Comparative Pharmacology
Head-to-head clinical analysis: GABAPENTIN versus LYRICA.
Peer-Reviewed Evidence
Head-to-head clinical analysis: GABAPENTIN versus LYRICA.
GABAPENTIN vs LYRICA
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
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.
Binds to the α2-δ subunit of voltage-gated calcium channels, reducing calcium influx and inhibiting release of excitatory neurotransmitters including glutamate, norepinephrine, and substance P.
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.
Oral: 75-150 mg twice daily or 50-100 mg three times daily; maximum 600 mg/day. Start at 75 mg twice daily.
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
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.
Terminal elimination half-life is 6.3 hours (range 5.5–6.7 hours) in patients with normal renal function. Half-life increases in renal impairment (up to 48 hours in anuria).
Renal: 76-81% unchanged in urine; biliary/fecal: <5% as metabolites; remainder (10-20%) as minor metabolites via urine.
Renal excretion of unchanged drug accounts for approximately 90% of elimination; less than 1% is secreted in feces or bile. Dose adjustment required in renal impairment (CrCl <60 mL/min).
Category A/B
Category C
Anticonvulsant
Anticonvulsant
"The risk or severity of adverse effects can be increased when Gabapentin is combined with Clemastine."