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Liofen XL 20 (Baclofen): Mechanism of Action in Spasticity Management

Pharmacology

Baclofen is a GABAB receptor agonist. Liofen XL is an extended-release formulation providing sustained delivery.

Mechanisms

  1. Presynaptic inhibition (spinal): GABAB activation on primary afferent terminals → ↓ Ca²⁺ influx → ↓ excitatory neurotransmitter (glutamate, substance P) release → reduced monosynaptic and polysynaptic reflexes.
  2. Postsynaptic hyperpolarization: K⁺ channel opening → neuronal inhibition.
  3. Supraspinal effects: Action on brainstem/thalamic circuits modulates descending facilitation.
  4. Muscle-level: Minor direct effect via Ca²⁺ channel modulation (controversial).

Clinical Use

  • Spasticity from MS, spinal cord injury, cerebral palsy, stroke.
  • Dosing: Start low (5 mg TID), titrate weekly; XL allows BID dosing.
  • Max 80–100 mg/day; monitor sedation, weakness, renal function.
  • Abrupt cessation → withdrawal (hallucinations, seizures, rebound spasticity) – taper slowly.

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