Comparative Pharmacology
Head-to-head clinical analysis: GABITRIL versus VALPROIC ACID.
Peer-Reviewed Evidence
Head-to-head clinical analysis: GABITRIL versus VALPROIC ACID.
GABITRIL vs VALPROIC ACID
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Tiagabine inhibits gamma-aminobutyric acid (GABA) reuptake into presynaptic neurons, thereby increasing synaptic GABA levels and enhancing inhibitory neurotransmission.
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.
Initial dose: 4 mg orally twice daily. Titrate by 4-8 mg/day every 2 weeks. Maximum dose: 56 mg/day in 2-4 divided doses.
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
Terminal elimination half-life is 7–9 hours in healthy adults. In patients with hepatic impairment, half-life is prolonged (up to 12–24 hours) due to reduced clearance. No significant effect of 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).
Approximately 70% of an oral dose is excreted in feces, 25% in urine, and 5% in bile. Renal elimination of unchanged drug is minimal (<2%); most is eliminated as metabolites.
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."