barbexaclone

N03AA04

Forms & Strengths

Oral tablets: 100 mg barbexaclone (equivalent to 60.8 mg phenobarbital and 39.2 mg l-amphetamine)

Adult Dosing

Epilepsy: Initial 100 mg to 200 mg daily, divided into 1 to 2 doses
Maintenance: Titrated based on clinical response and serum phenobarbital levels up to 400 mg daily

Pediatric Dosing

Children > 6 years: 2 mg/kg to 4 mg/kg body weight daily, adjusted according to clinical response and tolerability
Not recommended for children under 6 years due to lack of adequate safety data

Indications

Management of various forms of epilepsy, particularly generalized tonic-clonic seizures and focal seizures

Mechanism of Action

Combines phenobarbital (barbiturate) and l-amphetamine in a 1:1 molar ratio
Phenobarbital enhances GABA-A receptor activity, prolonging chloride channel opening and increasing seizure threshold
l-Amphetamine component acts as a central nervous system stimulant to counteract the sedative side effects of phenobarbital

Contraindications

Hypersensitivity to barbiturates, amphetamines, or any excipients
Acute intermittent porphyria
Severe respiratory depression
Severe hepatic or renal impairment
History of drug abuse or severe cardiovascular disease, arrhythmias, or severe hypertension

Adverse Reactions

Central nervous system: Somnolence, sedation, paradoxical excitement, insomnia, dizziness, headache
Cardiovascular: Tachycardia, palpitations, hypertension
Gastrointestinal: Nausea, vomiting, constipation
Dermatologic: Rash, allergic skin reactions, Stevens-Johnson syndrome (rare)
Metabolic/Endocrine: Osteomalacia, folate deficiency with chronic use

Drug Interactions

Central nervous system depressants (alcohol, opioids, benzodiazepines): Potentiates sedation and respiratory depression
CYP450 inducers/inhibitors: Phenobarbital is a potent inducer of CYP3A4, CYP2C9, and CYP2C19, decreasing concentrations of co-administered drugs (e.g., oral contraceptives, anticoagulants)
Monoamine Oxidase Inhibitors (MAOIs): Concurrent use with amphetamine component risks hypertensive crisis
Antihypertensive agents: Amphetamines may decrease the efficacy of antihypertensive drugs

Curated Content: Needs Vetting Before Put to Clinical Use