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Tramadol - Mechanism of action |  | Tramadol - Mechanism of action: Encyclopedia II - Tramadol - Mechanism of action |  | The mechanism of action of tramadol has yet to be fully elucidated, but it is believed to work through modulation of the GABAergic, noradrenergic and serotonergic systems. Tramadol [and its metabolite, known as M1] have been found to bind to μ-opioid receptors (thus exerting its effect on GABAergic transmission), and to inhibit reuptake of 5-HT and noradrenaline. The second mechanism is believed to contribute since the analgesic effects of tramadol are not fully antagonised by the μ-opioid receptor antagonist naloxone.
Although irrelevant to its mechanism of action, tramadol, unlike morphine, ...
See also:Tramadol, Tramadol - Mechanism of action, Tramadol - Dependence, Tramadol - Proprietary preparations |  | | Tramadol, Tramadol - Dependence, Tramadol - Mechanism of action, Tramadol - Proprietary preparations |  | |
|  |  | Tramadol: Encyclopedia II - Tramadol - Mechanism of action
Tramadol - Mechanism of action
The mechanism of action of tramadol has yet to be fully elucidated, but it is believed to work through modulation of the GABAergic, noradrenergic and serotonergic systems. Tramadol [and its metabolite, known as M1] have been found to bind to μ-opioid receptors (thus exerting its effect on GABAergic transmission), and to inhibit reuptake of 5-HT and noradrenaline. The second mechanism is believed to contribute since the analgesic effects of tramadol are not fully antagonised by the μ-opioid receptor antagonist naloxone.
Although irrelevant to its mechanism of action, tramadol, unlike morphine, has not been found to induce histamine release.
The serotonergic modulating properties of tramadol mean that it has the potential to interact with other serotonergic agents. There is an increased risk of serotonin syndrome when tramadol is taken in combination with reuptake inhibitors (e.g. SSRIs), agents that potentiate the effect of 5-HT (e.g., MAOIs), or 5-HT agonists.
Other related archives5-HT, GABAergic, German, Grünenthal GmbH, MAOIs, N02, SSRIs, analgesic, histamine, injectable, intramuscular, intravenous, morphine, naloxone, noradrenaline, noradrenergic, opioid, pharmaceutical company, serotonergic, serotonin syndrome
 Adapted from the Wikipedia article "Mechanism of action", under the G.N U Free Docmentation License. Please also see http://en.wikipedia.org/wiki |
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