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The actions of O-DSMT are similar to that of Tramadol, but it has a shorter half-life and lower potency than Tramadol. The metabolic pathways that produce O-DSMT are controlled by the presence or absence of the functional CYP2D6 enzyme, which can vary between individuals (see CYP2D6 genotype). The analgesic efficacy of O-DSMT is low compared to other opioids, but there is a significantly greater analgesic tolerance than other opioids.
O-Desmethyltramadol (O-DSMT) is an active metabolite of Tramadol. It is likely to be substantially inactive at the mu-opioid receptor as it does not appear to bind significantly to this receptor. The analgesic effects of O-DSMT are significantly lower than that of Tramadol, but tolerance to the analgesia is significantly greater.
Tramadol is a narcotic analgesic with weak opioid receptor agonist activity due to its active metabolite tramadol-O-desmethyl Tramadol (O-DSMT). Still, it is structurally unrelated to other opioid drugs. Because Tramadol has the potential for tolerance development, unlike traditional opioids, it is considered a "tolerance-building" opiate.
O-DSMT is a synthetic opioid with a weaker analgesic potency than Tramadol and a shorter half-life. O-DSMT can act as a prodrug of cyclohexylmethylthiofentanyl (CHMF) upon metabolism.
Oxycodone is a synthetic opioid used for pain relief and cough suppression. It is considered to be a strong opioid analgesic, used in moderate to severe pain as well as post-operative pain.
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Desmetramadol (INN), also known as O-desmethyl Tramadol (O-DSMT), is an opioid analgesic and the main active metabolite of Tramadol.
Sixteen patients have been reported who have developed seizures after taking Tramadol in combination with a CYP2D6 inhibitor, including three fatalities. In some cases, the seizure risk is increased when only one antagonist is taken (e.g., paroxetine or fluoxetine). In contrast, it can be minimized if two drugs at the same time are used that inhibit different metabolites (e.g., nefazodone and fluoxetine).
Tramadol is a drug that acts as an analgesic. When combined with drugs that inhibit the metabolic pathway of Tramadol, seizures may occur because of increased serum concentrations of the tramadol metabolite O-desmethyl tramadol.
The CYP2D6 enzyme metabolizes a wide range of pharmaceutical compounds, including many antidepressants and analgesics used to treat chronic pain. Tramadol is one such analgesic and is commonly prescribed for both acute and chronic pain syndromes.
The liver enzyme CYP2D6 demethylates Tramadol in the same way as codeine. So similar to the variation in effects seen with codeine, individuals with a less active form of CYP2D6 ("poor metabolizers") tend to get reduced analgesic effects from Tramadol. This also results in a ceiling effect (dependent on CYP2D6 availability) which limits Tramadol's range of therapeutic benefits in treating moderate pain.
Desmetramadol is an opioid analgesic and the main active metabolite of Tramadol. Desmetramadol is derived from the metabolism of Tramadol, which is mostly dependent on the activity of cytochrome P450 enzyme CYP2D6, with very low contribution from the alternative pathway CYP3A4.
Desmetramadol (INN), also called O-Desmethyltramadol (ODST), is an opioid analgesic and an active metabolite of Tramadol. It can be used in treating moderate to severe pain and is a moderate analgesic with a potency similar to morphine.