Alvimopan * (ADL 8 - 2698)是一种新型周边阿片拮抗物。

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Alvimopan * (ADL 8 - 2698)是一种新型周边阿片拮抗物。

J Surg. 2001年11月,182 (5):27 s-38s。

PubMed ID

11755894 (在PubMed

]

文摘

Alvimopan (ADL 8 - 2698;美国宾夕法尼亚州Adolor公司Exton)是一部小说,外围限制阿片拮抗物。口服后,特定于胃肠道(GI)的活动。ADL 8 - 2698系统吸收较低和高亲和力mu-opioid受体。在健康受试者,ADL 8 - 2698与loperamide-induced改变胃肠道转运和预防吗啡延迟oral-cecal渡越时间没有得罪中央介导阿片类药物的影响,如镇痛或瞳孔收缩。治疗阿片类天真的病人手术和接收阿片类药物对急性疼痛,口头诽谤联盟8 - 2698(6.0毫克)改善术后肠梗阻的管理(POI)通过缩短时间达到正常的肠功能,最终,住院。术后恶心和呕吐和总体发病率的胃肠道副作用减少患者ADL POI 8 - 2698。镇痛不妥协,因为没有变化值阿片样物质消费或视觉模拟量表(血管)患者疼痛分数患者ADL 8 - 2698和安慰剂。无药物相关副作用观察急性疼痛手术后的患者在最初的POI的研究。阿片类药物对慢性疼痛患者或阿片类药物成瘾,低剂量口服ADL 8 - 2698(0.5 - 3.0毫克)反转阿片类药物肠功能障碍(OBD)和归一化胃肠道活动。 These effects were evident without compromising opioid analgesia or inducing central nervous system symptoms of withdrawal. Some chronic opioid patients receiving apparently supramaximal doses of ADL 8-2698 (> or = 3.0 mg) reported localized GI side effects, possibly indicative of a localized GI withdrawal response. The most common side effects of ADL 8-2698 in chronic pain patients with OBD were abdominal pain, flatulence, and diarrhea. These effects were not observed in most OBD patients receiving lower doses of ADL 8-2698. Overall, ADL 8-2698 was well tolerated in clinical trials. Further studies to evaluate the efficacy and safety of ADL 8-2698 in clinical practice are in progress.

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药物靶点

药物	目标	类	生物	药理作用	行动
Alvimopan	Mu-type阿片受体	蛋白质	人类	是的	拮抗剂	细节