Academic Unit of Supportive Care, Department of Oncology, School of Medicine and Biomedical Science, Royal Hallamshire Hospital, Sheffield, UK.
Curr Opin Support Palliat Care. 2011 Mar;5(1):15-9. doi: 10.1097/SPC.0b013e3283437a39.
Cancer patients with moderate-to-severe pain require opioids for analgesia. Whereas early guidelines recommend oral morphine as the 'drug of choice', newer synthetic opioids can be given by a reliable and effective nonoral transdermal route. We examine the mode of action of transdermal patches and we review the evidence on two drugs, which are currently available in this formulation - buprenorphine and fentanyl - covering physicochemical characteristics and pharmacokinetics of the patches, clinical efficacy data and adverse effects.
Both buprenorphine and fentanyl possess ideal characteristics for transdermal delivery, being small molecules with high lipophilicity. Studies of buprenorphine patches show benefits but there is poor randomized controlled trial evidence comparing them with oral opioids. Fentanyl patches have been used for longer and have a larger body of evidence supporting their use, with data to suggest improved pain relief and reduced opioid side effects compared with sustained release oral morphine. Patients who have used both oral morphine and transdermal fentanyl express a preference for the patch drug.
Transdermal buprenorphine and fentanyl are now established for moderate-to-severe cancer pain. There is still a need for further comparative studies with other opioids, especially for buprenorphine.
中重度癌痛患者需要阿片类药物进行镇痛。尽管早期指南推荐口服吗啡作为“首选药物”,但新型合成阿片类药物可通过可靠有效的非口服透皮途径给予。我们研究了透皮贴剂的作用模式,并综述了目前可采用这种剂型的两种药物——丁丙诺啡和芬太尼的证据,涵盖了贴剂的理化特性和药代动力学、临床疗效数据和不良反应。
丁丙诺啡和芬太尼均具有理想的透皮给药特性,均为具有高亲脂性的小分子药物。丁丙诺啡贴剂的研究显示出获益,但比较其与口服阿片类药物的随机对照试验证据较少。芬太尼贴剂的使用时间更长,且有更多证据支持其使用,数据表明与口服美沙酮控释片相比,其能更好地缓解疼痛和减少阿片类药物的副作用。曾使用过口服吗啡和透皮芬太尼的患者对贴剂药物表示偏好。
透皮丁丙诺啡和芬太尼现已广泛用于中重度癌痛。仍需要与其他阿片类药物进行更多的比较研究,尤其是丁丙诺啡。