Baclofen

Baclofen
Clinical data
Trade names	Lioresal, Liofen, Gablofen, others
Other names	β-(4-chlorophenyl)-γ-aminobutyric acid (β-(4-chlorophenyl)-GABA)
AHFS/Drugs.com	Monograph
MedlinePlus	a682530
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: WARNINGRx-only;
Pharmacokinetic data
Bioavailability	Well-absorbed
Protein binding	30%
Metabolism	85% excreted in urine/faeces unchanged. 15% metabolised by deamination
Elimination half-life	1.5 to 4 hours
Excretion	Kidney (70–80%)
Identifiers
	IUPAC name (RS)-4-Amino-3-(4-chlorophenyl)butanoic acid;
CAS Number	1134-47-0 ;
PubChem CID	2284;
IUPHAR/BPS	1084;
DrugBank	DB00181 ;
ChemSpider	2197 ;
UNII	H789N3FKE8;
KEGG	D00241 ;
ChEBI	CHEBI:2972 ;
ChEMBL	ChEMBL701 ;
CompTox Dashboard (EPA)	DTXSID5022641 ;
ECHA InfoCard	100.013.170
Chemical and physical data
Formula	C10H12ClNO2
Molar mass	213.66 g·mol−1
3D model (JSmol)	Interactive image;
Chirality	Racemic 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) ; Key:KPYSYYIEGFHWSV-UHFFFAOYSA-N ;
	(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 (swallowed by mouth) or by intrathecal pump (delivered into the spinal canal via an implantable pump device). It is also sometimes used transdermally (applied topically to the skin) in combination with gabapentin and clonidine prepared at a compounding pharmacy.

Common side effects include sleepiness, weakness, and dizziness. Serious side effects may occur if baclofen is rapidly stopped including seizures and rhabdomyolysis. Use in pregnancy is of unclear safety while use during breastfeeding is probably safe. It is believed to work by decreasing levels of certain neurotransmitters. The adverse effects and safety profile associated with baclofen when it is combined with sedative drugs (for example alcohol or benzodiazepines) are unknown.

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

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