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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 shortage problem.

Methadone is a synthetic (man-made) narcotic. German scientists synthesized methadone during World War II because of a shortage of morphine. Methadone was introduced into the United States in 1947 as an analgesic.                                                                           

Abstract

Methadone is a synthetic (man-made) narcotic. German scientists synthesized methadone during World War II because of a shortage of morphine. Methadone was introduced into the United States in 1947 as an analgesic 

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Street names

Amidone
Chocolate Chip Cookies
Fizzies
Maria
Pastora
Bisquits
Dollies
Wafers

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Brand Names

Dolophine
Methadose
Methadone Diskets
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History

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 shortage problem.

It was only in 1947 that the drug was given the generic name “methadone” by the Council on Pharmacy and Chemistry of the American Medical Association. Since the patent rights of the I.G. Farbenkonzern and Farbwerke Hoechst were no longer protected each pharmaceutical company interested in the formula could buy the rights for commercial production of methadone for just one dollar.

Methadone was introduced into the United States in 1947 by Eli Lilly and Company as an analgesic. 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.
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Pharmacology

The chemical formula for methadone is: C21H27NO

Methadone acts by binding to the µ-opioid receptor, but also has some affinity for the NMDA ionotropic glutamate receptor. Methadone is metabolized by CYP3A4, CYP2B6, CYP2D6 and is a substrate for the P-Glycoprotein efflux protein in intestine and brain. The bioavailability and elimination half-life of methadone is subject to substantial inter-individual variability. Its main route of administration is oral. Adverse effects include hypoventilation, constipation and miosis, in addition to tolerance, dependence and withdrawal difficulties. The withdrawal period can be much more prolonged than with other opiates, spanning anywhere from two weeks to several months. It can also be found in urine samples six to ten weeks after the last dose. It was generally thought it left the system 2–3 days after last use but this is not the case, many factors contribute to how long it will stay in the system. It depends an individual's body weight, metabolism, history of use/abuse and many more factors.
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Uses

Methadone is used to reduce and/or eliminate the use of illicit opiates, the criminality associated with opiate use, and allows patients to improve their health and social productivity. In addition, enrollment in methadone maintenance has the potential to reduce the transmission of infectious diseases associated with opiate injection, such as hepatitis and HIV.The principal effects of methadone maintenance are to relieve narcotic craving, suppress the abstinence syndrome, and block the euphoric effects associated with opiates. Methadone maintenance has been found to be medically safe and non-sedating. It is also indicated for pregnant women addicted to opiates.

In Russia, methadone treatment is illegal. Health officials there are not convinced of the treatment's efficacy. Instead, doctors encourage immediate abstinence from drug use, rather than the gradual process that methadone substitution therapy entails. Patients are often given sedatives and painkillers to cope with withdrawal symptoms.
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Scheduling

Methadone is a Schedule II drug under the Controlled Substances Act with an accepted medical use as a pain reliever. Methadone has a high potential for abuse and use may lead to severe psychological or physical dependence.
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Psychological and physical addiction liability

Though methadone is used as an anti-addiction drug it can also cause addiction. Abuse of methadone can lead to physical and psychological dependence.

When an individual uses methadone, he/she may experience physical symptoms like sweating, itchy skin, or sleepiness. Individuals who abuse methadone risk becoming tolerant of and physically dependent on the drug.
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Long term effects

After taking methadone for periods of one year or longer, reports the National Highway Traffic Safety Administration, most recovering opiate addicted patients do not report adverse effects. However, lung and breathing problems can still arise after long-term use of methadone, reports the University of Maryland. Methadone, like other opioids, reduces the production of testosterone in both men and women, and can interfere with menstrual cycles in women when used for long periods of time. Additionally, long-term use of methadone can also cause reduced libido and sexual dysfunction in men and women, states the National Cancer Institute. These sorts of effects vary with each individual and dosage amount, yet they have the potential to alter a person's lifestyle and health, and should be weighed against the therapeutic effect of taking methadone for long periods of time.
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Physical effects

The effects of a methadone overdose are: Slow and shallow breathing, blue fingernails and lips, stomach spasms, clammy skin, convulsions, weak pulse, coma, and possible death
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Withdrawal Effects

When use is stopped, individuals may experience withdrawal symptoms including: Anxiety, muscle tremors, nausea, diarrhea, vomiting, and abdominal cramps.
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Medical Treatment options

Methadone is commonly prescribed to help treat opiate dependence. Psychosocial approaches to such dependence are successful in helping keep users in their treatment programme and result in better treatment outcomes than methadone alone.
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Psychological treatment options

Since 1972, methadone has been the primary medicine used to help people recover from dependence on heroin or prescription pain medication. Methadone is an opioid that helps reduce cravings and withdrawal by attaching to the same brain receptors as opioids such as heroin or prescription pain medication. Therapy with methadone lowers the risk that the patient may begin abusing opioids again by suppressing withdrawal symptoms.

Methadone has helped many patients successfully manage their opioid dependence. Patients may stay on methadone for a period of several months to a few years. Some people benefit from lifelong treatment. Individuals being treated with methadone may need to visit a clinic on a daily basis to receive their medication.
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Related drugs

The drugs that are similar to methadone are:

buprenorphine
naloxone
diamorphine
dihydrocodeine
dextropropoxyphene
dipipanone
dextromoramide

Related synthetic

Although chemically unlike morphine or heroin, methadone produces many of the same effects. It is available under the names: 

Levo-Polamidone
Polamidone
Heptanone
Heptadone
Heptadon

References

[1] http://www.indro-online.de/discovery.pdf
[2] http://www.cesar.umd.edu/cesar/drugs/methadone.asp
[3] http://www.nhtsa.gov/people/injury/research/job185drugs/methadone.htm
[4] http://www.cancer.gov/cancertopics/pdq/supportivecare/sexuality/HealthProfessional/page5/print
[5] http://www.livestrong.com/article/209186-long-term-effects-from-methadone-use/
[6] http://www.bis.gov.uk/files/file15406.pdf
[7] http://cmsaz.net/index.php?option=com_content&view=article&id=71&Itemid=99