Methadone (Dolophine, Amidone, Methadose, Physeptone, Heptadon and many others) is a synthetic opioid, used medically as an analgesic, antitussive and a maintenance anti-addictive for use in patients on opioids. It was developed in Nazi Germany in 1937. Although chemically unlike morphine or heroin, methadone also acts on the opioid receptors and thus produces many of the same effects. Methadone is also used in managing chronic pain due to its long duration of action and very low cost. In late 2004, the cost of a one-month supply of methadone was $20, as compared to an equivalent analgesic amount of meperidine (pethidine) at $120, up to $500 and more for hydromorphone, morphine, fentanyl, and extended-release oxymorphone.

Methadone's usefulness in treatment of opioid dependence is the result of several factors. It has cross-tolerance with other opioids including heroin and morphine, long duration of effects with the result that oral dosing with methadone will stabilise the condition of the patient by stopping and preventing the opioid withdrawal syndrome, and by at least partially blocking the "rush" resulting from intravenous injection of heroin, morphine, and similar drugs.

Today a number of pharmaceutical companies produce and distribute methadone, with only the racemic hydrochloride being available in the United States as of March 2008 but the tartrate and other salts of the laevorotary form (levomethadone, with trade names like Polamidone, Heptadon etc.), which is more potent and lacks the cardiac effects like lengthened QT interval caused by the dextrorotary form, being available in Europe and elsewhere. The major producer remains Mallinckrodt. Mallinckrodt sells bulk methadone to most of the producers of generic preparations and also distributes its own brand name product in the form of tablets, dispersible tablets and oral concentrate under the name Methadose in the United States.

History

The drug was given the trade name Dolophine from the Latin dolor meaning pain (Cf. Dipidolor for piritramide, Dolantin for pethidine, and the "-dol" ending in so many trade and chemical names for analgesics of all types in German, English, French, and other languages) and was not named either in honour of or personally by Adolf Hitler as explored in greater detail below.

On September 11, 1941 Bockmühl and Ehrhart filed an application for a patent for a synthetic substance they called Hoechst 10820 or polamidon (a name still in regular use in Germany) and whose structure had no relation to morphine or the opiate alkaloids (Bockmühl and Ehrhart, 1949).

Methadone was introduced into the United States in 1947 by Eli Lilly and Company as an analgesic (they gave it the trade name Dolophine, which is now registered to Roxane Laboratories). Since then, it has been best known for its use in treating narcotic addiction. A great deal of anecdotal evidence was available "on the street" that methadone might prove effective in treating heroin withdrawal and it had even been used in some hospitals. It was not until studies performed at the Rockefeller University in New York City by Professor Vincent Dole, along with Marie Nyswander and Mary Jeanne Kreek, that methadone was systematically studied as a potential substitution therapy. Their studies introduced a sweeping change in the notion that drug addiction was not necessarily a simple character flaw, but rather a disorder to be treated in the same way as other diseases. To date, methadone maintenance therapy has been the most systematically studied and most successful, and most politically polarizing, of any pharmacotherapy for the treatment of drug addiction patients.