英文药名: Tegretol(Carbamazepine Suspension)

中文药名: 得理多（卡马西平口服悬浮液）

生产厂家: Novartis

给药说明
 
一级分类：神经系统药物 二级分类：抗癫痫药物 三级分类：其他 
 
药品英文名
Carbamazepine
 
药品别名
氨甲酰苯卓、氨甲酰氮卓、叉癫宁、得利多、得利益多、芬来普辛、甲酰苯卓、卡巴咪唑、卡马咪嗪、卡平、立痛定、痛经宁、痛惊宁、痛可灵、退痛、酰氨咪唑、酰胺咪嗪
 
药物剂型
1.片剂：100mg，200mg，400mg；2.缓释片：200mg，400mg；3.咀嚼片：100mg，200mg；4.胶囊：200mg；5.糖浆：20mg(1ml)；6.栓剂：125mg，250mg。
 
药理作用
卡马西平为钠通道调节剂，其主要作用如下：
1.抗惊厥作用：可能是通过增强钠通道的灭活效能，限制突触后神经元高频动作电位的发放，以及通过阻断突触前钠通道和动作电位发放，阻断神经递质的释放，从而调节神经兴奋性，产生抗惊厥作用。
2.抗外周神经痛作用：可能是通过作用于γ-氨基丁酸(GABA)B受体而产生镇痛效应，并与调节Ca2＋通道有关。
3.抗利尿作用：可能与刺激抗利尿激素(ADH)释放和加强水分在远端肾小管的重吸收有关。
4.抗人格障碍和躁狂抑郁作用：可能与抑制多巴胺和肾上腺素的积蓄有关。
5.抗心律失常作用：本药可轻度延长房室传导、降低4相自动除极电位及延长浦氏纤维的动作电位时间。此外，本药还有膜稳定作用，对室性或室上性早搏均有效，可使症状消除，尤其对伴有慢性心功能不全者疗效更好。
 
药动学
本药口服吸收缓慢，且因人而异。口服本药400mg后4～5h血药浓度达峰值8～10μg/ml，但个体间差异很大，可在0.5～25μg/ml之间变动。本药抗癫痫作用的起效时间相差很大，约经8～72h可缓解三叉神经痛。达到稳态血药浓度的时间为40h(8～55h)，成人的治疗性血药浓度为4～12μg/ml。本药生物利用度为58%～85%，蛋白结合率约为76%。经肝脏代谢，能诱发自身代谢，半衰期平均为12～17h。主要代谢产物10，11-环氧化卡马西平的蛋白结合率为48%～53%，半衰期为5～8h。72%经肾脏排出，28%随粪便排出。
 
适应证
1.癫痫复杂部分性发作(精神运动性发作或颞叶癫痫)、全身强直阵挛性发作、上述两种混合性发作或其他部分性或全身性发作。
2.缓解三叉神经痛、舌咽神经痛、脊髓痨的闪电样痛、糖尿病周围神经痛、患肢痛、外伤后神经痛和某些疱疹后神经痛等神经源性疼痛。
3.预防或治疗躁狂抑郁症；治疗情感性精神分裂症、顽固性精神分裂症及边缘系统功能障碍有关的失控综合征等精神疾病。
4.尿崩症。
5.不安腿综合征(Ekbom综合征)、面肌抽搐。
6.戒酒综合征。
7.心律失常。
 
禁忌证
1.心脏房室传导阻滞者。
2.血小板、血常规及血清铁严重异常者。
3.有骨髓抑制病史者。
4.心、肝、肾功能不全者。
5.孕妇和哺乳期妇女。
6.对本药及三环类抗抑郁药过敏者。
 
注意事项
1.慎用：
(1)酒精中毒者；
(2)心脏疾病患者(包括器质性心脏病和充血性心脏病)；
(3)冠状动脉病患者；
(4)糖尿病患者；
(5)青光眼患者；
(6)对其他药物有血液方面不良反应史者(本药诱发骨髓抑制的危险性增加)；
(7)尿潴留者。
2.药物对老人的影响：老年患者对本药较敏感，可引起精神错乱、激动不安、焦虑、房室传导阻滞或心动过缓。
3.药物对妊娠的影响：本药能透过胎盘屏障，FDA妊娠分类为D类。
4.药物对哺乳的影响：本药可通过乳汁分泌，乳汁中浓度约为血药浓度的60%。
5.药物对检验值或诊断的影响：
(1)血尿素氮、丙氨酸氨基转移酶、天门冬氨酸氨基转移酶、碱性磷酸酶、血清胆红素、尿糖、尿蛋白含量检测值升高；
(2)甲状腺功能试验值降低；
(3)血钙浓度降低。.用药前后及用药时应当检查或监测：
(1)全血细胞计数(包括血小板、网织红细胞)以及血清铁检查。在给药前检查一次，治疗开始后应经常复查达2～3年：
(2)尿常规；
(3)血尿素氮；
(4)肝功能试验；
(5)卡马西平血药浓度测定；
(6)眼科检查(包括裂隙灯、检眼镜和眼压计检查)。
7.本药对癫痫典型或不典型失神发作、肌阵挛或失神张力发作无效，对锂剂、抗精神病药或抗抑郁药无效的或不能耐受的躁狂-抑郁症有效。
8.本药止痛效应限于神经源性疼痛。
9.饭后立即服药，可减少胃肠道反应。
10.服用本药应避免大量饮水，以防导致水中毒反应。
11.服药过程中可出现口渴，糖尿病患者可能引起尿糖增加。
12.开始时应用小剂量，然后逐渐增加，直到获得良好疗效或出现不良反应为止。已用其他抗癫痫药治疗的患者加用本药时，用量也应逐渐增加。在开始治疗的4周左右可能需要增加剂量，以避免由自身诱导所致的血药浓度降低。癫痫患者突然撤药可引起惊厥或癫痫持续状态。
13.遇有下列情况应停药：
(1)有肝脏中毒症状或活动性肝病时应立即停药。
(2)有骨髓抑制的明显证据时应立即停药。但如果癫痫症状只有应用本药才能控制时可考虑减量，密切随访白细胞计数，如白细胞计数逐渐回升，可再加大剂量，以达到控制癫痫发作的剂量。
(3)有心血管方面不良反应或出现皮疹时，应立即停药。
(4)用作特异性疼痛综合征的止痛药时，如果疼痛完全缓解，应每月减量或停药。
14.如发生嗜睡、眩晕、头昏、肌肉软弱或共济失调，需注意是否为中毒先兆。用药过量的症状有无尿、少尿、尿潴留、心血管方面的反应(包括传导阻滞、心律不齐、高血压、低血压、休克)、恶心、呕吐、共济失调、手足徐动及抽搐等，以儿童多见；还可出现反射亢进、运动减少、瞳孔散大、震颤、呼吸抑制。上述过量症状可在过量服药后1～3h内出现。
15.过量的治疗：
(1)需催吐或洗胃；给予药用炭或轻泻药阻止吸收；采取加速排泄的措施，如利尿。仅在严重中毒并有肾哀竭时才有指征进行透析。
(2)小儿严重中毒时可能需要换血，并需持续观察呼吸、心功能、血压、体温、瞳孔反应、肾和膀胱功能数天。如有呼吸抑制，应给氧，并进行机械辅助呼吸，必要时行气管插管。血压下降和休克时，可抬高双下肢、使用血容量扩张剂及升压药。出现惊厥时需用安定或巴比妥类药，但这两类药可能加重呼吸抑制、低血压和昏迷。患者如在过去一周内用过单胺氧化酶抑制药，则不宜用苯巴比妥。

不良反应
1.中枢神经系统：常见视力模糊、复视、眼球震颤、嗜睡。本药还可能激发潜在的精神病、引起老年人精神错乱或激动不安，不良反应发生率随血药浓度的增高而增高。罕见中枢神经毒性反应，表现为说话困难、口齿不清、抑郁、心神不定、强直以及难以解释的幻听、不能控制的躯体运动、幻视等。
2.消化系统：常见口渴、恶心、呕吐；少见严重腹泻；罕见过敏性肝炎，表现为黑尿、粪便颜色变浅、皮肤巩膜黄染等。
3.呼吸系统：罕见过敏性肺炎。
4.心血管系统：罕见心律失常，房室传导阻滞、心动过缓、充血性心力衰竭、水肿、高血压或低血压、血栓性静脉炎、昏厥等。
5.血液系统：罕见再生障碍性贫血，粒细胞减少、全血细胞减少、血小板减少性紫癜、骨髓抑制、淋巴结瘤。
6.内分泌代谢：可见低钠血症，表现为无力、恶心、呕吐、精神错乱、神经系统异常、恍惚以及痫样发作增多等；少见低钙血症，表现为癫痫发作频率增加、肌肉或腹部痉挛；罕见骨质疏松、急性间歇性卟啉症。
7.泌尿生殖系统：罕见肾中毒、急性肾衰竭。国外有导致性功能障碍的报道。
8.皮肤：少见Stevens-Johnson综合征、中毒性表皮坏死溶解症或红斑狼疮样综合征，表现为皮疹、荨麻疹、瘙痒、发热、骨关节痛、疲劳或无力等。
9.其他：罕见腺体瘤、感觉异常和周围神经炎。
 
用法用量
口服给药：
1.抗惊厥：开始时每次100mg，每天2～3次；第二天后每天增加100mg，直到出现疗效为止。维持时应根据情况调整至最低的有效量，分次服用。要注意剂量个体化，最高量每天不超过1200mg。
2.镇痛：开始时每次100mg，每天2次；第二天后隔日增加100～200mg，直至疼痛缓解，维持量为每天400～800mg，分次服用，每天最高剂量不超过1200mg。
3.糖尿病神经病变引起的疼痛：每次200mg，每天2～4次。
4.抗利尿：单用时每天300～600mg；与其他抗利尿药合用，则每天服200～400mg，分3～4次服用。
5.抗躁狂或抗精神病：开始时每天200～400mg，以后每周逐渐增加剂量，通常成年人的限量为1200mg，一般分3～4次服用。少数用至每天1600mg。
6.戒酒综合征：平均剂量为每次200mg，每天3～4次。对严重病例，最初几天的剂量可增加至每次400mg，每天3次。
7.心律失常：每天300～600mg，分2～3次服。
 
药物相应作用
1.本药与氯磺丙脲、氯贝丁酯(安妥明)、去氨加压素、赖氨加压素、垂体后叶素、加压素等合用时，可加强抗利尿作用。
2.洛沙平、马普替林、噻吨类、三环类抗抑郁药、红霉素、竹桃霉素、异烟肼、维拉帕米、地尔硫，右丙氧芬、维洛沙嗪、氟西汀、西咪替丁、乙酰唑胺、达那唑、地昔帕明等药可提高本药的血药浓度，出现毒性反应。
3.与对乙酰氨基酚合用(尤其是单次超量或长期大量使用)时，可增加肝脏中毒的危险，并使对乙酰氨基酚的疗效降低。
4.与腺苷合用，可增加心脏传导阻滞程度。
5.与碳酸酐酶抑制药合用时，出现骨质疏松的危险性增加，故出现早期症状时应立即停用碳酸酐酶抑制药，必要时给予相应的治疗。
6.与锂盐，甲氧氯普胺，或与精神安定药(如氟哌啶醇、硫利达嗪)合用，能增加神经系统的副作用。
7.与香豆素类抗凝药、雌激素、含雌激素的避孕药、环孢素、洋地黄类(地高辛除外)，多西环素、左甲状腺素或奎尼丁等合用时，可使后者药效降低。
8.本药可以降低诺米芬辛的吸收并加快其消除。
9.锂剂可以降低本药的抗利尿作用。
10.与口服避孕药合用，可发生阴道大出血及避孕失败。
11.与某些利尿药合用(如氢氯塞嗪、速尿)可引起低钠血症。
12.本药对非除极肌松剂(如泮库铵)有拮抗作用。
13.与单胺氧化酶(MAO)抑制药合用时，可引起高热或(和)高血压危象、严重惊厥甚至死亡，两药应用时应至少间隔14天。当本药作为抗惊厥药时，MAO抑制药可以改变癫痫发作的类型。
14.可降低酒精的耐受性。
15.葡萄柚汁可使本药血药浓度峰值增加。
 
专家点评
临床应用卡马西平治疗癫痫的范围越来越广，已成为治疗多种癫痫类型的首选药。该药对全面强直阵挛发作、单纯部分性发作、复杂部分性和混合型发作疗效较好。但对典型和不典型失神发作、肌阵挛或失张力发作无效，如错误应用，可加重癫痫发作。

Medication name
Generic name: Carbamazepine Suspension - Oral
Brand name(s): Tegretol
CHEMICAL NAME
CARBAMAZEPINE.

INDICATIONS
Tegretol(Carbamazepine) is used to prevent and control seizures. It is known as an anticonvulsant or anti-epileptic drug. It is also used to relieve one type of nerve pain (trigeminal neuralgia). This medication works by reducing excessive nerve signals in the brain and restoring the normal balance of nerve activity. This drug may also be used to treat certain mental/mood conditions (e.g., bipolar disorder, schizophrenia) and other types of nerve pain.

DIRECTIONS
Shake the bottle well before each dose. Measure out each dose carefully. Take Tegretol Suspension by mouth with meals, usually 3 or 4 times a day, or as directed by your doctor. Dosage is based on your medical condition and response to therapy. Your doctor may gradually increase your dose. Follow these directions carefully. For the treatment of trigeminal nerve pain, do not take more than 1,200 milligrams per day. Separate doses of this drug from other liquid medicines by at least 2 hours. Avoid eating grapefruit or drinking grapefruit juice while being treated with this medication unless your doctor instructs you otherwise. Grapefruit juice can increase the amount of certain medications in your bloodstream. Consult your doctor or pharmacist for more details. Take this medication regularly at evenly spaced intervals in order to get the most benefit from it. Remember to use it at the same times each day to keep the amount of medicine in your body at a constant level. Do not take more of this medicine than prescribed or stop taking it without consulting your doctor. Some conditions (e.g., seizures) may become worse when the drug is suddenly stopped. Your dose may need to be gradually decreased. Inform your doctor if your condition does not improve or worsens.
MISSED DOSE: If you miss a dose, use it as soon as you remember. If it is near the time of the next dose, skip the missed dose and resume your usual dosing schedule. Do not double the dose to catch up. Call your doctor if you miss more than one dose a day.

SIDE EFFECTS
Nausea, vomiting, dizziness, drowsiness, or unsteadiness may occur as your body adjusts to this medication. If any of these effects persist or worsen, notify your doctor or pharmacist promptly. Remember that your doctor has prescribed this medication because the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects. Tell your doctor immediately if any of these unlikely but serious side effects occur: chest pain, swelling of the ankles/feet, trouble breathing, fatigue, fast/slow/irregular heartbeat, persistent or severe headache, fainting, trouble urinating, change in the amount of urine, decreased sexual ability, unusual eye movements (nystagmus), vision changes, hearing problems, mental/mood changes, pain/redness/swelling of the arms or legs, numbness/tingling of the hands/feet, sun sensitivity, joint pain, hair loss. Tell your doctor immediately if any of these rare but very serious side effects occur: persistent nausea or vomiting, severe stomach/abdominal pain, yellowing eyes and skin, dark urine, swollen glands, persistent mouth sores. A very serious allergic reaction to this drug is unlikely, but seek immediate medical attention if it occurs. Symptoms of a serious allergic reaction may include: rash, itching, swelling, severe dizziness, trouble breathing. If you notice other effects not listed above, contact your doctor or pharmacist.

PRECAUTIONS
Before taking carbamazepine, tell your doctor or pharmacist if you are allergic to it; or to other anti-seizure medications (e.g., phenobarbital, phenytoin) or tricyclic antidepressants (e.g., amitriptyline, desipramine); or if you have any other allergies. This medication should not be used if you have certain medical conditions. Before using this medicine, consult your doctor or pharmacist if you have: decreased bone marrow function (bone marrow depression), a certain blood disorder (acute intermittent porphyria). Before using this medication, tell your doctor or pharmacist your medical history, especially of: high blood pressure, blood clots, blood vessel disease, heart disease (e.g., coronary artery disease, congestive heart failure, heart rhythm or conduction disorders), kidney disease, liver disease, glaucoma, mental/mood disorders, certain types of seizures (atypical absence seizures), history of decreased bone marrow function due to other drugs. This drug may make you dizzy or drowsy; use caution engaging in activities requiring alertness such as driving or using machinery. Limit alcoholic beverages. This medication may make you more sensitive to the sun. Avoid prolonged sun exposure, tanning booths or sunlamps. Use a sunscreen and wear protective clothing when outdoors. This medication is not recommended for use during pregnancy due to the risk of possible birth defects and complications in the infant at birth. Discuss the risks and benefits with your doctor. If you become pregnant while taking this drug, contact your doctor immediately. If you are pregnant, prenatal care including tests for spinal cord defects is recommended. This medication passes into breast milk and may have undesirable effects on a nursing infant. Therefore, breast-feeding while using this drug is not recommended. Consult your doctor before breast-feeding.

OVERDOSAGE
If overdose is suspected, contact your local poison control center or emergency room immediately. Symptoms of overdose may include: slowed breathing, loss of consciousness, muscle twitching, uncontrolled movements, very fast heartbeat.

INFORMATION
Do not share this medication with others. Store at room temperature below 86 degrees F (30 degrees C) away from light and moisture. Do not store in the bathroom. Keep all medicines away from children and pets.

NOTES
The above information is intended to supplement, not substitute for, the expertise and judgment of your physician,pharmacist, or other healthcare professional. It should not be construed to indicate that the use of the product is safe, appropriate, or effective for you. Consult your
healthcare professional before taking the product.

DRUG INTERACTIONS
Your healthcare professionals (e.g., doctor or pharmacist) may already be aware of any possible drug interactions and may be monitoring you for it. Do not start, stop or change the dosage of any medicine before checking with them first. Avoid taking MAO inhibitors (e.g., furazolidone, isocarboxazid, linezolid, moclobemide, phenelzine, procarbazine, selegiline, tranylcypromine) within 2 weeks before or after treatment with this medication. In some cases a serious, possibly fatal, drug interaction may occur. This drug should not be used with the following medications because very serious interactions may occur: delavirdine, nefazodone, telithromycin, voriconazole. Before using this medication, tell your doctor or pharmacist of all prescription and nonprescription/herbal products you may use, especially of: other anti-seizure medications (e.g., felbamate, valproic acid), lithium, SSRI antidepressants (e.g., fluoxetine), tramadol, drugs affecting liver enzymes that remove carbamazepine from your body (such as azole antifungals-including itraconazole, macrolide antibiotics-including erythromycin, cimetidine, rifamycins-including rifabutin, St John's wort, propoxyphene, danazol, calcium channel blockers-including verapamil). Carbamazepine can cause certain liver enzymes to speed up the removal of other drugs from your body, possibly decreasing their effectiveness. These affected drugs include: caspofungin, cyclosporine, doxycycline, HIV protease inhibitors (e.g., amprenavir, saquinavir), levothyroxine, psychiatric medications (e.g., clozapine, haloperidol, risperidone), theophylline, warfarin. This medication may decrease the effectiveness of birth control products that contain hormones including combination-type birth control pills, patches, injections, and implants. This can result in pregnancy. You may need to use an additional form of reliable birth control while using this medication. Consult your doctor or pharmacist for details. Tell your doctor or pharmacist if you also take drugs that cause drowsiness such as: certain antihistamines (e.g., diphenhydramine), anti-anxiety drugs (e.g., diazepam), medicine for sleep (e.g., sedatives), muscle relaxants, narcotic pain relievers (e.g., codeine), psychiatric medicines (e.g., phenothiazines such as chlorpromazine, tricyclic antidepressants such as amitriptyline), tranquilizers. Check the labels on all your medicines (e.g., cough-and-cold products) because they may contain ingredients that cause drowsiness. Ask your pharmacist about the safe use of those products. This product can affect the results of certain lab tests (e.g., thyroid function, some pregnancy tests). Make sure laboratory personnel and your doctors know you are using this drug.

Store at 20°-25°C (68°-77°F) [see USP Controlled Room Temperature].