User:Mr. Ibrahem/Methadone
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Methadone, sold under the brand name Dolophine among others, is an opioid used for opioid maintenance therapy in opioid dependence and for chronic pain management.[4] Detoxification using methadone can be accomplished in less than a month, or it may be done gradually over as long as six months.[4] While a single dose has a rapid effect, maximum effect can take up to five days of use.[4] The pain-relieving effects last about six hours after a single dose.[4][6] After long-term use, in people with normal liver function, effects last 8 to 36 hours.[4][5] Methadone is usually taken by mouth and rarely by injection into a muscle or vein.[4]
Clinical data | |
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Trade names | Dolophine, Methadose, others |
AHFS/Drugs.com | Monograph |
MedlinePlus | a682134 |
License data | |
Pregnancy category |
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Addiction liability | High[1] |
Routes of administration | By mouth, intravenous, insufflation, sublingual, rectal |
Drug class | Opioid |
Legal status | |
Legal status |
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Pharmacokinetic data | |
Bioavailability | 15-20% subcutaneous[2] 100% intravenous[2] |
Protein binding | 85–90%[2] |
Metabolism | Liver (CYP3A4, CYP2B6 and CYP2D6-mediated)[2][3] |
Onset of action | Rapid[4] |
Elimination half-life | 15 to 55 hours[3] |
Duration of action | Single dose: 4–8 h Prolonged use: • Withdrawal prevention: 1–2 days[4] • Pain relief: 8–12 hours[4][5] |
Excretion | Urine, faeces[3] |
Identifiers | |
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Chemical and physical data | |
Formula | C21H27NO |
Molar mass | 309.453 g·mol−1 |
3D model (JSmol) | |
Chirality | Racemic mixture |
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Side effects are similar to those of other opioids.[4] These frequently includes dizziness, sleepiness, vomiting, and sweating.[4] Serious risks include opioid abuse and a decreased effort to breathe.[4] Abnormal heart rhythms may also occur due to a prolonged QT interval.[4] The number of deaths in the United States involving methadone poisoning declined from 4,418 in 2011[7] to 3,300 in 2015.[8] Risks are greater with higher doses.[9] Methadone is made by chemical synthesis and acts on opioid receptors.[4]
Methadone was developed in Germany around 1937 to 1939 by Gustav Ehrhart and Max Bockmühl.[10][11] It was approved for use in the United States in 1947.[4] It is on the World Health Organization's List of Essential Medicines.[12] In 2013, about 41,400 kilograms were manufactured globally.[13] It is regulated similarly to other narcotic drugs.[14] It is not particularly expensive in the United States.[15]