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Indicated for the management of pain severe enough to require daily, around-the-clock, long-term opioid treatment and for which alternative treatment options are inadequate
Opioid-naive patients: 2.5 mg taken orally once every 8-12 hours; titrate slowly with dose increases no more frequent than every 3-5 days
Methadone 10mg acts by binding to the µ-opioid receptor, but also has some affinity for the NMDA ionotropic glutamate receptor. Methadone is metabolized by CYP3A4, CYP2B6, CYP2D6 and is a substrate for the P-glycoprotein efflux protein in the intestine and brain. The bioavailability and elimination half-life of methadone are subject to substantial inter-individual variability. Its main route of administration is oral. Adverse effects include sedation, hypoventilation, constipation, and miosis, in addition to tolerance, dependence, and withdrawal difficulties.