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Methadone Information

Drug Class: Narcotic Analgesic

Trade Names: Dolophine, Methadose

Description: Methadone is a synthetic opiate (opioid), first synthesized by German scientists during World War II and made commercially available in the United States in 1947. Although it was originally developed for use as an analgesic, methadone is mainly used today as a substitute for heroin in order to relieve some of the problems associated with heroin addiction. It is usually prescribed as a liquid syrup to be taken orally, but is also manufactured as tablets and ampoules for injection. Methadone maintenance programs are intended to reduce the risks associated with heroin addiction, such as heroin overdose, HIV or hepatitis infection from shared syringes, and risks due to criminal activity associated with the illicit drug market. Methadone mimics many of the effects of opiates such as heroin. However, there are many differences. For example, heroin produces an almost immediate "rush" or brief period of euphoria, which wears off relatively quickly, resulting in a strong craving to use more heroin. In contrast, methadone has a more gradual onset of action when administered orally. Its effects can last up to 24 hours, which allows the patient to take methadone only once a day without experiencing withdrawal symptoms. Research has demonstrated that, when methadone is given in regular doses by a physician, it has the ability to block the euphoria caused by heroin if the individual does try to take heroin. Despite methadone's role in the treatment of heroin addiction, it has addictive properties and also a high potential for abuse on the street. Methadone enters the illicit drug market primarily as a result of patients selling their prescriptions.

Excretion: In the 24-hour urine following a 5 mg oral methadone dose, unchanged methadone accounted for 5% of the dose, EDDP for 5%, and EMDP for less than 1%. In the 24-hour urine of methadone maintenance subjects, unchanged methadone may account for 5% to 50% of the dose and EDDP for 3% to 25%, with large variations due to urine pH, urine volume, dose, and rate of metabolism. Urinary concentrations of methadone and EDDP in these subjects ranging from 1,000 ng/ml to 50,000 ng/ml are commonly encountered.

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