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Heroin

diamorphine

Heroin ballicule: receptor binding, kinetics and half-life diagram
Mechanism of action: Heroin ballicule
Heroin mascot mnemonic cartoon
Visual mnemonic: Heroin mascot
“Heroine”

What it isDiacetylmorphine, a rapidly penetrating prodrug of morphine; palliative care in the UK, illicit in the US.

Why this oneIts lipid solubility gives faster CNS entry than morphine, which is both the clinical and the addictive property.

What limits itNo US medical use. Overdose deaths are driven by fentanyl adulteration rather than heroin itself.

Heroin molecular structure (skeletal formula)
Molecular structure: Heroin

FDA-approved for

Off-label

⚠ BOXED WARNINGS

Classes and tags

Clinical profile

Therapeutic safety burden3 / 4
Overdose danger4 / 4
Weight-gain liability0 / 4
Sedation liability2 / 4
QT / Torsades0 / 4
Direct muscarinic antagonism0 / 4
Embryofetal risk3 / 4

Defining liabilityRapid respiratory depression, overdose and dependence

Active metabolites

Open Heroin in the interactive console ↗

Memory aids: interaction avatars

Heroin CYP3A4 substrate avatar mnemonic
CYP3A4 substrate

Open Heroin in the interactive console ↗