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methaqualone

N05CM01

Forms & Strengths

Oral tablets: 150 mg, 200 mg, 300 mg
Combination formulations (e.g., methaqualone with diphenhydramine)

Adult Dosing

Insomnia: 150 mg to 300 mg orally once daily at bedtime
Sedation: 75 mg to 150 mg orally 3 to 4 times daily

Pediatric Dosing

Safety and efficacy not established in pediatric patients

Indications

Short-term treatment of insomnia (historically)
Sedative and hypnotic use (largely withdrawn due to high abuse potential and overdose toxicity)

Mechanism of Action

Acts as a central nervous system depressant
Potentiates GABA-A receptor activity, similar to barbiturates
Interacts with the barbiturate-binding site on the GABA-A receptor complex

Contraindications

Hypersensitivity to methaqualone
History of drug abuse or dependence
Severe hepatic impairment
Acute intermittent porphyria
Pregnancy and lactation

Adverse Reactions

Drowsiness, dizziness, and lethargy
Ataxia, headache, and hangover effect
Nausea, vomiting, and diarrhea
Severe respiratory depression in overdose
Coma, delirium, and death in massive overdose
Psychological and physical dependence with tolerance

Drug Interactions

Central nervous system depressants (alcohol, opioids, benzodiazepines, barbiturates): potentiation of sedation and respiratory depression
CYP450 inducers or inhibitors may alter metabolism and clearance

Curated Content: Needs Vetting Before Put to Clinical Use