Talk:Doxylamine

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Summary sheet: Doxylamine
Doxylamine
Doxylamine.svg
Chemical Nomenclature
Common names Unisom, doxylamine, doxylamine succinate
Systematic name N,N-dimethyl-2-(1-phenyl-1-pyridin-2-ylethoxy)ethanamine
Class Membership
Psychoactive class Deliriant
Chemical class Ethanolamine
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
Bioavailability 24.7%[citation needed]
Threshold 6.25 mg
Light 6.25 - 10 mg
Common 10 - 20 mg
Strong 20 - 50 mg
Heavy 50 mg +
Duration
Total 6 - 8 hours
Onset 20 - 30 minutes
After effects 1 - 6 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.


Doxylamine is a first generation antihistamine affecting histamine at H1 receptors. In addition, it has powerful anticholinergic effects. It is very closely related to diphenhydramine, an agent with the same properties and OTC status.

Chemistry

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Doxylamine is a part of the ethanolamine class of antihistamines.

Pharmacology

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Doxylamine has powerful antihistaminergic effects, more so than any other antihistamine available over the counter[citation needed], except for diphenhydramine. Compared to diphenhydramine (Benadryl), doxylamine has a faster onset and a shorter duration.

The primary metabolites of doxylamine are:

Doxylamine can cause false-positives for methadone in high enough doses.[1]

Subjective effects

The effects listed below are based upon the subjective effects index and personal experiences of PsychonautWiki contributors. These 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 of inducing a full range of effects. Likewise, adverse effects become much more likely on higher doses and may include serious injury or death.

* = shared with diphenhydramine


Physical effects
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Cognitive effects
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Experience reports

There are currently no anecdotal reports which describe the effects of this compound within our experience index. Additional experience reports can be found here:

Medical Uses

Doxylamine is used with pyridoxine to prevent morning sickness. It's also used as an over-the-counter sleep aid useful for alleviating short-term insomnia. Doxylamine is also a useful cough suppressant.[citation needed]

Toxicity and harm potential

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We also recommend that you conduct independent research and use harm reduction practices when using this substance.

For healthy adults, doxylamine is usually safe. The IARC has concluded that carcinogenic effects in humans are not a high-risk factor. Anticholinergic effects can pile up with other anticholinergics such as DPH, atropine, hyoscine, and hyoscyamine, tricyclic antidepressants, and some antipsychotics like promethazine and quetiapine. This can cause greatly increased delirium and heart rate/blood pressure. Additionally, doxylamine in high doses can cause rhabdomyolysis (the breakdown of skeletal muscle tissue), making it quite dangerous to frequently use or use large quantities.[2][3]

User should note that doxylamine can be extremely unpredictable and the mechanism by which it produces hallucinations has the potential to result in serious injury, hospitalization or death. Additionally, doxylamine puts users in a state where they have little control over their actions. Doxylamine can provoke bizarre and nonsensical behavior which may put the user at risk. It is strongly recommended that one use harm reduction practices when using this substance.

Lethal dosage

The LD50 is around 470mg/kg in mice.[4]

Tolerance and addiction potential

Doxylamine produces dependence with chronic use. In comparison to other hallucinogens, doxylamine has been reported to have significantly less abuse potential than other hallucinogens. This is simply because the vast majority of people who try it do not wish to repeat the experience.

Tolerance to many of the effects of doxylamine develops with repeated use. This results in users having to administer increasingly large doses to achieve the same effects. After that, it takes about 1 - 2 weeks for tolerance to return to baseline (in the absence of further consumption). Doxylamine presents cross-tolerance with all deliriants, meaning that after the consumption of doxylamine, all deliriants will have a reduced effect.

Dangerous interactions

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Although many psychoactive substances are reasonably safe to use on their own, they can quickly become dangerous or even life-threatening when taken with other substances. The following lists some known dangerous combinations, but cannot be guaranteed to include all of them. Independent research should always be conducted to ensure that a combination of two or more substances is safe to consume. Some interactions listed have been sourced from TripSit.

  • Stimulants - Because doxylamine increases BPM and BP and stimulants also do this, cardiac arrest, hypertensive crisis, stroke, and heart attack all become much more likely to occur. With very high doses, delirium can be potentiated to an extremely high level.
    • Bupropion - Bupropion also has deliriant-like effects by antagonizing cholinergic receptors.
  • Depressants - Depressants can make the sleepiness effect of doxylamine extremely pronounced, leading to a severe cognitive deficit. Therefore, any activity that must be done sober (driving, using firearms, etc.) must absolutely not be done.
  • Anticholinergics - Combining doxylamine with other antimuscarinics such as datura, diphenhydramine, and nutmeg can severely increase BPM and BP, and as such, cardiac arrest, hypertensive crisis, stroke, and heart attack all become much more likely to occur.
    • Bupropion - Bupropion also has deliriant effects by inhibiting nicotinic acetylcholine receptors. It is also a stimulant, marking two dangerous interactions.
  • Selective serotonin re-uptake inhibitors (SSRIs) - SSRIs can suppress the visual effects of doxylamine. However, this combination may elevate the risk of serotonin syndrome due to doxylamine's serotonergic effects.

Legal status

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  • US: Doxylamine is OTC.
  • Russia: Doxylamine is only available through a prescription.[citation needed]

See also

External links

Literature

References

  1. Syed, H., Som, S., Khan, N., & Faltas, W. (2009). Doxylamine toxicity: seizure, rhabdomyolysis and false positive urine drug screen for methadone. - PubMed - NCBI. Retrieved from https://www.ncbi.nlm.nih.gov/pubmed/21686586. DOI Link: https://doi.org/10.1136/bcr.09.2008.0879
  2. Syed, H., Som, S., Khan, N., & Faltas, W. (2009). Doxylamine toxicity: seizure, rhabdomyolysis and false positive urine drug screen for methadone. - PubMed - NCBI. Retrieved from https://www.ncbi.nlm.nih.gov/pubmed/21686586. DOI Link: https://doi.org/10.1136/bcr.09.2008.0879
  3. Leybishkis, B., Fasseas, P., & Ryan, K. F. (2001). Doxylamine overdose as a potential cause of rhabdomyolysis. - PubMed - NCBI. Retrieved from https://www.ncbi.nlm.nih.gov/pubmed/11465247
  4. ScienceLab - Material Safety Data Sheet Doxylamine succinate MSDS | http://www.sciencelab.com/msds.php?msdsId=9923890