VelocideX
Bluelighter
- Joined
- May 26, 2003
- Messages
- 4,745
Neophyte said:Be very carefull, according to the MIMS, basically the drug information book for docs/nurses/pharms, tramadol is actually an MAOI, MAOI+MDxx=dangerous, and MAOI's can be dangerous even after their halflife has expired
Really? I can't find that anywhere in MIMS.
Contraindications: Intoxication with alcohol, hypnotics, analgesics, opioids, psychotropics; MAOIs (concurrent or in the previous 14 days); not for use in narcotic withdrawal; opioid sensitivity; pregnancy
Drug Interactions: MAOIs (see Contra); CNS depressants incl anaesthetics, alcohol; mixed opiate agonists/ antagonists eg buprenorphine, pentazocine; drugs which lower seizure threshold eg SSRIs, TCAs, antipsychotics; carbamazepine; quinidine; ketoconazole, erythromycin; drugs that increase serotonin; coumarin derivatives
Tramadol is a centrally acting synthetic analgesic of the aminocyclohexanol group with opioid-like effects. It is not derived from natural sources, nor is it chemically related to opiates.
Pharmacology. Although preclinical testing has not completely explained the mode of action, at least two complementary mechanisms appear applicable: binding to mu-opioid receptors and inhibition of reuptake of noradrenaline and serotonin. The opioid-like activity of tramadol derives from low affinity binding of the parent compound to mu-opioid receptors and higher affinity binding of the principal active metabolite, mono O-desmethyltramadol, denoted M1, to mu-opioid receptors. In animal models, M1 is up to six times more potent than tramadol in producing analgesia and 200 times more potent in mu-opioid binding. The contribution of tramadol to human analgesia, relative to M1, is unknown.
Both human and animal studies have shown that antinociception induced by tramadol is only partially antagonised by the opiate antagonist naloxone. In addition, tramadol has been shown to inhibit reuptake of noradrenaline and serotonin in vitro, as have some other opioid analgesics. These latter mechanisms may contribute independently to the overall analgesic profile of tramadol.