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Methaqualone: Difference between revisions

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{{Short description|Sedative–hypnotic drug withdrawn due to recreational abuse}}
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== Medical use ==
Methaqualone primarily acts as a sedative, relieving anxiety and promoting sleep. Methaqualone binds to [[GABAA receptor|GABA-A receptors]], and it shows negligible affinity for a wide array of other potential targets, including other receptors and [[neurotransmitter transporter]]s.<ref name="Hammer-2015">{{cite journal | vauthors = Hammer H, Bader BM, Ehnert C, Bundgaard C, Bunch L, Hoestgaard-Jensen K, Schroeder OH, Bastlund JF, Gramowski-Voß A, Jensen AA | title = A Multifaceted GABAA Receptor Modulator: Functional Properties and Mechanism of Action of the Sedative-Hypnotic and Recreational Drug Methaqualone (Quaalude) | journal = Molecular Pharmacology | volume = 88 | issue = 2 | pages = 401–420 | date = August 2015 | pmid = 26056160 | pmc = 4518083 | doi = 10.1124/mol.115.099291 }}</ref> Methaqualone is a positive [[allosteric modulator]] at many subtypes of GABA-A receptor, similar to classical [[benzodiazepine]]s such as [[diazepam]]. GABA-A receptors are inhibitory, so methaqualone tends to inhibit action potentials, similar to GABA itself or other GABA-A agonists. Unlike most benzodiazepines, methaqualone acts as a negative allosteric modulator at a few GABA-A receptor subtypes, which tends to cause an excitatory response in neurons expressing those receptors. Because methaqualone can be either excitatory or inhibitory depending on the subunit composition of the GABA-A receptor, it can be characterized as a mixed GABA-A receptor modulator.<ref name="Hammer-2015" /> The methaqualone binding site is distinct from the [[benzodiazepine]], [[barbiturate]], and [[neurosteroid]] binding sites on the GABA-A receptor complex, and it may partially overlap with the [[etomidate]] binding site.<ref name="Hammer-2015" />
Methaqualone is a sedative that increases the activity of the [[GABA receptor]]s in the brain and nervous system, similarly to [[benzodiazepine]]s and [[barbiturate]]s.{{citation needed |date=May 2024}} When GABA activity is increased, it leads to a state of relaxation, anxiety relief, and sleep.<ref>{{Cite web | title = Methaqualone reference |url=http://www.enotes.com/methaqualone-reference/methaqualone |publisher=Enotes |url-status=dead |archive-url=https://web.archive.org/web/20120223014958/http://www.enotes.com/methaqualone-reference/methaqualone |archive-date=February 23, 2012}}</ref>
 
Methaqualone was not recommended for use while pregnant and is in [[pregnancy category#United States|pregnancy category D]].<ref>{{Cite web| work = TheDrugSafety.com |title=Methaqualone in Pregnancy and Breastfeeding|url=http://thedrugsafety.com/methaqualone/|access-date=15 August 2012|archive-url=https://web.archive.org/web/20121002101854/http://thedrugsafety.com/methaqualone/|archive-date=2012-10-02|url-status=dead}}</ref>
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== Pharmacology ==
Methaqualone peaks in the bloodstream within several hours, with a half-life of 20–60 hours. It has a diverse mechanism of action and mainly acts as a [[GABAA receptor|GABA<sub>A</sub> receptor]] modulator, leading to increased inhibitory transmission and downstream sedative effects via [[Allosteric modulator|allosteric modulation]] and [[Receptor agonism|agonism]] of several GABA<sub>A</sub>R subtypes.<ref>{{cite journal | vauthors name= "Hammer H, Bader BM, Ehnert C, Bundgaard C, Bunch L, Hoestgaard-Jensen K, Schroeder OH, Bastlund JF, Gramowski-Voß A, Jensen AA | display-authors = 6 | title = A Multifaceted GABAA Receptor Modulator: Functional Properties and Mechanism of Action of the Sedative-Hypnotic and Recreational Drug Methaqualone (Quaalude) | journal = Molecular Pharmacology | volume = 88 | issue = 2 | pages = 401–420 | date = August 2015" | pmid = 26056160 | pmc = 4518083 | doi = 10.1124/mol.115.099291 }}</ref>
 
Similar to other [[GABAergic]] agents, methaqualone will produce tolerance and physical dependence with extended periods of use.<ref>{{cite journal | vauthors = Suzuki T, Koike Y, Chida Y, Misawa M | title = Cross-physical dependence of several drugs in methaqualone-dependent rats | journal = Japanese Journal of Pharmacology | volume = 46 | issue = 4 | pages = 403–410 | date = April 1988 | pmid = 3404770 | doi = 10.1254/jjp.46.403 | doi-access = free }}</ref>
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== Society and culture ==
=== Brand names ===
It was sold under the brand name Quaalude and (sometimes stylized "Quāālude" in the [[United States]] and [[Canada]]),<ref>{{Cite book | vauthors = Rile K |title=Winter Music |date=1983 |publisher=Little, Brown and Company |location=Boston and Toronto |isbn=978-0-316-74657-1 |pages=[https://archive.org/details/wintermusic00rile/page/41 41, 59] |edition=First |url-access=registration |url=https://archive.org/details/wintermusic00rile/page/41 }}</ref> and Mandrax in the [[United Kingdom|UK]], [[South Africa]], and [[Australia]].
 
=== Regulation ===
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=== Sexual assault ===
{{Main|Drug-facilitated sexual assault}}
Actor [[Bill Cosby]] admitted in a 2015 civil deposition to giving Quaaludemethaqualone to women who took them of their own choice before [[Bill Cosby sexual assault cases|engagingallegedly insexually sexual activity withassaulting them]].<ref>{{Cite news | vauthors = Bowley G, Ember S |date=2015-07-19 |title=Bill Cosby, in Deposition, Said Drugs and Fame Helped Him Seduce Women |language=en-US |work=The New York Times |url=https://www.nytimes.com/2015/07/19/arts/bill-cosby-deposition-reveals-calculated-pursuit-of-young-women-using-fame-drugs-and-deceit.html |access-date=2023-01-24 |issn=0362-4331}}</ref><ref>{{Cite news | vauthors = Bowley G, Somaiya R |date=2015-07-07 |title=Bill Cosby Admission About Quaaludes Offers Accusers Vindication |language=en-US |work=The New York Times |url=https://www.nytimes.com/2015/07/08/business/bill-cosby-said-in-2005-he-obtained-drugs-to-give-to-women.html |access-date=2023-01-24 |issn=0362-4331}}</ref> Film director [[Roman Polanski]], awas filmconvicted director,in was accused1977 of administeringsexually Quaalude toassaulting a 13-year-old girl beforeafter sexually assaultinggiving her alcohol and methaqualone.<ref>{{Cite web |date=2018-01-30 |title=What does Hollywood's reverence for child rapist Roman Polanski tell us? |url=http://www.theguardian.com/film/2018/jan/30/hollywood-reverence-child-rapist-roman-polanski-convicted-40-years-on-run |access-date=2023-01-24 |website=the Guardian |language=en}}</ref>
 
=== Popular culture ===
Quaaludes are mentioned in the 1983 film ''[[Scarface (1983 film)|Scarface]]'', when
Al Pacino's character Tony Montana says, "Another quaalude... she'll love me again."
Quaaludes are also referenced extensively in the 2013 film [[The Wolf of Wall Street (2013 film)|''The Wolf of Wall Street'']].<ref>{{Cite web | vauthors = Loughrey C | date = 18 September 2017 |title=Jordan Belfort had to teach Leonardo DiCaprio how to look like he was on drugs for Wolf of Wall Street |url=https://www.independent.co.uk/arts-entertainment/films/news/wolf-of-wall-street-leonardo-dicaprio-jordan-belfort-look-like-on-drugs-for-movie-quualudes-a7952646.html |access-date= 24 January 2023 |website=The Independent |language=en}}</ref> Many songs also refer to quaaludes, including the following: [[David Bowie]]'s "[[Time (David Bowie song)|Time]]" ("Time, in quaaludes and red wine") and "[[Rebel Rebel]]" ("You got your cue line/And a handful of 'ludes"); "Cosmic Doo Doo" by the American [[country music]] singer-songwriter [[Blaze Foley]] ("Got some quaaludes in their purse"); "[[That Smell]]" by [[Lynyrd Skynyrd]] ("Can't speak a word when you're full of 'ludes"); "[[Flakes]]" by [[Frank Zappa]] ("(Wanna buy some mandies, Bob?)"); "[[Straight Edge (song)|Straight Edge]]" by [[Minor Threat]] ("Laugh at the thought of eating ludes"); and "Kind of Girl" by [[French Montana]] ("That high got me feelin' like the Quaaludes from ''Wolf of Wall Street''"). It is also used by Patrick Melrose in Edward St Aubyn's 1992 novel "Bad News".{{cn|date=May 2024}}
 
Parody [[glam rock]]er "Quay Lewd", one of the costumed performance personae used by [[The Tubes|Tubes]] singer [[Fee Waybill]], was named after the drug.
 
[[Law & Order: Special Victims Unit (season 18)|Season 18]] of ''[[Law & Order: Special Victims Unit]]'' addresses Quaalude administration as a [[date rape drug]] in episode 9, "Decline and Fall", which aired January 18, 2017.<ref>{{Cite web|url=https://www.christiantimes.com/trends/law-order-svu-season-18-episode-9-spoilers-bob-gunton-guest-stars-as-billionaire-rapist.html|title='Law & Order: SVU' season 18 episode 9 spoilers: Bob Gunton guest stars as billionaire rapist|website=The Christian Times|author=Janna Dela Cruz|language=en|date=January 15, 2017|access-date=February 19, 2023}}</ref><ref>{{Cite web|url=https://www.tvfanatic.com/2017/01/law-and-order-svu-season-18-episode-9-review-decline-and-fall/|website=TV Fanatic|title=Law & Order: SVU Season 18 Episode 9 Review: Decline and Fall|author=Jack Ori|date=January 18, 2017|access-date=February 19, 2023}}</ref>
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==Further reading ==
{{refbegin}}
* {{cite journal | vauthors = Hammer H, Bader BM, Ehnert C, Bundgaard C, Bunch L, Hoestgaard-Jensen K, Schroeder OH, Bastlund JF, Gramowski-Voß A, Jensen AA | display-authors = 6 | title = A Multifaceted GABAA Receptor Modulator: Functional Properties and Mechanism of Action of the Sedative-Hypnotic and Recreational Drug Methaqualone (Quaalude) | journal = Molecular Pharmacology | volume = 88 | issue = 2 | pages = 401–420 | date = August 2015 | pmid = 26056160 | pmc = 4518083 | doi = 10.1124/mol.115.099291 }}
{{refend}}
 
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[[Category:Amidines]]
[[Category:Withdrawn drugs]]
[[Category:South Africa and weapons of mass destruction]]
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