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部分中文溴西泮处方资料（仅供参考）

英文名称：Lexotan 　　

中文名称：立舒定

化学名称：7-Bromo-1,3-dihydro-5-(pyridin-2-yl)-2H-1,4-benzodiazepin-2-one
　　
名词解释：适应症为焦虑状态（急性紧张和焦虑状态，人际间接触困难，激越躁动，失眠，焦虑，激昂性抑郁反应）。Lexotan也是門診中常使用的藥品，在低劑量的時候，Lexotan可以選擇性的降低緊張和焦慮，如果高劑量的時候，則會顯現正靜和肌肉鬆弛作用的特性。
 
適應症：焦慮狀態(急性緊張和焦慮狀態，人際間接觸困難，激越躁動，失眠，焦慮，激昂性抑鬱反應）

副作用：疲勞、嗜睡、肌肉衰弱、情感麻木、警覺性降低、混亂、頭痛、暈眩、步態不穩、複視…等

注意事項：
benzodiazepines或類benzodiazepine藥品的使用，可能會導致這些藥物的生理或心理性依賴。
一旦生理性依賴產生，中止治療時將會伴隨有戒斷症狀的發生。包括頭痛、肌肉疼痛、極度焦慮、緊張、不寧、混亂和易激性。在嚴重情況時，可能會發生以下症狀：脫離解化、脫人格化、過急性、麻痺、四肢刺痛、對光線’聲響和肢體接觸過敏、幻覺或癲癇發作。
對重症肌無力的病人給予Bromazepam時，如果病人先前已存在肌肉衰弱，應加以留意。
對慢性呼吸機能不全的病人，由於Bromazepam可能有呼吸抑制的危險性，應特別小心注意。

禁忌：
Bromazepam不應使用於已知對benzodiazepines過敏、嚴重呼吸機能不全、嚴重肝功能不全（benzodiazepines並不適用於治療患有嚴重肝功能不全的病人，因為他們可能會引起腦病變）或睡眠無呼吸症候群的病人。
Benzodiazepines並不建議使用於精神疾病的第一線治療。
對於已知或懷疑可能對酒精、藥物或毒品依賴的病人，除非在極罕見的情況下，由醫療專業監督下，否則不應該給予benzodiazepines。

Bromazepam  
Bromazepam (marketed under several brand names, including Lectopam, Lexotan, Lexilium, Lexaurin, Brazepam, Bromaze, and Lexotanil)[1] is a benzodiazepine derivative drug, developed in the 1970s.[2][3] It has mainly anxiolytic and at higher doses also sedative, hypnotic and skeletal muscle relaxant properties.[4]

Systematic (IUPAC) name
9-bromo-6-pyridin-2-yl- 2,5-diazabicyclo [5.4.0]undeca- 5,8,10,12-tetraen- 3-one

Indications
Short-term treatment of anxiety or panic attacks, if a benzodiazepine is required.[5]
Premedication to alleviate anxiety before surgery.[6]

Side-effects
All common side-effects of benzodiazepines have been noted. Consult the article under diazepam. Bromazepam 3 times 6 mg daily for 2 weeks taken alone impaired learning capacities significantly in humans in an experiment. In combination with alcohol the impairments of learning capacity became even more pronounced.[7] Impairments to memory functions are common with bromazepam and include a reduced working memory and reduced ability to process environmental information.[8][9][10] Impaired memory, visual information processing and sensory data and impaired psychomotor performance.[11][12][13] Deterioration of cognition including attention capacity and impaired co-ordinative skills.[14][15] Unsteadiness after taking bromazepam is however less pronounced than other benzodiazepines such as lorazepam.[16] Impaired reactive and attention performance, which may impair driving skills.[17]

Drowsiness and decrease in libido.[18][19] Occasionally benzodiazepines can induce extreme alterations in memory such as anterograde amnesia and amnesic automatism which may have medico-legal consequences. Such reactions usually only occur at the higher dose end of the prescribing spectrum.[20]

Very rarely dystonia can develop.[21]

Up to 30% treated on a long-term basis develop a form of dependence, i.e. these patients cannot stop the medication without experiencing physical and/or psychological benzodiazepine withdrawal symptoms.

Leukopenia and liver-damage of the cholostatic type with or without jaundice (icterus) have additionally been seen; the original manufacturer Roche recommends regular laboratory examinations to be performed routinely.

Ambulatory patients should be warned that Bromazepam may impair the ability to drive vehicles and to operate machinery. The impairment is worsened by consumption of alcohol, because both act as central nervous system depressants. During the course of therapy, tolerance to the sedative effect usually develops.

Tolerance, dependence and withdrawal
Bromazepam shares with other benzodiazepines the risk of abuse, misuse, psychological dependence and/or physical dependence.[22][23] A withdrawal study demonstrated both psychological dependence and physical dependence on bromazepam including marked rebound anxiety after 4 weeks chronic use. Those whose dose was gradually reduced experienced no withdrawal.[24]

Patients treated with bromazepam for generalised anxiety disorder were found to experience withdrawal symptoms such as a worsening of anxiety, as well as the development of physical withdrawal symptoms when abruptly withdrawn from bromazepam.[25] Abrupt or over rapid withdrawal from bromazepam after chronic use even at therapeutic prescribed doses may lead to a severe withdrawal syndrome including status epilepticus and a condition resembling delerium tremens.[26][27][28]

Animal studies have shown that chronic administration of diazepam or bromazepam causes a decrease in spontaneous locomotor activity and the turnover of noradrenaline and dopamine and serotonin, decreased activity of tyrosine hydroxylase and increased levels of the catecholamines. During withdrawal of bromazepam or diazepam a fall in tryptophan, 5-hydroxytryptamine levels occurs as part of the benzodiazepine withdrawal syndrome.[29]

Contraindications and special precautions
Benzodiazepines require special precaution if used in the elderly, pregnancy, children, alcohol- or drug-dependent individuals and individuals with comorbid psychiatric disorders.[30]

Special Populations Elderly
In 1987, a team of scientists led by Ochs reported that the elimination half-life, peak serum concentration, and serum free fraction are significantly elevated and the oral clearance and volume of distribution significantly lowered in elderly subjects.[31] The clinical consequence is that the elderly should be treated with lower doses than younger patients.

Driving
Bromazepam may affect driving and ability to operate machinery.[32]

Pregnancy and breast feeding
Bromazepam is pregnancy category D, a classification which means that bromazepam has been shown to cause harm to the unborn child. The Hoffman LaRoche product information leaflet warns against breast feeding while taking bromazepam. There has been at least one report of sudden infant death syndrome linked to breast feeding while consuming bromazepam.[33][34]

Interactions
Cimetidine, fluvoxamine and propranolol causes a marked increase in the half life of bromazepam leading to increased accumulation of bromazepam.[35][36][37]

Pharmacology
Bromazepam is a "classical" benzodiazepine; other classical benzodiazepines include; diazepam, clonazepam, oxazepam, lorazepam, nitrazepam, flurazepam and clorazepate.[38] Its molecular structure is composed of a diazepine connected to a benzene ring and a pyridine ring, the benzene ring having a bromine atom attached to it.[39] It is a 1,4-benzodiazepine, which means that the nitrogens on the seven-sided diazepine ring are in the 1 and 4 positions.

Bromazepam binds to the GABA receptor GABAA, causing a conformational change and increasing inhibitory effects of GABA. Other neurotransmitters are not influenced. Bromazepam is intermediate-short acting benzodiazepine and is lipophilic, is metabolised hepatically via oxidative pathways.[40] It does not possess any antidepressant or antipsychotic qualities.[41]

After night time administration of bromazepam a highly significant reduction of gastric acid secretion occurs during sleep followed by a highly significant rebound in gastric acid production the following day.[42]

Bromazepam alters electrical status of the brain causing an increased beta activity and a decrease in alpha activity in the EEG recordings.[43]

Pharmacokinetics
Bromazepam is reported to be metabolized by a hepatic enzyme belonging to the Cytochrome P450 family of enzymes. In 2003, a team led by Dr. Oda Manami at Oita Medical University reported that CYP3A4 was not the responsible enzyme, seeing as itraconazole, a known inhibitor of CYP3A4, did not effect its metabolism.[44] In 1995, J. van Harten at Solvay Duphar B.V.'s Department of Clinical Pharmacology in Weesp reported that fluvoxamine, which is a potent inhibitor of CYP1A2, a less potent CYP3A4 inhibitor, and a negligible inhibitor of CYP2D6, does inhibit its metabolism.[45]

The active metabolite of bromazepam is hydroxybromazepam, which has half life approximately equal to bromazepam.[citation needed]

Overdose
Main article: Benzodiazepine overdose
Bromazepam is commonly involved in drug overdoses.[46] Bromazepam is a drug sometimes used in suicide attempts.[47] A severe bromazepam benzodiazepine overdose may result in a alpha pattern coma type.[48] The toxicity of bromazepam in overdosage increases when combined with other CNS depressant drugs such as alcohol or sedative hypnotic drugs.[49] Bromazepam is the most common benzodiazepine involved in intentional overdoses in France.[50]

Drug misuse
See also: Benzodiazepine drug misuse

Bromazepam has a similar misuse risk as other benzodiazepines such as diazepam.[51] In France car accidents involving psychotropic drugs in combination found benzodiazepines, mainly diazepam, nordiazepam, and bromazepam, to be the most common drug, almost twice that of the next most common drug cannabis.[52] Bromazepam has also been used for serious criminal offences including, robbery, homicide and to carry out sexual assaults.[53][54][55]

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 详细处方信息以本药内容附件PDF文件（2010102723423322.pdf）的“原文Priscribing Information”为准
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2010-10-28更新