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Effects vary widely by individual, dose, and context.
The cognitive effects of O-Desmethyltramadol can be broken down into several components which progressively intensify proportional to dosage. The general head space of codeine is described by many as one of intense euphoria, relaxation, anxiety suppression and pain relief.
The physical effects of O-Desmethyltramadol can be broken down into several components which progressively intensify proportional to dosage.
Moderate psychological addiction potential with risk of compulsive redosing. Tolerance develops rapidly with daily use, particularly with multiple daily doses, leading users to chase progressively harder to obtain positive effects, which is identified as a major driver of dependence.
Physical dependence develops within a week of heavy daily use. Withdrawal effects match those of other opioids, including sweating, vomiting, flu-like symptoms, runny nose, chills, lethargy, and headache, though reportedly milder in intensity compared to stronger opioids like diamorphine. At least 3-5 days of moderate to strong flu-like illness should be expected upon cessation.
Fatalities have been documented in a series of 9 cases involving O-DSMT combined with kratom alkaloids (sold as 'Krypton'), though all fatalities also involved additional drugs such as antidepressants, ethanol, and benzodiazepines. Postmortem blood concentrations in these cases ranged from 0.4-4.3 μg/g. Standalone O-DSMT fatality case reports do not exist in the literature, which may reflect relatively low prevalence of use rather than inherent safety. Fatal outcomes are suspected to be more likely at high doses or in combination with other CNS depressants.
Long-term chronic use may be associated with elevated hepatic damage markers including α-GST, ALT, AST, ALP, and GGT, particularly in individuals who are CYP2D6 extensive or ultrarapid metabolizers; however, decades of tramadol use in humans has not produced clear evidence of severe hepatotoxicity when used moderately.
Respiratory depression is the primary life-threatening effect in overdose; a sensation of labored breathing may occur at strong doses and represents a danger sign in overdose situations.
Seizure risk may be lower than with tramadol, though this has not been definitively confirmed. The (S) enantiomer demonstrated seizure-inducing capability in rats at doses that also caused significant respiratory depression. Studies of tramadol intoxication found O-DSMT plasma levels correlated with seizure onset, though co-ingestion of benzodiazepines or other opioids appeared to reduce seizure risk.
O-Desmethyltramadol has a limited independent history because it has never been marketed by pharmaceutical companies as a standalone medication, instead being encountered primarily as the principal active metabolite of the analgesic tramadol. Comparatively little research has been conducted on the…
As of January 2019, O-Desmethyltramadol is not specifically listed on controlled substance schedules. However, its status may vary by state or territory, and import regulations may still apply.
Controlled as a Class A substance, likely under provisions related to opioid analogues or specific scheduling. Class A carries the most severe penalties under the Misuse of Drugs Act 1971, with possession punishable by up to 7 years imprisonment and supply by up to life imprisonment.
As of January 2019, not scheduled under the Controlled Drugs and Substances Act. Not a controlled substance at the federal level.
As of January 2019, not specifically scheduled under the Controlled Substances Act at the federal level. However, the Federal Analogue Act may apply if sold for human consumption, as O-DSMT is structurally related to tramadol (a Schedule IV controlled substance).
