Methadone

Methadone is the strongest drug, many times stronger than heroin and causing no less dependence is headed by the podium of the strongest drugs. Initially, it was synthesized as an analogue of heroin and to treat the dependence of the latter, but methadone proved to be no less harmful and dangerous preamplifier causing no less dependence.
The history of methadone – the analgesic of the opiate series of synthetic origin – has more than 70 years. It was first synthesized in 1937 by German researchers Max Bockmuil and Gustav Erhart. In 1942, the industrial production of amidone, which was used as an analgesic for experimental purposes, was established. It is characterized by low cost, it is mainly used orally. For about 30 years, methadone is used for opium and other addictions as a substitute for the so-called. “Wild” or “street” drugs (narcotic drugs manufactured, distributed and used illegally with non-medical purposes) within the so-called. “Maintenance programs” (“Methadone maintenance program”). All these thirty years around this drug raging passions, sometimes far from medicine, which is due to the great social importance of the problem of drug addiction in general and, accordingly, the substances that cause it, in particular.

In the treatment of dependence on drugs (in particular, heroin), methadone is used as a substitute for heroin.

Methadone causes the same dependence as heroin. Methadone “breakage” occurs 3-4 weeks, while heroin – a few days. Overdose of methadone in almost 100% of cases ends in a lethal outcome. Compared with heroin, methadone is easier to manufacture, it is cheaper, and because of the lack of the need for intravenous injection, it also protects drug addicts from HIV.

However, a drug addict who takes methadone in a doctor’s dose, orally, does not get those euphoric sensations as when taking heroin, and seeks to get them through other means. Therefore, drug users prefer to inject methadone intravenously, at a higher dosage, along with a long period of “breakage” and a high cost in the cheroth market (which, in turn, is determined longer than heroin (up to 2 days), the duration of exposure On the body), makes controversial the use of methadone for rehabilitation.

In many countries, methadone is on Schedule I of the List of narcotic drugs, psychotropic substances and their precursors to be controlled (trafficking is prohibited).

Pharmacokinetics
Methadone is well absorbed with enteral application (41-90%). In the blood plasma the drug is detected as early as 30 minutes after administration, and the peak concentration occurs after 4 hours. Symptoms of analgesia appear 30-60 minutes after ingestion. After subcutaneous administration, a sufficient concentration in the blood is reached after 10 minutes, and peak concentration in the brain tissue after 1-2 hours.

Methadone binds strongly to blood and tissue proteins, so when repeated injections can accumulate in tissues. The half-life of methadone after a single intravenous administration is 14 hours, and half of the remaining dose is withdrawn within 55 hours as the tissue stocks of the drug are depleted. With the systematic administration of methadone, the half-life of the methadone is 22 hours.

pharmachologic effect
The clinical and pharmacological action of methadone is the same as that of morphine. Despite the long half-life (14 hours), the duration of analgesia does not exceed 4-5 hours. With repeated administration, a cumulative effect is observed (release of methadone from tissues). In the case of prolonged enteral administration, subsequent dosages of methadone should be reduced or increased intervals between doses.

Use in the clinic
Methadone is considered an excellent analgesic, the most suitable for eliminating chronic pain. It is used in the treatment of heroin addiction.