Rehabilitation Institute of Chicago, Center for Pain Management, Chicago, IL 60611, USA.
Mayo Clin Proc. 2012 Jul;87(7):683-94. doi: 10.1016/j.mayocp.2012.02.022.
Increased prescribing of opioid analgesics for chronic noncancer pain may reflect acceptance that opioid benefits outweigh risks of adverse events for a broadening array of indications and patient populations; however, a parallel increase in the abuse, misuse, and diversion of prescription opioids has resulted. There is an urgent need to reduce opioid tampering and subsequent abuse without creating barriers to safe, effective analgesia. Similar to the "magic bullet" concept of antibiotic development (kill the bacteria without harming the patient), the idea behind reformulating opioid analgesics is to make them more difficult to tamper with and abuse by drug abusers but innocuous to the compliant patient. As antibiotics exploit differences in bacterial and human physiology, tamper-resistant formulations depend on differences in the way drug abusers and compliant patients consume opioids. Most opioid abusers tamper with tablets to facilitate oral, intranasal, or intravenous administration, whereas compliant patients usually take intact tablets. Pharmaceutical strategies to deter opioid abuse predominantly focus on tablet tampering, incorporating physical barriers (eg, crush resistance) or embedded chemicals that render tampered tablets inert, unusable, or noxious. Deterring tampering and abuse of intact tablets is more challenging. At present, only a few formulations with characteristics designed to oppose tampering for abuse have received approval by the US Food and Drug Administration, and none has been permitted to include claims of abuse deterrence or tamper resistance in their labeling. This review discusses the potential benefits, risks, and limitations associated with available tamper-resistant opioids and those in development.
慢性非癌痛患者开具的阿片类镇痛药处方增加,可能反映出人们接受了这样一种观点,即对于更广泛的适应证和患者人群,阿片类药物的益处超过了不良反应的风险;然而,与此同时,处方阿片类药物的滥用、误用和转用也有所增加。目前迫切需要减少阿片类药物的篡改和随后的滥用,同时又不人为地为安全有效的镇痛制造障碍。与抗生素开发的“灵丹妙药”概念(杀死细菌而不伤害患者)类似,改造阿片类镇痛药背后的理念是使它们更难被药物滥用者篡改和滥用,同时对遵医嘱的患者无害。由于抗生素利用了细菌和人体生理学的差异,因此防篡改制剂依赖于药物滥用者和遵医嘱患者使用阿片类药物的方式的差异。大多数阿片类药物滥用者篡改片剂,以方便口服、鼻内或静脉给药,而遵医嘱的患者通常会服用完整的片剂。防止阿片类药物滥用的制药策略主要集中在片剂篡改上,包括物理障碍(例如,抗粉碎性)或嵌入的化学物质,使篡改后的片剂失效、无法使用或有毒。防止篡改和滥用完整片剂更具挑战性。目前,只有少数几种具有抗篡改设计特征的制剂已获得美国食品和药物管理局的批准,并且没有一种制剂被允许在其标签上声称具有防止滥用或抗篡改的功能。这篇综述讨论了现有和正在开发的防篡改阿片类药物的潜在益处、风险和局限性。