Drugs of abuse

What is the mechanism of action of quaaludes?

Answer: Quaaludes (methaqualone) are a sedative drug that produces its effect through increasing GABA receptor activity.

From https://www.theparisreview.org/blog/2014/01/28/free-of-ones-melancholy-self/

From https://www.theparisreview.org/blog/2014/01/28/free-of-ones-melancholy-self/

Methaqualone has a hypnotic and sedative function, meaning it enhances the duration or restfulness of sleep. Therefore, it is helpful as a treatment of insomnia. It is also a known muscle relaxant, which can help if a person is experiencing spasms.

Quaaludes act at the GABA receptor. The exact function has not be completely studied. Although, it is speculated that  methaqualone increases the duration of a chloride channel remaining open after GABA binds to a GABA-A receptor, making it a positive allosteric modulator. Increased chloride channel open time means increased inhibition of the cell.

The drug was developed in the early 1960s, and it became a popular recreational club drug in the 60s and 70s. It may be referred to as “ludes”, “soaps”, or “mandrakes”. It was taken off the market in 1983 due to high risk of abuse. Recreational use had dwindled to a minimum by the 1990s. According to the Drug Enforcement Agency and the Food and Drug Administration, it is classified as a Schedule I drug.

The drug can rapidly produce a tolerance, requiring a person to take progressively higher doses of drug to continue feeling the psychoactive effect.

The pharmaceutical company Rorer and Lemmon developed the drug, and pills were imprinted with the number 714. They may be referred to as “714s” because of this.

The name “quaalude” itself is a portmanteau of the phrase “quiet interlude,” in reference to the soporific effect of the compound.