Methadone is a synthetic opioid analgesic synthesized in 1937 by German scientists Max Bockmühl and Gustav Ehrhart at IG Farben (Hoechst-Am-Main) who were searching for an analgesic that would be easier to use during surgery and also have low addiction potential. Methadone is a Schedule II drug under the Single Convention on Narcotic Drugs. more...
On September 11, 1941 Bockmühl and Ehrhart filed an application for a patent for a synthetic substance they called Hoechst 10820 or polamidon and whose structure had no relation to morphine or the opioid alkaloids (Bockmühl and Ehrhart, 1949). Although chemically unlike morphine or heroin, methadone also acts on the opioid receptors and thus produces many of the same effects. Chemically, methadone is the simplest of the opioids.
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, though it 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 is 20 USD, as compared to an equivalent analgesic amount of Demerol at 120 USD. The old name Dolophine comes from the German Dolphium. The name derives from the Latin "dolor" (pain).
Methadone (as Dolophine) was first manufactured in the USA by Mallinckrodt pharmaceuticals, a St. Louis-based subsidiary of the Tyco International corporation. Mallinckrodt held the patent up until the early 1990s. Today a number of pharmaceutical companies produce and distribute methadone. However, 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, dispersable tablets and oral concentrate under the name "Methadose" in the United States. Generally, one will only hear "dolophine" used by older addicts who used the product in the 1960's and 1970's. Medical professionals who believe that dolophine is the generic name for methadone, when actually it is the reverse, may also use the old brand name. Myths abound about methadone and this is just another one.
Methadone has a slow metabolism and very high lipid solubility making it longer lasting than morphine-based drugs. Methadone has a typical half life of 24 hours or more, permitting the administration only once a day in heroin detoxification and maintenance programs. The most common mode of delivery at a Methadone clinic is in an oral solution. Methadone is almost as effective when administered orally as by injection. Just like heroin, tolerance and dependence frequently develop. However, unlike heroin and all other opioids, methadone and buprenorphine (a mixed agonist / antagonist), have a ceiling effect as it relates to tolerance. Current research in this area shows methadone has a unique affinity for the NMDA brain receptor. It is believed that NMDA (N-methyl-D-aspartic acid) may regulate psychic dependence and tolerance by exhibiting opioid antagonist-like activity. Withdrawal symptoms are generally less acutely severe than those of morphine and heroin, but are usually more prolonged. Considered generally effective in management of heroin addiction and harm reduction (reduction of HIV rates, etc...). At proper dosing, it controls the appetite for heroin. However, some heroin addicts feel that it is actually harder to quit methadone than heroin itself. Treatment at a methadone maintenance clinic is intended to be for an indefinite duration, as the treatment is not curative.
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