Tramadol

Tramadol hydrochloride (Ultram, Tramal) is a centrally acting synthetic analgesic used to treat moderate to moderately-severe pain. The drug has a wide range of applications, including treatment of rheumatoid arthritis, restless legs syndrome and fibromyalgia. It was developed by the pharmaceutical company Grünenthal GmbH in the late 1970s

Tramadol is a very weak μ-opioid receptor agonist, releases serotonin, and inhibits the reuptake of norepinephrine.While its analgesic action is thus rather distinct from opioids per se, tramadol is a synthetic analog of the phenanthrene alkaloid codeine. Tramadol is converted to O-desmethyltramadol, a significantly more potent μ-opioid agonist. The opioid agonistic effect of tramadol and its major metabolite(s) is almost exclusively mediated by such μ-opioid receptors. This further distinguishes tramadol from opioids in general (including morphine), which do not possess tramadol's degree of receptor subtype selectivity and which are much stronger opiate-receptor agonists. Similarly, the habituating properties of tramadol (such as they are) are arguably mainly due to μ-opioid agonism with contributions from serotonergic and noradrenergic effects.



MEDICAL USESTRAMADOL IS USED SIMILARLY TO CODEINE, TO TREAT MODERATE TO MODERATELY SEVERE PAIN. PHARMACOLOGICALLY, TRAMADOL IS SIMILAR TO LEVORPHANOL(ALBEIT WITH MUCH LOWER Μ-AGONISM), AS BOTH AGENTS ARE ALSO NMDA-ANTAGONISTS WITH SNRI ACTIVITY. DEXTROPROPOXYPHENE (DARVON) & M1-LIKE MOLECULE TAPENTADOL (NUCYNTA, A NEW SYNTHETIC ATYPICAL OPIOID MADE TO MIMIC THE AGONISTIC PROPERTIES OF TRAMADOL'S METABOLITE, M1(O-DESMETHYLTRAMADOL)) ALSO HAVE SIMILAR ACTIVITIES. TRAMADOL IS ALSO MOLECULARLY SIMILAR TO VENLAFAXINE (EFFEXOR) AND HAS SIMILAR SNRI EFFECTS, WITH ANTINOCICEPTIVE EFFECTS. IT HAS BEEN SUGGESTED THAT TRAMADOL COULD BE EFFECTIVE FOR ALLEVIATING SYMPTOMS OF DEPRESSION, ANXIETY, AND PHOBIAS BECAUSE OF ITS ACTION ON THE NORADRENERGIC AND SEROTONERGIC SYSTEMS, SUCH AS ITS "ATYPICAL" OPIOID ACTIVITY.HOWEVER, HEALTH PROFESSIONALS HAVE NOT ENDORSED ITS USE FOR THESE DISORDERS, CLAIMING IT MAY BE USED AS A UNIQUE TREATMENT (ONLY WHEN OTHER TREATMENTS FAILED), AND MUST BE USED UNDER THE CONTROL OF A PSYCHIATRIST.