美国食品和药品管理局（FDA）已经批准新的每日一次的奥卡西平缓释制剂（Oxtellar XR，制药公司Supernus）用于成人和6至17岁的儿童部分性发作的辅助治疗。
该剂型前身是SPN-804，建议剂量为成人每天1200至2400年毫克，年龄在6至17岁的儿童根据体重每天900至1800毫克。该产品将提供150毫克，300毫克，600毫克缓释片
批准日期：2017年2月2日  公司：Supernus，Inc
OXTELLAR XR（奥卡西平[oxcarbazepine]）缓释片，用于口服
美国最初批准：2000年
最近的重大变化
警告和注意事项：12/2015
作用机制
OxtellarXR®的药理活性主要通过奥卡西平的10-单羟基代谢物（MHD）[见临床药理学（12.3）]进行。 奥卡西平和MHD发挥其抗癫痫作用的确切机制尚不清楚; 然而，体外电生理学研究表明它们产生对电压敏感的钠通道的阻断，导致过度兴奋的神经膜的稳定，重复神经元放电的抑制和突触脉冲的传播的减少。 这些行为被认为对预防完整大脑中的癫痫发作非常重要。 此外，增加的钾电导和高压活化钙通道的调节可能有助于药物的抗惊厥作用。 没有证实奥卡西平或MHD与脑神经递质或调节剂受体位点的显着相互作用。
适应症和用法
OxtellarXR®是一种抗癫痫药物（AED），适用于：
成人：辅助治疗部分性癫痫发作
儿童：6至17岁儿童部分性癫痫发作的辅助治疗
剂量和给药
建议每日剂量为每天1,200毫克至2,400毫克
成人：每天一次服用600毫克。剂量增加可以每周间隔600mg每天增量进行，以达到推荐的每日剂量
儿童：目标剂量基于体重。滴定至目标剂量超过两到三周。每天一次以8mg / kg至10mg / kg开始。每周一次增加8mg/kg至10mg/kg，不超过600mg，以达到目标日剂量
肌酐清除率低于30mL/分钟的患者：以每天300毫克开始并缓慢增加
老年患者：从较低剂量（每天300毫克或450毫克）开始并缓慢增加
在将奥卡西平立即释放转化为OxtellarXR®时，可能需要更高剂量的OxtellarXR®
剂量形式和强度
缓释片剂：150mg，300mg和600mg
禁忌症
已知对奥卡西平或其任何组分的超敏反应
警告和注意事项
低钠血症：按建议监测钠。
过敏反应和血管神经性水肿。如果发生则停止
有过敏史的过敏史对卡马西平的反应：仅根据风险收益使用
严重的皮肤病学反应：如果观察到，则停止
自杀行为和想法：监测症状
退出OxtellarXR®：逐渐退出
多器官超敏反应：如果怀疑则停止使用
血液学反应：如果怀疑则停止
不良反应
最常见的（≥5％）和比安慰剂不良反应更频繁的是：头晕，嗜睡，头痛，平衡障碍，震颤，呕吐，复视，虚弱和疲劳。
要报告疑似不良反应，请致电（1-866-398-0833）联系Supernus，Inc。或致电1-800-FDA-1088或www.fda.gov/medwatch联系FDA
药物相互作用
苯妥英，卡马西平和苯巴比妥：共同给药降低了OxtellarXR®活性代谢产物的血液水平：可能需要更大剂量的OxtellarXR®。
口服避孕药：告知患者OxtellarXR®可能会降低激素避孕药的有效性。建议使用其他非激素避孕方法。
用于特定人群
怀孕：血浆中的活性代谢物水平可能会下降。监测患者。根据动物数据，可能会造成胎儿伤害。
严重肝功能损害：不推荐。
如何提供/存储和处理
提供的剂型
150毫克（黄色改良椭圆形片剂，一面印有“150”，可食用黑色墨水）。
瓶100片................................. NDC 17772-121-01
300毫克（棕色改良椭圆形片剂，一面印有“300”，可食用黑色墨水）。
瓶100片................................. NDC 17772-122-01
600毫克（棕红色改良椭圆形片剂，一面印有“600”，可食用黑色墨水）。
瓶100片.............................. NDC 17772-123-01
存储和处理
储存在25°C（77°F）; 允许的偏差在15°C至30°C（59°F至86°F）之间[参见USP控制的室温]。 避免光照，避免潮湿。 在紧密，耐光的容器中分配。
完整资料附件：
https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=aa610e56-1d1d-11e1-8bc2-0800200c9a66 
Oxtellar XR (oxcarbazepine) extended-release tablets for oral use
INDICATION
Oxtellar XR® is indicated as adjunctive therapy of partial seizures in adults and in children 6 years to 17 years of age.
IMPORTANT SAFETY INFORMATION
CONTRAINDICATIONS
Oxtellar XR is contraindicated in patients with a known hypersensitivity to oxcarbazepine or to any of its components.
WARNINGS & PRECAUTIONS
Clinically significant hyponatremia (sodium <125 mmol/L) may develop during treatment. Measurement and laboratory tests of serum sodium concentrations should be considered for patients during maintenance treatment with Oxtellar XR, particularly if the patient is receiving other medications known to decrease serum sodium levels. Discontinuation of oxcarbazepine treatment may be clinically required.
Rare cases of anaphylaxis and angioedema involving the larynx, glottis, lips, and eyelids have been reported in patients after taking the first or subsequent doses of oxcarbazepine. Angioedema associated with laryngeal edema can be fatal. If a patient develops any of these reactions after treatment with Oxtellar XR, the drug should be discontinued and an alternative treatment started. Do not rechallenge these patients with Oxtellar XR.
Inform patients who have had hypersensitivity reactions to carbamazepine that approximately 25% to 30% of them will experience hypersensitivity reactions with Oxtellar XR. Patients with a history of hypersensitivity reactions to carbamazepine should ordinarily be treated with Oxtellar XR only if the potential benefit justifies the potential risk. Discontinue Oxtellar XR immediately if signs or symptoms of hypersensitivity develop.
Serious dermatological reactions, including Stevens-Johnson syndrome and toxic epidermal necrolysis, have been reported in association with oxcarbazepine use. Should a patient develop a skin reaction while using Oxtellar XR, consideration should be given to discontinuing its use. (Please see WARNINGS section of complete prescribing information.)
Anyone considering prescribing Oxtellar XR must balance the risk of suicidal thoughts or behavior with the risk of untreated illness. Epilepsy and many other illnesses for which antiepileptic drugs are prescribed are themselves associated with morbidity and mortality and an increased risk of suicidal thoughts and behavior. Should suicidal thoughts and behavior emerge during Oxtellar XR treatment, the prescriber needs to consider whether the emergence of these symptoms in any given patient may be related to the illness being treated.
Patients, their caregivers, and families should be informed that antiepileptic drugs increase the risk of suicidal thoughts and behavior and should be advised of the need to be alert for the emergence or worsening of the signs and symptoms of depression, any unusual changes in mood or behavior, or the emergence of suicidal thoughts, behavior, or thoughts about self-harm. Behaviors of concern should be reported immediately to healthcare providers.
Withdrawal of Oxtellar XR should be done gradually to minimize the potential of increased seizure frequency.
Multi-organ hypersensitivity reactions have occurred in patients being treated with oxcarbazepine therapy. While there have been a limited number of reports, many of these cases resulted in hospitalization and some were life-threatening. Signs and symptoms of this disorder were diverse; however, patients typically, although not exclusively, presented with fever and rash associated with other organ system involvement disorders. If this reaction is suspected, discontinue Oxtellar XR and initiate an alternative treatment.
Rare reports of hematologic events such as pancytopenia, agranulocytosis, and leukopenia have been seen in patients treated with oxcarbazepine and discontinuation of therapy should be considered if any evidence of these hematologic events develop.
Due to physiological changes during pregnancy, plasma concentrations of the active metabolite of oxcarbazepine, the 10-monohydroxy derivative, may gradually decrease throughout pregnancy. Monitor patients carefully during pregnancy and through the postpartum period because the active metabolite concentrations or levels may increase after delivery. It is recommended that patients taking Oxtellar XR be enrolled in the NAAED Pregnancy Registry.
DOSING CONSIDERATIONS
Enzyme inducing antiepileptic drugs such as carbamazepine, phenobarbital, and phenytoin decrease the exposure to MHD, the active metabolite of Oxtellar XR. Dosage increases may be necessary.
In patients with severe renal impairment, initiate Oxtellar XR at a lower starting dose and increase, if necessary, at a slower than usual rate until the desired clinical response is achieved.
Concurrent use of Oxtellar XR with hormonal contraceptives and other oral or implant contraceptives may decrease plasma levels and render these contraceptives less effective. Additional non-hormonal forms of contraception are recommended.
ADVERSE REACTIONS
The most commonly observed (≥ 5%) adverse reactions seen in association with Oxtellar XR and more frequent than in placebo-treated patients were (1200 mg, 2400 mg, v placebo): dizziness (20%, 41%, v 15%), somnolence (12%, 14%, v 9%), headache (8%, 15%, v 7%), balance disorder (5%, 7%, v 5%), tremor (5%, 1%, v 2%), vomiting (6%, 15%, v 9%), diplopia (10%, 13%, v 4%), asthenia (3%, 7%, v 1%), and fatigue (6%, 3%, v 1%).
Please refer to the full Prescribing Information for Oxtellar XR.