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Methadone is an opioid analgesic used to treat severe pain that has not responded to other treatments. Also used to help with opioid detoxification and maintenance treatment.
Methadose, Diskets, Dolophine, Metadol, Metadol-D
Name in Generic Form
DrugBank Accession Number DB00333 for methadone
Methadone is a powerful synthetic analgesic that acts as both a full-opioid receptor (MOR) agonist and an antagonist of the N-methyl-d-aspartate (NMDA) receptor. Methadone, as a full MOR agonist, mimics the natural effects of opioids, endorphins, and enkephalins in the body by releasing neurotransmitters involved in pain transmission. It also has a number of distinguishing features that have contributed to its increased use over the last two decades, including a lower risk of neuropsychiatric toxicity compared to other opioids (due to a lack of active metabolites), minimal accumulation in renal failure, good bioavailability, low cost, and a long duration of action. 21,22,23,14,19,20
Methadone is particularly useful for the management of difficult-to-treat pain syndromes such as neuropathic pain and cancer pain, which require higher and more frequent doses of shorter-acting opioids due to its unique mechanism of action.
15,16,18 In addition to acting as an agonist of the – and -opioid receptors, an antagonist of the N-methyl-D-aspartate (NMDA) receptor, and an inhibitor of serotonin and norepinephrine uptake, methadone is also an antagonist of the N-methyl-D-aspartate (NMDA) receptor. 2,7 Methadone, in particular, dampens a major excitatory pain pathway within the central nervous system by inhibiting the NMDA receptor. 12 Methadone’s effects on NMDA inhibition may explain why it has better analgesic efficacy and lower opioid tolerance when compared to other opioids. 16,17
Methadone’s effects and risks are similar to those of other opioids such as morphine, hydromorphone, oxycodone, and fentanyl. It does, however, have a distinct pharmacokinetic profile. Methadone has a longer duration of action and half-life when compared to short-acting and even extended-release morphine formulations. Because of these effects, methadone is an excellent choice for the treatment of severe pain and addiction, as fewer doses are required to maintain analgesia and prevent opioid withdrawal symptoms. However, methadone has an unpredictable half-life with interindividual variability, which increases the risk of respiratory depression and overdose when starting or titrating therapy. 8
Methadone’s pharmacological actions include analgesia, opioid withdrawal symptoms suppression, sedation, miosis, sweating, hypotension, bradycardia, nausea and vomiting (via binding within the chemoreceptor trigger zone), and constipation. Methadone use at higher doses can cause respiratory depression, overdose, and death. 21,22,23
Opioid Agonist Treatment (OAT) or Opioid Substitution Therapy (OST) refers to the treatment of opioid addiction with methadone, buprenorphine, or slow-release oral morphine (SROM) (OST). The goal of substituting illicit opioids for long-acting opioids used in OAT is to prevent withdrawal symptoms for 24-36 hours after dosing, thereby reducing cravings and drug-seeking behaviors. The use of OAT is also intended to lead to social stabilization by lowering crime rates, incarceration, the use of illicit opioids like heroin or fentanyl, and, eventually, marginalization. 13 In addition to overdose, illegally obtained opioids can be injected and may be laced with other substances that increase the risk of harm or overdose. In an effort to reduce the risks associated with injection drug use, such as the transmission of HIV and Hepatitis C, as well as other complications such as skin infections, abscesses, and endocarditis, OAT is frequently combined with education about harm reduction, including the use of clean needles and injection supplies.