酒石酸唑吡坦片　　
中文正式名　酒石酸唑吡坦片
商品名及别名 乐坦 诺宾 思诺思 左吡登 唑吡坦
英文名 Zolpidem Tartrate Tablets
主要成分 本品主要成分及其化学名称为：本品的主要成分是酒石酸唑吡坦，其化学名为N,N,6-三甲基-2-(4-甲基苯基)-咪唑并[1,2-a]吡啶-3-乙酰胺酒石酸盐。
分子式及分子量 分子式：C19H21N3O2?C4H6O6 分子量：764.88
性状 本品为薄膜衣片，除去薄膜衣后显白色或类白色。
药理学特征 本品为一催眠剂，通过选择性地与中枢神经系统的ω1-受体亚型的结合，产生药理作用。本品小剂量时，能缩短入睡时间，延长睡眠时间；在较大剂量时，第2相睡眠、慢波睡眠(第3和第4相睡眠)时间延长，REM睡眠时间缩短。
药代学特征 据文献报道，酒石酸唑吡坦吸收快，起效迅速。口服生物利用度为70%，且在治疗剂量范围内显示线性动力学，口服后0.3～3小时血药浓度达峰值。消除半衰期，平均为2.4小时(0.7～3.5)，作用可维持6小时。血浆蛋白结合率为92.5%±0.1%。肝的首过效应为35%。重复服药不改变蛋白结合率，表明本品与其代谢物对结合部位缺乏竞争。成人的表观分布容积为0.54±0.2L/kg。老年人降至0.34±0.052L/kg。所有代谢物均无活性，且由尿中(56%)和粪便中(37%)排出。试验表明唑吡坦是不可透析的。
[适应症]
[作用与用途] 失眠症的短期治疗
服用方法 本品起效迅速，所以应在临睡前服用。成人的推荐剂量为每天10mg。老年人和体质虚弱者可能对本品较敏感，因此推荐剂量为第天5mg。
对于肝功能不全者，本品的清除代谢率降低，应从每天5mg剂量开始服用，对老年病人应特别注意。疗程可由几天至两周不等，最多四周(包括逐渐减量的时间)。注意，不得超过推荐和疗程服用。
不良反应 有证据表明，服用本品有与剂量相关的不良反应，尤其是对中枢神经系统的作用和胃肠蠕动增加。老年病人最易产生。临床试验中，10mg剂量以下观察到的不良反应有：嗜睡、头晕、头痛、恶心、腹泻和眩晕。
在长期临床试验中，极少观察到记忆障碍(顺行性遗忘)，夜间烦躁，抑郁综合症、精神障碍、意识障碍或复视、颤抖舞蹈步和跌倒。
使用苯二氮卓类或类似苯二氮卓类药物会出现如下副作用：烦躁、兴奋、过敏性、侵略性错觉、暴怒、梦魇、幻觉、精神病、过激行为和其他敌对行为。如出现这些症状，应停止用药。年老者更易出现这些症状。
禁忌症
　1、对本品过敏者禁用。
　2、梗阻性睡眠呼吸暂停综合征、重症肌无力、严重肝功能不全、急性呼吸功能不全伴呼吸抑制者禁用，抑郁型精神病患者慎用。
注意事项：
　1、连续服用速效的苯二氮卓类和类似苯二氮卓类药物几周后，其药效和催眠效果可能会有所降低，而产生耐受性。
　2、依赖性和失眠症反弹：依赖性：使用苯二氮卓类和类似苯二氮卓类药物可能会对这些药物产生躯体和精神依赖性。产生依赖性的风险随剂量的增加及治疗期的延长而增加。具有滥用药物和酗酒史者风险更大。一旦出现身体依赖性，立即停药会出现戒断症状，包括头痛、肌肉痛、极度焦虑紧张、烦躁、兴奋和谵妄。严重时会出现意识障碍、失去理智、听觉过敏、麻木、四肢麻刺感，对光、声音和身体接触过敏、出现幻觉和癫痫发作。
失眠症反弹：由苯二氮卓类和类似苯二氮卓类药物引起的短暂综合症状可能会使失眠症复发并增强。停止安眠治疗可能出现失眠症反弹。也可能伴随其它症状，包括情绪不稳、焦虑和烦躁。由于突然停药，会出现戒断症状或失眠症反弹，故应逐渐减少剂量。
　3、对驾车和操作机械能力的影响：虽然研究表明服用本品后，模拟车辆驾驶未受影响，但司机和机械操作者应注意，同别的催眠药一样，服用本品次日上午可能有睡意。
孕妇及哺乳
妇女用药 妊娠及哺乳期妇女禁用。
儿童用药 15岁以下儿童禁用。
药物相互作用 不宜同时饮酒，因酒精可能增强镇静效果，影响驾驶或操作机械能力。慎与中枢神经系统镇静剂合用：与抗精神病药(神经安定药)、催眠药、抗焦虑药、麻醉止痛药、抗癫痫药和有镇静作用的抗组胺药合用，能增强中枢抑制作用。不宜与抗抑郁药合用。
麻醉止痛剂可能会增强欣快症，从而导致精神依赖性增加。
抑制肝酶(特别是细胞色素P450)的化合物可能会增强苯二氮卓类或类似类苯二氮卓类药的作用。
药物过量 在过量用药病例中，有由意识障碍、嗜睡到轻度昏迷的报告。应进行全身检查和解救措施，如立即洗胃，必要时给予支持疗法等。当洗胃无效时，应使用活性碳减少吸收。即使出现兴奋，也要禁止使用镇静药物。出现严重症状时，可考虑使用氟马西尼(Flumazenil)。
规格 5mg
有效期 一年半
储藏 遮光，密闭在干燥处保存
批准文号 国药准字X20000114

Manufacturer:

Meda Pharmaceuticals

Pharmacological Class:

Imidazopyridine hypnotic

Active Ingredient(s):

Zolpidem tartrate 5mg, 10mg; sublingual tabs.

Indication(s):

Insomnia.

Pharmacology:

Zolpidem is a hypnotic agent that works by interacting with the GABA-BZ receptor complex. It shares some of the pharmacological effects of benzodiazepines despite being chemically dissimilar to the benzodiazepines, barbiturates, and other hypnotic agents. It selectively binds to some, but not all, of the benzodiazepine receptor subtypes, which may account for its lack of anticonvulsant and muscle relaxant properties.

When administered sublingually, this product dissolves and is absorbed rapidly. Concomitant food will delay its effect.

Clinical Trials:

Two clinical studies were conducted to evaluate zolpidem in the treatment of patients with chronic insomnia. A double-blind, parallel-group 5-week study in 75 adult outpatients compared 2 doses of zolpidem tartrate and placebo. Objective measurements indicated that zolpidem 10mg was superior to placebo on sleep latency for the first 4 weeks and on sleep efficiency for weeks 2 and 4.

In another study in adult outpatients with chronic insomnia, zolpidem 10mg was superior to placebo on a subjective measurement of sleep latency for all 4 weeks, and on subjective measurements of total sleep time, number of awakenings, and sleep quality for the first treatment week.

In the treatment of transient insomnia, normal adults in a sleep laboratory were evaluated on the first night in a double-blind, parallel-group trial comparing 7.5mg and 10mg of zolpidem tartrate to placebo. Both doses of the study drug were superior to placebo in objective measures of sleep latency, sleep duration, and number of awakenings.

In a crossover study involving normal adults with a mean age of 68 years experiencing transient insomnia during the first 2 nights in a sleep lab, zolpidem at doses of 5mg, 10mg, 15mg, and 20mg were compared to placebo. All of the zolpidem doses were superior to placebo for sleep latency, efficiency, duration, latency, quality, and number of awakenings.

Legal Classification:

CIV

Adults:

≥18 years: Place 1 tab under tongue and allow to dissolve; do not take with food, water, or alcohol. 10mg at bedtime (take only if able to get 7–8 hours of sleep before becoming active again). Elderly, debilitated, or hepatic impairment: 5mg at bedtime. Reevaluate periodically.

Children:

<18 years: not recommended.

Precaution(s):

Depression. Compromised respiratory function (eg, sleep apnea). Conditions that affect metabolism or hemodynamic response. Myasthenia gravis. Write Rx for smallest practical amount. Withdraw gradually. Elderly. Debilitated. Labor & delivery. Pregnancy (Cat.C). Nursing mothers.

Interaction(s):

Potentiated by alcohol, other CNS depressants (eg, imipramine, chlorpromazine), ketoconazole (reduce zolpidem dose). May be affected by sertraline, rifampin, CYP3A inhibitors.

Adverse Reaction(s):

CNS effects (eg, hallucinations, agitation, behavioral changes, depersonalization, amnesia), complex sleep-related behaviors (eg, sleep-driving), headache, drowsiness, dizziness, anaphylaxis, angioedema; others.

How Supplied:

SL tabs—10, 30, 100

Last Updated:

10/1/2009