), alprazolam (Xanax)] are at increased risk for seizures. Carbamazepine (Tegretol) may reduce the effect of bupropion by reducing the blood concentration of bupropion. Monamine oxidase inhibitors should not be combined with bupropion because of the risk of severe reactions. At least 14 days should elapse between discontinuation of an MAOI and initiation of bupropion. Bupropion may affect the action of warfarin (Coumadin).

【药品名称】盐酸安非他酮缓释片
【成份】盐酸安非他酮
【性状】本品为薄膜衣片，除去包衣后显类白色。
【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。
【适应症】（1）精神型抑郁症，特别是对用其它抗抑郁药治疗无效或不能耐受的抑郁病人。（2）用于戒烟的辅助治疗。
【不良反应】常见的不良反应有：激动、口干、失眠、头痛或偏头痛，恶心、呕吐，便秘、震颤、多汗、耳鸣、焦虑。
【禁忌症】
1、癫痫患者忌用；
2、单胺氧化酶（MAOI）抑制剂不能与本品同服，服用本品前至少14天不能使用单胺氧化酶抑制剂；
3、神经性食欲旺盛和厌食患者忌用；
4、本品与ZYBAN及其它含有安非他酮的药物（如ZybanTM）均不能合用；
5、对本品过敏者禁用。
【注意事项】
1、应该在医生指导下服用盐酸安非他酮，且不要超过医生所规定的疗程和随意增加安非他酮的剂量；
2、当开始治疗时期剂量要增加到每日150mg以上时，应划分成两个等剂量以减小癫痫的危险。在用剂量范围100mg-300mg/天治疗时，癫痫发生率大约为0.1%。较低的癫痫发生率是否与不同的配方或较低的剂量尚不明确。在使用本品时应考虑病人的临床状态和同时服用的药物。头部创伤史、以前的癫痫史、中枢神经系统肿瘤和同时服用降低癫痫阈值的药物可能增加癫痫的发生。过量应用乙醇、突然戒断醇或其它镇静剂；对鸦片、可卡因或刺激剂成瘾；应用超剂量刺激剂和anorectices；以及用口服降血糖药物或胰岛素治疗糖尿病等临床状态都可能引起癫痫风险增加；
3、在确信本品对病人执行那些需要判断或需要运动和识别技巧的任务时没有负面影响，否则他们不应该驾驶汽车或操作复杂的带有危险性的机器；
4、服用本品有轻微的肝细胞损伤，本品和它的代谢产物通过肾脏几乎完全排泄，幷且代谢物在尿排泄之前很可能在肝脏中发生结合，使得体内累计可能比正常人高。因此治疗肾脏或肝脏损伤的病人应该以较小的剂量开始；
5、为保证盐酸安非他酮缓释片的释放速率不会改变，应整片吞服。决不要咀嚼，划分或捣碎片剂；
6、本品中含有与用于帮助戒烟治疗的Zyban中相同的活性组分，因此本品不应与Zyban或任何其它含有bupropion的药物组成复方使用；
7、饮酒和停止饮酒都可能改变癫痫阈值，因此酒精的消耗应该减少到最小，如果可能，应该完全避免；
8、抑郁患者的自杀倾向是固有的，除非症状改善，所以处方必需是最小剂量的而且患者要在严密的控制之下；
9、年龄和性别对本品没有影响；
10、使用本品可能会改变患者的食欲或体重，需要考虑。
【药物相互作用】安非他酮可以减少药物代谢酶，改变合用药物的血药浓度。促进性药物如酰胺咪嗪、苯巴比妥、环磷酰胺，抑制性药物如甲青咪胍可影响安非他酮的药物活性。体外试验表明，安非他酮先被细胞色素P450ⅡB6同功酶代谢为吗琳代谢物，所以影响细胞色素P450的药物会影响安非他酮缓释片（如邻甲基苯海拉明和环磷酰胺），氨基苏醇代谢物不是由细胞色素P450系统生成的。动物研究表明，MAO抑制剂如苯乙肼可以提高安非他酮的急性毒性。少数临床资料表明，安非他酮和左氟多巴合用对患者有不利影响，合用时要小心，剂量增加要缓慢。能够降低癫痫发作阈值的药物和治疗因素在使用安非他酮时要非常慎重，使用较低的首剂量，剂量增加要缓慢。
【药物过量】怀疑服用过量后，如果患者是清醒的，则用吐根糖浆诱导呕吐，服用后12小时内每隔6小时服用一次活性碳，要检测基础指针、心电图，并且48小时心电监护，多喝水。如果病人昏迷、痉挛，则推荐使用胃肠插管灌洗，虽然临床过量服用速释性安非他酮后使用灌胃处理的病例很少，安非他酮缓释片没有，但在服用后12小时内药物还未完全吸收，采用此法认为是可行的。基于动物试验，推荐使用适当的苯二氮卓类药物和其它适当的方法治疗癫痫。

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详细处方信息以本药内容附件PDF文件（201242418493111.pdf）的“原文Priscribing Information”为准
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