药品信息:
--------------------------------------------------------------- 详细处方信息以本药内容附件PDF文件(20101508194719.pdf)的“原文Priscribing Information”为准 --------------------------------------------------------------- 部分中文溴化甲基纳曲酮处方资料(仅供参考)
溴化甲基纳曲酮( methylnaltrexone bromide) 商品名为 Relistor,由美国 Wyeth 公司和 Progenics 公司联合研究开发,2008 年 4 月经美国 FDA 批准上市,用于治疗阿片类药物引起的便秘 (opioid2induced constipation , OIC) 。Wyeth 公司申请了世界专利 WO 2008/ 030567 和美国专利 US 2008/ 0064743 对 Relistor 进行了专利保护。
阿片类药物在临床上有着广泛的应用 ,它通过与中枢神经系统(CNS) 内大脑和脊髓的μ阿片受体特异性作用而缓解疼痛。但是阿片类药物可与中枢神经系统以外(如胃肠道内) 的μ阿片受体作用而引起恶心、便秘等不良反应。Relistor 是纳曲酮的衍生物,为阿片受体拮抗剂,能选择性地拮抗肠道上的μ阿片受体,从而缓解阿片类镇痛药所引起的便秘症状。由于 Relistor 具有独特的化学结构 ,所以它不能穿过人体的血脑屏障 ,只能与外周的阿片受体作用 ,因而不会影响阿片类药物对中枢神经系统的止痛效果。
临床前以及对健康受试者试验证明,连续注射或口服 Relistor 都可以明显的缓解阿片类药物引起的便秘 ,且不良反应较少; Ⅲ期临床试验证明,对于使用阿片类药物的老年患者皮下注射 Relistor 0115~013 mg/kg ,具有理想的缓解 OIC 作用; 采用静脉注射给药, Relistor 能够减轻由阿片类药物诱导的尿潴留症状; Relistor 对于术后肠梗阻症状也有一定的治疗意义。Relistor 每隔一天皮下注射一次,如果需要可以缩短给药间隔 ,但是用药间隔不可短于24 h 。
Relistor 最常见的不良反应为腹痛、腹泻、胃肠胀气、头晕和恶心。每年 ,美国大约有150万名以上的患者因为罹患某种晚期疾病 (如癌症、晚期心肺疾病或艾滋病等) 而接受镇痛治疗 ,多数患者是服用阿片类药物进行镇痛 ,这些患者几乎都会出现可缓解性的便秘症状。Relistor 的问世能够为服用阿片类药所引发便秘(OIC) 的晚期疾病患者极大地减轻痛苦。
Information on RELISTOR RELISTOR (methylnaltrexone bromide) Subcutaneous Injection, a peripherally-acting muopioid receptor antagonist, is a sterile, clear and colorless to pale yellow aqueous solution. The chemical name for methylnaltrexone bromide is (R)-N-(cyclopropylmethyl) noroxymorphone methobromide. The molecular formula is C21H26NO4Br, and the molecular weight is 436.36. Each 3 mL vial contains 12 mg of methylnaltrexone bromide in 0.6 mL of water.
INDICATIONS RELISTOR® is indicated for the treatment of opioid-induced constipation in patients with advanced illness who are receiving palliative care, when response to laxative therapy has not been sufficient. Use of RELISTOR beyond four months has not been studied.
DOSING RELISTOR is administered as a subcutaneous injection. The usual schedule is one dose every other day, as needed, but no more frequently than one dose in a 24-hour period. The recommended dose of RELISTOR is 8 mg for patients weighing 38 to less than 62 kg (84 to less than 136 lb) or 12 mg for patients weighing 62 to 114 kg (136 to 251 lb). Patients whose weight falls outside of these ranges should be dosed at 0.15 mg/kg.
SIDE EFFECTS Including : Abdominal Pain;Flatulence;Nausea;Dizziness;Diarrhea;Hy perhidrosis. PRECAUTIONS Severe or Persistent Diarrhea If severe or persistent diarrhea occurs during treatment, advise patients to discontinue therapy with RELISTOR and consult their physician. Peritoneal Catheters Use of RELISTOR has not been studied in patients with peritoneal catheters.
Storage RELISTOR® should be stored at 20-25°C (68-77°F); excursions permitted to 15-30°C (59-86°F) .Do not freeze. Protect from light.
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