中文别名：  咪达唑仑、马来酸咪达唑仑、咪哒唑仑、咪唑安定、咪唑二氮卓
英文别名：  Dormicium、Midazolam Maleate、Midazolam Malesate
生产企业：  
药品类别：  镇静、催眠药 

【药理药动】
本品为咪唑苯甲二氮卓类衍生物。咪达唑仑在酸性溶液中可形成稳定的水溶性盐，对局部组织刺激比地西泮要小。在体内生理性 pH条件下，其亲脂性碱基释出，能迅速进入中枢神经系统，增强γ-氨基丁酸对神经传递的抑制，产生抗焦虑、催眠、抗惊厥、肌肉松弛和顺行性遗忘作用。其效力约为地西泮的 1.5～2倍。使脑血流量和颅内压降低，降低脑的氧代谢率对脑缺氧有保护作用。对呼吸系统有一定的抑制作用，其程度与剂量相关。对循环系统也有轻微抑制作用，不影响心肌收缩力，心率改变轻微，周围血管阻力和平均动脉压下降。本品无镇痛作用，无组胺释放作用。
【药动学】
由于脂溶性高，口服吸收迅速，1h内血浆浓度达峰值，但首过效应大，生物利用度仅 40％～50％，肌肉注射 30min产生最大效应，而静脉注射麻醉诱导比硫喷妥钠慢，一般 2～3min可达到足够的睡眠程度。血浆浓度 80ng/ml表现催眠作用，而达麻醉稳定状态血浆浓度需 200～400ng/ml。单次静脉注药后分布半减期为0.31±0.24h，消除半减期 2.4±0.8h，稳态分布容积 0.68±0.15L/kg，清除率 502±105ml／min。本品通过肝微粒体氧化过程中的羟化作用进行代谢，主要代谢产物α-羟基咪达唑仑有一定活性，但很快与葡糖醛酸结合经尿排出，24h 90％注入药物被代谢排出，以原形从尿中排出不到0.5％。
【适 应 症】
①麻醉前用药，消除患者紧张和恐惧，并可提高局麻药的惊厥阈。
②全麻诱导和维持，主要适用于不宣用硫喷妥钠的重危患者，也可用于门诊等小手术，但需与其他麻醉药合用。
③局部和区域麻醉时作为辅助用药，使患者安静入睡，减少患者紧张和体位不适。
④用于重症监护室(ICU)患者镇静。
⑤各种失眠症， 尤其是最初入睡困难者。
【用法用量】
口服 10mg，1h达高峰。肌肉注射 5～10mg，10～15min产生镇静作用，30～40min产生最大效应。静脉诱导：0.1～0.3mg/kg，注速 15～30s起效比硫喷妥钠要慢，比地西泮快。麻醉维持：可间断静注首量的 25％～30％，也可持续静滴 0.15mg/kg·h，但需与其他全麻药、镇痛药等合用。镇静用量酌减。过量可由地西泮拮抗药氟马西林(安易醒，Flumazenil)拮抗。
可溶于 5％葡萄糖溶液、生理盐水和平衡液，不能与硫喷妥钠相混。
静注过快或用量过大可引起呼吸暂停，尤其是年老或呼吸功能不全的患者。应备供氧等抢救设备才可使用本药静注。
6％～10％患者代谢本品有异常。
【用法及用量】用于控制失眠：睡前口服 7.5～15mg；肌注，手术前30～60min给药，成人剂量 10～15mg，儿童 0.15～0.20mg/kg。静注，手术前给药，成人 2.5～5mg。
用于麻醉诱导：成人静注 10～15mg，儿童0.2mg/kg。
【剂型与规格】
片剂：15mg/片。
注射剂：5mg/ml，15mg/3ml。
【不良反应】
血压下降,长期使用突然停药可引起停药综合征.
注射后会出现疼痛、触痛和血栓性静脉炎。个别患者可出现遗忘现象，少数可成瘾；麻醉诱导时少见呃逆、恶心、呕吐及咳嗽。
常见的副作用有局部疼痛和血栓性静脉炎。此外，还报道有血压下降、呼吸抑制和一过性精神性运动行为改变等。中枢性呼吸抑制时有报道，尤其是老年人，由于中枢神经系统敏感性增强，这种危险性更大。在一些病人身上，此药的作用时间延长、这使病人清醒推迟或呼吸困难。
突然停药后几小时即产生戒断症状(关节痛、心动过速、发热、焦虑)，再给药后即缓解。
【禁忌症】
通过胎盘可能会引起新生儿肌肉松软综合征。
重症肌无力、妊娠期妇女及对苯二氮卓类过敏者禁用；有严重器质性脑损伤、严重呼吸功能不全或一般状况差的患者慎用；服药后 4～6h内不宜驾驶车辆。
【药物相互作用】
①本身无镇痛作用，但与氟烷、恩氟烷合用时可降低其 MAC(最低肺泡有效浓度)。
②与氯胺酮合用可减少氯胺酮用量并减轻其不良反应。
③可增强非去极化肌松药的作用。
阿司匹林可缩短咪达唑仑诱导麻醉的时间，可能是由于竞争血浆蛋白结合点所致；咪达唑仑与红霉素同用，其血浆峰浓度升高；环孢素能抑制咪达唑仑的代谢，但环孢素用于抑制移植排斥反应的浓度很低，不足以发生相互作用；雷尼替丁可增加口服单剂量咪达唑仑的生物利用度，增强其镇静作用。咪达唑仑和甲己酮、丙酚也能发生协同作用；与芬太尼或舒芬太尼同用，可引起严重呼吸抑制及突然低血压，因而这些药合用时应严密监测血药浓度，并且适当减少剂量。

【原产地英文商品名】Midazolam 15mg x 20 pills
【原产地英文药品名】Dormicum
【中文参考商品译名】
注：以下产品是不同的规格和价格，购买时请以电话咨询为准！
·咪唑安定 15毫克/片 20片/盒
·咪唑安定 15毫克/片 30片/盒
【中文参考药品译名】Dormicum
【生产厂家中文参考译名】罗氏
【生产厂家英文名】Roche

Midazolam Indications Benzodiazepines are not recommended for the primary treatment of psychotic illness. Benzodiazepines should not be used alone to treat depression or anxiety associated with depression (suicide may be precipitated in such patients).

Severe hepatic impairment.

Insufficient data are available on midazolam to assess its safety during pregnancy. If the product is prescribed to a woman of childbearing potential, she should be warned to contact her physician regarding discontinuance of the product if she intends to become or suspects that she is pregnant.

If, exceptionally, it is considered by a physician that administration of the medicinal product during the last three months of pregnancy or during labour is essential, effects on the neonate such as hypothermia, hypotonia and moderate respiratory depression, can be expected, due to the pharmacological action of the product.

Moreover, infants born to mothers who took benzodiazepines chronically during the latter stages of pregnancy may have developed physical dependence and may be at some risk for developing withdrawal symptoms in the postnatal period.

Midazolam is excreted in breast milk. Do not use during lactation. This product is not suitable for use in children.

Midazolam (pronounced /mɪˈdæzəlæm/, and marketed in English-speaking countries under brand names Dormicum, Hypnovel, and Versed) is a short-acting drug in the benzodiazepine class that is used for treatment of acute seizures and for inducing sedation and amnesia before medical procedures. It has potent anxiolytic, amnestic, hypnotic, anticonvulsant, skeletal muscle relaxant, and sedative properties. Midazolam has a fast recovery time and is the most commonly used benzodiazepine as a premedication for sedation; less commonly it is used for induction and maintainance of anesthesia. Flumazenil is a benzodiazepine antagonist drug that can be used to treat an overdose of midazolam as well as to reverse sedation. However, flumazenil can trigger seizures in mixed overdoses and in benzodiazepine dependent individuals so is not used in most cases.

Administration of midazolam by nose or the buccal route (absorption via the gums and cheek) as an alternative to rectally administered diazepam is becoming increasingly popular for the emergency treatment of seizures in children.Midazolam is also used for endoscopy procedural sedation and sedation in intensive care. The anterograde amnesia property of midazolam is useful for premedication before surgery to inhibit unpleasant memories.Midazolam like other benzodiazepines has a rapid onset of action, high effectiveness and low toxicity level. Drawbacks of midazolam include drug interactions, tolerance, withdrawal syndrome as well as adverse events including cognitive impairment and sedation.Paradoxical effects occasionally occur and are most common in children, the elderly,and particularly after intravenous administration.

History
Midazolam is among about 35 benzodiazepines which are currently used medically, and was synthesised in 1975 by Walser and Fryer at Hoffmann-LaRoche, Inc in the United States. Owing to its water solubility, it was found to be less likely to cause thrombophlebitis than similar drugs. The benzodiazepine drug alprazolam was syntheseised in 1976 from midazolam and introduced to the United States Market in 1981.The anticonvulsant properties of midazolam were studied in the late 1970's, but it was not until the 1990s that it emerged as an effective treatment for convulsive status epilepticus. As of 2010[update], it is the most commonly used benzodiazepine in anesthetic medicine.In acute medicine, midazolam has become more popular than other benzodiazepines such as lorazepam and diazepam, because it is shorter lasting, is more potent, and causes less pain at the injection site. Midazolam is also becoming increasingly popular in veterinary medicine due to its water solubility.

Indications
Intravenous midazolam is indicated for procedural sedation (often in combination with an opioid, such as fentanyl), for pre-op sedation, for the induction of general anesthesia, and for sedation of ventilated patients in critical care units.Midazolam is superior to diazepam in impairing memory of endoscopy procedure but propofol has a quicker recovery time and a better memory impairing effect. It is the most popular benzodiazepine in the intensive care unit (ICU) because of its short elimination half life combined with its water solubility and its suitability for continuous infusion. However, for long-term sedation lorazepam is prefered due to its long duration of action,and propofol has advantages over midazolam when used in the ICU for sedation such as shorter weaning time and earlier tracheal extubation.There is evidence that buccal and intranasal midazolam is easier to administer and more effective than rectally administered diazepam in the emergency control of seizures.Midazolam is sometimes used to alleviate agitation, restlessness or anxiety at low doses during palliative care.Midazolam is considered a first line agent in palliative continuous deep sedation therapy during the last weeks of life when it is necessary to alleviate intolerable suffering unresponsive to other treatments.Midazolam is also sometimes used in neonates who are receiving mechanical ventilation, although morphine is prefered owing to its better safety profile for this indication.

Oral midazolam is indicated for the short term treatment of moderately severe insomnia in patients who have not reacted adequately to other hypnotics, and who have persistent trouble in falling asleep. Because of midazolam's extremely short duration, midazolam is not used for patients who have trouble staying asleep through the night; moderate to long acting benzodiazepines like temazepam, nitrazepam, flunitrazepam and lormetazepam are used for those purposes. Like other benzodiazepines, midazolam produces a decrease in delta activity, though the effect of benzodiazepines on delta may not be mediated via benzodiazepine receptors. Delta activity is an indicator of depth of sleep within non-REM sleep; it is thought to reflect sleep quality, with lower levels of delta sleep reflecting poorer sleep. Thus midazolam and other benzodiazepines cause a deterioration in sleep quality. Cyproheptadine may be superior to nitrazepam in the treatment of insomnia as it enhances sleep quality based on EEG studies.

Midazolam in combination with an antipsychotic drug is indicated for the acute management of schizophrenia when it is associated with aggressive or out of control behaviour. It is also is sometimes used for the acute management of seizures such as status epilepticus. Long-term use for the management of epilepsy is not recommended however, due to the significant risk of tolerance (which renders midazolam and other benzodiazepines ineffective) and the significant side effect of sedation. A benefit of midazolam is that in children it can be administered buccally or intranasally at home or at school for emergency control of acute seizures including status epilepticus. Midazolam is effective for refractory status epilepticus and has advantages of being water soluble, having a rapid onset of action and not causing metabolic acidosis from the propylene glycol vehicle which occurs with other benzodiazepines. Drawbacks include a high degree of breakthrough seizures—due to the short half life of midazolam—in over 50 percent of people treated as well as treatment failure in 14-18 percent of people with refactory status epilepticus. Tolerance develops rapidly to the anticonvulsant effect and the dose may need to be increased by several times to maintain anticonvulsant therapeutic effects. With prolonged use tolerance and tachyphylaxis can occur and the elimination half-life may increase, up to days.