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| Drug Class:
Narcotic
Analgesic |
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| Trade
Names: Dolophine, Methadose |
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| 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 methadones 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. |
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| 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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