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Baclofen information


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
  • US DailyMed: Baclofen
Pregnancy
category
  • AU: B3
Routes of
administration
oral, intrathecal, transdermal
ATC code
  • M03BX01 (WHO)
Legal status
Legal status
  • AU: S4 (Prescription only)
  • UK: POM (Prescription only)
  • US: WARNING[1]Rx-only[2][3][4][5][6]
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
IUPAC name
  • (RS)-4-Amino-3-(4-chlorophenyl)butanoic acid
CAS Number
  • 1134-47-0 checkY
PubChem CID
  • 2284
IUPHAR/BPS
  • 1084
DrugBank
  • DB00181 checkY
ChemSpider
  • 2197 checkY
UNII
  • H789N3FKE8
KEGG
  • D00241 checkY
ChEBI
  • CHEBI:2972 checkY
ChEMBL
  • ChEMBL701 checkY
CompTox Dashboard (EPA)
  • DTXSID5022641 Edit this at Wikidata
ECHA InfoCard100.013.170 Edit this at Wikidata
Chemical and physical data
FormulaC10H12ClNO2
Molar mass213.66 g·mol−1
3D model (JSmol)
  • Interactive image
ChiralityRacemic mixture
SMILES
  • NCC(CC(=O)O)c1ccc(Cl)cc1
InChI
  • 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.[7][8] It may also be used for hiccups and muscle spasms near the end of life,[8] and off-label to treat alcohol use disorder[9][10] or opioid withdrawal symptoms.[11] It is taken orally (swallowed by mouth) or by intrathecal pump (delivered into the spinal canal via an implantable pump device).[7] It is also sometimes used transdermally (applied topically to the skin) in combination with gabapentin and clonidine prepared at a compounding pharmacy.[12]

Common side effects include sleepiness, weakness, and dizziness.[7] Serious side effects may occur if baclofen is rapidly stopped including seizures and rhabdomyolysis.[7] Use in pregnancy is of unclear safety while use during breastfeeding is probably safe.[13] It is believed to work by decreasing levels of certain neurotransmitters.[7]

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.[14] In high doses the interaction can cause de novo seizures.[15]

Baclofen was approved for medical use in the United States in 1977.[7] It is available as a generic medication.[8][16] In 2021, it was the 103rd most commonly prescribed medication in the United States, with more than 6 million prescriptions.[17][18]

  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. ^ Cite error: The named reference Gablofen FDA label was invoked but never defined (see the help page).
  3. ^ "Lioresal- baclofen injection". DailyMed. Retrieved 7 November 2021.
  4. ^ "Ozobax- baclofen solution". DailyMed. Retrieved 7 November 2021.
  5. ^ "Lyvispah- baclofen granule". DailyMed. Retrieved 19 December 2021.
  6. ^ "Fleqsuvy- baclofen suspension". DailyMed. 4 February 2022. Retrieved 16 March 2022.
  7. ^ a b c d e f "Baclofen Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Retrieved 3 March 2019.
  8. ^ a b c British national formulary : BNF 76 (76 ed.). Pharmaceutical Press. 2018. p. 1092. ISBN 978-0-85711-338-2.
  9. ^ 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.
  10. ^ 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.
  11. ^ 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.
  12. ^ 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.
  13. ^ "Baclofen Pregnancy and Breastfeeding Warnings". Drugs.com. Retrieved 3 March 2019.
  14. ^ "Common questions about baclofen". nhs.uk. 3 March 2022. Retrieved 24 March 2024.
  15. ^ "Seizures Following High-Dose Baclofen With Alcohol". Medscape. Retrieved 24 March 2024.
  16. ^ "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.
  17. ^ "The Top 300 of 2021". ClinCalc. Archived from the original on 15 January 2024. Retrieved 14 January 2024.
  18. ^ "Baclofen - Drug Usage Statistics". ClinCalc. Retrieved 14 January 2024.

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Baclofen

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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...

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Intrathecal administration

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orally-administered baclofen. Intrathecal baclofen also carries none of the side effects, such as sleepiness, that typically occur with oral baclofen. However,...

Word Count : 714

Intrathecal pump

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the protective sheath surrounding the spinal cord. Medications such as baclofen, bupivacaine, clonidine, morphine, hydromorphone, fentanyl or ziconotide...

Word Count : 440

Phenibut

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Phenibut is thought to act as a GABAB receptor agonist, similarly to baclofen and γ-hydroxybutyrate (GHB). However, at low concentrations, phenibut mildly...

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Tizanidine

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sclerosis, and spastic cerebral palsy. Effectiveness appears similar to baclofen or diazepam. It is taken by mouth. Common side effects of tizanidine include...

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Depressant

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benzodiazepine) and a number of opioids. Gabapentinoids like gabapentin and baclofen are depressants and have anticonvulsant, and anxiolytic effects. Most anticonvulsants...

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Dystonia

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sizes. A baclofen pump has been used to treat patients of all ages exhibiting muscle spasticity along with dystonia. The pump delivers baclofen via a catheter...

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Spasticity

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exaggerated deep tendon reflex. Spasticity is often treated with the drug baclofen, which acts as an agonist at GABA receptors, which are inhibitory. Spastic...

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Antispasmodic

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has not been clearly shown for metaxalone, methocarbamol, chlorzoxazone, baclofen, or dantrolene. Applicable conditions include acute back or neck pain,...

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Muscle relaxant

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tetrazepam and other benzodiazepines, mephenoxalone, methocarbamol, dantrolene, baclofen. Drugs once but no longer or very rarely used to relax skeletal muscles...

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GABAB receptor

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determined by Norman Bowery and his team using radioactively labelled baclofen. GABABRs stimulate the opening of K+ channels, specifically GIRKs, which...

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Arbaclofen placarbil

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XP19986) is a prodrug of R-baclofen. Arbaclofen placarbil possesses more favorable pharmacokinetic profile than baclofen, with less fluctuations in plasma...

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Tolibut

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(GABA) and is the 4-methyl analogue of phenibut, and is also an analogue of baclofen where the 4-chloro substitution has been replaced with a 4-methyl substitution...

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Spastic diplegia

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are:[citation needed] Baclofen (and its derivatives), a gamma amino butyric acid (GABA) substitute in oral (pill-based) or intrathecal form. Baclofen is essentially...

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Hypertonia

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avoided. Baclofen, diazepam and dantrolene remain the three most commonly used pharmacologic agents in the treatment of spastic hypertonia. Baclofen is generally...

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GABA receptor

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of the GABAA receptor. The most striking discovery was the finding that baclofen (β-parachlorophenyl GABA), a clinically employed muscle relaxant mimicked...

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Gabapentinoid

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(R)-phenibut, >1 mM for (S)-phenibut, and 6 μM for baclofen. Based on the low affinity of baclofen for the α2δ subunit relative to the GABAB (26-fold...

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Ketamine

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(gabapentinoids): 4-Methylpregabalin Arbaclofen Arbaclofen placarbil Atagabalin Baclofen Gabapentin Gabapentin enacarbil Imagabalin Mirogabalin PD-200,347 PD-217...

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Cerebral palsy

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has been available in China since 2003. Medications such as diazepam, baclofen and botulinum toxin may help relax stiff muscles. Surgery may include lengthening...

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Trigeminal neuralgia

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withdrawal in as many as 23% of patients. Other options include lamotrigine, baclofen, gabapentin, amitriptyline and pimozide. Opioids are not usually effective...

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Lesogaberan

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of action as baclofen, but is anticipated to have fewer of the central nervous system side effects that limit the clinical use of baclofen for the treatment...

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Jamais vu

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Struck, Terry H. (June 2002). "Jamais vu episodes in relationship to baclofen treatment: A case report". Archives of Physical Medicine and Rehabilitation...

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Homotaurine

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full agonists GABA and baclofen at this receptor. In a study in rats, homotaurine reversed the catatonia induced by baclofen (the prototypical GABAB...

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Olivier Ameisen

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cardiologist who wrote a best-selling book about curing alcoholism using the drug baclofen. Ameisen began his medical studies in 1969 at age 16 at Université René...

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Alcoholism

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alcohol withdrawal severity as well as improving quality-of-life-ratings. Baclofen, a GABAB receptor agonist, is under study for the treatment of alcoholism...

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Status dystonicus

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be difficult but status dystonicus may respond to midazolam, propofol, baclofen and bilateral pallidal deep brain stimulation. Mariotti, P.; Fasano, A...

Word Count : 134

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