Drug intelligence / Profile preview

methadone

Development stage
Approved
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral, Intravenous, Intramuscular, Subcutaneous
01

Overview

Methadone is a synthetic opioid used primarily for the treatment of opioid use disorder (OUD) and as an analgesic for severe pain. It is a long-acting full agonist at the µ-opioid receptor and also acts as an antagonist at the N-methyl-D-aspartate (NMDA) receptor. Methadone reduces opioid cravings and withdrawal symptoms without producing the euphoria associated with other opioids. It can be administered orally or by injection but is most commonly given in liquid or tablet form for daily use in OUD treatment programs. Developed in Germany in the late 1930s by Gustav Ehrhart and Max Bockmühl, it was approved for medical use in 1947 and has since become a key component of medication-assisted therapy for addiction recovery[2][3][4][5][8].

Brand names
DolophineMethadoseMethadose Sugar-FreeDiskets
Other names
methadone hydrochlorideamidone
02

Targets

DOR (Opioid Receptor Delta 1)MOR (Mu opioid receptor)NMDAR (Glutamate receptor ionotropic, NMDA)KCNH2 (Voltage-gated potassium channel subfamily H member 2)KOR (Kappa opioid receptor)HTR3A (5-hydroxytryptamine receptor 3A)CHRNA7 (α7 nicotinic receptor)

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