Thiofentanyl
Thiofentanyl is a potent synthetic opioid that is an analog of fentanyl. It is approximately 5,000 times more potent than morphine in animal models.
Chemistry
Thiofentanyl is a 4-anilidopiperidine derivative, which refers to the fact that the molecule is based on a piperidine structure with an anilido (phenylamino) group at the 4-position. The "thio" in the name refers to the replacement of the carbonyl oxygen in the fentanyl structure with a sulfur atom.
Pharmacology
Like other opioids, thiofentanyl acts by binding to the mu-opioid receptor. This leads to an increase in the pain threshold and a reduction in the perception of pain. The exact mechanism of action is not fully understood, but it is believed to involve a decrease in the release of substance P and other neurotransmitters involved in the transmission of pain signals in the central nervous system.
Effects
The effects of thiofentanyl are similar to those of other opioids and include analgesia, sedation, nausea, and respiratory depression. Due to its high potency, the risk of overdose and death is significantly higher than with other opioids.
Legal status
Thiofentanyl is a Schedule I controlled substance in the United States, indicating that it has a high potential for abuse and no accepted medical use.
See also
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Contributors: Prab R. Tumpati, MD