DARK Classics in Chemical Neuroscience: Methaqualone

Abstract

Commonly known as “Quaaludes,” methaqualone (1) is a sedative–hypnotic medication, with effects resembling barbiturates and other downers, that exerts its effects through modulation of γ-aminobutyric acid type A receptors (GABAAR). Following the discovery of the sedative and euphoric effects of methaqualone (1), it was quickly adopted by pharmaceutical companies and promoted by clinicians around the world as a “safe” sleeping pill option, and for a period it was available over the counter. The popularity of methaqualone (1) soared worldwide, and many people began to use it recreationally for its sedative–hypnotic-like psychoactive effects. Not long after its introduction, many individuals began to misuse the drug leading to overdoses and drug dependence which brought to light methaqualone’s (1) addictive nature. In this review, the background, synthesis, pharmacology, metabolism, and pharmacokinetics of methaqualone (1) will be covered along with its discovery, history, and the derivatives that are currently available around the world through manufacture in clandestine laboratories.

Structural insights into GABAA receptor potentiation by Quaalude

“…Methaqualone, commonly known as Quaalude, is a central nervous system (CNS) depressant that was prescribed in the 1960s–1980s as a sedative-hypnotic 1 . The drug promotes relaxation, calmness, drowsiness, and euphoria, and it was originally advertised as a safer alternative to barbiturates to treat insomnia 1 .…”

“…Methaqualone, commonly known as Quaalude, is a central nervous system (CNS) depressant that was prescribed in the 1960s–1980s as a sedative-hypnotic 1 . The drug promotes relaxation, calmness, drowsiness, and euphoria, and it was originally advertised as a safer alternative to barbiturates to treat insomnia 1 . Methaqualone was reported to induce deep sleep in patients with insomnia and to give rise to fewer side effects compared to barbiturates, including post-hypnotic drowsiness, fatigue, and headaches 2 , 3 .…”

A descrição matemática da detecção eletroanalítica da metaqualona, baseada na sua eletrooxidação sobre o compósito da poli(5-amino-1,4-naftoquinona) com o oxihidróxido de cobalto

“…Outrossim, a dose de 8 gramas é considerada letal, e o uso excessivo do fármaco ou o seu uso acompanhado à intoxicação alcoólica, pode levar ao coma. Destarte, o desenvolvimento dos métodos da análise da metaqualona é uma tarefa realmente atual [11][12][13][14][15], e os métodos eletroanalíticos dar--lhe-iam uma solução interessante.…”