21 Facts About Methadone

Methadone, sold under the brand names Dolophine and Methadose among others, is a synthetic opioid agonist used for chronic pain and for opioid dependence.

Methadone is usually taken by mouth and rarely by injection into a muscle or vein.

Methadone is made by chemical synthesis and acts on opioid receptors.

Methadone was developed in Germany around 1937 to 1939 by Gustav Ehrhart and Max Bockmuhl.

Methadone has been widely used for pregnant women addicted to opioids.

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Methadone is used as an analgesic in chronic pain, often in rotation with other opioids.

Methadone has been implicated in contributing to significant tooth decay.

Methadone fills the same opioid receptors in the brain as heroin and other prescription painkillers making it a suitable substitute.

Methadone is metabolized by CYP3A4, CYP2B6, CYP2D6, and is a substrate, or in this case target, for the P-glycoprotein efflux protein, a protein which helps pump foreign substances out of cells, in the intestines and brain.

Methadone has been shown to reduce neuropathic pain in rat models, primarily through NMDA receptor antagonism.

Methadone acted as a potent, noncompetitive a3ß4 neuronal nicotinic acetylcholine receptor antagonist in rat receptors, expressed in human embryonic kidney cell lines.

Methadone has a slow metabolism and very high fat solubility, making it longer lasting than morphine-based drugs.

Methadone has a typical elimination half-life of 15 to 60 hours with a mean of around 22.

Methadone is available in traditional pill, sublingual tablet, and two different formulations designed for the person to drink.

Methadone is almost as effective when administered orally as by injection.

Methadone was developed in 1937 in Germany by scientists working for I G Farbenindustrie AG at the Farbwerke Hoechst who were looking for a synthetic opioid that could be created with readily available precursors, to solve Germany's opium and morphine shortage problem.

Methadone was introduced into the United States in 1947 by Eli Lilly and Company as an analgesic under the trade name Dolophine.

Methadone was studied as a treatment for opioid addiction at the Addiction Research Center of the Narcotics Farm in Lexington, Kentucky in the 1950s, and by Rockefeller University physicians Robert Dole and Marie Nyswander in the 1960s in New York City.

Methadone is a Schedule I controlled substance in Canada and Schedule II in the United States, with an ACSCN of 9250 and a 2014 annual aggregate manufacturing quota of 31, 875 kilos for sale.

Methadone intermediate is controlled, under ACSCN 9226 under Schedule II, with a quota of 38, 875 kilos.

Methadone is regulated internationally as a Schedule I controlled substance under the United Nations Single Convention on Narcotic Drugs of 1961.