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盐酸氯米帕明Anafranil(Clomipramine)

——【安拿芬尼】快速缓解强迫症、抑郁症

2006-03-16 20:00:58  作者:新特药房  来源:新特药房药讯  浏览次数:131  文字大小:【】【】【

通用名称:盐酸氯米帕明   
商品名称:安拿芬尼   
英文名称:Clomipramine   
汉语拼音:Yan Suan Lv Mi Pa Ming
成份
活性成份:盐酸氯米帕明   
分子式:C19H23CIN2. HCL   
分子量:351.32   

性状   
本药为浅黄色圆形双凸面糖衣片,除去糖衣后呈白色。化学名为3-氯-5-[3-(二甲氨基)丙基]-10,11-二氢-5H-二苯[b,f]-氮杂盐酸盐。 
 
药理作用   
本药主要是通过抑制神经元对释放于突触间隙的去甲肾上腺素和5-羟色胺的再摄取,而产生抗抑郁作用,且具有广谱的药理学作用,包括α1-抗肾上腺素、抗胆碱能、抗组织胺和抗5-羟色胺能(5-HT-受体阻滞)等作用。治疗范围广,能改善抑郁综合征的各种表现,特别是缺乏动力,情绪低落,同时对持续存在的焦虑也有作用。 
 
药代动力学   
口服后吸收完全,在药物分布容积和清除率方面个体差异性大,采用推荐的治疗剂量,产生的稳态浓度范围为20-175 ng/mL。蛋白结合率为97.6%;脑脊液中的浓度约相当于血浆浓度的2%。分布容积 :约12 L/kg体重。活性代谢物去甲氯米帕明达到稳定血药浓度的方式与氯米帕明相似。在老年患者,肝脏对本药的代谢作用较弱,故血药浓度较高。β相血浆消除半衰期为21小时。2/3以水溶性结合形式从尿中排出,约1/3从粪便排出。 
 
适应症   
各种病因和症状表现的抑郁状态 :内源性、反应性、神经症性、器质性、隐匿性及更年期性抑郁症。
与精神分裂症和人格障碍伴随的抑郁。
由于早老、神经症性及精神病性的抑郁性心理障碍,包括其相应的躯体表现。
强迫综合征,恐怖症和惊恐发作,伴有发作性睡病的猝倒症,慢性疼痛状态、夜间遗尿(5岁以上,且首先排除可能的器质性病因)。 
 
用法用量   
原则上先使用最小剂量,然后慎重地逐渐增加剂量,特别是对老年及青少年患者。
抑郁症、强迫症和恐怖症 治疗初期 :25 mg/次,每日2-3次,以后的剂量视患者对药物的耐受性逐渐增加,在治疗第1周,每隔2-3天增加25 mg,直至100-150 mg/日;病情严重时,最大剂量可增加到250 mg/日。一旦病情显著改善,则应将剂量调整到维持量,即平均50-100 mg/日。
惊恐发作、旷野恐怖 初期服用10 mg/日,可与苯二氮类药物合用,根据患者对药物的耐受程度来增加剂量以达理想疗效。同时撤用苯二氮类药物。每日所需量差距很大,从25-100 mg不等,如病情需要,可增至150 mg/日,治疗应至少持续6个月,在此期间可逐渐减少维持量。
发作性睡病猝倒症 25-75 mg/日。
慢性疼痛状态 10-150 mg/日。
老年患者初始剂量为10 mg/日,10日内逐步增加剂量到30-50 mg/日,以后维持此量直到治疗结束。
儿童初始用10 mg/日,在10日内,14岁以上的儿童增至50 mg/日或更多;8-14岁儿童用量增至20-50 mg/日;5-7岁儿童增至20 mg/日。
夜间遗尿(限于5岁及5岁以上儿童) 初期剂量 :12岁以上儿童25-75 mg/日;9-12岁儿童25-50 mg/日;5-8岁儿童20-30 mg/日。在用药1周内无充分疗效时,应给予更高剂量。晚饭后一次性给药,但对入睡不久便遗尿的儿童要预先(下午4时)给予部分剂量。获得预期疗效后,应逐渐减少维持量,并继续治疗1-3个月。

不良反应   

嗜睡,短时疲劳,不安感,食欲增加,定向力障碍和幻觉,焦虑,躁狂,攻击行为,记忆损害,失眠,抑郁加重。晕眩、震颤、头痛、肌阵挛,谵妄,语言障碍,感觉异常,肌无力,肌强直。
心血管系统反应如体位性低血压,窦性心动过速,心悸,心电图改变。
胃肠道症状有恶心、呕吐,腹部不适口干、出汗、便秘。
视力调节失调、视物模糊,排尿障碍。偶见热潮红、瞳孔放大。
内分泌系统及代谢失调症状,如溢乳,乳房增大,体重增加,性欲和性功能失调。
皮肤过敏反应,对光敏感,瘙痒。
偶见耳鸣,突然中断治疗时,可能出现戒断症状。
长期使用三环类抗抑郁药可导致龋齿的发病率升高。
由于三环类抗抑郁药的兴奋作用,它可使激越的患者和伴随精神分裂症的患者出现焦虑不安和过度兴奋。
对敏感者及老年患者,三环类抗抑郁药可能会诱发药源性精神病(谵妄),夜间多见。
患有低血压或循环功能不稳定的患者,可能出现血压降低的药物反应。 

禁忌症   
严禁与MAO(单胺氧化酶)抑制剂合用。心肌梗塞急性发作期,对二苯氮类三环抗抑郁药过敏者禁用。 
 
注意事项   
以下疾病患者慎用 :
心血管功能不全,房室传导阻滞,心律不齐。
窄角型青光眼。
由排尿受阻引起的排尿障碍(例如前列腺疾病患者)。
低惊厥阈(如各种病因引起的脑损害癫痫、酒精中毒等)。
严重的肝、肾疾患。
肾上腺髓质肿瘤(黑色素细胞瘤、神经母细胞瘤)。
甲状腺机能亢进或用甲状腺制剂合并治疗的患者,老年人。
长期接受三环类抗抑郁药治疗时应进行肝、肾功能监测。
有双向情感障碍的患者,可能会由抑郁转向轻躁狂或躁狂。对于有自杀危险的患者,治疗期间应严加监控。
本药可影响驾驶和操作机器的能力。 
 
孕妇及哺乳期妇女用药   
妊娠期间应避免使用本药。由于活性物质可进入乳汁,应停止哺乳或停药。 
 
药物相互作用   

本药与MAOI可发生严重的相互作用,如活动过度、高血压危象、高热、痉挛、谵妄、昏迷,必须绝对保证两药之间相隔至少14天。
本药能减少或消除可乐定、胍乙定、倍他尼定、利血平和甲基多巴的抗高血压作用。
可增强拟交感神经药,如肾上腺素、去甲肾上腺素、苯丙胺(滴鼻剂和含拟交感神经作用的局麻药)对心血管的作用。也能增加酒精及其它中枢抑制剂(如巴比妥类、苯二氮类或全身麻醉药),抗胆碱能药物(如阿托品、比哌立登、左旋多巴)的作用。
奎尼丁类抗心律失常药可降低三环抗抑郁药的血浆浓度。
本药与苯妥英合用可引起血清苯妥英浓度的升高。
神经松弛剂、类固醇激素、哌醋甲酯及西咪替丁可升高三环抗抑郁药的血浆浓度。 
 
药物过量   
症状 严重的抗胆碱能反应,一般在服药后0.5-2小时出现。可出现下列症状 :
植物神经系统 :口干、视觉障碍、呕吐、瞳孔放大、出汗、少尿或无尿、发烧、高热。
中枢神经系统 :共济失调、烦躁、激越、反射亢进,肌强直,舞蹈病样及手足徐动症样的运动,惊厥、头晕、木僵、昏迷。锥体及锥体外系症状。
心血管系统 :心动过速或过缓、传导障碍、心律不齐、心功能不全。极罕见心脏停博、休克等情况。
呼吸系统 :呼吸抑制或呼吸停止。
电解质紊乱和酸碱平衡失调。
治疗 如口服应催吐,洗胃,给予活性炭。需连续监护心血管功能数天及给予对症支持治疗。腹膜透析和血液透析无效。 

贮藏/有效期   
有效期5年。 
Anafranil reviewbyPharmacy and Drugs

Anafranil belongs to the family of tricyclic antidepressants and is most commonly used to treat the symptoms of obsessive-compulsive disorders. Generically prescribed as clomipramine, it is also used to treat symptoms related to panic attacks, arm burning and hair pulling and other body abusive disorders, narcoleptic pain, premenstrual syndrome, and phobias.

It is not uncommon for patients to experience suicidal thoughts when first starting Anafranil. While it is vital to avoid alcohol to help minimize these thoughts and behaviors, it is also important to avoid alcohol to avoid the risk of potential seizures.

Anafranil should be taken with food in order to prevent an upset stomach. A patient that is scheduled for a surgical procedure may very well have to come off the medication prior to surgery. Prolonged exposure to the sun may result in severe sunburns, as tricyclic antidepressants increase sensitivity to sunlight and temperature.

There are basic risks that coincide with a medication like Anafranil. It is absolutely vital that a minimum of five weeks has gone by if a patient has been taking an MAO inhibitor or and ACE inhibitor or most types of anti-psychotic medications. Any previous medication associated with mental health may result in a fatal interaction with Anafranil.

Other patients that have certain health issues should not be prescribed this or any other tricyclic antidepressant. Patients with seizure or heart impairment histories, those with a kidney or liver disease, patients who have been diagnosed with bi-polar disorder, and those with glaucoma or difficulty urinating should not use Anafranil.

Overdoses of Anafranil are not only fatal nearly 100% of the time, but they lead to a violent death for the patient. Extreme heart rates and drowsiness is followed by confusion and agitation. Vomiting, blurry vision, and profuse sweating and swelling set in within minutes. Muscle stiffness and difficulty breathing make the patient very uncomfortable, and the blue tint to their fingers and lips are a sign that oxygen is not getting through the body adequately. A coma mercifully sets in shortly after the convulsions begin, and almost always, the final stage is death.

Severe side effects when the medication is taken normally can result in death as well and it is vital that the patient report these symptoms to their physician immediately. Symptoms such as chest pain that spreads down the arm or sudden numbness or weakness that monopolizes one side of the body are signs of heart attacks and strokes. Sudden onset headaches and confusion and a lack of coordination may also be a sign of a stroke. Fainting, pale skin, easy bruising or bleeding, and frequent urination are all serious side effects that require medical attention. The patient should seek immediate medical attention if they experience a fever accompanied with accelerated heart rate, confusion, sweating, and muscle stiffness.

Less serious side effects that can typically be tolerated include nausea, vomiting, and constipation or diarrhea. Dry mouth with an altered taste is common, as is appetite and weight fluctuations. Sleep problems with vivid night terrors occur in about 20% of patients. Sweating, blurry vision, and sexual dysfunction are fairly typical.

The list of dangerously interactive medication is very long and prior to starting any medication, the patient should seek their physician’s advice. Heart and blood pressure medications, anti psychotics, blood thinners, hormones, seizure medications, cold and allergy drugs, Tagamet, phenytoin, and every psychotropic medication are one the list.

For those patients who can withstand the side effects and exercise caution when utilizing other medications, Anafranil can significantly reduce symptoms and return patients to a reasonable quality of life.

Anafranil (clomipramine hydrochloride capsules, USP), is an antiobsessional drug that belongs to the class (dibenzazepine) of pharmacologic agents known as tricyclic antidepressants. Anafranil is available as capsules of 25, 50, and 75 mg for oral administration. Clomipramine hydrochloride is 3-chloro-5- [3-(dimethylamino)propyl] -10,11-dihydro-5H-dibenz [b,f]azepine monohydrochloride. Clomipramine hydrochloride is a white to off-white crystalline powder. It is freely soluble in water, in methanol, and in methylene chloride, and insoluble in ethyl ether and in hexane.

Anafranil has the following structural formula:

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