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Identification
NameBaclofen
Accession NumberDB00181  (APRD00551)
TypeSmall Molecule
GroupsApproved
DescriptionBaclofen 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 Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Ava-baclofentablet20 mgoralAvanstra Inc2011-10-112014-08-21Canada
Ava-baclofentablet10 mgoralAvanstra Inc2011-10-112014-08-21Canada
Baclofentablet10 mgoralSanis Health Inc2010-02-25Not applicableCanada
Baclofentablet10 mgoralApotex Inc1994-12-312014-08-23Canada
Baclofentablet20 mgoralSanis Health Inc2010-02-25Not applicableCanada
Baclofentablet20 mgoralApotex Inc1994-12-312014-08-23Canada
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 Pharmaceuticals CompanyNot applicableNot applicableCanada
Co Baclofen Tablets 20mgtablet20 mgoralCobalt Pharmaceuticals CompanyNot applicableNot applicableCanada
Dom-baclofen-tab 10mgtablet10 mgoralDominion Pharmacal1995-12-31Not applicableCanada
Dom-baclofen-tab 20mgtablet20 mgoralDominion Pharmacal1995-12-31Not applicableCanada
Ftp-baclofentablet10 mgoralFtp Pharmacal Inc.1998-10-092004-08-03Canada
Ftp-baclofentablet20 mgoralFtp Pharmacal Inc.1998-10-092004-08-03Canada
Gablofeninjection50 ug/mLintrathecalMallinckrodt Inc (Brand Pharmaceuticals)2010-11-19Not applicableUs
Gablofeninjection500 ug/mLintrathecalMallinckrodt Inc (Brand Pharmaceuticals)2010-11-19Not applicableUs
Gablofeninjection1000 ug/mLintrathecalMallinckrodt Inc (Brand Pharmaceuticals)2012-07-10Not applicableUs
Gablofeninjection2000 ug/mLintrathecalMallinckrodt Inc (Brand Pharmaceuticals)2010-11-19Not applicableUs
Lioresalinjection2 mg/mLintrathecalMedtronic Neuromodulation2003-05-08Not applicableUs
Lioresalinjection.5 mg/mLintrathecalMedtronic Neuromodulation1992-06-17Not applicableUs
Lioresalinjection2 mg/mLintrathecalMedtronic Neuromodulation1992-06-17Not applicableUs
Lioresalinjection.05 mg/mLintrathecalMedtronic Neuromodulation1996-11-07Not applicableUs
Lioresal D.S. Tab 20mgtablet20 mgoralNovartis Pharmaceuticals Canada Inc1985-12-31Not applicableCanada
Lioresal Intrathecal 0.05mg/mlsolution0.05 mgintrathecalNovartis Pharmaceuticals Canada Inc1994-12-31Not applicableCanada
Lioresal Intrathecal 0.5mg/mlsolution0.5 mgintrathecalNovartis Pharmaceuticals Canada Inc1994-12-31Not applicableCanada
Lioresal Intrathecal 2mg/mlsolution2 mgintrathecalNovartis Pharmaceuticals Canada Inc1994-12-31Not applicableCanada
Lioresal Tab 10mgtablet10 mgoralNovartis Pharmaceuticals Canada Inc1978-12-31Not 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 Pharmaceuticals Ulc1994-12-31Not applicableCanada
Mylan-baclofentablet10 mgoralMylan Pharmaceuticals Ulc1994-12-31Not 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 mgoralTeva Canada Limited1997-12-16Not applicableCanada
Ratio-baclofentablet10 mgoralTeva Canada Limited1997-12-16Not applicableCanada
Riva-baclofentablet10 mgoralLaboratoire Riva Inc2003-03-03Not applicableCanada
Riva-baclofentablet20 mgoralLaboratoire Riva Inc2003-03-03Not applicableCanada
Sandoz Baclofentablet10 mgoralSandoz Canada IncorporatedNot applicableNot applicableCanada
Sandoz Baclofentablet20 mgoralSandoz Canada IncorporatedNot applicableNot applicableCanada
Val-baclofen Intrathecalsolution2 mgintrathecalValeant Canada Lp Valeant Canada S.E.C.2014-06-06Not 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
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-baclofen Tablets - 10mgtablet10 mgoralApotex Inc1994-12-31Not applicableCanada
Apo-baclofen Tablets - 20mgtablet20 mgoralApotex Inc1994-12-31Not applicableCanada
Baclofentablet20 mg/1oralDIRECT RX2014-01-01Not applicableUs
Baclofentablet10 mg/1oralAmerican Health Packaging2015-02-15Not applicableUs
Baclofentablet20 mg/1oralA S Medication Solutions1988-07-21Not applicableUs
Baclofentablet20 mg/1oralNorthstar Rx LLC2011-01-01Not applicableUs
Baclofentablet10 mg/1oralLake Erie Medical DBA Quality Care Products LLC2010-05-19Not applicableUs
Baclofentablet20 mg/1oralCardinal Health1988-07-21Not applicableUs
Baclofentablet20 mg/1oralQualitest Pharmaceuticals2005-08-30Not applicableUs
Baclofentablet10 mg/1oralIVAX Pharmaceuticals, Inc.1988-07-21Not applicableUs
Baclofentablet20 mg/1oralSt Marys Medical Park Pharmacy2014-04-20Not applicableUs
Baclofentablet10 mg/1oralMc Kesson Packaging Services A Business Unit Of Mc Kesson Corporation2007-07-01Not applicableUs
Baclofentablet20 mg/1oralMc Kesson Contract Packaging2011-12-12Not applicableUs
Baclofentablet20 mg/1oralMajor Pharmaceuticals2015-07-15Not applicableUs
Baclofentablet10 mg/1oralAv Kare, Inc.2014-08-25Not applicableUs
Baclofentablet10 mg/1oralH.J. Harkins Company, Inc.2010-07-15Not applicableUs
Baclofentablet10 mg/1oralClinical Solutions Wholesale2010-10-20Not applicableUs
Baclofentablet20 mg/1oralUpsher Smith Laboratories, Inc.2010-10-20Not applicableUs
Baclofentablet20 mg/1oralProficient Rx LP2005-12-01Not applicableUs
Baclofentablet20 mg/1oralPreferred Pharmaceuticals, Inc2012-04-30Not applicableUs
Baclofentablet20 mg/1oralAidarex Pharmaceuticals LLC2005-08-30Not applicableUs
Baclofentablet10 mg/1oralMed Health Pharma, LLC2011-01-01Not applicableUs
Baclofentablet10 mg/1oralREMEDYREPACK INC.2011-10-10Not applicableUs
Baclofentablet10 mg/1oralPhysicians Total Care, Inc.2010-03-05Not applicableUs
Baclofentablet10 mg/1oralLannett Company, Inc.2007-07-01Not applicableUs
Baclofentablet20 mg/1oralREMEDYREPACK INC.2015-06-15Not applicableUs
Baclofentablet20 mg/1oralDispensing Solutions, Inc.2005-08-30Not applicableUs
Baclofentablet10 mg/1oralSTAT Rx USA LLC1991-09-18Not applicableUs
Baclofentablet10 mg/1oralNcs Health Care Of Ky, Inc Dba Vangard Labs2010-07-15Not applicableUs
Baclofentablet10 mg/1oralDIRECT RX2014-01-01Not applicableUs
Baclofentablet20 mg/1oralAmerican Health Packaging2015-02-15Not applicableUs
Baclofentablet10 mg/1oralRebel Distributors Corp.2004-07-01Not applicableUs
Baclofentablet20 mg/1oralLake Erie Medical DBA Quality Care Products LLC2010-11-15Not applicableUs
Baclofentablet10 mg/1oralPd Rx Pharmaceuticals, Inc.2010-07-15Not applicableUs
Baclofentablet20 mg/1oralIVAX Pharmaceuticals, Inc.1988-07-21Not applicableUs
Baclofentablet20 mg/1oralREMEDYREPACK INC.2014-12-04Not applicableUs
Baclofentablet10 mg/1oralMc Kesson Packaging Services A Business Unit Of Mc Kesson Corporation2011-04-11Not applicableUs
Baclofentablet10 mg/1oralAmerican Health Packaging2012-09-032015-12-29Us
Baclofentablet10 mg/1oralMarlex Pharmaceuticals Inc2014-12-01Not applicableUs
Baclofentablet20 mg/1oralAv Kare, Inc.2014-08-25Not applicableUs
Baclofentablet20 mg/1oralState of Florida DOH Central Pharmacy2014-01-01Not applicableUs
Baclofentablet20 mg/1oralLake Erie Medical & Surgical Supply DBA Quality Care Products LLC2010-10-20Not applicableUs
Baclofentablet20 mg/1oralMed Health Pharma, LLC2011-01-01Not applicableUs
Baclofentablet10 mg/1oralClinical Solutions Wholesale2010-10-20Not applicableUs
Baclofentablet10 mg/1oralMajor Pharmaceuticals1998-07-21Not applicableUs
Baclofentablet10 mg/1oralProficient Rx LP2005-12-01Not applicableUs
Baclofentablet10 mg/1oralPreferred Pharmaceuticals, Inc2012-04-30Not applicableUs
Baclofentablet10 mg/1oralCardinal Health2015-07-15Not applicableUs
Baclofentablet20 mg/1oralSTAT Rx USA LLC1991-09-18Not applicableUs
Baclofentablet10 mg/1oralREMEDYREPACK INC.2012-03-13Not applicableUs
Baclofentablet10 mg/1oralCardinal Health2010-07-15Not applicableUs
Baclofentablet20 mg/1oralLannett Company, Inc.2005-12-01Not applicableUs
Baclofentablet10 mg/1oralREMEDYREPACK INC.2015-12-16Not applicableUs
Baclofentablet10 mg/1oralDispensing Solutions, Inc.2005-08-30Not applicableUs
Baclofentablet20 mg/1oralNcs Health Care Of Ky, Inc Dba Vangard Labs2010-07-15Not applicableUs
Baclofentablet20 mg/1oralDIRECT RX2014-01-01Not applicableUs
Baclofentablet10 mg/1oralPreferred Pharmaceuticals, Inc2004-07-01Not applicableUs
Baclofentablet20 mg/1oralRebel Distributors Corp.2004-07-01Not applicableUs
Baclofentablet10 mg/1oralUnit Dose Services1988-07-21Not applicableUs
Baclofentablet10 mg/1oralClinical Solutions Wholesale, Llc2010-10-20Not applicableUs
Baclofentablet10 mg/1oralMylan Pharmaceuticals Inc.2010-02-18Not applicableUs
Baclofentablet10 mg/1oralREMEDYREPACK INC.2015-02-25Not applicableUs
Baclofentablet20 mg/1oralMc Kesson Packaging Services A Business Unit Of Mc Kesson Corporation2011-05-31Not applicableUs
Baclofentablet20 mg/1oralAvera Mc Kennan Hospital2015-03-31Not applicableUs
Baclofentablet20 mg/1oralMarlex Pharmaceuticals Inc2014-12-01Not applicableUs
Baclofentablet20 mg/1oralPd Rx Pharmaceuticals, Inc.2005-08-30Not applicableUs
Baclofentablet10 mg/1oralState of Florida DOH Central Pharmacy2014-01-01Not applicableUs
Baclofentablet20 mg/1oralRebel Distributors Corp2010-07-15Not applicableUs
Baclofentablet20 mg/1oralREMEDYREPACK INC.2013-02-11Not applicableUs
Baclofentablet10 mg/1oralNew Horizon Rx Group, LLC2013-08-25Not applicableUs
Baclofentablet20 mg/1oralMajor Pharmaceuticals1998-07-21Not applicableUs
Baclofentablet10 mg/1oralBryant Ranch Rrepack2007-07-01Not applicableUs
Baclofentablet10 mg/1oralPreferred Pharmaceuticals, Inc.2012-03-28Not applicableUs
Baclofentablet10 mg/1oralREMEDYREPACK INC.2016-03-25Not applicableUs
Baclofentablet10 mg/1oralNorthstar Rx LLC2011-01-01Not applicableUs
Baclofentablet10 mg/1oralREMEDYREPACK INC.2012-03-15Not applicableUs
Baclofentablet20 mg/1oralCardinal Health1998-07-21Not applicableUs
Baclofentablet10 mg/1oralQualitest Pharmaceuticals2005-08-30Not applicableUs
Baclofentablet10 mg/1oralDIRECT RX2014-01-01Not applicableUs
Baclofentablet20 mg/1oralAmerican Health Packaging2012-09-032016-02-29Us
Baclofentablet10 mg/1oralUpsher Smith Laboratories, Inc.2010-10-20Not applicableUs
Baclofentablet10 mg/1oralProficient Rx LP1988-07-21Not applicableUs
Baclofentablet10 mg/1oralPreferred Pharmaceuticals, Inc.2014-10-22Not applicableUs
Baclofentablet10 mg/1oralAidarex Pharmaceuticals LLC2005-08-30Not applicableUs
Baclofentablet20 mg/1oralUnit Dose Services2010-07-15Not applicableUs
Baclofentablet20 mg/1oralClinical Solutions Wholesale, Llc2010-10-20Not applicableUs
Baclofentablet20 mg/1oralMylan Pharmaceuticals Inc.2010-02-18Not applicableUs
Baclofentablet10 mg/1oralREMEDYREPACK INC.2015-03-20Not applicableUs
Baclofentablet20 mg/1oralMc Kesson Packaging Services A Business Unit Of Mc Kesson Corporation2005-12-01Not applicableUs
Baclofentablet10 mg/1oralBlenheim Pharmacal, Inc.2013-11-15Not applicableUs
Baclofentablet10 mg/1oralREMEDYREPACK INC.2011-04-04Not applicableUs
Baclofentablet20 mg/1oralPhysicians Total Care, Inc.2009-04-17Not applicableUs
Baclofentablet10 mg/1oralRebel Distributors Corp2010-07-15Not applicableUs
Baclofentablet20 mg/1oralH.J. Harkins Company, Inc.2010-07-15Not applicableUs
Baclofentablet10 mg/1oralSt Marys Medical Park Pharmacy2014-01-15Not applicableUs
Baclofentablet10 mg/1oralMajor Pharmaceuticals2015-07-15Not applicableUs
Baclofentablet20 mg/1oralBryant Ranch Rrepack2007-07-01Not applicableUs
Baclofentablet10 mg/1oralMc Kesson Contract Packaging2011-11-14Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Equipto - Baclofen External Cream Compounding KitkittopicalAlvix Laboratories, LLC2015-01-20Not applicableUs
International Brands
NameCompany
BaclonUniao Quimica (Brazil)
KemstroSchwarz (United States)
Lioresal IntrathecalNovartis Pharmaceuticals
Nu-BaclofenNu-Pharm
Brand mixtures
NameLabellerIngredients
Gapeam BudibacAlvix Laboratories, LLC
SaltsNot Available
Categories
UNIIH789N3FKE8
CAS number1134-47-0
WeightAverage: 213.661
Monoisotopic: 213.05565634
Chemical FormulaC10H12ClNO2
InChI KeyInChIKey=KPYSYYIEGFHWSV-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
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as gamma amino acids and derivatives. These are amino acids having a (-NH2) group attached to the gamma carbon atom.
KingdomOrganic compounds
Super ClassOrganic acids and derivatives
ClassCarboxylic acids and derivatives
Sub ClassAmino acids, peptides, and analogues
Direct ParentGamma amino acids and derivatives
Alternative Parents
Substituents
  • Gamma amino acid or derivatives
  • 3-phenylpropanoic-acid
  • Phenylpropylamine
  • Aralkylamine
  • Halobenzene
  • Chlorobenzene
  • Amino fatty acid
  • Fatty acyl
  • Benzenoid
  • Monocyclic benzene moiety
  • Aryl halide
  • Aryl chloride
  • Monocarboxylic acid or derivatives
  • Carboxylic acid
  • Hydrocarbon derivative
  • Primary amine
  • Organooxygen compound
  • Organonitrogen compound
  • Organochloride
  • Organohalogen compound
  • Primary aliphatic amine
  • Carbonyl group
  • Amine
  • Aromatic homomonocyclic compound
Molecular FrameworkAromatic homomonocyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationFor 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.
PharmacodynamicsBaclofen 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 actionBaclofen 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.
Related Articles
AbsorptionRapidly and almost completely absorbed from the GI tract.
Volume of distribution
  • 59 L
Protein binding30%
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 eliminationIn 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 life2.5-4 hours
Clearance
  • 180 mL/min
ToxicityLD50=45 mg/kg (male mice, IV); LD50=78 mg/kg (male rat, IV)
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
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 )
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
Tabletoral10 mg/1
Tabletoral20 mg/1
Kittopical
Injectionintrathecal1000 ug/mL
Injectionintrathecal2000 ug/mL
Injectionintrathecal50 ug/mL
Injectionintrathecal500 ug/mL
Kittopical
Injectionintrathecal.05 mg/mL
Injectionintrathecal.5 mg/mL
Injectionintrathecal2 mg/mL
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 point206-208 °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 FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
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
References
Synthesis Reference

Wayne Levadoux, Denis Groleau, Michael Trani, Robert Lortie, “Streptomyces microorganism useful for the preparation of®-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
AHFS Codes
  • 12:20.12
PDB EntriesNot Available
FDA labelDownload (135 KB)
MSDSDownload (73.4 KB)
Interactions
Drug Interactions
Drug
7-NitroindazoleThe risk or severity of adverse effects can be increased when 7-Nitroindazole is combined with Baclofen.
AcepromazineThe risk or severity of adverse effects can be increased when Acepromazine is combined with Baclofen.
AceprometazineThe risk or severity of adverse effects can be increased when Aceprometazine is combined with Baclofen.
adipiplonThe risk or severity of adverse effects can be increased when adipiplon is combined with Baclofen.
AgomelatineThe risk or severity of adverse effects can be increased when Agomelatine is combined with Baclofen.
AlfaxaloneThe risk or severity of adverse effects can be increased when Alfaxalone is combined with Baclofen.
AlfentanilThe risk or severity of adverse effects can be increased when Alfentanil is combined with Baclofen.
AlphacetylmethadolThe risk or severity of adverse effects can be increased when Alphacetylmethadol is combined with Baclofen.
AlprazolamThe risk or severity of adverse effects can be increased when Alprazolam is combined with Baclofen.
AmisulprideThe risk or severity of adverse effects can be increased when Amisulpride is combined with Baclofen.
AmitriptylineThe risk or severity of adverse effects can be increased when Baclofen is combined with Amitriptyline.
AmobarbitalThe risk or severity of adverse effects can be increased when Amobarbital is combined with Baclofen.
AmoxapineThe risk or severity of adverse effects can be increased when Baclofen is combined with Amoxapine.
AmperozideThe risk or severity of adverse effects can be increased when Amperozide is combined with Baclofen.
AripiprazoleThe risk or severity of adverse effects can be increased when Aripiprazole is combined with Baclofen.
ArticaineThe risk or severity of adverse effects can be increased when Articaine is combined with Baclofen.
AsenapineThe risk or severity of adverse effects can be increased when Asenapine is combined with Baclofen.
AzaperoneThe risk or severity of adverse effects can be increased when Azaperone is combined with Baclofen.
AzelastineBaclofen may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
AzelastineThe risk or severity of adverse effects can be increased when Azelastine is combined with Baclofen.
BarbitalThe risk or severity of adverse effects can be increased when Barbital is combined with Baclofen.
BenzocaineThe risk or severity of adverse effects can be increased when Benzocaine is combined with Baclofen.
Benzyl alcoholThe risk or severity of adverse effects can be increased when Benzyl alcohol is combined with Baclofen.
BrexpiprazoleThe risk or severity of adverse effects can be increased when Baclofen is combined with Brexpiprazole.
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Baclofen.
BrimonidineThe risk or severity of adverse effects can be increased when Baclofen is combined with Brimonidine.
BromazepamThe risk or severity of adverse effects can be increased when Bromazepam is combined with Baclofen.
BrompheniramineThe risk or severity of adverse effects can be increased when Baclofen is combined with Brompheniramine.
BrotizolamThe risk or severity of adverse effects can be increased when Brotizolam is combined with Baclofen.
BupivacaineThe risk or severity of adverse effects can be increased when Bupivacaine is combined with Baclofen.
BuprenorphineThe risk or severity of adverse effects can be increased when Buprenorphine is combined with Baclofen.
BuspironeThe risk or severity of adverse effects can be increased when Buspirone is combined with Baclofen.
ButabarbitalThe risk or severity of adverse effects can be increased when Butabarbital is combined with Baclofen.
ButacaineThe risk or severity of adverse effects can be increased when Butacaine is combined with Baclofen.
ButalbitalThe risk or severity of adverse effects can be increased when Baclofen is combined with Butalbital.
ButambenThe risk or severity of adverse effects can be increased when Butamben is combined with Baclofen.
ButethalThe risk or severity of adverse effects can be increased when Butethal is combined with Baclofen.
ButorphanolThe risk or severity of adverse effects can be increased when Butorphanol is combined with Baclofen.
CarbamazepineThe risk or severity of adverse effects can be increased when Carbamazepine is combined with Baclofen.
CarbinoxamineThe risk or severity of adverse effects can be increased when Baclofen is combined with Carbinoxamine.
CarfentanilThe risk or severity of adverse effects can be increased when Carfentanil is combined with Baclofen.
CarisoprodolThe risk or severity of adverse effects can be increased when Baclofen is combined with Carisoprodol.
CetirizineThe risk or severity of adverse effects can be increased when Baclofen is combined with Cetirizine.
Chloral hydrateThe risk or severity of adverse effects can be increased when Chloral hydrate is combined with Baclofen.
ChlordiazepoxideThe risk or severity of adverse effects can be increased when Chlordiazepoxide is combined with Baclofen.
ChlormezanoneThe risk or severity of adverse effects can be increased when Chlormezanone is combined with Baclofen.
ChloroprocaineThe risk or severity of adverse effects can be increased when Chloroprocaine is combined with Baclofen.
ChlorphenamineThe risk or severity of adverse effects can be increased when Baclofen is combined with Chlorphenamine.
ChlorpromazineThe risk or severity of adverse effects can be increased when Chlorpromazine is combined with Baclofen.
ChlorprothixeneThe risk or severity of adverse effects can be increased when Chlorprothixene is combined with Baclofen.
ChlorzoxazoneThe risk or severity of adverse effects can be increased when Baclofen is combined with Chlorzoxazone.
CinchocaineThe risk or severity of adverse effects can be increased when Cinchocaine is combined with Baclofen.
CitalopramThe risk or severity of adverse effects can be increased when Baclofen is combined with Citalopram.
ClemastineThe risk or severity of adverse effects can be increased when Baclofen is combined with Clemastine.
ClidiniumThe risk or severity of adverse effects can be increased when Baclofen is combined with Clidinium.
ClobazamThe risk or severity of adverse effects can be increased when Baclofen is combined with Clobazam.
clomethiazoleThe risk or severity of adverse effects can be increased when clomethiazole is combined with Baclofen.
ClomipramineThe risk or severity of adverse effects can be increased when Baclofen is combined with Clomipramine.
ClonazepamThe risk or severity of adverse effects can be increased when Baclofen is combined with Clonazepam.
ClonidineThe risk or severity of adverse effects can be increased when Baclofen is combined with Clonidine.
ClorazepateThe risk or severity of adverse effects can be increased when Clorazepate is combined with Baclofen.
ClozapineThe risk or severity of adverse effects can be increased when Clozapine is combined with Baclofen.
CocaineThe risk or severity of adverse effects can be increased when Cocaine is combined with Baclofen.
CodeineThe risk or severity of adverse effects can be increased when Codeine is combined with Baclofen.
CyclizineThe risk or severity of adverse effects can be increased when Baclofen is combined with Cyclizine.
CyclobenzaprineThe risk or severity of adverse effects can be increased when Cyclobenzaprine is combined with Baclofen.
CyproheptadineThe risk or severity of adverse effects can be increased when Baclofen is combined with Cyproheptadine.
DantroleneThe risk or severity of adverse effects can be increased when Baclofen is combined with Dantrolene.
DapiprazoleThe risk or severity of adverse effects can be increased when Dapiprazole is combined with Baclofen.
DapoxetineThe risk or severity of adverse effects can be increased when Baclofen is combined with Dapoxetine.
deramciclaneThe risk or severity of adverse effects can be increased when deramciclane is combined with Baclofen.
DesfluraneThe risk or severity of adverse effects can be increased when Desflurane is combined with Baclofen.
DesipramineThe risk or severity of adverse effects can be increased when Baclofen is combined with Desipramine.
DesloratadineThe risk or severity of adverse effects can be increased when Baclofen is combined with Desloratadine.
DetomidineThe risk or severity of adverse effects can be increased when Detomidine is combined with Baclofen.
DexbrompheniramineThe risk or severity of adverse effects can be increased when Baclofen is combined with Dexbrompheniramine.
DexmedetomidineThe risk or severity of adverse effects can be increased when Dexmedetomidine is combined with Baclofen.
DextromoramideThe risk or severity of adverse effects can be increased when Dextromoramide is combined with Baclofen.
DextropropoxypheneThe risk or severity of adverse effects can be increased when Dextropropoxyphene is combined with Baclofen.
DezocineThe risk or severity of adverse effects can be increased when Dezocine is combined with Baclofen.
DiazepamThe risk or severity of adverse effects can be increased when Diazepam is combined with Baclofen.
DifenoxinThe risk or severity of adverse effects can be increased when Baclofen is combined with Difenoxin.
DihydrocodeineThe risk or severity of adverse effects can be increased when Dihydrocodeine is combined with Baclofen.
DihydroetorphineThe risk or severity of adverse effects can be increased when Dihydroetorphine is combined with Baclofen.
DihydromorphineThe risk or severity of adverse effects can be increased when Dihydromorphine is combined with Baclofen.
DimenhydrinateThe risk or severity of adverse effects can be increased when Baclofen is combined with Dimenhydrinate.
DiphenhydramineThe risk or severity of adverse effects can be increased when Diphenhydramine is combined with Baclofen.
DiphenoxylateThe risk or severity of adverse effects can be increased when Diphenoxylate is combined with Baclofen.
DoramectinThe risk or severity of adverse effects can be increased when Doramectin is combined with Baclofen.
DoxepinThe risk or severity of adverse effects can be increased when Baclofen is combined with Doxepin.
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Baclofen.
DoxylamineThe risk or severity of adverse effects can be increased when Baclofen is combined with Doxylamine.
DPDPEThe risk or severity of adverse effects can be increased when DPDPE is combined with Baclofen.
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Baclofen.
DroperidolThe risk or severity of adverse effects can be increased when Droperidol is combined with Baclofen.
DrotebanolThe risk or severity of adverse effects can be increased when Drotebanol is combined with Baclofen.
DyclonineThe risk or severity of adverse effects can be increased when Dyclonine is combined with Baclofen.
EcgonineThe risk or severity of adverse effects can be increased when Ecgonine is combined with Baclofen.
ECGONINE METHYL ESTERThe risk or severity of adverse effects can be increased when ECGONINE METHYL ESTER is combined with Baclofen.
EfavirenzThe risk or severity of adverse effects can be increased when Baclofen is combined with Efavirenz.
EnfluraneThe risk or severity of adverse effects can be increased when Enflurane is combined with Baclofen.
EntacaponeThe risk or severity of adverse effects can be increased when Baclofen is combined with Entacapone.
EscitalopramThe risk or severity of adverse effects can be increased when Baclofen is combined with Escitalopram.
EstazolamThe risk or severity of adverse effects can be increased when Estazolam is combined with Baclofen.
EszopicloneThe risk or severity of adverse effects can be increased when Eszopiclone is combined with Baclofen.
EthanolBaclofen may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
EthanolThe risk or severity of adverse effects can be increased when Ethanol is combined with Baclofen.
EthchlorvynolThe risk or severity of adverse effects can be increased when Ethchlorvynol is combined with Baclofen.
EthosuximideThe risk or severity of adverse effects can be increased when Baclofen is combined with Ethosuximide.
EthotoinThe risk or severity of adverse effects can be increased when Baclofen is combined with Ethotoin.
Ethyl carbamateThe risk or severity of adverse effects can be increased when Ethyl carbamate is combined with Baclofen.
Ethyl loflazepateThe risk or severity of adverse effects can be increased when Ethyl loflazepate is combined with Baclofen.
EthylmorphineThe risk or severity of adverse effects can be increased when Ethylmorphine is combined with Baclofen.
EtidocaineThe risk or severity of adverse effects can be increased when Etidocaine is combined with Baclofen.
EtifoxineThe risk or severity of adverse effects can be increased when Etifoxine is combined with Baclofen.
EtizolamThe risk or severity of adverse effects can be increased when Etizolam is combined with Baclofen.
EtomidateThe risk or severity of adverse effects can be increased when Etomidate is combined with Baclofen.
EtoperidoneThe risk or severity of adverse effects can be increased when Baclofen is combined with Etoperidone.
EtorphineThe risk or severity of adverse effects can be increased when Etorphine is combined with Baclofen.
EzogabineThe risk or severity of adverse effects can be increased when Baclofen is combined with Ezogabine.
FelbamateThe risk or severity of adverse effects can be increased when Baclofen is combined with Felbamate.
FencamfamineThe risk or severity of adverse effects can be increased when Fencamfamine is combined with Baclofen.
FenfluramineThe risk or severity of adverse effects can be increased when Baclofen is combined with Fenfluramine.
FentanylThe risk or severity of adverse effects can be increased when Fentanyl is combined with Baclofen.
FexofenadineThe risk or severity of adverse effects can be increased when Baclofen is combined with Fexofenadine.
FlibanserinThe risk or severity of adverse effects can be increased when Baclofen is combined with Flibanserin.
FludiazepamThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Baclofen.
FlunarizineThe risk or severity of adverse effects can be increased when Baclofen is combined with Flunarizine.
FlunitrazepamThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Baclofen.
FluoxetineThe risk or severity of adverse effects can be increased when Baclofen is combined with Fluoxetine.
FlupentixolThe risk or severity of adverse effects can be increased when Flupentixol is combined with Baclofen.
FluphenazineThe risk or severity of adverse effects can be increased when Fluphenazine is combined with Baclofen.
FlurazepamThe risk or severity of adverse effects can be increased when Flurazepam is combined with Baclofen.
FluspirileneThe risk or severity of adverse effects can be increased when Fluspirilene is combined with Baclofen.
Fluticasone PropionateThe risk or severity of adverse effects can be increased when Baclofen is combined with Fluticasone Propionate.
FluvoxamineThe risk or severity of adverse effects can be increased when Baclofen is combined with Fluvoxamine.
FosphenytoinThe risk or severity of adverse effects can be increased when Baclofen is combined with Fosphenytoin.
FospropofolThe risk or severity of adverse effects can be increased when Fospropofol is combined with Baclofen.
GabapentinThe risk or severity of adverse effects can be increased when Gabapentin is combined with Baclofen.
gabapentin enacarbilThe risk or severity of adverse effects can be increased when Baclofen is combined with gabapentin enacarbil.
Gamma Hydroxybutyric AcidThe risk or severity of adverse effects can be increased when Gamma Hydroxybutyric Acid is combined with Baclofen.
GlutethimideThe risk or severity of adverse effects can be increased when Glutethimide is combined with Baclofen.
GuanfacineThe risk or severity of adverse effects can be increased when Baclofen is combined with Guanfacine.
HalazepamThe risk or severity of adverse effects can be increased when Halazepam is combined with Baclofen.
HaloperidolThe risk or severity of adverse effects can be increased when Haloperidol is combined with Baclofen.
HalothaneThe risk or severity of adverse effects can be increased when Halothane is combined with Baclofen.
HeroinThe risk or severity of adverse effects can be increased when Heroin is combined with Baclofen.
HexobarbitalThe risk or severity of adverse effects can be increased when Hexobarbital is combined with Baclofen.
HydrocodoneThe risk or severity of adverse effects can be increased when Hydrocodone is combined with Baclofen.
HydromorphoneThe risk or severity of adverse effects can be increased when Hydromorphone is combined with Baclofen.
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Baclofen.
HydroxyzineThe risk or severity of adverse effects can be increased when Baclofen is combined with Hydroxyzine.
IloperidoneThe risk or severity of adverse effects can be increased when Baclofen is combined with Iloperidone.
ImipramineThe risk or severity of adverse effects can be increased when Baclofen is combined with Imipramine.
IndalpineThe risk or severity of adverse effects can be increased when Baclofen is combined with Indalpine.
IsofluraneThe risk or severity of adverse effects can be increased when Isoflurane is combined with Baclofen.
KetamineThe risk or severity of adverse effects can be increased when Ketamine is combined with Baclofen.
KetazolamThe risk or severity of adverse effects can be increased when Ketazolam is combined with Baclofen.
KetobemidoneThe risk or severity of adverse effects can be increased when Ketobemidone is combined with Baclofen.
LacidipineBaclofen may increase the hypotensive activities of Lacidipine.
LamotrigineThe risk or severity of adverse effects can be increased when Baclofen is combined with Lamotrigine.
LevetiracetamThe risk or severity of adverse effects can be increased when Baclofen is combined with Levetiracetam.
LevobupivacaineThe risk or severity of adverse effects can be increased when Levobupivacaine is combined with Baclofen.
LevocabastineThe risk or severity of adverse effects can be increased when Baclofen is combined with Levocabastine.
LevocetirizineThe risk or severity of adverse effects can be increased when Baclofen is combined with Levocetirizine.
LevodopaThe risk or severity of adverse effects can be increased when Baclofen is combined with Levodopa.
Levomethadyl AcetateThe risk or severity of adverse effects can be increased when Levomethadyl Acetate is combined with Baclofen.
LevomilnacipranThe risk or severity of adverse effects can be increased when Baclofen is combined with Levomilnacipran.
LevorphanolThe risk or severity of adverse effects can be increased when Levorphanol is combined with Baclofen.
LidocaineThe risk or severity of adverse effects can be increased when Lidocaine is combined with Baclofen.
LithiumThe risk or severity of adverse effects can be increased when Lithium is combined with Baclofen.
LofentanilThe risk or severity of adverse effects can be increased when Lofentanil is combined with Baclofen.
LoratadineThe risk or severity of adverse effects can be increased when Baclofen is combined with Loratadine.
LorazepamThe risk or severity of adverse effects can be increased when Lorazepam is combined with Baclofen.
LoxapineThe risk or severity of adverse effects can be increased when Loxapine is combined with Baclofen.
Lu AA21004The risk or severity of adverse effects can be increased when Baclofen is combined with Lu AA21004.
LurasidoneThe risk or severity of adverse effects can be increased when Lurasidone is combined with Baclofen.
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Baclofen.
Magnesium SulfateThe risk or severity of adverse effects can be increased when Baclofen is combined with Magnesium Sulfate.
MaprotilineThe risk or severity of adverse effects can be increased when Baclofen is combined with Maprotiline.
MeclizineThe risk or severity of adverse effects can be increased when Baclofen is combined with Meclizine.
MedetomidineThe risk or severity of adverse effects can be increased when Medetomidine is combined with Baclofen.
MelatoninThe risk or severity of adverse effects can be increased when Melatonin is combined with Baclofen.
MelperoneThe risk or severity of adverse effects can be increased when Melperone is combined with Baclofen.
MepivacaineThe risk or severity of adverse effects can be increased when Mepivacaine is combined with Baclofen.
MeprobamateThe risk or severity of adverse effects can be increased when Meprobamate is combined with Baclofen.
MesoridazineThe risk or severity of adverse effects can be increased when Mesoridazine is combined with Baclofen.
MetaxaloneThe risk or severity of adverse effects can be increased when Baclofen is combined with Metaxalone.
MethadoneThe risk or severity of adverse effects can be increased when Methadone is combined with Baclofen.
Methadyl AcetateThe risk or severity of adverse effects can be increased when Methadyl Acetate is combined with Baclofen.
MethapyrileneThe risk or severity of adverse effects can be increased when Methapyrilene is combined with Baclofen.
MethaqualoneThe risk or severity of adverse effects can be increased when Methaqualone is combined with Baclofen.
MethocarbamolThe risk or severity of adverse effects can be increased when Baclofen is combined with Methocarbamol.
MethohexitalThe risk or severity of adverse effects can be increased when Methohexital is combined with Baclofen.
MethotrimeprazineThe risk or severity of adverse effects can be increased when Methotrimeprazine is combined with Baclofen.
MethoxyfluraneThe risk or severity of adverse effects can be increased when Methoxyflurane is combined with Baclofen.
MethsuximideThe risk or severity of adverse effects can be increased when Baclofen is combined with Methsuximide.
MethylphenobarbitalThe risk or severity of adverse effects can be increased when Methylphenobarbital is combined with Baclofen.
MetyrosineBaclofen may increase the sedative activities of Metyrosine.
MidazolamThe risk or severity of adverse effects can be increased when Midazolam is combined with Baclofen.
MilnacipranThe risk or severity of adverse effects can be increased when Baclofen is combined with Milnacipran.
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Baclofen.
MirtazapineBaclofen may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.
MirtazapineThe risk or severity of adverse effects can be increased when Mirtazapine is combined with Baclofen.
MolindoneThe risk or severity of adverse effects can be increased when Molindone is combined with Baclofen.
MorphineThe risk or severity of adverse effects can be increased when Morphine is combined with Baclofen.
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Baclofen.
NabiloneThe risk or severity of adverse effects can be increased when Baclofen is combined with Nabilone.
NalbuphineThe risk or severity of adverse effects can be increased when Nalbuphine is combined with Baclofen.
NitrazepamThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Baclofen.
Nitrous oxideThe risk or severity of adverse effects can be increased when Nitrous oxide is combined with Baclofen.
NormethadoneThe risk or severity of adverse effects can be increased when Normethadone is combined with Baclofen.
NortriptylineThe risk or severity of adverse effects can be increased when Baclofen is combined with Nortriptyline.
OlanzapineThe risk or severity of adverse effects can be increased when Baclofen is combined with Olanzapine.
OlopatadineThe risk or severity of adverse effects can be increased when Baclofen is combined with Olopatadine.
OndansetronThe risk or severity of adverse effects can be increased when Ondansetron is combined with Baclofen.
OpiumThe risk or severity of adverse effects can be increased when Opium is combined with Baclofen.
OrphenadrineBaclofen may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
OrphenadrineThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Baclofen.
OsanetantThe risk or severity of adverse effects can be increased when Osanetant is combined with Baclofen.
OxazepamThe risk or severity of adverse effects can be increased when Oxazepam is combined with Baclofen.
OxprenololThe risk or severity of adverse effects can be increased when Oxprenolol is combined with Baclofen.
OxybuprocaineThe risk or severity of adverse effects can be increased when Oxybuprocaine is combined with Baclofen.
OxycodoneThe risk or severity of adverse effects can be increased when Oxycodone is combined with Baclofen.
OxymorphoneThe risk or severity of adverse effects can be increased when Oxymorphone is combined with Baclofen.
PaliperidoneThe risk or severity of adverse effects can be increased when Paliperidone is combined with Baclofen.
ParaldehydeBaclofen may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
ParaldehydeThe risk or severity of adverse effects can be increased when Paraldehyde is combined with Baclofen.
ParoxetineThe risk or severity of adverse effects can be increased when Baclofen is combined with Paroxetine.
PentazocineThe risk or severity of adverse effects can be increased when Pentazocine is combined with Baclofen.
PentobarbitalThe risk or severity of adverse effects can be increased when Pentobarbital is combined with Baclofen.
PerampanelThe risk or severity of adverse effects can be increased when Baclofen is combined with Perampanel.
PerospironeThe risk or severity of adverse effects can be increased when Perospirone is combined with Baclofen.
PerphenazineThe risk or severity of adverse effects can be increased when Perphenazine is combined with Baclofen.
PethidineThe risk or severity of adverse effects can be increased when Pethidine is combined with Baclofen.
PhenobarbitalThe risk or severity of adverse effects can be increased when Phenobarbital is combined with Baclofen.
PhenoxyethanolThe risk or severity of adverse effects can be increased when Phenoxyethanol is combined with Baclofen.
PhenytoinThe risk or severity of adverse effects can be increased when Baclofen is combined with Phenytoin.
PimozideThe risk or severity of adverse effects can be increased when Pimozide is combined with Baclofen.
PipamperoneThe risk or severity of adverse effects can be increased when Pipamperone is combined with Baclofen.
PipotiazineThe risk or severity of adverse effects can be increased when Baclofen is combined with Pipotiazine.
PizotifenThe risk or severity of adverse effects can be increased when Baclofen is combined with Pizotifen.
PomalidomideThe risk or severity of adverse effects can be increased when Baclofen is combined with Pomalidomide.
PramipexoleBaclofen may increase the sedative activities of Pramipexole.
PramocaineThe risk or severity of adverse effects can be increased when Pramocaine is combined with Baclofen.
PrazepamThe risk or severity of adverse effects can be increased when Prazepam is combined with Baclofen.
PregabalinThe risk or severity of adverse effects can be increased when Pregabalin is combined with Baclofen.
PrilocaineThe risk or severity of adverse effects can be increased when Prilocaine is combined with Baclofen.
PrimidoneThe risk or severity of adverse effects can be increased when Baclofen is combined with Primidone.
ProcaineThe risk or severity of adverse effects can be increased when Procaine is combined with Baclofen.
ProchlorperazineThe risk or severity of adverse effects can be increased when Prochlorperazine is combined with Baclofen.
PromazineThe risk or severity of adverse effects can be increased when Promazine is combined with Baclofen.
PromethazineThe risk or severity of adverse effects can be increased when Baclofen is combined with Promethazine.
ProparacaineThe risk or severity of adverse effects can be increased when Proparacaine is combined with Baclofen.
PropofolThe risk or severity of adverse effects can be increased when Propofol is combined with Baclofen.
PropoxycaineThe risk or severity of adverse effects can be increased when Propoxycaine is combined with Baclofen.
ProtriptylineThe risk or severity of adverse effects can be increased when Baclofen is combined with Protriptyline.
PSD502The risk or severity of adverse effects can be increased when PSD502 is combined with Baclofen.
QuazepamThe risk or severity of adverse effects can be increased when Quazepam is combined with Baclofen.
QuetiapineThe risk or severity of adverse effects can be increased when Quetiapine is combined with Baclofen.
RamelteonThe risk or severity of adverse effects can be increased when Baclofen is combined with Ramelteon.
RemifentanilThe risk or severity of adverse effects can be increased when Remifentanil is combined with Baclofen.
RemoxiprideThe risk or severity of adverse effects can be increased when Remoxipride is combined with Baclofen.
ReserpineThe risk or severity of adverse effects can be increased when Reserpine is combined with Baclofen.
RisperidoneThe risk or severity of adverse effects can be increased when Risperidone is combined with Baclofen.
RomifidineThe risk or severity of adverse effects can be increased when Romifidine is combined with Baclofen.
RopiniroleBaclofen may increase the sedative activities of Ropinirole.
RopivacaineThe risk or severity of adverse effects can be increased when Ropivacaine is combined with Baclofen.
RotigotineBaclofen may increase the sedative activities of Rotigotine.
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Baclofen.
S-EthylisothioureaThe risk or severity of adverse effects can be increased when S-Ethylisothiourea is combined with Baclofen.
ScopolamineThe risk or severity of adverse effects can be increased when Baclofen is combined with Scopolamine.
SecobarbitalThe risk or severity of adverse effects can be increased when Secobarbital is combined with Baclofen.
SertindoleThe risk or severity of adverse effects can be increased when Sertindole is combined with Baclofen.
SertralineThe risk or severity of adverse effects can be increased when Baclofen is combined with Sertraline.
SevofluraneThe risk or severity of adverse effects can be increased when Sevoflurane is combined with Baclofen.
Sodium oxybateThe risk or severity of adverse effects can be increased when Sodium oxybate is combined with Baclofen.
StiripentolThe risk or severity of adverse effects can be increased when Baclofen is combined with Stiripentol.
SufentanilThe risk or severity of adverse effects can be increased when Sufentanil is combined with Baclofen.
SulpirideThe risk or severity of adverse effects can be increased when Sulpiride is combined with Baclofen.
SuvorexantThe risk or severity of adverse effects can be increased when Baclofen is combined with Suvorexant.
TapentadolThe risk or severity of adverse effects can be increased when Baclofen is combined with Tapentadol.
TasimelteonThe risk or severity of adverse effects can be increased when Baclofen is combined with Tasimelteon.
TemazepamThe risk or severity of adverse effects can be increased when Temazepam is combined with Baclofen.
TetrabenazineThe risk or severity of adverse effects can be increased when Baclofen is combined with Tetrabenazine.
TetracaineThe risk or severity of adverse effects can be increased when Tetracaine is combined with Baclofen.
TetrodotoxinThe risk or severity of adverse effects can be increased when Tetrodotoxin is combined with Baclofen.
ThalidomideBaclofen may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
ThalidomideThe risk or severity of adverse effects can be increased when Thalidomide is combined with Baclofen.
ThiamylalThe risk or severity of adverse effects can be increased when Thiamylal is combined with Baclofen.
ThiopentalThe risk or severity of adverse effects can be increased when Thiopental is combined with Baclofen.
ThioridazineThe risk or severity of adverse effects can be increased when Thioridazine is combined with Baclofen.
ThiothixeneThe risk or severity of adverse effects can be increased when Thiothixene is combined with Baclofen.
TiagabineThe risk or severity of adverse effects can be increased when Baclofen is combined with Tiagabine.
TiletamineThe risk or severity of adverse effects can be increased when Tiletamine is combined with Baclofen.
TizanidineThe risk or severity of adverse effects can be increased when Baclofen is combined with Tizanidine.
TolcaponeThe risk or severity of adverse effects can be increased when Baclofen is combined with Tolcapone.
TopiramateThe risk or severity of adverse effects can be increased when Baclofen is combined with Topiramate.
TramadolThe risk or severity of adverse effects can be increased when Tramadol is combined with Baclofen.
Trans-2-PhenylcyclopropylamineThe risk or severity of adverse effects can be increased when Trans-2-Phenylcyclopropylamine is combined with Baclofen.
TranylcypromineThe risk or severity of adverse effects can be increased when Tranylcypromine is combined with Baclofen.
TrazodoneThe risk or severity of adverse effects can be increased when Baclofen is combined with Trazodone.
TriazolamThe risk or severity of adverse effects can be increased when Triazolam is combined with Baclofen.
TrifluoperazineThe risk or severity of adverse effects can be increased when Trifluoperazine is combined with Baclofen.
TriflupromazineThe risk or severity of adverse effects can be increased when Triflupromazine is combined with Baclofen.
TrimipramineThe risk or severity of adverse effects can be increased when Baclofen is combined with Trimipramine.
TriprolidineThe risk or severity of adverse effects can be increased when Baclofen is combined with Triprolidine.
Valproic AcidThe risk or severity of adverse effects can be increased when Valproic Acid is combined with Baclofen.
VigabatrinThe risk or severity of adverse effects can be increased when Baclofen is combined with Vigabatrin.
VilazodoneThe risk or severity of adverse effects can be increased when Baclofen is combined with Vilazodone.
VortioxetineThe risk or severity of adverse effects can be increased when Baclofen is combined with Vortioxetine.
XylazineThe risk or severity of adverse effects can be increased when Xylazine is combined with Baclofen.
ZaleplonThe risk or severity of adverse effects can be increased when Zaleplon is combined with Baclofen.
ZiconotideThe risk or severity of adverse effects can be increased when Baclofen is combined with Ziconotide.
ZimelidineThe risk or severity of adverse effects can be increased when Baclofen is combined with Zimelidine.
ZiprasidoneThe risk or severity of adverse effects can be increased when Ziprasidone is combined with Baclofen.
ZolazepamThe risk or severity of adverse effects can be increased when Zolazepam is combined with Baclofen.
ZolpidemThe risk or severity of adverse effects can be increased when Zolpidem is combined with Baclofen.
ZonisamideThe risk or severity of adverse effects can be increased when Baclofen is combined with Zonisamide.
ZopicloneThe risk or severity of adverse effects can be increased when Zopiclone is combined with Baclofen.
ZotepineThe risk or severity of adverse effects can be increased when Zotepine is combined with Baclofen.
ZuclopenthixolThe risk or severity of adverse effects can be increased when Zuclopenthixol is combined with Baclofen.
Food Interactions
  • Avoid alcohol.
  • Take without regard to meals.

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
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
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
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 ]
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Drug created on June 13, 2005 07:24 / Updated on September 27, 2016 02:26