Comparative Pharmacology
Head-to-head clinical analysis: GABLOFEN versus ROBAXIN.
Peer-Reviewed Evidence
Head-to-head clinical analysis: GABLOFEN versus ROBAXIN.
GABLOFEN vs ROBAXIN
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; depresses polysynaptic reflexes at spinal cord and supraspinal levels, possibly via glycine receptor agonism and GABAergic modulation.
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).
1500 mg orally 4 times daily, or 750 mg orally every 4 hours as needed. Maximum 6 g/day. For IV use: 1 g (10 mL) as a single intravenous injection or infusion.
None Documented
None Documented
Terminal half-life 5-7 hours; clinically relevant for dosing interval of every 6-8 hours.
1-2 hours in adults; clinically, multiple daily dosing required to maintain effect.
Renal: 70-80% unchanged; biliary/fecal: <5% as metabolites. Total clearance 2.5-3.0 L/h.
Renal excretion of metabolites accounts for 99% of elimination; <1% excreted as unchanged drug in urine.
Category C
Category C
Skeletal Muscle Relaxant
Skeletal Muscle Relaxant