Tramadol hydrochloride (Tramadol) trans-(+)- 2 - [(dimethylamino) methyl] -1 - (3-methoxyphenyl) cyclohexanol (as hydrochloride). It is a white crystalline powder, odorless, bitter taste, easily soluble in water and ethanol.
Mode of action - to activate opiate receptors (mu, delta and kappa) in the pre-and postsynaptic membranes of nociceptive afferent fiber systems in the brain and the digestive tract, promotes the opening of potassium and calcium channels, causing hyperpolarization of the membrane and inhibits the conduct of the nerve impulse. Slows down the destruction of catecholamines and stabilize their content in the CNS. Analgesic effect is caused by decreased activity of nociceptive and increase - antinociceptive systems.
The first publications on the use of Tramadol in the clinic are beginning 80-ies of XX century, ie its medical use is already 20-year history.
Opioid agonists m (mu) receptors include substances and drugs of different analgesic power, including the traditional strong opioid painkillers - morphine, fentanyl, piritramid, as well as the less powerful - promedol, prosidol, tramadol, codeine. This group is characterized by opioids such adverse properties associated with depression stem structures and centers of the medulla oblongata, like sedation (rarely, euphoria), general weakness, depression of cough reflex, in large doses - respiratory depression (bradypnea, apnea) and cardiovascular (hypotension, bradycardia) . In addition to these inhibitory influences of opioid agonists have an activating effect on the vomiting center to the possible development of nausea and vomiting, as well as on smooth muscles of hollow organs, resulting in dysmotility may be the last (constipation, urinary retention, and bile, a tendency to bronchospasm). All of these serious side effects are most pronounced in the most powerful of opioid analgesics (fentanyl, morphine) and less evident in preparations with less analgesic potential [16].
All opioid agonists, except for tramadol, have a specific ability to cause dependence - physical and mental, so they included the International Convention on the drug in the category of drugs under control [47], and are subject to special rules for the appointment, discharge, record keeping, storage, transportation, accounting, certain relevant orders of the Ministry of Health