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Table of Contents
- Dosage
- Cognitive Effects
- Plateaus
- Toxicity and Harm Potential
- Dependence and Abuse Potential
- Overdose
- Dangerous Interactions
- Legal Status and Availability
Exploring Dextromethorphan: A Dissociative Substance
Understanding DXM
Dextromethorphan (DXM), known by various street names such as robo, dex, DM, and DXM, belongs to the morphinan class of dissociative substances. It serves as the primary active component in numerous over-the-counter (OTC) cold and cough medications. Exceeding approved doses of DXM can induce dissociative effects akin to ketamine and phencyclidine (PCP). Its mechanism of action involves acting as a noncompetitive NMDA receptor antagonist.
Historical Context and Regulation
First reported in 1953, DXM gained approval for cough suppression in the United States in 1958. Following its approval, it entered the market as an OTC medication under the name Romilar. By 1975, the widespread abuse of DXM led to its voluntary removal from the OTC market. Subsequently, efforts were made to deter abuse by introducing refined DXM products containing unpalatable additives.
Rise in Recreational Use
Despite regulatory measures, recreational consumption of DXM persists and is increasingly prevalent, particularly among teenagers drawn to its low cost and accessibility.
Effects and Variability
DXM consumption elicits 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 an alcohol-like intoxication, while higher doses induce experiences reminiscent of ketamine or PCP. Many report significant discomfort, including nausea and a heavy body load.
Interindividual Variability
The effects and tolerability of DXM vary significantly among users, possibly due to genetic differences affecting metabolism. Consequently, experiences with DXM can range from unpleasant or neutral to profound psychedelic encounters.
Considerations for Dosage
It's important to note that DXM in freebase form, such as that found in Robocough RoboTablets, is approximately 27-37% more potent than its hydrobromide form due to higher DXM concentration by weight. Accurate dosage calculations are crucial to avoid potential overdose incidents.
Controversy Surrounding Toxicity
The toxicity of DXM in recreational doses remains uncertain and has sparked controversy. Some evidence suggests that excessive use of NMDA antagonists like DXM may have neurotoxic effects. Numerous documented cases of DXM dependence and abuse underscore the importance of harm reduction practices when using this substance.
Unveiling the History and Cultural Impact of Dextromethorphan (DXM)
The Early Origins
The precursor to dextromethorphan (DXM), racemethorphan, was initially documented in Swiss and US patent applications by Hoffmann-La Roche in 1946 and 1947, respectively. This led to the granting of a patent in 1950. In 1952, a breakthrough occurred with the resolution of racemethorphan isomers using tartaric acid. Subsequent testing in 1954, funded by the US Navy and CIA, explored DXM as a potential nonaddictive substitute for codeine.
FDA Approval and OTC Status
In 1958, the Food and Drug Administration (FDA) granted approval for DXM as an over-the-counter (OTC) antitussive, or cough suppressant. Initially hailed as a solution to issues associated with codeine phosphate, such as sedation and opiate dependence, DXM later encountered challenges akin to dissociative anesthetics like phencyclidine and ketamine.
The Romilar Era
Throughout the 1960s and 1970s, dextromethorphan became readily available in tablet form under the brand name Romilar. However, due to rampant misuse, Romilar tablets were withdrawn from circulation in 1973 after a surge in sales. They were subsequently replaced by cough syrup formulations in an effort to curtail abuse.
Internet Era and Accessibility
The proliferation of internet access in the 1990s facilitated the rapid dissemination of information regarding DXM. Online discussion groups emerged, focusing on the use and procurement of the substance. By 1996, DXM HBr powder could be obtained in bulk from online retailers, offering users an alternative to consuming DXM in syrup preparations.
Legal Restrictions and Regulations
The evolving landscape of DXM regulation saw significant changes, particularly in California. As of January 1, 2012, the sale of dextromethorphan to minors in the state became prohibited except with a doctor's prescription, reflecting growing concerns surrounding its recreational use and abuse.
Unraveling the Chemistry of Dextromethorphan (DXM)
Molecular Structure
Dextromethorphan belongs to the morphinan class, characterized by its dextrorotatory nature. Its molecular structure features a phenanthrene core with an aromatic ring (benzene) linked to two saturated rings (cyclohexane). Additionally, it incorporates a saturated piperidine ring attached to R9 and R13 of the core structure. DXM is methylated at RN and methoxylated at R3, respectively.
Pharmacological Mechanisms
Mechanism of Action
The precise pharmacological workings of DXM are not fully elucidated. However, in vitro studies suggest its primary mechanism involves the blockade of N-methyl-D-aspartate (NMDA) receptors, which are glutamate receptors responsible for excitatory signaling in the central nervous system. This mechanism is akin to ketamine and PCP.
Metabolism and Effects
DXM acts as a prodrug, metabolizing into its more potent form, dextrorphan, which mediates its dissociative effects. Additionally, DXM exhibits other pharmacological actions, including nonselective serotonin reuptake inhibition, alpha-3 beta-4 nicotinic receptor antagonism, and sigma-1 receptor agonism.
Metabolism and Variability
Metabolic Pathways
DXM undergoes O-demethylation into dextrorphan by the CYP2D6 enzyme and N-demethylation into 3-methoxymorphinan by CYP3A4 enzyme, with lesser involvement of CYP3A5. Dextrorphan and 3-methoxymorphinan further metabolize into 3-hydroxymorphinan through various pathways.
Individual Variations
Metabolic variations among individuals significantly impact the DXM experience. Poor metabolizers exhibit higher DXM to dextrorphan ratios, leading to increased potency and duration of effects. Inhibitors of CYP2D6 and CYP3A4 can similarly alter DXM metabolism.
Dextrorphan: The Active Metabolite
Pharmacological Profile
Dextrorphan, generated via O-demethylation of DXM, contributes to its psychoactive effects. It serves as a potent NMDA receptor antagonist and exhibits lesser activity as a selective serotonin reuptake inhibitor.
Binding Affinities
Dextrorphan displays varied binding affinities across different receptor sites, including NMDA, sigma-1, and serotonin transporters, among others.
3-Methoxymorphinan and 3-Hydroxymorphinan
Metabolites and Actions
3-Methoxymorphinan (3MM) arises from the N-demethylation of DXM and possesses local anesthetic effects. 3-Hydroxymorphinan (3HM), generated through multiple pathways, exhibits neuroprotective and neurotrophic properties.
Subjective Effects
Physical and Visual Effects
DXM induces a range of physical sensations including stimulation, sedation, bodily lightness, enhanced bodily control, and euphoria. Visual effects encompass enhancements, distortions, and hallucinatory states.
Hallucinatory States
At high doses, DXM can provoke hallucinatory states involving external and internal hallucinations, though less reliably than other psychedelics.
Deciphering Dosage Guidelines for Dextromethorphan (DXM)
Understanding Threshold Levels
Threshold: 75 mg
At this dosage, users may begin to perceive subtle effects of DXM, marking the threshold of its psychoactive properties. However, the experience remains mild and may not encompass the full spectrum of DXM effects.
Exploring Common Dosages
Light: 100 - 200 mg
Light doses of DXM typically range between 100 to 200 mg. At this level, users may experience mild euphoria and subtle alterations in perception, often described as similar to an alcohol-like intoxication.
Assessing Strong Effects
Common: 200 - 400 mg
Doses falling within the 200 to 400 mg range are considered common and can elicit more pronounced effects of DXM. Users may experience significant dissociation, time distortion, and bodily hallucinations, resembling effects akin to ketamine or PCP.
Heavy Dosages and Beyond
Strong: 400 - 700 mg
Heavy: 700 mg +
Strong doses of DXM, ranging from 400 to 700 mg, can induce intense dissociative experiences characterized by profound alterations in perception, loss of motor control, and ego dissolution. At doses exceeding 700 mg, the effects become heavy, potentially leading to overwhelming experiences and increased risk of adverse effects.
It's crucial for users to carefully consider their dosage based on their tolerance, sensitivity, and desired effects to mitigate potential risks associated with DXM consumption.
Navigating the Cognitive Effects of Dextromethorphan (DXM)
Analyzing Cognitive Responses
- Analysis suppression
- Anxiety suppression or Anxiety: While DXM typically suppresses anxiety, panic attacks can occur at heavy dosages.
- Conceptual thinking
- Confusion
- Cognitive euphoria: Though commonly reported, this effect can unpredictably manifest as cognitive dysphoria, particularly at higher doses.
- Cognitive fatigue
- Creativity enhancement
- Decreased libido
- Déjà vu
- Delusion: More likely at higher doses.
- Depersonalization
- Derealization
- Disinhibition: Significant even at moderate dosages.
- Ego inflation
- Dream potentiation
- Emotion enhancement: More prominent than with most dissociatives.
- Empathy, affection, and sociability enhancement: Similar to but less pronounced than with MDMA or MDA.
- Immersion enhancement
- Increased sense of humor: Mostly present below the upper plateaus.
- Increased libido: Exclusively felt in low doses.
- Increased music appreciation: Intense, especially at lower plateaus.
- Memory suppression
- Ego death
- Amnesia: Usually only present with higher dosages, contributing to partial to complete memory loss of the experience.
- Focus suppression
- Motivation suppression
- Novelty enhancement
- Personal bias suppression
- Personal meaning enhancement: Typically only present on the lower plateaus.
- Thought deceleration
- Time distortion: Often feels stretched out.
- Sleepiness
Auditory Effects
- Auditory enhancement
- Auditory suppression
- Auditory distortion
- Auditory hallucination
Disconnective Effects
- Cognitive disconnection
- Physical disconnection
- Visual disconnection
Multi-sensory Effects
- Synaesthesia: Rare and non-reproducible, more likely at higher doses.
Transpersonal Effects
- Spirituality enhancement
- Existential self-realization
- Unity and interconnectedness
Afterglow
The afterglow is characterized by feelings of euphoria, rejuvenation, relaxation, and a light bounciness. Cognitive manifestations include a loss of anxiety, contentment, increased music appreciation, and mild derealization or depersonalization.
Deciphering the DXM Plateaus
Understanding the Gradations of Experience
The DXM community categorizes the effects of oral DXM use into five distinct "plateaus," each characterized by qualitatively different experiences.
First Plateau (1.5 - 2.5 mg/kg)
- Effects: The first plateau typically entails mild experiences, often described as akin to feeling "drunk."
- Common Effects: Cognitive euphoria, increased music appreciation, time distortion, pupil dilation, and stimulation.
Second Plateau (2.5 - 7.5 mg/kg)
- Considered the most recreational plateau.
- Effects: More sedating than stimulating, with intensified euphoria and visual disconnection.
- Additional Effects: Wakefulness, physical euphoria, spatial disorientation, perception of bodily lightness, frame rate suppression, and amplified music appreciation.
Third Plateau (7.5 - 15 mg/kg)
- Intensity surpasses the second plateau.
- Effects: Pronounced dissociation, sedation, nausea (during comeup), memory suppression, auditory and internal hallucinations, cognitive dysphoria, and euphoria.
- Notable Experiences: Omnipotent feelings, closed eye visuals (CEVs), introspection, and mood enhancement in the afterglow.
Fourth Plateau (15 - 20 mg/kg)
- Highly intense with heightened effects.
- Effects: External hallucinations, complete dissociation, and intensified experiences from the third plateau.
- Caution: High risk of injury and overdose, advised against due to danger.
Fifth Plateau (Plateau Sigma)
- Achieved through specific dosing methods or unintentional redosing.
- Effects: Unpleasant and unpredictable experience, often involving delirious hallucinations, dysphoria, delirium, psychosis, and anxiety.
- Risks: Potential for serotonin syndrome and neurotoxicity, strongly advised against due to severe consequences.
Unveiling the Risks: DXM Toxicity and Harm Potential
Incomplete Knowledge and Anecdotal Insights
The toxicity and long-term health effects of recreational DXM (Dextromethorphan) use remain largely unstudied in scientific contexts, leaving the exact toxic dosage uncertain. Anecdotal evidence suggests that low to moderate doses of DXM alone do not typically lead to negative health effects, but caution is advised.
Mitigating Risks through Interval Usage
- DXM users often advocate for waiting periods between doses to prevent potential organ damage.
- Guidelines suggest waiting one week after the first plateau, two weeks after the second, and so forth, allowing the body time to metabolize chemicals and return to baseline levels.
Neurotoxicity Speculations and Memory Issues
- Early concerns regarding DXM-induced neurotoxicity and lesions have not been supported by animal studies.
- Chronic users frequently report lingering memory, attention, and mood problems even after ceasing usage.
- Studies on rats suggest that adolescent DXM use may impair learning into adulthood.
Encountering Dependence and Abuse Potential
- Chronic DXM use can lead to dependence and moderate abuse potential.
- Withdrawal symptoms upon cessation may include fatigue, apathy, flashbacks, and constipation, among others.
- Long-term and high-dose usage can result in toxic psychosis and permanent psychological issues.
Tolerance Development and Cross-Tolerance
- Prolonged DXM use leads to tolerance, requiring larger doses for desired effects.
- DXM use also induces cross-tolerance with other dissociatives, reducing their effects.
Speculation on Irreversible Tolerance
- Some users report an irreversible tolerance to DXM, suggesting a "50 trip limit" after which unique effects diminish permanently.
- The cause of this phenomenon remains unknown but may indicate neurotoxicity.
Navigating Overdose Risks
- DXM overdose risks become significant at roughly 15mg/kg to 20mg/kg.
- Overdose symptoms vary widely, including hallucinations, psychosis, confusion, increased heart rate, and severe balance issues.
- Serious effects such as respiratory depression, dangerously high fever, seizures, and serotonin syndrome are possible.
Handling DXM Overdose
- Interruption of a DXM overdose experience may provoke violent responses due to delusions.
- Medical attention or supervision is crucial to prevent severe complications like respiratory depression, choking, or organ damage.
- Death from DXM toxicity is rare but can result from complications like elevated heart rate and rhabdomyolysis.
Recognizing Dangerous Interactions
- Combining DXM with other substances can lead to unpredictable and potentially life-threatening interactions.
- Notable interactions include benzodiazepines, cannabis, amphetamines, and opioids, among others.
- Independent research is essential to ensure the safety of substance combinations.
Legal Status and Availability
DXM's legal status varies by country, with some permitting over-the-counter sales and others requiring prescriptions or restricting sales to pharmacies.
Frequently Asked Questions (FAQ)
Q1: What is DXM and how is it used?
DXM, or Dextromethorphan, is a dissociative substance commonly found in cough medicines and cold remedies. It is often used recreationally for its psychoactive effects.
Q2: What are the different dosage levels of DXM?
DXM dosage is categorized into thresholds and plateaus, with threshold doses starting at around 75 mg and heavy doses exceeding 700 mg.
Q3: What cognitive effects can DXM produce?
DXM can induce a wide range of cognitive effects, including analysis suppression, anxiety suppression or induction, confusion, creativity enhancement, and memory suppression, among others.
Q4: What are the plateaus associated with DXM use?
The plateaus of DXM use describe qualitatively distinct levels of intoxication, ranging from the first plateau with mild effects to the fifth plateau, also known as Plateau Sigma, which can result in delirious hallucinations and psychosis.
Q5: What are the potential risks and toxicity of DXM use?
DXM use can pose risks of dependence, abuse, and overdose. Chronic usage may lead to memory, attention, and mood issues. Overdose symptoms can range from hallucinations to respiratory depression and even serotonin syndrome.
Q6: Are there any dangerous interactions associated with DXM use?
Combining DXM with certain substances, such as benzodiazepines, cannabis, or opioids, can result in unpredictable and potentially life-threatening interactions. Independent research is essential before combining substances.
Q7: What is the legal status of DXM?
The legal status of DXM varies by country, with some permitting over-the-counter sales and others requiring prescriptions or restricting sales to pharmacies.
Q8: How can I reduce the risks associated with DXM use?
Practicing harm reduction strategies, such as using DXM sparingly, following dosage guidelines, and avoiding risky substance combinations, can help reduce the potential risks associated with DXM use.
To prepare the content, the following materials were used:
- FDA Substance Registration System
- Hazardous Substances Data Bank. National Library of Medicine. 28 August 2008. Retrieved 22 August 2014. 3,4-Methylenedioxymethamphetamine
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