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WARNINGMIXING OR WITHDRAWAL CAN BE DANGEROUS
Ordinary doses in combination with other depressants can fatally stop breathing. After prolonged dependency, stopping suddenly can also cause seizures or delirium; seek medical help.
Baclofen
β-(4-chlorophenyl)-GABA
Lioresal, Gablofen, Kemstro, Liofen, Fleqsuvy
Baclofen is a depressant and muscle relaxant of the butyric acid class that acts as a GABA-B receptor agonist.citation needed Originally synthesized in 1962 to treat epilepsy, it proved ineffective for that purpose but was later approved in 1977 for managing muscle spasticity. Chemically related to phenibut, pregabalin, and gabapentin, it produces sedation, anxiety suppression, and moderate euphoria. It has also been researched as a potential treatment for alcohol dependence.12
Dosage & Duration
Dosage
Doses are population estimates that vary widely between individuals.
Threshold~5 mg
Light5-20 mg
Moderate20-50 mg
Strong50-75 mg
Heavy75+ mg
Bioavailability
70-85%
Doses exceeding 125 mg carry substantial risk of blackout and respiratory depression. Tolerance to effects builds quickly with repeated administration.
Duration
Onset15-75 minutes
Come Up1-1.5 hours
Peak1-2 hours
Offset1.5-2.5 hours
After Effects6-12 hours
Total8-14 hours
Half-life
2-6 hours
Subjective Effects
Legacy content. A statistically backed ontology from Mindstate Design Labs is coming soon.
The baclofen experience is dominated by muscle relaxation, sedation, and anxiety suppression, with a mild euphoria reported at recreational doses. The overall character is frequently compared to phenibut, a structurally related GABA-B agonist, though baclofen is generally considered less recreational. Sensory alteration is essentially absent; the experience is defined by its depressant body effects and a calm, dulled mental state.
Physical
Pronounced muscle relaxation and a heavy, sedated body feeling are the core physical effects, often accompanied by drowsiness, weakness, and dizziness. Nausea, headaches, and impaired motor coordination can occur, and respiratory depression becomes a serious risk at high doses.
Sedation
Uncomfortable
Cognitive
The headspace is calm and anxiolytic, with reduced anxiety as the most consistently reported mental effect alongside a mild euphoria. At higher doses, concentration and memory become noticeably impaired, and thinking takes on a foggy, sedated quality.
Emotional
Suppressions
Pharmacology
Pharmacodynamics
Baclofen acts as an agonist at the GABA-B receptor, binding to both the B1 and B2 subunits on pre- and post-synaptic neurons.citation needed Receptor activation causes neuronal hyperpolarization through potassium influx, reducing presynaptic calcium entry and decreasing the release of excitatory neurotransmitters, which inhibits both mono- and polysynaptic reflex transmission at the spinal cord. Baclofen also blocks α2δ subunit-containing voltage-gated calcium channels, though with weak affinity (Ki = 156 μM) that is considered likely not clinically relevant. GABA-B receptor activation is additionally thought to reduce dopaminergic activity in the mesolimbic pathway.3
Pharmacokinetics
Baclofen is rapidly absorbed through the gastrointestinal tract following oral administration, with a bioavailability of approximately 70-85%.4 Only about 15% of the oral dose is metabolized in the liver, primarily through deamination.citation needed The elimination half-life following oral administration ranges from approximately 2 to 6 hours, with longer estimates of approximately 5.6 to 6.8 hours also described.
Dangerous
Highest riskThese combinations are considered extremely harmful and should always be avoided. Reactions to these drugs taken in combination are highly unpredictable and have a potential to cause death.
DissociativesStimulants
Caution
Use cautionThese combinations are not usually physically harmful, but may produce undesirable effects, such as physical discomfort or overstimulation. Extreme use may cause physical health issues. Synergistic effects may be unpredictable. Care should be taken when choosing to use this combination.
1,2-BenzodiazepineAbacavirAcarboseAcebutololAceclofenac
Tolerance
Tolerance timelines are rules of thumb, not exact schedules, and vary widely between individuals and use patterns.
Full Tolerance
Tolerance to sedative-hypnotic effects can appear after only several days of uninterrupted baclofen use.
Cross Tolerance
GABAergic depressants
Baseline Reset
Following cessation, tolerance returns to baseline within 7-14 days.
Harm Potential
Addiction & Dependence
Psychological
ModerateModerate abuse potential with risk of psychological dependence. Compulsive redosing has been reported as an after effect of use.
Physical
HighPhysical dependence develops with chronic use, potentially occurring within weeks of regular dosing at low or high doses. Withdrawal syndrome resembles benzodiazepine and alcohol withdrawal, with symptoms ranging from anxiety, tremors, and insomnia to severe manifestations including hallucinations, delirium, psychosis, seizures, and extreme muscle rigidity resembling neuroleptic malignant syndrome.citation needed Abrupt discontinuation is not advised; gradual tapering is necessary.
Toxicity
Central Nervous System
CNS depression including sedation, somnolence, and ataxia occurs at therapeutic and recreational doses; overdose may cause altered mental status, hypothermia, and coma that can mimic brain death.citation needed
Respiratory
Respiratory depression and insufficiency may occur, particularly at higher doses or in overdose; risk increases significantly when combined with other CNS depressants.citation needed
Cardiovascular
Cardiovascular depression is possible at high doses; overdose may cause bradycardia, tachycardia, hypertension, and cardiac conduction abnormalities, though these effects are uncommon.citation needed
Musculoskeletal
Rhabdomyolysis may occur if baclofen use is stopped abruptly after chronic administration; this is a withdrawal complication rather than a direct toxic effect during use.citation needed
Renal
Baclofen should be avoided in chronic kidney disease and end-stage renal disease as even small doses can cause excessive toxicity due to impaired drug clearance; this represents accumulation toxicity rather than direct nephrotoxicity.citation needed
Psychosis Risk
Psychosis, hallucinations (auditory, visual, and tactile), delusions, delirium, confusion, disorientation, and mania may occur during withdrawal from chronic use, particularly with abrupt discontinuation.citation needed These psychiatric symptoms are associated with the withdrawal syndrome rather than acute intoxication.
Seizure Risk
Seizures may occur in overdose or with abrupt discontinuation after chronic use.citation needed Withdrawal-related seizures are a serious concern requiring gradual tapering when discontinuing therapy. High-dose combinations with sedatives may also precipitate de novo seizures.
History & Culture
Discovery and Development
Baclofen was first synthesized in 1962 by Swiss chemist Heinrich Keberle at Ciba-Geigy in Basel, Switzerland.citation needed The compound was designed with the intention of enhancing the lipophilicity of gamma-aminobutyric acid (GABA) to enable penetration of the blood-brain barrier, with…
Legality
International
1961 Single Convention: baclofen is not scheduled.
1971 Convention on Psychotropic Substances: baclofen is not scheduled.
1988 Convention: baclofen is not listed in precursor Tables I or II.
By Country
Prescription8
United StatesPrescription onlyFederal Food, Drug, and Cosmetic Act; current DailyMed labeling37
Current official medicine law and labeling establish baclofen as prescription-only in United States.
CanadaPrescription onlyHealth Canada Drug Product Database9
Current official medicine records identify baclofen as prescription-only in Canada.
GermanyPrescription onlyArzneimittelverschreibungsverordnung, Anlage 112
Current official medicine law and labeling establish baclofen as prescription-only in Germany.
RussiaPrescription onlyRussian Ministry of Health Order No. 100n of 7 March 2025 (current dispensing rules, effective 1 September 2025 through 1 September 2031), Order No. 1094n of 24 November 2021 (prescription procedure, current through 1 March 2028), and Order No. 653n of 28 October 2025 amending the PKU list in Order No. 459n (baclofen except intrathecal dosage form, effective 1 March 2026 through 1 September 2030); Government Resolution No. 681 of 30 June 1998, current Roszdravnadzor-hosted consolidation amended 11 June 2025 (controlled narcotic/psychotropic list); Code of Administrative Offences Article 14.4.2(1.1) and Criminal Code Articles 228 and 234.131415161718192021222324
Current Russian law distinguishes prescription/PKU regulation from narcotic, psychotropic and Article 234 strong-substance control. Ordinary baclofen medicines are in the PKU list from 1 March 2026 except intrathecal dosage forms, and current dispensing rules route PKU medicines through form 148-1/u-88. The current Resolution No. 681 and Resolution No. 964 schedules do not list baclofen. These instruments do not support criminal prosecution of a patient merely for storing or transporting baclofen without a valid prescription. Article 14.4.2(1.1) penalties concern a covered retailer's dispensing of a PKU medicine without prescription; they are not a blanket possession penalty for the patient. Active Ministry registry records are effective in July/August 2026; Order No. 653n commenced on 1 March 2026 and ends in 2030, Order No. 100n has a 2025–2031 term, Roszdravnadzor posted Resolution No. 681 in 2026, and the current consolidated code records were amended in July/August 2026.
SwedenPrescription onlyRegulated as a prescription medication. Available through pharmacies with a valid prescription from a licensed healthcare provider.25
TurkeyPrescription onlyLaw No. 1262 on Pharmaceutical and Medical Preparations (İspençiyari ve Tıbbi Müstahzarlar Kanunu), Articles 1, 7, 12 and 18–20; Law No. 2313 on the Control of Narcotic Drugs; Turkish Penal Code No. 5237 (TCK), Articles 188, 190 and 191. The applicable framework also includes Law No. 7496 (Official Gazette 1 March 2024, No. 32476) and the current consolidated text of Law No. 1262.26272829303132333435
In Turkey, baclofen requires a prescription; the official Turkish patient leaflet directs that it be prescribed and used as directed, and the LİORESAL product record identifies it as Beyaz Reçete and Aktif. The official KÜB was renewed 30 July 2025; as of 28 August 2026, the product record reports an active tablet, supporting current marketed treatment. Baclofen is a normal/white-prescription medicine, not a narcotic or NPS. The official 2025 Narkotik report's TCK 188/191 penalty ranges concern narcotic/psychotropic substances and do not, without a substance-specific controlled designation, convert ordinary lawful baclofen possession into a narcotics offense. Law No. 1262 remains relevant to prescription-only supply: unauthorized dispensing or unlawful product sale can trigger medicine-law enforcement. The white-prescription classification applies to the identified product; classification of a particular pack or transaction may depend on its live TİTCK/Medula record.
United KingdomPrescription onlyHuman Medicines Regulations 2012; current baclofen product authorisation36
Current official medicine records identify baclofen as prescription-only in United Kingdom.
References
Source Pages
Citations
- Roberta Agabio, Rosella Saulle, Susanne Rösner, & Silvia Minozzi. (January 2023). Baclofen for alcohol use disorder. The Cochrane Database of Systematic Reviews, 1(1). https://doi.org/10.1002/14651858.cd012557.pub31
- Caitlin N. Kent, Charlotte Park, & Craig W. Lindsley. (n.d.). Classics in Chemical Neuroscience: Baclofen. ACS Chemical Neuroscience. https://doi.org/10.1021/acschemneuro.0c002541
- Jia W Romito, Emily R Turner, John A Rosener, Landon Coldiron, Ashutosh Udipi, Linsey Nohrn, Jacob Tausiani, & Bryan T Romito. (2021). Baclofen therapeutics, toxicity, and withdrawal: A narrative review. SAGE Open Medicine, 9. https://doi.org/10.1177/205031212110221971
- StatPearls [Internet]. StatPearls Publishing (May 2022). https://pubmed.ncbi.nlm.nih.gov/30252293/1
- Holly E. Perry MD, Robert O. Wright MD, Michael W. Shannon MD, & Alan D. Woolf MD. (June 1998). Baclofen overdose: drug experimentation in a group of adolescents. Pediatrics, 101(6), 1045–1048. https://doi.org/10.1542/peds.101.6.10451
- Baclofen. Chemistry World (n.d.). https://www.chemistryworld.com/podcasts/baclofen/3010770.article1
- Baclofen in alcohol use disorder: An analysis of the data provided by the French 'Temporary Recommendation for Use' 2014–2017 cohort. Drug and Alcohol Dependence Reports (October 2022). https://pmc.ncbi.nlm.nih.gov/articles/PMC9597083/1
- Health Canada Drug Product Database. health-products.canada.ca (n.d.). https://health-products.canada.ca/dpd-bdpp/index-eng.jsp1
- Renaud de Beaurepaire, & Benjamin Rolland. (2022). Baclofen in alcohol use disorder: An analysis of the data provided by the French "Temporary Recommendation for Use" 2014–2017 cohort. Frontiers in Psychiatry. https://doi.org/10.3389/fpsyt.2022.9497501
Article Status
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Josie Kins · Updated the article · also 1,4-Butanediol, 1B-LSD, 1cP-AL-LAD and 573 more
Josie Kins · Updated the article · also 1,4-Butanediol, 1B-LSD, 1cP-AL-LAD and 573 more
Josie Kins · Updated the article · also 1,4-Butanediol, 1B-LSD, 1cP-AL-LAD and 573 more
Josie Kins · Updated the article · also 1,4-Butanediol, 1B-LSD, 1cP-AL-LAD and 573 more
Josie Kins · Updated the article · also 1,4-Butanediol, 1B-LSD, 1cP-AL-LAD and 573 more
Josie Kins · Updated the article · also 1,4-Butanediol, 1B-LSD, 1cP-AL-LAD and 573 more
Josie Kins · Updated the article · also 1,4-Butanediol, 1B-LSD, 1cP-AL-LAD and 573 more
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