Opium analgesic Tramadol
by admin on December 20, 2010
Tramadol (TRM), chemical name: 2 – (e) – [(dimethylamino) methyl] -1 – (e) – (3-methoxyphenyl)-cyclone hexane-1-(a) is a synthetic opium agonist with properties -anta-gonista, centrally acting analgesic of moderate strength, like codeine, Pentazocine, Propoksifenu. It is widely and effectively used for analgesia in the treatment and surgery, particularly in the coronary, cancer and orthopedic pain. The remedy is a hydrochloride, TRM, and is available under different names: Mabron (Cyprus), and Mendesik Tradol (India), Sintradon (Yugoslavia), Protradon (Czech Republic) and others, but most common in the Russian Federation is the TRA-MAL, manufactured under license Company Gryunental (Germany), which has been synthesized, studied and released the drug for therapeutic use in the world market. In the early stages of learning TRM when it was installed opium mechanism of analgesic action (TRM possesses selectivity for opium receptors), it was referred to narcotic analgesics. However, further research and application experience in clinical practice have shown a low incidence of side effects of opiate-type. which include, above all the weakening of respiratory function, the manifestation of euphoria, the development of drug dependence and tolerance, at the therapeutic (100 mg) and even triple therapy (300 mg ) doses of TPM compared with equivalent doses of analgesic effects of morphine. Side effects that are typical in the case of receiving opium such as nausea, dizziness, vomiting, weakness, dryness of the mouth occur with prolonged use of TRM, but do not exceed 5% of the total registered around 13,000 cases. Even more rare manifestations are of respiratory depression, urinary retention, constipation. Development of tolerance and drug dependence with chronic administration of therapeutic doses of TPM is exceptional and it was not mentioned when using TPM for three months (225-258 mg daily), as the expression of withdrawal syndrome. Special experiments with the participation of twelve former drug addicts and six opium-dependent addicts undergoing methadone treatment, it was showing that TPM does not produce morphine-like effect, has a low drug activity, and not a substitute for morphine in opiate addiction for people with low or moderate levels of opiate dependence, at least up to doses of 300 mg. With regard to the inhibition of opium, binding TRM is 10 times less effective than codeine in 1000 than methadone, and 6000 times than morphine. To produce morphine-like effects in tolerant subjects require higher doses. According to the currently accepted classification TPM are not drugs and attributed to strong agents. In appointing the TPM, restrictions are imposing on certain activities related to the need to show quick response, and advised to avoid prolonged periods of admission. Nevertheless, there are indications of non-medical use of TRM persons with opiate (heroin) addiction at doses much higher than therapeutic. In this case, a large number of side effects, including the development of addiction to the drug. This necessitates the study of the effect of high doses of TPM and a direct comparison with the prototypical opium.