Drug Guide

Methadone

By Anthony McDaniel, M.D.

Methadone (also known as Symoron, Dolophine, Amidone, Methadose, Physeptone, Heptadon, Phy and many other names) 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 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 owing to its long duration of action and very low cost. Methadone was introduced into the United States in 1947 by Eli Lilly and Company. Methadone is useful in the treatment of opioid dependence. It has cross-tolerance with other opioids including heroin and morphine and a long duration of effect. Oral doses of methadone can stabilize patients by mitigating opioid withdrawal syndrome. Higher doses of methadone can block the euphoric effects of heroin, morphine, and similar drugs. As a result, properly dosed methadone patients can reduce or stop altogether their use of these substances.

Methadone is approved for different indications in different countries. Common is approval as an analgesic and approval for the treatment of opioid dependence. It is not intended to reduce the use of non-narcotic drugs such as cocaine, methamphetamine, or alcohol. Today, a number of pharmaceutical companies produce and distribute methadone. The racemic hydrochloride is the only form available in most countries, such as the Netherlands, Belgium, France and in the United States, as of March 2008. The tartrate and other salts of the laevorotary form (levomethadone, with trade names including Polamidone and Heptadon) are available in Europe and elsewhere. These are possibly more potent and lack the cardiac effects such as lengthened QT interval caused by the dextrorotary form. The major producer remains Mallinckrodt, who 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.

As with other opioid medications, tolerance and dependence usually develop with repeated doses. Tolerance to the different physiological effects of methadone varies; tolerance to euphoria develops quickly, whereas tolerance to constipation, sedation, and respiratory depression develops slowly (if ever). Withdrawal symptoms have shown to be up to twice as severe than those of morphine or heroin at equivalent doses and are significantly more prolonged; methadone withdrawal symptoms can last for several weeks or more. A general guideline is a 1:1 ratio for trouble free detox. Being on a constant dose of say 100 mg. for one year, can take 18–24 months for safe detoxification. At high maintenance doses, sudden cessation of therapy can result in withdrawal symptoms described as "the worst withdrawal imaginable," lasting from weeks to months. There is a trend in the management of opiate addiction towards the reduction of a patient's methadone dosage to a point where they can be switched to buprenorphine or another opiate with an easier withdrawal profile. When detoxing at a recommended rate (typically 1-2 mgs per week), withdrawal is either minimal or nonexistent, as the patient's body has time to adjust to each reduction in dose.

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