Baclofen

Generic Details

Generic Name

Baclofen

Other Names

  • Lioresal
  • Gablofen
  • Kemstro

Drug Class

  • Muscle Relaxant
  • GABA Receptor Agonist

Chemical Formula

C10H12ClNO2

Molecular Weight

213.66 g/mol

Mechanism of Action

  • Activates GABA receptors in the spinal cord, inhibiting the transmission of signals from spinal cord nerves to muscles, resulting in muscle relaxation.

Indications

  • Spasticity (muscle stiffness/spasm) associated with conditions such as multiple sclerosis, spinal cord injuries, and cerebral palsy

Common Dosage Forms

  • Tablet
  • Injection

Typical Dosage

  • 5-20 mg three times a day, gradually increased as needed

Pediatric Dosage

  • Dosing based on weight and severity of condition, typically starting at lower end and adjusted cautiously

Geriatric Dosage

  • Lower initial doses to account for reduced liver/kidney function and increased sensitivity

Side Effects

  • Drowsiness
  • Dizziness
  • Weakness
  • Fatigue
  • Nausea
  • Headache

Contraindications

  • Hypersensitivity to baclofen
  • History of stroke
  • Severe psychiatric conditions

Pregnancy Category

  • C - Risk cannot be ruled out

Lactation Safety

  • Limited data available, caution advised

Drug Interactions

  • Alcohol
  • CNS depressants (e.g., benzodiazepines)
  • Antihypertensives

Overdose Symptoms

  • Severe drowsiness
  • Respiratory depression
  • Hypotension
  • Coma

Antidote for Overdose

  • Activated charcoal
  • Laxatives
  • Supportive care

Storage Conditions

  • Store at room temperature away from moisture and heat

Pharmacokinetics

  • Absorption: Well absorbed orally
  • Distribution: Crosses the blood-brain barrier, widely distributed in the body
  • Metabolism: Primarily hepatic
  • Excretion: Mainly renally excreted

Precautions

  • May cause sedation, use caution when driving or operating machinery
  • Abrupt withdrawal may result in hallucinations or seizures

Warnings

  • May cause CNS depression, use with caution in elderly

Others

  • Regular monitoring of liver and renal function recommended during long-term use