CAS Number: 1134-47-0

Baclofen | 1134-47-0

Baclofen is a gamma-aminobutyric acid type B (GABA-B) receptor agonist used clinically for multiple indications. It is employed in managing hypertonia in children with cerebral palsy, where it is considered a first-line oral treatment for generalized dystonia, and can also be administered intrathecally. Additionally, it is used off-label for alcohol use disorder. From a pharmaceutical development perspective, an efficient large-scale method has been established to produce enantiomerically pure (R)- and (S)-baclofen hydrochloride via chiral resolution using 2-oxazolidinones as chiral auxiliaries, which allows for high optical purity (>99% ee) and simultaneous isolation of both enantiomers. However, clinical evidence also indicates that high doses of baclofen (e.g., 200 mg/day) can induce a reversible narcolepsy-like presentation characterized by excessive daytime sleepiness, sleep attacks, and cataplexy-like episodes, which resolve upon dose reduction—a phenomenon possibly explained by GABA-B–mediated inhibition of orexin neurons.

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References

  • The use of baclofen to reduce alcohol-attributable hospitalizations and emergency department admissions
    Baclofen was associated with a reduced incidence of alcohol-attributable hospitalizations (IRR = 0.64; 95% CI: 0.53∼0.77) and ED admissions (IRR = 0.56; 95% CI: 0.49∼0.65) in multivariate models. No statistically significant reduction was observed in any admission method in either the pre- or post-exposure period. A dose-dependent response in ED admissions was observed with baclofen, i.e. >60 mg/day associated with a greater decrease in the IRR (0.25, 95% CI: 0.10∼0.62) relative to doses of <30 (0.63, 95% CI: 0.53∼0.75) and 30–60 mg/day (IRR = 0.50, 95% CI: 0.40∼0.63).
    DOI: 10.1016/j.alcohol.2025.03.002
  • G-186 Renal Roulette: Perils of Baclofen Overdose and Withdrawal
    This case report describes a 46-year-old man with depression who developed profound obtundation, hypotension requiring norepinephrine, and acute kidney injury (AKI) after intentional baclofen overdose. His clinical course was complicated by delayed neurological recovery due to prolonged baclofen clearance—exacerbated by AKI and saturation kinetics—followed by severe agitation and choreiform movements consistent with acute baclofen withdrawal upon renal recovery. The authors highlight that baclofen toxicity and withdrawal can be life-threatening even with normal baseline kidney function, emphasizing the need for close renal monitoring, supportive care, cautious reintroduction of baclofen to prevent withdrawal, and careful consideration if hemodialysis is used to avoid rapid drug removal that may trigger withdrawal symptoms.
    DOI: 10.1053/j.ajkd.2026.02.187
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