Methaqualone
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Methaqualone is a
hypnotic Hypnotic (from Greek ''Hypnos'', sleep), or soporific drugs, commonly known as sleeping pills, are a class of (and umbrella term for) psychoactive drugs whose primary function is to induce sleep (or surgical anesthesiaWhen used in anesthesia ...
sedative A sedative or tranquilliser is a substance that induces sedation by reducing irritability or excitement. They are CNS depressants and interact with brain activity causing its deceleration. Various kinds of sedatives can be distinguished, but ...
. It was sold under the brand names Quaalude ( ) and Sopor among others, which contained 300 mg of methaqualone, and sold as a combination drug under the brand name Mandrax, which contained 250 mg methaqualone and 25 mg
diphenhydramine Diphenhydramine (DPH) is an antihistamine and sedative mainly used to treat allergies, insomnia, and symptoms of the common cold. It is also less commonly used for tremor in parkinsonism, and nausea. It is taken by mouth, injected into ...
within the same tablet, mostly in Europe. Commercial production of methaqualone was halted in the mid-1980s due to widespread abuse and addictiveness. It is a member of the quinazolinone class. The sedative–hypnotic activity of methaqualone was first noted in 1955. In 1962, methaqualone was patented in the United States by Wallace and Tiernan. Its use peaked in the early 1970s for the treatment of
insomnia Insomnia, also known as sleeplessness, is a sleep disorder in which people have trouble sleeping. They may have difficulty falling asleep, or staying asleep as long as desired. Insomnia is typically followed by daytime sleepiness, low energy, ...
, and as a sedative and
muscle relaxant A muscle relaxant is a drug that affects skeletal muscle function and decreases the muscle tone. It may be used to alleviate symptoms such as muscle spasms, pain, and hyperreflexia. The term "muscle relaxant" is used to refer to two major therap ...
. Methaqualone became increasingly popular as a
recreational drug Recreational drug use indicates the use of one or more psychoactive drugs to induce an altered state of consciousness either for pleasure or for some other casual purpose or pastime by modifying the perceptions and emotions of the user. When a ...
and
club drug Club drugs, also called rave drugs or party drugs, are a loosely defined category of recreational drugs which are associated with discothèques in the 1970s and nightclubs, dance clubs, electronic dance music (EDM) parties, and raves in the ...
in the late 1960s and 1970s, known variously as "ludes" or "disco biscuits" due to its widespread use during the popularity of
disco Disco is a genre of dance music and a subculture that emerged in the 1970s from the United States' urban nightlife scene. Its sound is typified by four-on-the-floor beats, syncopated basslines, string sections, brass and horns, electric p ...
in the 1970s, or "sopers" (also "soaps") in the United States and Canada, and "mandrakes" and "mandies" in the United Kingdom, Australia and New Zealand. The substance was sold both as a free base and as a salt (hydrochloride). This use means the drug is controlled in most countries, and is so under Schedule II of the United Nations Convention on Psychotropic Substances.


Medical use

Methaqualone is a sedative that increases the activity of the
GABA receptor The GABA receptors are a class of receptors that respond to the neurotransmitter gamma-aminobutyric acid (GABA), the chief inhibitory compound in the mature vertebrate central nervous system. There are two classes of GABA receptors: GABAA and ...
s in the brain and nervous system, similarly to
benzodiazepine Benzodiazepines (BZD, BDZ, BZs), sometimes called "benzos", are a class of depressant drugs whose core chemical structure is the fusion of a benzene ring and a diazepine ring. They are prescribed to treat conditions such as anxiety disorders, ...
s and
barbiturate Barbiturates are a class of depressant drugs that are chemically derived from barbituric acid. They are effective when used medically as anxiolytics, hypnotics, and anticonvulsants, but have physical and psychological addiction potential a ...
s. When GABA activity is increased, blood pressure drops and breathing and pulse rates slow, leading to a state of deep relaxation. These properties explain why methaqualone was originally mainly prescribed for insomnia. Methaqualone was not recommended for use while pregnant and is in
pregnancy category D The pregnancy category of a medication is an assessment of the risk of fetal injury due to the pharmaceutical, if it is used as directed by the mother during pregnancy. It does ''not'' include any risks conferred by pharmaceutical agents or thei ...
.


Overdose

An overdose can lead to nervous system shutdown,
coma A coma is a deep state of prolonged unconsciousness in which a person cannot be awakened, fails to respond normally to painful stimuli, light, or sound, lacks a normal wake-sleep cycle and does not initiate voluntary actions. Coma patients exhi ...
and
death Death is the irreversible cessation of all biological functions that sustain an organism. For organisms with a brain, death can also be defined as the irreversible cessation of functioning of the whole brain, including brainstem, and brain ...
. Additional effects are
delirium Delirium (also known as acute confusional state) is an organically caused decline from a previous baseline of mental function that develops over a short period of time, typically hours to days. Delirium is a syndrome encompassing disturbances ...
,
convulsion A convulsion is a medical condition where the body muscles contract and relax rapidly and repeatedly, resulting in uncontrolled shaking. Because epileptic seizures typically include convulsions, the term ''convulsion'' is sometimes used as a ...
s, hypertonia, hyperreflexia,
vomiting Vomiting (also known as emesis and throwing up) is the involuntary, forceful expulsion of the contents of one's stomach through the mouth and sometimes the nose. Vomiting can be the result of ailments like food poisoning, gastroenter ...
,
kidney failure Kidney failure, also known as end-stage kidney disease, is a medical condition in which the kidneys can no longer adequately filter waste products from the blood, functioning at less than 15% of normal levels. Kidney failure is classified as eit ...
, coma, and death through
cardiac The heart is a muscular organ in most animals. This organ pumps blood through the blood vessels of the circulatory system. The pumped blood carries oxygen and nutrients to the body, while carrying metabolic waste such as carbon dioxide to t ...
or
respiratory arrest Respiratory arrest is a sickness caused by apnea (cessation of breathing) or respiratory dysfunction severe enough it will not sustain the body (such as agonal breathing). Prolonged apnea refers to a patient who has stopped breathing for a long pe ...
. It resembles barbiturate poisoning, but with increased motor difficulties and a lower incidence of cardiac or respiratory depression. The standard single tablet adult dose of Quaalude brand of methaqualone was 300 mg when made by Lemmon. A dose of 8000 mg is lethal and a dose as little as 2000 mg could induce a coma if taken with an
alcoholic beverage An alcoholic beverage (also called an alcoholic drink, adult beverage, or a drink) is a drink that contains ethanol, a type of Alcohol (chemistry), alcohol that acts Alcohol (drug), as a drug and is produced by Ethanol fermentation, fermentat ...
.


Pharmacology

Methaqualone peaks in the bloodstream within several hours, with a half-life of 20–60 hours. While the salt methaqualone hydrochloride is typically used clinically, methaqualone free-base was also marketed, namely as the methaqualone component of Mandrax, a combination drug which contained 250 mg methaqualone and 25 mg
diphenhydramine Diphenhydramine (DPH) is an antihistamine and sedative mainly used to treat allergies, insomnia, and symptoms of the common cold. It is also less commonly used for tremor in parkinsonism, and nausea. It is taken by mouth, injected into ...
within the same tablet. Oral dosage forms of methaqualone hydrochloride were manufactured as capsules, whereas oral dosage forms of methaqualone free-base were manufactured as tablets. Regular users build up a physical tolerance, requiring larger doses for the same effect.


History

Methaqualone was first synthesized in India in 1951 by Indra Kishore Kacker and
Syed Husain Zaheer Syed Husain Zaheer was an Indian chemist, politician and the director general of the Council of Scientific and Industrial Research (CSIR), the largest research and development organisation in India. Prior to taking up the directorship of CSIR, H ...
, who were conducting research on finding new antimalarial medications. By 1965, it was the most commonly prescribed sedative in Britain, where it has been sold legally under the names Malsed, Malsedin, and Renoval. In 1965, a methaqualone/antihistamine combination was sold as the sedative drug Mandrax in Europe, by Roussel Laboratories (now part of Sanofi S.A.). In 1972, it was the sixth-bestselling sedative in the US, where it was legal under the
brand name A brand is a name, term, design, symbol or any other feature that distinguishes one seller's good or service from those of other sellers. Brands are used in business, marketing, and advertising for recognition and, importantly, to create an ...
Quaalude. Quaalude in the United States was originally manufactured in 1965 by the
Fort Washington, Pennsylvania Fort Washington is a census-designated place and suburb of Philadelphia in Montgomery County, Pennsylvania, United States. The population was 5,446 at the 2010 census. History Prior to the Revolutionary War the Fort Washington area was settl ...
, based pharmaceutical firm William H. Rorer, Inc. The drug name "Quaalude" is a
portmanteau A portmanteau word, or portmanteau (, ) is a blend of wordsMaalox. In 1978, Rorer sold the rights to manufacture Quaalude to the Lemmon Company of
Sellersville, Pennsylvania Sellersville is a borough in Bucks County, Pennsylvania. The population was 4,249 at the 2010 census. It is in the Pennridge School District. History Sellersville was founded in the early 18th century. It was centered on a major road known as ...
. At that time, Rorer chairman John Eckman commented on Quaalude's bad reputation stemming from illegal manufacture and use of methaqualone, and illegal sale and use of legally prescribed Quaalude: "Quaalude accounted for less than 2% of our sales, but created 98% of our headaches." Both companies still regarded Quaalude as an excellent sleeping drug. Lemmon, well aware of Quaalude's public image problems, used advertisements in medical journals to urge physicians "not to permit the abuses of illegal users to deprive a legitimate patient of the drug". Lemmon also marketed a small quantity under another name, Mequin, so doctors could prescribe the drug without the negative connotations. The rights to Quaalude were held by the JB Roerig & Company division of
Pfizer Pfizer Inc. ( ) is an American multinational pharmaceutical and biotechnology corporation headquartered on 42nd Street in Manhattan, New York City. The company was established in 1849 in New York by two German entrepreneurs, Charles Pfize ...
, before the drug was discontinued in the United States in 1985, mainly due to its psychological addictiveness, widespread abuse, and illegal recreational use.


Society and culture


Brand names

It was sold under the brand name Quaalude and sometimes stylized "Quāālude" in the
United States The United States of America (U.S.A. or USA), commonly known as the United States (U.S. or US) or America, is a country Continental United States, primarily located in North America. It consists of 50 U.S. state, states, a Washington, D.C., ...
and
Canada Canada is a country in North America. Its ten provinces and three territories extend from the Atlantic Ocean to the Pacific Ocean and northward into the Arctic Ocean, covering over , making it the world's second-largest country by to ...
, and Mandrax in the UK,
South Africa South Africa, officially the Republic of South Africa (RSA), is the southernmost country in Africa. It is bounded to the south by of coastline that stretch along the South Atlantic and Indian Oceans; to the north by the neighbouring coun ...
, and
Australia Australia, officially the Commonwealth of Australia, is a sovereign country comprising the mainland of the Australian continent, the island of Tasmania, and numerous smaller islands. With an area of , Australia is the largest country by ...
.


Regulation

Methaqualone was initially placed in Schedule I as defined by the UN
Convention on Psychotropic Substances The Convention on Psychotropic Substances of 1971 is a United Nations treaty designed to control psychoactive drugs such as amphetamine-type stimulants, barbiturates, benzodiazepines, and psychedelics signed in Vienna, Austria on 21 February ...
, but was moved to Schedule II in 1979. In Canada, methaqualone is listed in Schedule III of the
Controlled Drugs and Substances Act The ''Controlled Drugs and Substances Act'' (french: Loi réglementant certaines drogues et autres substances) (the ''Act'') is Canada's federal drug control statute. Passed in 1996 under Prime Minister Jean Chrétien's government, it repeal ...
and requires a prescription, but it is no longer manufactured. Methaqualone is banned in India. In the United States it was withdrawn from the market in 1983 and made a Schedule I drug in 1984.


Recreational

Methaqualone became increasingly popular as a recreational drug in the late 1960s and 1970s, known variously as "ludes" or "sopers" (also "soaps") in the United States and "mandrakes" and "mandies" in the UK, Australia and New Zealand. ''Sopor'' is a Latin word for sleep. The drug was more tightly regulated in Britain under the
Misuse of Drugs Act 1971 The Misuse of Drugs Act 1971 is an Act of the Parliament of the United Kingdom. It represents action in line with treaty commitments under the Single Convention on Narcotic Drugs, the Convention on Psychotropic Substances, and the United Nati ...
and in the U.S. from 1973. It was withdrawn from many developed markets in the early 1980s. In the United States it was withdrawn in 1983 and made a Schedule I drug in 1984. It has a DEA ACSCN of 2565 and in 2022 the aggregate annual manufacturing quota for the United States was 60 grams. Mention of its possible use in some types of cancer and AIDS treatments has periodically appeared in the literature since the late 1980s. Research does not appear to have reached an advanced stage. The DEA has also added the methaqualone analogue mecloqualone (also a result of some incomplete clandestine syntheses) to Schedule I as ACSCN 2572, with a manufacturing quota of 30 g. Gene Haislip, the former head of the Chemical Control Division of the Drug Enforcement Administration (DEA), told the PBS documentary program ''
Frontline Front line refers to the forward-most forces on a battlefield. Front line, front lines or variants may also refer to: Books and publications * ''Front Lines'' (novel), young adult historical novel by American author Michael Grant * ''Frontlines ...
'', "We beat 'em." By working with governments and manufacturers around the world, the DEA was able to halt production and, Haislip said, "eliminated the problem". Methaqualone was manufactured in the United States under the name Quaalude by the pharmaceutical firms Rorer and Lemmon with the numbers 714 stamped on the tablet, so people often referred to Quaalude as 714's, "Lemmons", or "Lemmon 7's". Methaqualone was also manufactured in the US under the trade names Sopor and Parest. After the legal manufacture of the drug ended in the United States in 1982, underground laboratories in
Mexico Mexico (Spanish language, Spanish: México), officially the United Mexican States, is a List of sovereign states, country in the southern portion of North America. It is borders of Mexico, bordered to the north by the United States; to the so ...
continued the illegal manufacture of methaqualone throughout the 1980s, continuing the use of the "714" stamp, until their popularity waned in the early 1990s. Drugs purported to be methaqualone are in a significant majority of cases found to be inert, or contain diphenhydramine or benzodiazepines. Illicit methaqualone is one of the most commonly used recreational drugs in
South Africa South Africa, officially the Republic of South Africa (RSA), is the southernmost country in Africa. It is bounded to the south by of coastline that stretch along the South Atlantic and Indian Oceans; to the north by the neighbouring coun ...
. Manufactured clandestinely, often in India, it comes in tablet form, but is smoked with marijuana. This method of ingestion is known as "white pipe". It is popular elsewhere in Africa and in India.


Chemical weapon – Project Coast

Illegal efforts to weaponize methaqualone have occurred. During the 1980s, the
apartheid Apartheid (, especially South African English: , ; , "aparthood") was a system of institutionalised racial segregation that existed in South Africa and South West Africa (now Namibia) from 1948 to the early 1990s. Apartheid was ...
regime in South Africa ordered the covert manufacture of a large amount of methaqualone at the front company
Delta G Scientific Company Delta G Scientific Company was originally a front company established April 1982 in Weldegraan, Pretoria by the South African Defence Force to research and produce chemical weapons within a covert operation known as Project Coast. Medchem Conso ...
, as part of a then-secret chemical weapons programme known as
Project Coast Project Coast was a 1980s top-secret chemical and biological weapons (CBW) program instituted by the apartheid-era government of South Africa. Project Coast was the successor to a limited postwar CBW program, which mainly produced the lethal age ...
. Methaqualone was given the codename ''MosRefCat'' (Mossgas Refinery Catalyst). Details of this activity came to light during the 1998 hearings of the post-apartheid Truth and Reconciliation Commission.


See also

*
Bill Cosby sexual assault cases It emerged in late 2014 that Bill Cosby, an American media personality, sexually assaulted dozens of women throughout his career. Cosby made significant contributions to American and African-American culture, and is well known in the United State ...
* Drug-facilitated sexual assault * ''The Wolf of Wall Street'' (2013 film)


References


Further reading

*


External links


Erowid Vault – Methaqualone (Quaaludes)
{{Authority control GABAA receptor positive allosteric modulators Quinazolinones Sedatives Hypnotics Amidines Withdrawn drugs