What is the half-life of Baclofen (GABA receptor agonist)?

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Half-Life of Baclofen

Baclofen has a half-life of approximately 3.5 to 5 hours in patients with normal renal function, though this can be significantly prolonged in overdose situations or renal impairment. 1

Pharmacokinetic Properties

Standard Half-Life Parameters:

  • The FDA-approved drug label indicates baclofen is rapidly absorbed and eliminated primarily by the kidney in unchanged form 1
  • Clinical studies in healthy volunteers demonstrate a half-life of 5.24 hours after oral administration and 5.79 hours after intravenous administration 2
  • A large pharmacokinetic study in alcohol use disorder patients found a half-life of 4.4 hours with racemic baclofen 3
  • After oral administration in pediatric studies, the half-life ranged from 2.3 to 3.4 hours 4

Clinical Context and Variations

Intrathecal Administration:

  • When administered intrathecally for spasticity, baclofen clearance from cerebrospinal fluid occurs with a half-life of 5 hours 5

Overdose Situations:

  • In baclofen overdose, the half-life can be dramatically prolonged up to 34 hours, necessitating extended monitoring and potentially requiring hemodialysis or continuous venovenous hemofiltration 6
  • During hemofiltration treatment for overdose, the elimination half-life was reduced to 4.8 hours 6

Renal Function Impact

Critical Consideration:

  • Baclofen is excreted primarily unchanged by the kidneys, with relatively large intersubject variation in elimination 1
  • Patients with renal impairment will have significantly prolonged half-lives, though specific values are not well-established in the literature
  • The FDA label notes there is "relatively large intersubject variation in absorption and/or elimination" 1

Practical Implications

Dosing Frequency:

  • The short half-life of 3.5-5 hours necessitates three-times-daily dosing for most clinical applications 7
  • This contrasts with longer-acting muscle relaxants or GABA agonists that may allow once or twice-daily dosing

Withdrawal Risk:

  • The relatively short half-life means abrupt discontinuation can rapidly lead to withdrawal syndrome, as therapeutic levels decline within 15-25 hours (3-5 half-lives) 2

Professional Medical Disclaimer

This information is intended for healthcare professionals. Any medical decision-making should rely on clinical judgment and independently verified information. The content provided herein does not replace professional discretion and should be considered supplementary to established clinical guidelines. Healthcare providers should verify all information against primary literature and current practice standards before application in patient care. Dr.Oracle assumes no liability for clinical decisions based on this content.

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