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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.

 于2010-02-10更新