阿片类药物引起的便秘:去丁丙诺啡在丁丙诺啡治疗个体中的作用的基本原理。

IF 5.1 Q1 SUBSTANCE ABUSE Substance Abuse and Rehabilitation Pub Date : 2016-06-14 eCollection Date: 2016-01-01 DOI:10.2147/SAR.S100998
Lynn R Webster, Michael Camilleri, Andrew Finn
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引用次数: 12

摘要

丁丙诺啡和丁丙诺啡-纳洛酮固定联合治疗阿片类药物依赖是有效的,但便秘是最常见的副作用之一。有证据表明,当患者从舌下丁丙诺啡-纳洛酮片剂或片剂切换到双层生物可降解黏附口腔膜制剂时,便秘的发生率较低,而双层口腔膜促进了药物在口腔黏膜的单向流动,但减少便秘的机制尚不清楚。药代动力学模拟表明,长期舌下给药的丁丙诺啡可能使患者暴露于比丁丙诺啡更高浓度的去甲丁丙诺啡,而长期口腔给药的丁丙诺啡浓度高于去甲丁丙诺啡。因为去甲丁丙诺啡是一种对多阿片受体有效的完全激动剂,去甲丁丙诺啡暴露的差异可能解释了丁丙诺啡-纳洛酮舌下配方和口腔膜配方在治疗后出现的便秘的差异。为了更好地理解和管理阿片类药物依赖患者发生阿片类药物诱导便秘的风险,本文综述了丁丙诺啡和丁丙诺啡-纳洛酮制剂的临床概况,并对临床试验中治疗性便秘的发生率进行了综述。这些数据被用来提出暴露于去丁丙诺啡(一种丁丙诺啡的活性代谢物)在阿片类药物引起的便秘的病理生理学中的潜在作用。
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Opioid-induced constipation: rationale for the role of norbuprenorphine in buprenorphine-treated individuals.

Buprenorphine and buprenorphine-naloxone fixed combinations are effective for managing patients with opioid dependence, but constipation is one of the most common side effects. Evidence indicates that the rate of constipation is lower when patients are switched from sublingual buprenorphine-naloxone tablets or films to a bilayered bioerodible mucoadhesive buccal film formulation, and while the bilayered buccal film promotes unidirectional drug flow across the buccal mucosa, the mechanism for the reduced constipation is unclear. Pharmacokinetic simulations indicate that chronic dosing of sublingually administered buprenorphine may expose patients to higher concentrations of norbuprenorphine than buprenorphine, while chronic dosing of the buccal formulation results in higher buprenorphine concentrations than norbuprenorphine. Because norbuprenorphine is a potent full agonist at mu-opioid receptors, the differences in norbuprenorphine exposure may explain the observed differences in treatment-emergent constipation between the sublingual formulation and the buccal film formulation of buprenorphine-naloxone. To facilitate the understanding and management of opioid-dependent patients at risk of developing opioid-induced constipation, the clinical profiles of these formulations of buprenorphine and buprenorphine-naloxone are summarized, and the incidence of treatment-emergent constipation in clinical trials is reviewed. These data are used to propose a potential role for exposure to norbuprenorphine, an active metabolite of buprenorphine, in the pathophysiology of opioid-induced constipation.

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