Thursday, August 3, 2017

Recreational Use of Fentanyl

Fentanyl, also known as fentanil, is an opioid pain medication with a rapid onset and short duration of action. It is a potent agonist of μ-opioid receptors in the brain. Fentanyl is 50 to 100 times more potent than morphine, but some fentanyl analogues, which are designed to mimic the pharmacological effects of the original drug, may be as much as 10,000 times more potent than morphine.

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.

Recreational Use

Illicit use of pharmaceutical fentanyl and its analogues first appeared in the mid-1970s in the medical community and continues in the present. United States authorities classify fentanyl as a narcotic and an opioid. To date, more than 12 different analogues of fentanyl have been produced clandestinely and identified in the U.S. drug traffic. The biological effects of the fentanyl analogues are similar to those of heroin, with the exception that many users report a noticeably less euphoric high associated with the drug and stronger sedative and analgesic effects.

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. Estonia has the highest rate of 3-methylfentanyl overdose deaths in the EU, due to its high rate of recreational use.

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 Connecticut and Pennsylvania have launched investigations into its diversion from the legitimate pharmaceutical market, including Cephalon's "sales and promotional practices for Provigil, Actiq and Gabitril".

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 United States market. Because of the extremely high strength of pure fentanyl powder, it is very difficult to dilute appropriately, and often the resulting mixture may be far too strong and, therefore, very dangerous.

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 United States and Canada, heavily concentrated in the cities of Dayton, Ohio; Chicago; Detroit; and Philadelphia.

Several large quantities of illicitly produced fentanyl have been seized by U.S. law enforcement agencies. In June 2006, 945 grams (2.08 lbs) of 83 %-pure fentanyl powder was seized by Border Patrol agents in California from a vehicle that had entered from Mexico. Mexico is the source of much of the illicit fentanyl for sale in the U.S. However, in April 2006, there was one domestic fentanyl lab discovered by law enforcement in Azusa, California. The lab was a source of counterfeit 80 mg OxyContin tablets containing fentanyl instead of oxycodone, as well as bulk fentanyl and other drugs. In November 2016, the DEA uncovered an operation making counterfeit oxycodone and Xanax from a home in Cottonwood Heights, Utah. They found about 70,000 pills in the appearance of oxycodone and more than 25,000 in the appearance of Xanax. The DEA reported that millions of pills could have been distributed from this location over the course of time. The accused owned a pill press and ordered fentanyl in powder form from China.

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 Rhode Island associated with acetylfentanyl, a synthetic opioid analog of fentanyl that has never been licensed for medical use. In a separate study conducted by the CDC, 82% of fentanyl overdose deaths involved illegally manufactured fentanyl, while only 4% were suspected to originate from a prescription.

Beginning in 2015, Canada has seen a widespread number of fentanyl overdoses. Authorities suspect that the drug is being imported from Asia to the western coast by organized crime groups in powder form and being pressed into pseudo-OxyContin tablets. Traces of the drug have also been found in other recreational drugs including cocaine, MDMA, and heroin. The drug has been implicated in multiple deaths from the homeless to young professionals, including multiple teens and young parents. Because of the rising deaths across the country, Health Canada is putting a rush on a review of the prescription-only status of Naloxone in an effort to combat overdoses of the drug.

No comments:

Post a Comment