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ThiofentanylThiofentanyl is considered to be one of the first ever designer drugs. It is an opioid analgesic and analogue of the powerful painkiller fentanyl.

It has been sold as an illicit drug in the black market. In the early 1980s it made a brief appearance as a fentanyl analogue that was sold as a heroin substitute to opiate addicts.

This was put to an end by the Federal Analogue act, which made many fentanyl analogues Schedule I and Schedule II drugs that were illegal to sell or posses without the appropriate licence. The Federal analogue act is considered to be the first time an attempt was made to control an entire family of drug compounds based on similarity of structure, rather than one at a time.

Thiofentanyl would be considered to be a designer drug as it was sold as a drug that would produce the effect of banned substances, while evading drug legislation due to an alteration of its chemical structure.

It is made along the same synthetic route as fentanyl. The difference being that 2-(2-bromoethyl)thiophene is replaced with  phenethyl bromide in one step of the synthesis.

Thiofentanyl is now a Schedule I substance in Candada and the United States and a Class A drug in the UK.

In recent times Thiofentanyl has become rare as a drug of abuse. There are other more common fentanyl analogues that have been used more recently such as acetylfentanyl.

Fentanyl analogues like Thiofentanyl all tend to share a number of common characteristics.

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Firstly almost all of them are extremely potent pain killers. They tend to be many hundreds of times more potent than morphine and even heroin. A dose that looks like a few grains of salt may be enough to kill by overdose.

Secondly, they all tend to cause heavy respiratory depression. In comparison to other opiates and opioid drugs like morphine, heroin and oxycodon, fentanyl and its analogues produce greater respiratory depression relative to the euphoria they produce. Drug users that user these compounds as direct replacements for heroin will tend to self administer at the upper end what is considered to be a safe dose in order to get their high. Hence these drugs are associated with respiratory arrest giving them low margin of safety for recreational drugs.

Just like fentanyl, thiofentanyl is highly psychologically and physically addictive.

Physical dependence will manifest with continual daily use. Withdrawal effects will begin only a few hours after the last dose of thiofentanyl. It is these symptoms that force many to continue using these drugs.

The full withdrawal has been described as “inhuman” by some reports on the internet. Symptoms include severe cramps and muscle pain, fever, headache, sweating, dehydration, insomnia, restlessness, profuse vomiting and nausea, fatigue, depression, anxiety, racing thoughts and a rapid heart rate.

Unfortunately once an individual has come clean they are actually in one of the most dangerous phases of their recovery. A relapse at this time is common and is often fatal due to their markedly reduced tolerance. The dose that once got them high will kill them once they are clean.