Baclofen

Category: pharmacological

Aliases: Lioresal

Pharmacological Mechanism

GABA-B receptor agonist — pre- and post-synaptic K+ conductance activation reduces spinal cord motor neuron excitability. First-line for spasticity in MS, spinal cord injury, cerebral palsy. Intrathecal pump for severe cases. Withdrawal seizures + rebound spasticity if abruptly stopped.

Half-Life (t½)

PO: 4h

Dosing Guidelines

• PO: Typical 40 mg (Range: 5–80 mg)

Target Organ Systems

• nervous

Pathways It Modulates

• GABA-A receptor signaling (activator) — GABA-B (metabotropic, Gi-coupled)
• GABA-B receptor signaling (activator) — GABA-B orthosteric agonist (antispasticity)
• Metabotropic glutamate receptors (activator) — GABA-B (parallel inhibitory autoreceptor — analogous mechanism)

Chemical Identifiers

• PubChem CID: 2284
• Formula: C10H12ClNO2
• Molecular weight: 213.66 g/mol
• InChIKey: KPYSYYIEGFHWSV-UHFFFAOYSA-N
• SMILES: C1=CC(=CC=C1C(CC(=O)O)CN)Cl

References

• PMID 23973998