DARK Classics in Chemical Neuroscience: Methaqualone
Joseph A. Inger, Elias R. Mihan, Jhansi Kolli, Craig W. Lindsley, Aaron M. Bender
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 (GABA A R). 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.