It is on the World Health Organization's List of Essential Medicines, the most effective and safe medicines needed in a health system. Fentanyl was first made by Paul Janssen in 1960, following the medical inception of pethidine (also known as meperidine, marketed as Demerol) several years earlier. Janssen developed fentanyl by assaying analogues of the structurally related drug pethidine for opioid activity. The widespread use of fentanyl triggered the production of fentanyl citrate (the salt formed by combining fentanyl and citric acid in a 1:1 stoichiometric ratio), which entered medical use as a general anaesthetic under the trade name Sublimaze in the 1960s.
In the mid-1990s, fentanyl was introduced for palliative use with the fentanyl patch, followed in the next decade by the introduction of the fentanyl lollipop, dissolving tablets, and sublingual spray which are absorbed through the tissues inside the mouth. As of 2012, fentanyl was the most widely used synthetic opioid in medicine. In 2013, 1,700 kilograms (3,750 lbs) were used globally.
Fentanyl is also used as a recreational drug, leading to thousands of overdose deaths from 2000 to 2017. Deaths have also resulted from improper medical use. Fentanyl has a relatively wide therapeutic index (270) which makes it a very safe surgical anesthetic when monitored carefully; however, its potency requires careful measurements of highly diluted fentanyl in solution.
Illicit use of pharmaceutical fentanyl and its analogues first appeared in the mid-1970s in the medical community and continues in the present.
Fentanyl analogues may be hundreds of times more potent than street heroin, and tend to produce significantly more respiratory depression, making it much more dangerous than heroin to users. Fentanyl is used orally, smoked, snorted, or injected. Fentanyl is sometimes sold as heroin, often leading to overdoses. Many fentanyl overdoses are initially classified as heroin overdoses.
Fentanyl is sometimes sold on the black market in the form of transdermal fentanyl patches such as Duragesic, diverted from legitimate medical supplies. The gel from inside the patches may be ingested or injected.
Another form of fentanyl that has appeared on the streets is the Actiq lollipop formulation. The pharmacy retail price ranges from $15 to $50 per unit based on the strength of the lozenge, with the black market cost ranging from $5 to $25, depending on the dose. The attorneys general of
Non-medical use of fentanyl by individuals without opiate tolerance can be very dangerous and has resulted in numerous deaths. Even those with opiate tolerances are at high risk for overdoses. Once the fentanyl is in the user's system, it is extremely difficult to stop its course because of the nature of absorption. Illicitly synthesized fentanyl powder has also appeared on the
Some heroin dealers mix fentanyl powder with heroin to increase potency or compensate for low-quality heroin. In 2006, illegally manufactured, non-pharmaceutical fentanyl often mixed with cocaine or heroin caused an outbreak of overdose deaths in the
Several large quantities of illicitly produced fentanyl have been seized by
The "China White" form of fentanyl refers to any of a number of clandestinely produced analogues, especially α-methylfentanyl (AMF). This Department of Justice document lists "China White" as a synonym for a number of fentanyl analogues, including 3-methylfentanyl and α-methylfentanyl, which today are classified as Schedule I drugs in the United States. Part of the motivation for AMF is that, despite the extra difficulty from a synthetic standpoint, the resultant drug is relatively more resistant to metabolic degradation. This results in a drug with an increased duration.
In June 2013, the United States Centers for Disease Control and Prevention (CDC) issued a health advisory to emergency departments alerting to 14 overdose deaths among intravenous drug users in
Beginning in 2015,