Pain Clinic, General Hospital Klagenfurt Klagenfurt, Austria.
Ther Clin Risk Manag. 2006 Mar;2(1):115-25.
By virtue of their efficacy, opioid analgesics have long been used for the treatment of both acute and chronic pain. Concerns regarding their safety and tolerability have frequently prevented this class of drugs achieving their full therapeutic potential, and their reported association with drug abuse and dependence has led to a reduced acceptance by many patients. Indeed, there is a variety of opioid-like side effects which are common to all members of the class, but some opioids have a more favourable safety profile than others. Buprenorphine is a semisynthestic opioid with a mu-agonistic and kappa-antagonistic receptor-binding profile. Studies over the past two decades have shown buprenorphine to have a complex and unique pharmacological profile, which results in enhanced therapeutic benefits combined with a favourable safety profile. Having been underused before, the development of a new transdermal drug delivery system for buprenorphine has revived interest in this substance. Transdermal buprenorphine (Gruenenthal GmbH, Aachen, Germany) provides a noninvasive method of rate-controlled drug release ensuring constant and predictable serum buprenorphine levels over a prolonged period. This preparation has been shown to be advantageous for long-term treatment of chronic pain patients providing reliable pain control, few adverse events, and good patient acceptance.
由于其疗效，阿片类镇痛药长期以来一直被用于治疗急性和慢性疼痛。但由于对其安全性和耐受性的担忧，这一类药物往往无法发挥其全部治疗潜力，而且据报道，它们与药物滥用和依赖有关，这导致许多患者对其接受程度降低。事实上，该类药物的所有成员都存在各种阿片样副作用，但有些阿片类药物的安全性比其他药物更好。丁丙诺啡是一种半合成阿片类药物，具有 μ 激动剂和 κ 拮抗剂受体结合特性。过去二十年的研究表明，丁丙诺啡具有复杂而独特的药理学特性，这使其在具有良好安全性的同时，还能带来更多的治疗益处。由于之前使用不足，丁丙诺啡新的透皮给药系统的开发重新引起了人们对这种物质的兴趣。丁丙诺啡透皮贴剂（德国阿亨的 Grünenthal GmbH）提供了一种非侵入性的控释给药方法，可确保在较长时间内持续、可预测的血清丁丙诺啡水平。这种制剂已被证明对慢性疼痛患者的长期治疗具有优势，可提供可靠的疼痛控制、不良事件少且患者接受度好。
