Global InformationMethadone information
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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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| Pharmacokinetic data | |
| Bioavailability | 15-20% subcutaneous[6] 100% intravenous[6] |
| Protein binding | 85–90%[6] |
| Metabolism | Liver (CYP3A4, CYP2B6 and CYP2D6-mediated)[6][8] |
| Onset of action | Rapid[7] |
| Elimination half-life | 15 to 55 hours[8] |
| Duration of action | Single dose: 4–8 h Prolonged use: • Withdrawal prevention: 1–2 days[7] • Pain relief: 8–12 hours[7][9] |
| Excretion | Urine, faeces[8] |
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| ECHA InfoCard | 100.000.907 |
| Chemical and physical data | |
| Formula | C21H27NO |
| Molar mass | 309.453 g·mol−1 |
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| Chirality | Racemic mixture |
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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.[7] 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.[7] While a single dose has a rapid effect, maximum effect can take up to five days of use.[7][14] After long-term use, in people with normal liver function, effects last 8 to 36 hours.[7][9] Methadone is usually taken by mouth and rarely by injection into a muscle or vein.[7]
Side effects are similar to those of other opioids.[7] These frequently include dizziness, sleepiness, vomiting, and sweating.[7][15] Serious risks include opioid abuse and respiratory depression.[7] Abnormal heart rhythms may also occur due to a prolonged QT interval.[7] 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.[7]
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.[7][21] It is on the World Health Organization's List of Essential Medicines.[22]
- ^ "CSD Entry METHAD01: (6R)-Dimethylamino-4,4-diphenyl-3-heptanone, L-Methadone". Cambridge Structural Database: Access Structures. Cambridge Crystallographic Data Centre. Retrieved 22 November 2020.
- ^ Bye E (1974). "Crystal Structures of Synthetic Analgetics. II. l-Methadone". Acta Chem. Scand. 28b: 5–12. doi:10.3891/acta.chem.scand.28b-0005.
- ^ https://www.medsafe.govt.nz/consumers/cmi/m/Methatabs.pdf
- ^ Bonewit-West K, Hunt SA, Applegate E (2012). Today's Medical Assistant: Clinical and Administrative Procedures. Elsevier Health Sciences. p. 571. ISBN 9781455701506.
- ^ "FDA-sourced list of all drugs with black box warnings (Use Download Full Results and View Query links.)". nctr-crs.fda.gov. FDA. Retrieved 22 October 2023.
- ^ a b c d e Fredheim OM, Moksnes K, Borchgrevink PC, Kaasa S, Dale O (August 2008). "Clinical pharmacology of methadone for pain". Acta Anaesthesiologica Scandinavica. 52 (7): 879–889. doi:10.1111/j.1399-6576.2008.01597.x. PMID 18331375. S2CID 25626479.
- ^ a b c d e f g h i j k l m n "Methadone Hydrochloride". The American Society of Health-System Pharmacists. Archived from the original on 23 December 2015. Retrieved 22 December 2015.
- ^ a b c Brown R, Kraus C, Fleming M, Reddy S (November 2004). "Methadone: applied pharmacology and use as adjunctive treatment in chronic pain" (PDF). Postgraduate Medical Journal. 80 (949): 654–659. doi:10.1136/pgmj.2004.022988. PMC 1743125. PMID 15537850. Archived (PDF) from the original on 2 May 2014.
- ^ a b Toombs JD, Kral LA (April 2005). "Methadone treatment for pain states". American Family Physician. 71 (7): 1353–1358. PMID 15832538. Archived from the original on 5 September 2017.
- ^ Anderson IB, Kearney TE (January 2000). "Use of methadone". The Western Journal of Medicine. 172 (1): 43–46. doi:10.1136/ewjm.172.1.43. PMC 1070723. PMID 10695444.
- ^ Volkow ND, Wargo EM (August 2018). "Overdose Prevention Through Medical Treatment of Opioid Use Disorders". Annals of Internal Medicine. 169 (3): 190–192. doi:10.7326/M18-1397. PMID 29913514. S2CID 49300767.
- ^ Cite error: The named reference
JosephStancliffLangrodwas invoked but never defined (see the help page). - ^ World Health Organization (2009). Clinical Guidelines for Withdrawal Management and Treatment of Drug Dependence in Closed Settings. Geneva: World Health Organization.
{{cite book}}: CS1 maint: date and year (link) - ^ Grissinger M (August 2011). "Keeping patients safe from methadone overdoses". P & T. 36 (8): 462–466. PMC 3171821. PMID 21935293.
- ^ "Methadone". The Substance Abuse and Mental Health Services Administration. 16 June 2015. Retrieved 14 October 2020.
- ^ "Data table for Figure 1. Age-adjusted drug-poisoning and opioid-analgesic poisoning death rates: United States, 1999–2011" (PDF). CDC. Archived (PDF) from the original on 23 November 2015. Retrieved 22 December 2015.
- ^ Rudd RA, Seth P, David F, Scholl L (December 2016). "Increases in Drug and Opioid-Involved Overdose Deaths - United States, 2010-2015". MMWR. Morbidity and Mortality Weekly Report. 65 (50–51): 1445–1452. doi:10.15585/mmwr.mm655051e1. PMID 28033313.
- ^ Chou R, Turner JA, Devine EB, Hansen RN, Sullivan SD, Blazina I, et al. (February 2015). "The effectiveness and risks of long-term opioid therapy for chronic pain: a systematic review for a National Institutes of Health Pathways to Prevention Workshop". Annals of Internal Medicine. 162 (4): 276–286. doi:10.7326/M14-2559. PMID 25581257. S2CID 207538295.
- ^ Methadone Matters: Evolving Community Methadone Treatment of Opiate Addiction. CRC Press. 2003. p. 13. ISBN 9780203633090. Archived from the original on 23 December 2015.
- ^ Kleiman MA, Hawdon JE (2011). "Diphenypropylamine Derivatives". Encyclopedia of Drug Policy. SAGE Publications. ISBN 9781506338248. Archived from the original on 23 December 2015.
- ^ Kuehn, B. M. (2005). Methadone Treatment Marks 40 Years. JAMA: The Journal of the American Medical Association, 294(8), 887–889. doi:10.1001/jama.294.8.887
- ^ World Health Organization (2021). World Health Organization model list of essential medicines: 22nd list (2021). Geneva: World Health Organization. hdl:10665/345533. WHO/MHP/HPS/EML/2021.02.