Comparative Pharmacology
Head-to-head clinical analysis: CELONTIN versus LYRICA CR.
Peer-Reviewed Evidence
Head-to-head clinical analysis: CELONTIN versus LYRICA CR.
CELONTIN vs LYRICA CR
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.
Binds to the alpha-2-delta subunit of voltage-gated calcium channels in the central nervous system, reducing calcium influx and inhibiting excitatory neurotransmitter release (e.g., glutamate, norepinephrine, substance P).
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 75 mg orally twice daily (150 mg/day), or 50 mg three times daily (150 mg/day). Based on efficacy and tolerability, may increase to 150 mg twice daily (300 mg/day) after 1 week, then to 225 mg twice daily (450 mg/day) if needed. Maximum dose 450 mg/day. Take with food. Administer whole; do not split, crush, or chew.
None Documented
None Documented
Terminal elimination half-life: 40-60 hours in adults, 30-45 hours in children; prolonged liver disease or renal impairment may increase half-life.
6.3 hours (mean terminal elimination half-life); correlates with creatinine clearance, prolonged in renal impairment.
Renal: approximately 40-60% as unchanged drug; hepatic metabolism accounts for the remainder, with metabolites excreted renally.
Primarily renal excretion as unchanged drug (98-99% of absorbed dose); <0.1% biliary/fecal.
Category C
Category C
Anticonvulsant
Anticonvulsant