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Methadone, sold under the brand names Dolophine and Methadose among others, is a synthetic opioid agonist used for opioid maintenance therapy in opioid dependence and for chronic pain management.[3] Detoxification using methadone can be accomplished in less than a month, or it may be done gradually over as long as six months.[3] While a single dose has a rapid effect, maximum effect can take up to five days of use.[3] The pain-relieving effects last about six hours after a single dose.[3][6] After long-term use, in people with normal liver function, effects last 8 to 36 hours.[3][5] Methadone is usually taken by mouth and rarely by injection into a muscle or vein.[3]
Side effects are similar to those of other opioids.[3] These frequently includes dizziness, sleepiness, vomiting, and sweating.[3][7] Serious risks include opioid abuse and respiratory depression.[3] Abnormal heart rhythms may also occur due to a prolonged QT interval.[3] The number of deaths in the United States involving methadone poisoning declined from 4,418 in 2011[8] to 3,300 in 2015.[9] Risks are greater with higher doses.[10] Methadone is made by chemical synthesis and acts on opioid receptors.[3]
Methadone was developed in Germany around 1937 to 1939 by Gustav Ehrhart and Max Bockmühl.[11][12] It was approved for use in the United States in 1947.[3] It is on the World Health Organization’s List of Essential Medicines, the safest and most effective medicines needed in a health system.[13] In 2013, about 41,400 kilograms were manufactured globally.[14] It is regulated similarly to other narcotic drugs.[15] It is not particularly expensive in the United States.[16]
In Russia, methadone is illegal. Brazilian footballer assistant Robson Oliveira was arrested in 2019 upon arriving in Russia with methadone tablets sold legally in other countries and has been in jail since then for what was considered drug trafficking under Russian law
How to use Methadone HCL
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Read the Medication Guide provided by your pharmacist before you start using methadone and each time you get a refill. If you have any questions, ask your doctor or pharmacist.
Take this medication by mouth on a regular schedule as directed by your doctor, not as needed for sudden (breakthrough) pain. You may take this drug with or without food. If you have nausea, it may help to take this drug with food. Ask your doctor or pharmacist about other ways to decrease nausea (such as lying down for 1 to 2 hours with as little head movement as possible).
Carefully measure the dose using a special measuring device/spoon. Do not use a household spoon because you may not get the correct dose. If your medication comes in an oral dosing syringe, use the syringe to measure the dose. Do not inject the medication. Before taking, mix the dose in at least 1 ounce (30 milliliters) of water or other liquid as directed. Drink all of the mixture right away. Do not prepare a supply in advance.
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The dosage is based on your medical condition and response to treatment.
This medication may cause withdrawal reactions, especially if it has been used regularly for a long time or in high doses. In such cases, withdrawal symptoms (such as restlessness, watering eyes, runny nose, nausea, sweating, muscle aches) may occur if you suddenly stop using this medication. To prevent withdrawal reactions, your doctor may reduce your dose gradually. Consult your doctor or pharmacist for more details, and report any withdrawal reactions right away.
Medical uses
Opioid addiction
Methadone is used for the treatment of opioid use disorder. It may be used as a maintenance therapy or in shorter periods for detoxification to manage opioid withdrawal symptoms. Its use for the treatment of addiction is usually strictly regulated. In the US, outpatient treatment programs must be certified by the federal Substance Abuse and Mental Health Services Administration (SAMHSA) and registered by the Drug Enforcement Administration (DEA) in order to prescribe methadone for opioid addiction.
A 2009 Cochrane review found methadone was effective in retaining people in treatment and in the reduction or cessation of heroin use as measured by self-report and urine/hair analysis but did not affect criminal activity or risk of death.[18]
Treatment of opioid-dependent persons with methadone follows one of two routes: maintenance or detoxification.[19] Methadone maintenance therapy (MMT) usually takes place in outpatient settings. It is usually prescribed as a single daily dose medication for those who wish to abstain from illicit opioid use. Treatment models for MMT differ. It is not uncommon for treatment recipients to be administered methadone in a specialist clinic, where they are observed for around 15–20 minutes post dosing, to reduce risk of diversion of medication.[20]
The duration of methadone treatment programs range from a few months to several years. Given opioid dependence is characteristically a chronic relapsing/remitting disorder, MMT may be lifelong. The length of time a person remains in treatment depends on a number of factors. While starting doses may be adjusted based on the amount of opioids reportedly used, most clinical guidelines suggest doses start low (e.g. at doses not exceeding 40 mg daily) and are incremented gradually.[21][22]
Methadone maintenance has been shown to reduce the transmission of blood borne viruses associated with opioid injection, such as hepatitis B and C, and/or HIV.[21] The principal goals of methadone maintenance are to relieve opioid cravings, suppress the abstinence syndrome, and block the euphoric effects associated with opioids.
Chronic methadone dosing will eventually lead to neuroadaptation, characterised by a syndrome of tolerance and withdrawal (dependence). However, when used correctly in treatment, maintenance therapy has been found to be medically safe, non-sedating, and can provide a slow recovery from opioid addiction.[21] Methadone has been widely used for pregnant women addicted to opioids.[21]
Pain
Methadone is used as an analgesic in chronic pain, often in rotation with other opioids.[23][24] Due to its activity at the NMDA receptor, it may be more effective against neuropathic pain; for the same reason, tolerance to the analgesic effects may be less than that of other opioids