Non-medical use of dextromethorphan

Since their introduction, preparations containing the over-the-counter drug dextromethorphan have been used in a manner inconsistent with their labeling, often as a recreational drug or for spiritual experiences. Dextromethorphan has little to no psychological effect in the doses used medically, however alteration of consciousness generally occurs following ingestion of approximately 4 to 50 times the therapeutic dose over a relatively short period of time.

People who study the specific effects of psychotropic substances classify DXM as a dissociative drug, a major subclass of hallucinogenic drugs. It generally does not produce withdrawal symptoms characteristic of physically addictive substances, but psychological addiction has been reported by some users.

History

Early history

In 1958 the Food and Drug Administration (FDA) approved the use of dextromethorphan as an antitussive, in response to the rampant recreational use of, and addiction to, the now DEA-scheduled codeine that was present in cough medicines at the time. The perceived advantages of dextromethorphan in comparison to codeine were the lack of physical addiction, no abuse potential and the absence of a sedative-like effect from a normal dosage. Two years after its approval, dextromethorphan was finally marketed in the United States as Romilar, a dextromethorphan-only pill, which touted itself as the safe cough medicine alternative to the heavily abused codeine. While it did produce few side effects, it did not take long for a few (ab)users to discover dextromethorphan's non-medical use potential. This most likely came from users of codeine based cough medicine who wondered if the new medicine had any recreational use potential.

1970s

The removal of Romilar from shelves in 1973 left many wondering if dextromethorphan would be phased out in favor of a new compound less susceptible to abuse that could alleviate coughs as well as codeine and dextromethorphan. Manufacturers instead re-released dextromethorphan to the public in syrup form, which is theoretically harder to misuse. While some allege that reports of abuse went down mainly because of the unattractive delivery agent, William White, a dextromethorphan researcher, suggests the plunge in DXM abuse cases was mainly due to the availability of more appealing hallucinogens such as LSD, and psilocybin.

1980s

The 1980s saw Dextromethorphan abuse remain localized in small groups of users, notably the hardcore punk community.^* While many now regard DXM's potential for abuse as common knowledge, in the 1980s due to the lack of widespread Internet access and sources for reputable information on drugs, many were left in the dark about its psychoactive properties.

Early 1990s

The early 90s trend of DXM use followed closely to the 80s due to the War on Drugs, and the lack of information about dextromethorphan. The Internet began to take shape around the world at this time allowing many to communicate with a defined topic at hand. Much of the early (and current) dissemination of knowledge on DXM was conducted on Usenet, calling attention to an obscure psychoactive drug. As the availability of access to the Internet became more common, dedicated websites with more accurate (and more scientific) information concerning DXM appeared, and were easily found by many. This flow of information has only increased with time. The growth of the Internet and the ease of spreading information also led to deaths from DXM coming to light. There are now websites largely focusing on documenting the circumstances of these deaths.

Late 1990s - present

As of the late 1990s, dextromethorphan became available in pure powder form from various grey-market chemical retailers. As the United States Drug Enforcement Administration became increasingly aware of online research chemical sales, it launched Operation Web Tryp, which completed on July 21, 2004. The operation resulted in ten arrests and the shutdown of several websites selling research chemicals. Because many of the online vendors also sold DXM in pure powder form, this affected the recreational DXM community by making DXM powder significantly harder to find, forcing some users to use over-the-counter medical products instead.

Dextromethorphan is most frequently consumed in the form of over-the-counter cough medicine preparations. Commonly used brands worldwide are Robitussin, Romilar, Coricidin, Zicam and Delsym. Slang terms for DXM often relate to the brands, such as "tussin" or "robo" "dex," and "skittles" (in reference to the physical appearance of Coricidin). Colloquially, use of DXM for its psychoactive effects is frequently referred to as "dexing," "tussing," or "robotripping."

It should be noted that Coricidin, a popular preparation of DXM, is extremely dangerous at recreational doses because it also contains Chlorpheniramine Maleate, which is potentially fatal at high doses (see Preparations and their Risks)

William White's DXM FAQ

The plateau model of DXM effects seems to have emerged largely from the Internet drug culture of the mid-1990s, especially William White's FAQ. This document, which was little known outside the online drug community, details DXM's effects, chemistry and dangers in lengthy detail. Using science, history and hands-on reports from individual users, White's manual acted as a virtual manual for the interested dextromethorphan user. While originally presenting DXM as generally benign, White, receiving various reports from users reporting apparent long-term effects, changed his introduction to warn users more vigorously. The most known claim was lesions caused in the brain from heavy dextromethorphan use called Olney's Lesions.These claims have since been refuted, and William White retracted most of his claims.^*

Effects

While the maximum FDA approved dose of dextromethorphan is 30 mg, in significantly higher doses of 150 mg to 2000 mg, dextromethorphan is recreationally used as a dissociative drug that can cause depersonalization, euphoria, dissociation, dreamlike mental effects, visual and aural hallucinations, and in sufficiently high doses, out of body experiences. Some use high doses for spiritual purposes or to attain a greater self-knowledge. The recreational effects of dextromethorphan typically last between 4 - 8 hours, although the duration may increase with higher doses.

The author of the DXM FAQ, William White, opined that the levels of the DXM experience come in dose-dependent stages, or "plateaus," with each plateau possessing different characteristic effects Some users observe distinctive differences between each plateau. Further information on DXM and DXM's plateaus may be found in [http://www.erowid.org/chemicals/dxm/dxm.shtml Erowid's DXM Vault. This system for distinguishing doses is very popular within the DXM community. It is common to see the plateau system discussed (with varying accuracy to the original specification) on DXM web sites and news articles.

Lower plateau doses of dextromethorphan are characterized by a mild intoxication and euphoria similar to a combination of MDA and alcohol, due to its serotonin and dopamine reuptake inhibition. Often, audio intake is altered, leaving the user with an altered peception of music and sound. This alteration allows the brain to process sounds slower, making music sound different, more defined and bold. Music often adds to the pleasure of a DXM experience.

Moderate doses tend to decrease agility, coordination and affect the user's perception of time. Some users report euphoria, while others do not. Sound may take on a flanging effect and the user may have difficulty distinguishing distances between objects. Dissociative cognitive effects become apparent, resulting in the user feeling "detached" or "disconnected" from reality. Closed eye hallucinations may be observable.

High doses have been compared to ketamine and can include significant depersonalization and dissociation, bizarre thought patterns, and the user often feeling completely disconnected from external reality. Marked changes in visual perception are increasingly noticeable and can include lilliputian hallucinations. Coordination is significantly impaired, and many users are unable to move comfortably. Out of body experiences and religious experiences are common. The highest nonlethal doses of DXM bring about a separation from reality which has much in common with forms of psychosis: extreme schizophrenic hallucinations, such as hearing voices, seeing entities with eyes open, and experiencing a total breakdown of reality. Dextromethorphan becomes toxic at 20 - 30 mg per kg of bodyweight, producing vomiting, fever, and possibly death, and high doses may be dangerous.

Neutral effects of using DXM include "robo-walk" ( when a user on DXM walks like a robot due to loss of coordination ), discoordination, trismus and bruxia (clenched jaw, teeth-grinding), and heavy pupil dilation. Negative effects can include diarrhea, vomiting, and severe nausea due to the consistency of cough syrup, and are more prevalent when it is imbibed in an extremely short amount of time. Using DXM can also cause hangovers on the following day, and should not be used in combination with alcohol. Excessive use over a long period of time can have adverse effects on the liver, pancreas, and kidneys due to the extremely high concentration of glucose in cough syrup.

Some DXM mixtures have the active ingredient listed 'dextromethorphan polystirex' on the bottle. This means the DXM molecule with the hydrobromic acid base is suspended inside a plastic-molecule capsule which extends DXM's half-life to 10-12 hours. This half-life extenstion is because half of the DXM takes about 3 hours to break down due to being inside the polystirex. Because of this long metabolizing method, the blood stream receives a greater DXM to DXO ratio. Using Delsym often, will create tolerance very fast compared to just DXM products without the polystirex mixture. Usually no more than three 3oz Delsym bottles in one month. Using more than that will probably only inhibit serotonin and dopamine reuptake but will not bind to the NDMA, σ₁ and σ₂ receptors.

Legality

While antitussive preparations containing DXM are legal to purchase from most pharmacies worldwide, it may be illegal to purchase bulk DXM that is intended for laboratory use if one intends to use it recreationally.

In the United States, 2003 saw Texas and North Dakota vote against bills that would prohibit the sale of products containing DXM to minors. In 2004 California also followed suit and voted against a bill similar to the ones proposed in Texas and North Dakota. Although these three states have been unable to pass these bills, New York in 2004 passed legislation making the distribution of two or more dextromethorphan-containing products to a minor a misdemeanor (Bill Summary - S06244). This variation in States’ decision to restrict the availability of dextromethorphan to minors is a contested matter.

In 2005, the Virginia General Assembly considered HB 2045, a bill to make distribution of DXM to minors a Class 1 misdemeanor^*.

A few pharmacies around the United States have started to put DXM-containing products behind the counter and putting an age limit of 18 on purchasing them (notably Coricidin brand products). It is possible that this stems from concerns regarding shoplifting rather than recreational use.

DXM is specifically excluded from regulation under the Schedules of the Single Convention on Narcotic Drugs.

DXM appears to be available over the counter in most countries other than Hong Kong and Thailand ^*.

Preparations and their risks

Most over-the-counter cough medicines contain other drugs besides dextromethorphan that can be quite dangerous when taken in high doses. These ingredients include acetaminophen (Also referred to as paracetamol or APAP) and chlorpheniramine (an anticholinergic antihistamine contained in Coricidin Cough & Cold which can cause severe and life-threatening symptoms including: seizures, shortness of breath or troubled breathing, weakness, loss of consciousness, severe dry mouth, nose, or throat, bleeding from skin, mouth, eyes, rectum, and vagina, and possibly death^*). It is likely that brompheniramine, another antihistamine, would cause the same complications as chlorpheniramine. Some cough medications also often contain guaifenesin (an expectorant), which can cause nausea and vomiting in high doses. Pseudoephedrine (a decongestant) may cause other complications as well, such as dangerous hypertension potentially leading to coma or death, if enough is ingested.

Coricidin Cough & Cold (CCC) in particular is a common source of DXM in the United States for uninformed users. There have been reports of deaths resulting from overdose of dextromethorphan combined with chlorpheniramine maleate, an antihistamine found in CCC. Taking Coricidin in excessive amounts, such as those required for recreational dextromethorphan use, and is generally considered to be extremely dangerous, thus Coricidin is not under any circumstances to be considered a safe source of DXM. Nonetheless, among many users it has remained a popular choice, possibly due to ignorance, or that it contains more DXM than most products at 30mg a pill. Some users have taken to shoplifting it and similar preparations to such an extent that some stores have stopped selling the product, made it available only by request to the pharmacist, or made it unavailable to minors. Dextromethorphan can be extracted from Coricidin tablets in cold water, but this procedure is not widely used or known, but is available from the internet.

Some users have extracted Dextromethorphan from cough medicine using ammonia, naphtha and lemon juice (citric acid), in a process typically called the "Agent Lemon extraction." The extraction, when properly performed, is said to remove most of the hydrobromic acid ions and guaifenesin (if the preparation contains it) from the cough syrup. However, it does not remove other ingredients such as pseudoephedrine or paracetamol ^*, which are toxic in high doses.

Erowid.org has compiled a list of some DXM-containing products and their other active ingredients, available here.

Dangers

There have been a small number of dextromethorphan overdose deaths documented in medical and media reports. Even when used alone, dextromethorphan overdoses have been fatal, although all fatalities that have been reported only occurred at very high doses. Lethal toxicity starts at approximately 20mg/kg, which is about 1360mg for a 150lb (68kg) person.

It is currently unknown whether or not recreational doses of DXM are safe.

With dextromethorphan, as with most other drugs, concurrant use of other medications is not recommended. Many medications can be substrates or inhibitors of the liver enzyme used in the metabolism of dextromethorphan, CYP2D6. Selective serotonin reuptake inhibitors (SSRIs) are a class of drugs that inhibit the cytochrome P450-2D6 enzyme responsible for metabolizing DXM down into dextrorphan (DXO). This inhibition can cause brain serotonin to build to dangerous levels, engendering a potentially fatal reaction known as serotonin syndrome.

Monoamine oxidase inhibitors interact with almost all medications, including dextromethorphan. The combination is almost always fatal.

Approximately 5% of caucasians have a functional deficiency in the enzyme CYP2D6, which metabolizes DXM and many other drugs (such as the opioids) ^*. Enzyme-deficient individuals can overdose very easily, potentially leading to hospitalization. Thus, those who choose to use DXM recreationally are cautioned to start with a low dose.

William E. White published a paper on Usenet claiming that high doses of disassociatives (including Dextromethorphan) may cause brain damage in the form of NMDA neurotoxicity (NAN or Olney's lesions). A researcher named John Olney demonstrated that high doses of NMDA antagonists, the class of drugs to which dextromethorphan belongs, produced small lesions in the brains of lab rats, which are now known as Olney's lesions. The doses required to produce damage are far in excess of human recreational doses, but there have not been studies on long-term, lower-dose use. However, White's article has been challenged by one Cliff Anderson in his paper, The Bad News Isn't In. White later retracted his original claims in a response to Cliff Anderson's paper though he still warns of possible long term damage from using DXM.

External links

The DXM Harm Reduction Project
Coricidin (Dextromethorphan + Chlorpheniramine Maleate) Harm Reduction, specifically about Coricidin.
The Third Plateau - harm reduction and community site.
The Dextromethorphan FAQ - the exhaustive FAQ on DXM by William White
The Vaults of Erowid
The Dextroverse - harm reduction and community site.

References

Bem JL, Peck R. Dextromethorphan. An overview of safety issues. Drug Saf. 1992;7:190-199.
Otton SV, Wu D, et al. Inhibition by fluoxetine of cytochrome P450 2D6 activity. Clin. Pharmacol. & Therapeutics. 1993;53:401- 409.
Zhou GZ, Musacchio JM. Computer-assisted modeling of multiple dextromethorphan and sigma binding sites in guinea pig brain. Eur. J. Pharmacol.. 1991;206:261-269.
White, William E. (1995) The Dextromethorphan FAQ: Answers to Frequently Asked Questions about Dextromethorphan, version 4.0.

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