Comparative Pharmacology
Head-to-head clinical analysis: LYRICA CR versus PHENYTOIN.
Head-to-head clinical analysis: LYRICA CR versus PHENYTOIN.
LYRICA CR vs PHENYTOIN
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
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).
Phenytoin is a hydantoin anticonvulsant that stabilizes neuronal membranes and decreases seizure activity by increasing efflux or decreasing influx of sodium ions across cell membranes in the motor cortex during generation of nerve impulses. It use-dependently blocks voltage-gated sodium channels, prolonging their inactivation phase and reducing high-frequency repetitive firing of action potentials.
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.
Oral: 300-400 mg/day in 3-4 divided doses; IV: 15-20 mg/kg loading dose, then 300 mg/day maintenance.
None Documented
None Documented
Clinical Note
moderatePhenytoin + Digoxin
"The metabolism of Digoxin can be increased when combined with Phenytoin."
Clinical Note
moderateFosphenytoin + Digoxin
"The metabolism of Digoxin can be increased when combined with Fosphenytoin."
Clinical Note
moderatePhenytoin + Digitoxin
"The metabolism of Digitoxin can be increased when combined with Phenytoin."
Clinical Note
moderateFosphenytoin + Digitoxin
"The metabolism of Digitoxin can be increased when combined with Fosphenytoin."
6.3 hours (mean terminal elimination half-life); correlates with creatinine clearance, prolonged in renal impairment.
Average terminal half-life 22 hours (range 7–42 hours) in adults; dose-dependent due to saturation of metabolism at therapeutic concentrations (10–20 mg/L). Half-life increases with higher doses.
Primarily renal excretion as unchanged drug (98-99% of absorbed dose); <0.1% biliary/fecal.
Primarily hepatic metabolism (>95%); less than 5% excreted unchanged in urine. Renal excretion of metabolites (glucuronides) accounts for ~80% of elimination; biliary/fecal excretion of metabolites ~20%.
Category C
Category D/X
Anticonvulsant
Anticonvulsant