Dextromethorphan hydrobromide (DXM for short) is an antitussive drug that is found in many over-the-counter cold remedies and cough syrups.

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Dextromethorphan hydrobromide (DXM for short) is an antitussive drug that is

found in many over-the-counter cold remedies and cough syrups.

http://www.answers.com/topic/dextromethorphan

 

In considerably higher doses, DXM is a powerful dissociative psychedelic drug.

 

History

Dextromethorphan was first patented with U.S. Patent 2,676,177.

 

In 1958 the FDA approved the use of dextromethorphan as an anti-tussive, in

response to the rampant recreational use of, and addition to, the now

government-regulated 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 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 not take recreational codeine users long to unlock the abuse

potential of dextromethorphan, it took thirteen years from Romilar’s initial

debut for it to be withdrawn from the shelves.

 

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 was harder to abuse in quantity. 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 (White, 1997).

 

The 1980s saw Dextromethorphan abuse remain localized in small communities of

users as the War on Drugs began to ramp up its presence in a drug drenched

United States. While many now regard DXM's potential for abuse as common

knowledge, in the 1980s due to the lack of the Internet and sources for

reputable information on drugs, many were left in the dark about its

dissociative properties.

 

It was not until the beginnings of the Internet were people around the world

able to share information concerning the abuse of drugs in the late 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 dissemination of knowledge on DXM was conducted on Usenet,

calling attention to an obscure recreational 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.

 

Chemistry and Pharmacology

Dextromethorphan is the dextrorotary-enantiomer of the opioid-receptor agonist

levomethorphan. Unlike most opioids, it has not been reported to possess

significant analgesic properties or dependence-liability. It is, however, a

potent antitussive and has largely replaced codeine in this indication. It is

perhaps the most widely available and used antitussive currently marketed.

 

An active metabolite of dextromethorphan is dextrorphan, the 3-hydroxy

derivative of dextromethorphan.

 

The effects of dextromethorphan are believed to be caused by both

dextromethorphan and dextrorphan. Dextromethorphan is predominantly metabolized

by the liver, by the hepatic cytochrome P450 enzyme known as CYP2D6. There is a

significant proportion of the population who have a functional deficiency in

this enzyme (CYP2D6 poor metabolizers). As CYP2D6 is the primary metabolic

pathway in the inactivation of dextromethorphan, the duration of action and

effects of dextromethorphan are significantly increased in such poor

metabolizers. Deaths and hospitalizations have been reported in poor metabolizer

recreational users.

 

A large number of medications (including antidepressants) are potent inhibitors

of CYP2D6 (see CYP2D6 article). There exists, therefore, the potential of

drug-drug interactions between dextromethorphan and concomitant medications.

There have been reports of fatal consequences arising from such interactions.

 

Dextromethorphan crosses the blood-brain barrier, and the following

pharmacological actions have been reported:

 

NMDA glutamatergic receptor antagonist

dopamine reuptake inhibitor

ó1 and ó2 receptor agonist

á3â4 nicotinic receptor antagonist [1]

(http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve & db=pubmed & dopt=Abstr\

act & list_uids=10869398)

serotonin reuptake inhibitor [2]

(http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve & db=pubmed & dopt=Abstr\

act & list_uids=1636059)

 

 

Effects

The advantages of dextromethorphan over codeine are the absence of constipation

and (physical) addiction; it is also less sedative, and has little to no

psychological effect in the doses used medically (typically no more than 30 mg,

or slightly more, spread over several hours; 10-15 mg is a common dose in cough

syrups). It is safe to assume that addiction is impossible, or phenomenally

improbable, for use as recommended; the medical dose of dextromethorphan likely

has less psychological effect than the alcohol in mouthwash, and definitely less

than the caffeine in some headache remedies. Addiction has not been reported

with a first plateau dose recreational dose of dextromethorphan, which extends

to a 2.5 mg/kg dose (up to ten times maximal recommended dose for a 200 pound

adult). A somewhat overweight adult man might have to take 15 pills to reach the

top of that range.

 

The FDA approved dose of dextromethorphan is 30 mg. In significantly higher

doses of 150 mg to 2 g,

dextromethorphan is recreationally used as a psychedelic drug that can cause

dissociation and dreamlike mental effects, as well as visual and aural

hallucinations that can last eight hours or longer in sufficiently high dosage,

and can even include " out of body experiences " at very high doses, though this

is uncommon; some use high doses for attempts at spirituality or self-knowledge.

 

Slang terms for DXM include tussin (generic and store-brand cough syrup is often

sold under the name Tussin). Use of DXM for its psychoactive effects is often

referred to colloquially as " dexing " , " tussing " , or " robotripping " (the latter

term appears to be derived from Robitussin, a brand name of a popular line of

over-the-counter products containing the drug). DXM is not commonly used

recreationally, at least deliberately; see mention of MDMA below.

 

Most drugs have an effect that is proportional to the dose — drinking twice as

much coffee will make one more alert and restless, but will not have

significantly different effects.

 

DXM, however, is unusual in that its effects are nonlinear with respect to dose,

and are grouped into " plateaus " , of which there are typically regarded to be

four. DXM users soon developed unique terminology describing the unique effects

of dextromethorphan.

Plateaus are usually described in terms of dextromethorphan dosage per body

weight (i.e. mg/kg). The dosages associated with the various plateaus have been

described extensively in the DXM FAQ (see external links).

 

The first plateau is characterized by a slight but noticeable " speedy " stimulant

effect, a feeling of inebriation, and an altered sense of movement and position.

The second plateau is an extension of the first plateau. The third plateau has a

set of effects that are significantly " darker " than the earlier plateaus, and

lead to a significantly dissociated effect.

 

The fourth plateau is an extremely dissociative effect, to the point that the

user becomes totally unaware of their physical surroundings.

 

The first plateau can be mildly euphoric, and tends to allow somewhat normal

physical activity. Movement can feel pleasurable (motion euphoria). Music may

sound incredible, or totally wrong. The second plateau results in a noticeably

different shuffling gait (the so-called robo-walk), and can occasionally result

in mild delusions of reference. Intermediate-term and working memory is more

impaired, and time distortion becomes apparent. Some users have a wide-eyed

staring expression (though they may not realize it) at and above these dose

levels. Those encountering a user at or above the second plateau will likely

realize they are high. Starting at higher second plateau dosages, the user

generally feels " disconnected " from reality.

 

The third and fourth plateaus — which according to most should not be explored

without a sober trip sitter — are partially to fully dissociative. At these very

high doses, the user may not want to move around, or may not be consciously

capable of movement. However, due to confusion, disconnection from reality, and

delusions, the presence of an experienced sitter is recommended.

 

While low doses of dextromethorphan can cause euphoria of sorts, most would not

suggest that DXM be used as a cheap, quasilegal substitute for marijuana or

ecstasy, both of which can — unlike large quantities of DXM — be used alone in

relative safety, albeit with possibly decreased enjoyment.

 

It is for all practical purposes simply not possible for a person under the

influence of upper plateau quantities of DXM to appear sober in person or on the

phone due to confusion and very slow reaction time (multiple seconds). Do not

drive on DXM, or swim either alone or on more than first plateau quantities.

 

DXM can also cause vomiting, fever and death. There is also the possibility of

psychological addiction.

 

Two deaths are in the medical literature for use of DXM alone, one of which was

a suicide. This should be contrasted with almost all other drugs, legal and

otherwise. However using DXM at recreational doses bears risks such as brain

damage and psychotic breaks which have not occurred with many drugs (and are

probably impossible with marijuana, ecstasy, and sane doses of LSD, among

others).

 

Also, high-dose use of DXM brings a separation from reality which has much in

common with forms of psychosis. Extreme schizophrenic hallucinations (hearing

voices, seeing entities with eyes open, experiencing a breakdown of reality) are

the hallmark of Plateau Sigma. Over half the people who had a Plateau Sigma

experience have said it was extremely unpleasant and that they would never

repeat it.

 

For more information, see William White's DXM FAQ, available by searching the

web, or from several of the links below. This resource is considered one of the

most useful for anyone considering use of DXM. It should be noted that the FAQ

was last updated in the Clinton administration, and does not include recent

deaths, particularly due to Coricidin Cough and Cold (CCC).

 

Legality

While DXM is legal to purchase from stores, it may be illegal to purchase bulk

DXM that is intended for laboratory use only from online vendors, if one intends

to use it recreationally. There have been no prosecutions for use or possession

by private individuals. The DEA in July, 2004, made arrests on several online

vendors under the Federal Analogues Act of 1986; most of these vendors were

pursued for selling analogues of controlled substances as well as DXM.

 

2003 saw Texas and North Dakota vote against bills that would prohibit the

purchase 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 2 or more Dextromethorphan

containing products to a minor a criminal misdemeanor (Bill Summary - S06244).

This variation in States’ decision to restrict the availability of

Dextromethorphan from minors is a hotly contested federalist matter that

advocates of abuse prevention must keep in mind while formulating programs.

 

Safety

Most over-the-counter cough medicines contain other drugs besides

dextromethorphan and can be quite dangerous when taken in high doses.

 

These ingredients include acetaminophen, also known as paracetamol or APAP (very

high possibility of fatal liver damage with as few as eight

acetaminophen-containing pills) and chlorphenamine (a deleriant antihistamine

which can cause severe allergic reactions and death) contained in Coricidin

Cough and Cold. Coricidin should not be used recreationally: see the paragraph

on it below.

Some cough suppressants also often contain guaifenesin which contributes to the

nausea and vomiting that some experience when taking this drug.

 

Acetaminophen in particular deserves more detailed discussion. There are three

enzymatic pathways used in the liver to break it down, and the two typically

found are safe for the body. When these two become overwhelmed, the third

pathway processes acetaminophen into a chemical that is quite toxic to the

liver.

 

Fatal liver damage can occur before any symptoms become evident, causing a

painful, lingering death over several days to weeks; additionally, a user who is

in a hangover from significant quantities of DXM may not notice that anything is

wrong even once symptoms begin to occur. To put it simply,

acetaminophen-containing preparations are not safe for recreational use, and in

high recreational quantities death is the more probable outcome.

 

Liver toxicity can occur at doses as low as 8-10 pills, at the bottom of the

first plateau. Acetaminophen overdoses can be corrected without much permanent

harm as long as the individual gets to an emergency room within about eight

hours. After that, toxic effects become apparent.

 

Other preparations contain high doses of pseudoephedrine, a stimulant drug that

is very closely related to ephedrine. It is unwise for high doses of these drugs

to be purposefully used together because DXM gives stimulant effects itself.

 

High doses of pseudoephedrine can raise blood pressure to dangerous levels,

bringing with it the chance for a glaucoma crisis, heart attack, stroke, and

death.

 

Coricidin Cough and Cold (CCC) in particular is a typical source of DXM for

casual users, especially those in high school who may not have credit cards and

so cannot buy pure DXM from online merchants, and who see it as a preferable

alternative to large quantities of cough syrup. Many deaths or psychotic breaks

have resulted from recreational use of Coricidin in particular.

 

It contains a drug (chlorpheniramine maleate) that is broken down by the same

liver enzyme that decomposes DXM, and taking more than the recommended dose of

Coricidin Cough & Cold can be highly hazardous, especially to those individuals

with a CYP2D6 enzyme deficiency and those with a history of allergic reaction to

antihistamines, clorpheniramine in particular.

 

Also, some young users have taken to shoplifting CCC and similar preparations to

such an extent that some stores have either stopped selling them (making it less

available to legitimate users) or made them available only by request to the

pharmacist (making bulk purchases impossible). CCC is generally not regarded as

a safe source of DXM, especially in the ammount required to achieve an

upper-plateau trip.

 

Very large ammounts of CCC has caused many dozens of hospitalizations, and

several deaths, and the general advice is that for those who wish to use more

than 500 mg of DXM but cannot get it in pure form is to either not use DXM, or

use products (largely syrups) with no other active ingredients.

 

Dangers

There have been several dextromethorphan overdose deaths documented in medical

and media reports. Even when used alone, dextromethorphan overdoses have been

fatal.

 

It should be noted that the symptoms of upper second plateau and higher DXM use

are nearly impossible to conceal, and may be quite frightening, especially to

those who do not know that the user has used a drug; they are similar to a

temporary psychosis. At the fourth plateau the individual has little to no

connection with external reality, and may have extreme difficulty moving.

Most users find that use at or below the second plateau is more pleasant; the

two upper plateaus can be quite disturbing or frightening, and are largely used

for spiritual self-improvement. Psychotic breaks are more common in the upper

two plateaus.

 

While DXM has a truly horrific taste (in its pure form or extract, or as cough

syrup), and is not a safe drug if taken in any manner, it is considered

difficult to inject and is toxic to smoke. DXM HBr and the free base have very

high vaporization points, and if the user extracted the chemical from commercial

cough preparations, some of the inactives may have survived the extraction to

yield a very harsh, possibly toxic smoke. Either way, DXM HBr releases ammonia

and other toxins and should never be smoked.

 

Additionally, users should not inject DXM, since injection, even with sterile

equipment, can be quite hazardous in the hands of the inexperienced. One of the

problems with injecting DXM HBr is its marginal solubility in water compared to

other injected drugs. Due to this low solubility and high dose (into the gram

range, higher than almost every drug except alcohol), injection of DXM would

require injecting a large quantity of material — a good recipe for a sterile

abscess. Swallowing may not be pleasant, but it is the safest option.

 

William E. White published a paper on Usenet claiming that high doses of DXM may

cause brain damage in the form of NMDA antagonist neurotoxicity (NAN or Olney's

lesions). John Olney demonstrated that high doses of NMDA antagonists, the class

of drugs to which DXM belongs, caused brain cell death in animal studies.

 

The characteristic brain lesions produced are thus named Olney's lesions. The

doses required to instantly 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 Cliff Anderson in his paper

The Bad News Isn't In (http://www.erowid.org/chemicals/dxm/dxm_health2.shtml).

 

DXM should only be taken with extra caution and reading by those taking either

prescribed prescription or OTC medications, particularly antidepressants. The

reason is two-fold: with antidepressants there is risk of developing serotonin

syndrome, and many medications are either substrates or inhibitors of the liver

enzyme used in the metabolism of dextromethorphan. This has the effect of

minimizing hallucinations but maximizing confusion, and can cause the trip to

literally last for days. A first or second plateau trip is probably nothing to

worry about, though you may not enjoy all the effects your non-medicated friends

might.

 

Since DXM is legal, and a highly psychoactive dose can be purchased in bulk for

the cost of a box of cereal, it is often sold as MDMA (aka Ecstasy), a practice

that endangers users of MDMA.

 

While DXM significantly impairs judgement, and can confuse the user greatly, it

is not a common drug in date rape since it has an extremely bitter taste,

comparable only perhaps with milkweed sap. It would be nearly impossible to

conceal an incapacitating dose of DXM in food or drink, due to its unbelievably

bitter taste being noticeable in any food item.

 

See also

Dissociatives

Ketamine

Nitrous oxide

PCP

Federal Analogues Act of 1986

http://www.answers.com/topic/dextromethorphan

 

External links

The DXM Harm Reduction Project (http://www.dextromethorphan.ws/)

Coricidin (Dextromethorphan + Chlorpheniramine Maleate) Harm Reduction

(http://www.coricidin.org/), specifically about Coricidin.

The Third Plateau (http://www.third-plateau.org/) - harm reduction and community

site.

 

The Dextromethorphan FAQ (http://www.erowid.org/chemicals/dxm/faq/dxm_faq.shtml)

- the exhaustive FAQ on DXM by William White

The Vaults of Erowid (http://www.erowid.org/chemicals/dxm/)

The Dextroverse (http://www.dextroverse.org/)

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