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二钾氯氮Clorazepate Dipotassium(氯卓酸钾)

[ 人气:86 | 日期: 2022-05-09 | 返回 | 打印 ]
二钾氯氮Clorazepate Dipotassium(氯卓酸钾)
药品名称:二钾氯氮Clorazepate Dipotassium(氯卓酸钾)
药品别名:安定羧酸钾盐,氯氮卓二钾,氯草酸二钾,Belseren,DikaliiClorazepas,Tranxeneo(氯卓酸钾)
英 文 名:Clorazepate Dipotassium
药品价格:HK$ 美国市场售价 34.87 美元
研发公司:迈蓝(MYLAN)制药公司
适 用 症:治疗抗焦虑、抗惊厥、镇静催眠,以及缓解急性酒精戒断综合症。
型号规格:有3.75mg/7.5mg/15mg三种规格,每瓶100片。
药品详情:

二钾氯氮Clorazepate Dipotassium(氯卓酸钾)简述】
 
    二钾氯氮又名安定羧酸钾盐,氯氮卓二钾,氯草酸二钾,Belseren,DikaliiClorazepas,Tranxeneo(氯卓酸钾),英文名Clorazepate Dipotassium,是一类具有强镇静催眠作用的精神类药品。

二钾氯氮Clorazepate Dipotassium(氯卓酸钾)_香港济民药业

二钾氯氮Clorazepate Dipotassium(氯卓酸钾)_香港济民药业

二钾氯氮Clorazepate Dipotassium(氯卓酸钾)_香港济民药业
 
【二钾氯氮Clorazepate Dipotassium(氯卓酸钾) 适应症】
 
    二钾氯氮Clorazepate Dipotassium(氯卓酸钾)治疗抗焦虑、抗惊厥、镇静催眠,以及缓解急性酒精戒断综合症。
 
【二钾氯氮Clorazepate Dipotassium(氯卓酸钾) 规格】
 
    本品为片剂,有3.75mg/7.5mg/15mg三种规格,每瓶100片。
 
【二钾氯氮Clorazepate Dipotassium(氯卓酸钾) 服用方法】
 
    1.成人常用量:①抗焦虑。一次7.5~15mg,每日2~4次,或每晚睡前顿服15mg。②用于酒精戒断综合征,首次口服30mg,然后15mg,每日2~4次,以后逐步减量。③抗惊厥,初量7.5mg,每日3次,需要时每周增加7.5mg,每日剂量最大不超过90mg。年老体弱者减量。
 
    2.小儿常用量:抗惊厥,9~12岁,首次7.5mg, 每日2次,以后每周增加7.5mg, 每日总量不超过60mg。12岁以上同成人。
 
【二钾氯氮Clorazepate Dipotassium(氯卓酸钾) 注意事项】
 
    1.对某一苯二氮卓类药过敏者,对其他同类药也可能过敏。
 
    2.本类药大都可以通过胎盘。除用作抗癫痫外,在此期间尽量勿用。孕妇长期使用可引起依赖,使新生儿呈现撤药症状。在妊娠最后数周用于催眠,可使新生儿中枢神经活动有所抑制,在分娩前或分娩时使用本类药,可导致新生儿肌张力软弱。
 
    3.苯二氮卓类药对小儿特别是幼儿的中枢神经异常敏感,新生儿不易将本类药代谢为无活性的产物,因此中枢神经可持久的抑制。
 
    4.老年人的中枢神经对本类药也较敏感,静注亦可出现呼吸暂停、低血压、心动过缓甚至心跳停止。
 
    5.下列情况应慎用:①中枢神经系统处于抑制状态的急性酒精中毒;②昏迷或休克时注射地西泮可延长清除半衰期;③有药物滥用或成瘾史;④癫痫患者突然停药可导致发作;⑤肝功能损害可延长清除半衰期;⑥运动过多症,可发生药效反常;⑦低蛋白血症,可导致患者嗜睡,尤其是氯氮卓和地西泮;⑧严重的精神抑郁可使病情加重,甚至产生自杀倾向,应采取预防措施,但阿普唑仑例外;⑨伴呼吸困难的重症肌无力患者的病情可加重;⑩急性或隐性发生闭角型青光眼发作,因本类药可能有抗胆碱效应;⑾严重慢性阻塞性肺部病变,可加重通气衰竭;⑿肾功能损害可延迟本类药的清除半衰期。⒀超量体征有:持续的精神紊乱,嗜睡深沉,震颤,持续的说话不清,站立不稳,心动过缓,呼吸短促或困难,严重的肌无力。本类药没有特效的拮抗药,遇有超量或中毒,宜及早进行对症处理,包括催吐或洗胃等,以及呼吸和循环方面支持疗法;如有兴奋异常,不能用巴比妥类药,以免中枢性兴奋加剧或延长中枢神经系统的抑制。
 
【二钾氯氮Clorazepate Dipotassium(氯卓酸钾) 不良反应】
 
    1.较少见的不良反应有:精神错乱、情绪抑郁、头痛、恶心、呕吐、排尿障碍等。老年、体弱、幼儿、肝病和低蛋白血症患者,对本类药的中枢性抑制较敏感。注射给药时容易引起呼吸抑制、低血压、肌无力、心动过缓或心跳停止。高龄衰老、危重、肺功能不全以及心血管功能不稳定等患者,静注过速或与中枢抑制药合用时,发生率更高,情况也更严重。
 
    2.突然停药后要注意可能发生撤药症状。一般半衰期短或中等的本类药,停药后2~3天出现,半衰期长者则在停药后10~20天发生。撤药症状中,较多见的为睡眠困难,异常的激惹状态和神经质;较少见的或罕见的有腹部或胃痉挛、精神错乱、惊厥、肌肉痉挛、恶心或呕吐、颤抖和多汗。严重的撤药症状多见于长期服用过量的患者;也有曾在连续服用,血药浓度一直保持在安全有效范围内,几个月后突然停药而发生。失眠反跳现象、神经质、激惹,多数见于长时期单次夜间服药,撤药后发生。半衰期短的停药后发生快而严重的撤药反应。
 
【二钾氯氮Clorazepate Dipotassium(氯卓酸钾) 生产厂家】
 
    二钾氯氮Clorazepate Dipotassium(氯卓酸钾)由迈蓝(MYLAN)制药公司研发生产。

 
Tranxen(Clorazepate Dipotassium)

 
Clorazepate, sold under the brand names Tranxene among others, is a benzodiazepine medication. It possesses anxiolytic, anticonvulsant, sedative, hypnotic, and skeletal muscle relaxant properties. Clorazepate is an unusually long-lasting benzodiazepine and serves as a majoritive prodrug for the equally long-lasting desmethyldiazepam, which is rapidly produced as an active metabolite. Desmethyldiazepam is responsible for most of the therapeutic effects of clorazepate.[1]
 
It was patented in 1965 and approved for medical use in 1967.[2]
 
Medical uses
 
Clorazepate is used in the treatment of anxiety disorders and insomnia. It may also be prescribed as an anticonvulsant or muscle relaxant.[3] It is also used as a premedication.[4]
Clorazepate is prescribed principally in the treatment of alcohol withdrawal and epilepsy, although it is also a useful anxiolytic because of its long half-life. The normal starting dosage range of Clorazepate is 15 to 60 mg per day. The drug is to be taken two to four times per day. Dosages as high as 90 to 120 mg per day may be used in the treatment of acute alcohol withdrawal. In the United States and Canada, Clorazepate is available in 3.75, 7.5, and 15 mg capsules or tablets. In Europe, tablet formations are 5 mg, 10 mg, 20 mg and 50 mg.[5] Clorazepate SD (controlled release) is available and may have a reduced incidence of adverse effects. The sustained-release formulation of clorazepate has some advantages in that, if a dose is missed, less profound fluctuations in blood plasma levels occur, which may be helpful to some people with epilepsy at risk of break-through seizures.[6]
 
Contraindications
 
Benzodiazepines require special precaution if used in the elderly, children, alcohol- or drug-dependent individuals and individuals with comorbid psychiatric disorders.[9]
 
Chlorazepate if used late in pregnancy, the third trimester, causes a definite risk a severe benzodiazepine withdrawal syndrome in the neonate with symptoms including hypotonia, and reluctance to suck, to apnoeicspells, cyanosis, and impaired metabolic responses to cold stress. Floppy infant syndrome and sedation in the newborn may also occur. Symptoms of floppy infant syndrome and the neonatal benzodiazepine withdrawal syndrome have been reported to persist from hours to months after birth.[10]
 
Special precaution is required when using clorazepate in the elderly because the elderly metabolise clorazepate more slowly, which may result in excessive drug accumulation. Additionally the elderly are more sensitive to the adverse effects of benzodiazepines compared to younger individuals even when blood plasma levels are the same. Use of benzodiazepines in the elderly is only recommended for 2 weeks and it is also recommended that half of the usual daily dose is prescribed.[6]
 
Adverse effects
 
Adverse effects of clorazepate include, tolerance, dependence, withdrawal reactions, cognitive impairment, confusion, anterograde amnesia, falls in the elderly, ataxia, hangover effects, and drowsiness. It is unclear whether cognitive deficits resulting from the long-term use of benzodiazepines return to normal or persist indefinitely after withdrawal from benzodiazepines. Benzodiazepines are also known to cause or worsen depression. Paradoxical effects including excitement and paradoxical worsening of seizures can sometimes result from the use of benzodiazepines. Children, the elderly, individuals with a history of alcohol abuse or a history of aggressive behavior and anger are at greater risk of developing paradoxical reactions to benzodiazepines.[6]
 
Tolerance, dependence and withdrawal
 
Delirium has been noted from discontinuation from clorazepate[7] A benzodiazepine dependence occurs in approximately one third of patients who take benzodiazepines for longer than 4 weeks, which is characterised by a withdrawal syndrome upon dose reduction. When used for seizure control, tolerance may manifest itself with an increased rate of seizures as well an increased risk of withdrawal seizures. In humans, tolerance to the anticonvulsant effects of clorazepate occurs frequently with regular use. Due to the development of tolerance, benzodiazepines are, in general, not considered appropriate for the long-term management of epilepsy; increasing the dose may result only in the developing of tolerance to the higher dose combined with worsened adverse effects. Cross-tolerance occurs between benzodiazepines, meaning that, if individuals are tolerant to one benzodiazepine, they will display a tolerance to equivalent doses of other benzodiazepines. Withdrawal symptoms from benzodiazepines include a worsening of pre-existing symptoms as well as the appearance of new symptoms that were not pre-existing. The withdrawal symptoms may range from mild anxiety and insomnia to severe withdrawal symptoms such as seizures and psychosis. Withdrawal symptoms can be difficult in some cases to differentiate between pre-existing symptoms and withdrawal symptoms. Use of high doses, long-term use and abrupt or over-rapid withdrawal increases increase the severity of withdrawal syndrome.[6] However, tolerance to the active metabolite of clorazepate may occur more slowly than with other benzodiazepines.[6] Regular use of benzodiazepines causes the development of dependence characterised by tolerance to the therapeutic effects of benzodiazepines and the development of the benzodiazepine withdrawal syndromeincluding symptoms such as anxiety, apprehension, tremor, insomnia, nausea, and vomitingupon cessation of benzodiazepine use. Withdrawal from benzodiazepines should be gradual as abrupt withdrawal from high doses of benzodiazepines may cause confusion, toxic psychosis, convulsions, or a condition resembling delirium tremens. Abrupt withdrawal from lower doses may cause depression, nervousness, rebound insomnia, irritability, sweating, and diarrhea.[8]
 


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