Identification
NameBaclofen
Accession NumberDB00181  (APRD00551)
TypeSmall Molecule
GroupsApproved
Description

Baclofen is a gamma-amino-butyric acid (GABA) derivative used as a skeletal muscle relaxant. Baclofen stimulates GABA-B receptors leading to decreased frequency and amplitude of muscle spasms. It is especially useful in treating muscle spasticity associated with spinal cord injury. It appears to act primarily at the spinal cord level by inhibiting spinal polysynaptic afferent pathways and, to a lesser extent, monosynaptic afferent pathways.

Structure
Thumb
Synonyms
(+-)-Baclofen
4-Amino-3-(4-chlorophenyl)butyric acid
Baclofene
Baclofeno
Baclofenum
beta-(4-Chlorophenyl)gaba
beta-(Aminomethyl)-4-chlorobenzenepropanoic acid
beta-(Aminomethyl)-P-chlorohydrocinnamic acid
beta-(P-Chlorophenyl)-gamma-aminobutyric acid
DL-4-Amino-3-P-chlorophenylbutanoic acid
DL-Baclofen
gamma-Amino-beta-(P-chlorophenyl)butyric acid
External IDs Not Available
Product Ingredients
IngredientUNIICASInChI KeyDetails
Baclofen hydrochloride64OSE3996V 28311-31-1WMNUVYYLMCMHLU-UHFFFAOYSA-NDetails
Product Images
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Ava-baclofenTablet10 mgOralAvanstra Inc2011-10-112014-08-21Canada
Ava-baclofenTablet20 mgOralAvanstra Inc2011-10-112014-08-21Canada
BaclofenTablet10 mgOralSanis Health Inc2010-02-25Not applicableCanada
BaclofenTablet10 mgOralApotex Corporation1994-12-312014-08-23Canada
BaclofenTablet20 mgOralSanis Health Inc2010-02-25Not applicableCanada
BaclofenTablet20 mgOralApotex Corporation1994-12-312014-08-23Canada
Baclofen InjectionSolution0.05 mgIntrathecalTeligent OuNot applicableNot applicableCanada
Baclofen InjectionSolution0.5 mgIntrathecalTeligent OuNot applicableNot applicableCanada
Baclofen InjectionSolution2 mgIntrathecalTeligent OuNot applicableNot applicableCanada
Baclofen Tablets - 10mgTablet10 mgOralBdh Inc.1995-12-312000-08-03Canada
Baclofen Tablets - 20mgTablet20 mgOralBdh Inc.1995-12-312000-08-03Canada
Baclofen Tablets 10mgTablet10 mgOralPrempharm Inc1997-01-052005-08-05Canada
Baclofen Tablets 20mgTablet20 mgOralPrempharm Inc1997-01-052005-08-05Canada
Baclofen-10 - TabTablet10 mgOralPro Doc Limitee1996-12-31Not applicableCanada
Baclofen-20 - TabTablet20 mgOralPro Doc Limitee1996-12-31Not applicableCanada
Co Baclofen Tablets 10mgTablet10 mgOralCobalt LaboratoriesNot applicableNot applicableCanada
Co Baclofen Tablets 20mgTablet20 mgOralCobalt LaboratoriesNot applicableNot applicableCanada
Dom-baclofen-tab 10mgTablet10 mgOralDominion Pharmacal1995-12-31Not applicableCanada
Dom-baclofen-tab 20mgTablet20 mgOralDominion Pharmacal1995-12-31Not applicableCanada
Ftp-baclofenTablet20 mgOralFtp Pharmacal Inc.1998-10-092004-08-03Canada
Ftp-baclofenTablet10 mgOralFtp Pharmacal Inc.1998-10-092004-08-03Canada
GablofenInjection500 ug/mLIntrathecalMallinckrodt Inc (Brand Pharmaceuticals)2010-11-19Not applicableUs
GablofenInjection, solution500 ug/mLIntrathecalPiramal Critical Care Inc2017-04-01Not applicableUs
GablofenInjection50 ug/mLIntrathecalMallinckrodt Inc (Brand Pharmaceuticals)2010-11-19Not applicableUs
GablofenInjection, solution1000 ug/mLIntrathecalPiramal Critical Care Inc2017-04-01Not applicableUs
GablofenInjection1000 ug/mLIntrathecalMallinckrodt Inc (Brand Pharmaceuticals)2012-07-10Not applicableUs
GablofenInjection, solution50 ug/mLIntrathecalPiramal Critical Care Inc2017-04-01Not applicableUs
GablofenInjection, solution2000 ug/mLIntrathecalPiramal Critical Care Inc2017-04-01Not applicableUs
GablofenInjection2000 ug/mLIntrathecalMallinckrodt Inc (Brand Pharmaceuticals)2010-11-19Not applicableUs
LioresalInjection.5 mg/mLIntrathecalMedtronic Neuromodulation1992-06-17Not applicableUs
LioresalInjection2 mg/mLIntrathecalMedtronic Neuromodulation2003-05-08Not applicableUs
LioresalInjection2 mg/mLIntrathecalMedtronic Neuromodulation1992-06-17Not applicableUs
LioresalInjection.05 mg/mLIntrathecalMedtronic Neuromodulation1996-11-07Not applicableUs
Lioresal (baclofen)Injection40 mg/20mLIntrathecalSaol Therapeutics Inc.2017-04-04Not applicableUs
Lioresal (baclofen)Injection.05 mg/mLIntrathecalSaol Therapeutics Inc.2017-04-04Not applicableUs
Lioresal (baclofen)Injection10 mg/20mLIntrathecalSaol Therapeutics Inc.2017-07-05Not applicableUs
Lioresal (baclofen)Injection10 mg/5mLIntrathecalSaol Therapeutics Inc.2017-07-05Not applicableUs
Lioresal D.S. Tab 20mgTablet20 mgOralNovartis1985-12-31Not applicableCanada
Lioresal Intrathecal 0.05mg/mlSolution0.05 mgIntrathecalNovartis1994-12-31Not applicableCanada
Lioresal Intrathecal 0.5mg/mlSolution0.5 mgIntrathecalNovartis1994-12-31Not applicableCanada
Lioresal Intrathecal 2mg/mlSolution2 mgIntrathecalNovartis1994-12-31Not applicableCanada
Lioresal Tab 10mgTablet10 mgOralNovartis1978-12-31Not applicableCanada
Med Baclofen Tab 10mgTablet10 mgOralMedican Pharma Incorporated1995-12-312011-03-29Canada
Med Baclofen Tab 20mgTablet20 mgOralMedican Pharma Incorporated1995-12-312011-03-29Canada
Mylan-baclofenTablet20 mgOralMylan Pharmaceuticals1994-12-31Not applicableCanada
Mylan-baclofenTablet10 mgOralMylan Pharmaceuticals1994-12-31Not applicableCanada
Novo-baclofenTablet10 mgOralNovopharm Limited1997-01-312015-10-26Canada
Novo-baclofenTablet20 mgOralNovopharm Limited1997-01-312015-10-26Canada
Penta-baclofen TabletsTablet10 mgOralPentapharm Ltd.Not applicableNot applicableCanada
Penta-baclofen TabletsTablet20 mgOralPentapharm Ltd.Not applicableNot applicableCanada
PHL-baclofenTablet10 mgOralPharmel Inc1998-02-16Not applicableCanada
PHL-baclofenTablet20 mgOralPharmel Inc1998-02-16Not applicableCanada
PMS-baclofenTablet10 mgOralPharmascience Inc1994-12-31Not applicableCanada
PMS-baclofen Tab 20mgTablet20 mgOralPharmascience Inc1994-12-31Not applicableCanada
Ratio-baclofenTablet20 mgOralTeva1997-12-16Not applicableCanada
Ratio-baclofenTablet10 mgOralTeva1997-12-16Not applicableCanada
Riva-baclofenTablet10 mgOralLaboratoire Riva Inc2003-03-03Not applicableCanada
Riva-baclofenTablet20 mgOralLaboratoire Riva Inc2003-03-03Not applicableCanada
Sandoz BaclofenTablet20 mgOralSandoz Canada IncorporatedNot applicableNot applicableCanada
Sandoz BaclofenTablet10 mgOralSandoz Canada IncorporatedNot applicableNot applicableCanada
Val-baclofen IntrathecalSolution0.05 mgIntrathecalValeant Canada Lp Valeant Canada S.E.C.2014-06-06Not applicableCanada
Val-baclofen IntrathecalSolution0.5 mgIntrathecalValeant Canada Lp Valeant Canada S.E.C.2014-06-06Not applicableCanada
Val-baclofen IntrathecalSolution2 mgIntrathecalValeant Canada Lp Valeant Canada S.E.C.2014-06-06Not applicableCanada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-baclofen Tablets - 10mgTablet10 mgOralApotex Corporation1994-12-31Not applicableCanada
Apo-baclofen Tablets - 20mgTablet20 mgOralApotex Corporation1994-12-31Not applicableCanada
BaclofenTablet20 mg/1OralLake Erie Medical Dba Quality Care Produts Llc2005-12-01Not applicableUs
BaclofenTablet10 mg/1OralPd Rx Pharmaceuticals, Inc.1988-07-21Not applicableUs
BaclofenTablet10 mg/1OralMajor1998-07-21Not applicableUs
BaclofenTablet10 mg/1OralUnit Dose Services1988-07-21Not applicableUs
BaclofenTablet10 mg/1OralMarlex Pharmaceuticals Inc2014-12-01Not applicableUs
BaclofenTablet20 mg/1OralRebel Distributors2010-07-15Not applicableUs
BaclofenTablet20 mg/1OralH.J. Harkins Company2010-07-15Not applicableUs
BaclofenTablet10 mg/1OralCardinal Health2015-07-15Not applicableUs
BaclofenTablet10 mg/1OralRemedy Repack2015-03-202017-04-14Us
BaclofenTablet20 mg/1OralProficient Rx LP2005-12-01Not applicableUs
BaclofenTablet20 mg/1OralRebel Distributors2004-07-01Not applicableUs
BaclofenTablet10 mg/1OralCardinal Health2007-07-01Not applicableUs
BaclofenTablet20 mg/1OralLake Erie Medical Dba Quality Care Produts Llc2010-11-152017-01-26Us
BaclofenTablet10 mg/1OralRemedy Repack2011-10-10Not applicableUs
BaclofenTablet20 mg/1OralCardinal Health1988-07-212017-04-14Us
BaclofenTablet10 mg/1OralMylan Pharmaceuticals2010-02-18Not applicableUs
BaclofenTablet20 mg/1OralNu Care Pharmaceuticals,inc.2005-12-01Not applicableUs
BaclofenTablet20 mg/1OralCardinal Health2015-07-15Not applicableUs
BaclofenTablet20 mg/1OralMc Kesson Contract Packaging2011-12-12Not applicableUs
BaclofenTablet20 mg/1OralRemedy Repack2015-06-152017-04-14Us
BaclofenTablet10 mg/1OralA S Medication Solutions2011-01-012017-06-20Us
BaclofenTablet10 mg/1OralPreferreed Pharmaceuticals Inc.2014-10-22Not applicableUs
BaclofenTablet20 mg/1OralMc Kesson Packaging Services A Buisness Unit Of Mc Kesson Corporation2005-12-01Not applicableUs
BaclofenTablet20 mg/1OralTeva1988-07-21Not applicableUs
BaclofenTablet20 mg/1OralMc Kesson Packaging Services A Buisness Unit Of Mc Kesson Corporation2011-01-01Not applicableUs
BaclofenTablet20 mg/1OralLake Erie Medical &Surgical Supply Dba Quality Care Products Llc2010-10-20Not applicableUs
BaclofenInjection.05 mg/mLIntrathecalSintetica s.a.2016-05-09Not applicableUs
BaclofenTablet20 mg/1OralRemedy Repack2013-02-112017-01-25Us
BaclofenTablet10 mg/1OralLake Erie Medical Dba Quality Care Produts Llc1988-07-21Not applicableUs
BaclofenTablet10 mg/1OralNew Horizon Rx Group, LLC2013-08-25Not applicableUs
BaclofenTablet20 mg/1OralQualitest2005-08-30Not applicableUs00603 2407 21 nlmimage10 e023707b
BaclofenTablet20 mg/1Oralbryant ranch prepack2005-08-30Not applicableUs
BaclofenTablet20 mg/1OralDirectrx2014-01-01Not applicableUs
BaclofenTablet10 mg/1OralA S Medication Solutions2005-08-302017-06-20Us
BaclofenTablet20 mg/1OralUnit Dose Services1988-07-21Not applicableUs
BaclofenTablet20 mg/1OralClinical Solutions Wholsesale2010-10-20Not applicableUs
BaclofenTablet20 mg/1OralMajor2015-07-15Not applicableUs
BaclofenTablet20 mg/1OralRemedy Repack2017-04-07Not applicableUs
BaclofenTablet10 mg/1OralStat Rx USA1991-09-18Not applicableUs
BaclofenTablet20 mg/1OralAv Kare, Inc.2014-08-25Not applicableUs
BaclofenTablet10 mg/1OralState of Florida DOH Central Pharmacy2014-01-01Not applicableUs
BaclofenTablet20 mg/1OralNorth Star Rx Llc2011-01-01Not applicableUs
BaclofenTablet10 mg/1OralRemedy Repack2012-03-152016-10-15Us
BaclofenTablet10 mg/1OralCardinal Health2010-07-15Not applicableUs00904 3365 61 nlmimage10 0e328774
BaclofenTablet20 mg/1OralPd Rx Pharmaceuticals, Inc.2005-08-30Not applicableUs
BaclofenTablet20 mg/1OralAmerincan Health Packaging2012-09-032016-02-29Us
BaclofenTablet20 mg/1OralSt. Marys Medical Park Pharmacy2012-04-01Not applicableUs
BaclofenTablet10 mg/1OralPreferreed Pharmaceuticals Inc.2012-03-28Not applicableUs
BaclofenTablet20 mg/1OralPreferreed Pharmaceuticals Inc.2016-05-04Not applicableUs
BaclofenTablet10 mg/1OralAmerincan Health Packaging2015-02-15Not applicableUs
BaclofenTablet10 mg/1OralUpsher Smith Laboratories2010-10-20Not applicableUs
BaclofenTablet20 mg/1OralPreferreed Pharmaceuticals Inc.2017-02-22Not applicableUs
BaclofenTablet10 mg/1Oralbryant ranch prepack2005-08-30Not applicableUs
BaclofenTablet10 mg/1OralAmerincan Health Packaging2012-09-032015-12-29Us
BaclofenTablet10 mg/1OralRemedy Repack2015-12-162017-06-20Us
BaclofenTablet10 mg/1OralA S Medication Solutions2005-08-302017-06-20Us
BaclofenTablet20 mg/1OralA S Medication Solutions1988-07-212017-06-20Us
BaclofenTablet10 mg/1OralNucare Pharmaceuticals, Inc.2007-07-01Not applicableUs
BaclofenTablet20 mg/1OralMajor1998-07-21Not applicableUs
BaclofenTablet20 mg/1OralUnit Dose Services1988-07-21Not applicableUs00172 4097 60 nlmimage10 7b26bde5
BaclofenTablet20 mg/1OralMarlex Pharmaceuticals Inc2014-12-01Not applicableUs
BaclofenTablet10 mg/1OralRebel Distributors2010-07-15Not applicableUs
BaclofenTablet10 mg/1OralH.J. Harkins Company2010-07-15Not applicableUs
BaclofenTablet20 mg/1OralNucare Pharmaceuticals, Inc.2005-12-01Not applicableUs
BaclofenTablet10 mg/1OralProficient Rx LP1988-07-21Not applicableUs
BaclofenTablet20 mg/1OralA S Medication Solutions1988-07-212017-06-20Us
BaclofenTablet10 mg/1OralProficient Rx LP2005-12-01Not applicableUs
BaclofenTablet10 mg/1OralAidarex Pharmaceuticals LLC2005-08-30Not applicableUs
BaclofenTablet10 mg/1OralLake Erie Medical Dba Quality Care Produts Llc2007-07-01Not applicableUs
BaclofenTablet10 mg/1OralMed Pharma Co., Ltd.2011-01-01Not applicableUs
BaclofenTablet10 mg/1OralDirectrx2014-01-01Not applicableUs
BaclofenTablet10 mg/1OralClinical Solutions Wholsesale2010-10-202017-07-01Us00832 1024 00 nlmimage10 6e233779
BaclofenTablet20 mg/1OralMylan Pharmaceuticals2010-02-18Not applicableUs
BaclofenTablet10 mg/1OralA S Medication Solutions2007-07-012017-06-20Us
BaclofenTablet20 mg/1OralStat Rx USA1991-09-18Not applicableUs
BaclofenTablet10 mg/1OralRemedy Repack2011-04-042016-10-13Us
BaclofenTablet20 mg/1OralPhysicians Total Care, Inc.2009-04-17Not applicableUs
BaclofenTablet10 mg/1OralRemedy Repack2017-05-18Not applicableUs
BaclofenTablet20 mg/1OralDispensing Solutions, Inc.2005-08-30Not applicableUs
BaclofenTablet10 mg/1OralLannett Company, Inc.2007-07-01Not applicableUs
BaclofenTablet20 mg/1OralPreferreed Pharmaceuticals Inc.2012-04-30Not applicableUs
BaclofenInjection10 mg/20mLIntrathecalSintetica s.a.2016-05-09Not applicableUs
BaclofenTablet20 mg/1OralLake Erie Medical Dba Quality Care Produts Llc1988-07-21Not applicableUs
BaclofenTablet10 mg/1OralNcs Health Care Of Ky, Inc Dba Vangard Labs2010-07-15Not applicableUs
BaclofenTablet20 mg/1OralA S Medication Solutions2005-12-012017-06-20Us
BaclofenTablet10 mg/1OralRebel Distributors2004-07-01Not applicableUs
BaclofenTablet10 mg/1OralLake Erie Medical Dba Quality Care Produts Llc2010-05-19Not applicableUs
BaclofenTablet20 mg/1OralCardinal Health1998-07-21Not applicableUs
BaclofenTablet10 mg/1OralSt. Marys Medical Park Pharmacy2014-01-15Not applicableUs
BaclofenTablet10 mg/1OralMc Kesson Contract Packaging2011-11-14Not applicableUs
BaclofenTablet10 mg/1OralRemedy Repack2015-01-26Not applicableUs
BaclofenTablet10 mg/1OralA S Medication Solutions1988-07-212017-06-20Us
BaclofenTablet10 mg/1OralUnit Dose Services1988-07-21Not applicableUs
BaclofenTablet20 mg/1OralAmerincan Health Packaging2015-02-15Not applicableUs
BaclofenTablet20 mg/1OralUpsher Smith Laboratories2010-10-20Not applicableUs
BaclofenTablet20 mg/1OralRemedy Repack2014-12-03Not applicableUs
BaclofenTablet20 mg/1OralAidarex Pharmaceuticals LLC2005-08-30Not applicableUs
BaclofenTablet20 mg/1OralProficient Rx LP1988-07-21Not applicableUs
BaclofenTablet20 mg/1OralMed Pharma Co., Ltd.2011-01-01Not applicableUs
BaclofenTablet20 mg/1OralDirectrx2014-01-01Not applicableUs
BaclofenTablet10 mg/1OralClinical Solutions Wholsesale2010-10-202017-07-01Us00832 1025 00 nlmimage10 73233989
BaclofenTablet10 mg/1OralQualitest2005-08-30Not applicableUs
BaclofenTablet10 mg/1OralRemedy Repack2017-02-10Not applicableUs
BaclofenTablet20 mg/1Oralbryant ranch prepack2005-08-30Not applicableUs
BaclofenTablet20 mg/1OralAvera Mc Kennan Hospital2015-03-31Not applicableUs
BaclofenTablet10 mg/1OralDirectrx2014-01-01Not applicableUs
BaclofenTablet20 mg/1OralA S Medication Solutions2005-08-302017-06-20Us
BaclofenTablet20 mg/1OralUnit Dose Services1988-07-21Not applicableUs
BaclofenTablet10 mg/1OralClinical Solutions Wholsesale2010-10-20Not applicableUs
BaclofenTablet10 mg/1OralMajor2015-07-15Not applicableUs
BaclofenTablet10 mg/1OralRemedy Repack2017-03-24Not applicableUs
BaclofenTablet10 mg/1OralBlenheim Pharmacal, Inc.2013-11-15Not applicableUs
BaclofenTablet10 mg/1OralAv Kare, Inc.2014-08-25Not applicableUs00527 1330 10 nlmimage10 874443c2
BaclofenTablet20 mg/1OralState of Florida DOH Central Pharmacy2014-01-01Not applicableUs
BaclofenTablet10 mg/1OralPreferreed Pharmaceuticals Inc.2004-07-01Not applicableUs
BaclofenTablet10 mg/1OralMc Kesson Packaging Services A Buisness Unit Of Mc Kesson Corporation2007-07-01Not applicableUs
BaclofenTablet10 mg/1OralTeva1988-07-21Not applicableUs
BaclofenTablet10 mg/1OralMc Kesson Packaging Services A Buisness Unit Of Mc Kesson Corporation2011-01-01Not applicableUs
BaclofenTablet10 mg/1OralNorth Star Rx Llc2011-01-01Not applicableUs
BaclofenTablet10 mg/1OralRemedy Repack2012-03-132017-02-22Us00172 4096 60 nlmimage10 b726dbe6
BaclofenTablet10 mg/1OralPhysicians Total Care, Inc.2010-03-05Not applicableUs
BaclofenTablet10 mg/1Oralbryant ranch prepack1988-07-21Not applicableUs
BaclofenTablet10 mg/1OralDispensing Solutions, Inc.2005-08-30Not applicableUs
BaclofenTablet20 mg/1OralLannett Company, Inc.2005-12-01Not applicableUs
BaclofenTablet10 mg/1OralPreferreed Pharmaceuticals Inc.2012-04-30Not applicableUs00603 2406 21 nlmimage10 92204932
BaclofenInjection40 mg/20mLIntrathecalSintetica s.a.2016-05-09Not applicableUs
BaclofenTablet10 mg/1OralAtlantic Biologicals Corps.2010-10-20Not applicableUs
BaclofenTablet20 mg/1OralNcs Health Care Of Ky, Inc Dba Vangard Labs2010-07-15Not applicableUs
BaclofenTablet10 mg/1OralRemedy Repack2016-03-25Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Equipto - Baclofen External Cream Compounding KitKitTopicalAlvix Laboratories2015-01-20Not applicableUs
International Brands
NameCompany
BaclonUniao Quimica (Brazil)
KemstroSchwarz (United States)
Lioresal IntrathecalNovartis Pharmaceuticals
Nu-BaclofenNu-Pharm
Brand mixtures
NameLabellerIngredients
Gapeam BudibacAlvix Laboratories
Categories
UNIIH789N3FKE8
CAS number1134-47-0
WeightAverage: 213.661
Monoisotopic: 213.05565634
Chemical FormulaC10H12ClNO2
InChI KeyKPYSYYIEGFHWSV-UHFFFAOYSA-N
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)
IUPAC Name
4-amino-3-(4-chlorophenyl)butanoic acid
SMILES
NCC(CC(O)=O)C1=CC=C(Cl)C=C1
Pharmacology
Indication

For the alleviation of signs and symptoms of spasticity resulting from multiple sclerosis, particularly for the relief of flexor spasms and concomitant pain, clonus, and muscular rigidity.

Structured Indications
Pharmacodynamics

Baclofen is a muscle relaxant and antispastic. Baclofen is useful for the alleviation of signs and symptoms of spasticity resulting from multiple sclerosis, particularly for the relief of flexor spasms and concomitant pain, clonus, and muscular rigidity. Although Baclofen is an analog of the putative inhibitory neurotransmitter gamma-aminobutyric acid (GABA), there is no conclusive evidence that actions on GABA systems are involved in the production of its clinical effects. In studies with animals, Baclofen has been shown to have general CNS depressant properties as indicated by the production of sedation with tolerance, somnolence, ataxia, and respiratory and cardiovascular depression. Baclofen is rapidly and extensively absorbed and eliminated. Absorption may be dose-dependent, being reduced with increasing doses. Baclofen is excreted primarily by the kidney in unchanged form and there is relatively large intersubject variation in absorption and/or elimination.

Mechanism of action

Baclofen is a direct agonist at GABAB receptors. The precise mechanism of action of Baclofen is not fully known. It is capable of inhibiting both monosynaptic and polysynaptic reflexes at the spinal level, possibly by hyperpolarization of afferent terminals, although actions at supraspinal sites may also occur and contribute to its clinical effect.

TargetKindPharmacological actionActionsOrganismUniProt ID
Gamma-aminobutyric acid type B receptor subunit 1Proteinyes
agonist
HumanQ9UBS5 details
Gamma-aminobutyric acid type B receptor subunit 2Proteinyes
agonist
HumanO75899 details
Related Articles
Absorption

Rapidly and almost completely absorbed from the GI tract.

Volume of distribution
  • 59 L
Protein binding

30%

Metabolism

~ 15% of the dose is metabolized in the liver, primarily by deamination. 70-80% of the dose is excreted unchanged or as metabolites in urine and the remainder is excreted in feces.

Route of elimination

In a study using radiolabeled baclofen, approximately 85% of the dose was excreted unchanged in the urine and feces. Baclofen is excreted primarily by the kidney as unchanged drug; 70 - 80% of a dose appears in the urine as unchanged drug. The remainder is excreted as unchanged drug in the feces or as metabolites in the urine and feces.

Half life

2.5-4 hours

Clearance
  • 180 mL/min
Toxicity

LD50=45 mg/kg (male mice, IV); LD50=78 mg/kg (male rat, IV)

Affected organisms
  • Humans and other mammals
PathwaysNot Available
Pharmacogenomic Effects/ADRs Not Available
Interactions
Drug Interactions
DrugInteractionDrug group
7-NitroindazoleThe risk or severity of adverse effects can be increased when 7-Nitroindazole is combined with Baclofen.Experimental
AcepromazineThe risk or severity of adverse effects can be increased when Acepromazine is combined with Baclofen.Approved, Vet Approved
AceprometazineThe risk or severity of adverse effects can be increased when Aceprometazine is combined with Baclofen.Approved
AdipiplonThe risk or severity of adverse effects can be increased when adipiplon is combined with Baclofen.Investigational
AgomelatineThe risk or severity of adverse effects can be increased when Agomelatine is combined with Baclofen.Approved, Investigational
AlfaxaloneThe risk or severity of adverse effects can be increased when Alfaxalone is combined with Baclofen.Vet Approved
AlfentanilThe risk or severity of adverse effects can be increased when Alfentanil is combined with Baclofen.Approved, Illicit
AllopregnanoloneThe risk or severity of adverse effects can be increased when Baclofen is combined with Sage 547.Investigational
AlphacetylmethadolThe risk or severity of adverse effects can be increased when Alphacetylmethadol is combined with Baclofen.Experimental, Illicit
AlprazolamThe risk or severity of adverse effects can be increased when Alprazolam is combined with Baclofen.Approved, Illicit, Investigational
AmisulprideThe risk or severity of adverse effects can be increased when Amisulpride is combined with Baclofen.Approved, Investigational
AmitriptylineThe risk or severity of adverse effects can be increased when Baclofen is combined with Amitriptyline.Approved
AmobarbitalThe risk or severity of adverse effects can be increased when Amobarbital is combined with Baclofen.Approved, Illicit
AmoxapineThe risk or severity of adverse effects can be increased when Baclofen is combined with Amoxapine.Approved
AmperozideThe risk or severity of adverse effects can be increased when Amperozide is combined with Baclofen.Experimental
AripiprazoleThe risk or severity of adverse effects can be increased when Aripiprazole is combined with Baclofen.Approved, Investigational
ArticaineThe risk or severity of adverse effects can be increased when Articaine is combined with Baclofen.Approved
AsenapineThe risk or severity of adverse effects can be increased when Asenapine is combined with Baclofen.Approved
AzelastineBaclofen may increase the central nervous system depressant (CNS depressant) activities of Azelastine.Approved
AzelastineThe risk or severity of adverse effects can be increased when Baclofen is combined with Azelastine.Approved
BarbitalThe risk or severity of adverse effects can be increased when Barbital is combined with Baclofen.Illicit
BenperidolThe risk or severity of adverse effects can be increased when Baclofen is combined with Benperidol.Investigational
BenzocaineThe risk or severity of adverse effects can be increased when Benzocaine is combined with Baclofen.Approved
Benzyl alcoholThe risk or severity of adverse effects can be increased when Benzyl alcohol is combined with Baclofen.Approved
BrexpiprazoleThe risk or severity of adverse effects can be increased when Baclofen is combined with Brexpiprazole.Approved
BrimonidineThe risk or severity of adverse effects can be increased when Baclofen is combined with Brimonidine.Approved
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Baclofen.Approved
BromazepamThe risk or severity of adverse effects can be increased when Bromazepam is combined with Baclofen.Approved, Illicit
BrompheniramineThe risk or severity of adverse effects can be increased when Baclofen is combined with Brompheniramine.Approved
BrotizolamThe risk or severity of adverse effects can be increased when Brotizolam is combined with Baclofen.Approved, Withdrawn
BupivacaineThe risk or severity of adverse effects can be increased when Bupivacaine is combined with Baclofen.Approved, Investigational
BuprenorphineBaclofen may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.Approved, Illicit, Investigational, Vet Approved
BuspironeThe risk or severity of adverse effects can be increased when Buspirone is combined with Baclofen.Approved, Investigational
ButabarbitalThe risk or severity of adverse effects can be increased when Butabarbital is combined with Baclofen.Approved, Illicit
ButalbitalThe risk or severity of adverse effects can be increased when Baclofen is combined with Butalbital.Approved, Illicit
ButethalThe risk or severity of adverse effects can be increased when Butethal is combined with Baclofen.Approved, Illicit
ButorphanolThe risk or severity of adverse effects can be increased when Butorphanol is combined with Baclofen.Approved, Illicit, Vet Approved
CarbamazepineThe risk or severity of adverse effects can be increased when Carbamazepine is combined with Baclofen.Approved, Investigational
CarbinoxamineThe risk or severity of adverse effects can be increased when Baclofen is combined with Carbinoxamine.Approved
CarfentanilThe risk or severity of adverse effects can be increased when Carfentanil is combined with Baclofen.Illicit, Vet Approved
CarisoprodolThe risk or severity of adverse effects can be increased when Baclofen is combined with Carisoprodol.Approved
CetirizineThe risk or severity of adverse effects can be increased when Baclofen is combined with Cetirizine.Approved
Chloral hydrateThe risk or severity of adverse effects can be increased when Chloral hydrate is combined with Baclofen.Approved, Illicit, Vet Approved
ChlordiazepoxideThe risk or severity of adverse effects can be increased when Chlordiazepoxide is combined with Baclofen.Approved, Illicit
ChlormezanoneThe risk or severity of adverse effects can be increased when Chlormezanone is combined with Baclofen.Approved, Withdrawn
ChloroprocaineThe risk or severity of adverse effects can be increased when Chloroprocaine is combined with Baclofen.Approved
ChlorphenamineThe risk or severity of adverse effects can be increased when Baclofen is combined with Chlorphenamine.Approved
ChlorpromazineThe risk or severity of adverse effects can be increased when Chlorpromazine is combined with Baclofen.Approved, Vet Approved
ChlorprothixeneThe risk or severity of adverse effects can be increased when Chlorprothixene is combined with Baclofen.Approved, Withdrawn
ChlorzoxazoneThe risk or severity of adverse effects can be increased when Baclofen is combined with Chlorzoxazone.Approved
CinchocaineThe risk or severity of adverse effects can be increased when Cinchocaine is combined with Baclofen.Approved, Vet Approved
CitalopramThe risk or severity of adverse effects can be increased when Baclofen is combined with Citalopram.Approved
ClemastineThe risk or severity of adverse effects can be increased when Baclofen is combined with Clemastine.Approved
ClidiniumThe risk or severity of adverse effects can be increased when Baclofen is combined with Clidinium.Approved
ClobazamThe risk or severity of adverse effects can be increased when Baclofen is combined with Clobazam.Approved, Illicit
ClomipramineThe risk or severity of adverse effects can be increased when Baclofen is combined with Clomipramine.Approved, Vet Approved
ClonazepamThe risk or severity of adverse effects can be increased when Baclofen is combined with Clonazepam.Approved, Illicit
ClonidineThe risk or severity of adverse effects can be increased when Baclofen is combined with Clonidine.Approved
ClorazepateThe risk or severity of adverse effects can be increased when Clorazepate is combined with Baclofen.Approved, Illicit
ClozapineThe risk or severity of adverse effects can be increased when Clozapine is combined with Baclofen.Approved
CocaineThe risk or severity of adverse effects can be increased when Cocaine is combined with Baclofen.Approved, Illicit
CodeineThe risk or severity of adverse effects can be increased when Codeine is combined with Baclofen.Approved, Illicit
CyclizineThe risk or severity of adverse effects can be increased when Baclofen is combined with Cyclizine.Approved
CyclobenzaprineThe risk or severity of adverse effects can be increased when Cyclobenzaprine is combined with Baclofen.Approved
CyproheptadineThe risk or severity of adverse effects can be increased when Baclofen is combined with Cyproheptadine.Approved
DantroleneThe risk or severity of adverse effects can be increased when Baclofen is combined with Dantrolene.Approved
DapiprazoleThe risk or severity of adverse effects can be increased when Dapiprazole is combined with Baclofen.Approved
DapoxetineThe risk or severity of adverse effects can be increased when Baclofen is combined with Dapoxetine.Investigational
DeramciclaneThe risk or severity of adverse effects can be increased when deramciclane is combined with Baclofen.Investigational
DesfluraneThe risk or severity of adverse effects can be increased when Desflurane is combined with Baclofen.Approved
DesipramineThe risk or severity of adverse effects can be increased when Baclofen is combined with Desipramine.Approved
DesloratadineThe risk or severity of adverse effects can be increased when Baclofen is combined with Desloratadine.Approved, Investigational
DesvenlafaxineThe risk or severity of adverse effects can be increased when Baclofen is combined with Desvenlafaxine.Approved
DexbrompheniramineThe risk or severity of adverse effects can be increased when Baclofen is combined with Dexbrompheniramine.Approved
DexmedetomidineThe risk or severity of adverse effects can be increased when Dexmedetomidine is combined with Baclofen.Approved, Vet Approved
DextromoramideThe risk or severity of adverse effects can be increased when Dextromoramide is combined with Baclofen.Experimental, Illicit
DextropropoxypheneThe risk or severity of adverse effects can be increased when Dextropropoxyphene is combined with Baclofen.Approved, Illicit, Withdrawn
DezocineThe risk or severity of adverse effects can be increased when Dezocine is combined with Baclofen.Approved
DiazepamThe risk or severity of adverse effects can be increased when Diazepam is combined with Baclofen.Approved, Illicit, Vet Approved
DifenoxinThe risk or severity of adverse effects can be increased when Baclofen is combined with Difenoxin.Approved, Illicit
DihydrocodeineThe risk or severity of adverse effects can be increased when Dihydrocodeine is combined with Baclofen.Approved, Illicit
DihydroetorphineThe risk or severity of adverse effects can be increased when Dihydroetorphine is combined with Baclofen.Experimental, Illicit
DihydromorphineThe risk or severity of adverse effects can be increased when Dihydromorphine is combined with Baclofen.Experimental, Illicit
DimenhydrinateThe risk or severity of adverse effects can be increased when Baclofen is combined with Dimenhydrinate.Approved
DiphenhydramineThe risk or severity of adverse effects can be increased when Diphenhydramine is combined with Baclofen.Approved
DiphenoxylateThe risk or severity of adverse effects can be increased when Diphenoxylate is combined with Baclofen.Approved, Illicit
DoxepinThe risk or severity of adverse effects can be increased when Baclofen is combined with Doxepin.Approved
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Baclofen.Approved, Vet Approved
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Baclofen.Approved, Illicit
DroperidolDroperidol may increase the central nervous system depressant (CNS depressant) activities of Baclofen.Approved, Vet Approved
DrotebanolThe risk or severity of adverse effects can be increased when Drotebanol is combined with Baclofen.Experimental, Illicit
DuloxetineThe risk or severity of adverse effects can be increased when Baclofen is combined with Duloxetine.Approved
DyclonineThe risk or severity of adverse effects can be increased when Dyclonine is combined with Baclofen.Approved
EcgonineThe risk or severity of adverse effects can be increased when Ecgonine is combined with Baclofen.Experimental, Illicit
EcopipamThe risk or severity of adverse effects can be increased when Baclofen is combined with Ecopipam.Investigational
EfavirenzThe risk or severity of adverse effects can be increased when Baclofen is combined with Efavirenz.Approved, Investigational
EltanoloneThe risk or severity of adverse effects can be increased when Baclofen is combined with Pregnanolone.Investigational
EnfluraneThe risk or severity of adverse effects can be increased when Enflurane is combined with Baclofen.Approved, Vet Approved
EntacaponeThe risk or severity of adverse effects can be increased when Baclofen is combined with Entacapone.Approved, Investigational
EscitalopramThe risk or severity of adverse effects can be increased when Baclofen is combined with Escitalopram.Approved, Investigational
EstazolamThe risk or severity of adverse effects can be increased when Estazolam is combined with Baclofen.Approved, Illicit
EszopicloneThe risk or severity of adverse effects can be increased when Eszopiclone is combined with Baclofen.Approved
EthanolBaclofen may increase the central nervous system depressant (CNS depressant) activities of Ethanol.Approved
EthchlorvynolThe risk or severity of adverse effects can be increased when Ethchlorvynol is combined with Baclofen.Approved, Illicit, Withdrawn
EthosuximideThe risk or severity of adverse effects can be increased when Baclofen is combined with Ethosuximide.Approved
EthotoinThe risk or severity of adverse effects can be increased when Baclofen is combined with Ethotoin.Approved
Ethyl carbamateThe risk or severity of adverse effects can be increased when Ethyl carbamate is combined with Baclofen.Withdrawn
Ethyl loflazepateThe risk or severity of adverse effects can be increased when Ethyl loflazepate is combined with Baclofen.Approved, Illicit
EthylmorphineThe risk or severity of adverse effects can be increased when Ethylmorphine is combined with Baclofen.Approved, Illicit
EtidocaineThe risk or severity of adverse effects can be increased when Etidocaine is combined with Baclofen.Approved
EtifoxineThe risk or severity of adverse effects can be increased when Etifoxine is combined with Baclofen.Withdrawn
EtizolamThe risk or severity of adverse effects can be increased when Etizolam is combined with Baclofen.Approved
EtomidateThe risk or severity of adverse effects can be increased when Etomidate is combined with Baclofen.Approved
EtoperidoneThe risk or severity of adverse effects can be increased when Baclofen is combined with Etoperidone.Approved
EtorphineThe risk or severity of adverse effects can be increased when Etorphine is combined with Baclofen.Illicit, Vet Approved
EzogabineThe risk or severity of adverse effects can be increased when Baclofen is combined with Ezogabine.Approved
FelbamateThe risk or severity of adverse effects can be increased when Baclofen is combined with Felbamate.Approved
FencamfamineThe risk or severity of adverse effects can be increased when Fencamfamine is combined with Baclofen.Approved, Illicit, Withdrawn
FentanylThe risk or severity of adverse effects can be increased when Fentanyl is combined with Baclofen.Approved, Illicit, Investigational, Vet Approved
FexofenadineThe risk or severity of adverse effects can be increased when Baclofen is combined with Fexofenadine.Approved
FlibanserinThe risk or severity of adverse effects can be increased when Baclofen is combined with Flibanserin.Approved
FludiazepamThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Baclofen.Approved, Illicit
FlunarizineThe risk or severity of adverse effects can be increased when Baclofen is combined with Flunarizine.Approved
FlunitrazepamThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Baclofen.Approved, Illicit
FluoxetineThe risk or severity of adverse effects can be increased when Baclofen is combined with Fluoxetine.Approved, Vet Approved
FlupentixolThe risk or severity of adverse effects can be increased when Flupentixol is combined with Baclofen.Approved, Withdrawn
FluphenazineThe risk or severity of adverse effects can be increased when Fluphenazine is combined with Baclofen.Approved
FlurazepamThe risk or severity of adverse effects can be increased when Flurazepam is combined with Baclofen.Approved, Illicit
FluspirileneThe risk or severity of adverse effects can be increased when Fluspirilene is combined with Baclofen.Approved
Fluticasone propionateThe risk or severity of adverse effects can be increased when Baclofen is combined with Fluticasone Propionate.Approved
FluvoxamineThe risk or severity of adverse effects can be increased when Fluvoxamine is combined with Baclofen.Approved, Investigational
FosphenytoinThe risk or severity of adverse effects can be increased when Baclofen is combined with Fosphenytoin.Approved
FospropofolThe risk or severity of adverse effects can be increased when Fospropofol is combined with Baclofen.Approved, Illicit
GabapentinThe risk or severity of adverse effects can be increased when Gabapentin is combined with Baclofen.Approved, Investigational
Gabapentin EnacarbilThe risk or severity of adverse effects can be increased when Baclofen is combined with gabapentin enacarbil.Approved
Gamma Hydroxybutyric AcidThe risk or severity of adverse effects can be increased when Gamma Hydroxybutyric Acid is combined with Baclofen.Approved, Illicit
GepironeThe risk or severity of adverse effects can be increased when Baclofen is combined with Gepirone.Investigational
GlutethimideThe risk or severity of adverse effects can be increased when Glutethimide is combined with Baclofen.Approved, Illicit
GuanfacineThe risk or severity of adverse effects can be increased when Baclofen is combined with Guanfacine.Approved, Investigational
HalazepamThe risk or severity of adverse effects can be increased when Halazepam is combined with Baclofen.Approved, Illicit, Withdrawn
HaloperidolThe risk or severity of adverse effects can be increased when Haloperidol is combined with Baclofen.Approved
HalothaneThe risk or severity of adverse effects can be increased when Halothane is combined with Baclofen.Approved, Vet Approved
HeroinThe risk or severity of adverse effects can be increased when Heroin is combined with Baclofen.Approved, Illicit
HexobarbitalThe risk or severity of adverse effects can be increased when Hexobarbital is combined with Baclofen.Approved
HydrocodoneBaclofen may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.Approved, Illicit
HydromorphoneThe risk or severity of adverse effects can be increased when Hydromorphone is combined with Baclofen.Approved, Illicit
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Baclofen.Approved
IloperidoneThe risk or severity of adverse effects can be increased when Baclofen is combined with Iloperidone.Approved
ImipramineThe risk or severity of adverse effects can be increased when Baclofen is combined with Imipramine.Approved
IndalpineThe risk or severity of adverse effects can be increased when Baclofen is combined with Indalpine.Investigational, Withdrawn
IsofluraneThe risk or severity of adverse effects can be increased when Isoflurane is combined with Baclofen.Approved, Vet Approved
KetamineThe risk or severity of adverse effects can be increased when Ketamine is combined with Baclofen.Approved, Vet Approved
KetazolamThe risk or severity of adverse effects can be increased when Ketazolam is combined with Baclofen.Approved
KetobemidoneThe risk or severity of adverse effects can be increased when Ketobemidone is combined with Baclofen.Approved
LacidipineBaclofen may increase the hypotensive activities of Lacidipine.Approved
LamotrigineThe risk or severity of adverse effects can be increased when Baclofen is combined with Lamotrigine.Approved, Investigational
LevetiracetamThe risk or severity of adverse effects can be increased when Baclofen is combined with Levetiracetam.Approved, Investigational
LevobupivacaineThe risk or severity of adverse effects can be increased when Levobupivacaine is combined with Baclofen.Approved
LevocabastineThe risk or severity of adverse effects can be increased when Baclofen is combined with Levocabastine.Approved
LevocetirizineThe risk or severity of adverse effects can be increased when Baclofen is combined with Levocetirizine.Approved
LevodopaThe risk or severity of adverse effects can be increased when Baclofen is combined with Levodopa.Approved
Levomethadyl AcetateThe risk or severity of adverse effects can be increased when Levomethadyl Acetate is combined with Baclofen.Approved
LevomilnacipranThe risk or severity of adverse effects can be increased when Baclofen is combined with Levomilnacipran.Approved
LevorphanolThe risk or severity of adverse effects can be increased when Levorphanol is combined with Baclofen.Approved
LidocaineThe risk or severity of adverse effects can be increased when Lidocaine is combined with Baclofen.Approved, Vet Approved
LithiumThe risk or severity of adverse effects can be increased when Lithium is combined with Baclofen.Approved
LofentanilThe risk or severity of adverse effects can be increased when Lofentanil is combined with Baclofen.Illicit
LoratadineThe risk or severity of adverse effects can be increased when Baclofen is combined with Loratadine.Approved
LorazepamThe risk or severity of adverse effects can be increased when Lorazepam is combined with Baclofen.Approved
LoxapineThe risk or severity of adverse effects can be increased when Loxapine is combined with Baclofen.Approved
LurasidoneThe risk or severity of adverse effects can be increased when Lurasidone is combined with Baclofen.Approved
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Baclofen.Approved, Vet Approved
MaprotilineThe risk or severity of adverse effects can be increased when Baclofen is combined with Maprotiline.Approved
MeclizineThe risk or severity of adverse effects can be increased when Baclofen is combined with Meclizine.Approved
MelatoninThe risk or severity of adverse effects can be increased when Melatonin is combined with Baclofen.Approved, Nutraceutical, Vet Approved
MelperoneThe risk or severity of adverse effects can be increased when Melperone is combined with Baclofen.Approved
MepivacaineThe risk or severity of adverse effects can be increased when Mepivacaine is combined with Baclofen.Approved, Vet Approved
MeprobamateThe risk or severity of adverse effects can be increased when Meprobamate is combined with Baclofen.Approved, Illicit
MesoridazineThe risk or severity of adverse effects can be increased when Mesoridazine is combined with Baclofen.Approved
MetaxaloneThe risk or severity of adverse effects can be increased when Baclofen is combined with Metaxalone.Approved
MethadoneThe risk or severity of adverse effects can be increased when Methadone is combined with Baclofen.Approved
Methadyl AcetateThe risk or severity of adverse effects can be increased when Methadyl Acetate is combined with Baclofen.Approved, Illicit
MethapyrileneThe risk or severity of adverse effects can be increased when Methapyrilene is combined with Baclofen.Withdrawn
MethaqualoneThe risk or severity of adverse effects can be increased when Methaqualone is combined with Baclofen.Illicit, Withdrawn
MethocarbamolThe risk or severity of adverse effects can be increased when Baclofen is combined with Methocarbamol.Approved, Vet Approved
MethohexitalThe risk or severity of adverse effects can be increased when Methohexital is combined with Baclofen.Approved
MethotrimeprazineBaclofen may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.Approved
MethoxyfluraneThe risk or severity of adverse effects can be increased when Methoxyflurane is combined with Baclofen.Approved, Vet Approved
MethsuximideThe risk or severity of adverse effects can be increased when Baclofen is combined with Methsuximide.Approved
MethylecgonineThe risk or severity of adverse effects can be increased when ECGONINE METHYL ESTER is combined with Baclofen.Experimental
MethylphenobarbitalThe risk or severity of adverse effects can be increased when Methylphenobarbital is combined with Baclofen.Approved
MetyrosineBaclofen may increase the sedative activities of Metyrosine.Approved
MidazolamThe risk or severity of adverse effects can be increased when Midazolam is combined with Baclofen.Approved, Illicit
MilnacipranThe risk or severity of adverse effects can be increased when Baclofen is combined with Milnacipran.Approved
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Baclofen.Approved, Investigational
MirtazapineBaclofen may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.Approved
MolindoneThe risk or severity of adverse effects can be increased when Molindone is combined with Baclofen.Approved
MorphineThe risk or severity of adverse effects can be increased when Morphine is combined with Baclofen.Approved, Investigational
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Baclofen.Approved, Investigational
NalbuphineThe risk or severity of adverse effects can be increased when Nalbuphine is combined with Baclofen.Approved
NefazodoneThe risk or severity of adverse effects can be increased when Baclofen is combined with Nefazodone.Approved, Withdrawn
NitrazepamThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Baclofen.Approved
Nitrous oxideThe risk or severity of adverse effects can be increased when Nitrous oxide is combined with Baclofen.Approved, Vet Approved
NorfluraneThe risk or severity of adverse effects can be increased when Baclofen is combined with 1,1,1,2 Tetrafluoroethane.Investigational
NormethadoneThe risk or severity of adverse effects can be increased when Normethadone is combined with Baclofen.Approved, Illicit
NortriptylineThe risk or severity of adverse effects can be increased when Baclofen is combined with Nortriptyline.Approved
OlanzapineThe risk or severity of adverse effects can be increased when Olanzapine is combined with Baclofen.Approved, Investigational
OlopatadineThe risk or severity of adverse effects can be increased when Baclofen is combined with Olopatadine.Approved
OndansetronThe risk or severity of adverse effects can be increased when Ondansetron is combined with Baclofen.Approved
OpiumThe risk or severity of adverse effects can be increased when Opium is combined with Baclofen.Approved, Illicit
OrphenadrineBaclofen may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
OsanetantThe risk or severity of adverse effects can be increased when Osanetant is combined with Baclofen.Investigational
OxazepamThe risk or severity of adverse effects can be increased when Oxazepam is combined with Baclofen.Approved
OxethazaineThe risk or severity of adverse effects can be increased when Baclofen is combined with Oxetacaine.Investigational
OxprenololThe risk or severity of adverse effects can be increased when Oxprenolol is combined with Baclofen.Approved
OxybuprocaineThe risk or severity of adverse effects can be increased when Oxybuprocaine is combined with Baclofen.Approved
OxycodoneThe risk or severity of adverse effects can be increased when Oxycodone is combined with Baclofen.Approved, Illicit, Investigational
OxymorphoneThe risk or severity of adverse effects can be increased when Oxymorphone is combined with Baclofen.Approved, Investigational, Vet Approved
PaliperidoneThe risk or severity of adverse effects can be increased when Paliperidone is combined with Baclofen.Approved
ParaldehydeBaclofen may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.Approved
ParoxetineThe risk or severity of adverse effects can be increased when Baclofen is combined with Paroxetine.Approved, Investigational
PentazocineThe risk or severity of adverse effects can be increased when Pentazocine is combined with Baclofen.Approved, Vet Approved
PentobarbitalThe risk or severity of adverse effects can be increased when Pentobarbital is combined with Baclofen.Approved, Vet Approved
PerampanelPerampanel may increase the central nervous system depressant (CNS depressant) activities of Baclofen.Approved
PerazineThe risk or severity of adverse effects can be increased when Baclofen is combined with Perazine.Investigational
PerospironeThe risk or severity of adverse effects can be increased when Perospirone is combined with Baclofen.Approved
PerphenazineThe risk or severity of adverse effects can be increased when Perphenazine is combined with Baclofen.Approved
PethidineThe risk or severity of adverse effects can be increased when Pethidine is combined with Baclofen.Approved
PhenobarbitalThe risk or severity of adverse effects can be increased when Phenobarbital is combined with Baclofen.Approved
PhenytoinThe risk or severity of adverse effects can be increased when Baclofen is combined with Phenytoin.Approved, Vet Approved
PimozideThe risk or severity of adverse effects can be increased when Pimozide is combined with Baclofen.Approved
PipamperoneThe risk or severity of adverse effects can be increased when Pipamperone is combined with Baclofen.Approved
PipotiazineThe risk or severity of adverse effects can be increased when Baclofen is combined with Pipotiazine.Approved
PiritramideThe risk or severity of adverse effects can be increased when Baclofen is combined with Piritramide.Investigational
PomalidomideThe risk or severity of adverse effects can be increased when Baclofen is combined with Pomalidomide.Approved
PramipexoleBaclofen may increase the sedative activities of Pramipexole.Approved, Investigational
PramocaineThe risk or severity of adverse effects can be increased when Pramocaine is combined with Baclofen.Approved
PrazepamThe risk or severity of adverse effects can be increased when Prazepam is combined with Baclofen.Approved, Illicit
PregabalinThe risk or severity of adverse effects can be increased when Pregabalin is combined with Baclofen.Approved, Illicit, Investigational
PrilocaineThe risk or severity of adverse effects can be increased when Prilocaine is combined with Baclofen.Approved
PrimidoneThe risk or severity of adverse effects can be increased when Baclofen is combined with Primidone.Approved, Vet Approved
ProcaineThe risk or severity of adverse effects can be increased when Procaine is combined with Baclofen.Approved, Investigational, Vet Approved
ProchlorperazineThe risk or severity of adverse effects can be increased when Prochlorperazine is combined with Baclofen.Approved, Vet Approved
PromazineThe risk or severity of adverse effects can be increased when Promazine is combined with Baclofen.Approved, Vet Approved
PromethazineThe risk or severity of adverse effects can be increased when Baclofen is combined with Promethazine.Approved
ProparacaineThe risk or severity of adverse effects can be increased when Proparacaine is combined with Baclofen.Approved, Vet Approved
PropofolThe risk or severity of adverse effects can be increased when Propofol is combined with Baclofen.Approved, Investigational, Vet Approved
PropoxycaineThe risk or severity of adverse effects can be increased when Propoxycaine is combined with Baclofen.Approved
ProtriptylineThe risk or severity of adverse effects can be increased when Baclofen is combined with Protriptyline.Approved
QuazepamThe risk or severity of adverse effects can be increased when Quazepam is combined with Baclofen.Approved, Illicit
QuetiapineThe risk or severity of adverse effects can be increased when Quetiapine is combined with Baclofen.Approved
RacloprideThe risk or severity of adverse effects can be increased when Baclofen is combined with Raclopride.Investigational
RamelteonThe risk or severity of adverse effects can be increased when Baclofen is combined with Ramelteon.Approved, Investigational
RemifentanilThe risk or severity of adverse effects can be increased when Remifentanil is combined with Baclofen.Approved
RemoxiprideThe risk or severity of adverse effects can be increased when Remoxipride is combined with Baclofen.Approved, Withdrawn
ReserpineThe risk or severity of adverse effects can be increased when Reserpine is combined with Baclofen.Approved
RisperidoneThe risk or severity of adverse effects can be increased when Risperidone is combined with Baclofen.Approved, Investigational
RitanserinThe risk or severity of adverse effects can be increased when Baclofen is combined with Ritanserin.Investigational
RopiniroleBaclofen may increase the sedative activities of Ropinirole.Approved, Investigational
RopivacaineThe risk or severity of adverse effects can be increased when Ropivacaine is combined with Baclofen.Approved
RotigotineBaclofen may increase the sedative activities of Rotigotine.Approved
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Baclofen.Approved
ScopolamineThe risk or severity of adverse effects can be increased when Baclofen is combined with Scopolamine.Approved
SecobarbitalThe risk or severity of adverse effects can be increased when Secobarbital is combined with Baclofen.Approved, Vet Approved
SepranoloneThe risk or severity of adverse effects can be increased when Baclofen is combined with Uc1010.Investigational
SertindoleThe risk or severity of adverse effects can be increased when Sertindole is combined with Baclofen.Approved, Withdrawn
SertralineThe risk or severity of adverse effects can be increased when Baclofen is combined with Sertraline.Approved
SevofluraneThe risk or severity of adverse effects can be increased when Sevoflurane is combined with Baclofen.Approved, Vet Approved
Sodium oxybateSodium oxybate may increase the central nervous system depressant (CNS depressant) activities of Baclofen.Approved
StiripentolThe risk or severity of adverse effects can be increased when Baclofen is combined with Stiripentol.Approved
SufentanilThe risk or severity of adverse effects can be increased when Sufentanil is combined with Baclofen.Approved, Investigational
SulpirideThe risk or severity of adverse effects can be increased when Sulpiride is combined with Baclofen.Approved
SuvorexantBaclofen may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.Approved
TandospironeThe risk or severity of adverse effects can be increased when Baclofen is combined with Tandospirone.Investigational
TapentadolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Baclofen.Approved
TasimelteonThe risk or severity of adverse effects can be increased when Baclofen is combined with Tasimelteon.Approved
TemazepamThe risk or severity of adverse effects can be increased when Temazepam is combined with Baclofen.Approved
TetrabenazineThe risk or severity of adverse effects can be increased when Baclofen is combined with Tetrabenazine.Approved
TetracaineThe risk or severity of adverse effects can be increased when Tetracaine is combined with Baclofen.Approved, Vet Approved
TetrodotoxinThe risk or severity of adverse effects can be increased when Tetrodotoxin is combined with Baclofen.Investigational
ThalidomideBaclofen may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.Approved, Investigational, Withdrawn
ThiamylalThe risk or severity of adverse effects can be increased when Thiamylal is combined with Baclofen.Approved, Vet Approved
ThiopentalThe risk or severity of adverse effects can be increased when Thiopental is combined with Baclofen.Approved, Vet Approved
ThioridazineThe risk or severity of adverse effects can be increased when Thioridazine is combined with Baclofen.Withdrawn
ThiothixeneThe risk or severity of adverse effects can be increased when Thiothixene is combined with Baclofen.Approved
TiagabineThe risk or severity of adverse effects can be increased when Baclofen is combined with Tiagabine.Approved
TiaprideThe risk or severity of adverse effects can be increased when Baclofen is combined with Tiapride.Approved, Investigational
TizanidineThe risk or severity of adverse effects can be increased when Baclofen is combined with Tizanidine.Approved
TolcaponeThe risk or severity of adverse effects can be increased when Baclofen is combined with Tolcapone.Approved, Withdrawn
TopiramateThe risk or severity of adverse effects can be increased when Baclofen is combined with Topiramate.Approved
TramadolThe risk or severity of adverse effects can be increased when Tramadol is combined with Baclofen.Approved, Investigational
Trans-2-PhenylcyclopropylamineThe risk or severity of adverse effects can be increased when Trans-2-Phenylcyclopropylamine is combined with Baclofen.Experimental
TranylcypromineThe risk or severity of adverse effects can be increased when Tranylcypromine is combined with Baclofen.Approved
TrazodoneThe risk or severity of adverse effects can be increased when Trazodone is combined with Baclofen.Approved, Investigational
TriazolamThe risk or severity of adverse effects can be increased when Triazolam is combined with Baclofen.Approved
TrifluoperazineThe risk or severity of adverse effects can be increased when Trifluoperazine is combined with Baclofen.Approved
TriflupromazineThe risk or severity of adverse effects can be increased when Triflupromazine is combined with Baclofen.Approved, Vet Approved
TrimipramineThe risk or severity of adverse effects can be increased when Baclofen is combined with Trimipramine.Approved
TriprolidineThe risk or severity of adverse effects can be increased when Baclofen is combined with Triprolidine.Approved
Valproic AcidThe risk or severity of adverse effects can be increased when Valproic Acid is combined with Baclofen.Approved, Investigational
VenlafaxineThe risk or severity of adverse effects can be increased when Baclofen is combined with Venlafaxine.Approved
VigabatrinThe risk or severity of adverse effects can be increased when Baclofen is combined with Vigabatrin.Approved
VortioxetineThe risk or severity of adverse effects can be increased when Vortioxetine is combined with Baclofen.Approved
ZaleplonThe risk or severity of adverse effects can be increased when Zaleplon is combined with Baclofen.Approved, Illicit, Investigational
ZiconotideThe risk or severity of adverse effects can be increased when Baclofen is combined with Ziconotide.Approved
ZimelidineThe risk or severity of adverse effects can be increased when Baclofen is combined with Zimelidine.Withdrawn
ZiprasidoneThe risk or severity of adverse effects can be increased when Ziprasidone is combined with Baclofen.Approved
ZolpidemBaclofen may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.Approved
ZonisamideThe risk or severity of adverse effects can be increased when Baclofen is combined with Zonisamide.Approved, Investigational
ZopicloneThe risk or severity of adverse effects can be increased when Zopiclone is combined with Baclofen.Approved
ZotepineThe risk or severity of adverse effects can be increased when Zotepine is combined with Baclofen.Approved
ZuclopenthixolThe risk or severity of adverse effects can be increased when Zuclopenthixol is combined with Baclofen.Approved, Investigational
Food Interactions
  • Avoid alcohol.
  • Take without regard to meals.
References
Synthesis Reference

Wayne Levadoux, Denis Groleau, Michael Trani, Robert Lortie, "Streptomyces microorganism useful for the preparation of (R)-baclofen from the racemic mixture." U.S. Patent US5843765, issued April, 1994.

US5843765
General References
  1. Dzitoyeva S, Dimitrijevic N, Manev H: Gamma-aminobutyric acid B receptor 1 mediates behavior-impairing actions of alcohol in Drosophila: adult RNA interference and pharmacological evidence. Proc Natl Acad Sci U S A. 2003 Apr 29;100(9):5485-90. Epub 2003 Apr 11. [PubMed:12692303 ]
  2. Mezler M, Muller T, Raming K: Cloning and functional expression of GABA(B) receptors from Drosophila. Eur J Neurosci. 2001 Feb;13(3):477-86. [PubMed:11168554 ]
  3. See S, Ginzburg R: Skeletal muscle relaxants. Pharmacotherapy. 2008 Feb;28(2):207-13. doi: 10.1592/phco.28.2.207. [PubMed:18225966 ]
External Links
ATC CodesM03BX01 — Baclofen
AHFS Codes
  • 12:20.12
PDB EntriesNot Available
FDA labelDownload (135 KB)
MSDSDownload (73.4 KB)
Clinical Trials
Clinical Trials
PhaseStatusPurposeConditionsCount
0Not Yet RecruitingTreatmentOsteoarthritis of the Hands1
0RecruitingTreatmentDrug Abuse1
0Unknown StatusTreatmentAtaxia Telangiectasia (AT)1
1CompletedNot AvailableHealthy Volunteers / Obese, Otherwise Healthy Volunteers1
1CompletedBasic ScienceAlcohol Dependence1
1CompletedTreatmentAlcohol Dependence1
1CompletedTreatmentBaclofen Withdrawal Syndrome1
1CompletedTreatmentCHEYNE Stokes Respiration1
1CompletedTreatmentHealthy Volunteers1
1CompletedTreatmentSafety and Pharmacokinetics of Intravenous Baclofen1
1, 2CompletedTreatmentCerebral Palsy (CP) / Spasticity1
1, 2CompletedTreatmentLiver Cirrhosis, Alcoholic1
1, 2Not Yet RecruitingTreatmentIntravenous Baclofen1
2CompletedBasic ScienceMarijuana Dependence1
2CompletedOtherAlcohol Dependence / Alcohol Drinking / Alcohol Drinking Related Problems / Alcoholism / Anxiety Disorder1
2CompletedTreatmentAlcoholism1
2CompletedTreatmentCocaine-Related Disorders3
2CompletedTreatmentDisseminated Sclerosis / Spasticity1
2CompletedTreatmentLiver Cirrhosis / Muscle Cramps1
2CompletedTreatmentMarijuana Dependence1
2CompletedTreatmentSpastic Diplegic Cerebral Palsy1
2RecruitingTreatmentAlcohol Use Disorder (AUD)1
2RecruitingTreatmentAlcoholism1
2RecruitingTreatmentNicotine Dependence1
2TerminatedPreventionAlcohol Withdrawal Syndrome(AWS) / Alcoholism1
2TerminatedTreatmentCerebral Anoxia / Comatose / Dysautonomia / Hypertonia / Traumatic Brain Injury (TBI)1
2TerminatedTreatmentNicotine Dependence1
2TerminatedTreatmentNicotine Dependence / Nicotine Use Disorder / Smoking / Tobacco Use Disorders1
2WithdrawnTreatmentDependence, Cocaine1
2WithdrawnTreatmentHepatocellular,Carcinoma1
2, 3CompletedTreatmentAlcohol Dependence2
2, 3CompletedTreatmentAlcoholism1
2, 3CompletedTreatmentFemale Genital Diseases1
3CompletedSupportive CareChronic Myeloproliferative Disorders / Leukemias / Lymphoproliferative Disorders / Malignant Lymphomas / Multiple Myeloma and Plasma Cell Neoplasm / Myelodysplastic Syndromes / Myelodysplastic/Myeloproliferative Neoplasms / Neurotoxicity / Pain / Unspecified Adult Solid Tumor, Protocol Specific1
3CompletedTreatmentAlcohol Dependence1
3CompletedTreatmentCerebral Palsy (CP) / Spasticity1
3CompletedTreatmentDisseminated Sclerosis2
3CompletedTreatmentDisseminated Sclerosis / Spasticity1
3CompletedTreatmentGERD1
3CompletedTreatmentSevere Spasticity1
3RecruitingTreatmentAlcohol Withdrawal Syndrome(AWS)1
3RecruitingTreatmentAlcoholism1
3Unknown StatusTreatmentAlcohol Dependence / Severe alcoholic liver disease1
4CompletedTreatmentAlcohol Dependence1
4CompletedTreatmentAlcohol Use Disorders (AUD) / Chronic Hepatitis C Infection1
4CompletedTreatmentRecurrent Crying Spells1
4CompletedTreatmentRumination Disorders / Supra-gastric Belching1
4RecruitingOtherAlcohol Use Disorder (AUD)1
4RecruitingSupportive CareMuscle Spasticity1
4RecruitingTreatmentLow Back Pain (LBP)1
4SuspendedTreatmentSleep1
4TerminatedBasic ScienceLower Urinary Tract Symptoms (LUTS) / Occasional Constipation / Over Active Bladder1
4Unknown StatusSupportive CareCerebral Palsy (CP)1
4Unknown StatusTreatmentCerebral Palsy (CP) / GERD1
Not AvailableCompletedBasic ScienceBrain GABA-B Function / No Conditions1
Not AvailableCompletedDiagnosticGastroesophageal Reflux Disease1
Not AvailableCompletedPreventionAlcohol Withdrawal Delirium1
Not AvailableCompletedTreatmentBulimia Nervosa (BN) / Eating Disorders1
Not AvailableCompletedTreatmentSpinal Cord Injuries (SCI)1
Not AvailableEnrolling by InvitationNot AvailableArthritis / Gout Acute / Headaches / Migraines / Muscle Spasms / Radicular syndrome / Synovitis / Tendonitis1
Not AvailableTerminatedTreatmentNon-Cardiac Chest Pain1
Not AvailableUnknown StatusTreatmentLiver Cirrhosis / Muscle Cramps1
Not AvailableWithdrawnTreatmentAutism Spectrum Disorder (ASD) / Tactile Defensiveness1
Pharmacoeconomics
Manufacturers
  • Medtronic inc
  • Schwarz pharma inc
  • Actavis totowa llc
  • Caraco pharmaceutical laboratories ltd
  • Impax laboratories inc
  • Ivax pharmaceuticals inc sub teva pharmaceuticals usa
  • Lannett holdings inc
  • Matrix laboratories ltd
  • Mylan pharmaceuticals inc
  • Northstar healthcare holdings ltd
  • Teva pharmaceuticals usa inc
  • Usl pharma inc
  • Vintage pharmaceuticals inc
  • Watson laboratories inc
  • Novartis pharmaceuticals corp
Packagers
Dosage forms
FormRouteStrength
InjectionIntrathecal10 mg/20mL
InjectionIntrathecal40 mg/20mL
TabletOral10 mg/1
TabletOral20 mg/1
KitTopical
InjectionIntrathecal1000 ug/mL
InjectionIntrathecal2000 ug/mL
InjectionIntrathecal50 ug/mL
InjectionIntrathecal500 ug/mL
Injection, solutionIntrathecal1000 ug/mL
Injection, solutionIntrathecal2000 ug/mL
Injection, solutionIntrathecal50 ug/mL
Injection, solutionIntrathecal500 ug/mL
KitTopical
InjectionIntrathecal.05 mg/mL
InjectionIntrathecal.5 mg/mL
InjectionIntrathecal2 mg/mL
InjectionIntrathecal10 mg/5mL
SolutionIntrathecal0.05 mg
SolutionIntrathecal0.5 mg
SolutionIntrathecal2 mg
TabletOral10 mg
TabletOral20 mg
Prices
Unit descriptionCostUnit
Lioresal it 0.05 mg/1 ml amp84.0USD ml
Lioresal it 10 mg/5 ml kit51.6USD ml
Lioresal Intrathecal 2 mg/ml44.64USD ml
Lioresal Intrathecal 0.05 mg/ml14.89USD ml
Baclofen powder14.38USD g
Lioresal it 10 mg/20 ml kit12.9USD ml
Lioresal Intrathecal 0.5 mg/ml11.16USD ml
Lioresal D.S. 20 mg Tablet1.4USD tablet
Baclofen 20 mg tablet0.92USD tablet
Lioresal 10 mg Tablet0.72USD tablet
Apo-Baclofen 20 mg Tablet0.59USD tablet
Mylan-Baclofen 20 mg Tablet0.59USD tablet
Nu-Baclo 20 mg Tablet0.59USD tablet
Phl-Baclofen 20 mg Tablet0.59USD tablet
Pms-Baclofen 20 mg Tablet0.59USD tablet
Ratio-Baclofen 20 mg Tablet0.59USD tablet
Baclofen 10 mg tablet0.51USD tablet
Apo-Baclofen 10 mg Tablet0.3USD tablet
Mylan-Baclofen 10 mg Tablet0.3USD tablet
Nu-Baclo 10 mg Tablet0.3USD tablet
Phl-Baclofen 10 mg Tablet0.3USD tablet
Pms-Baclofen 10 mg Tablet0.3USD tablet
Ratio-Baclofen 10 mg Tablet0.3USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US6024981 No1998-04-092018-04-09Us
US6221392 No1998-04-092018-04-09Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point (°C)206-208 °CKeberle, H., Faigle, J.W. and Wilhelm, M.; U.S. Patent 3,471,548; October 7, 1969; assigned to Ciba Corporation. Keberle, H., Faigle, J.W. and Wilhelm, M.; U.S. Patent 3,634,428; January 11, 1972; assigned to Ciba Corporation.
water solubility2090 mg/LNot Available
logP1.3Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.712 mg/mLALOGPS
logP-0.82ALOGPS
logP-0.78ChemAxon
logS-2.5ALOGPS
pKa (Strongest Acidic)3.89ChemAxon
pKa (Strongest Basic)9.79ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area63.32 Å2ChemAxon
Rotatable Bond Count4ChemAxon
Refractivity54.83 m3·mol-1ChemAxon
Polarizability21.13 Å3ChemAxon
Number of Rings1ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.978
Blood Brain Barrier+0.9339
Caco-2 permeable+0.5668
P-glycoprotein substrateNon-substrate0.7373
P-glycoprotein inhibitor INon-inhibitor0.9825
P-glycoprotein inhibitor IINon-inhibitor0.9842
Renal organic cation transporterNon-inhibitor0.8435
CYP450 2C9 substrateNon-substrate0.8746
CYP450 2D6 substrateNon-substrate0.8426
CYP450 3A4 substrateNon-substrate0.7618
CYP450 1A2 substrateNon-inhibitor0.9046
CYP450 2C9 inhibitorNon-inhibitor0.9071
CYP450 2D6 inhibitorNon-inhibitor0.736
CYP450 2C19 inhibitorNon-inhibitor0.8215
CYP450 3A4 inhibitorNon-inhibitor0.8309
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9204
Ames testNon AMES toxic0.8621
CarcinogenicityNon-carcinogens0.7401
BiodegradationNot ready biodegradable0.7362
Rat acute toxicity3.1364 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9478
hERG inhibition (predictor II)Non-inhibitor0.8578
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
LC-MS/MSLC-MS/MS Spectrum - LC-ESI-QTOF , negativesplash10-03dr-0950000000-33d21cbb6740c1f1aee1View in MoNA
LC-MS/MSLC-MS/MS Spectrum - LC-ESI-QQ , positivesplash10-03di-1590000000-8a64733764308ba98f9aView in MoNA
LC-MS/MSLC-MS/MS Spectrum - LC-ESI-QQ , positivesplash10-0f6t-0900000000-6647c58db763b4df68a0View in MoNA
LC-MS/MSLC-MS/MS Spectrum - LC-ESI-QQ , positivesplash10-0udi-0900000000-72d6d878c9c2f29d846aView in MoNA
LC-MS/MSLC-MS/MS Spectrum - LC-ESI-QQ , positivesplash10-014i-1900000000-18f69033596a03ee643aView in MoNA
LC-MS/MSLC-MS/MS Spectrum - LC-ESI-QQ , positivesplash10-014i-1900000000-997473c303f07afcdf4eView in MoNA
LC-MS/MSLC-MS/MS Spectrum - LC-ESI-ITFT , positivesplash10-0002-0900000000-d1da4625d180fe0af521View in MoNA
LC-MS/MSLC-MS/MS Spectrum - LC-ESI-QTOF , positivesplash10-03di-0190000000-bd0fff49defde62ed0faView in MoNA
LC-MS/MSLC-MS/MS Spectrum - LC-ESI-QTOF , positivesplash10-0ik9-0790000000-1a50b0b7f24aaaf6a87eView in MoNA
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
MSMass Spectrum (Electron Ionization)splash10-000i-2900000000-963f049a4367a1d5a5f5View in MoNA
Taxonomy
DescriptionThis compound belongs to the class of chemical entities known as gamma amino acids and derivatives. These are amino acids having a (-NH2) group attached to the gamma carbon atom.
KingdomChemical entities
Super ClassOrganic compounds
ClassOrganic acids and derivatives
Sub ClassCarboxylic acids and derivatives
Direct ParentGamma amino acids and derivatives
Alternative ParentsPhenylpropanoic acids / Chlorobenzenes / Aralkylamines / Amino fatty acids / Aryl chlorides / Amino acids / Monocarboxylic acids and derivatives / Carboxylic acids / Organopnictogen compounds / Organochlorides
SubstituentsGamma amino acid or derivatives / 3-phenylpropanoic-acid / Amino fatty acid / Chlorobenzene / Aralkylamine / Halobenzene / Aryl chloride / Aryl halide / Monocyclic benzene moiety / Fatty acyl
Molecular FrameworkAromatic homomonocyclic compounds
External Descriptorsmonocarboxylic acid, primary amino compound, monochlorobenzenes, gamma-amino acid (CHEBI:2972 )

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
General Function:
G-protein coupled gaba receptor activity
Specific Function:
Component of a heterodimeric G-protein coupled receptor for GABA, formed by GABBR1 and GABBR2. Within the heterodimeric GABA receptor, only GABBR1 seems to bind agonists, while GABBR2 mediates coupling to G proteins. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such a...
Gene Name:
GABBR1
Uniprot ID:
Q9UBS5
Uniprot Name:
Gamma-aminobutyric acid type B receptor subunit 1
Molecular Weight:
108319.4 Da
References
  1. Bowery NG: GABAB receptor pharmacology. Annu Rev Pharmacol Toxicol. 1993;33:109-47. [PubMed:8388192 ]
  2. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  3. Garcia-Gil L, de Miguel R, Romero J, Perez A, Ramos JA, Fernandez-Ruiz JJ: Perinatal delta9-tetrahydrocannabinol exposure augmented the magnitude of motor inhibition caused by GABA(B), but not GABA(A), receptor agonists in adult rats. Neurotoxicol Teratol. 1999 May-Jun;21(3):277-83. [PubMed:10386831 ]
  4. Lehmann A: GABAB receptors as drug targets to treat gastroesophageal reflux disease. Pharmacol Ther. 2009 Jun;122(3):239-45. doi: 10.1016/j.pharmthera.2009.02.008. Epub 2009 Mar 19. [PubMed:19303900 ]
  5. Motalli R, Louvel J, Tancredi V, Kurcewicz I, Wan-Chow-Wah D, Pumain R, Avoli M: GABA(B) receptor activation promotes seizure activity in the juvenile rat hippocampus. J Neurophysiol. 1999 Aug;82(2):638-47. [PubMed:10444662 ]
  6. Mott DD, Li Q, Okazaki MM, Turner DA, Lewis DV: GABAB-Receptor-mediated currents in interneurons of the dentate-hilus border. J Neurophysiol. 1999 Sep;82(3):1438-50. [PubMed:10482760 ]
  7. Ogasawara T, Itoh Y, Tamura M, Mushiroi T, Ukai Y, Kise M, Kimura K: Involvement of cholinergic and GABAergic systems in the reversal of memory disruption by NS-105, a cognition enhancer. Pharmacol Biochem Behav. 1999 Sep;64(1):41-52. [PubMed:10494996 ]
  8. Pittman QJ: The action is at the terminal. J Physiol. 1999 Nov 1;520 Pt 3:629. [PubMed:10545129 ]
  9. Stringer JL, Lorenzo N: The reduction in paired-pulse inhibition in the rat hippocampus by gabapentin is independent of GABA(B) receptor receptor activation. Epilepsy Res. 1999 Feb;33(2-3):169-76. [PubMed:10094428 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
General Function:
G-protein coupled gaba receptor activity
Specific Function:
Component of a heterodimeric G-protein coupled receptor for GABA, formed by GABBR1 and GABBR2. Within the heterodimeric GABA receptor, only GABBR1 seems to bind agonists, while GABBR2 mediates coupling to G proteins. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such a...
Gene Name:
GABBR2
Uniprot ID:
O75899
Uniprot Name:
Gamma-aminobutyric acid type B receptor subunit 2
Molecular Weight:
105820.52 Da
References
  1. Belley M, Sullivan R, Reeves A, Evans J, O'Neill G, Ng GY: Synthesis of the nanomolar photoaffinity GABA(B) receptor ligand CGP 71872 reveals diversity in the tissue distribution of GABA(B) receptor forms. Bioorg Med Chem. 1999 Dec;7(12):2697-704. [PubMed:10658574 ]
  2. Braun M, Wendt A, Buschard K, Salehi A, Sewing S, Gromada J, Rorsman P: GABAB receptor activation inhibits exocytosis in rat pancreatic beta-cells by G-protein-dependent activation of calcineurin. J Physiol. 2004 Sep 1;559(Pt 2):397-409. Epub 2004 Jul 2. [PubMed:15235087 ]
  3. Bowery NG: GABAB receptor pharmacology. Annu Rev Pharmacol Toxicol. 1993;33:109-47. [PubMed:8388192 ]
  4. Filippov AK, Couve A, Pangalos MN, Walsh FS, Brown DA, Moss SJ: Heteromeric assembly of GABA(B)R1 and GABA(B)R2 receptor subunits inhibits Ca(2+) current in sympathetic neurons. J Neurosci. 2000 Apr 15;20(8):2867-74. [PubMed:10751439 ]
  5. Jones KA, Tamm JA, Craig DA, Ph D, Yao W, Panico R: Signal transduction by GABA(B) receptor heterodimers. Neuropsychopharmacology. 2000 Oct;23(4 Suppl):S41-9. [PubMed:11008066 ]
  6. Lehmann A: GABAB receptors as drug targets to treat gastroesophageal reflux disease. Pharmacol Ther. 2009 Jun;122(3):239-45. doi: 10.1016/j.pharmthera.2009.02.008. Epub 2009 Mar 19. [PubMed:19303900 ]
  7. Martin SC, Russek SJ, Farb DH: Molecular identification of the human GABABR2: cell surface expression and coupling to adenylyl cyclase in the absence of GABABR1. Mol Cell Neurosci. 1999 Mar;13(3):180-91. [PubMed:10328880 ]
  8. Pittman QJ: The action is at the terminal. J Physiol. 1999 Nov 1;520 Pt 3:629. [PubMed:10545129 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Plays an important role in the excretion/detoxification of endogenous and exogenous organic anions, especially from the brain and kidney. Involved in the transport basolateral of steviol, fexofenadine. Transports benzylpenicillin (PCG), estrone-3-sulfate (E1S), cimetidine (CMD), 2,4-dichloro-phenoxyacetate (2,4-D), p-amino-hippurate (PAH), acyclovir (ACV) and ochratoxin (OTA).
Gene Name:
SLC22A8
Uniprot ID:
Q8TCC7
Uniprot Name:
Solute carrier family 22 member 8
Molecular Weight:
59855.585 Da
References
  1. Ohtsuki S, Asaba H, Takanaga H, Deguchi T, Hosoya K, Otagiri M, Terasaki T: Role of blood-brain barrier organic anion transporter 3 (OAT3) in the efflux of indoxyl sulfate, a uremic toxin: its involvement in neurotransmitter metabolite clearance from the brain. J Neurochem. 2002 Oct;83(1):57-66. [PubMed:12358729 ]
  2. Mori S, Takanaga H, Ohtsuki S, Deguchi T, Kang YS, Hosoya K, Terasaki T: Rat organic anion transporter 3 (rOAT3) is responsible for brain-to-blood efflux of homovanillic acid at the abluminal membrane of brain capillary endothelial cells. J Cereb Blood Flow Metab. 2003 Apr;23(4):432-40. [PubMed:12679720 ]
Drug created on June 13, 2005 07:24 / Updated on July 25, 2017 17:50