Fentanyl Drug Information
Classification
Fentanyl (Duragesic, Sublimaze, ) is an extremely fast- acting synthetic narcotic analgesic, of high potency (approximately 100 times that of morphine) and short duration of action. There are several analogues and derivatives of fentanyl which are also abused, and many have higher potencies. Pharmaceutical fentanyl has been available since 1963 as an anesthetic supplement and is available as a citrate salt for intravenous (IV) or intramuscular (IM) injection. Transdermal, sublingual, and trans buccal preparations are also available for management of chronic pain or for breakthrough cancer pain. Fentanyl abuse among healthcare workers has become popular due to the drugs euphoric effects and availability. Due to the lipophilicity of the drug, fentanyl rapidly crosses the blood-brain barrier, producing fast and pronounced CNS effects such as heightened euphoria and respiratory depression. Toxic effects include muscle rigidity, seizures, coma, and hypotension. Fentanyl also has similar tolerance and physical dependence properties to those of morphine.
Metabolism
Fentanyl is rapidly metabolized by the liver to the inactive metabolites, norfentanyl, hydroxyfentanyl, and hydroxynorfentanyl.
Fentanyl is administered I.V. or I.M. at single dosage levels of 25 – 100 µg as needed, transdermally at dosages of 25 – 100 µg/hr for 72 hours for chronic pain management, or by oral transmucosal dosages of 200 – 1600 µg for breakthrough cancer pain. Patients using transdermal patches had urine fentanyl concentrations ranging from 32-137 ng/mL and urine norfentanyl concentrations of 176-695 ng/mL.
Abuse
Illicit fentanyl can be extracted from patches and then smoked or injected. Drug cartels are now mixing powdered fentanyl with heroin and cocaine prior to smuggling the drugs into the United States.These combinations have led to several overdose deaths.
Adverse effects with increased or prolonged abuse of fentanyl include increased anxiety, irritability, aggressiveness, paranoia and hypersexuality. Physiological effects can include dilated pupils, dry mouth, hippus, increased body temperature and tachycardia. In overdose situations, a person my experience hallucinations, coma or death.
Laboratory drug testing: Methods of Analysis
Immunoassay screens are commercially available for detecting fentanyl in urine specimens. Confirmation of the presumptive positives is performed using a specific technique such as gas chromatography-mass spectrometry (GC-MS) or liquid chromatography-tandem mass spectrometry (LC-MS/MS). Redwood Toxicology Laboratory utilizes LC-MS/MS for confirming presumptive positive results from an immunoassay or mass spectrometry based screen.
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Drug information data is not definitive and should be used for reference guidelines only.