Heroin

alkaloid · nervous · respiratory · IV · Intranasal · Inhaled · Intramuscular

Heroin, an alkaloid. Diacetylmorphine — a lipophilic morphine prodrug that crosses the blood-brain barrier rapidly, then is deacetylated to… IV half-life 0.1 h.

Diacetylmorphine — a lipophilic morphine prodrug that crosses the blood-brain barrier rapidly, then is deacetylated to 6-monoacetylmorphine and morphine, the active µ-opioid agonists. The fast onset accounts for the intense "rush"; effects (analgesia, euphoria, respiratory depression) are morphine-mediated.

PubChem CID 5462328. Prodrug — µ-opioid occupancy belongs to morphine/6-MAM (see morphine). Plasma t½ deferred.

Pharmacokinetics

• IV — t½ 3 min · ka 60 h⁻¹