Methadone
Dolophine · Methadose
Opioid AgonistSchedule IIGeneric availableTDM data
Methadone is a synthetic opioid that acts as a full agonist at mu-opioid receptors, with additional antagonist activity at the NMDA receptor. Its long half-life allows once-daily dosing for opioid use disorder maintenance. It also has weak serotonin and norepinephrine reuptake inhibition properties.
Compare Methadone →FDA-Approved Indications
- Opioid use disorder: detoxification and maintenance treatment
- Management of pain severe enough to require daily, around-the-clock, long-term opioid treatment and for which alternative treatment options are inadequate
What Sets This Drug Apart
- Full mu-opioid agonist for OUD maintenance — longest track record of any medication-assisted treatment (since 1960s)
- Boxed warning for QTc prolongation and torsades de pointes — unique among opioid agonist treatments for OUD
- Extremely long and variable half-life (8-59 hours) — delayed peak respiratory depression creates accumulation danger during initiation
- NMDA receptor antagonism may provide benefit in neuropathic pain syndromes beyond typical opioid analgesia
- Must be dispensed through certified Opioid Treatment Programs (OTPs) — cannot be prescribed for OUD in typical outpatient settings
- Preferred pharmacotherapy for OUD in pregnancy (ACOG/SAMHSA) despite risk of neonatal opioid withdrawal syndrome
Boxed Warning
Life-threatening respiratory depression: Monitor closely during initiation and dose titration
Boxed Warning
QT prolongation and serious cardiac arrhythmias (torsades de pointes): ECG monitoring recommended at initiation and dose changes
Boxed Warning
Accidental ingestion, especially by children, can result in fatal overdose
Boxed Warning
Neonatal opioid withdrawal syndrome: Prolonged use during pregnancy can result in NOWS
Boxed Warning
Risks from concomitant use with benzodiazepines or other CNS depressants: concomitant use increases risk of respiratory depression, coma, an
Boxed Warning
OUD treatment: must be dispensed only through certified opioid treatment programs (OTPs)