Heads up!
We’ve moved some things around. Take a quick tour to learn what has changed.
Take the tour
No thanks!
Baclofen
Identification
- Name
- Baclofen
- Accession Number
- DB00181
- Description
Baclofen is a gamma-aminobutyric acid (GABA) agonist used as a skeletal muscle relaxant used for the relief of painful and uncomfortable muscle spasms caused by a variety of conditions. It is known to be particularly useful in treating muscle spasticity associated with spinal cord injury Label.
This drug has recently been studied for the management of alcohol withdrawal, however, a conclusion has not been made regarding baclofen efficacy in this condition 5, 6, 12.
This drug was initially approved by the FDA in 1992 18. It is available in tablet form Label, injection form 18, and powder form (for suspension) 15.
- Type
- Small Molecule
- Groups
- Approved
- Structure
Structure for Baclofen (DB00181)
- Weight
- Average: 213.661
Monoisotopic: 213.05565634 - Chemical Formula
- C10H12ClNO2
- Synonyms
- (+-)-Baclofen
- 4-Amino-3-(4-chlorophenyl)butyric acid
- Baclofen
- Baclofène
- 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
Pharmacology
- Indication
Baclofen is administered for the relief of signs and symptoms of spasticity resulting from multiple sclerosis, particularly for the relief of flexor spasms and associated pain and clonus, in addition to muscular rigidity Label.
Patients receiving this drug should have reversible spasticity for baclofen to promote the restoration of residual function. This drug is not indicated in the treatment of skeletal muscle spasm caused by rheumatic disorders. The efficacy of baclofen in stroke, cerebral palsy, and Parkinson's disease has not been determined and, therefore, baclofen is not recommended for these conditions Label.
- Associated Conditions
- Contraindications & Blackbox Warnings
Learn about our commercial Contraindications & Blackbox Warnings data.
Learn More- Pharmacodynamics
In neurological diseases associated with spasm of the skeletal muscles, the clinical effects of baclofen occur due to baclofen action on reflex muscle contractions and of significant relief from painful spasm, automatism, as well as clonus. Baclofen, when used as indicated, improves mobility, increasing levels of independence, and facilitates both passive and active physiotherapy. Baclofen also stimulates gastric acid secretion 16.
GABA-B receptor activation by baclofen may produce protective neurological effects. Baclofen also possesses anti-inflammatory properties that may be of interest in the study of addiction treatment 12. Preclinical studies have shown that GABA-B receptors have roles in memory storage and retrieval, reward, motivation, mood, as well as anxiety. Neuroimaging studies in humans indicate that baclofen produces region-specific alterations in brain activity.
- Mechanism of action
The exact mechanism of action of baclofen is not fully understood at this time Label, 17. Many studies indicate that baclofen is a GABA-B receptor agonist 2, 8, 9, 10, 11. Despite this, there is no conclusive evidence that the effects of baclofen on GABA systems are involved in the production of its clinical effects Label.
Baclofen is an effective and widely used antispastic agent with a spinal site of action. Its mechanism of action and pharmacological properties are different from the effects of other antispastic agents. In addition, baclofen has central sites of action, shown by its adverse event profile and general CNS depressant properties 16. GABA-B receptors interact with signal transduction pathways and neurotransmitter systems. Baclofen exerts an antinociceptive effect. The clinical significance of this warrants further research data for clarification.
Baclofen depresses monosynaptic and polysynaptic reflex transmission, by various actions, and possibly including the stimulation of GABAβ-receptors. This stimulation results in the inhibition of excitatory neurotransmitter (glutamate and aspartate) release, which may normally contribute to pain and spasticity16. Although baclofen is an analog of the inhibitory neurotransmitter gamma-amino-butyric acid (GABA), there are no conclusive data indicating GABA systems are involved in its clinical effects Label.
Target Actions Organism UGamma-aminobutyric acid type B receptor subunit 1 agonistHumans AGamma-aminobutyric acid type B receptor subunit 2 agonistHumans - Absorption
Rapidly and almost completely absorbed from the gastrointestinal tract. Absorption may be dose-dependent, being reduced with increased doses Label.
Baclofen, when introduced directly into the intrathecal space, allows for effective CSF concentrations to be achieved with resulting plasma concentrations 100 times less than concentrations occurring with oral administration 17, Label.
- Volume of distribution
Apparent volume of distribution: 59 liters Label.
Baclofen does not readily cross the blood-brain barrier Label.
- Protein binding
30% Label
- Metabolism
Approximately 15% of the dose is metabolized in the liver, mainly by deamination Label.
In a clinical study with radiolabeled baclofen, approximately 85% of the dose was excreted unchanged in the urine and feces. The γ-hydroxy metabolite, 3-(p-chlorophenyl)-4-hydroxybutyric acid, is formed by the deamination of baclofen Label.
Because baclofen is partially metabolized in the liver, patients with impaired liver function should be regularly monitored with liver function tests 16.
Hover over products below to view reaction partners
- Route of elimination
Baclofen is rapidly and extensively eliminated from the body. There is significant intersubject variation in elimination rates. Baclofen is excreted mainly by the kidney as unchanged drug. Seventy to eighty (70 - 80%) of a dose is measured in the urine as unchanged drug. The remainder of the dose is excreted as unchanged drug in the feces or as metabolites in the urine and feces. Excretion is complete within 72 hours after administration Label.
- Half-life
Elimination half-life: Approximately 5.5 hours Label.
- Clearance
Total systemic clearance: 180 mL/min Label Renal clearance: 103 mL/min Label
Baclofen is primarily excreted unchanged by the kidneys. It should be administered cautiously, and it may be necessary to reduce the dosage in patients with reduced renal function Label.
- Adverse Effects
Learn about our commercial Adverse Effects data.
Learn More- Toxicity
LD50 after oral administration in rats: 145 mg/kg MSDS
Overdosage: Vomiting, muscular hypotonia, drowsiness, accommodation disorders, coma, respiratory depression, and seizures may occur with overdosage Label.
Pregnancy: This drug is a pregnancy category C drug. There are no adequate and well-controlled studies that have been performed with pregnant women. Baclofen should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus Label.
Excretion in breastmilk: It is unknown whether this drug is excreted in human breast milk. Because many drugs are excreted in human milk, caution is warranted when baclofen is administered to a nursing woman Label.
- Affected organisms
- Humans and other mammals
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Unlock Additional DataAbacavir Baclofen may decrease the excretion rate of Abacavir which could result in a higher serum level. Acarbose The therapeutic efficacy of Acarbose can be decreased when used in combination with Baclofen. Acebutolol The risk or severity of adverse effects can be increased when Baclofen is combined with Acebutolol. Aceclofenac Aceclofenac may decrease the excretion rate of Baclofen which could result in a higher serum level. Acemetacin Acemetacin may decrease the excretion rate of Baclofen which could result in a higher serum level. Acetaminophen Baclofen may decrease the excretion rate of Acetaminophen which could result in a higher serum level. Acetazolamide The risk or severity of adverse effects can be increased when Baclofen is combined with Acetazolamide. Acetohexamide The therapeutic efficacy of Acetohexamide can be decreased when used in combination with Baclofen. Acetophenazine The risk or severity of adverse effects can be increased when Baclofen is combined with Acetophenazine. Acetylsalicylic acid Acetylsalicylic acid may decrease the excretion rate of Baclofen which could result in a higher serum level. Additional Data Available- Extended DescriptionExtended Description
Extended description of the mechanism of action and particular properties of each drug interaction.
Learn more - Severity
- Evidence Level
- ActionAction
An effect category for each drug interaction. Know how this interaction affects the subject drug.
Learn more
- Food Interactions
- Avoid alcohol.
- Take with food. Take with food or milk to reduce gastric irritation.
Products
- Product Ingredients
Ingredient UNII CAS InChI Key Baclofen hydrochloride 64OSE3996V 28311-31-1 WMNUVYYLMCMHLU-UHFFFAOYSA-N - Product Images
- International/Other Brands
- Baclon (Uniao Quimica (Brazil)) / Lioresal Intrathecal (Novartis Pharmaceuticals) / Nu-Baclofen (Nu-Pharm)
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Unlock Additional DataBaclofen Tablet 20 mg/1 Oral Vintage Pharmaceuticals, LLC 2007-05-17 2007-05-17 US 
Baclofen Tablet 10 mg Oral Apotex Corporation 1994-12-31 2014-08-23 Canada 
Baclofen Tablet 10 mg Oral Sanis Health Inc 2010-02-25 Not applicable Canada Baclofen Tablet 10 mg/1 Oral Caraco Pharmaceutical Laboratories, Ltd. 2007-03-30 Not applicable US Baclofen Tablet 10 mg/1 Oral Vintage Pharmaceuticals, LLC 2007-05-17 2007-05-17 US Baclofen Tablet 20 mg Oral Apotex Corporation 1994-12-31 2014-08-23 Canada Baclofen Tablet 20 mg Oral Sanis Health Inc 2010-02-25 Not applicable Canada Baclofen Tablet 20 mg/1 Oral Caraco Pharmaceutical Laboratories, Ltd. 2007-03-30 Not applicable US Baclofen Injection Solution Intrathecal Sterimax Inc 2014-06-06 Not applicable Canada Baclofen Injection Solution Intrathecal Teligent Ou 2017-08-25 Not applicable Canada Additional Data Available- Application NumberApplication Number
A unique ID assigned by the FDA when a product is submitted for approval by the labeller.
Learn more - Product CodeProduct Code
A governmentally-recognized ID which uniquely identifies the product within its regulatory market.
Learn more
- Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Unlock Additional DataApo-baclofen Tablet Oral Apotex Corporation 1994-12-31 Not applicable Canada Apo-baclofen Tablet Oral Apotex Corporation 1994-12-31 Not applicable Canada Ava-baclofen Tablet Oral Avanstra Inc 2011-10-11 2014-08-21 Canada Ava-baclofen Tablet Oral Avanstra Inc 2011-10-11 2014-08-21 Canada Baclofen Tablet 20 mg/1 Oral Avera McKennan Hospital 2015-03-31 2017-05-24 US 
Baclofen Tablet 10 mg/1 Oral Caremark L.L.C. 2003-09-26 2011-07-31 US Baclofen Tablet 20 mg/1 Oral Dispensing Solutions, Inc. 2005-08-30 Not applicable US Baclofen Tablet 10 mg/1 Oral REMEDYREPACK INC. 2013-12-11 2016-10-22 US 
Baclofen Tablet 10 mg/1 Oral Par Pharmaceutical 2005-08-30 Not applicable US 
Baclofen Tablet 10 mg/1 Oral bryant ranch prepack 2007-07-01 Not applicable US Additional Data Available- Application NumberApplication Number
A unique ID assigned by the FDA when a product is submitted for approval by the labeller.
Learn more - Product CodeProduct Code
A governmentally-recognized ID which uniquely identifies the product within its regulatory market.
Learn more
- Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Equipto - Baclofen External Cream Compounding Kit Baclofen (1 g/1g) Kit Topical Alvix Laboratories 2015-01-20 2018-03-08 US Gapeam Budibac Baclofen (1 g/1g) + Amantadine hydrochloride (1 g/1g) + Bupivacaine hydrochloride anhydrous (1 g/1g) + Cyclobenzaprine hydrochloride (1 g/1g) + Diclofenac sodium (1 g/1g) + Gabapentin (1 g/1g) + Pentoxifylline (1 g/1g) Kit Topical Alvix Laboratories 2014-12-05 2018-03-08 US Innoprax-5 Baclofen (3 g/3g) + Amantadine hydrochloride (8 g/8g) + Diclofenac sodium (3 g/3g) + Gabapentin (6 g/6g) + Lidocaine hydrochloride (5 g/5g) Kit Topical Accumix Pharmaceuticals 2014-12-15 2015-07-17 US
Categories
- ATC Codes
- M03BX01 — Baclofen
- Drug Categories
- Agents Causing Muscle Toxicity
- Amino Acids
- Amino Acids, Peptides, and Proteins
- Aminobutyrates
- Butyrates
- Central Nervous System Agents
- Central Nervous System Depressants
- Drugs that are Mainly Renally Excreted
- GABA Agents
- GABA Agonists
- GABA-B Receptor Agonists
- Gaba-derivative Skeletal Muscle Relaxants
- gamma-Aminobutyric Acid-ergic Agonist
- Muscle Relaxants
- Muscle Relaxants, Centrally Acting Agents
- Muscle Relaxants, Peripherally Acting Agents
- Musculo-Skeletal System
- Neurotransmitter Agents
- Chemical TaxonomyProvided by Classyfire
- Description
- This 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.
- Kingdom
- Organic compounds
- Super Class
- Organic acids and derivatives
- Class
- Carboxylic acids and derivatives
- Sub Class
- Amino acids, peptides, and analogues
- Direct Parent
- Gamma amino acids and derivatives
- Alternative Parents
- Phenylpropanoic acids / Chlorobenzenes / Aralkylamines / Amino fatty acids / Aryl chlorides / Amino acids / Monocarboxylic acids and derivatives / Carboxylic acids / Organopnictogen compounds / Organochlorides show 4 more
- Substituents
- 3-phenylpropanoic-acid / Amine / Amino acid / Amino fatty acid / Aralkylamine / Aromatic homomonocyclic compound / Aryl chloride / Aryl halide / Benzenoid / Carbonyl group show 18 more
- Molecular Framework
- Aromatic homomonocyclic compounds
- External Descriptors
- monocarboxylic acid, primary amino compound, monochlorobenzenes, gamma-amino acid (CHEBI:2972)
Chemical Identifiers
- UNII
- H789N3FKE8
- CAS number
- 1134-47-0
- InChI Key
- 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
References
- Synthesis Reference
- US5843765
- General References
- 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]
- 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]
- See S, Ginzburg R: Skeletal muscle relaxants. Pharmacotherapy. 2008 Feb;28(2):207-13. doi: 10.1592/phco.28.2.207. [PubMed:18225966]
- Brennan JL, Leung JG, Gagliardi JP, Rivelli SK, Muzyk AJ: Clinical effectiveness of baclofen for the treatment of alcohol dependence: a review. Clin Pharmacol. 2013 Jul 3;5:99-107. doi: 10.2147/CPAA.S32434. Print 2013. [PubMed:23869179]
- Liu J, Wang LN: Baclofen for alcohol withdrawal. Cochrane Database Syst Rev. 2017 Aug 20;8:CD008502. doi: 10.1002/14651858.CD008502.pub5. [PubMed:28822350]
- Liu J, Wang LN: Baclofen for alcohol withdrawal. Cochrane Database Syst Rev. 2013 Feb 28;(2):CD008502. doi: 10.1002/14651858.CD008502.pub3. [PubMed:23450582]
- Dario A, Tomei G: A benefit-risk assessment of baclofen in severe spinal spasticity. Drug Saf. 2004;27(11):799-818. doi: 10.2165/00002018-200427110-00004. [PubMed:15350152]
- Finnimore AJ, Roebuck M, Sajkov D, McEvoy RD: The effects of the GABA agonist, baclofen, on sleep and breathing. Eur Respir J. 1995 Feb;8(2):230-4. [PubMed:7758556]
- Chen K, Li HZ, Ye N, Zhang J, Wang JJ: Role of GABAB receptors in GABA and baclofen-induced inhibition of adult rat cerebellar interpositus nucleus neurons in vitro. Brain Res Bull. 2005 Oct 30;67(4):310-8. doi: 10.1016/j.brainresbull.2005.07.004. [PubMed:16182939]
- Fu Z, Yang H, Xiao Y, Zhao G, Huang H: The gamma-aminobutyric acid type B (GABAB) receptor agonist baclofen inhibits morphine sensitization by decreasing the dopamine level in rat nucleus accumbens. Behav Brain Funct. 2012 Jul 10;8:20. doi: 10.1186/1744-9081-8-20. [PubMed:22559224]
- Di Ciano P, Everitt BJ: The GABA(B) receptor agonist baclofen attenuates cocaine- and heroin-seeking behavior by rats. Neuropsychopharmacology. 2003 Mar;28(3):510-8. doi: 10.1038/sj.npp.1300088. Epub 2002 Oct 14. [PubMed:12629530]
- de Beaurepaire R: A Review of the Potential Mechanisms of Action of Baclofen in Alcohol Use Disorder. Front Psychiatry. 2018 Oct 17;9:506. doi: 10.3389/fpsyt.2018.00506. eCollection 2018. [PubMed:30459646]
- Hara T, Nakajima M, Sugano H, Karagiozov K, Hirose E, Goto K, Arai H: Pregnancy and Breastfeeding during Intrathecal Baclofen Therapy - A Case Study and Review. NMC Case Rep J. 2018 Jun 25;5(3):65-68. doi: 10.2176/nmccrj.cr.2017-0191. eCollection 2018 Jul. [PubMed:30023142]
- Baclofen tablets [Link]
- Baclofen powder, DailyMed [Link]
- Pacifen Medsafe NZ [File]
- Lioresal (intrathecal) FDA label [File]
- Gablofen (Baclofen injection) FDA label [File]
- External Links
- Human Metabolome Database
- HMDB0014327
- KEGG Drug
- D00241
- PubChem Compound
- 2284
- PubChem Substance
- 46508181
- ChemSpider
- 2197
- BindingDB
- 24182
- 1292
- ChEBI
- 2972
- ChEMBL
- CHEMBL701
- Therapeutic Targets Database
- DAP000257
- PharmGKB
- PA448533
- Guide to Pharmacology
- GtP Drug Page
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Baclofen
- AHFS Codes
- 12:20.12 — Gaba-derivative Skeletal Muscle Relaxants
- FDA label
- Download (135 KB)
- MSDS
- Download (73.4 KB)
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Active Not Recruiting Basic Science Spasticity, Muscle 1 4 Completed Treatment Alcohol Dependence 1 4 Completed Treatment Alcohol Use Disorders (AUD) / Hepatitis C Viral Infection 1 4 Completed Treatment Back Pain Lower Back 1 4 Completed Treatment Recurrent Crying Spells 1 4 Completed Treatment Rumination Disorders / Supra-gastric Belching 1 4 Completed Treatment Severe Spasticity 1 4 Completed Treatment Spasticity 1 4 Not Yet Recruiting Treatment Hiccups 1 4 Not Yet Recruiting Treatment Spastic Hemiplegia / Stroke Sequelae 1
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
- Actavis Group
- Advanced Pharmaceutical Services Inc.
- Aidarex Pharmacuticals LLC
- Alphapharm Party Ltd.
- Amerisource Health Services Corp.
- Apotheca Inc.
- A-S Medication Solutions LLC
- Bryant Ranch Prepack
- Caraco Pharmaceutical Labs
- Cardinal Health
- Caremark LLC
- Comprehensive Consultant Services Inc.
- Corepharma LLC
- Direct Dispensing Inc.
- Dispensing Solutions
- Diversified Healthcare Services Inc.
- Genpharm LP
- Heartland Repack Services LLC
- Innoviant Pharmacy Inc.
- Ivax Pharmaceuticals
- Keltman Pharmaceuticals Inc.
- Lake Erie Medical and Surgical Supply
- Lannett Co. Inc.
- Major Pharmaceuticals
- Mckesson Corp.
- Medisca Inc.
- Medtronic
- Murfreesboro Pharmaceutical Nursing Supply
- Mylan
- Northstar Rx LLC
- Novartis AG
- Nucare Pharmaceuticals Inc.
- Palmetto Pharmaceuticals Inc.
- PD-Rx Pharmaceuticals Inc.
- Pharmaceutical Packaging Center
- Physicians Total Care Inc.
- Piramal Healthcare
- Preferred Pharmaceuticals Inc.
- Prepak Systems Inc.
- Prescription Dispensing Service Inc.
- Qualitest
- Rebel Distributors Corp.
- Remedy Repack
- Resource Optimization and Innovation LLC
- Sandhills Packaging Inc.
- Southwood Pharmaceuticals
- St Mary's Medical Park Pharmacy
- Stat Rx Usa
- UDL Laboratories
- United Research Laboratories Inc.
- USL Pharma Inc.
- Vangard Labs Inc.
- Vintage Pharmaceuticals Inc.
- Watson Pharmaceuticals
- Dosage Forms
Form Route Strength Injection, solution Intrathecal 10 mg/20mL Injection, solution Intrathecal 1000 ug/1mL Injection, solution Intrathecal 40 mg/20mL Tablet Oral 20 mg Tablet Oral 5 mg/1 Injection Intrathecal 10 mg/20mL Injection Intrathecal 40 mg/20mL Solution Intrathecal 0.05 mg Tablet 25 MG Tablet 10 MG Solution Injection 0.05 mg/1ml Injection 10 mg/20ml Injection 10 mg/5ml Injection 40 mg/20ml Injection, solution Intrathecal 0.05 MG/ML Tablet Oral 25 MG Tablet Oral 10 mg/1 Tablet Oral 20 mg/1 Solution Intrathecal 10 mg Kit Topical 1 g/1g Injection Intrathecal 1000 ug/1mL Injection Intrathecal 2000 ug/1mL Injection Intrathecal 50 ug/1mL Injection Intrathecal 500 ug/1mL Injection, solution Intrathecal 2000 ug/1mL Injection, solution Intrathecal 50 ug/1mL Injection, solution Intrathecal 500 ug/1mL Kit Topical Tablet, orally disintegrating Oral 10 mg/1 Tablet, orally disintegrating Oral 20 mg/1 Injection Intrathecal 0.05 mg/1mL Injection Intrathecal 0.5 mg/1mL Injection Intrathecal 2 mg/1mL Injection, solution Intrathecal 0.05 MG/1ML Injection, solution Intrathecal 10 MG/5ML Injection Intrathecal 10 mg/5mL Tablet Oral 10 mg Tablet Tablet 5 mg Solution Intrathecal Tablet Oral Solution Oral 5 mg/5mL - Prices
Unit description Cost Unit Lioresal it 0.05 mg/1 ml amp 84.0USD ml Lioresal it 10 mg/5 ml kit 51.6USD ml Lioresal Intrathecal 2 mg/ml 44.64USD ml Lioresal Intrathecal 0.05 mg/ml 14.89USD ml Baclofen powder 14.38USD g Lioresal it 10 mg/20 ml kit 12.9USD ml Lioresal Intrathecal 0.5 mg/ml 11.16USD ml Lioresal D.S. 20 mg Tablet 1.4USD tablet Baclofen 20 mg tablet 0.92USD tablet Lioresal 10 mg Tablet 0.72USD tablet Apo-Baclofen 20 mg Tablet 0.59USD tablet Mylan-Baclofen 20 mg Tablet 0.59USD tablet Nu-Baclo 20 mg Tablet 0.59USD tablet Phl-Baclofen 20 mg Tablet 0.59USD tablet Pms-Baclofen 20 mg Tablet 0.59USD tablet Ratio-Baclofen 20 mg Tablet 0.59USD tablet Baclofen 10 mg tablet 0.51USD tablet Apo-Baclofen 10 mg Tablet 0.3USD tablet Mylan-Baclofen 10 mg Tablet 0.3USD tablet Nu-Baclo 10 mg Tablet 0.3USD tablet Phl-Baclofen 10 mg Tablet 0.3USD tablet Pms-Baclofen 10 mg Tablet 0.3USD tablet Ratio-Baclofen 10 mg Tablet 0.3USD tablet DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region Unlock Additional DataUS6221392 No 2001-04-24 2018-04-09 US US6024981 No 2000-02-15 2018-04-09 US US10610502 No 2019-08-30 2039-08-30 US Additional Data Available- Filed On
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 207 MSDS boiling point (°C) Decomposes MSDS water solubility slightly soluble FDA label logP 1.3 http://www.hmdb.ca/metabolites/HMDB0014327 Caco2 permeability 0.9 https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6186984/ pKa 9.62 + 0.1 (amino group) and 3.87 + 0.1 (carboxyl group) http://www.labriva.com/monographies/02242151eng.pdf - Predicted Properties
Property Value Source Water Solubility 0.712 mg/mL ALOGPS logP -0.82 ALOGPS logP -0.78 ChemAxon logS -2.5 ALOGPS pKa (Strongest Acidic) 3.89 ChemAxon pKa (Strongest Basic) 9.79 ChemAxon Physiological Charge 0 ChemAxon Hydrogen Acceptor Count 3 ChemAxon Hydrogen Donor Count 2 ChemAxon Polar Surface Area 63.32 Å2 ChemAxon Rotatable Bond Count 4 ChemAxon Refractivity 54.83 m3·mol-1 ChemAxon Polarizability 21.13 Å3 ChemAxon Number of Rings 1 ChemAxon Bioavailability 1 ChemAxon Rule of Five Yes ChemAxon Ghose Filter No ChemAxon Veber's Rule No ChemAxon MDDR-like Rule No ChemAxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.978 Blood Brain Barrier + 0.9339 Caco-2 permeable + 0.5668 P-glycoprotein substrate Non-substrate 0.7373 P-glycoprotein inhibitor I Non-inhibitor 0.9825 P-glycoprotein inhibitor II Non-inhibitor 0.9842 Renal organic cation transporter Non-inhibitor 0.8435 CYP450 2C9 substrate Non-substrate 0.8746 CYP450 2D6 substrate Non-substrate 0.8426 CYP450 3A4 substrate Non-substrate 0.7618 CYP450 1A2 substrate Non-inhibitor 0.9046 CYP450 2C9 inhibitor Non-inhibitor 0.9071 CYP450 2D6 inhibitor Non-inhibitor 0.736 CYP450 2C19 inhibitor Non-inhibitor 0.8215 CYP450 3A4 inhibitor Non-inhibitor 0.8309 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.9204 Ames test Non AMES toxic 0.8621 Carcinogenicity Non-carcinogens 0.7401 Biodegradation Not ready biodegradable 0.7362 Rat acute toxicity 3.1364 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.9478 hERG inhibition (predictor II) Non-inhibitor 0.8578
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- 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 coup...
- Gene Name
- GABBR1
- Uniprot ID
- Q9UBS5
- Uniprot Name
- Gamma-aminobutyric acid type B receptor subunit 1
- Molecular Weight
- 108319.4 Da
References
- Bowery NG: GABAB receptor pharmacology. Annu Rev Pharmacol Toxicol. 1993;33:109-47. [PubMed:8388192]
- 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]
- 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]
- 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]
- 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]
- 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]
- Pittman QJ: The action is at the terminal. J Physiol. 1999 Nov 1;520 Pt 3:629. [PubMed:10545129]
- 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]
- Fu Z, Yang H, Xiao Y, Zhao G, Huang H: The gamma-aminobutyric acid type B (GABAB) receptor agonist baclofen inhibits morphine sensitization by decreasing the dopamine level in rat nucleus accumbens. Behav Brain Funct. 2012 Jul 10;8:20. doi: 10.1186/1744-9081-8-20. [PubMed:22559224]
- Chen K, Li HZ, Ye N, Zhang J, Wang JJ: Role of GABAB receptors in GABA and baclofen-induced inhibition of adult rat cerebellar interpositus nucleus neurons in vitro. Brain Res Bull. 2005 Oct 30;67(4):310-8. doi: 10.1016/j.brainresbull.2005.07.004. [PubMed:16182939]
- Kind
- Protein
- Organism
- Humans
- 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 coup...
- Gene Name
- GABBR2
- Uniprot ID
- O75899
- Uniprot Name
- Gamma-aminobutyric acid type B receptor subunit 2
- Molecular Weight
- 105820.52 Da
References
- 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]
- Bowery NG: GABAB receptor pharmacology. Annu Rev Pharmacol Toxicol. 1993;33:109-47. [PubMed:8388192]
- 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]
- 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]
- 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]
- Pittman QJ: The action is at the terminal. J Physiol. 1999 Nov 1;520 Pt 3:629. [PubMed:10545129]
- Fu Z, Yang H, Xiao Y, Zhao G, Huang H: The gamma-aminobutyric acid type B (GABAB) receptor agonist baclofen inhibits morphine sensitization by decreasing the dopamine level in rat nucleus accumbens. Behav Brain Funct. 2012 Jul 10;8:20. doi: 10.1186/1744-9081-8-20. [PubMed:22559224]
- Chen K, Li HZ, Ye N, Zhang J, Wang JJ: Role of GABAB receptors in GABA and baclofen-induced inhibition of adult rat cerebellar interpositus nucleus neurons in vitro. Brain Res Bull. 2005 Oct 30;67(4):310-8. doi: 10.1016/j.brainresbull.2005.07.004. [PubMed:16182939]
Drug created on June 13, 2005 07:24 / Updated on September 27, 2020 08:17
Are you a
new drug developer?
Contact us to learn more about our customized products and solutions.
![]({"CS-Molecular-Health-1.jpg":"/assets/ads/CS-Molecular-Health-1-19e76f023997d5ac198da2cb9976457f7b9ba733f0ea8a780fe21191c759e8fa.jpg","Drug-Dev-2.jpg":"/assets/ads/Drug-Dev-2-7c3039d93245f493c23278efbf759e4f933848a676262d579087d5cc516af179.jpg","Drug-Search-3.jpg":"/assets/ads/Drug-Search-3-7346c33d2133f62b46cbfbbe2b666e78f955c6847e242692c6081fec37c4d10d.jpg","PM-3.jpg":"/assets/ads/PM-3-13494ac4c996d71619127a11f685681418d4280832dec162c0b2c9c8bc2eda50.jpg","OD-Webinar-1.jpg":"/assets/ads/OD-Webinar-1-f9357f6d57fef5e411aa1c0439ef46c86d9151214434659d096eeed6407b799b.jpg","DDI-3.jpg":"/assets/ads/DDI-3-12808cf864d540ad43757b10b08fc52ae93e793b0c6e81345555187b2840ad09.jpg","EMR-2.jpg":"/assets/ads/EMR-2-adacf8de3f42cb06d6676d06fce611c29781db6ad30776cd18b72a7d8e69f0c8.jpg","Covid.jpg":"/assets/ads/Covid-eed8f17668b0308db62ce3c656f5e2f562376e9185ae08dda5ce6ed9ab0bbd1f.jpg","CS-Molecular-Health-2.jpg":"/assets/ads/CS-Molecular-Health-2-22f41f94b3f87e44a1dcaa8f6c03dc411ab69558efd4f3148ff9bb6adaa956dc.jpg","PM-5.jpg":"/assets/ads/PM-5-d0dc031e0fa0d0097d912eff07b7e80b27b867264dd5b055e379a57bfa2a8723.jpg","DDI-4.jpg":"/assets/ads/DDI-4-313b9c374b937fd78bb2ade652b9b030abb9e6cb90efd35833f793e384e8185b.jpg","Discover-1.jpg":"/assets/ads/Discover-1-b48ae6a3872eeb442f4c22a9a1d867428c83a917ec78a8c3ff4e02f84c5d4fef.jpg","Discover-2.jpg":"/assets/ads/Discover-2-6e7759998ee0fdc234cd84eea962f2480f0c7dafadabd785924918420decb102.jpg","Repurpose-1.jpg":"/assets/ads/Repurpose-1-265fbec40f0eac18d51d3ec4f558c10cb623d834ea75e0296259e458b72ee6d4.jpg","Repurpose-2.jpg":"/assets/ads/Repurpose-2-d12bd1d18b92d36eab60e71e6fd59acf04ef60a53783570e11eef397a0e0f4f5.jpg","PM-6.jpg":"/assets/ads/PM-6-3ae66e41f7ae1e851a0910be89141cf2533509b46df6379464efc885d5ee2f07.jpg","Drug-Search-4.jpg":"/assets/ads/Drug-Search-4-2a9102bd41f16e8c40c9d8044d1dcb6f206ff80107cc269aa83d02ea683bc829.jpg","DDI-5.jpg":"/assets/ads/DDI-5-fa1c287946f4044094c723161577cb5ac631f9cd1217446e510dc79ace6cb94e.jpg","TH-1.jpg":"/assets/ads/TH-1-55a9077bb39e8c38a68c67b555b8091d21a9d41b1c21c7daed3fe53e6f9f3c97.jpg","TH-2.jpg":"/assets/ads/TH-2-1d488747fa4af00ab970a48dba0b228b054d166aa22c1760a310e2b72dd22589.jpg","ThriveHealth-1.jpg":"/assets/ads/ThriveHealth-1-fe42678c71bf2ec7d508fde77efbe9f0aa868c5fa03bd39a7e1c97cefac0fa9d.jpg","ThriveHealth-2.jpg":"/assets/ads/ThriveHealth-2-32bb14bb00de8a1b2efc2a51ce37f490c01e76dac7b9c09b6b831c50640b6567.jpg","ThriveHealth-3.jpg":"/assets/ads/ThriveHealth-3-e184eae1745f8aa22525b294b761ee89f5a854a434d50e5d6d37c0b77f2cf523.jpg","ThriveHealth-4.jpg":"/assets/ads/ThriveHealth-4-218f710e6d20831711d0920e585b986217c38f38d9849b8dd32bb56f68d2eea9.jpg"})
Stay in the know!
As part of our commitment to providing the most up-to-date drug information, we will be releasing #DrugBankUpdates with our newly added curated drug pages.
#DrugBankUpdates