Methaqualone
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| Systematic (IUPAC) name | |
| '2-methyl-3-o-tolyl-4(3H)-quinazolinone; 3,4-dihydro-2-methyl-4-oxo-3-o-tolylquinazoline; 2-methyl-3-(2-methylphenyl)-4-(3H)-quinazolinone |
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| Clinical data | |
| Pregnancy cat. | D (US) |
| Legal status | Prohibited (S9) (AU) Schedule III (CA) Schedule I (US) |
| Identifiers | |
| CAS number | 72-44-6  |
| ATC code | N05CM01 |
| PubChem | CID 6292 |
| DrugBank | DB04833 |
| ChemSpider | 6055 |
| UNII | 7ZKH8MQW6T |
| KEGG | D00557 |
| ChEMBL | CHEMBL282052 |
| Chemical data | |
| Formula | C16H14N2O |
| Mol. mass | 250.30 g/mol |
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| Physical data | |
| Melt. point | 113 °C (235 °F) |
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Methaqualone (meth-a-KWAY-lohn; brand name Quaalude pron.: /ˈkweɪluːd/ KWAY-lewd) is a sedative-hypnotic drug that is similar in effect to barbiturates, a general central nervous system depressant. The sedative-hypnotic activity was first noted by Indian researchers in the 1950s and in 1962 methaqualone itself was patented in the US by Wallace and Tiernan.[1] Its use peaked in the early 1970s as a hypnotic, for the treatment of insomnia, and as a sedative and muscle relaxant. It has also been used illegally as a recreational drug. Clandestinely produced methaqualone is seized by government agencies and police forces around the world.
Methaqualone was first synthesized in India in 1951 by Indra Kishore Kacker and Syed Hussain Zaheer,[2][3] and was soon introduced to Japanese and European consumers as a safe barbiturate substitute.[citation needed] 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, by Roussel Laboratories (now part of Sanofi-Aventis). In 1972 it was the sixth-bestselling sedative in the USA,[4] where it was legal under the brand name Quaalude.
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Uses [edit]
Medical [edit]
Methaqualone is a depressant that increases the activity of the GABA receptors in the brain and nervous system. When GABA activity is increased, blood pressure drops and the breathing and pulse rates slow, leading to a state of deep relaxation. These properties explain why methaqualone was originally mainly prescribed for insomnia,[5] most commonly in 300 mg dosage.
Methaqualone peaks in the bloodstream within several hours, its effects generally lasting four to eight hours. Regular users build up a physical tolerance, requiring larger doses for the same effect. Overdose can lead to nervous system shut down, coma and death.[6]
Methaqualone is not recommended for use while pregnant and is in pregnancy category D.[7] Methaqualone is available in Canada by prescription as a Schedule III drug[citation needed].
Recreational [edit]
Methaqualone became increasingly popular as a recreational drug in the late 1960s and early 1970s, known variously as 'ludes or sopers (also soapers) in the U.S. and mandrakes and mandies in Great Britain. The drug was sometimes used during sexual activity due to heightened sensitivity and lowered inhibition coupled with relaxation and euphoria.[citation needed]
The drug was often used by people who went dancing at glam rock clubs in the early 1970s and at discos in the late 1970s. (One slang term for Quaalude was disco biscuits.) In the mid-1970s there were bars in Manhattan called juice bars that only served non-alcoholic drinks that catered to people who liked to dance on methaqualone.[8]
Smoking methaqualone, either by itself or as an adulterant added to various legal and illegal smoking mixtures, gained popularity in the US among a few during the mid-1970s. Because the various binders and inert ingredients that were contained in the pill form were toxic when smoked, this practice was roundly decried by the medical community as a serious health risk. Smoking methaqualone pills can lead to emphysema and other chronic lung disorders, most notably talcosis.
The drug was more tightly regulated in Britain under the Misuse of Drugs Act 1971 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 1982 and made a Schedule I drug in 1984.
Gene Haislip, the former head of the Chemical Control Division of the Drug Enforcement Agency (DEA), told the PBS documentary program Frontline: "We beat 'em." By working with governments and manufacturers around the world, the DEA was able to halt production and, Haislip says, "eliminated the problem".[9][10][11]
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 714s, "Lemmons", or "Lemmon 7s". Methaqualone was also manufactured in the USA 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 continued illegal manufacture of methaqualone all through the 1980s, continuing the use of the "714" stamp, until their popularity waned in the early 1990s. Bristol Myers manufactured this drug until taken out of the market in 1982 as well.[citation needed]
Methaqualone is one of the most commonly used drugs in South Africa.[12][13] Commonly known as Mandrax, M-pills, buttons, or smarties, it is not taken orally but is crushed and mixed in a pipe with cannabis. The drug's price of R90[citation needed] (about US$8) together with readily available cheap, low-grade marijuana, makes methaqualone one of the preferred hard drugs of the lower-income, mid and upper sections of South African society.[12]
Effects [edit]
Effects can include euphoria, drowsiness, reduced heart rate, reduced respiration, increased sexual arousal (aphrodisia), and paresthesias (numbness of the fingers and toes). Larger doses can bring about respiratory depression, slurred speech, headache, and photophobia (a symptom of excessive sensitivity to light).
Overdose [edit]
An overdose can cause delirium, convulsions, hypertonia, hyperreflexia, vomiting, renal failure, coma, and death through cardiac or respiratory arrest. It resembles barbiturate poisoning, but with increased motor difficulties and a lower incidence of cardiac or respiratory depression. Toxicity is treated with diazepam and sometimes other anticonvulsants.[citation needed]
Drug testing [edit]
Urine drug test of gas-liquid chromatography (GLC) confirmation up to 72 hours after the last intake is a practical way of detecting methaqualone use in individuals.[14]
To avoid a false positive Substance Abuse and Mental Health Services Administration (SAMHSA) determined the initial cut off level of 300 ng/ml for forensic and workplace drug testing of methaqualone. Only after the confirmatory test of 200 ng/ml will a person be considered positive and possibly face penalties or workplace disciplinary action.[15] As reported by Quest Diagnostics in 2011, methaqualone had a 0% positive drug testing rate in the US, making it one of the least abused drugs in that year.[16]
See also [edit]
- Methaqualone in popular culture
- Cloroqualone
- Diproqualone
- Etaqualone
- Mebroqualone
- Mecloqualone
- Methylmethaqualone
References [edit]
- ^ US Patent 3135659 - Hydroxy and Alkoxy Aryl Quinazolones
- ^ p. 142, A survey of reported synthesis of methaqualone and some positional and structural isomers, Etienne F. van Zyl, Forensic Science International 122, #2-3 (1 November 2001), pp. 142–149, doi:10.1016/S0379-0738(01)00484-4.
- ^ Potential Analgesics. Part I. Synthesis of substituted 4-quinazolones, I. K. Kacker and S. H. Zaheer, J. Ind. Chem. Soc. 28 (1951), pp. 344–346.
- ^ GC/MS Assays for Abused Drugs in Body fluids, p. 39
- ^ "methaqualone reference". Enotes.
- ^ "recreational drugs tranquilizers". drug library eu.
- ^ Drug Safety. "Methaqualone in Pregnancy and Breastfeeding". Retrieved 15 August 2012.
- ^ Lawrence Young (31). "METHAQUALONE". Drug Text. International Substance Use Library. Retrieved 27 July 2012.
- ^ "The Meth Epidemic – Haislip discusses parallels to current Methamphetamine epidemic".
- ^ Ferns, Sean, "Lecture: Gene Haislip : The Chemical Connection: A Historical Perspective on Chemical Control", Drug Enforcement Administration Museum Lecture Series, Arlington, Virginia, October 25, 2007
- ^ Piccini, Sara, "DRUG WARRIOR: THE DEA’S GENE HAISLIP ’60, B.C.L. ’63 BATTLED WORLDWIDE AGAINST THE ILLEGAL DRUG TRADE — AND SCORED A RARE VICTORY", William & Mary Alumni Magazine, The College of William & Mary, Spring 2010
- ^ a b "Mandrax". DrugAware. Reality Media. 2003. Retrieved 2009-08-13.
- ^ McCarthy G, Myers B, Siegfried N. Treatment for methaqualone dependence in adults. Cochrane Database of Systematic Reviews. 2005 Apr 18;(2):CD004146. PMID 15846700
- ^ "methaqualone drug testing". National Institute of Health.
- ^ "methaqualone drug testing". Testcountry.
- ^ "workplace drug test positive rates". quest diagnostics.
External links [edit]
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