Comparative Pharmacology
Head-to-head clinical analysis: GABLOFEN versus PARAFLEX.
Peer-Reviewed Evidence
Head-to-head clinical analysis: GABLOFEN versus PARAFLEX.
GABLOFEN vs PARAFLEX
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
GABLOFEN (baclofen) is a GABA-B receptor agonist that reduces spinal reflex transmission and inhibits excitatory neurotransmitter release.
Centrally acting muscle relaxant; inhibits polysynaptic reflexes at the spinal cord level, possibly by depressing the central nervous system.
10 mg orally three times daily, may increase by 10 mg/day every 3 days to a maximum of 80 mg/day (20 mg four times daily).
250-500 mg orally once daily, may increase to 500 mg twice daily if needed. Maximum 500 mg/day.
None Documented
None Documented
Terminal half-life 5-7 hours; clinically relevant for dosing interval of every 6-8 hours.
Terminal elimination half-life is approximately 2–3 hours, allowing for multiple daily dosing.
Renal: 70-80% unchanged; biliary/fecal: <5% as metabolites. Total clearance 2.5-3.0 L/h.
Renal excretion of unchanged drug and metabolites accounts for approximately 50% of an oral dose; fecal excretion accounts for about 20%.
Category C
Category C
Skeletal Muscle Relaxant
Skeletal Muscle Relaxant