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Diacetylmorphine, also known as diamorphine or heroin, is a potent small molecule opioid agonist that acts primarily on the mu-type opioid receptor (MOR). In the context of the German Heroin Trial led by Universitätsklinikum Hamburg-Eppendorf, it was evaluated as a maintenance treatment for individuals with severe, treatment-resistant opioid dependence. The therapy involves the supervised administration of pharmaceutical-grade, injectable diacetylmorphine, typically three times daily, to improve the physical and mental health of patients, reduce illicit drug consumption, and increase treatment retention compared to traditional oral methadone maintenance. Diacetylmorphine acts as a prodrug, rapidly metabolizing into 6-monoacetylmorphine and morphine, which then bind to opioid receptors in the central nervous system to produce its therapeutic and pharmacological effects.
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