Baclofen

Skeletal muscle relaxant (centrally-acting), Antispastic, GABA-B receptor agonist

Baclofen

Lioresal (oral, intrathecal pump), Ozobax / Fleqsuvy (oral suspension), Gablofen (intrathecal), Lyvispah (oral granules)

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Summary

Classes

Skeletal muscle relaxant (centrally-acting), Antispastic, GABA-B receptor agonist

Pharmacy

Starting dose

Oral: 5 mg PO TID, titrate by 5 mg per dose every 3 days. Intrathecal: bolus test dose, then continuous infusion via implanted pump

Preparations

Tablets 5, 10, 20 mg; oral suspension 5 mg/5 mL (Ozobax, Fleqsuvy); intrathecal injection 50, 500, 1000, 2000 mcg/mL (Lioresal Intrathecal, Gablofen); oral granules (Lyvispah)

US FDA Max

80 mg/day oral (higher off-label)

Pharmacology

Routes

Oral, intrathecal (via implanted infusion pump)

Onset

1-2 hours (oral)

Duration

4-6 hours (oral, TID-QID dosing)

Half-life

3-4 hours

Bioavailability

~70-85% (oral)

Pregnancy

Limited human data.^{[citation needed]}

Legal status

Rx-only in US. Not a controlled substance

Purported mechanism

Selective agonist at the GABA-B receptor (the only metabotropic GABA receptor; distinct from the ionotropic GABA-A targeted by benzodiazepines and Z-class hypnotics). Reduces excitatory neurotransmitter release presynaptically and hyperpolarizes postsynaptic membranes, producing antispastic effect particularly at spinal cord interneurons.▲0▼ Severe withdrawal syndrome is the marquee adverse-event concern, especially with abrupt cessation of intrathecal administration: hyperthermia, altered mental status, hyperreflexia, rhabdomyolysis, and multiorgan failure can develop within 24-72 hours and progress to death. Gradual taper is essential after extended use; intrathecal pump failures are a recognized emergency.