Fast Fact and Concept #103: Oral Transmucosal Fentanyl Citrate-OTFC (ACTIQ®)

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Title: Fast Fact and Concept #103: Oral Transmucosal Fentanyl Citrate-OTFC (ACTIQ®)

Author(s): Deb Gordon; Mark Schroeder

This Fast Fact reviews how and when to use OTFC for pain.

Educational Objective(s)
Learn indications for use of Actiq. Learn starting dose and titration schedule for Actiq. Review pharmacokinetics of Actiq.

Oral transmucosal fentanyl citrate (OTFC) is a solid formulation of fentanyl that resembles a lozenge on a handle, it is intended for oral transmucosal administration. OTFC is indicated for: Breakthrough cancer pain in patients already receiving and who are tolerant (receiving at least equivalent of 60 mg oral morphine per 24 hours) to opioid therapy for underlying persistent cancer pain.

Compared to morphine and hydromorphone, fentanyl is a lipid-soluble opioid and, when placed in saliva under normal conditions of the mouth, is 80% non-ionized making it the only opioid suitable for transmucosal absorption. Fentanyl is ~ 100 times more potent than morphine. However, bioavailability of OTFC depends on the fraction of the dose that is absorbed through the oral mucosa (~25%) and the fraction that is swallowed (~75%; but swallowed dose is only partially bioavailable). OTFC can produce a rapid onset of analgesia, even during unit consumption (fentanyl begins to cross the blood-brain barrier in as little as 3-5 minutes), with peak effect at 20-40 minutes after the start of administration; total duration of activity is 2 to 3 hours. The amount of fentanyl absorbed from each single dose remains stable over multiple administrations. This fact, combined with fentanyl's short half-life, reduces the risk of a cumulative increase in serum level with repetitive doses.

Prescribing Information:

Patient Information on Consumption Technique and Storage:
Place unit next to buccal mucosa, between cheek and gum, moving the unit gently side to side. 15 minutes is the ideal amount of time to consume a unit to achieve the desired onset and peak effect. ACTIQ units are designed for one time administration. Patients should be instructed to remove the unit from their mouth if excessive opioid-related side effects develop. The following factors will decrease transmucosal absorption:

Instruct patients to utilize the manufacturer?s safety containers to store the dosage units, and discard any unused portion of the OTFC by dissolving it under hot tap water. Partially used units should not be stored and re-used. The drug should be stored at room temperature, and not be frozen. The Average Wholesale Price is $249xx for #30 200ug lozenges.

Acknowledgement: The Fast Fact is adapted with permission from: Pain Management Fast Facts-??Minute Inservice; University of Wisconsin Pain Team, D Gordon, RN.


- Fine, P.G., & Streisand, J.B. (1998). A review of oral transmucosal fentanyl citrate: potent, rapid and noninvasive opioid analgesia. Journal of Palliative Medicine, 1 (1), 55-63.
- Portenoy, R.K., Payne, R., Coluzzi, P., Raschko, J.W., Lyss, A., Busch, M.A., Frigerio, V., Ingham, J., Loseth, D.B., Nordbrock, E., Rhiner, M. (1999). Oral transmucosal fentanyl citrate (OTFC) for the treatment of breakthrough pain in cancer patients: a controlled dose titration study. Pain, 79, 303-312.
-Physicians Desk Reference, 2003

Copyright/Referencing Information: Users are free to download and distribute Fast Facts for educational purposes only. Citation for referencing: Gordon D and Schroeder M. Fast Facts and Concepts #103: Oral Transmucosal Fentanyl Citrate-OTFC (ACTIQ®) December 2003. End-of-Life Physician Education Resource Center www.eperc.mcw.edu.

Disclaimer: Fast Facts provide educational information, this information is not medical advice. Health care providers should exercise their own independent clinical judgment. Some Fast Fact information cites the use of a product in dosage, for an indication, or in a manner other than that recommended in the product labeling. Accordingly, the official prescribing information should be consulted before any such product is used.

Creation Date: 12/2003

Format: Handouts

Purpose: Instructional Aid, Self-Study Guide, Teaching

Training: Fellows, 3rd/4th Year Medical Students, PGY1 (Interns), PGY2-6, Physicians in Practice
Specialty: Anesthesiology, Emergency Medicine, Family Medicine, General Internal Medicine, Geriatrics, Hematology/Oncology, Neurology, OB/GYN, Ophthalmology, Pulmonary/Critical Care, Pediatrics, Psychiatry, Surgery
Non-Physician: Nurses

ACGME Competencies: Medical Knowledge, Patient Care

Keyword(s): Oral Transmucosal Fentanyl Citrate, ACTIQ, Addiction, Chronic non-malignant pain, Controlled substance regulations, Pain, Pain assessment, Pain treatment

The Fast Facts series is distributed for educational use only and does not constitute medical advice. For the most current version of Fast Facts visit the EPERC web site at www.eperc.mcw.edu. This mirror version is provided subject to copyright restrictions for educational use within the Inter-Instutional Collaborating Network on End-of-Life Care (IICN).