Talk:Doxylamine

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Summary sheet: Doxylamine

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

This chemistry section is incomplete. You can help by adding to it.

Doxylamine is a part of the ethanolamine class of antihistamines.

Pharmacology

This pharmacology section is incomplete. You can help by adding to it.

Doxylamine has powerful antihistaminergic effects, more so than any other antihistamine available over the counter, except for diphenhydramine. Compared to diphenhydramine (Benadryl), doxylamine has a faster onset (20-30 minutes versus 45 minutes) and a shorter duration.

The primary metabolites of doxylamine are:

• N-desmethyldoxylamine
• N,N-didesmethyldoxylamine
• doxylamine N-oxide.

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

Subjective effects

Disclaimer: The effects listed below cite the Subjective Effect Index (SEI), an open research literature based on anecdotal user reports and the personal analyses of PsychonautWiki contributors. As a result, they should be viewed with a healthy degree of skepticism.

It is also worth noting that these effects will not necessarily occur in a predictable or reliable manner, although higher doses are more liable to induce the full spectrum of effects. Likewise, adverse effects become increasingly likely with higher doses and may include addiction, severe injury, or death ☠.

* = shared with diphenhydramine

Physical effects

• • Increased heart rate* - Doxylamine inhibits the action of acetylcholine. In the heart, acetylcholine functions as an inhibitory neurotransmitter, decreasing blood pressure and heart rate.
  • Increased blood pressure* - Doxylamine inhibits the action of acetylcholine. In the heart, acetylcholine functions as an inhibitory neurotransmitter, decreasing blood pressure and heart rate.
  • Dehydration - Dry mouth is reported to be very common with Doxylamine. Similar to DPH.
  • Motor control loss
  • Restless leg syndrome
  • Dizziness
  • Skin flushing

Cognitive effects

• • Delirium* - Because of doxylamine's blocking (antagonizing) action on muscarinic acetylcholine receptors, it causes severe delirium. It works by lowering the use potential of acetylcholine by competitively blocking the mAChRs. This causes hallucinations, severe confusion, and terror.
  • Sleepiness* - In terms of its effects on the user's physical energy levels, doxylamine is most commonly considered to be extremely tiring. It is often used and sold as a sleep aid at 25 and 12.5 mg dosages.
  • Cognitive euphoria - This effect is only present in low doses; in higher doses, it transforms intoDysphoria*
  • Delusions*
  • Delirium*
  • Increased libido - This effect is only present in low doses.
  • Unspeakable horrors*

Visual effects

• • Drifting*
  • Internal hallucinations*
  • External hallucinations*
  • Depth perception distortions

Auditory effects

• • Hallucinations*
  • Enhancements*
  • Suppression*

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:

• Erowid Experience Vaults: Doxylamine

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.

Toxicity and harm potential

This toxicity and harm potential section is a stub. As a result, it may contain incomplete or even dangerously wrong information! You can help by expanding upon or correcting it. Note: Always conduct independent research and use harm reduction practices if 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.

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.

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 [[Cross-tolerance::all deliriants]], meaning that after the consumption of doxylamine, all deliriants will have a reduced effect.

Dangerous interactions

This dangerous interactions section is a stub. As such, it may contain incomplete or invalid information. You can help by expanding upon or correcting it.

Warning: Many psychoactive substances that are reasonably safe to use on their own can suddenly become dangerous and even life-threatening when combined with certain other substances. The following list provides some known dangerous interactions (although it is not guaranteed to include all of them).

Always conduct independent research (e.g. Google, DuckDuckGo, PubMed) to ensure that a combination of two or more substances is safe to consume. Some of the listed interactions 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

This legality section is a stub. As such, it may contain incomplete or wrong information. You can help by expanding it.

• US: Doxylamine is OTC.
• Russia: Doxylamine is only available through a prescription.

See also

• Responsible use

External links

• Doxylamine (Wikipedia)