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 is a prescription medicine used with other medicines to treat partial seizures in adults and children 6 to 17 years of age.
IMPORTANT SAFETY INFORMATION
Do not take Oxtellar XR if you are allergic to oxcarbazepine or any of the other ingredients in Oxtellar XR.
Oxtellar XR can cause serious side effects, including a low level of sodium in your blood. Symptoms of low blood sodium include nausea, tiredness, lack of energy, headache, confusion, and more frequent or more severe seizures. Similar symptoms that are not related to low sodium may occur from taking Oxtellar XR. Other serious side effects include seizures happening more often or becoming worse, trouble concentrating, problems with your speech and language, feeling confused, feeling sleepy and tired, and trouble walking and with coordination. The most common side effects include dizziness, sleepiness, headache, problems with walking and coordination (unsteadiness), shakiness, nausea, vomiting, double vision, weakness, and tiredness. These are not all of the possible side effects of Oxtellar XR. For more information, ask your healthcare provider or pharmacist.
Like other antiepileptic drugs, Oxtellar XR may cause suicidal thoughts or actions in a very small number of people, about 1 in 500. Before you take Oxtellar XR, tell your healthcare provider if you have or have had depression, mood problems, or suicidal thoughts or behavior. Call a healthcare provider right away if you have thoughts about suicide or dying, attempts to commit suicide, have new or worse depression or new or worse anxiety, feel agitated or restless, experience panic attacks, trouble sleeping (insomnia), or new or worse irritability, feel or act more aggressive, angry, or violent, act on dangerous impulses, have an extreme increase in activity and talking (mania), or experience other unusual changes in behavior or mood.
Oxtellar XR may also cause allergic reactions or serious problems which may affect organs and other parts of your body like the liver or blood cells. You may or may not have a rash with these types of reactions. Call your healthcare provider right away if you have any of the following: swelling of your face, eyes, lips, or tongue, trouble swallowing or breathing, a skin rash, hives, fever, swollen glands, or sore throat that does not go away or comes and goes, painful sores in the mouth or around your eyes, yellowing of your skin or eyes, unusual bruising or bleeding, severe fatigue or weakness, severe muscle pain, frequent infections, or infections that do not go away. Many people who are allergic to carbamazepine are also allergic to Oxtellar XR. Tell your healthcare provider if you are allergic to carbamazepine.
Before taking Oxtellar XR, tell your healthcare provider about all your medical conditions, including if you have or have had suicidal thoughts or actions, depression or mood problems, have liver problems, have kidney problems, use birth control medicine, are pregnant or plan to become pregnant, or are breastfeeding or plan to breastfeed. Oxtellar XR passes into breast milk. You and your healthcare provider should discuss whether you should take Oxtellar XR or breastfeed. You should not do both.
Oxtellar XR may harm your unborn baby. Tell your healthcare provider right away if you become pregnant while taking Oxtellar XR. If you use birth control medicine, Oxtellar XR may cause your birth control medicine to be less effective.
Tell your healthcare provider about all the medicines you take, including prescription and non-prescription medicines, vitamins, and herbal supplements. Taking Oxtellar XR with certain other medicines may cause side effects or affect how well they work. Do not start or stop other medicines without talking to your healthcare provider. Especially tell your healthcare provider if you take: carbamazepine, phenobarbital, phenytoin, or birth control medicine.
Do not stop taking Oxtellar XR without talking to your healthcare provider. Stopping Oxtellar XR suddenly can cause serious problems, including seizures that will not stop. Take Oxtellar XR exactly as prescribed.
Do not drive, operate heavy machinery, or do other dangerous activities until you know how Oxtellar XR affects you. Oxtellar XR may slow your thinking and motor skills.
Do not drink alcohol or take other drugs that make you sleepy or dizzy while taking Oxtellar XR until you talk to your healthcare provider. Oxtellar XR taken with alcohol or drugs that cause sleepiness or dizziness may make your sleepiness or dizziness worse.
Please refer to the full Prescribing Information and Medication Guide for additional important patient information.
You are encouraged to report negative side effects of prescription drugs to the FDA. Visit www.fda.gov/medwatch, or call 1-800-FDA-1088.