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Specification
Product Name: Dextromethorphan
IUPAC Name: (4bS,8aR,9S)-3-Methoxy-11-methyl-6,7,8,8a,9,10-hexahydro-5H-9,4b-(epiminoethano)phenanthrene
Other Names: DXM, DMO, DM, Dex, Robitussin, Delsym, DexAlone, Duract
Molecular Formula: None
Molar Mass: 237.26 g·mol−1
Effect: stimulant, psychedelic
Purity of the substance: 99.9%
Physical properties: Crystals, Powder
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Table of Contents

  1. Introduction
  2. Dosage
  3. Physical Effects
    • Stimulation & Sedation
    • Perception of Bodily Lightness
    • Bodily Control Enhancement
    • Spontaneous Bodily Sensations
    • Physical Euphoria
    • Appetite Suppression
    • Changes in Felt Bodily Form
    • Motor Control Loss
    • Spatial Disorientation
    • Nausea
    • Temperature Regulation Suppression
    • Increased Bodily Temperature
    • Increased Blood Pressure
    • Increased Heart Rate
    • Increased Perspiration
    • Muscle Spasms
    • Orgasm Suppression
    • Decreased Libido
    • Difficulty Urinating
    • Itchiness
    • Cough Suppression
    • Pain Relief
    • Muscle Relaxation
    • Optical Sliding
    • Dizziness
    • Gustatory Hallucination
    • Physical Autonomy
    • Tactile Suppression
    • Pupil Dilation
    • Gait Alteration
  4. Visual Effects
    • Enhancements
    • Suppression
    • Distortions
    • Geometry
    • Hallucinatory States
  5. Cognitive Effects
  6. Auditory Effects
  7. Disconnective Effects
  8. Multi-sensory Effects
  9. Transpersonal Effects
  10. Afterglow
  11. Plateaus
  12. Toxicity and Harm Potential
  13. Dependence and Abuse Potential
  14. Overdose
  15. Dangerous Interactions
  16. Legal Status

Understanding Dextromethorphan (DXM): A Dissociative Substance

Introduction to DXM

Dextromethorphan (DXM), also known by various street names such as robo, dex, DM, and DXM, belongs to the morphinan class of dissociative substances. This compound serves as the primary active ingredient in numerous over-the-counter (OTC) cold and cough medications. Despite its medicinal purposes, exceeding approved doses of DXM can lead to dissociative effects akin to those induced by ketamine and phencyclidine (PCP). It operates as a noncompetitive NMDA receptor antagonist [1].

Historical Context and Regulation

DXM was initially identified in 1953 and received approval for use as a cough suppressant in the United States in 1958 [2]. Subsequently, it was introduced into the market as an OTC medication under the brand name Romilar. However, by 1975, the widespread abuse of DXM had become apparent, prompting the voluntary removal of Romilar from the OTC market [3]. In response to the abuse, manufacturers began formulating DXM products with additives aimed at deterring misuse, such as incorporating ingredients with unpalatable tastes.

Persistence of Recreational Use

Despite efforts to curb misuse, recreational use of DXM continues to be a concerning trend, particularly among teenagers drawn to its low cost and accessibility [4].

Effects and Variability

DXM induces a range of subjective effects, including dissociation, time distortion, bodily hallucinations, immersion enhancement, loss of motor control, euphoria, and ego dissolution. Users often liken low doses to alcohol intoxication, while higher doses yield experiences reminiscent of ketamine or PCP. Many users also report experiencing significant discomfort, including nausea, attributed to the substance's strong body load.

Individual responses to DXM vary widely, likely influenced by genetic factors underlying metabolism. Consequently, some individuals find DXM experiences unpleasant or neutral, while others describe them as profound and mystical.

Potency Considerations

It's essential to recognize that DXM in freebase form, such as that found in products like Robocough RoboTablets, is approximately 27-37% more potent than its hydrobromide form due to its higher DXM concentration by weight. Users must adjust their dosage calculations accordingly to avoid potential overdose risks.

Safety and Controversy

The toxicity of DXM in recreational doses remains ambiguous and contentious. While some evidence suggests that excessive use of NMDA antagonists like DXM may have neurotoxic effects, definitive conclusions remain elusive. Numerous cases of DXM dependence and abuse have been documented. Therefore, it is strongly advised to practice harm reduction measures when using this substance.

History and Culture of Dextromethorphan (DXM)

Origins and Approval

The racemic parent compound of dextromethorphan, racemethorphan, was initially outlined in Swiss and US patent applications by Hoffmann-La Roche in 1946 and 1947, respectively. The patent for this compound was granted in 1950. The resolution of the two isomers of racemethorphan using tartaric acid was published in 1952. Subsequently, DXM underwent successful testing in 1954 as part of research funded by the US Navy and CIA, aiming to find nonaddictive substitutes for codeine.

DXM received approval from the FDA in 1958 as an over-the-counter antitussive, or cough suppressant. Initially, DXM was seen as a solution to some of the issues associated with the use of codeine phosphate as a cough suppressant, such as sedation and opiate dependence. However, akin to dissociative anesthetics like phencyclidine and ketamine, DXM later became linked with nonmedical use.

Cultural Evolution

During the 1960s and 1970s, dextromethorphan became available in tablet form over the counter under the brand name Romilar. However, due to frequent misuse, Romilar was removed from shelves in 1973 after a surge in sales. It was replaced with cough syrup in an effort to mitigate abuse.

The advent of widespread internet access in the 1990s facilitated rapid dissemination of information about DXM, leading to the formation of online discussion groups focused on its use and acquisition. As early as 1996, DXM HBr powder could be bought in bulk from online retailers, providing users with an alternative to consuming DXM in syrup form. Additionally, as of January 1, 2012, the state of California prohibits the sale of dextromethorphan to minors without a doctor's prescription.

Chemistry and Pharmacology

Chemical Structure

Dextromethorphan belongs to the morphinan class and is a dextrorotatory molecule. It features a phenanthrene core structure with one aromatic ring (benzene) bound to two saturated rings (cyclohexane). Additionally, it contains a saturated piperidine ring attached to specific positions (R9 and R13) of the core structure. DXM is substituted at RN with a methyl group and at R3 with a methoxy group.

Pharmacological Mechanisms

The pharmacology of DXM is not fully elucidated. In vitro studies suggest that its primary mechanism of action is the blockade of N-methyl-D-aspartate (NMDA) receptors, which are glutamate receptors responsible for excitatory signaling in the central nervous system. This action is akin to ketamine and PCP [1].

Rather than directly acting as an NMDA receptor antagonist, dextromethorphan acts as a prodrug of its more potent metabolite, dextrorphan, which mediates its dissociative effects.

Additional pharmacological mechanisms include nonselective serotonin reuptake inhibition, alpha-3 beta-4 nicotinic receptor antagonism, and sigma-1 receptor agonism.

Metabolism

DXM is metabolized into dextrorphan (DXO) and 3-methoxymorphinan (MEM) by specific cytochrome P450 enzymes. Individual variations in metabolism significantly impact the nature of the DXM experience, with poor metabolizers experiencing increased potency and duration due to higher DXM to DXO ratios in the bloodstream.

Psychoactive Metabolites

Dextrorphan, produced by the O-demethylation of dextromethorphan, is a potent NMDA receptor antagonist, contributing to the psychoactive effects of DXM. It also exhibits serotonin reuptake inhibition and nicotinic receptor antagonism.

3-Methoxymorphinan, formed by the N-demethylation of dextromethorphan, has local anesthetic effects.

3-Hydroxymorphinan, derived from the metabolism of dextrorphan and 3-methoxymorphinan, displays neuroprotective and neurotrophic effects.

Subjective Effects

The subjective effects of DXM are often described as hallucinogenic, impairing, disorienting, and less clear-headed compared to substances like MXE and ketamine. These effects vary widely among individuals and doses, with higher doses increasing the likelihood of experiencing the full spectrum of effects. However, it's important to note that adverse effects, including addiction and severe injury, become more likely at higher doses.

Dosage Guidelines for Dextromethorphan (DXM)

Threshold

The threshold dosage for experiencing the effects of dextromethorphan (DXM) is typically around 75 mg.

Light

Light doses of DXM range from 100 to 200 mg. At this dosage range, users may begin to perceive mild effects.

Common

A common dose of DXM falls between 200 to 400 mg. This dosage range is where users typically experience moderate effects.

Strong

Strong doses of DXM range from 400 to 700 mg. At this dosage level, users may encounter intense effects.

Heavy

Doses exceeding 700 mg are considered heavy. At this dosage range, users may experience extremely potent effects.

It's crucial to emphasize that individual responses to DXM can vary significantly, and factors such as tolerance, metabolism, and overall health should be considered when determining dosage. Additionally, higher doses of DXM increase the likelihood of experiencing adverse effects, including addiction, severe injury, or death. Therefore, it's essential to approach DXM use with caution and adhere to harm reduction practices.

Physical Effects of Dextromethorphan (DXM)

Stimulation & Sedation

At lower, recreational doses, DXM tends to be predominantly stimulating. However, it can induce waves of tiredness or a desire to lay down in a sleep-like state. As higher doses are approached, the experience typically becomes very sedating and lethargic, sometimes resulting in immobility.

Perception of Bodily Lightness

DXM can create a sensation of bodily lightness, making the body feel weightless and floating. This effect can be strangely stimulating, encouraging physical activities at low to moderate doses by making movement feel effortless.

Bodily Control Enhancement

Inconsistently present at lower doses, bodily control enhancement can be noticeable. However, at higher plateaus, it can transition into motor control loss, gait alteration, and spatial disorientation.

Spontaneous Bodily Sensations

The DXM "body high" is characterized by a sharp, pleasurable, and warm tingling sensation, often localized to the hands, feet, and head. It ranges from empowering stimulation at lower doses to a heavy body load at higher doses.

Physical Euphoria

DXM can induce feelings of physical euphoria ranging from mild pleasure to powerful, all-encompassing bliss.

Appetite Suppression

DXM typically leads to strong appetite suppression, which may persist into the following day.

Changes in Felt Bodily Form

Prominent at moderate or high doses, changes in felt bodily form can occur.

Motor Control Loss

At higher doses, DXM can lead to a loss of gross and fine motor control, balance, and coordination. It's crucial to sit down before the onset to prevent falling and potential injury.

Spatial Disorientation

A spinning sensation is common, resulting in mild disorientation as if one were falling through a hole.

Nausea

DXM may cause extreme nausea and vomiting, particularly during the come-up phase. This can be more intense and consistent than nausea produced by similar substances like ketamine and MXE.

Temperature Regulation Suppression

DXM can moderately increase body temperature at moderate to high doses.

Increased Blood Pressure and Heart Rate

DXM can lead to an increase in both systolic and diastolic blood pressure along with an elevated heart rate.

Increased Perspiration

Increased bodily temperature combined with temperature regulation suppression can result in increased perspiration.

Muscle Spasms

DXM use may lead to muscle spasms.

Orgasm Suppression and Decreased Libido

DXM can suppress orgasm and decrease libido.

Difficulty Urinating

Difficulty urinating may become more apparent with escalating doses and could lead to a complete inability to urinate at high doses.

Itchiness

Colloquially known as "robo-itch," itchiness can vary among users and is caused by histamine release.

Cough Suppression and Pain Relief

As DXM is commonly used as a cough medicine, it has the same effect in recreational doses. It may also provide pain relief.

Muscle Relaxation and Optical Sliding

Muscle relaxation can be inconsistent and may alternate with bouts of muscle twitching. Optical sliding can occur at higher doses, leading to a sense of visual distortion.

Dizziness and Gustatory Hallucination

DXM can induce dizziness, especially at higher doses, and may lead to incapability to stand up willingly. Gustatory hallucination, altering the perception of taste, can also occur.

Physical Autonomy and Tactile Suppression

At very high doses, users may find themselves awake in strange locations with no recollection of how they got there. Tactile suppression, partially to entirely suppressing the sense of touch, can create feelings of numbness in the extremities.

Pupil Dilation and Gait Alteration

Pupil dilation is noticeable at moderate to high doses, while gait alteration, colloquially known as "robo-walking," is a common effect of DXM.

Visual Effects of Dextromethorphan (DXM)

Enhancements

DXM can enhance colors, magnify visual perceptions, and improve peripheral vision. It may also enhance the frame rate and produce colorful geometric patterns.

Suppression

DXM can suppress visual functions, leading to double vision, pattern recognition suppression, and frame rate suppression. Nystagmus, the involuntary movement of the eyes, may occur at high doses.

Distortions

Visual distortions on DXM can include afterimages, depth perception distortions, drifting visuals, and changes in perspective. Scenery may appear sliced or stretched, and tracers may be present.

Geometry

The visual geometry produced by DXM is described as bright, colorful, and intricate, with psychedelic characteristics. It may involve intricate patterns and may transform into hallucinatory states with closed eyes.

Hallucinatory States

At high doses, DXM can induce a full range of hallucinatory states, including external and internal hallucinations characterized by autonomous entities, landscapes, and scenarios. These states may be less consistent than those induced by other psychedelics.

Toxicity and Harm Potential of Dextromethorphan (DXM)

Lack of Scientific Studies

The toxicity and long-term health effects of recreational DXM use in humans have not been studied scientifically, and the exact toxic dosage remains unknown.

Anecdotal Evidence and Harm Reduction Practices

Anecdotal evidence suggests that trying DXM at low to moderate doses by itself and using it sparingly may not lead to negative health effects. However, many DXM users recommend waiting a week between respective plateaus before using DXM again to potentially prevent or minimize severe damage to organs such as the kidneys, heart, and liver. This waiting period allows the body to filter out toxic chemicals and return to baseline levels. Heavy users report that failure to follow these guidelines could lead to chemical buildup over time, necessitating longer waiting periods between uses.

Neurotoxicity Concerns

While early speculation suggested that DXM might cause neurotoxicity and Olney's lesions, animal studies have not demonstrated this effect. However, chronic users often report significant issues with memory, attention, and mood that persist for months after discontinuing usage. Oral administration of DXM during adolescence has been shown to impair learning in rats during adulthood.

Dependence, Abuse Potential, and Withdrawal

DXM can produce dependence with chronic use and has moderate abuse potential. Withdrawal symptoms may include fatigue, apathy, flashbacks, constipation, insomnia, nightmares, inability to feel pleasure, impaired memory, attention deficit, decreased libido, panic attacks, impaired learning, tremors, yellowing of the skin, hives, muscle pain, toxic psychosis, and other psychological problems.

Tolerance and Cross-Tolerance

Tolerance to DXM develops with prolonged and repeated use, requiring users to administer increasingly large doses to achieve the same effects. DXM also produces cross-tolerance with all dissociatives, reducing the effects of other dissociative substances.

Permanent Tolerance and "50 Trip Limit"

Some users report an irreversible, permanent tolerance to DXM, which may develop over time and correlate with the number of doses ingested throughout a person's lifetime. This phenomenon, known as the "50 trip limit," remains unexplained but is speculated to be indicative of neurotoxicity.

Overdose

Anecdotal evidence suggests that DXM overdose becomes significant at doses ranging from approximately 15mg/kg to 20mg/kg, or roughly 1000mg - 1500mg in a 70kg person. Overdose effects can include delusions, hallucinations, psychosis, confusion, panic attacks, mania, sedation, severe balance issues, increased heart rate, nystagmus, amnesia, anesthesia, respiratory depression, dangerously high fever, seizures, serotonin syndrome, and other life-threatening complications. Death from DXM toxicity is rare but may occur due to complications such as extremely elevated heart rate and blood pressure, urinary retention, rhabdomyolysis, fever, seizures, and brain cell death.

Dangerous Interactions

DXM can interact dangerously with various substances, including benzodiazepines, cannabis, DOx, 25x-NBOMe, 2C-T-x, 5-MeO-xxT, amphetamines, cocaine, ΑMT, PCP, MDMA, alcohol, GHB, opioids, MAOIs, SSRIs, antihistamines, and others. These interactions can lead to unexpected and potentially life-threatening complications.

Legal Status

The legal status of DXM varies by country. In most countries, DXM is available over the counter or by prescription. Some countries impose age restrictions on purchasing DXM-containing products.

FAQ (Frequently Asked Questions)

1. Is DXM safe to use?

The safety of DXM use varies depending on factors such as dosage, frequency of use, and individual health conditions. While low to moderate doses may not lead to immediate negative effects, chronic and high-dose usage can pose significant risks to physical and mental health.

2. How much DXM should I take?

Dosage recommendations for DXM vary depending on desired effects and individual tolerance. It's essential to start with a low dose and gradually increase if necessary, always staying within safe limits. See the Dosage section for more information.

3. Can DXM cause addiction?

Yes, DXM has moderate abuse potential and can lead to dependence with chronic use. Users may experience withdrawal symptoms if they suddenly stop using DXM after developing dependence.

4. What are the signs of DXM overdose?

Signs of DXM overdose can include delusions, hallucinations, psychosis, confusion, panic attacks, sedation, increased heart rate, respiratory depression, seizures, and serotonin syndrome. Seek medical help immediately if you suspect DXM overdose.

5. Are there any dangerous interactions with DXM?

Yes, DXM can interact dangerously with various substances, including benzodiazepines, cannabis, MDMA, alcohol, opioids, and others. These interactions can lead to unexpected and potentially life-threatening complications. Always research potential interactions before combining substances.

6. What is the legal status of DXM?

The legal status of DXM varies by country. In most countries, it is available over the counter or by prescription. Some countries impose age restrictions on purchasing DXM-containing products. Check local regulations before purchasing or using DXM.


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