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F paracetamol, with the recommended dose being one or two pills every four to six hours. Note that unlike most other opioids opiates, Tramadol is not considered a controlled substance in many countries (US and Canada, among others), and is available with only a normal prescription. According to Erowid, there have also been reports that, in a few countries, Tramadol is available over-the-counter without a prescription at all. Contents 1 Mechanism of action 2 Metabolism 3 Adverse effects 4 Dependence 5 Illegal use 6 Proprietary preparations 7 Often used to treat 8 Trivia 9 References 10 External links edit Mechanism of action The mode of action of tramadol has yet to be fully understood, but it is believed to work through modulation of the GABAergic, noradrenergic and serotonergic systems. The contribution of non-opioid activity is demonstrated by the analgesic effects of tramadol not being fully antagonised by the μ-opioid receptor antagonist naloxone. Tramadol is marketed as a racemic information regarding


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mixture with a weak affinity for the μ-opioid receptor (approximately 1 6th that of morphine). The (+)-enantiomer is approximately four times more potent than the (-)-enantiomer in terms of μ-opioid receptor affinity and 5-HT reuptake, whereas the (-)-enantiomer is responsible for noradrenaline reuptake effects (Shipton, 2000). These actions appear to produce a synergistic analgesic effect, with (+)-tramadol exhibiting 10-fold higher analgesic activity than (-)-tramadol (Goeringer et al., 1997). 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 serotonin reuptake inhibitors (e.g. SSRIs), since these agents not only potentiate the effect of 5-HT but also inhibit tramadol's metabolism. It is suggested that tramadol could be effective for alleviating symptoms of depression and anxiety because of its action on GABAergic,

information regarding the medication tramadol Re with a weak affinity for the μ-opioid receptor (approximately 1 6th that of morphine). The (+)-enantiomer is approximately four times more potent than the (-)-enantiomer in terms of μ-opioid receptor affinity and 5-HT reuptake information regarding the medication tramadol, whereas the (-)-enantiomer is responsible for noradrenaline reuptake effects (Shipton information regarding the medication tramadol, 2000). These actions appear to produce a synergistic analgesic effect information regarding the medication tramadol, with (+)-tramadol exhibiting 10-fold higher analgesic activity than (-)-tramadol (Goeringer et al. information regarding the medication tramadol, 1997). 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 sy information regarding the medication tramadol.

information regarding the medication tramadol Ndrome when tramadol is taken in combination with serotonin reuptake inhibitors (e.g. SSRIs) information regarding the medication tramadol, since these agents not only potentiate the effect of 5-HT but also inhibit tramadol's metabolism. It is suggested that tramadol could be effective for alleviating symptoms of depression and anxiety because of its action on GABAergic information regarding the medication tramadol, noradrenergic and serotonergic systems. However information regarding the medication tramadol, health professionals generally do not suggest use of the drug for treatment of such disorders. Tramadol may also be used to treat hypertension when other treatments have failed. edit Metabolism Tramadol undergoes hepatic metabolism via the cytochrome P450 isozyme CYP2D6 information regarding the medication tramadol, being O- and N-demethylated to 5 different metabolites. Of these information regarding the medication tramadol, M1 is the most significant since it has 200 times the μ-affinity of (+)-tramadol information regarding the medication tramadol, and furthermore has an elimination half-life of 9 hours compared to 6 hours for tramadol itself. In the 6% of the population who have slow CYP2D6 activity information regarding the medication tramadol, there is therefore a slightly reduced analgesic effect. Phase II hepatic metabolism renders the metabolites water-soluble and they are renally excreted. Thus reduced doses may be used in renal and hepatic impairment. edit Adverse effects The most commonly reported adverse drug reactions are nausea information regarding the medication tramadol, vomiting and sweating. Drowsiness is reported information regarding the medication tramadol, although it is less of an issue .

information regarding the medication tramadol Ethylated to 5 different metabolites. Of these information regarding the medication tramadol, M1 is the most significant since it has 200 times the μ-affinity of (+)-tramadol information regarding the medication tramadol, and furthermore has an elimination half-life of 9 hours compared to 6 hours for tramadol itself. In the 6% of the population who have slow CYP2D6 activity information regarding the medication tramadol, there is therefore a slightly reduced analgesic effect. Phase II hepatic metabolism renders the metabolites water-soluble and they are renally excreted. Thus reduced doses may be used in renal and hepatic impairment. edit Adverse effects The most commonly reported adverse drug reactions are nausea information regarding the medication tramadol, vomiting and sweating. Drowsiness is reported information regarding the medication tramadol, although it is less of an issue c.

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