Methadone: Effects, Uses & Risks

Methadone is known as an active ingredient in heroin withdrawal. The opioid has powerful analgesic effects.

What is methadone?

Methadone is known as an active ingredient in heroin withdrawal. The opioid has powerful analgesic effects. Methadone is an opioid that is produced entirely synthetically. The active ingredient became known as a substitute for heroin withdrawal. Since 2005, methadone has been on the WHO list of essential medicines. Methadone was developed in 1937 by the German chemists Max Bockmühl (1882-1949) and Gustav Ehrhart (1894-1971), who worked for I.G. Farben. A patent application for the active ingredient followed in 1938. However, the analgesic effect of methadone was not established until 1942. Definitive proof of this effect was provided in 1945. After the end of the Second World War, methadone reached the USA through the expropriation of patents and regulations, where it received its common name in 1947. The manufacturing right could be acquired by any company, so methadone was marketed under different names. After I.G. Farben was dissolved in Germany in 1949, the drug also entered the market there as a strong analgesic. The use of methadone as a substitute against heroin dependence began in the 1960s. In this context, the drug served as a substitute. In this way, patients were to achieve sustained abstinence from heroin.

Pharmacological effect

The therapy of a heroin addiction includes not only fighting the physical addiction, but also the psychological dependence. After stopping the drug, the affected person thinks only about how to obtain it again. She also suffers from nausea, sweating and trembling. In such a case, physicians also speak of craving. Methadone is used to combat this effectively. The synthetic opioid binds to the same docking sites in the body as heroin. However, because it blocks the receptors for a longer period of time, the euphoria that occurs with heroin use is much less pronounced and the typical “heroin kick” is absent. Another effect is the reduction or prevention of withdrawal symptoms. If the correct methadone dose is achieved, the patient is able to cope with everyday life more easily again. In addition, he feels better without the withdrawal symptoms and has control over his physical and mental strength again. In this way, he can gradually return to a normal life. The effect of methadone, which is administered orally, begins about 30 minutes after it is administered. About four hours after ingestion, the drug reaches its peak effect, which prevails for about 24 hours, provided the correct dosage has been chosen. About 80 percent of methadone is absorbed in the intestine. From there, it reaches the central nervous system, where it exerts its positive effect. The drug is excreted via the kidneys. Methadone achieves a faster effect when it is injected into the bloodstream for the treatment of pain. Even then, the drug is eliminated from the body via the kidneys.

Medical application and use

For use, methadone is primarily used to combat heroin addiction. In this way, heroin is replaced by another drug whose administration is controlled. Over time, the methadone dose decreases more and more to gradually wean the affected person off heroin. As levomethadone, the opioid is also administered to treat severe pain. This may be the case, for example, in cancer patients. It is also discussed whether methadone may have a positive influence on the fight against tumors. Individual cases suggest this, but no large-scale studies have been funded to date. Methadone is administered orally by swallowing a syrup. The drug is taken once a day, which is done under the supervision of a physician or pharmacist in the initial phase. After a certain period of therapy, it is possible for the patient to take his or her weekly methadone requirement in the comfort of his or her own home. If methadone is used for pain, it can be administered in the form of drops or injectable solutions. The recommended daily dose varies between 2.5 and 7.5 milligrams.

Risks and side effects

During the initial phase of methadone treatment, various side effects may be experienced. These primarily include sedation, which is experienced during the first four to six weeks. The sedative effect usually diminishes as treatment progresses. Sweating and constipation are also common, due to the effects of methadone on the autonomic nervous system. However, as treatment progresses, the nervous system becomes tolerant to methadone. Other conceivable side effects include headache, nausea, vomiting, itching, dry mouth, slower breathing, and sleep disturbances. In such cases, lowering the methadone dose may be appropriate. Methadone poisoning caused by an overdose is of particular concern. This can sometimes even assume life-threatening proportions. However, the risk of dying from untreated heroin addiction is significantly higher. Reasons for deaths from methadone include improper intake or the use of other drugs such as alcohol. Among other things, this increases the risk of respiratory paralysis. Methadone intoxication is noticeable by a flat slow pulse, constriction of the pupils, drop in blood pressure, loss of consciousness and decreased respiration. In the worst cases, respiratory arrest may occur. If such symptoms develop, an emergency physician should be notified immediately. Methadone should not be administered if the patient is suffering from significant liver dysfunction.