Diacétylmorphine

Diacétylmorphine, known in English as diacetylmorphine and commonly referred to as heroin, is a semi-synthetic opioid derived from morphine. It is produced by acetylating morphine at the 3- and 6-hydroxyl groups, yielding a diacetate ester. This chemical modification increases lipophilicity and enables rapid entry into the brain after administration.

Pharmacology: Diacetylmorphine is more potent than morphine and produces a rapid onset of euphoria due to swift central nervous system penetration. In the body it is hydrolyzed first to 6-monoacetylmorphine and then to morphine, with both metabolites contributing to analgesic and sedative effects.

History and regulation: First synthesized in the 19th century and marketed by Bayer in the late 1800s as a cough suppressant and analgesic, diacetylmorphine was later found to be highly addictive. Its medical use was restricted or banned in many countries during the 20th century. In a handful of places, diacetylmorphine is used under strict medical supervision for opioid substitution, typically in supervised heroin-assisted treatment programs.

Risks: Use carries substantial risks of addiction, dependence, tolerance, respiratory depression, overdose and infectious disease transmission when injected. Illicit preparations may contain adulterants or potent fentanyl analogs, increasing danger. Long-term use can cause hormonal, immune, and cognitive effects, as well as organ complications.

Related compounds include morphine and 6-monoacetylmorphine.