设为首页 加入收藏

TOP

Lendormin Tablets(Brotizolam)溴噻二氮卓片
药店国别  
产地国家 德国 
处 方 药: 是 
所属类别 0.25毫克/片 30片/盒 
包装规格 0.25毫克/片 30片/盒 
计价单位: 盒 
生产厂家中文参考译名:
勃林格殷格翰公司
生产厂家英文名:
Boehringer Ingelheim
该药品相关信息网址1:
http://m.pharmer.org/category/tags/lendormin
该药品相关信息网址2:
该药品相关信息网址3:
原产地英文商品名:
Lendormin 0.25mg/Tablets 30Tablets/box
原产地英文药品名:
Brotizolam
中文参考商品译名:
Lendormin片 0.25毫克/片 30片/盒
中文参考药品译名:
溴噻二氮卓
曾用名:
嗅替唑仑
简介:

 

部份中文溴噻二氮卓处方资料(仅供参考)
【药理与适用症】
嗅替唑仑具催眠、抗激动、抗惊厥、肌肉松弛等作用。低剂量时具有良好的催眠效果,可缩短入睡时间,减少醒觉次数,延长总睡眠时间。口服后迅速被吸收,0.5~2小时达峰浓度。血浆蛋白结合率高,约为89%、95%。t1/2为3.6~7.9小时。经肝脏代谢,大部分自肾脏排出。临床适用于治疗失眠症。
【用法与用量】
口服:失眠症推荐剂量为0.25mg,睡前服。老年人0.125mg。术前催眠0.5mg。
【性状】
嗅替唑仑为无色结晶,熔点212~214℃
【副作用与毒性】
1.不良反应偶见胃肠道不适、头痛、眩晕,高血压患者血压下降。大剂量用药时(尤其对嗅替唑仑敏感的患者),可见次晨乏力,注意力不集中。
2.嗅替唑仑可能产生耐药性或进展性健忘。
3.禁用于对苯二氮卓类过敏者,重症肌无力、精神病、急性闭角型青光眼、急性呼吸功能不全、肝功能不良等患者及妊娠、哺乳期妇女、18岁以下青少年。
4.与中枢抑制药、抗组胺药、巴比妥类药同服时,可增加嗅替唑仑作用。

Brotizolam (marketed under brand name Lendormin) is a sedative-hypnotic thienodiazepine drug which is a benzodiazepine analog. It possesses anxiolytic, anticonvulsant, hypnotic, sedative and skeletal muscle relaxant properties, and is considered to be similar in effect to short-acting benzodiazepines such as triazolam. It is used in the short term treatment of severe or debilitating insomnia. Brotizolam is an extremely potent drug and has shown anti-anxiety activity at doses as low as 80 to 100 micrograms, but the usual hypnotic dose of brotizolam is 0.125 to 0.25 milligrams, and it is rapidly eliminated with an average half-life of 4.4 hours (range 3.6 - 7.9 hours).
The drug was developed by a team led by T Nishiyama while working for Takeda Chemical Industries in 1976 in Japan.
Brotizolam is not approved for sale in the UK, United States or Canada. It is approved for sale in the Netherlands, Germany, Belgium, Austria, Portugal, Israel, Italy and Japan.
Indications -
Insomnia. Brotizolam is prescribed for the short term treatment, 2 – 4 weeks only of severe or debilitating insomnia. Insomnia can be described as a difficulty falling asleep, frequent awakening, early awakenings or a combination of each. Brotizolam is a short-acting benzodiazepine and is sometimes used in patients who have difficulty in maintaining sleep or getting to sleep. Hypnotics should only be used on a short term basis or in those with chronic insomnia on an occasional basis.
Premedication. Brotizolam, in a dose of 0.25 mg can be used as a premedication prior to surgery, this dose was found to be comparable in efficacy to 2 mg flunitrazepam as a premedicant prior to surgery.
Side effects -
Common side effects of brotizolam are typical of hypnotic benzodiazepines and are related to CNS depression, and include somnolence, ataxia, headache, anterograde amnesia, dizziness, fatigue, impairment of motor functions, slurred speech, confusion, and clumsiness.
Less common side effects include hypotension, respiratory depression, hallucinations, nausea and vomiting, palpitations, and paradoxical reactions (i.e. aggression, anxiety, violent behavior, etc.).
Brotizolam can cause residual side effects the next day such as impaired cognitive and motor functions as well as drowsiness. Disruption of sleep patterns may also occur such as suppression of REM sleep. These side effects are more likely to when taken in higher doses (above 0.5–1 mg).
In clinical trials brotizolam 0.125 to 0.5 mg improved sleep in insomniacs similarly to nitrazepam 2.5 and 5 mg, flunitrazepam 2 mg and triazolam 0.25 mg, whilst brotizolam 0.5 mg was shown to be superior to flurazepam 30 mg, but inferior to temazepam 30 mg in some studies. Brotizolam at dosages below 0.5 mg at night usually produced minimal morning drowsiness; no residual impairment of psychomotor performance occurs following dosages within the recommended range of 0.125 to 0.25 mg. No serious side effects have been reported to date and the most frequently observed adverse experiences are drowsiness, headache and dizziness. Mild rebound insomnia may occur in some patients when treatment is stopped.
Pharmacology -
Brotizolam has been shown in animal studies to be a very high potency benzodiazepine, and it may be the most potent benzodiazepine used on humans. Although further studies need to be done to confirm this. The elimination half-life of brotizolam is 3–6 hours. It is absorbed rapidly after administration; after administration it is metabolised into active metabolites, one of which is far less potent than brotizolam and the other is only present in very small amounts in the blood and thus the metabolites of brotizolam do not have any pharmacological effect in humans. Brotizolam induces impairment of motor function and has hypnotic properties.
Brotizolam increases the slow wave light sleep (SWLS) in a dose-dependent manner whilst suppressing deep sleep stages. Less time is spent in stages 3 and 4 which are the deep sleep stages when benzodiazepines such as brotizolam are used. Benzodiazepines are therefore not good hypnotics in the treatment of insomnia. The suppression of deep sleep stages by benzodiazepines may be especially problematic to the elderly as they naturally spend less time in the deep sleep stage.
Abuse -
See also: Benzodiazepine drug misuse
Brotizolam is a drug with a potential for abuse. Drug misuse is defined as taking the drug to achieve a 'high', or continuing to take the drug in the long term against medical advice.
 Abuse of brotizolam, although not widespread, was a problem in Hong Kong back in the late 1980s and 1990s. To control benzodiazepine abuse in Hong Kong, the Government's Pharmacy and Poisons Board reclassified benzodiazepines as Dangerous Drugs in October 1990. Apart from formal prescriptions, detailed records were then required for the supply and dispensing of these drugs. These regulations were applied initially only to brotizolam, triazolam and flunitrazepam as they were the major benzodiazepines of abuse. The impact of these regulatory changes on benzodiazepine use has been studied by analyzing the sales patterns of seven benzodiazepines between 1990-1993. In 1991, the sales of flunitrazepam and triazolam fell, but the sales of five unrestricted benzodiazepines increased. Particular problems arose with the trafficking and abuse of nimetazepam and the abuse of temazepam within that same year in 1991. The regulations that were originally only applied to brotizolam, triazolam and flunitrazepam were now being extended to include all benzodiazepines by January 1992. A regulation requiring the use of proper prescriptions and detailed records for the supply and dispensing of benzodiazepines, appears to have curbed, at least partially, their abuse in Hong Kong. There is still some problems with temazepam, nimetazepam, triazolam, and brotizolam but it is not major.

】【打印繁体】【投稿】【收藏】 【推荐】【举报】【评论】 【关闭】 【返回顶部
分享到QQ空间
分享到: 
上一篇Provigil tablets 100mg(modafin.. 下一篇Seroxat CR Tablets 25mg(paroxet..

相关栏目

最新文章

图片主题

热门文章

推荐文章