化学名：3-(5H-Dibenzo[a,d]cyclohepten-5-ylidene)-N,N-dimethylpropan-1-amine hydrochloride

中文名称：盐酸环苯扎林

中文别名：5-(3-二甲氨基丙烯)二苯并[a,e]环庚三烯盐酸盐 

分类名称
一级分类：麻醉药及其辅助药物 二级分类：骨骼肌松弛药 三级分类： 
 
药品别名
胺苯环庚烯、胺苯庚烯、Flexeril、Novo-Cycloprine、Flexiban、Yurelax
 
药物剂型
环苯扎林片剂：10mg/片。
 
药理作用
本品为骨骼肌松弛药，在结构上与三环类抗抑郁药相似，主要作用于中枢神经系统的大脑脑干而非脊髓水平，不作用于神经接头，也不直接作用于骨骼肌，主要作用机制是通过影响γ和α运动系统从而降低强直躯体的运动能力。本品能够减轻局部骨骼肌痉挛，而不影响肌肉功能，对中枢神经系统疾病引起的肌肉痉挛无效。本品亦具有抗胆碱能作用。
 
药动学
本品口服后迅速吸收，存在剂量吸收饱和现象，血药浓度个体差异大，某些患者首关效应较明显，一次剂量作用可维持12～24h。血浆蛋白结合率约93%，给药后约4h达血药浓度峰值，平均生物利用度为55%。在肝脏广泛代谢为葡萄糖醛酸结合物，经肾排泄。本品消除缓慢，半衰期为1～3h。
 
适应证
用于缓解局部肌肉痉挛及其伴随症状，如疼痛、触痛、活动受限以及日常生活行为限制等(作为休息和物理治疗的辅助药)。但本品对脑、脊髓疾病或儿童脑性瘫痪引起的痉挛无效。
 
禁忌证
1.对本品过敏者禁用。
2.2周内服用过单胺氧化酶抑制剂者(可致高热、惊厥甚至死亡)禁用。
3.心肌梗死的急性恢复期、心律失常、心脏传导阻滞或充血性心力衰竭患者禁用。
4.甲状腺功能亢进者禁用。
5.儿童、妊娠期妇女头3个月禁用。
 
注意事项
1.本品可影响患者操作机械或驾车的能力，服用本品期间应避免进行此类工作。
2.在停用单胺氧化酶抑制剂14天后方可开始使用本品治疗。
3.药物过量的表现 过量服用本品时可能产生瞬间幻觉、激惹、过度反射、肌强直、呕吐、高热等。还可引起嗜睡、低体温、心动过速及心律失常(如束支传导阻滞)、充血性心力衰竭、瞳孔放大、抽搐、严重低血压、昏迷或休克等。
4.本品属于三环类药物，需注意长期服用本品后突然停药可能出现戒断症状(如恶心、呕吐、头痛不适)，但是这些反应并非说明本品具有成瘾性。
5.老年患者用药时应监测肾功能。
6.闭角型青光眼及眼内压增高者慎用。
7.前列腺增生或有尿潴留病史者慎用。
8.正接受抗胆碱能药物治疗者慎用。
9.老年患者使用本品时发生中枢神经系统不良反应(如幻觉、惊厥)的危险性增加。本品主要经肾脏排出，因此老年患者应注意用药剂量。
10.哺乳期妇女慎用。
 
不良反应
常见嗜睡、口干和眩晕。少见疲劳、衰弱、恶心、便秘、消化不良、味觉异常、视物模糊、头痛、神经质及谵妄。罕见以下症状：1.心血管系统：心动过速、心律不齐、心悸及低血压。消化系统：呕吐、胃痛、胃肠胀气、腹泻、舌肿胀、肝功能异常、黄疸及胆汁淤积。3.骨骼肌肉：局部肌肉无力。4.神经/精神系统：运动失调、眩晕、构音障碍、震颤、肌张力亢进、惊厥、肌肉抽搐、定向障碍、失眠、情绪沮丧、感觉异常、焦虑、妄想、幻觉、激动及兴奋。5.泌尿系统：尿频和(或)尿潴留。6.皮肤：出汗。7.过敏反应：血管性水肿、颜面浮肿、瘙痒、风疹等。8.其他：晕厥、味觉缺乏及耳鸣。
 
用法用量
口服给药，每次10mg，每日3次。每日剂量不超过60mg，连续服药不超过2～3周。
 
药物相应作用
1.中枢神经系统抑制药(如催眠药、抗焦虑药、抗抑郁药等)可增强本品作用，合用时需密切监控或减少本品用量。
2.抗胆碱药可增强本品的抗胆碱能作用。
3.与曲马朵合用可增加癫痫发作的危险性。
4.本品结构与三环类抗抑郁药类似，而三环类抗抑郁药与单胺氧化酶抑制剂合用可能引起高血压危象、严重惊厥，甚至死亡，因此禁止本品与单胺氧化酶抑制剂合用。
5.氟西汀通过对细胞色素P450肝酶系统的影响而抑制本品的代谢，增加QT间期延长的危险性。
6.本品可降低胍乙啶及同类药物的抗高血压作用。乙醇可增强本品的作用。

【原产地英文商品名】FLEXERIL Generic 5mg/tab 100tabs/bottle
【原产地英文药品名】CYCLOBENZAPRINE HCL
【原产地英文化合物名称】3-(5H-Dibenzo[a,d]cyclohepten-5-ylidene)-N,N-dimethylpropan-1-amine hydrochloride
【中文参考商品译名】
注：以下产品不同规格和不同价格，购买时请以电话咨询服务为准！
·FLEXERIL仿制药 5毫克/片 100片/瓶
·FLEXERIL仿制药 10毫克/片 100片/瓶
【中文参考药品译名】盐酸环苯扎林
【中文参考化合物名称】5-(3-二甲氨基丙烯)二苯并[a,e]环庚三烯盐酸盐

GENERIC NAME: cyclobenzaprine

BRAND NAME: Flexeril, Amrix

DRUG CLASS AND MECHANISM: Cyclobenzaprine is a muscle relaxant. Specifically, cyclobenzaprine relieves muscle spasm when the spasm is due to local problems, that is, in the muscle itself and not in the nerves controlling the muscles. Cyclobenzaprine has no effect on muscle function. Cyclobenzaprine seems to accomplish its beneficial effect through a complex mechanism within the nervous system, probably in the brainstem. The FDA approved cyclobenzaprine in August 1977.

PRESCRIPTION: Yes

GENERIC AVAILABLE: Yes

PREPARATIONS: Tablets: 5 and 10 mg. Capsules (Extended Release): 15 and 30 mg.

STORAGE: Tablets should be stored between 15-30 C (59-86 F).

PRESCRIBED FOR: Cyclobenzaprine is used with rest and physical therapy for short-term relief of muscle spasms associated with acute painful muscle and skeletal conditions. It is only for short-term use, up to two or three weeks.

DOSING: The recommended dose of cyclobenzaprine dose is 5 or 10 mg three times daily using immediate release tablets or 15 or 30 mg once daily using extended release tablets.

DRUG INTERACTIONS: Cyclobenzaprine is chemically related to the tricyclic class of antidepressants (for example, amitriptyline [ Elavil, Endep], nortriptyline [ Pamelor]). As such, it should not be taken with or within two weeks of any monoamine oxidase (MAO) inhibitor, for example, isocarboxazid (Marplan), phenelzine (Nardil), tranylcypromine (Parnate), and procarbazine (Matulane). High fever, convulsions, and even death can occur when these drugs are used together. Additionally, cyclobenzaprine interacts with other medications and drugs that slow the brain's processes, such as alcohol, barbiturates, benzodiazepines (for example, diazepam [Valium], lorazepam [ Ativan]), and narcotics.

PREGNANCY: There are no adequate studies of cyclobenzaprine in pregnant women. However, studies in animals suggest no important effects on the fetus. Cyclobenzaprine therefore can be used in pregnancy if the physician feels that it is necessary.

NURSING MOTHERS: It is not known whether cyclobenzaprine is secreted in milk. However, since it is related to the tricyclic antidepressants, some of which are excreted in breast milk, caution is advised in using this medication in women who are breastfeeding.

SIDE EFFECTS: Common side effects of cyclobenzaprine include drowsiness, dry mouth, fatigue, headaches, and dizziness. Other reported side effects include nausea, constipation, blurred vision, unpleasant taste, nervousness, confusion, acid reflux, and abdominal pain or discomfort. Abrupt cessation after prolonged therapy may cause withdrawal symptoms such as headaches, nausea, and weakness.