Baclofen
GABA-B agonist prescription muscle relaxant, off-label anxiolytic and anti-alcohol-craving agent.
The links above are labelled third-party affiliate links. MolekulaX does not sell and does not verify product quality.
Pharmacology
Contents
WHAT IS BACLOFEN?
Detailed overview
Baclofen is a chlorophenyl derivative of GABA and a selective GABA-B receptor agonist, approved primarily as a skeletal muscle relaxant for spasticity (multiple sclerosis, spinal cord injury). Activating GABA-B receptors opens potassium channels and inhibits calcium channels, hyperpolarizing neurons and reducing excitatory neurotransmission, which underlies its muscle-relaxing, anxiolytic and craving-reducing effects. Although it is not licensed for anxiety or sleep, it is used off-label as a mild anxiolytic and, at higher doses, in the treatment of alcohol dependence, for which France granted a specific authorization. It is a prescription medicine that must never be stopped abruptly because of the risk of severe withdrawal seizures.
Mechanism
GABA-B receptor agonist
Half-life
about 3-4 hours (oral)
Legal status
Prescription medicine (muscle relaxant)
Receptor profile
- GABA-B receptorsStrong
- Spinal reflex inhibition (spasticity)Strong
- Presynaptic calcium channels (reduced glutamate release)Moderate
- GIRK potassium channels (neuronal hyperpolarization)Moderate
Safety
Side effects, stop signs, contraindications
Side effects · 6
- Drowsiness, sedation, dizziness and fatigue, especially early in treatment
- Dose-related muscle weakness and hypotonia
- Nausea, dry mouth and gastrointestinal discomfort
- Headache, confusion and less commonly mood changes
- Dangerous withdrawal on abrupt discontinuation: seizures, hallucinations, rebound spasticity; must always be tapered
- Overdose can cause respiratory depression and coma, particularly with alcohol or other CNS depressants
Contraindications · 5
- Never stop abruptly after long-term use due to the risk of withdrawal seizures: gradual tapering is mandatory
- Avoid combining with alcohol, benzodiazepines and opioids due to additive CNS and respiratory depression
- Renal impairment: reduced clearance can cause accumulation, dose reduction is needed
- Caution in epilepsy or lowered seizure threshold
- Pregnancy and breastfeeding: only under clear medical indication and supervision
Related Nootropics
Same therapeutic category
Studies
Related research and clinical findings
Optimal Dose of Baclofen for the Treatment of Alcohol Use Disorder: A Systematic Review and Dose-Response Meta-analysis
Systematic review
Baclofen promotes alcohol abstinence in alcohol dependent cirrhotic patients with hepatitis C virus (HCV) infection
Barrault C, et al.
Efficacy and safety of alcohol reduction pharmacotherapy according to treatment duration in patients with alcohol dependence or alcohol use disorder: A systematic review and network meta-analysis
Systematic review
Medications for alcohol use disorder promote abstinence in alcohol-associated cirrhosis: Results from a systematic review and meta-analysis
Systematic review
Influence of GABA(A) and GABA(B) receptor activation on auditory sensory gating and its association with anxiety in healthy volunteers
Human study
A single, clinically relevant dose of the GABA(B) agonist baclofen impairs visuomotor learning
Human study
FAQ
FAQ
GABA-B agonist prescription muscle relaxant, off-label anxiolytic and anti-alcohol-craving agent.
Telegram
Have a question about Baclofen?
Reach out to us on Telegram for a personalized stack. We'll be happy to help.
Personalized consultation
Want a detailed conversation tailored to your data?
Fill out the prep intake form (your goals, training and health data), and the advisor prepares from it to give genuinely personalized guidance.
Fill out the form~5–7 min · prep questionnaire · confidential · GDPR-compliant
Structure & chemistry
The information here is strictly for educational and scientific purposes. It does not replace medical advice or clinical consultation, and it does not encourage illegal substance or pharmaceutical use. Data is sourced. When in doubt, consult your doctor.