Desert Pams, Palm Springs Drug Rehab: What is Ecstasy?
Ecstasy is the popular or “street” name for a substance identified chemically as methylenedioxy amphetamine or methylenedioxy-methamphetamine. The initial letters of the major portions of the latter name (Methylenedioxy-Methamphetamine) give rise to the acronym MDMA, by which this substance is commonly designated in the clinical and research literature. As the name implies, MDMA is a derivative of methamphetamine (known by such street names as “speed,” “crystal” and “meth” among others) and its parent compound amphetamine. A closely related compound, N-ethyl-methylene-dioxyamphetamine or MDEA, differs from MDMA only in having a 2-carbon ethyl group, rather than a 1-carbon methyl group, attached to the nitrogen atom of the amphetamine structure.
The name “ecstasy” is in fact used somewhat unselectively. In earlier years, the name was applied to methylenedioxyamphetamine (MDA). MDEA is also sometimes called ecstasy by its vendors and users, but is more often referred to as Eve. The compounds are closely similar in their chemistry and in their biological effects, so that the description of MDMA in the rest of this review also applies in the main to MDEA, and to a considerable extent to MDA.
Ecstasy differs from amphetamine and methamphetamine in one important respect. It has a methylenedioxy group attached to the aromatic ring of the amphetamine molecule. In this respect, it resembles the structure of the hallucinogenic material mescaline. As a result, the pharmacological effects of MDMA are a blend of those of the amphetamines and mescaline, as will be described in later sections of this review. This group of substances is frequently referred to as “designer drugs,” because, when illicit laboratories began to produce them for nonmedical use, the blend of amphetamine-like and mescaline-like effects was intentionally sought and could be achieved reliably by the appropriate design of the drug molecule. All of these substances resemble the natural neurotransmitters epinephrine (adrenaline), dopamine and most of their biological actions and effects resemble those of epinephrine, dopamine and serotonin.
The chemical name for ecstasy is methylenedioxymethamphetamine (MDMA). The chemical structure is similar to that of amphetamine (a stimulant) and mescaline (a hallucinogen). It is a street drug that is only made in illegal labs. It is usually sold as a tablet, capsule, or powder. The tablets vary in shape, size, color, and in the amount of ecstasy they contain. They may be stamped with a logo. This does not guarantee how pure the tablet is. Tablets may not have any ecstasy in them at all. They may contain cornstarch, soaps and detergents, or contain other drugs, such as: Caffeine, ephedrine, methamphetamine, LSD, PCP, ketamine Ecstasy combined with LSD is sometimes called “candy-flipping”
A product that is sold as “herbal ecstasy” does not contain MDMA. It usually has ephedrine in it. Ephedrine is a natural stimulant. Abuse of ephedrine-containing products has been associated with an increased risk of stroke, heart attack, and death.
Like the amphetamines, MDMA and its related compounds are amines that can exist either as free bases or as salts of various acids. The free bases are volatile and, indeed, amphetamine itself was first marketed in this form in an inhaler, for use as a nasal decongestant. Theoretically, MDMA and MDEA could also be used in this fashion, but the methylenedioxy group raises the boiling point of the free base so high that it is impossible to use it by sniffing the vapour. The salts, on the other hand, are not volatile but are quite soluble in water and can, therefore, be administered intravenously, orally or by “snorting” the powder. MDMA is almost always taken by mouth and is prepared as single-dose tablets for this purpose.
As sold illicitly in Europe and North America, MDMA is typically prepared in very professional-looking tablets stamped with a wide variety of symbols according to the whim or imagination of the maker (see illustration in Theune and colleagues). However, the actual composition of the tablets varies greatly, with respect to both the drug(s) contained in them and the amounts. Several different laboratories have analyzed street samples sold in their localities, and have found that the drug sold as “ecstasy” may be MDMA, MDEA, MDA, PMA (para-methoxyamphetamine), MBDB -methylenedioxy-phenyl-N-methylbutanamine), ephedrine or varying mixtures of these, though the great majority consist of a single active drug. The typical dosage range of MDMA for recreational use varies from 50 mg to 150 mg, but the amount per tablet in different batches of tablets may vary 70-fold or more, from almost zero to well over 100 mg.
The total amount consumed per occasion varies greatly among users. In Europe, North America and Australia, MDMA has been used primarily as a party drug rather than by solitary users. Its current popularity arises from its use at “raves,” the all-night dance parties at which it is taken to postpone fatigue and allow the user to dance energetically for hours on end. For this purpose, the most common dosage has been 1–2 tablets during the course of the party, but occasional case reports have indicated doses as high as 10 tablets in combination with other drugs, usually with toxic outcomes. In 2 fatal cases, the actual amount taken is uncertain because the victims ingested the drug unknowingly, their drinks having been “spiked” with it by friends playing a joke on them
MDMA is readily absorbed from the intestinal tract and reaches its peak concentration in the plasma about 2 hours after oral administration. Doses of 50 mg, 75 mg and 125 mg to healthy human volunteers produced peak blood concentrations of 106 ng/mL, 131 ng/mL and 236 ng/mL respectively. These concentrations are quite low, because the drug passes readily into the tissues, and much of it is bound to tissue constituents. It is helpful to remember these peak concentrations for comparison with the levels found in patients who have suffered the serious and sometimes fatal adverse effects described later in this review.
The drug is broken down metabolically, mainly in the liver, where an enzyme designated CYP2D6 is chiefly responsible. However, several different enzymes are involved in its degradation, and some of these appear to be saturated at relatively low concentrations of the drug. Consequently, as the dose is increased and the higher-affinity enzymes are saturated, disproportionately large increases in blood and brain concentrations of the drug occur. Therefore, small increases in dosage may carry the risk of large increases in toxicity.
Elimination of the drug from the body is moderately slow, the half-life for MDMA disappearance from the blood being of the order of 8 hours. Because it takes about 5 half-lives (i.e., about 40 hours for MDMA) for over 95% of the drug to be cleared from the body, this may explain the persistence of troublesome after-effects for one or 2 days after use. Some of the metabolites of MDMA are still pharmacologically active, especially its first metabolite, MDA, so that the duration of action may be somewhat longer than the duration of MDMA itself in the body.
The desired effects for which MDMA is used are closely similar to those that account for the continuing popularity of the other amphetamines. Physically, it produces a marked increase in wakefulness, endurance and sense of energy, sexual arousal, and postponement of fatigue and sleepiness. The accompanying psychological effects are described as a sense of euphoria, well-being, sharpened sensory perception, greater sociability, extraversion, heightened sense of closeness to other people, and greater tolerance of their views and feelings.
The latter effects have given rise to the claim that MDMA represents a distinct class of drugs designated “empathogens” or “entactogens” that may be of potential value as an aid in psychotherapy. Similar claims were made earlier for MDA, LSD and other hallucinogens but, despite claims of success in noncontrolled trials with MDA,1 no lasting benefit was found in a 10-year follow-up study of patients treated with LSD. No comparable study has been conducted on patients treated with MDMA, and the recent clinical literature contains almost no reference to its use in psychotherapy. However, it is not possible to say whether this is because of disappointment with the results, or because of difficulty obtaining the drug since its change in legal status
Like the amphetamines, MDMA also has adverse effects on many physical functions, even when taken in moderate doses for the recreational purposes described earlier. Because the basic action of the amphetamines involves increased arousal and alertness, it is usually accompanied by an increase in tension, which is manifested as muscular tension, jaw clenching, tooth grinding (bruxism) and constant restless movement of the legs. The increased muscle activity, together with a direct action of the drug on the thermoregulatory system in the brain, leads to an increase in body temperature. Stiffness and pain in the lower-back and limb muscles are very common complaints during the first 2–3 days after the use of MDMA. Headache, nausea, loss of appetite, blurred vision, dry mouth and insomnia are other commonly reported physical symptoms during the drug experience and immediately afterwards. Heart rate and blood pressure, which are usually elevated during the drug experience, tend to fluctuate more widely than normal during the following days.
Undesired psychological acute effects commonly reported during the drug experience similarly represent an exaggeration of the effects for which the drug is taken. The increased arousal, if carried to excess, is converted into hyperactivity, flight of ideas (with a resulting inability to focus one’s thoughts in a sustained and useful manner) and insomnia. Related complaints often include mild hallucinations, depersonalization (a feeling of separation of the self from the body), anxiety, agitation, and bizarre or reckless behaviour. Occasionally these symptoms lead to panic attacks, delirium or even brief psychotic episodes that usually (but not always) resolve rapidly when the drug action wears off. The day or 2 after drug use, the most common mental or mood complaints are difficulty concentrating, depression, anxiety and fatigue. These symptoms strongly resemble, in miniature, the “crash” that is typically seen as a withdrawal reaction after the prolonged euphoria or manic state produced by heavy use of amphetamine, cocaine or other central nervous system stimulants. Despite these complaints, the majority of users find the overall balance of the experience positive rather than negative but, with frequent repetition of the experience, the negative effects tend to become more prominent and the beneficial or pleasurable ones less so.
