O-Desmethyltramadol

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Death may occur when opiates are combined with other depressants such as benzodiazepines, barbiturates, thienodiazepines, alcohol or other GABAergic substances.[1]

It is strongly discouraged to combine these substances, particularly in common to heavy doses.

O-Desmethyltramadol
Skeletal structures of molecules of the (1R,2R) (Left) and (1S,2S) (Right) isomers of O-desmethyltramadol.
O-Desmethyltramadol (Racemate).svg
Chemical Nomenclature
Common names O-Desmethyltramadol
Substitutive name O-DSMT
Systematic name 3-(2-((dimethylamino)methyl)-1-hydroxycyclohexyl)phenol
Class Membership
Psychoactive class Opioid
Chemical class Phenyl / Cyclohexane
Routes of Administration

WARNING: Always start with lower doses due to differences between individual body weight, tolerance, metabolism, and personal sensitivity. See responsible use section.



Oral
Dosage
Threshold 5 - 10 mg
Light 10 - 25 mg
Common 25 - 50 mg
Strong 50 - 100 mg
Heavy 100 mg +
Duration
Total 3 - 6 hours
Onset 20 - 40 minutes
Peak 2 - 3 hours
Offset 2 - 3 hours
After effects 1 - 2 hours









DISCLAIMER: PW's dosage information is gathered from users and resources for educational purposes only. It is not a recommendation and should be verified with other sources for accuracy.

Summary sheet: O-Desmethyltramadol

O-Desmethyltramadol (O-DSMT, desmetramadol) is an opioid analgesic and an active metabolite which is produced in the liver after the consumption of tramadol.[2] It has little to no history of human usage but is easily accessible through the use of certain online research chemical vendors.

In comparison to tramadol, O-DSMT lacks any stimulation and feels considerably closer to that of a traditional opiate. It is also stronger in terms of its potency and has a significantly shorter duration.

Chemistry

(+/-)O-Desmethyltramadol, or 3-(2-((dimethylamino)methyl)-1-hydroxycyclohexyl)phenol, is an atypical synthetic opioid. O-Desmethyltramadol is loosely analogous to codeine, but is not a morphinan opiate. Instead, it contains two rings including a cyclohexane ring that is bonded to a phenyl ring at R1. This phenyl ring is substituted at R3 with a hydroxy group (OH-). An additional hydroxy group is found at the same location the cyclohexane ring is bonded to at the phenyl ring, R1. O-DMST features a third substitution on its cyclohexane ring at R2. Here the ring is bonded to a dimethylamine group connected through a methylene bridge.

O-Desmethyltramadol is atypical as it is found in a racemate (combination) of its stereoisomers. Stereoisomers are two molecules that share the same chemical structure, but are three-dimensional mirror images of each other. Tramadol is produced as a racemate of its two isomers because the combination is proven to be more effective. Flipping the direction of the R2 and R1 bonds results in the R- and S- enantiomers of O-Desmethyltramadol. O-DMST is nearly identical to tramadol, and is named for the lack of the methyl group of tramadol's R3 methoxy substituion.

Pharmacology

O-DSMT is considerably more potent as a μ-opioid agonist compared to tramadol.[3] Additionally, unlike tramadol, it is a high-affinity ligand of the δ- and κ-opioid receptors.[4]

The two enantiomers of O-DSMT show quite distinct pharmacological profiles;[5] both (+) and (−)-O-DSMT are inactive as serotonin reuptake inhibitors,[6] but (−)-O-DSMT retains activity as a norepinephrine reuptake inhibitor,[7] and so the mix of both the parent compound and metabolites contributes significantly to the complex pharmacological profile of tramadol. While the multiple receptor targets can be beneficial in the treatment of pain (especially complex pain syndromes such as neuropathic pain), it increases the potential for drug interactions compared to other opioids, and may also contribute to side effects.

Opioids exert their effects by binding to and activating the μ-opioid receptor. This occurs because opioids structurally mimic endogenous endorphins which are naturally found within the body and also work upon the μ-opioid receptor set. The way in which opioids structurally mimic these natural endorphins results in their euphoria, pain relief and anxiolytic effects. This is because endorphins are responsible for reducing pain, causing sleepiness, and feelings of pleasure. They can be released in response to pain, strenuous exercise, orgasm, or general excitement.

Subjective effects

The effects listed below are based upon the subjective effects index and personal experiences of PsychonautWiki contributors. The listed effects should be taken with a grain of salt and will rarely (if ever) occur all at once, but heavier doses will increase the chances and are more likely to induce a full range of effects. Likewise, adverse effects become much more likely on higher doses and may include injury or death.

Physical effects
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Cognitive effects
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Toxicity and harm potential

O-DSMT has a moderate potential toxicity relative to its dose due to its potency. As with all opioids, long-term effects can vary but can include diminished libido, apathy and memory loss. It is also potentially lethal when mixed with depressants like alcohol or benzodiazepines.

O-DSMT has recently been marketed as a currently legal substitute for illegal opioid drugs, either in powder form or mixed into various other preparations. One such blend was sold under the brand Krypton and contains powdered kratom leaf (Mitragyna speciosa) laced with O-DSMT and was reportedly linked to at least 9 accidental deaths from overdose during 2010–2011.[8][9][10]

It is strongly recommended that one use harm reduction practices when using this drug.

Tolerance and addiction potential

As with other opioids, the chronic use of O-DSMT can be considered moderately addictive with a high potential for abuse and is capable of causing psychological dependence among certain users. When addiction has developed, cravings and withdrawal symptoms may occur if a person suddenly stops their usage.

Tolerance to many of the effects of O-DSMT develops with prolonged and repeated use. The rate at which this occurs develops at different rates for different effects, with tolerance to the constipation-inducing effects developing particularly slowly for instance. This results in users having to administer increasingly large doses to achieve the same effects. After that, it takes about 3 - 7 days for the tolerance to be reduced to half and 1 - 2 weeks to be back at baseline (in the absence of further consumption). O-DSMT presents cross-tolerance with all other opioids, meaning that after the consumption of O-DSMT all opioids will have a reduced effect.

Dangerous interactions

Although many drugs are safe on their own, they can become dangerous and even life-threatening when combined with other substances. The list below contains some common potentially dangerous combinations, but may not include all of them. Certain combinations may be safe in low doses of each but still increase the potential risk of death. Independent research should always be done to ensure that a combination of two or more substances is safe before consumption.

  • Depressants (1,4-BD, 2M2B, alcohol, barbiturates, benzodiazepines, GHB/GBL, methaqualone) - This combination can result in dangerous or even fatal levels of respiratory depression. These substances potentiate the muscle relaxation, sedation and amnesia caused by one another and can lead to unexpected loss of consciousness at high doses. There is also an increased risk of vomiting during unconsciousness and death from the resulting suffocation. If this occurs, users should attempt to fall asleep in the recovery position or have a friend move them into it.
  • Dissociatives - This combination can result in an increased risk of vomiting during unconsciousness and death from the resulting suffocation. If this occurs, users should attempt to fall asleep in the recovery position or have a friend move them into it.
  • Stimulants - It is dangerous to combine O-DSMT, a depressant, with stimulants due to the risk of excessive intoxication. Stimulants decrease the sedative effect of O-DSMT, which is the main factor most people consider when determining their level of intoxication. Once the stimulant wears off, the effects of O-DSMT will be significantly increased, leading to intensified disinhibition as well as other effects. If combined, one should strictly limit themselves to only taking a certain amount of O-DSMT.

Legal issues

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This legality section is a stub.

As such, it may contain incomplete or wrong information. You can help by expanding it.

There is little information online regarding the international legalities of O-Desmethyltramadol possession but it is confirmed as a controlled substance within the United Kingdom.[11]

  • United Kingdom - It is illegal to produce, supply, or import this drug under the Psychoactive Substance Act, which came into effect on May 26th, 2016.[12]

See also

External links

References

  1. Risks of Combining Depressants (Tripsit) | https://tripsit.me/combining-depressants/
  2. Effects of the central analgesic tramadol and its main metabolite, O-desmethyltramadol, on rat locus coeruleus neurons (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/8220877
  3. Pharmacology of tramadol (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/9190321
  4. Anticonvulsant and proconvulsant effects of tramadol, its enantiomers and its M1 metabolite in the rat kindling model of epilepsy (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/10991912
  5. Actions of tramadol, its enantiomers and principal metabolite, O-desmethyltramadol, on serotonin (5-HT) efflux and uptake in the rat dorsal raphe nucleus (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/9389855
  6. Effects of the central analgesic tramadol on the uptake and release of noradrenaline and dopamine in vitro (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/8467366
  7. Effects of the central analgesic tramadol on the uptake and release of noradrenaline and dopamine in vitro (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/8467366
  8. Kratom alkaloids and O-desmethyltramadol in urine of a "Krypton" herbal mixture consumer (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/21112167
  9. Krypton--new, deadly Internet drug. Since October 2009, nine young people have died in Sweden (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/21294331
  10. Unintentional fatal intoxications with mitragynine and O-desmethyltramadol from the herbal blend Krypton (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/8220877
  11. http://www.legislation.gov.uk/ukdsi/2013/9780111532980/pdfs/ukdsi_9780111532980_en.pdf
  12. Psychoactive Substances Act 2016 (Legislation.gov.uk) | http://www.legislation.gov.uk/ukpga/2016/2/contents/enacted