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methaqualone, combinations

N05CX02

Forms & Strengths

Historically available as oral tablets (often combined with diphenhydramine or antihistamines)
Schedule I controlled substance in the United States; no longer commercially available in most countries due to high abuse potential

Adult Dosing

No longer clinically recommended or approved for medical use
Historical hypnotic dose: 150 mg to 300 mg orally at bedtime
Historical sedative dose: 75 mg orally up to 4 times daily

Pediatric Dosing

Safety and efficacy not established in pediatric patients
Not recommended for use in children

Indications

Historically used for the short-term treatment of insomnia
Historically used for daytime sedation and anxiety relief

Mechanism of Action

Acts as a positive allosteric modulator at GABA-A receptors, enhancing GABAergic neurotransmission in the central nervous system
Depresses the central nervous system, producing sedation, hypnosis, skeletal muscle relaxation, and anxiolysis

Contraindications

Hypersensitivity to methaqualone or combination ingredients
History of substance use disorder or drug addiction
Severe hepatic impairment
Acute porphyria

Adverse Reactions

Central nervous system depression, somnolence, dizziness, and ataxia
Respiratory depression (potentially fatal in overdose)
Hangover effect, fatigue, and confusion
Tolerance, psychological dependence, and physical dependence with chronic use
Severe withdrawal syndrome upon abrupt cessation

Drug Interactions

Central nervous system depressants (alcohol, opioids, benzodiazepines, barbiturates) resulting in profound sedation and respiratory depression
CYP450 inducers or inhibitors may alter systemic clearance

Curated Content: Needs Vetting Before Put to Clinical Use