GABA-A positive allosteric modulator + NMDA antagonist + 5-HT3 agonist + acute DA release. Metabolised by ADH → acetaldehyde (toxic) → ALDH → acetate. East Asian populations often carry ALDH2 *2 variant → acetaldehyde accumulation → facial flushing + increased cancer risk. Zero-order kinetics above ~0.08 g/L (saturable ADH).
Half-Life (t½)
PO: 0.25h, IV: 0.25h
Dosing Guidelines
PO: Typical 14 g (Range: 14–14 g)
IV: Typical 14 g (Range: 14–14 g)
Target Organ Systems
nervous
endocrine
Interactions
Acetaminophen (major): Chronic ethanol induces CYP2E1 (CL ↑73% in alcoholics, Girre 1994 chlorzoxazone probe). APAP is only ~5–10% cleared by CYP2E1 (the NAPQI/toxic pathway), so the total-clearance bump is small (~7%). The clinical concern is glutathione depletion + raised NAPQI causing hepatotoxicity at lower APAP doses — not kinetic AUC shift. Limit APAP ≤2 g/d in heavy drinkers.