DXM
Dextromethorphan (also known as DXM and Dex) is a dissociative substance of the morphinan class that produces long-lived dissociative and antitussive (cough suppressant) effects when administered.
DXM is the primary active ingredients in many common over-the-counter (OTC) cold and cough medicines, including generic drug labels and store brands. It is also used in other areas of medicine, ranging from pain relief to psychological applications. In its pure form, DXM occurs as a white powder, although it is most commonly consumed in tablet, capsule, or syrup forms.
In the United States and elsewhere, DXM has been noted for having a culture of recreational consumption as a legal, commonly-available, "OTC high." When exceeding label-specified maximum dosages, it acts as a serotonergic dissociative that produces potent and long-lived hallucinogenic effects with a strong "body load" that can range from pleasant to intolerable. In high doses, this produces effects similar to, yet distinct from, the dissociative states produced by other common dissociatives such as ketamine and phencyclidine (PCP).
DXM is the primary active ingredients in many common over-the-counter (OTC) cold and cough medicines, including generic drug labels and store brands. It is also used in other areas of medicine, ranging from pain relief to psychological applications. In its pure form, DXM occurs as a white powder, although it is most commonly consumed in tablet, capsule, or syrup forms.
In the United States and elsewhere, DXM has been noted for having a culture of recreational consumption as a legal, commonly-available, "OTC high." When exceeding label-specified maximum dosages, it acts as a serotonergic dissociative that produces potent and long-lived hallucinogenic effects with a strong "body load" that can range from pleasant to intolerable. In high doses, this produces effects similar to, yet distinct from, the dissociative states produced by other common dissociatives such as ketamine and phencyclidine (PCP).
DXM was first discovered in 1954 as part of US Navy and CIA-funded research on possible substitutes for codeine and dihydrocodeine. The purpose was to find a less sedating antitussive (cough suppressant) agent with a lower potential for dependence. Shortly after its approval by the FDA in 1958 as an over-the-counter antitussive, anecdotal reports of recreational use began to spread.
During the 1960s and 1970s, a tablet form preparation named "Romilar" was sold over-the-counter as a DXM-containing antitussive. DXM was excluded from the Controlled Substances Act of 1970 which allowed its sale to continue.
Romilar was taken off the OTC-market in 1975, as its rising popularity as a legal dissociative drug was recognized. After its removal many companies began to sell DXM preparations in syrup form, which created an unpleasant taste if consumed in large quantities, so as to make them unappealing for recreational use.
Dextromorphan is a dextrorotatory molecule of the morphinan class. It contains a phenanthrene core structure with one aromatic ring (benzene) bound to two saturated rings (cyclohexane). Additionally, it contains a saturated piperidine ring attached to R9 and R13 of the core structure. DXM is substituted at RN with a methyl group and at R3 with a methoxy group.
DXM acts as an NMDA receptor antagonist. NMDA receptors allow for electrical signals to pass between neurons in the brain and spinal column; for the signals to pass, the receptor must be open. Dissociatives close the NMDA receptors by blocking them. This disconnection of neurons leads to loss of feeling, difficulty moving, and eventually what is known as the “hole”.
The mechanism of action behind DXM is via multiple effects, including actions as a nonselective serotonin reuptake inhibitor, alpha-3 beta-4 nicotinic receptor antagonist and a sigma-1 receptor agonist.
At high doses, DXM can cause an increase in systolic and diastolic blood pressure along with an increase in heart rate. DXM also increases blood plasma levels of adrenocorticotropic hormone (ACTH) and corticosterone.
During the 1960s and 1970s, a tablet form preparation named "Romilar" was sold over-the-counter as a DXM-containing antitussive. DXM was excluded from the Controlled Substances Act of 1970 which allowed its sale to continue.
Romilar was taken off the OTC-market in 1975, as its rising popularity as a legal dissociative drug was recognized. After its removal many companies began to sell DXM preparations in syrup form, which created an unpleasant taste if consumed in large quantities, so as to make them unappealing for recreational use.
Dextromorphan is a dextrorotatory molecule of the morphinan class. It contains a phenanthrene core structure with one aromatic ring (benzene) bound to two saturated rings (cyclohexane). Additionally, it contains a saturated piperidine ring attached to R9 and R13 of the core structure. DXM is substituted at RN with a methyl group and at R3 with a methoxy group.
DXM acts as an NMDA receptor antagonist. NMDA receptors allow for electrical signals to pass between neurons in the brain and spinal column; for the signals to pass, the receptor must be open. Dissociatives close the NMDA receptors by blocking them. This disconnection of neurons leads to loss of feeling, difficulty moving, and eventually what is known as the “hole”.
The mechanism of action behind DXM is via multiple effects, including actions as a nonselective serotonin reuptake inhibitor, alpha-3 beta-4 nicotinic receptor antagonist and a sigma-1 receptor agonist.
At high doses, DXM can cause an increase in systolic and diastolic blood pressure along with an increase in heart rate. DXM also increases blood plasma levels of adrenocorticotropic hormone (ACTH) and corticosterone.
DXM is O-demethylated into Dextrorphan (DXO / D-3-hydroxy-N-methylmorphinan) by the CYP2D6 enzyme. DXM is also N-demethylated into 3-methoxymorphinan (MEM / Morphinan) by the CYP3A4 enzyme and to a lesser extent CYP3A5.
Dextrorphan and 3-methoxymorphinan are both metabolized into 3-hydroxymorphinan. Dextrorphan is N-demethylated by CYP3A4 and 3-Methoxymorphinan is O-demethylated by CYP2D6. CYP2D6 O-demethylation is more effective than CYP3A4 N-demethylation.
Dextrorphan is produced by O-demethylation of dextromethorphan through the CYP2D6 enzyme and contributes to the psychoactive effects of dextromethorphan. It is pharmacologically similar to that of dextromethorphan (DXM). However, dextrorphan is much more potent as an NMDA receptor antagonist as well as much less active as a selective serotonin reuptake inhibitor. It is also about 3-fold less potent of a α3β4 nicotinic receptor antagonist than DXM and has a lower affinity for sigma-1 receptors.
3-Methoxymorphinan (also known as 3MM) is produced by the N-demethylation of dextromethorphan by the CYP3A4 enzyme and inhibits the CYP2D6 enzyme.[18] It has local anaesthetic effects.
3-Hydroxymorphinan (also known as 3HM) is produced by O-demethylation of 3-methoxymorphinan by CYP2D6 and metabolization of dextrorphan by CYP3A4 and CYP3A5. 3-Hydroxymorphinan exhibits neuroprotective and neurotrophic effects.
Dextrorphan and 3-methoxymorphinan are both metabolized into 3-hydroxymorphinan. Dextrorphan is N-demethylated by CYP3A4 and 3-Methoxymorphinan is O-demethylated by CYP2D6. CYP2D6 O-demethylation is more effective than CYP3A4 N-demethylation.
Dextrorphan is produced by O-demethylation of dextromethorphan through the CYP2D6 enzyme and contributes to the psychoactive effects of dextromethorphan. It is pharmacologically similar to that of dextromethorphan (DXM). However, dextrorphan is much more potent as an NMDA receptor antagonist as well as much less active as a selective serotonin reuptake inhibitor. It is also about 3-fold less potent of a α3β4 nicotinic receptor antagonist than DXM and has a lower affinity for sigma-1 receptors.
3-Methoxymorphinan (also known as 3MM) is produced by the N-demethylation of dextromethorphan by the CYP3A4 enzyme and inhibits the CYP2D6 enzyme.[18] It has local anaesthetic effects.
3-Hydroxymorphinan (also known as 3HM) is produced by O-demethylation of 3-methoxymorphinan by CYP2D6 and metabolization of dextrorphan by CYP3A4 and CYP3A5. 3-Hydroxymorphinan exhibits neuroprotective and neurotrophic effects.
PHYSICAL EFFECTS
STIMULATION AND SEDATION - At lower, recreational doses, DXM is predominantly stimulating, in so much as one cannot fall asleep while on it while occasionally also encouraging physical activities such as walking or socializing. However, it can produce waves of tiredness, or the desire to lay down with the eyes closed in a sleep-like state. As higher dosages are approached however, the experience generally turns very sedating, sometimes resulting in the user not moving at all.
PERCEPTION OF BODILY LIGHTNESS - This creates the sensation that the body is floating and has become entirely weightless. This effect is strangely stimulating and encourages physical activities at low to moderate dosages by making the body feel light and effortless to move.
SPONTANEOUS PHYSICAL SENSATIONS - The DXM "body high" is a sharp, pleasurable tingling sensation which can be localized to the hands, feet, and head. In lower doses, it can produce an empowering stimulated sensation.
PHYSICAL EUPHORIA - This results in feelings of physical euphoria which range between mild pleasure to powerful, all-encompassing bliss.
APPETITE SUPPRESSION - This can persist throughtout the next day.
MOTOR CONTROL LOSS - A loss of gross and fine motor control alongside balance and coordination is prominent within DXM and becomes especially strong at higher dosages. This suggests that one should be sitting down before the onset to prevent falling over and becoming injured.
SPATIAL DISSOCIATION - A spinning sensation is commonly felt that can result in mild disorientation as if one were falling through a hole.
NAUSEA - DXM can sometimes produce extreme nausea and vomiting, typically during the come up phase of the experience. This is more intense and consistent than the nausea produced by ketamine and MXE. This is likely not caused just by DXM itself, but rather by the medium which contains the DXM, which is usually syrup or gelatin capules. When pure DXM is consumed it is rare to experience nausea.
INCREASED PERSPIRATION - This is the result of a combination of increased bodily temperature and temperature regulation suppression.
ITCHINESS - This effect is colloquially known as "robo-itch". Many users never experience this effect while some individuals can experience it quite intensely. It is caused by histamine release.
DIZZINESS - At higher dosages this can result in incapability to willingly stand up.
PHYSICAL AUTONAMY - At very high dosages some may find to awake in strange locations, sometimes while standing or walking with no recollection of how they got there.
TACTILE SUPPRESSION - This partially to entirely suppresses sense of touch, creating feelings of numbness within the extremities. It is responsible for the anesthetic properties of this substance.
GAIT ALTERATION - This is a common effect on DXM and is commonly referred to as "robo walking". As with itchiness, some users may never experience this effect while others may experience it quite intensly.
PUPIL DIALATION
GUSTORY HALLUCINATION
OPTICAL SLIDING
PAIN RELIEF
COUGH SUPPRESSION
CHANGES IN FELT BODILY FORM
MUSCLE SPASMS
INCREASED BLOOD PRESSURE
INCREASED HEART RATE
INCREASED BODILY TEMPERATURE
TEMPERATURE REGULATION SUPPRESSION
VISUAL EFFECTS
PERIPHERAL VISION ENHANCEMENT - This effect usually only occurs at low doses.
FRAME RATE ENHANCEMENT - This effect is rare and occasionally experienced on the lower plateaus. It appears to be setting dependent.
DOUBLE VISION - This component is prevalent at moderate to heavy dosages and makes reading impossible unless one closes an eye.
PATTERN RECOGNITION SUPPRESSION- This effect generally occurs at higher dosages and makes one unable to recognize and interpret perceivable visual data. Examples can include an inability to recognize human faces or motion.
NYSTAGMUS - At very high dosages one may be incapable of recognizing things such as movement of objects or human faces.
DRIFTING - Visual drifting has been reported to occur on DXM, although it is uncommon. This effect is unrealistic in appearance. The distortions fast and smooth in motion, and are fleeting in appearance.
GEOMETRY - The visual geometry that can be experienced on DXM can be described as very bright, colorful, psychedelic and intricate when compared to that of ketamine or MXE, but darker than psychedelics like LSD. It does not extend beyond level 4 and can be comprehensively described through its variations as intricate in complexity, algorithmic in style, synthetic in feel, unstructured in organization, brightly lit in lighting, multicoloured in scheme, glossy in shading, soft in edges, small in size, slow in speed, smooth in motion, equal in rounded and angular corners, immersive in-depth and consistent in intensity.
ENVIRONMENTAL CUBISM
ENVIRONEMNTAL ORBISM
PERSPECTIVE DISTORTIONS
SCENERY SLICING
TRACERS
VISUAL HAZE
VISUAL STRETCHING
VISUAL ACUITY SUPPRESSION OR ENHANCEMENT
DISTORTIONS
AFTER IMAGES
DEPTH PERCEPTION ENHANCEMENT
The head space of DXM is often described as distinctly hallucinogenic, impairing, disorientating and generally less clear-headed in comparison to that of MXE and ketamine. The cognitive effects of DXM can be broken down into several separate subcomponents which are listed and described below:
ANXIETY SUPPRESSION - Although DXM typically suppresses anxiety, it is also able to produce it in certain conditions.
COGNITIVE EUPHORIA - While states of cognitive euphoria are commonly reported, this effect can unpredictably manifest itself as cognitive dysphoria for no apparent reason, particularly at higher doses.
DELUSION - This effect can occur spontaneously among some users and is more likely to occur at higher doses.
EMOTIONAL ENHANCEMENT - Though this effect isn't as consistent as it is with other commonly used hallucinogens it is more prominent than with most dissociatives.
INCREASED LIBIDO - This is exclusively felt in low doses.
INCREASED MUSIC APPRECIATION - This effect can be very intense with DXM, especially at the lower plateaus. Listening to music while on DXM greatly intensifies the experience and produces strong euphoria.
AMNESIA - This effect is usually only present with higher dosages, past the threshold for ego death (which can vary between people based on their individual metabolism). It can range from partial to complete memory loss of the experience.
PERSONAL BIAS SUPRESSION - This effect is not usually as pronounced as it is with other more commonly used hallucinogens such as LSD or psilocin.
PERSONAL MEANING ENHANCEMENT - This effect is typically only present on the lower plateaus and varies in its believability and content.
TIME DISTORTION - Time while on DXM often feels very stretched out, for example, it may feel like an hour has passed when in reality only ten minutes have passed.
CONCEPTUAL THINKING
ANALYSIS ENHANCEMENT
FEELINGS OF IMPENDING DOOM
DEREALIZATION
EGO INFLATION OR DECREASE
DREAM POTENTIATION IMMERSION ENHANCEMENT
MEMORY SUPPRESSION
EGO DEATH
NOVELTY ENHANCEMENT
THOUGHT ACCELERATION
CREATIVITY ENHANCEMENT
DECREASED LIBIDO
DEJA VU
WAKEFULNESS
DEPERSONALIZATION
AUDITORY EFFECTS
AUDITORY ENHANCEMENT
AUDITORY SUPPRESSION
AUDITORY DISTORTION
AUDITORY HALLUCINATION
DISCONNECTIVE EFFECTS
PHYSICAL DISCONNECTION - Although this effect is present, it is usually not as powerful or as consistent as with ketamine or PCP.
VISUAL DISCONNECTION - This eventually results in the DXM's equivalent of the "K-hole" or more specifically, holes, spaces and voids alongside of structures.
COGNITIVE DISCONNECTION
MULTI-SENSORY EFFECTS
SYNAESTHESIA - In its fullest manifestation, this is a very rare and non-reproducible effect. Increasing the dosage can increase the likelihood of this occurring, but seems only to be a prominent part of the experience among those who are already predisposed to synaesthetic states.
TRANSPERSONAL EFFECTS
SPIRITUALITY ENHANCEMENT
EXISTENTIAL SELF-REALIZATION
UNITY AND INNERCONNECTEDNESS
AFTERGLOW
The afterglow is a feeling that can occur within the 24 hours after the end of the experience. It can be described regarding its physical sensation as one of euphoria, rejuvenation, relaxation and a light bounciness. Regarding its cognitive effects, it often comes in the form as a loss of anxiety, feelings of content, and a noticeable increase in one's ability to appreciate music and other sensory stimuli that are sometimes accompanied with mild derealization or depersonalization.
PLATEAUS
FIRST (1.5 - 2.5 mg/kg) - The effects felt in the first plateau are usually not very intense. They can include but are not limited to: cognitive euphoria, increased music appreciation, time distortion, pupil dilation, and stimulation. First plateau is often described as a "drunk" feeling.
SECOND (2.5 - 7.5 mg/kg) - Most DXM users consider this the to be the most recreational plateau. The second plateau is more sedating than stimulating, euphoria and visual disconnection are more intense. Additional effects of the second plateau can include but are not limited to: Wakefulness, physical euphoria, spatial disorientation. Many users of DXM do not proceed past the second plateau, as the desired effects are thought to be outweighed by the increasingly unpredictable adverse physical and cognitive effects as well as a more pronounced "body load".
THIRD (7.5 - 15 mg/kg) - The effects of the third plateau can include but are not limited to: sedation, nausea, memory suppression and ego death, auditory hallucinations, internal hallucinations, cognitive dysphoria, anxiety, delusions, and all the effects of the second plateau.
FOURTH (15 - 20 mg/kg) - Doses of DXM in this range and beyond are considered to be very dangerous and are associated with a high risk of injury and overdose, and are therefore advised against. The effects of the fourth plateau can include but are not limited to external hallucinations, complete dissociation, and all the effects of the third plateau, with greater intensity.
FIFTH (also known as "Plateau Sigma") - A common method to experience the so-called "Plateau Sigma" is to take second plateau dose, followed by another second plateau dose three hours later, then at the peak of the second dose, take a fourth plateau dose. Plateau Sigma may also occur unintentionally from redosing. It is nearly always a very unpleasant and unpredictable experience. The experience can last from one day to four days. Plateau Sigma usually results in delirious hallucinations, dysphoria, delirium, psychosis, and anxiety. Plateau Sigma has a high potential to cause serotonin syndrome and is therefore strongly advised against.
DOSAGE
Threshold - 100 mg
Light - 100 - 200 mg
Common - 200 - 400 mg
Strong - 400 - 700 mg
Heavy - 700 mg +
TRANSPERSONAL EFFECTS
SPIRITUALITY ENHANCEMENT
EXISTENTIAL SELF-REALIZATION
UNITY AND INNERCONNECTEDNESS
AFTERGLOW
The afterglow is a feeling that can occur within the 24 hours after the end of the experience. It can be described regarding its physical sensation as one of euphoria, rejuvenation, relaxation and a light bounciness. Regarding its cognitive effects, it often comes in the form as a loss of anxiety, feelings of content, and a noticeable increase in one's ability to appreciate music and other sensory stimuli that are sometimes accompanied with mild derealization or depersonalization.
PLATEAUS
FIRST (1.5 - 2.5 mg/kg) - The effects felt in the first plateau are usually not very intense. They can include but are not limited to: cognitive euphoria, increased music appreciation, time distortion, pupil dilation, and stimulation. First plateau is often described as a "drunk" feeling.
SECOND (2.5 - 7.5 mg/kg) - Most DXM users consider this the to be the most recreational plateau. The second plateau is more sedating than stimulating, euphoria and visual disconnection are more intense. Additional effects of the second plateau can include but are not limited to: Wakefulness, physical euphoria, spatial disorientation. Many users of DXM do not proceed past the second plateau, as the desired effects are thought to be outweighed by the increasingly unpredictable adverse physical and cognitive effects as well as a more pronounced "body load".
THIRD (7.5 - 15 mg/kg) - The effects of the third plateau can include but are not limited to: sedation, nausea, memory suppression and ego death, auditory hallucinations, internal hallucinations, cognitive dysphoria, anxiety, delusions, and all the effects of the second plateau.
FOURTH (15 - 20 mg/kg) - Doses of DXM in this range and beyond are considered to be very dangerous and are associated with a high risk of injury and overdose, and are therefore advised against. The effects of the fourth plateau can include but are not limited to external hallucinations, complete dissociation, and all the effects of the third plateau, with greater intensity.
FIFTH (also known as "Plateau Sigma") - A common method to experience the so-called "Plateau Sigma" is to take second plateau dose, followed by another second plateau dose three hours later, then at the peak of the second dose, take a fourth plateau dose. Plateau Sigma may also occur unintentionally from redosing. It is nearly always a very unpleasant and unpredictable experience. The experience can last from one day to four days. Plateau Sigma usually results in delirious hallucinations, dysphoria, delirium, psychosis, and anxiety. Plateau Sigma has a high potential to cause serotonin syndrome and is therefore strongly advised against.
DOSAGE
Threshold - 100 mg
Light - 100 - 200 mg
Common - 200 - 400 mg
Strong - 400 - 700 mg
Heavy - 700 mg +
Коментари
Публикуване на коментар