DXM

Also known as

Dextromethorphan, dex, robo, syrup, robotussin, robitussin, skittles, triple c, tussin, CCC, poor man's PCP, rojo, velvet

Classification

Hallucinogen

Overview

It is a synthetic antitussive (i.e. cough suppressant) drug of the morphinan class. It is one of the active ingredients in many over-the-counter common cold and cough medicines, including generic drug labels and store brands. Dextromethorphan has also found other uses in medicine, ranging from pain relief to psychological applications .

Dextromethorphan (DXM) is a cough-suppressing ingredient found in a variety of over-the-counter cold and cough medications. Like PCP and Ketamine, dextromethorphan is a dissociative anaesthetic, meaning DXM effects can include hallucinations .

The d-isomer of the codeine analog of levorphanol. Dextromethorphan shows high affinity binding to several regions of the brain, including the medullary cough centre. This compound is an NMDA receptor antagonist (receptors, N-methyl-D-aspartate) and acts as a non-competitive channel blocker. It is one of the widely used antitussives, and is also used to study the involvement of glutamate receptors in neurotoxicity .

Medical usage

For treatment and relief of dry cough .

What does it look like?

In its pure form, dextromethorphan occurs as a white powder, although it is most commonly consumed in tablet, capsule, or syrup forms .

Cough syrup and cough and cold tablets or gel caps that are available without a prescription. Also, dextromethorphan can be purchased in a powder form, often over the internet .

Dextromethorphan occurs as white crystals, is sparingly soluble in water, and freely soluble in alcohol .

DXM can come in the form of cough syrup, tablets, capsules, or powder .

Source

Dextromethorphan is a synthetic compound .

Why take it?

Sought after effects

• euphoria,
• mood lift,
• increased giggling and laughing,
• dissociation of mind from body,
• creative dream-like experiences,
• increased tactile sensation .

Undesired effects

• vomiting,
• dizziness,
• body itching,
• rash, red blotchy skin,
• diarrhoea,
• fever,
• tachycardia .

Abuse

This drug has been used for abuse. Orally in doses of 300 mg to 1800 mg in adults it can cause intoxication with hyperexcitability, visual and/or auditory hallucinations , . It has been reported that sniffing 0.25 g two to three times a day over 2 to 3 months produced euphoria and restlessness for up to 2 hours followed by dizziness, nausea, depression and fatigue , .

How long do its effects last?

Onset of effects

• oral - 30 - 120 minutes .
• all ROA's - 20 - 60 minutes .

Come up

• oral - 60 - 120 minutes .

Peak

• oral - 3 - 6 hours .

Offset

• oral - 2 - 4 hours .

Duration of effects

• oral - 8 - 12 hours .
• all ROA's - 6 - 8 hours .

After-effects

• oral - 4 - 24 hours .
• all ROA's - 1 - 12 hours .

Pharmacology

Pharmacodynamics

Dextromethorphan suppresses the cough reflex by a direct action on the cough centre in the medulla of the brain. Dextromethorphan shows high affinity binding to several regions of the brain, including the medullary cough centre. This compound is an NMDA receptor antagonist and acts as a non-competitive channel blocker. It is one of the widely used antitussives, and is also used to study the involvement of glutamate receptors in neurotoxicity .

The antitussive effects of dextromethorphan and the metabolite dextrorphan are secondary to binding in the CNS at non-opioid receptors. Dextromethorphan does not have analgesic or addictive properties, although abuse and dependence have been described . One of the major metabolites, dextrorphan has cough suppressant activity .

Absorption

Rapidly absorbed from the gastrointestinal tract .

Metabolism

Hepatic. Rapidly and extensively metabolised to dextrorphan (active metabolite). One well known metabolic catalyst involved is a specific cytochrome P450 enzyme known as 2D6, or CYP2D6 .

Following oral administration, dextromethorphan is rapidly absorbed from the gastrointestinal tract, where it enters the bloodstream and crosses the blood-brain barrier. Dextromethorphan shows high affinity binding to several regions of the brain, including the medullary cough centre. The first-pass through the hepatic portal vein results in some of the drug being metabolised into an active metabolite of dextromethorphan, dextrorphan, the 3-hydroxy derivative of dextromethorphan. The therapeutic activity of dextromethorphan is believed to be caused by both the drug and this metabolite. Dextromethorphan is predominantly metabolised by the liver, by various hepatic enzymes. Through various pathways, the drug undergoes (O-demethylation (which produces dextrorphan), N-demethylation, and partial conjugation with glucuronic acid and sulfate ions .

Half-life

3 - 6 hours . The half life of the parent compound is approximately 2 to 4 hours in people with normal metabolism .

Elimination

Dextromethorphan and its metabolites are excreted via the kidney. Depending on the metabolism phenotype up to 11% may be excreted unchanged or up to 100% as demethylated conjugated morphinan compounds . In the first 24 hours after dosing, less than 0.1% is eliminated in the faeces , .

Lethal dosage

LD50 3.3377 mol/kg in rats .

Mechanism of action

Dextromethorphan is an opioid-like drug that binds to and acts as antagonist to the NMDA glutamatergic receptor, it is an agonist to the opioid sigma 1 and sigma 2 receptors, it is also an alpha3/beta4 nicotinic receptor antagonist and targets the serotonin reuptake pump. Dextromethorphan is rapidly absorbed from the gastrointestinal tract, where it enters the bloodstream and crosses the blood-brain barrier. The first-pass through the hepatic portal vein results in some of the drug being metabolised into an active metabolite of dextromethorphan, dextrorphan, the 3-hydroxy derivative of dextromethorphan .

Mode of use

Abusers of DXM describe the following four dose-dependent "plateaus" -

Plateau	Dose (mgs)	Behavioural effects
First	100 - 200	Mild stimulation
Second	200 - 400	Euphoria and hallucinations
Third	300 - 600	Distorted visual perceptions,
		Loss of motor coordination
Fourth	500 - 1500	Out-of-body sensations

DXM is abused in high doses to experience euphoria and visual and auditory hallucinations. Abusers take various amounts depending on their body weight and the effect they are attempting to achieve. Some abusers ingest 250 to 1,500 milligrams in a single dosage, far more than the recommended therapeutic dosages .

Signs of usage

• confusion,
• dizziness,
• double or blurred vision,
• slurred speech,
• impaired physical coordination,
• abdominal pain,
• nausea and vomiting,
• rapid heartbeat,
• drowsiness,
• numbness of fingers and toes,
• disorientation ,
• changes in appearance or habits,
• isolation from the family, spending evenings behind a locked bedroom door,
• evasiveness or secretive behaviour,
• many hours spent away from home without explanation,
• missing money,
• changes in appetite,
• hostility and anger,
• lying,
• mood changes without apparent reason,
• changes in relationships with friends or family,
• inability to focus,
• poor coordination,
• sullen mood or depression,
• silence, withdrawn periods ,
• disorientation and confusion,
• dizziness or loss of coordination,
• stomach spasms,
• drowsiness,
• slow, laboured breathing,
• muscle twitches,
• vomiting,
• intoxication symptoms such as slurred speech,
• fast heart rate,
• loss of sense perceptions,
• loss of memory,
• inability to focus,
• rashes,
• itchy skin,
• numb extremities .

Effects

Physical effects

• changes in felt bodily form,
• gustatory hallucinations,
• physical autonomy,
• physical euphoria,
• spatial disorientation,
• appetite suppression,
• cough suppression,
• pain relief,
• perception of bodily lightness,
• sedation,
• tactile suppression,
• dizziness,
• increased blood pressure,
• increased heart rate,
• increased perspiration,
• itchiness,
• muscle spasms,
• nausea,
• optical sliding,
• temperature regulation suppression .

Cognitive effects

• cognitive euphoria,
• conceptual thinking,
• depersonalisation,
• derealisation,
• déjà vu,
• time distortion,
• creativity enhancement,
• dream potentiation,
• emotionality enhancement,
• immersion enhancement,
• increased libido,
• increased music appreciation,
• novelty enhancement,
• personal meaning enhancement,
• amnesia,
• cognitive fatigue,
• decreased libido,
• disinhibition,
• information processing suppression,
• memory suppression,
• personal bias suppression,
• thought deceleration,
• unity and interconnectedness .

Visual effects

• after images,
• environmental cubism,
• environmental orbism,
• perspective distortions,
• scenery slicing,
• tracers,
• visual haze,
• acuity suppression,
• double vision,
• frame rate suppression,
• pattern recognition suppression,
• visual disconnection,
• geometry,
• autonomous entities,
• external hallucinations,
• internal hallucinations,
• perspective alterations,
• scenarios and plots,
• settings, sceneries, and landscapes .

Auditory effects

• auditory distortion,
• auditory enhancement,
• auditory hallucinations,
• auditory suppression .

Minor effects

Less common or rare

• confusion,
• constipation,
• dizziness (mild),
• drowsiness (mild),
• headache,
• nausea or vomiting,
• stomach pain .

Positive

• euphoria,
• mood lift,
• increased giggling and laughing,
• dissociation of mind from body,
• creative dream-like experiences,
• increased tactile sensation,
• some users report empathy and forgiveness towards other people .

Neutral

• pupil dilation,
• visual stop motion effect (flanging or strobing),
• visual and aural (auditory) hallucinations,
• decreased sexual functioning (difficulty achieving orgasm),
• confusion, disorientation,
• skin sensitivity, alters tactile (touch) and skin sensations,
• robotic, zombie-like walking, "robo-walk",
• dis-coordination, reduced agility,
• loss of appetite,
• involuntary flexing of muscles,
• feelings of merging with adjacent objects like a couch or bed (with higher doses),
• some users report feeling disconnected, isolated from others, (positive when sought) .

Negative

• vomiting,
• dizziness,
• body itching,
• rash, red blotchy skin,
• diarrhoea,
• fever,
• tachycardia .

Overdose

• blurred vision,
• confusion,
• difficulty in urination,
• drowsiness or dizziness,
• nausea or vomiting (severe),
• shakiness and unsteady walk,
• slowed breathing,
• unusual excitement, nervousness, restlessness, or irritability (severe) .

Dangerous interactions

Although many drugs are safe on their own, they can become dangerous and even life-threatening when combined with other substances. The list below contains some common potentially dangerous combinations, but may not include all of them. Certain combinations may be safe in low doses of each but still increase the potential risk of death. Independent research should always be done to ensure that a combination of two or more substances is safe before consumption .

• Depressants - This combination potentiates the muscle relaxation, sedation and amnesia caused by one another and can lead to unexpected loss of consciousness at high doses. There is also an increased risk of vomiting during unconsciousness and death from the resulting suffocation. If this occurs, users should attempt to fall asleep in the recovery position or have a friend move them into it. Examples include benzodiazepines, GBL / GHB, 2M2B, opioids, and most commonly, alcohol.
• Stimulants - This combination typically potentiates the anxiety-inducing, manic, delusional and disinhibiting aspects of dissociatives, particularly those without pronounced motor and consciousness-suppression components, like ketamine does, which can increase the likelihood of a panic event or psychotic episode. Prominent examples include PCP and its analogs 3-MeO-PCP, MXE, as well as diarylethylamine class dissociatives like diphenidine or ephenidine. There is also evidence that suggests that combining these two increases their neurotoxicity. Anecdotally, worsened comedowns are also commonly reported when these two classes of substances are combined. Also, this combination will produce a combined depressant effect which can cause dangerous levels of respiratory depression.
• Stimulants - A dangerous rise in blood pressure and heart rate can occur when DXM is combined with a stimulant such as amphetamine and/or cocaine .

Dangerous

• αMT,
• PCP,
• MDMA,
• Alcohol - Both substances potentiate the ataxia and sedation caused by the other and can lead to unexpected loss of consciousness at high doses. Place affected patients in the recovery position to prevent vomit aspiration from excess. Additionally CNS depression can lead to difficulty breathing. Avoid on anything higher than 1st plateau.
• GBL / GHB - Both substances cause ataxia and bring a risk of vomiting and unconsciousness. If the patient falls unconscious while under the influence there is a severe risk of vomit aspiration if they are not placed in the recovery position. This combination is hard to predict.
• Opioids - CNS depression, difficult breathing, heart issues, hepatoxic, just very unsafe combination all around. Additionally if one takes dxm, their tolerance of opiates goes down slightly, thus causing additional synergistic effects.
• Tramadol,
• MAOIs - High risk of serotonin syndrome.
• SSRIs - High risk of serotonin syndrome .

Unsafe

• DOx - The DOx class as psychedelic stimulants have the potential to mask the effects of DXM and could lead to redosing to an unsafe level. DXM can also potentiate DOx resulting in an unpleasantly intense experience.
• NBOMes,
• 2C-T-x,
• 5-MeO-xxT - Little information exists about this combination.
• Amphetamines - Both substances raise heart rate, in extreme cases, panic attacks caused by these drugs have led to more serious heart issues.
• Cocaine - Both substances raise heart rate, in extreme cases, panic attacks caused by these drugs have led to more serious heart issues .

Withdrawal

• fatigue,
• vomiting,
• diarrhoea,
• insomnia,
• nightmares,
• memory issues,
• panic attacks,
• intense cravings,
• flashbacks .

Withdrawal Issues

• Nausea, stomach cramps, and other unpleasant gastro-intestinal effects are common and may persist for days after use.
• Itching and other skin reactions have been reported.
• The large amount of glucose, thickeners, etc., present in many cough syrups may be hard on your kidneys and pancreas .

Paraphernalia

A person abusing DXM may leave behind empty blister packs or empty bottles of cough medication. Vicks, Coricidin, Robitussin and Triaminic formulas all may contain dextromethorphan .

Addiction treatment options

Addiction treatment

Dextromethorphan rehab typically involves a combination of psychological counseling and cognitive-behavioural therapy. The psychological counseling is intended to help the recovering user self-assess his or her dextromethorphan use to figure out the psychological reasons behind the drug abuse or addiction.

Counseling can also help the person understand the full effects and dangers of dextromethorphan, which can help motivate the individual to fully participate in the dextromethorphan (DXM) addiction treatment program. Psychological counseling can take the form of individual or group therapy.

Some dextromethorphan (DXM) addiction treatment programs also include family counseling sessions as part of the treatment in order to get the entire family involved in the recovery process. Cognitive-behavioural therapy is a type of counseling designed to teach practical techniques for avoiding dextromethorphan use and resisting the temptation to use the drug again. This could involve role-playing scenarios that the recovering user might encounter or discussing possible responses to someone offering a hit of dextromethorphan.

Some treatment centres take a more holistic approach to dextromethorphan (DXM) addiction treatment. These types of rehab facilities might include programmes such as music or art therapy, traditional Chinese medicine, or yoga practice to help the user overcome his or her psychological addiction. Dextromethorphan (DXM) addiction treatment can take place in an inpatient or outpatient setting. The choice between these two options depends on the degree of addiction and the individual needs of the person seeking treatment. While there is not a need for medically monitored detox, a residential treatment programme can still be useful for a dextromethorphan addict.

One major advantage of an inpatient residential programme is that it removes the person from social peer groups that can tempt the former user into starting to take the drug again. However, it is necessary to choose a programme that also teaches the recovering drug abuser how to adapt to life outside the inpatient centre once he or she returns to normal life .

History

The racemic parent compound racemorphan was first described in a Swiss and US patent application from Hoffmann-La Roche in 1946 and 1947, respectively; a patent was granted in 1950. A resolution of the two isomers of racemorphan with tartaric acid was published in 1952, and DXM was successfully tested in 1954 as part of US Navy and CIA-funded research on nonaddictive substitutes for codeine.

The FDA approved DXM in 1958 after research supported its legitimacy and effectiveness as a cough suppressant. After its approval, it was introduced as an OTC medication under the name Romilar, which was introduced as a replacement for codeine containing cough remedies in an effort to cut down on abuse. In early 1960's Beat poets Allen Ginsberg and Peter Orlovsky, musicians such as Daevid Allen Soft Machine, and alternative authors such as Jack Kerouac known to have used DXM in the form of Romilar. In 1973, Romilar was taken off the shelves after a burst in sales because of frequent misuse, and was replaced by cough syrup in an attempt to cut down on abuse. In 1975, the popularity and extensive abuse of DXM was recognised, and Romilar was removed from the OTC market. However, DXM was specifically excluded from the Controlled Substances Act (CSA) of 1970, therefore, it was still legal to produce and use.

A few years after its removal from OTC, companies began introducing refined DXM products (e.g., Robitussin, Vicks-44, Dextrotussion) that were designed to limit recreational use by creating an unpleasant taste if consumed in large quantities. Within a short time those same manufactures began to produce forms of DXM with "some appealing flavouring," which led at least one researcher to suggest that the cycle of recreational abuse may be repeated. In 1996, DXM HBr powder could be purchased in bulk from online retailers, allowing users to avoid consuming DXM in syrup preparations .

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