Comparative Pharmacology
Head-to-head clinical analysis: PARADIONE versus VALPROIC ACID.
Peer-Reviewed Evidence
Head-to-head clinical analysis: PARADIONE versus VALPROIC ACID.
PARADIONE vs VALPROIC ACID
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Paradione (paramethadione) is an oxazolidinedione anticonvulsant that suppresses neuronal activity in the motor cortex by increasing the threshold for repetitive neuronal firing and reducing synaptic transmission. Its exact mechanism is unclear but involves modulation of T-type calcium channels and enhancement of GABAergic inhibition.
Increases GABA concentration in the brain by inhibiting GABA transaminase and succinic semialdehyde dehydrogenase; also blocks voltage-gated sodium channels and T-type calcium channels.
100 mg orally three times daily; maximum 600 mg/day.
Initial: 10-15 mg/kg/day orally (divided 2-3 times), increase by 5-10 mg/kg/week; maintenance: 30-60 mg/kg/day. IV infusion: same oral dose, rate ≤20 mg/min.
None Documented
None Documented
Clinical Note
moderateValproic acid + Fluticasone propionate
"The risk or severity of adverse effects can be increased when Valproic acid is combined with Fluticasone propionate."
Clinical Note
moderateValproic acid + Sulfisoxazole
"The metabolism of Sulfisoxazole can be decreased when combined with Valproic acid."
Clinical Note
moderateValproic acid + Cyclosporine
"The metabolism of Cyclosporine can be decreased when combined with Valproic acid."
Clinical Note
moderateValproic acid + Fluconazole
12-24 hours (terminal); prolonged in renal impairment
Terminal elimination half-life is 9–16 hours in adults; shorter in children (6–9 hours) and longer in neonates (20–30 hours), elderly, or hepatic impairment (up to 18 hours).
Renal: 70% unchanged; biliary/fecal: 25%; metabolic: 5%
Primarily hepatic metabolism (>95%), with less than 3% excreted unchanged in urine. Minor fecal excretion (~5%).
Category C
Category D/X
Anticonvulsant
Anticonvulsant
"The metabolism of Fluconazole can be decreased when combined with Valproic acid."