Comparative Pharmacology
Head-to-head clinical analysis: CELONTIN versus GABAPENTIN.
Peer-Reviewed Evidence
Head-to-head clinical analysis: CELONTIN versus GABAPENTIN.
CELONTIN vs GABAPENTIN
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Increases levels of gamma-aminobutyric acid (GABA) in the central nervous system, possibly by inhibiting GABA transaminase or enhancing GABA release; also reduces calcium influx into neurons, stabilizing neuronal membranes.
Gabapentin is a structural analog of GABA but does not bind to GABA receptors. It binds to the α2δ subunit of voltage-gated calcium channels, reducing calcium influx and decreasing the release of excitatory neurotransmitters.
300 mg orally three times daily, increased by 300 mg every 3-4 days as tolerated; usual maintenance dose 900-2400 mg/day in divided doses.
Initial dose: 300 mg orally once daily on day 1, 300 mg twice daily on day 2, then 300 mg three times daily on day 3; titrate as needed up to 1800-3600 mg/day in three divided doses. Maximum single dose: 1200 mg. Dose adjustments for renal impairment should be made based on creatinine clearance.
None Documented
None Documented
Clinical Note
moderateGabapentin + Fluticasone propionate
"The risk or severity of adverse effects can be increased when Gabapentin is combined with Fluticasone propionate."
Clinical Note
moderateGabapentin + Erythromycin
"The metabolism of Erythromycin can be decreased when combined with Gabapentin."
Clinical Note
moderateGabapentin + Fluconazole
"The serum concentration of Fluconazole can be increased when it is combined with Gabapentin."
Clinical Note
moderateGabapentin + Clemastine
Terminal elimination half-life: 40-60 hours in adults, 30-45 hours in children; prolonged liver disease or renal impairment may increase half-life.
5-7 hours (normal renal function); prolonged to 50-140 hours in end-stage renal disease; half-life independent of dose due to linear kinetics.
Renal: approximately 40-60% as unchanged drug; hepatic metabolism accounts for the remainder, with metabolites excreted renally.
Renal: 76-81% unchanged in urine; biliary/fecal: <5% as metabolites; remainder (10-20%) as minor metabolites via urine.
Category C
Category A/B
Anticonvulsant
Anticonvulsant
"The risk or severity of adverse effects can be increased when Gabapentin is combined with Clemastine."