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O-desmethyl- tramadol

What it isThe M1 metabolite of tramadol, formed by CYP2D6, and the actual mu agonist.

Why it mattersTramadol itself is a weak opioid — this metabolite provides essentially all the opioid analgesia.

What it changesIt is why CYP2D6 poor metabolizers get no analgesia and ultra-rapid metabolizers get dangerous opioid effect from a normal dose.

FDA-approved for

NO BOXED WARNINGS

Principal riskThis is why tramadol fails in CYP2D6 poor metabolizers and kills ultra-rapid metabolizers, inclu

Classes and tags

Clinical profile

Direct muscarinic antagonism0 / 4

Mechanism of action: O-desmethyl- tramadol ballicule

O-desmethyl- tramadol ballicule: receptor binding, kinetics and half-life diagram

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