近日,美国食品药品监督管理局已批准RELISTOR®（甲基纳曲酮溴化物）片剂用于治疗患有慢性非癌性疼痛的成人的阿片类药物引起的便秘（OIC）。RELISTOR片（450毫克，每天一次）用于治疗患有慢性非癌性疼痛的成年人的OIC。 之前，RELISTOR皮下注射剂（12mg和8mg）于2008年被批准用于接受姑息治疗的晚期疾病成年人的OIC治疗，2014年被批准用于治疗慢性非癌性疼痛成年人的OIC。
批准日期：2016年7月19日 公司：Valeant Pharmaceuticals International, Inc
RELISTOR（溴甲基纳曲酮[methylnaltrexone bromide]）片，口服
RELISTOR（甲基纳曲酮溴化物[methylnaltrexone bromide]）注射液，用于皮下使用
美国初次批准：2008年
作用机理
甲基纳曲酮是在阿片类药物受体上的阿片类药物结合的选择性拮抗剂。作为季胺，甲基纳曲酮穿越血脑屏障的能力受到限制。这使甲基纳曲酮可以在胃肠道等组织中充当外围作用的类阿片受体拮抗剂，从而减少阿片类药物的便秘作用，而不会影响阿片类药物对中枢神经系统（CNS）的镇痛作用。
适应症和用途
•RELISTOR是阿片类药物拮抗剂。RELISTOR片剂和RELISTOR注射剂可用于治疗患有慢性非癌性疼痛的成人（包括与先前癌症相关的慢性疼痛或其治疗且不需要频繁（例如每周）阿片类药物的患者）的阿片类药物引起的便秘（OIC）剂量增加。
•RELISTOR注射剂用于治疗因活动性癌症引起的晚期疾病或疼痛而需要阿片类药物剂量递增以进行姑息治疗的成年人中的OIC。
剂量和给药
管理说明。
•一旦使用，应紧邻厕所设施。
•如果还停止使用阿片类止痛药的治疗，请中止治疗。
•在患有慢性非癌性疼痛和OIC的成年患者中：
•接受阿片类药物少于4周的患者可能对RELISTOR的反应较弱。
•开始RELISTOR之前，应停止所有维持泻药治疗；如果3天后对RELISTOR的反应欠佳，可能会恢复泻药。
•当改变阿片类药物治疗以避免不良反应时，重新评估对RELISTOR的持续需求。
•对于患有慢性非癌性疼痛和OIC的患者，在一天的第一顿饭前至少30分钟空腹服用RELISTOR片剂。
加药
•对于患有慢性非癌性疼痛的成年患者的OIC：
•RELISTOR片剂：建议剂量为每天一次450mg，每天早晨。
•RELISTOR注射剂：推荐剂量为每天一次皮下注射12mg。
•对于成年晚期患者的OIC：
•预填充注射器仅适用于需要8mg或12mg RELISTOR注射剂量的患者。将小瓶用于需要其他剂量RELISTOR注射的患者。
•RELISTOR注射剂：关于推荐剂量，请参见完整处方信息中的表1；根据需要每隔一天服用一剂，但在24小时内不得超过一剂。
剂量调整
•根据适应症，在肾或肝功能不全中查看完整的处方信息剂量调整。
RELISTOR注射液的制备和给药。
•仅用于皮下使用。
•注入上臂，腹部或大腿。旋转注射部位。
剂量形式和强度
•片剂：150mg甲基纳曲酮溴化物。
•注射：
•在单剂量预填充注射器中使用8mg/0.4mL甲基纳曲酮溴化物。
•在单剂量预填充注射器或单剂量小瓶中使用12mg/0.6mL甲基纳曲酮溴化物。
禁忌症
患有已知或疑似机械性胃肠道梗阻且复发性梗阻风险增加的患者。
警告和注意事项
•胃肠道穿孔：考虑到已知或怀疑胃肠道病变的患者的总体风险获益。监测严重，持续或恶化的腹痛；如果出现症状，请停药。
•严重或持续性腹泻：如果在治疗期间发生严重或持续性腹泻，请中止治疗。
•阿片类药物戒断：考虑血脑屏障破坏的患者的总体风险获益。密切监测阿片类药物戒断症状。
不良反应
最常见的不良反应是：
成人慢性非癌性疼痛患者的OIC。
•RELISTOR片（≥2％）：腹痛，腹泻，头痛，腹胀，呕吐，多汗症，焦虑症，肌肉痉挛，鼻漏和发冷。
•RELISTOR注射液（≥1％）：腹痛，恶心，腹泻，多汗症，潮热，震颤和发冷。
成人晚期病人的OIC。
•RELISTOR注射液（≥5％）：腹痛，肠胃气胀，恶心，头晕和腹泻。
要报告可疑的不良反应，请致电1-800-321-4576联系Valeant Pharmaceuticals North America LLC，或致电1-800-FDA-1088与FDA联系，或访问WWW.FDA.GOV/MEDWATCH。
药物相互作用
•其他阿片类药物拮抗剂：可能产生加和效应并增加阿片类药物戒断风险；避免同时使用。
在特定人群中的使用
•怀孕：可能会使胎儿的阿片类药物戒断。
•哺乳期：不建议母乳喂养。
包装供应/存储和处理方式
供应方式
RELISTOR 12MG/0.6ML PF SYR 7 METHYLNALTREXONE BROMIDE  VALEANT PHARMACEUTICALS INT'L  65649055103
RELISTOR 8MG/0.4ML PF SYR 7  METHYLNALTREXONE BROMIDE  SALIX PHARM INC (DISC)  65649055204
RELISTOR 150MG TAB 90  METHYLNALTREXONE BROMIDE  VALEANT PHARMACEUTICALS INT'L 65649015090
RELISTOR 12 MG PFS 1  METHYLNALTREXONE BROMIDE  VALEANT PHARMACEUTICALS INT'L 65649055107
RELISTOR 12 MG VL 1   METHYLNALTREXONE BROMIDE  SALIX PHARM INC (DISC) 65649055102
存储
片剂
储存温度最高为25°C（77°F）； 允许在15°至30°C（59°至86°F）的范围内进行偏移[请参阅USP控制的室温]。
注射
存放在20°至25°C（68°至77°F）; 允许在15°至30°C（59°至86°F）的范围内进行偏移[请参阅USP控制的室温]。
不要冻结。避光。
完整说明资料附件：
https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=c488fb7c-0a5b-487c-b452-996809d1cb99
RELISTOR(methylnaltrexone bromide) tablets, for oral use
RELISTOR(methylnaltrexone bromide) injection, for subcutaneous use
Initial U.S. Approval: 2008
INDICATIONS
RELISTOR(methylnaltrexone bromide)is a prescription medicine used to treat constipation in adults that is caused by prescription pain medicines called opioids.
RELISTOR tablets and RELISTOR injection are used to treat constipation caused by opioids in adults with long-lasting(chronic)pain that is not caused by active cancer.
RELISTOR injection is also used to treat constipation caused by opioids in adults with advanced illness or pain caused by active cancer and who need increases in their opioid dose for pain management.
IMPORTANT SAFETY INFORMATION
Do not take RELISTOR if you have a bowel blockage(called an intestinal obstruction)or have a history of bowel blockage.
RELISTOR can cause serious side effects such as a tear in your stomach or intestinal wall(perforation). Stomach pain that is severe can be a sign of a serious medical condition. If you get stomach pain that is severe, does not go away, or gets worse, stop taking RELISTOR and get emergency medical help right away.
Stop using RELISTOR and call your healthcare provider if you get diarrhea that is severe or that does not go away during treatment with RELISTOR.
You may have symptoms of opioid withdrawal during treatment with RELISTOR including sweating, chills, diarrhea, stomach pain, anxiety, and yawning. Tell your healthcare provider if you have any of these symptoms.
Tell your healthcare provider if you have kidney or liver problems.
Tell your healthcare provider if you have any stomach or bowel(intestines)problems, including stomach ulcer, Crohn’s disease, diverticulitis, cancer of the stomach or bowel, or Ogilvie’s syndrome.
Tell your healthcare provider if you are pregnant or plan to become pregnant. Taking RELISTOR during pregnancy may cause opioid withdrawal symptoms in your unborn baby. Tell your healthcare provider right away if you become pregnant during treatment with RELISTOR.
Taking RELISTOR while you are breastfeeding may cause opioid withdrawal in your baby. You should not breastfeed during treatment with RELISTOR. You and your healthcare provider should decide if you will take RELISTOR or breastfeed. You should not do both.
Also, tell your healthcare provider about all of the medicines you take, including prescription and over the-counter medicines, vitamins, and herbal supplements.
In a clinical study, the most common side effects of RELISTOR tablets in people with long-lasting(chronic)pain that is not caused by cancer include: stomach-area (abdomen) pain, diarrhea, headache, swelling or a feeling of fullness or pressure in your abdomen, sweating, anxiety, muscle spasms, runny nose, and chills.
In a clinical study, the most common side effects of RELISTOR injection in people with long-lasting(chronic)pain that is not caused by cancer include: stomach-area (abdomen) pain, nausea, diarrhea, sweating, hot flush, tremor, and chills.
In clinical studies, the most common side effects of RELISTOR injection in people receiving treatment for their advanced illness include: stomach-area(abdomen)pain, gas, nausea, dizziness, and diarrhea.