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The principal chemical component of ecstasy is MDMA, or 3,4-methylenedioxymethamphetamine. MDMA is a phenethylamine related structurally to amphetamines and mescaline. Having been isolated and experimented with at least a decade previously, MDMA was first described and prepared for patent submission in December 1912. Its patent was issued two years later in Germany to E. Merck Pharmaceuticals. Once manufactured mostly in the laboratories of Holland and Belgium, ecstasy is now also made in the United States, Canada, Germany, Mexico, Brazil, east Asia, and southeast Asia, and is sometimes laced with methamphetamine or other substances. In its pure forms, MDMA's effects combine the loss of inhibitions of alcohol, the auditory intensification of marijuana, the hallucinogenic effects of mild LSD, and the sleep-defying, energy-boosting effects of amphetamines. Because of the somatic and psychological effects it induces, MDMA has been dubbed an “entactogen,” which means “to touch within” in Greek.

In the 1960s and 1970s, psychiatrists, clinicians and users had called MDMA “Adam,” “Empathy,” and “penicillin for the soul.” By the 1980s and 1990s it was called “E,” “X,” and “XTC,” before “ecstasy” was settled upon. Since then, locally specific terms for ecstasy have proliferated as the manufacturing process has been broken into constituent parts and expanded into several countries. Ecstasy tablets are now generally the size of aspirin tablets and come in a variety of shapes and colors, most of them being imprinted with likenesses of butterflies, hearts, doves, arrows, birds, Playboy bunnies, automobiles, Hollywood movies, and cartoon superheroes.

In the late 1970s and early 1980s the Berkeley chemist Alexander Shulgin recorded the results of his and others’ experimentation with MDMA and helped popularize the drug. Medical doctors, psychiatrists, and interested onlookers also occasionally used MDMA to treat clinical symptoms and syndromes including suicidal thoughts, clinical depression, phobias, post-traumatic stress disorder (PTSD), and drug addiction. A leading proponent of the clinical psychological use of MDMA is the South Carolina-based Dr. Michael Mithoefer. In 2001 the U.S. Food and Drug Administration approved his research protocol that proposed to enroll 20 American women who had suffered sexual violence and to provide MDMA and nondrug psychotherapy to 12 women and a placebo and nondrug psychotherapy to another eight. However, it took until 2004 before an Institutional Review Board would sanction his study. From 2004 to 2008, and alongside his psychiatric nurse wife Linda Mithoefer and other colleagues, he carried out this study. They found a high rate of clinical response (10/12, 83 percent) in those who received preparatory nondrug psychotherapy, two eight-hour experimental sessions of MDMA and then follow-up, nondrug psychotherapy, compared with those who received no MDMA (2/8, 25 percent). Study participants experienced no serious adverse events, no significant increases in blood pressure, and no neurocognitive side effects. Having been funded by the Multidisciplinary Association for Psychedelic Studies (MAPS), the Mithoefers have since enrolled 16 military service veterans (male and female) who have been diagnosed with PTSD in the past decade.

The amount of ecstasy in the average tablet, which is likely adulterated with other chemicals, is about 70–100 milligrams.

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MDMA was experimented with in a number of clinical settings until 1985, when it was classified a Schedule I drug (classed with LSD, cocaine, and heroin as warranting no medical use thereof) after lengthy and acrimonious legal debate. Its eventual illegality has greatly restricted its manufacture and use, but has also changed its cultural status, led to rising prices and wholesale rearrangements in its manufacturing and distribution and perhaps to its growing abuse. Increases in ecstasy use occurred throughout the 1990s in the wake of social movements, the arrival and spread of human immunodeficiency virus and acquired immune deficiency syndrome (HIV and AIDS), technological innovations, accelerated travel, and political developments. Seeming declines in ecstasy use in the United States began to occur at the turn of the millennium and were for several years reported widely. Globally, fewer than one percent of the population between the ages of 16 and 65 use ecstasy; however, rates of use appear to be increasing. Based on United Nations data, Australia has the highest rates of use, with approximately 4 percent of the adult population using ecstasy annually. Additionally, ethnographic, clinical and other evidence suggests that there has been an upsurge in use in the United States since then and that it has spread into new groups, including African American and Hispanic youth. General Population Surveys (GPS) conducted throughout Europe support contentions that ecstasy use has stabilized, perhaps even declined. Nearly 6 percent of young Europeans claim ever to have used it, and 1.7 percent reported having used it in the past year. Only in Sweden and Finland do females report greater use than males. In the United States, estimates of prevalence of use made by the Monitoring the Future surveys suggest declining use but perhaps also sharply declining perceptions of risks of its use between 2008 and 2009. The National Survey on Drug Use and Health reported a steep increase from 2005 to 2008 in first-use, engaged in by 615,000 Americans in the former year but 894,000 American in the latter.

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