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Methadone was orignally synthesized by chemists during World War II in Germany as a substitute for the pain reliever morphine. Methadone has about the same analgesic strength as morphine, but it is longer acting (25 hours v 2-6 hours). Methadone was first available commercially in the United States in 1947, and was initially used as a long-acting pain killer. It was not until the mid-1960's that Methadone began to be used to treat chronic narcotic addiction.

The main pharmacological properties of methadone are similar to morphine and other opiate narcotics (Demerol, codeine, Dilaudid, Oxycontin, Heroin, etc.). Cross tolerance occurs with all the opiates, that is, the administration of one opiate will eliminate the withdrawal symptoms of any other opiate. The major difference among the opiates is the strength, length of action, and most effective route of use. Methadone is as strong as morphine. Its effects last 24-26 hours, and it is most effective when ingested orally. All methadone preparations (tablet v liquid) are equally effective at equal doses. Only the vehicle, the "stuff" which the active medication is added and held together with, differs. Preference for one form of methadone over another is merely a matter of personal preference, and has no basis in pharmacology.

Methadone is a tolerance-producing central nervous system depressant. It produces insensitivity to pain, sedation, slowing of respirations, lowering of blood pressure, constipation, slowing of pulse, and nausea. The subjective effects following single doses in non-addicted individuals are similar to those noted after morphine or heroin use; feelings of well being, drowsiness and euphoria.

Tolerance develops to the pain-relieving, nauseant, sedative, euphoric, respiratory and cardiovascular effects. However, no tolerance develops to methadone's ability to prevent withdrawal symptoms. Therefore, once the opiate-addicted individual is stabilized on methadone, she/he can function normally (physically and psychologically) without requiring ever increasing doses to eliminate withdrawal symptoms and remain physiologically comfortable. This occurs regardless of the stabilizing dose of methadone. In some patients, and at higher doses, methadone may help decrease anxiety although it is not effective as a potent mood elevator.

The most common side effects of methadone are weight gain, constipation, increased intake of fluids, increased frequency of urination, tingling in the hands and feet, increased sweating, skin rash, nausea, and delayed ejaculation. However, these symptoms are typically mild and temporary.

Methadone is administered orally and is gradually absorbed into the body through the intestines and liver. From the liver, it is released slowly into the blood stream. This slow release into the blood stream keeps maintenance patients from experiencing a rapid narcotic high and keeps them above the blood level for experiencing intense withdrawal symptoms. Methadone can also chemically block the craving for opiates, even though it does not produce the euphoria of the short-acting opiates. At doses greater than available in illicit opiates, methadone produces a "blocking effect" to the high of illicit opiates. However, methadone does not block the intoxicating effects of non-opiate drugs, such as alcohol, sedatives, tranquilizers and stimulants. Use of other intoxicating drugs may produce overdose and death. Most overdoses occur when methadone maintained individuals supplement their prescribed methadone with other central nervous system depressants. Particularly dangerous when used in combination with methadone are Placidyl, Xanax, Valium, methaqualone, illicit methadone and large amounts of alcohol.

The character and severity of withdrawal symptoms that appear when an opiate is discontinued depends on many factors, particularly the drug itself, dose, duration of use, interval between doses, health, personality and expectations and motivations of the patient. The symptoms of abrupt discontinuation of methadone are insomnia, anxiety, hypertension, irritability, chills, excessive sweating, "running" nose and eyes, enlarged pupils, sore, achy joints and muscles, muscle spasms, abdominal cramps, nausea, vomiting and diarrhea. Symptoms may appear 24-48 hours after the last dose of methadone and most major symptoms are minimal by the 14th day. However, general discomfort, loss of appetite and insomnia may persist for as long as six months. These symptoms can be drastically reduced and often eliminated by withdrawing the methadone on a slow, deliberate schedule of dose decreases managed by a physician. The longer the process, the less the discomfort during withdrawal.

Methadone maintenance is a long-term treatment for opiate addiction. The patient must regularly visit the clinic and receive daily methadone. Many patients lead normal productive lives by working, caring for their families and enjoying a healthy, active lifestyle while maintained on methadone. Methadone is not known to cause any physical or mental deterioration, even after 15 years or more of use. Since methadone programs are voluntary, the length of time a patient remains in treatment depends greatly upon the patient. Studies show that patents are more apt to stay in treatment for relatively longer periods of time if they are over 30 years old, married, have dependent children and have spent time in jail during their addiction to opiates.

Methadone is not a cure for opiate addiction. It is pharmacologic treatment which suppresses opiate withdrawal symptoms and lessens the craving for other opiates. Coupled with therapy, methadone facilitates both interpersonal interactions involved in strengthening motivation, changing lifestyles and breaking the cycle of life patterns and stress reactions which underlie relapse.

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