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R-Methadone

levomethadone

R-Methadone ballicule: receptor binding, kinetics and half-life diagram
Mechanism of action: R-Methadone ballicule

What it isThe R-enantiomer of methadone, carrying essentially all the mu opioid activity.

Why this oneRacemic methadone’s analgesia comes from this enantiomer, which is marketed alone as levomethadone in some European countries.

What limits itIt does not avoid the QT prolongation entirely, and the long variable half-life is unchanged.

R-Methadone molecular structure (skeletal formula)
Molecular structure: R-Methadone

FDA-approved for

Off-label

NO BOXED WARNINGS

Principal riskIt does not avoid the QT prolongation entirely, and the long variable half-life is unchanged

Classes and tags

Clinical profile

Direct muscarinic antagonism0 / 4

Serotonin and MAOI

Provisional washout figures

SRI significance2 / 4
MAO-A inhibition0 / 4
Serotonin release0 / 4

Elevating mechanismWeak/borderline SRI

Evidence confidenceLow

InterpretationThe enantiomer that carries racemic methadone's mu activity and its reuptake inhibition.

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