英文药名: Zarontin(Ethosuximide) 中文药名: 乙琥胺片 品牌药生产厂家: Pfizer 药品名称 中文别名：乙琥胺、柴浪丁、紫朗丁 英文别名：Atysmal、Emeside、Ethymal、Etomal、Mesentol、Pemal、Petinimid、Pyknolepsinum、Simatin、Succimal、Suximal、Suxin、Suxinutin、Thetamid、Zarondan、Zarontin 外文名: Ethosuximide ,Zarontin 生产厂家 Pfizer 辉瑞 药理作用 癫痫：俗称"羊角疯",是一组临床综合征，其特征为反复发作的大脑神经元异常放电，导致暂时性大脑功能失调，临床表现为运动、感觉、意识、植物神经、精神等不同障碍。 （1）乙琥胺属于抗癫痫药。 （2）本品口服吸收后，能抑制大脑运动皮质神经传递，减少癫痫发作。 适应症 　　 为癫痫小发作首选药。疗效好不良反应小。对肌阵挛发作和失张力发作亦有效，对强直性阵挛发作无效。 用法用量 　　 剂量：３～６岁每日为２５０ｍｇ。６岁以上的儿童及成人，每日为５００ｍｇ，１次口服。以后可酌情渐增剂量。一般是每４～７日增加２５０ｍｇ，直至满意控制症状而不良反应最小为止。 如６岁以上儿童日剂量超过０．７５～１ｇ时，成人日剂量达２ｇ时，则需分次服药。 任何疑问，请遵医嘱！ 注意事项 （1）有贫血者应慎用。 （2）孕妇慎用。本品对于孕妇的安全性尚不清楚。乙琥胺可以透过胎盘，可用于乙琥胺能够控制癫痫发作的妊娠妇女，在怀孕期间应当继续使用。不能突然停药，否则可诱发癫痫发作。孕妇。 （3）哺乳期妇女应慎用。 （4）严重肝、肾功能不全者慎用，用药时应减量，并应定期检查肝肾功能。 （5）对大、小发作混合性癫痫的治疗应合用苯巴比妥或苯妥英钠。 （6）可与食物或牛奶同服，以减少对胃部刺激。 （7）停药时须逐步减量，以免失神状态出现。 （8）当用于代替其它抗癫痫药时应逐步增量。 （9）合并用药时也应逐步增加剂量，以便达到所需的血药浓度。 （10）当与静脉注射地西泮合用时，初次剂量可以较大，以求迅速达到有效血药浓度40～100微克/毫升。 （11）成人剂量超过一日1.5克，6岁以下儿童超过1.0克时，应密切注意毒性反应。 （12）与琥珀酰亚胺类，如甲琥胺、苯琥胺等有叉过敏反应。 （13）服药期间应定期监测白细胞和肝、肾功能。 不良反应 ◆ 在服用本品期间，如果感到不适要尽快告诉医师或药师。情况紧急可先停止服药。 ◆ 如果用药合理，该药品可给您带来满意的疗效，也可能产生一些不良反应，但不是每人都发生，您可能不会遇到任何一个，不必紧张。 以下是乙琥胺可能产生的不良反应： （1）常见恶心、呕吐、上腹部不适、食欲减退；其次眩晕、头痛、嗜睡、幻觉及呃逆。 （2）偶见粒细胞减少、白细减少、再生障碍性贫血；有时可引起肝、肾损害。故用药时需注意检查血象肝肾功能。 （3）个别患者可出现荨麻疹、红斑狼疮等过敏反应，应立即停药。与甲琥胺、苯琥胺可发生交叉过敏反应。 药物相互作用 　 (1)与氟哌啶醇合用可改变癫痫发作的形式和频率，需调整本品的药用量，氟哌啶醇的血药浓度也可因而显著下降。 (2)与三环抗抑郁药以及吩噻嗪类和噻吨类抗精神病药合用，可降低抗惊厥效应，需调整用量。 (3)本品能使诺米芬新(nomifensine)的吸收减少，消除增快。 (4)与其他抗惊厥药的相互作用不显著，偶有认为可能使苯妥英的血药浓度有所增加。 (5)与卡马西平合用时，两者的代谢可能都加快，而血药浓度降低。 ①本药与碱性药物合用时，可使排泄减慢，使血药浓度增高；反之，与酸性药物合用时则可加速排泄降低疗效。 ②与卡马西平合用，使两药在体内的代谢加速，血药浓度降低。 ③本药常与丙戊酸类药合用，但无相互干涉的依据。但有报道，本药患者加用丙戊酸类药后乙琥胺药血浓度增高，半减期延长。与异烟肼合用后，血清药浓度也增高。 药物过量 立即停药。 如果认为自己或他人可能服用本品过量时，即使没有明显的不适或中毒迹象，也应立即打电话给医师或药师联系，或去最近医院看就诊检查。 急性过量的症状为恶心、呕吐和中枢神经抑制（包括伴有吸吸抑制的昏迷）。治疗：对于意识清醒的患者可采用催吐，对于意识不清的患者可采用气管保护下的洗胃（用活性炭）。同时采用综合的支持疗法，必要时可采用血液透析疗法。乙琥胺的t1/2长，因此，血浆药物浓度缓慢减退。 规格 胶囊剂：每胶囊250mg。 糖浆: 250mg/5ml。 PHARMACOLOGY   Pharmacokinetics: Ethosuximide is completely and rapidly absorbed from the gastrointestinal tract. Peak plasma levels occur 1 to 7 hours after a single oral dose. Ethosuximide is not significantly bound to plasma proteins; therefore, the drug is present in saliva and CSF in concentrations approximately equal to that of the plasma. Therapeutic concentrations are in the range of 280 to 710 µmol/L (40 to 100 µg/mL). Ethosuximide is extensively metabolized to at least 3 plasma metabolites. Only 12 to 20% of the drug is excreted unchanged in the urine. The elimination half-life for the drug is 40 to 60 hours in adults and 30 hours in children. INDICATIONS The control of absence (petit mal) epilepsy. CONTRAINDICATIONS Ethosuximide should not be used in patients who are hypersensitive to succinimides or components of these products. WARNINGS Blood dyscrasias, including some with fatal outcomes, have been reported to be associated with the use of ethosuximide; therefore, periodic blood counts should be performed. Should signs and/or symptoms of infection (e.g., sore throat, fever) develop, blood count determinations should be considered at that point. Ethosuximide is capable of producing morphological and functional changes in the animal liver. In humans, abnormal liver and renal function studies have been reported. Administer ethosuximide with extreme caution to patients with known liver or renal disease. Periodic urinalysis and liver function studies are advised for all patients receiving the drug. Only available with prescription Cases of systemic lupus erythematosus have been reported with the use of ethosuximide. The physician should be alert to this possibility. Pregnancy: Recent reports indicate an association between the use of anticonvulsant drugs and an elevated incidence of birth defects in children born to epileptic women taking such medication during pregnancy. The incidence of congenital malformations in the general population is regarded to be approximately 2%; in children of treated epileptic women this incidence may be increased 2- to 3-fold. The increase is largely due to specific defects, e.g., congenital malformations of the heart, and cleft lip and/or palate. Nevertheless, the great majority of mothers receiving anticonvulsant medications deliver normal infants. Data are more extensive with respect to phenytoin and phenobarbital, but these drugs are also the most commonly prescribed anticonvulsants. Some reports indicate a possible similar association with the use of other anticonvulsants, including trimethadione and paramethadione. However, the possibility also exists that other factors, e.g., genetic predisposition or the epileptic condition itself may contribute to or may be mainly responsible for the higher incidence of birth defects. Anticonvulsant drugs should not be discontinued in patients in whom the drug is administered to prevent major seizures, because of the strong possibility of precipitating status epilepticus with attendant hypoxia and risk to both the mother and the unborn child. With regard to drugs given for minor seizures, the risk of discontinuing medication prior to or during pregnancy should be weighed against the risk of congenital defects in the particular case and with the particular family history. Epileptic women of childbearing age should be encouraged to seek professional counsel and should report the onset of pregnancy promptly to their physician. Where the necessity for continued use of antiepileptic medication is in doubt, appropriate consultation might be indicated. The preceding considerations should be borne in mind and ethosuximide should be used in women of childbearing potential only when the expected benefits to the patient warrant the possible risk to a fetus. Lactation: Mothers receiving ethosuximide should not breast-feed their infants. Children: Safety and effectiveness in pediatric patients below the age of 3 years have not been established (see Dosage). Occupational Hazards: Ethosuximide may impair the mental and/or physical abilities required for the performance of potentially hazardous tasks, such as driving a motor vehicle or other such activity requiring alertness. PRECAUTIONS Ethosuximide, when used alone in mixed types of epilepsy, may increase the frequency of grand mal seizures in some patients. As with other anticonvulsants, it is important to proceed slowly when increasing or decreasing dosage, as well as when adding or eliminating other medication. Abrupt withdrawal of anticonvulsant medication may precipitate absence (petit mal) status. Information to Be Provided to the Patient: Occupational Hazards: Ethosuximide may impair the mental and/or physical abilities required for the performance of potentially hazardous tasks, such as driving a motor vehicle or other such activity requiring alertness; therefore the patient should be cautioned accordingly. Patients taking ethosuximide should be advised of the importance of adhering strictly to the prescribed dosage regimen. Patients should be instructed to promptly contact their physician if they develop signs and/or symptoms (e.g., sore throat, fever) suggesting an infection. Drug Interactions: Since ethosuximide may interact with concurrently administered antiepileptic drugs, periodic serum level determinations of these drugs may be necessary (e.g., ethosuximide may elevate phenytoin serum levels and valproic acid has been reported to both increase and decrease ethosuximide levels). Carcinogenicity, Mutagenesis, and Impairment of Fertility: There have been no adequate, well-controlled studies on the carcinogenicity, mutagenicity, or impairment of fertility of this product. PRECAUTIONS Ethosuximide, when used alone in mixed types of epilepsy, may increase the frequency of grand mal seizures in some patients. As with other anticonvulsants, it is important to proceed slowly when increasing or decreasing dosage, as well as when adding or eliminating other medication. Abrupt withdrawal of anticonvulsant medication may precipitate absence (petit mal) status. Information to Be Provided to the Patient: Occupational Hazards: Ethosuximide may impair the mental and/or physical abilities required for the performance of potentially hazardous tasks, such as driving a motor vehicle or other such activity requiring alertness; therefore the patient should be cautioned accordingly. Patients taking ethosuximide should be advised of the importance of adhering strictly to the prescribed dosage regimen. Patients should be instructed to promptly contact their physician if they develop signs and/or symptoms (e.g., sore throat, fever) suggesting an infection. Drug Interactions: Since ethosuximide may interact with concurrently administered antiepileptic drugs, periodic serum level determinations of these drugs may be necessary (e.g., ethosuximide may elevate phenytoin serum levels and valproic acid has been reported to both increase and decrease ethosuximide levels). Carcinogenicity, Mutagenesis, and Impairment of Fertility: There have been no adequate, well-controlled studies on the carcinogenicity, mutagenicity, or impairment of fertility of this product. ADVERSE EFFECTS Gastrointestinal: Gastrointestinal symptoms occur frequently and include anorexia, vague gastric upset, nausea and vomiting, cramps, epigastric and abdominal pain, weight loss, and diarrhea. There have been reports of gum hypertrophy and swelling of the tongue. Hemopoietic: leukopenia, agranulocytosis, pancytopenia, aplastic anemia, with or without bone marrow suppression and eosinophilia. Nervous system: Neurologic and sensory reactions reported during therapy with ethosuximide have included drowsiness, headache, dizziness, euphoria, hiccups, irritability, hyperactivity, lethargy, fatigue, and ataxia. Psychiatric or psychological aberrations associated with ethosuximide administration have included disturbances of sleep, night terrors, inability to concentrate, and aggressiveness. These effects may be noted particularly in patients who have previously exhibited psychological abnormalities. There have been rare reports of paranoid psychosis, increased libido, and increased state of depression with overt suicidal intentions. Integumentary: Dermatologic manifestations which have occurred with the administration of ethosuximide have included urticaria, Stevens-Johnson syndrome, systemic lupus erythematosus, and pruritic erythematous rashes. Genitourinary: microscopic hematuria, vaginal bleeding. Miscellaneous: myopia, hirsutism. OVERDOSAGE Symptoms: Acute overdoses may produce nausea, vomiting, and CNS depression including coma with respiratory depression. A relationship between ethosuximide toxicity and its plasma levels has not been established. The therapeutic range is 280 to 710 µmol/L, although levels as high as 1050 µmol/L have been reported without signs of toxicity. Treatment: Treatment should include emesis (unless the patient is or could rapidly become obtunded, comatose, or convulsing) or gastric lavage, activated charcoal, cathartics and general supportive measures. Hemodialysis may be useful to treat ethosuximide overdose. Forced diuresis and exchange transfusions are ineffective. DOSAGE Initial dose: children aged 3 to 6 years, 250 mg daily; older patients, 500 mg daily in divided doses. The dose thereafter must be individualized according to response and tolerance. Medicament should be increased by small increments: e.g., increase daily dose by 250 mg every 4 to 7 days until control is achieved with minimal side effects. Daily dosage of 1 to 1.5 g in divided doses frequently controls seizures; however, it may be necessary to exceed this amount by slow increases and careful evaluation of patient’s response. Dosage exceeding 1.5 g daily, in divided doses, should be administered only under the strictest supervision of the physician. The optimal dose for most children is 20 mg/kg/day. This dose has given average plasma levels within the accepted therapeutic range of 280 to 710 µmol/L (40 to 100 µg/mL). Subsequent dose schedules can be based on effectiveness and plasma level determinations. Ethosuximide may be administered in combination with other anticonvulsants when other forms of epilepsy coexist with absence (petit mal). The optimal dosage for most children is 20 mg/kg/day. SUPPLIED Capsules: Each soluble gelatin capsule, embossed “PD 237” contains: ethosuximide 250 mg. Nonmedicinal ingredients: D&C Yellow No. 10, FD&C Red No. 3, gelatin, glycerin, polyethylene glycol and sorbitol. Bottles of 100. Store between 15 and 25°C and protect from heat. Syrup: Each 5 mL contains: ethosuximide 250 mg. Nonmedicinal ingredients: alcohol, citric acid anhydrous, FD&C Yellow No. 6, flavoring agents, glycerin, purified water, saccharin sodium, sodium benzoate, sodium citrate, sucrose and vanillin. Alcohol: 3%. Energy: 62.76 kJ (15 kcal)/5 mL. Sodium: <1 mmol (6.7 mg)/5 mL. Gluten-, lactose-, parabens-, sulfite- and tartrazine-free. Bottles of 500 mL. Store between 15 and 25°C and protect from freezing and light.