Baclofen

Baclofen
Clinical data
Trade namesLioresal, 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-life2.5 to 7 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
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) Y
  • Key:KPYSYYIEGFHWSV-UHFFFAOYSA-N Y
  (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. It may also be used for hiccups and muscle spasms near the end of life, and off-label to treat alcohol use disorder or opioid withdrawal symptoms. It is taken orally or by intrathecal pump (delivered into the spinal canal via an implantable pump device). It is sometimes used transdermally (applied topically to the skin) in combination with gabapentin and clonidine prepared at a compounding pharmacy. It is believed to work by decreasing levels of certain neurotransmitters.

Baclofen should be avoided in the setting of chronic kidney disease and end stage renal disease as even small doses can cause excessive toxicity. Common side effects include sleepiness, weakness, and dizziness. Serious side effects, such as seizures and rhabdomyolysis, may occur if use of baclofen is stopped abruptly. Use during pregnancy is of unclear safety, whilst use during breastfeeding is likely safe, and even more so if oral administration is avoided.

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. In high doses the interaction can cause de novo seizures.

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