Southam M A
Alza Corporation, Palo Alto, CA 94303-0802, USA.
Anticancer Drugs. 1995 Apr;6 Suppl 3:29-34. doi: 10.1097/00001813-199504003-00005.
The transdermal route of drug delivery has been used for the effective administration of therapeutic agents for more than a decade. The most important consideration in selecting a drug for transdermal delivery is the potential for improving therapeutic efficacy. The development of a transdermal fentanyl system provided an opportunity to add fentanyl to the armamentarium of strong opioids available for the treatment of cancer pain. The transdermal route of administration has advantages over both the oral and parenteral routes. In addition, patient and caregiver factors allow improved acceptance of and compliance to strong opioids and therefore improved analgesic outcome. Four transdermal fentanyl systems are available, providing delivery rates ranging from 25-100 micrograms/h; higher rates can be achieved by multiple system application. The system releases fentanyl continuously for 3 days when applied to the skin. Concentrations of fentanyl in the blood are measurable within a few hours of system application. Fentanyl serum concentrations increase gradually, generally levelling off after 12-24 h and remaining relatively constant for the remainder of the 3-day period. Steady state serum concentrations are reached by the second application. Clinical trials have established the efficacy and safety of transdermal fentanyl for the treatment of cancer pain. Transdermal fentanyl is not licensed for the treatment of acute pain, e.g. postoperative pain, and should not be prescribed for this purpose.
经皮给药途径用于有效施用治疗剂已有十多年了。选择用于经皮给药的药物时，最重要的考虑因素是提高治疗效果的潜力。透皮芬太尼系统的开发为在可用于治疗癌痛的强效阿片类药物药库中添加芬太尼提供了机会。经皮给药途径相对于口服和肠胃外给药途径都具有优势。此外，患者和护理人员因素使得对强效阿片类药物的接受度和依从性得到改善，从而改善镇痛效果。有四种透皮芬太尼系统可供使用，提供的给药速率范围为25 - 100微克/小时；通过应用多个系统可实现更高的速率。该系统应用于皮肤时，会持续释放芬太尼3天。在系统应用后的几个小时内，血液中的芬太尼浓度即可测量。芬太尼血清浓度逐渐升高，一般在12 - 24小时后趋于平稳，并在3天的剩余时间内保持相对稳定。第二次应用时达到稳态血清浓度。临床试验已证实透皮芬太尼治疗癌痛的有效性和安全性。透皮芬太尼未获许可用于治疗急性疼痛，如术后疼痛，不应为此目的开具处方。
