diacetylmorfiini

Diacetylmorfiini, also known as diamorphine or heroin, is the diacetyl ester of morphine. By converting morphine’s two hydroxyl groups into acetyl esters, diacetylmorfiini becomes highly lipophilic, which allows it to cross the blood–brain barrier rapidly. In the body, it is quickly deacetylated to 6-monoacetylmorphine and then to morphine, with the morphine molecules responsible for its pharmacological effects.

Historically, diacetylmorfiini was first synthesized in the 19th century and was later marketed by Bayer in 1898 as a cough suppressant and pain reliever. It was initially promoted as a non-addictive alternative to morphine, a claim that proved inaccurate. The substance soon became widely abused and is now tightly regulated in most jurisdictions.

Pharmacologically, diacetylmorfiini is a potent agonist of the mu-opioid receptor. Its high lipophilicity leads to a rapid onset of effects, including analgesia, euphoria, and sedation, followed by potential respiratory depression and other opioid-related adverse effects. Because it is a prodrug that is rapidly converted to morphine, its clinical effects are largely attributable to morphine after metabolism. The drug carries a high risk of tolerance, physical dependence, and withdrawal upon cessation.

Medical use and regulation vary by country. In some places, diamorphine is used under strict medical supervision for severe pain or in certain opioid-dependence treatment programmes. In most other contexts, diacetylmorfiini is a controlled substance with stringent controls to prevent non-medical use and distribution. Safety, legality, and availability are closely tied to local regulatory frameworks.