Moderate-to-severe chronic pain
Third line
Full μ-opioid agonist for moderate-to-severe chronic cancer and non-cancer pain. SED uses methadone for opioid rotation in tolerance and when a neuropathic pain component is present.
Synthetic opioid, full mu-receptor agonist
ATC code: N07BC02 (Methadone)
Brand names
Dolophine, Methadose
Methadone is a full mu-opioid receptor agonist with a long half-life (T1/2 24–36 hours). It is used in opioid substitution therapy and for chronic pain refractory to other opioids. The drug blocks the hERG potassium channel and markedly prolongs the QT interval, especially at doses above 100 mg/day, with reported cases of torsades de pointes. Methadone also acts as a weak NMDA antagonist and inhibits serotonin reuptake; serotonergic reactions have been reported with SSRIs, SNRIs, and linezolid. Methadone is fully prohibited from circulation in Russia.
Third line
Full μ-opioid agonist for moderate-to-severe chronic cancer and non-cancer pain. SED uses methadone for opioid rotation in tolerance and when a neuropathic pain component is present.
Opens the checker prefilled with this drug. Pick the second one from your regimen.
Direct links to regulator labels. Open in a new tab.
FDA Category C. Methadone is the WHO and SEPB preferred substitution therapy for opioid dependence in pregnancy. Maternal opioid withdrawal carries higher fetal risk than methadone maintenance. About 60% of exposed newborns develop neonatal abstinence syndrome requiring inpatient management.
Compatible. Hale L3. Transfers into milk (RID about 2–3%) without reaching clinically meaningful infant concentration at stable maintenance doses. WHO and AAP consider it compatible; breastfeeding can reduce the severity of neonatal abstinence syndrome. Infant sedation and respiration are monitored.
Reference information, not a clinical decision. Discuss feeding pauses or changes with your physician or an IBCLC.
Methadone is evaluated for the following indications with varying evidence strength: Moderate-to-severe chronic pain (evidence tier B). See the full indication matrix with dosing and citations above on this page.
Common side effects of Methadone (≥ 1 in 100): Sedation, Constipation, Nausea and vomiting, Sweating, Erectile dysfunction. See the Safety section for uncommon and serious reactions.
FDA category C. FDA Category C. Methadone is the WHO and SEPB preferred substitution therapy for opioid dependence in pregnancy. Maternal opioid withdrawal carries higher fetal risk than methadone maintenance. About 60% of exposed newborns develop neonatal abstinence syndrome requiring inpatient management.
Compatible. Hale L3. Transfers into milk (RID about 2–3%) without reaching clinically meaningful infant concentration at stable maintenance doses. WHO and AAP consider it compatible; breastfeeding can reduce the severity of neonatal abstinence syndrome. Infant sedation and respiration are monitored.
Methadone is contraindicated in: Hypersensitivity to methadone; Respiratory depression; Severe asthma or COPD; Paralytic ileus; MAOI use within the past 14 days. Full list in the Safety section.