Baclofen

Baclofen
Clinical data
Trade namesLioresal, Liofen, Gablofen, others
Other namesβ-(4-chlorophenyl)-γ-aminobutyric acid (β-(4-chlorophenyl)-GABA)
AHFS/Drugs.comMonograph
MedlinePlusa682530
License data
Pregnancy
category
  • AU: B3
Routes of
administration		oral, intrathecal, transdermal
ATC code
Legal status
Legal status
Pharmacokinetic data
BioavailabilityWell-absorbed
Protein binding30%
Metabolism85% excreted in urine/faeces unchanged. 15% metabolised by deamination
Elimination half-life1.5 to 4 hours
ExcretionKidney (70–80%)
Identifiers
  • (RS)-4-Amino-3-(4-chlorophenyl)butanoic acid
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.013.170 Edit this at Wikidata
Chemical and physical data
FormulaC10H12ClNO2
Molar mass213.66 g·mol−1
3D model (JSmol)
ChiralityRacemic mixture
  • NCC(CC(=O)O)c1ccc(Cl)cc1
  • InChI=1S/C10H12ClNO2/c11-9-3-1-7(2-4-9)8(6-12)5-10(13)14/h1-4,8H,5-6,12H2,(H,13,14) checkY
  • Key:KPYSYYIEGFHWSV-UHFFFAOYSA-N checkY
  (verify)

Baclofen, sold under the brand name Lioresal among others, is a medication used to treat muscle spasticity such as from a spinal cord injury or multiple sclerosis.[8][9] It may also be used for hiccups and muscle spasms near the end of life,[9] and off-label to treat alcohol use disorder[10][11] or opioid withdrawal symptoms.[12] It is taken orally (swallowed by mouth) or by intrathecal pump (delivered into the spinal canal via an implantable pump device).[8] It is also sometimes used transdermally (applied topically to the skin) in combination with gabapentin and clonidine prepared at a compounding pharmacy.[13]

Common side effects include sleepiness, weakness, and dizziness.[8] Serious side effects may occur if baclofen is rapidly stopped including seizures and rhabdomyolysis.[8] Use in pregnancy is of unclear safety while use during breastfeeding is probably safe.[14] It is believed to work by decreasing levels of certain neurotransmitters.[8]

The adverse effects and safety profile associated with baclofen when it is combined with sedative drugs (for example alcohol or benzodiazepines) range depending on the dose and the individual. The interaction may increase the sedative effects of all ingested sedatives and as such is not generally recommended.[15] In high doses the interaction can cause de novo seizures.[16]

Baclofen was approved for medical use in the United States in 1977.[8] It is available as a generic medication.[9][17] In 2022, it was the 104th most commonly prescribed medication in the United States, with more than 6 million prescriptions.[18][19]

  1. ^ "FDA-sourced list of all drugs with black box warnings (Use Download Full Results and View Query links.)". nctr-crs.fda.gov. FDA. Retrieved 22 October 2023.
  2. ^ "Product monograph brand safety updates". Health Canada. 6 June 2024. Retrieved 8 June 2024.
  3. ^ Cite error: The named reference Gablofen FDA label was invoked but never defined (see the help page).
  4. ^ "Lioresal- baclofen injection". DailyMed. Retrieved 7 November 2021.
  5. ^ "Ozobax- baclofen solution". DailyMed. Retrieved 7 November 2021.
  6. ^ "Lyvispah- baclofen granule". DailyMed. Retrieved 19 December 2021.
  7. ^ "Fleqsuvy- baclofen suspension". DailyMed. 4 February 2022. Retrieved 16 March 2022.
  8. ^ a b c d e f "Baclofen Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Retrieved 3 March 2019.
  9. ^ a b c British national formulary : BNF 76 (76 ed.). Pharmaceutical Press. 2018. p. 1092. ISBN 978-0-85711-338-2.
  10. ^ Agabio R, Saulle R, Rösner S, Minozzi S (January 2023). "Baclofen for alcohol use disorder". The Cochrane Database of Systematic Reviews. 1 (1): CD012557. doi:10.1002/14651858.cd012557.pub3. PMC 9837849. PMID 36637087.
  11. ^ Ahmadi-Abhari SA, Akhondzadeh S, Assadi SM, Shabestari OL, Farzanehgan ZM, Kamlipour A (February 2001). "Baclofen versus clonidine in the treatment of opiates withdrawal, side-effects aspect: a double-blind randomized controlled trial". Journal of Clinical Pharmacy and Therapeutics. 26 (1): 67–71. doi:10.1111/j.1365-2710.2001.00325.x. PMID 11286609. S2CID 28295723.
  12. ^ Assadi SM, Radgoodarzi R, Ahmadi-Abhari SA (November 2003). "Baclofen for maintenance treatment of opioid dependence: a randomized double-blind placebo-controlled clinical trial [ISRCTN32121581]". BMC Psychiatry. 3: 16. doi:10.1186/1471-244X-3-16. PMC 293465. PMID 14624703.
  13. ^ Allen Jr LV (17 November 2010). "Baclofen 2%, Gabapentin 6%, and Clonidine Hydrochloride 0.1% in Pluronic Lecithin Organogel". U.S. Pharmacist. Jobson Medical Information LLC. Retrieved 9 August 2023.
  14. ^ "Baclofen Pregnancy and Breastfeeding Warnings". Drugs.com. Retrieved 3 March 2019.
  15. ^ "Common questions about baclofen". nhs.uk. 3 March 2022. Retrieved 24 March 2024.
  16. ^ "Seizures Following High-Dose Baclofen With Alcohol". Medscape. Retrieved 24 March 2024.
  17. ^ "Competitive Generic Therapy Approvals". U.S. Food and Drug Administration (FDA). 29 June 2023. Archived from the original on 29 June 2023. Retrieved 29 June 2023.
  18. ^ "The Top 300 of 2022". ClinCalc. Archived from the original on 30 August 2024. Retrieved 30 August 2024.
  19. ^ "Baclofen Drug Usage Statistics, United States, 2013 - 2022". ClinCalc. Retrieved 30 August 2024.