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.