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Table of Contents

1. History and Culture
2. Chemistry
3. Pharmacology
4. Physical Effects
5. Visual Effects
6. Cognitive Effects
7. Auditory Effects
8. Medical Uses
9. Toxicity and Harm Potential
10. Lethal Dosage
11. Tolerance and Addiction Potential
12. Dangerous Interactions
13. Legal Status

Exploring Doxylamine: A Potent Deliriant with Medicinal Potential

Introduction to Doxylamine

Doxylamine, known under various brand names such as Unisom, Vicks, Robitussin, and Coricidin, belongs to the ethanolamine class of deliriants. As an alternative active antihistamine to diphenhydramine, it is commonly utilized in over-the-counter (OTC) cold medicines. Additionally, it is employed as a morning sickness medication when combined with vitamin B6. Administered in therapeutic doses, it serves as a hypnotic and allergy medication. However, when consumed excessively, it acts as a deliriant akin to diphenhydramine and datura. Typically found in the form of a 25mg pill, doxylamine is often presented as its succinic acid salt, known as doxylamine succinate.

Historical Context and Medical Use

First described around 1948 or 1949, doxylamine gained prominence through its inclusion in a morning sickness formula called Bendectin, comprising doxylamine, vitamin B6, and dicyclomine. Presently, it serves as an OTC medication for short-term insomnia and allergies, with additional applications in alleviating nausea and morning sickness among pregnant individuals.

Pharmacological Effects and Subjective Experience

Doxylamine exerts its pharmacological effects as a reverse agonist of the H1-histamine receptor and a mild antagonist of the muscarinic acetylcholine M1-5 receptors. Its subjective effects closely resemble those of other generation 1 antihistamines, encompassing dry mouth, vivid external hallucinations, tachycardia, dysphoria, sedation, amnesia, anxiety, and memory suppression. At lower doses, it induces a hypnotic-sedative state akin to ethanol, while higher doses precipitate a state of delirium, albeit milder than that induced by diphenhydramine. Users often describe the experience with doxylamine as soft, cozy, and dreamy compared to the effects of diphenhydramine.

Considerations on Abuse Potential and Safety

Despite its pharmacological properties, the abuse potential of doxylamine remains inadequately studied. However, its inherently dysphoric nature suggests a low likelihood of abuse. The measured LD50 (median lethal dose) of doxylamine in adults is approximately 500mg/kg. Moreover, it has not been implicated as carcinogenic or teratogenic. Prolonged use of doxylamine results in the development of tolerance, necessitating increased dosages to achieve the desired effects over time.

In conclusion, doxylamine stands as a potent deliriant with recognized medicinal applications, albeit with considerations regarding its potential for abuse and long-term use. Understanding its pharmacological profile and subjective effects is crucial for its safe and effective utilization in clinical and OTC settings.

History and Culture

Origins and Medical Use

Doxylamine, initially described in 1948 or 1949 by Nathan Sperber and colleagues, gained early recognition for its medicinal potential. In 1956, it entered the market as a component of Bendectin, a morning sickness formula combining doxylamine, vitamin B6, and dicyclomine. However, concerns arose regarding congenital limb defects, leading to a reformulation in 1976 and subsequent withdrawal from the market in 1983. Despite the absence of conclusive studies linking Bendectin to congenital defects, it wasn't until 2013 that the formula reemerged in the U.S. under the brand name Diclegis for morning sickness treatment.

Incorporation into Cold Formulas

Since 1966, doxylamine succinate has been utilized in Vicks cold formulas as a sedating agent, alongside compounds like dextromethorphan, acetaminophen, and phenylephrine. While the intoxicating effects of consuming NyQuil or Vicks are primarily attributed to dextromethorphan, doxylamine may contribute to the overall experience. However, this form of "tripping" is uncommon due to the toxicity of acetaminophen and the unpalatable taste of the syrup.

Chemistry

Doxylamine, chemically known as N,N-dimethyl-2-(1-phenyl-1-pyridin-2-ylethoxy)ethanamine, belongs to the ethanolamine antihistamine class. Differing from diphenhydramine, it features a pyridine and a phenyl group instead of two phenyls, with an additional methyl group attached to the carbon connecting the aromatic rings. In its freebase form, doxylamine appears as a clear and colorless liquid under standard conditions, while as the succinate salt, it manifests as a white powder.

Pharmacology

Doxylamine primarily acts as an inverse agonist of the H1-histamine receptor, imparting its antihistamine and sedative properties. Additionally, it functions as an antagonist of the muscarinic acetylcholine receptors, contributing to its deliriant effects. Metabolized in the liver by cytochrome P450 enzymes CYP2D6, CYP1A2, and CYP2C9, its primary metabolites include N-desmethyldoxylamine, N,N-didesmethyldoxylamine, and doxylamine N-oxide. Peak blood levels are attained 1.5-2.5 hours post-administration, with a half-life of 10-12 hours.

Other Pharmacological Considerations

Doxylamine may yield false-positives for methadone at sufficiently high doses. Its bioavailability is 24.7% for oral administration and 70.8% for intranasal administration.

Subjective Effects

(Note: The following subjective effects are based on anecdotal user reports and the SEI. They may not occur predictably or reliably and carry risks such as addiction, severe injury, or death. Higher doses are more likely to induce the full spectrum of effects.)

Dosage

Bioavailability

Doxylamine demonstrates a bioavailability of approximately 24.7%.

Dosage Guidelines

• Threshold: The minimum threshold dose for doxylamine is around 10 mg.
• Light: A light dosage typically ranges between 75 and 200 mg.
• Common: Common doses fall within the range of 200 to 350 mg.
• Strong: Strong effects are typically experienced with doses between 350 and 600 mg.
• Heavy: Doses exceeding 600 mg are considered heavy and may lead to intensified effects and potential risks.

Physical Effects

Sedation

Doxylamine induces profound sedation, often resulting in a deeply lethargic state. Even at low doses, it is commonly utilized as a sleep aid. Notably, doxylamine tends to be more sedating than diphenhydramine.

Spontaneous Bodily Sensations

The "body high" experienced with doxylamine is akin to that of diphenhydramine, albeit less uncomfortable and dysphoric. Some users even describe it as mildly euphoric.

Muscle Relaxation and Contractions

At higher doses, doxylamine may lead to muscle contractions. Additionally, users often report a perception of bodily heaviness, making movement challenging.

Restless Leg Syndrome

While less pronounced than with diphenhydramine, some users may experience restless leg syndrome with doxylamine, although others may not experience it at all.

Tactile Sensations and Hallucinations

Users may experience either tactile enhancement or suppression. Tactile hallucinations, commonly manifesting as sensations of insects crawling on the skin, often accompany visual hallucinations.

Nausea and Abnormal Heartbeat

Nausea and abnormal heartbeat can occur due to doxylamine's anticholinergic effects. Dry mouth is a common side effect, as with other antihistamines.

Other Physical Effects

Doxylamine may also induce dizziness, frequent urination coupled with difficulty urinating, gustatory hallucinations, increased heart rate, increased bodily temperature, temperature regulation suppression, increased perspiration, motor control loss, physical fatigue, pupil dilation, skin flushing, temporary erectile dysfunction, and visual disturbances.

Visual Effects

Threshold and Hallucinations

Doxylamine's hallucinatory threshold appears to be higher than that of diphenhydramine, with hallucinations typically occurring at higher dosages.

Visual Distortions

Visual effects may include double vision, pattern recognition suppression, visual acuity suppression, distortions, drifting, brightness alteration, visual haze, and hallucinatory states ranging from external to internal hallucinations.

Cognitive Effects

Anxiety and Paranoia

While anxiety and paranoia are common with doxylamine, they are reportedly less intense than with diphenhydramine.

Sleepiness and Wakefulness

Doxylamine is known for its extreme sedative effects, often inducing sleepiness even at low doses. However, wakefulness is less common compared to diphenhydramine.

Dysphoria and Euphoria

Although typically dysphoric, some users may experience feelings of euphoria at lower doses of doxylamine.

Other Cognitive Effects

Additional cognitive effects may include confusion, cognitive fatigue, creativity suppression, decreased libido or increased libido, delirium, delusion, depression, derealization, disinhibition, dysarthria, emotion suppression, feelings of impending doom, focus suppression, increased music appreciation, language suppression, memory suppression, thought deceleration, thought disorganization, and time distortion.

Auditory Effects

Auditory effects of doxylamine may include hallucinations, enhancements, and suppression.

Medical Uses

Doxylamine is commonly employed as an over-the-counter sleep aid and cough suppressant. It may also be used in combination with pyridoxine to alleviate morning sickness during pregnancy.

Toxicity and Harm Potential

While typically safe for healthy adults, doxylamine can pose risks when combined with other substances, particularly those with anticholinergic effects. High doses may lead to rhabdomyolysis and other serious complications.

Lethal Dosage

The LD50 of doxylamine in mice is approximately 470mg/kg.

Tolerance and Addiction Potential

Chronic use of doxylamine can lead to dependence, although its abuse potential is lower compared to other hallucinogens. Tolerance develops with repeated use, necessitating higher doses to achieve the same effects.

Dangerous Interactions

Combining doxylamine with certain substances, such as stimulants, depressants, benzodiazepines, anticholinergics, and SSRIs, can result in dangerous or life-threatening outcomes.

Legal Status

In the United States, doxylamine is available over the counter as a sleep aid. However, its availability may vary in other countries, with some requiring a prescription for its use.

Frequently Asked Questions (FAQ)

Q: What is the history behind doxylamine?

A: Doxylamine was first described in 1948 or 1949 and gained popularity as a morning sickness remedy in the 1950s. It was later withdrawn from the market due to concerns over birth defects but reappeared in 2013 under the brand name Diclegis.

Q: How does doxylamine affect the body?

A: Doxylamine primarily acts as an inverse agonist of the H1-histamine receptor, resulting in sedation and antihistamine effects. It also antagonizes muscarinic acetylcholine receptors, leading to deliriant effects at higher doses.

Q: What are the common physical effects of doxylamine?

A: Physical effects may include sedation, muscle relaxation, dry mouth, increased heart rate, nausea, and difficulty urinating, among others.

Q: What visual effects can be experienced with doxylamine?

A: Visual effects may include distortions, drifting, brightness alteration, visual haze, and hallucinations, ranging from external to internal.

Q: Is doxylamine safe to use?

A: While generally safe for healthy adults when used as directed, doxylamine can pose risks when combined with other substances, particularly those with anticholinergic effects.

Q: Can doxylamine lead to addiction?

A: Chronic use of doxylamine can lead to dependence and tolerance, although its abuse potential is lower compared to other hallucinogens.

Q: What are some dangerous interactions to be aware of?

A: Combining doxylamine with stimulants, depressants, benzodiazepines, anticholinergics, or SSRIs can result in dangerous or life-threatening outcomes.

Q: What is the legal status of doxylamine?

A: In the United States, doxylamine is available over the counter as a sleep aid. However, its availability may vary in other countries, with some requiring a prescription for its use.