Comparative Pharmacology
Head-to-head clinical analysis: CELONTIN versus GABAPENTIN ENACARBIL.
Peer-Reviewed Evidence
Head-to-head clinical analysis: CELONTIN versus GABAPENTIN ENACARBIL.
CELONTIN vs GABAPENTIN ENACARBIL
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 enacarbil is a prodrug of gabapentin. It binds to the α2δ subunit of voltage-gated calcium channels, inhibiting calcium influx and reducing release of excitatory neurotransmitters such as glutamate, norepinephrine, and substance P. This modulates neuronal excitability and pain transmission.
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: 600 mg orally once daily; titrate to 600 mg three times daily; max 2400 mg/day divided three times daily.
None Documented
None Documented
Clinical Note
moderateGabapentin enacarbil + Venlafaxine
"The risk or severity of adverse effects can be increased when Gabapentin enacarbil is combined with Venlafaxine."
Clinical Note
moderateGabapentin enacarbil + Nefazodone
"The risk or severity of adverse effects can be increased when Gabapentin enacarbil is combined with Nefazodone."
Clinical Note
moderateGabapentin enacarbil + Stiripentol
"The risk or severity of adverse effects can be increased when Gabapentin enacarbil is combined with Stiripentol."
Clinical Note
moderateTerminal elimination half-life: 40-60 hours in adults, 30-45 hours in children; prolonged liver disease or renal impairment may increase half-life.
Terminal half-life of gabapentin: 5–7 hours in patients with normal renal function. Renal impairment prolongs half-life proportionally to creatinine clearance decline.
Renal: approximately 40-60% as unchanged drug; hepatic metabolism accounts for the remainder, with metabolites excreted renally.
Renal: 100% as unchanged gabapentin (prodrug is rapidly hydrolyzed to gabapentin after absorption). No biliary or fecal elimination of active drug.
Category C
Category A/B
Anticonvulsant
Anticonvulsant
Gabapentin enacarbil + Pomalidomide
"The risk or severity of adverse effects can be increased when Gabapentin enacarbil is combined with Pomalidomide."