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Carfentanil or carfentanyl, formerly sold under the brand name Wildnil, is an extremely potent opioid analgesic used in veterinary medicine to anesthetize large animals such as elephants and rhinoceroses.[1] It is a structural analogue of the synthetic opioid analgesic fentanyl.[2] It is typically administered in this context by tranquilizer dart.[1] Carfentanil has also been used in humans to image opioid receptors.[1] It has additionally been used as a recreational drug, typically by injection, insufflation, or inhalation.[1] Deaths have been reported in association with carfentanil.[1][3]

Effects and side effects of carfentanil in humans are similar to those of other opioids and include euphoria, relaxation, pain relief, pupil constriction, drowsiness, sedation, slowed heart rate, low blood pressure, lowered body temperature, loss of consciousness, and suppression of breathing.[1] The effects of carfentanil, including overdose, can be reversed by the opioid antagonists naloxone and naltrexone, though higher doses than usual may be necessary compared to other opioids.[1][3][4]: 23  It acts as an ultrapotent and highly selective agonist of the μ-opioid receptor.[1]

Carfentanil was first synthesized in 1974 by a team of chemists at Janssen Pharmaceuticals which included Paul Janssen.[5] It was introduced into veterinary medicine in 1986.[1] Carfentanil is legally controlled in most jurisdictions. carfentanyl powder Cas 59708-52-0 for sale, carfentanyl powder Cas 59708-52-0 for sale, carfentanyl powder Cas 59708-52-0 for sale, carfentanyl powder Cas 59708-52-0 for sale, carfentanyl powder Cas 59708-52-0 for sale, carfentanyl powder Cas 59708-52-0 for sale, carfentanyl powder Cas 59708-52-0 for sale, carfentanyl powder Cas 59708-52-0 for sale, carfentanyl powder Cas 59708-52-0 for sale, carfentanyl powder Cas 59708-52-0 for sale, carfentanyl powder Cas 59708-52-0 for sale, carfentanyl powder Cas 59708-52-0 for sale, carfentanyl powder Cas 59708-52-0 for sale, carfentanyl powder Cas 59708-52-0 for sale, carfentanyl powder Cas 59708-52-0 for sale, carfentanyl powder Cas 59708-52-0 for sale, carfentanyl powder Cas 59708-52-0 for sale, 

Uses

Veterinary use

Chosen for its high therapeutic index, carfentanil was first sold in 1986 under the brand name “Wildnil” for use in combination with an α2-receptor agonist as a tranquilizing agent[4]: 9  for large ungulates, hippos, rhinos, elephants, and large carnivores.[5][6][7] Commercial production of Wildnil ceased in 2003; the drug is now available only in compounded form and not available for veterinary use due to human abuse.[6][8][9] Since then, etorphine has become the standard tranquilizing agent for large mammals, with diprenorphine as the preferred reversal agent. Diprenorphine was also used previously to reverse the effects of carfentanil.[10]

Clinical use

Carfentanil has been used at doses of less than 7 μg as a radiotracer for positron emission tomography imaging of the μ-opioid receptor in the brain in humans.[1]

Pharmacology

Pharmacodynamics

Carfentanil acts as a highly selective agonist of the μ-opioid receptor.[11] It showed affinity values (Ki) of 0.051 nM for the μ-opioid receptor, 4.7 nM for the δ-opioid receptor, and 13 nM for the κ-opioid receptor in rat brain.[11] Thus, carfentanil displayed 90- and 250-fold selectivity for the μ-opioid receptor over the δ-opioid receptor and the κ-opioid receptor, respectively.[11] With human proteins, the affinities were 0.024 nM for the μ-opioid receptor, 3.3 nM for the δ-opioid receptor, and 43 nM for the κ-opioid receptor, demonstrating 140- and 1,800-fold selectivity for the μ-opioid receptor over the δ- and κ-opioid receptors, respectively.[9] Carfentanil appears to have higher affinity for the μ1-opioid receptor over the μ2-opioid receptor.[1] Carfentanil has approximately 10,000 times the analgesic potency of morphine, 4,000 times the potency of heroin, and 20 to 100 times the potency of fentanyl in animal studies.[1][3][9] The effects of carfentanil are reversed by μ-opioid receptor antagonists like naloxone and naltrexone, though higher than normal doses of these agents may be necessary in humans due to the extremely high potency of carfentanil.[1][3]

Pharmacokinetics

A lipophilic chemical that can easily cross the blood–brain barrier, carfentanil has a very rapid onset of action and is longer acting than fentanyl.[4]: 9  Its elimination half-life in humans was 42 to 51 minutes following an intravenous bolus at an average dose of 1.34 μg (19 ng/kg).[1][3] However, in a case study of recreational exposure, the half-lives of carfentanil and its metabolite norcarfentanil were estimated to be 5.7 hours and 11.8 hours, respectively.[1][12]

Chemistry

Nomenclature for derivatives of fentanyl

Carfentanil is an analogue of fentanyl and is also known as (4‑methoxycarbonyl)fentanyl. Related analogues of fentanyl include 4‑phenylfentanyl, lofentanil (3‑methylcarfentanyl), N-methylnorcarfentanil, R-30490 (4‑methoxymethylfentanyl), sufentanil, and thiafentanil.

History

The first reported case of carfentanil overdose in a person was in 1986 when a veterinarian accidentally splashed 1.5 mg carfentanil citrate into his eyes and mouth. Sedation occurred within 2 minutes and naltrexone was administered. The veterinarian was hospitalised but made a full recovery within a day. carfentanyl powder Cas 59708-52-0 for sale

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How to Use Carfentanil?

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The side effects of Carfentanill abuse may include nausea, vomiting, dizziness, hallucinations, confusion, seizures, respiratory depression, coma, and death. Chemspowder

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Increase in illicit use

See also: Gray death

Over three hundred cases of overdose related to fentanyl and Carfentanil analogues were reported between August and November 2016 in several of the United States, including Ohio, West Virginia, Indiana, Kentucky and Florida.[13] In 2017, a Milwaukee, Wisconsin man died from a Carfentanil overdose, likely taken unknowingly with another illegal drug such as heroin or cocaine.[14] Carfentanil is most often taken with heroin or by users who believe they are taking heroin. Carfentanil is added to or sold as heroin because it is less expensive, easier to obtain, and easier to manufacture than heroin.[15]

Seizures by authorities

Authorities in Latvia and Lithuania reported seizing Carfentanil as an illicit drug in the early 2000s.[16]

Around 2016, the United States and Canada reported a dramatic increase in shipment of carfentanil and other strong opioid drugs to customers in North America from Chinese chemical supply firms. In June 2016, the Royal Canadian Mounted Police seized one kilogram of carfentanil shipped from China in a box labeled “printer accessories”. According to the Canada Border Services Agency, the shipment contained 50 million potentially lethal doses of the drug, in containers labeled as toner cartridges for HP LaserJet printers.[15]

Carfentanil was not a controlled substance in China until 1 March 2017,[17] and until then was manufactured legally and sold openly over the Internet, being actively marketed by several Chinese chemical companies.[15]

Moscow theater hostage crisis

Main article: Moscow theater hostage crisis

In 2012, a team of researchers at the British chemical and biological defence laboratories at Porton Down found carfentanil and remifentanil in clothing from two British survivors of the 2002 Moscow theater hostage crisis and in the urine from a third survivor. The team concluded that the Russian military had used an aerosol mist of carfentanil and remifentanil to subdue Chechen hostage takers.[18] Researchers had previously surmised from the available evidence that the Moscow emergency services had not been informed of the use of the agent, despite being instructed to bring opioid antagonists to the scene. Unaware that hundreds of patients had been exposed to high doses of strong opioids, the emergency workers failed to bring sufficient quantities of naloxone and naltrexone to counteract the effects of carfentanil and remifentanil. One hundred and twenty-five people exposed to the aerosol are confirmed to have died from respiratory failure during the incident.[19]

Potential as a chemical weapon

The toxicity of carfentanil in humans and its ready commercial availability has raised concerns over its potential use as a chemical weapon of mass destruction by rogue nations and terrorist groups. The toxicity of carfentanil has been compared to that of nerve gas

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Carfentanil, or carfentanyl (also known as 4-carbomethoxyfentanyl) is an analog of the synthetic opioid analgesic fentanyl. It is 10,000 times more potent than morphine, making it among the most potent commercially used opioids. Carfentanil was first synthesized in 1974 by a team of chemists at Janssen Pharmaceutica. It is marketed under the trade name wildnil as a general anesthetic agent for large animals, such as elephants.

Medical Uses of Carfentanyl:

Carfentanyl has limited medical applications and is primarily used in veterinary medicine for immobilizing large animals during procedures. Its potency allows for effective sedation and pain relief in animals that would otherwise require high doses of traditional opioids. However, due to its strength, Carfentanyl is not suitable for human use and is strictly controlled.

Carfentanyl and Opioid Addiction:

Carfentanyl has been found in heroin and even fentanyl sold on the streets, starting in July 2016 in Ohio, when 35 overdoses and 6 deaths occurred in 3 days. Law enforcement and emergency medical personnel warn that carfentanyl sold illicitly looks like other drugs found on the street, including cocaine and heroin because it is an odorless, white powder.

Individuals struggling with opioid addiction who purchase painkillers illicitly or use heroin are at risk of encountering opioids that are adulterated with carfentanil.

Illicit Use and Dangers:

Carfentanyl has gained notoriety for its presence in illicit drug markets, where it is often mixed with other substances, such as heroin or cocaine. This poses significant risks to users, as the potency of Carfentanyl can lead to overdose and respiratory depression. Its presence in street drugs has contributed to a rise in opioid-related fatalities in recent years.

Safety Considerations:

Due to its extreme potency, Carfentanyl poses significant risks to both users and those who come into contact with it. Even small amounts can be lethal, and accidental exposure can occur through inhalation, ingestion, or skin contact. Proper handling and safety protocols are crucial when working with Carfentanyl, and it should only be used by trained professionals in controlled settings.

Legal Status and Regulation:

Carfentanyl is classified as a Schedule II controlled substance in the United States, indicating its high potential for abuse and limited medical use. Its production, distribution, and possession are strictly regulated to prevent misuse and protect public health. It is important to adhere to all legal requirements and regulations when working with Carfentanil.

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What is carfentanil?

Carfentanil powder is an analogue of the synthetic opioid analgesic fentanyl.
Carfentanil is:

  • 100 times stronger than the same amount of fentanyl
  • 1.000 times stronger than heroin (by weight)
  • A structural analogue of fentanyl
  • A remedy with short duration of action and rapid onset of action
  • Significantly more potent in its effect than other known opioids
  • Used in veterinary medicine as an anesthetic for large animals

special feature: Carfentanil reduces pain response in rats more effectively than any other opioid.

Origin and development

  • First synthesis: 1974
  • Developed by: A team at Janssen Pharmaceutica
  • Person involved: Paul Jansen
  • Trade name in veterinary medicine: Wild Nile

Potency in comparison

substance Relative potency compared to morphine (weight) Remark
Morphine 1x Underlying value
Fentanyl 100x

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Carfentanil 10.000x Effect starts from 1 microgram
Sufentanil 500-1000x Less potent than carfentanil

Note: Carfentanil is not intended for human use due to its extreme potency.

Effect and receptor binding

Carfentanil/carfentanyl acts primarily as an agonist at the mu-opioid receptors.

Other receptors:

  • Kappa receptors
  • Delta receptors
  • NMDA receptors
  • Nicotinic acetylcholine receptors

Neurotransmitter release:

  • Endorphine
  • Serotonin
  • Norepinephrine
  • Adrenalin

Mechanism: In addition to opioid binding, carfentanil inhibits the reuptake of serotonin and noradrenaline.

Toxicity and lethal dose

substance Lethal dose (intravenous) Overdose mortality rate
Carfentanil 20 micrograms > 90%
Cocaine 1,2 mg
Heroin 75 mg

Carfentanil is considered one of the deadliest substances in existence; even tiny doses are potentially fatal.

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Carfentanil is an analogue of the synthetic opioid analgesic fentanyl, and is one of the most potent opioids known (also the most potent opioid used commercially). Carfentanil has a quantitative potency approximately 10,000 times that of morphine and 100 times that of fentanyl, with activity in humans starting at about 1 microgram. Carfentanil is intended for large-animal use only as its extreme potency makes it inappropriate for use in humans.

Carfentanil Pharmacology

Carfentanil acts primarily on the mu (some kappa and delta) opioid receptors as an agonist. It will induce similar effects of analgesia as other opioids, however, due to its potency, it will also induce strong side effects such as sedation. Consequently, that is why it is used as a tranquilizer for large animals. Carfentanil interacts predominately with the opioid mu-receptor. These mu-binding sites are discretely distributed in the brain, spinal cord, and other tissues. It exerts its principal pharmacologic effects on the central nervous system. Its primary actions of therapeutic value are analgesia and sedation. Carfentanil also depresses the respiratory centers, depresses the cough reflex, and constricts the pupils.

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International availability and legal status

  • In most countries Carfentanil illegal
  • Anonymous online orders are recorded in Canada and Australia
  • Partial use in research and veterinary medicine under strict regulation

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