Methadone
Opioid medication / From Wikipedia, the free encyclopedia
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Methadone, sold under the brand names Dolophine and Methadose among others, is a synthetic opioid agonist used for chronic pain and also for opioid use disorder.[8] It is used to treat chronic pain, and it is also used to treat addiction to heroin or other opioids.[10][11] Prescribed for daily use, the medicine relieves cravings and removes withdrawal symptoms.[12] Withdrawal management using methadone can be accomplished in less than a month,[13] or it may be done gradually over a longer period of time, or simply maintained for the rest of the patient's life.[8] While a single dose has a rapid effect, maximum effect can take up to five days of use.[8][14] After long-term use, in people with normal liver function, effects last 8 to 36 hours.[8][9] Methadone is usually taken by mouth and rarely by injection into a muscle or vein.[8]
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Trade names | Dolophine, Methadose, Methatab,[3] others |
AHFS/Drugs.com | Monograph |
MedlinePlus | a682134 |
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Addiction liability | High[4] |
Routes of administration | By mouth, intravenous, insufflation, sublingual, rectal |
Drug class | Opioid |
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Bioavailability | 15-20% subcutaneous[6] 100% intravenous[6] |
Protein binding | 85–90%[6] |
Metabolism | Liver (CYP3A4, CYP2B6 and CYP2D6-mediated)[6][7] |
Onset of action | Rapid[8] |
Elimination half-life | 15 to 55 hours[7] |
Duration of action | Single dose: 4–8 h Prolonged use: • Withdrawal prevention: 1–2 days[8] • Pain relief: 8–12 hours[8][9] |
Excretion | Urine, faeces[7] |
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ECHA InfoCard | 100.000.907 |
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Formula | C21H27NO |
Molar mass | 309.453 g·mol−1 |
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Chirality | Racemic mixture |
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Side effects are similar to those of other opioids.[8] These frequently include dizziness, sleepiness, vomiting, and sweating.[8][15] Serious risks include opioid abuse and respiratory depression.[8] Abnormal heart rhythms may also occur due to a prolonged QT interval.[8] The number of deaths in the United States involving methadone poisoning declined from 4,418 in 2011[16] to 3,300 in 2015.[17] Risks are greater with higher doses.[18] Methadone is made by chemical synthesis and acts on opioid receptors.[8]
Methadone was developed in Germany in the late 1930s by Gustav Ehrhart and Max Bockmühl.[19][20] It was approved for use as an analgesic in the United States in 1947, and has been used in the treatment of addiction since the 1960s.[8][21] It is on the World Health Organization's List of Essential Medicines.[22]