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MOVANTIK(naloxegol)Tablets

2014-09-28 00:21:30 作者：新特药房来源：互联网浏览次数：351 文字大小：【大】【中】【小】

简介： Movantik是第一个口服用于治疗阿片诱导性便秘的μ-阿片受体拮抗剂9月16日，美国FDA批准了阿斯利康及其合作伙伴Nektar公司的新药Movantik（通用名：naloxegol）上市，用于口服治疗因使用阿片类药物引起的便 ...

关键字：naloxegol药品商标名movantik 阿片类便秘副作用阿片拮抗剂优先审评

Movantik是第一个口服用于治疗阿片诱导性便秘的μ-阿片受体拮抗剂
9月16日，美国FDA批准了阿斯利康及其合作伙伴Nektar公司的新药Movantik（通用名：naloxegol）上市，用于口服治疗因使用阿片类药物引起的便秘（OIC）。在两个共有1352位至少服用4周阿片类止疼药且表现便秘副作用的患者参与的临床实验中，连续12周服用12.5毫克和25毫克两个剂量的Movantik和安慰剂对照组相比，治疗组便秘好转患者的比例（41%和44%）明显高于安慰剂组（29%），而且这两个临床实验的结果相仿。Movantik常见的副作用包括腹痛、腹泻、头痛和胀气。
请参阅MOVANTIK部份处方资料
MOVANTIK™ (naloxegol)片，为口服使用，C-II
作用机制
Naloxegol是一种阿片拮抗剂结合在µ-阿片受体。当在推荐剂量水平给药时，naloxegol功能作为一种外周作用µ-阿片受体拮抗剂在组织中例如胃肠道，因此减低阿片类药物的便秘效应。
Naloxegol是纳洛酮聚二醇化衍生物，和对P-糖蛋白转运蛋白(P-gp)的底物。还有，在naloxegol中聚乙二醇部分的存在减低其被动通透性当与纳洛酮比较。由于减低通透性和的增加外排naloxegol跨越血脑屏障，与P-gp底物相关性质，预计在推荐剂量水平，naloxegol的CNS穿透是可忽略不计限制与中枢性介导阿片类镇痛干扰潜能。
适应证和用途
MOVANTIK(naloxegol)是一个阿片拮抗剂适用为在有慢性非癌症疼痛成年患者阿片-诱导便秘(OIC)的治疗。
剂量和给药方法
⑴MOVANTIK开始前终止维持润肠通便治疗；如患者服用MOVANTIK共3天后有阿片-诱导便秘[OTC]症状可恢复缓泻药。
⑵开始MOVANTIK前不需要改变镇痛给药方案。
⑶在曾服用阿片类药物共至少4周患者中MOVANTIK曾被显示是有效。
⑷服用当天首次进餐前至少空胃1小时或餐后2小时。
⑸整吞片，不要压碎或咀嚼。
⑹避免消耗葡萄柚或葡萄柚汁。
⑺如终止治疗也终止用阿片痛药物。
推荐剂量:
⑻25 mg每天1次；如不能耐受，减低至12.5 mg每天1次。
⑼肾受损(CLcr < 60mL/min)：12.5mg每天1次；如耐受增加至25 mg每天1次和监视不良反应。
剂型和规格
片：12.5mg和25mg。
禁忌证
⑴患者有已知或怀疑胃肠道阻塞和处在复发阻塞风险增加。
⑵与强CYP3A4抑制剂同时使用(如，克拉霉素[clarithromycin]，酮康唑[ketoconazole])
⑶对MOVANTIK或任何其赋形剂已知严重或严重超敏性反应。
警告和注意事项
⑴胃肠道穿孔：在有已知或怀疑GI道病变患者中开率总体风险获益。监视严重，持续或恶化腹痛；如症状发生终止。
⑵阿片类戒断：在有对血-脑屏障破坏患者中考虑总体风险获益。监视阿片类戒断症状。(5.2)
不良反应
在临床试验中最常见不良反应(3%)是：腹痛，腹泻，恶心，胀气，呕吐，和头痛(6.1)
报告怀疑不良反应，联系AstraZeneca电话1-800-236-9933或FDA电话1-800-FDA-1088或www.fda.gov/medwatch.
药物相互作用
⑴中度CYP3A4抑制剂(如，地尔硫卓[diltiazem]，红霉素[erythromycin]，[维拉帕米]verapamil)：增加naloxegol浓度；避免同时使用；如不可避免，减低剂量至12.5mg每天1次和监视不良反应。
⑵强CYP3A4诱导剂(如，利福平[rifampin])：naloxegol浓度减低；不建议同时使用。
⑶其他阿片拮抗剂：对相加作用潜能和阿片类戒断增加的风险；避免同时使用。
特殊人群中使用
⑴妊娠：在胎儿中可能促进阿片类戒断。
⑵哺乳母亲：终止药物或哺乳考虑药物对母亲的重要性。
⑶肝受损：在严重受损中避免使用。
US FDA Approves MOVANTIK™ (naloxegol) Tablets C-II
On September 16, the US Food and Drug Administration approved MOVANTIK™ (naloxegol) tablets C-II as the first once-daily oral peripherally acting mu-opioid receptor antagonist (PAMORA) for the treatment of opioid-induced constipation (OIC) in adults with chronic non-cancer pain.
Opioids play an important role in chronic pain relief by binding to mu-receptors in the central nervous system, but they also bind to mu-receptors in the gastrointestinal tract. That is why patients taking opioids for chronic pain can develop OIC.
For patients who take opioids for chronic pain, constipation is one of the most common side effects, which can continue throughout their pain management therapy.
MOVANTIK is expected to be available by prescription in pharmacies nationwide in the first half of 2015.
MOVANTIK strengthens AstraZeneca’s existing portfolio of medicines and aligns with our strategic focus on scientific leadership. AstraZeneca is dedicated to filling an unmet need for adult patients taking prescription opioids for chronic non-cancer pain who are experiencing OIC not adequately relieved by laxatives. It reflects our ongoing commitment to developing treatment options and supporting health care providers, patients and caregivers.
Important Safety Information for MOVANTIK
■MOVANTIK is contraindicated in:
■Patients with known or suspected gastrointestinal (GI) obstruction and patients at increased risk of recurrent obstruction due to the potential for GI perforation
■Patients receiving strong CYP3A4 inhibitors (e.g., clarithromycin, ketoconazole) because these medications can significantly increase exposure to naloxegol which may precipitate opioid withdrawal symptoms
■Patients with a known serious or severe hypersensitivity reaction to MOVANTIK or any of its excipients
■Cases of GI perforation have been reported with the use of another peripherally acting opioid antagonist in patients with conditions that may be associated with localized or diffuse reduction of structural integrity in the wall of the GI tract. Monitor for severe, persistent, or worsening abdominal pain; discontinue if this symptom develops
■Symptoms consistent with opioid withdrawal, including hyperhidrosis, chills, diarrhea, abdominal pain, anxiety, irritability, and yawning, occurred in patients treated with MOVANTIK. Patients receiving methadone in the clinical trials were observed to have a higher frequency of GI adverse reactions that may have been related to opioid withdrawal than patients receiving other opioids. Patients with disruptions to the blood-brain barrier may be at increased risk for opioid withdrawal or reduced analgesia. Monitor for symptoms of opioid withdrawal when using MOVANTIK in such patients.
■The most common adverse reactions with MOVANTIK in clinical trials were: abdominal pain (21%), diarrhea (9%), nausea (8%), flatulence (6%), vomiting (5%), headache (4%), and hyperhidrosis (3%)
Please see full US Prescribing Information
http://www.azpicentral.com/movantik/movantik.pdf
You are encouraged to report negative side effects of prescription drugs to the FDA. Visit http://www.fda.gov/medwatch, or call 1-800-FDA-1088