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Table of Contents

1. Introduction
2. History and Culture
3. Chemistry
4. Pharmacology
5. Dosage
6. Receptor Site Binding Affinity
7. Physical Effects
8. Visual Effects
9. Cognitive Effects
10. Auditory Effects
11. After Effects
12. Forms of Diphenhydramine
13. Understanding Dimenhydrinate
14. Toxicity and Harm Potential
15. Overdose Risks
16. Psychosis
17. Dependence and Abuse Potential
18. Dangerous Interactions
19. Legal Status

Understanding Diphenhydramine: A Closer Look

Introduction to Diphenhydramine

Diphenhydramine, known under various names such as DPH, Dimedrol, and Benadryl, belongs to the ethanolamine class and serves as a first-generation H1 antihistamine. Its primary application lies in the treatment of allergies, available widely over-the-counter. However, when consumed beyond recommended doses, diphenhydramine can induce potent deliriant effects.

Historical Background

Synthesized for the first time in 1943, diphenhydramine earned the distinction of being the inaugural prescription antihistamine sanctioned by the U.S. Food and Drug Administration in 1946. Gradually, by the 1980s, it garnered approval for over-the-counter usage. Presently, it finds application not only in allergy treatment but also addresses conditions like itchiness, insomnia, motion sickness, nausea, and symptoms associated with Parkinson's disease.

Effects and Experiences

Users of diphenhydramine report a spectrum of subjective effects, including sedation, anxiety, tactile hallucinations, memory suppression, thought disorganization, dysphoria, and external hallucinations. At lower doses, individuals typically experience a sedative, body-high sensation, while higher doses plunge them into states of delirium, characterized by vivid and convincing hallucinations. However, doses falling between these extremes often induce discomfort and dysphoria.

Concerns and Risks

Notably, diphenhydramine consumption frequently triggers significant nausea and bodily discomfort, commonly referred to as "body load." Most individuals experimenting with diphenhydramine report negative experiences and express no desire to repeat them. Its abuse potential is generally deemed low due to the unpleasant effects it elicits. Despite this, the toxicity of its recreational use remains inadequately studied. Anecdotal evidence suggests that chronic usage, characterized by high doses and repeated administration, may result in persistent hallucinations and cognitive impairments. Moreover, high doses have been associated with seizures and cardiotoxicity.

Harm Reduction Practices

Given the potential risks associated with diphenhydramine, it is highly recommended to employ harm reduction strategies when using this substance. Such practices may include careful dosage management, avoiding frequent use, and seeking medical guidance if experiencing adverse effects.

Unraveling the History and Cultural Impact

Discovery and Early Approval

Diphenhydramine, the brainchild of George Rieveschl, emerged onto the pharmaceutical scene in 1943, courtesy of Rieveschl's endeavors while at the University of Cincinnati. Just three years later, in 1946, it secured the notable distinction of becoming the inaugural prescription antihistamine sanctioned by the United States Food and Drug Administration (FDA).

Contributions to Pharmacological Research

The 1960s marked a significant milestone in diphenhydramine's journey, as researchers uncovered its ability to inhibit the reuptake of the neurotransmitter serotonin. This revelation triggered a fervent quest for antidepressants with similar structures but fewer side effects, culminating in the groundbreaking invention of fluoxetine (Prozac), a selective serotonin reuptake inhibitor (SSRI).

Delving into the Chemical Composition

Structural Overview

Diphenhydramine, chemically known as 2-(diphenylmethoxy)-N,N-dimethylethanamine, falls under the organic compound category within the ethanolamine class. Its intricate chemical structure comprises an ethylamine chain bearing two methyl groups bonded to the terminal nitrogen group RN. Additionally, this chain features a substitution at R2 with a diphenylmethoxy group, giving rise to an ether formation. The diphenylmethoxy group, in turn, consists of two aromatic phenyl rings attached to a methoxy group CH3O-.

Formation as a Hydrochloride Salt

Diphenhydramine is commonly synthesized as a hydrochloride salt for pharmaceutical applications.

Unveiling Pharmacological Mechanisms

Receptor Activity and Antagonism

Diphenhydramine operates as an inverse agonist at the peripheral histamine H1 receptor and a central histamine H1 receptor. This peripheral inverse agonism underlies its efficacy in alleviating allergic reactions. Additionally, like many first-generation antihistamines, it acts as a competitive antagonist at mACH receptors.

Impact on Neurotransmission

The precise mechanisms underlying diphenhydramine's effects remain elusive. However, it is understood to antagonize acetylcholine receptors, primarily contributing to its observed effects such as delirium, sedation, and vivid hallucinations, alongside uncomfortable physical side effects.

Receptor Affinities and Channel Inhibition

Diphenhydramine exhibits multifaceted pharmacological actions, including the blockade of sodium channels and the inhibition of serotonin reuptake. Moreover, it blocks voltage-gated potassium channels (VGKCs), potentially predisposing individuals to torsades de points, a cardiac condition associated with sudden cardiac death.

The receptor binding affinities for diphenhydramine are documented as follows, contributing to its diverse range of physiological effects.

Navigating Dosage Guidelines

Understanding Bioavailability

Diphenhydramine boasts a bioavailability range of 40-60%, denoting the proportion of the administered dose that enters circulation and produces its intended effects within the body.

Threshold Dosage

To elicit discernible effects, individuals typically require an initial dose of 25 mg, marking the threshold for diphenhydramine's physiological response.

Exploring Dosage Ranges

Light Dosage Range

Entry into the realm of perceptible effects often occurs within the light dosage range of 100 to 200 mg, where users may begin to experience subtle alterations in sensory perception.

Common Dosage Range

For those seeking a more pronounced impact, the common dosage range spans from 200 to 400 mg. Within this bracket, users can anticipate a moderate to significant shift in their mental and physical state.

Strong Dosage Range

Venturing into the strong dosage range, encompassing 400 to 700 mg, individuals are likely to encounter intensified effects, potentially leading to profound alterations in consciousness and perception.

Heavy Dosage Range

The heavy dosage range, surpassing 700 mg and beyond, represents territory fraught with heightened risk and potential for severe adverse reactions. Individuals venturing into this domain should exercise extreme caution, as the likelihood of experiencing overwhelming effects increases significantly.

Unveiling Receptor Binding Affinities

Histamine Receptors

• H1 Receptor: Diphenhydramine exhibits a binding affinity ranging from 9.6 to 16 nM, indicating a moderate to strong affinity for this receptor subtype.

• H2 Receptor: Data regarding binding affinity for the H2 receptor is currently unavailable, necessitating further investigation to elucidate diphenhydramine's interaction with this subtype.

• H3 Receptor: Diphenhydramine displays minimal binding affinity for the H3 receptor, with values surpassing 10,000 nM, indicating negligible interaction with this receptor subtype.

• H4 Receptor: Similarly, diphenhydramine exhibits negligible binding affinity for the H4 receptor, with values exceeding 10,000 nM, suggesting minimal involvement with this receptor subtype.

Muscarinic Acetylcholine Receptors (mAChRs)

• M1 Receptor: Diphenhydramine demonstrates a binding affinity ranging from 80 to 100 nM for the M1 receptor, indicating a moderate affinity for this subtype.

• M2 Receptor: Binding affinity for the M2 receptor spans from 120 to 490 nM, reflecting a variable affinity level for this subtype.

• M3 Receptor: Diphenhydramine showcases a binding affinity ranging from 84 to 299 nM for the M3 receptor, suggesting a moderate affinity for this subtype.

• M4 Receptor: With a binding affinity ranging from 53 to 112 nM, diphenhydramine displays a moderate affinity for the M4 receptor subtype.

• M5 Receptor: Diphenhydramine exhibits a binding affinity ranging from 30 to 260 nM for the M5 receptor, indicating a variable affinity level for this subtype.

Serotonin Transporter (SERT)

• SERT: Diphenhydramine's interaction with the serotonin transporter (SERT) yields binding affinities equal to or greater than 3,800 nM, indicating a lower affinity for this target compared to other receptors.

Unveiling Physical Effects

Sedation

Diphenhydramine induces significant sedation, often utilized in low doses as a sleep aid. However, this sedative effect is accompanied by a profound body load, leading to discomfort. Paradoxically, higher doses may exhibit stimulating qualities, hindering actual rest.

Spontaneous Bodily Sensations

Users frequently report sharp and painful jolts of electricity coursing through their bodies uncontrollably, akin to hiccups in rhythm.

Perception of Bodily Heaviness

One of the most prominent effects of diphenhydramine is the sensation of immense bodily weight, making movement exceedingly challenging and uncomfortable.

Restless Leg Syndrome

Restless legs emerge as a prominent and distressing side effect of diphenhydramine, with potential to persist for days post-consumption, particularly with chronic abuse.

Tactile Enhancement and Suppression

At peak effects, users may experience heightened tactile sensations including touch, pain, warmth, and orgasms. Conversely, diphenhydramine can also induce feelings of numbness throughout the body.

Nausea

Depending on dosage, diphenhydramine can either suppress or induce nausea. Low doses are effective in nausea suppression, while higher doses may exacerbate it significantly.

Abnormal Heartbeat

Diphenhydramine's ability to prolong the QT interval can lead to torsades de pointes, an abnormal heart rhythm potentially resulting in sudden cardiac death.

Other Physical Effects

Additional physical effects include cough suppression, dehydration, dizziness, frequent or difficult urination, gustatory hallucinations, increased blood pressure, increased heart rate, increased bodily temperature, temperature regulation suppression, increased perspiration, loss of motor control, muscle cramps and spasms, olfactory hallucinations, physical fatigue, pupil constriction or dilation, rapid breathing, skin flushing, temporary erectile dysfunction, and itchiness.

Delving into Visual Effects

Visual Hallucinations

While diphenhydramine induces visual hallucinations, it does not enhance visual stimuli like psychedelics. Instead, it tends to degrade visual acuity, leading to increased hallucinations and diminished vision, particularly in darker environments.

Other Visual Effects

Additional visual effects include double vision, pattern recognition suppression, visual acuity suppression, distortions, drifting, object alteration, brightness alteration, visual haze, floats, hallucinatory states, external and internal hallucinations, peripheral information misinterpretation, shadow people, transformations, and unspeakable horrors.

Cognitive Effects Explored

Analysis Suppression

At higher doses, diphenhydramine can halt external information processing, rendering individuals incapable of performing simple tasks or making decisions.

Anxiety & Paranoia

Diphenhydramine is commonly associated with extreme anxiety and paranoia, though these effects may diminish at threshold doses.

Other Cognitive Effects

Additional cognitive effects include sleepiness, wakefulness, dysphoria, cognitive fatigue, confusion, creativity suppression, decreased libido, delirium, delusion, depression, derealization, disinhibition, dream potentiation, dysarthria, emotion suppression, feelings of impending doom, focus suppression, increased music appreciation, language suppression, memory suppression and amnesia, motivation suppression, psychosis, thought deceleration, thought disorganization, and time distortion.

Auditory Effects Discussed

Auditory Hallucinations

Voices and screams are commonly reported auditory hallucinations induced by diphenhydramine.

Other Auditory Effects

Other auditory effects include auditory suppression and enhancement.

After Effects Considered

After Effects

After consuming diphenhydramine, individuals may experience a range of aftereffects including anxiety, brightness alteration, cognitive fatigue, dehydration, depression, gustatory hallucinations, irritability, motivation suppression, physical fatigue, sleepiness, thought deceleration, and visual acuity suppression.

Exploring Forms of Diphenhydramine

Pills

Diphenhydramine is available in pill form, commonly found over the counter and online. Well-known brands include Benadryl, Benylin, Dramamine, Nytol, Sominex, and ZzzQuil. These products may occasionally contain other medications such as dextromethorphan, guaifenesin, or acetaminophen, necessitating caution to prevent overdosing on other substances.

Liquid

Liquid diphenhydramine is also available over the counter and online, offering an alternative administration method. Popular brands include Benadryl and ZzzQuil. Similar to pill forms, liquid formulations may occasionally contain additional medications, requiring vigilance to avoid unintentional overdose.

Powder

Diphenhydramine in powdered form is accessible online, suitable for oral ingestion or injection. However, alternative routes of administration are strongly discouraged due to the substance's propensity to cause severe burns and tissue dehydration.

Understanding Dimenhydrinate

Dimenhydrinate, a combination drug of Diphenhydramine and 8-Chlorotheophylline, is marketed under various names including Draminate, Dramamine, and Gravol. Primarily used to treat nausea, dimenhydrinate is available in tablet, liquid, and suppository forms. It is approximately half as potent as pure diphenhydramine by weight. The inclusion of 8-Chlorotheophylline, a caffeine-like stimulant, may exacerbate diphenhydramine's cardiovascular effects and contribute to increased restlessness during the experience.

Assessing Toxicity and Harm Potential

The toxicity and long-term health effects of recreational diphenhydramine use remain inadequately studied. Diphenhydramine's unpredictable nature and propensity to induce hallucinations pose risks of serious injury, hospitalization, or fatality. Users may exhibit bizarre and nonsensical behavior, endangering themselves and others. Anecdotal reports suggest potential renal and bladder issues with chronic use, akin to ketamine cystitis. Cumulative use has tentatively been associated with an elevated risk of developing dementia.

Exploring Overdose Risks

The overdose threshold for diphenhydramine is commonly cited around 1000 milligrams; however, individuals may overdose with lower doses, particularly when concurrently consuming other substances. Overdose symptoms mirror heavy dosage effects, including delirium, psychosis, anxiety, confusion, increased heart rate, elevated blood pressure, dryness, urinary retention, dizziness, and dilated pupils. Severe cases may entail seizures, dangerous arrhythmias, and cardiovascular complications, necessitating immediate medical attention.

Considering Psychosis

User reports indicate that diphenhydramine significantly elevates the risk of psychosis and delirium compared to other hallucinogens. Numerous online accounts describe episodes of psychotic delirium, amnesia, and severe consequences, often leading to hospitalization or fatality. Recreational use is strongly discouraged, with emphasis on employing extreme caution and harm reduction practices, including trip sitting by a sober individual.

Examining Dependence and Abuse Potential

Chronic diphenhydramine use may lead to dependence, although its abuse potential appears lower compared to other hallucinogens. Tolerance to its effects develops with repeated use, necessitating escalating doses to achieve desired effects. Cross-tolerance with other deliriants further complicates dosage management and risk assessment.

Identifying Dangerous Interactions

Combining diphenhydramine with certain substances can result in dangerous interactions, including serotonin syndrome when co-administered with selective serotonin reuptake inhibitors (SSRIs), abnormal cardiac rhythm when combined with stimulants, and respiratory depression when used alongside benzodiazepines. Caution and thorough research are essential to mitigate risks associated with polydrug use.

Legal Status

Diphenhydramine's legal status varies among countries. In the United States, it is widely available over the counter without a prescription. However, some countries impose age restrictions on its purchase. For instance, in Zambia, possession and sale of diphenhydramine are illegal, with reported cases of foreign nationals detained for possession. In Poland, diphenhydramine is not classified as a controlled substance but is available over the counter only in combination medications containing paracetamol.

Frequently Asked Questions (FAQ)

1. What is diphenhydramine?

• Diphenhydramine, also known as DPH, Dimedrol, or Benadryl, is a first-generation H1 antihistamine commonly used to treat allergies, insomnia, motion sickness, and other conditions.

2. How does diphenhydramine work?

• Diphenhydramine works by blocking the action of histamine at H1 receptors, resulting in its antihistaminic effects. It also has anticholinergic properties, contributing to its sedative and hallucinogenic effects.

3. What are the different forms of diphenhydramine available?

• Diphenhydramine is available in pill, liquid, and powdered forms. It is commonly found in products such as Benadryl, ZzzQuil, Dramamine, and others.

4. Is diphenhydramine safe to use?

• While diphenhydramine is generally safe when used as directed, recreational use can pose risks of toxicity, overdose, and adverse effects. It is important to use caution and adhere to recommended dosages.

5. What are the potential side effects of diphenhydramine?

• Diphenhydramine can cause a range of side effects including sedation, hallucinations, nausea, abnormal heartbeat, dry mouth, dizziness, and cognitive impairment, among others.

6. Can diphenhydramine lead to dependence or addiction?

• Chronic use of diphenhydramine may lead to dependence, but its abuse potential is considered lower compared to other hallucinogens. Tolerance can develop with repeated use, requiring higher doses to achieve desired effects.

7. Are there any dangerous interactions with diphenhydramine?

• Yes, diphenhydramine can interact dangerously with certain substances, including SSRIs, stimulants, benzodiazepines, and other anticholinergic medications. It is important to research potential interactions and use caution when combining substances.

8. What is the legal status of diphenhydramine?

• The legal status of diphenhydramine varies by country. In the United States, it is available over the counter without a prescription. However, some countries may impose age restrictions or require a prescription for purchase.