Fentanyl Confirmation, Urine
Clinical Information Discusses physiology, pathophysiology, and general clinical aspects, as they relate to a laboratory test
Fentanyl is an extremely fast acting synthetic opioid related to the phenylpiperidiens.(1,2) It is available in injectable as well as transdermal formulations.(1) The analgesic effects of fentanyl is similar to those of morphine and other opioids(1): it interacts predominantly with the opioid mu-receptor. These mu-binding sites are discretely distributed in the human brain, spinal cord, and other tissue.(1,3)
Fentanyl is approximately 80% to 85% protein bound. In plasma, the protein binding capacity of fentanyl decreases with increasing ionization of the drug. Alterations in pH may affect its distribution between plasma and the central nervous system (CNS). The average volume of distribution for fentanyl is 6 L/kg (range 3-8).(3,4)
In humans, the drug appears to be metabolized primarily by oxidative N-dealkylation to norfentanyl and other inactive metabolites that do not contribute materially to the observed activity of the drug. Within 72 hours of intravenous (IV) administration, approximately 75% of the dose is excreted in urine, mostly as metabolites with <10% representing unchanged drug.(3,4)
The mean elimination half-life is (1-3):
-IV: 2 to 4 hours
-Iontophoretic transdermal system (Ionsys) terminal half-life: 16 hours
-Transdermal patch: 17 hours (13-22 hours, half-life is influenced by absorption rate)
- Lozenge: 7 hours
- Buccal tablet
- 100 mcg to 200 mcg: 3 to 4 hours
- 400 mcg to 800 mcg: 11 to 12 hours
In clinical settings, fentanyl exerts its principal pharmacologic effects on the CNS. In addition to analgesia, alterations in mood (euphoria, dysphoria) and drowsiness commonly occur.(1,3) Because the biological effects of fentanyl are similar to those of heroin and other opioids, fentanyl has become a popular drug of abuse.
Detection and confirmation of illicit drug use involving fentanyl
The presence of fentanyl >0.20 ng/mL or norfentanyl >1.0 ng/mL is a strong indicator that the patient has used fentanyl.
Cautions Discusses conditions that may cause diagnostic confusion, including improper specimen collection and handling, inappropriate test selection, and interfering substances
Urine concentrations do not correlate well to serum drug levels. For therapeutic drug management, monitor serum levels using FENTS/89654 Fentanyl, Serum.
For situations where chain-of-custody is required, a Chain-of-Custody Kit is available, see COCH/9426 Chain-of-Custody Processing.
Reference Values Describes reference intervals and additional information for interpretation of test results. May include intervals based on age and sex when appropriate. Intervals are Mayo-derived, unless otherwise designated. If an interpretive report is provided, the reference value field will state this.
Clinical References Provides recommendations for further in-depth reading of a clinical nature
1. Gutstein HB, Akil H: Opioid analgesics. In Goodman & Gilman's: The Pharmacological Basis of Therapeutics. Vol. 11. Edited by JG LL Hardman, AG Gilman. New York, McGraw-Hill Book Company Inc. 2006, Chapter 21
2. Kerrigan S, Goldberger BA: Opioids. In Principles of Forensic Toxicology. 2nd Edition. Edited by ZB Levine. Washington DC, AACC Press, 2003, pp 187-205
3. Package insert: DURAGESIC (fentanyl transdermal system). Janssen Pharmaceutica Products. Titusville, NJ. LP, 2006
4. Baselt RC: Disposition of Toxic Drugs and Chemicals in Man. 8th edition. Foster City, CA. Biomedical Publications, 2008, pp 616-619