Mystakidou Kyriaki, Katsouda Emmanuela, Parpa Efi, Vlahos Lambros, Tsiatas Marinos L
Department of Radiology, Pain Relief & Palliative Care Unit, University of Athens, Athens, Greece.
Drug Deliv. 2006 Jul-Aug;13(4):269-76. doi: 10.1080/10717540500394661.
Oral transmucosal fentanyl citrate (OTFC; brand name Actiq, Cephalon, UT) is a new opioid formulation that incorporates fentanyl into a lozenge and allows drug delivery through the buccal mucosa. This kind of absorption avoids first-pass metabolism, yielding a bioavailability substantially greater than oral administration. OTFC has a rapid onset of action and a short duration of effect. These characteristics, which resemble the course of a typical breakthrough pain episode, resulted in making OTFC the first opioid analgesic formulation specifically developed and approved for control of breakthrough pain in cancer patients. Apart from that, OTFC has been used in a variety of clinical situations of noncancer pain. This review article presents the synthesis; clinical pharmacology; pharmacokinetic and pharmacodynamic properties, toxicity, and clinical efficacy of this novel agent.
口腔黏膜枸橼酸芬太尼（OTFC；商品名Actiq，Cephalon公司，美国犹他州）是一种新型阿片类药物制剂，它将芬太尼制成含片，可通过颊黏膜给药。这种吸收方式避免了首过代谢，生物利用度显著高于口服给药。OTFC起效迅速，作用持续时间短。这些特点与典型的爆发性疼痛发作过程相似，使得OTFC成为首个专门开发并获批用于控制癌症患者爆发性疼痛的阿片类镇痛制剂。除此之外，OTFC还被用于多种非癌性疼痛的临床情况。这篇综述文章介绍了这种新型药物的合成、临床药理学、药代动力学和药效学特性、毒性及临床疗效。
