Talk:Doxylamine

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Template:SubstanceBox/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.

History and culture

This History and culture section is a stub. As a result, it may contain incomplete or wrong information. You can help by expanding it.

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.

Pharmacology

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

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

This subjective effects section is a stub. As such, it is still in progress and may contain incomplete or wrong information. You can help by expanding or correcting it.

Physical effects

* = shared with diphenhydramine

• 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.

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*

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. 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 is not addictive, but insomniacs can become dependent on the use of doxylamine to fall asleep.

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.
• Antimuscarinics - 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.

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.

See also

• Responsible use

To Brack

I undid this because:

1. Wikipedia, although it is based on good faith, is not an acceptable source. I tried going to the stated reference there and it brought me to a DNS error.

2. I have found other references that dispute this.

3. The range of 50-500 is extremely broad when referring to an LD₅₀.

If you can find another source of numbers, please do so. I don't like redoing edits, because I find it comes off as condescending or rude, but I decided this was necessary. --Corticosteroid (talk) 01:12, 15 September 2017 (CEST)