Baclofen

Identification

Summary

Baclofen is a GABA-ergic agonist used to manage severe spasticity of cerebral or spinal origin in adult and pediatric patients.

Brand Names

Gablofen, Kemstro, Lioresal, Ozobax

Generic Name

Baclofen

DrugBank Accession Number

DB00181

Background

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

3D

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MOLSDF3D-SDFPDBSMILESInChI

Similar Structures

Structure for Baclofen (DB00181)

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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.

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Associated Conditions

• Joint Pain
• Soreness, Muscle
• Flexor spasm
• Reversible Spasticity
• Severe cerebral origin Spasticity
• Severe spinal cord origin Spasticity

Contraindications & Blackbox Warnings

Contraindications & Blackbox Warnings

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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	agonist	Humans
AGamma-aminobutyric acid type B receptor subunit 2	agonist	Humans

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

• Baclofen
  • 3-(p-chlorophenyl)-4-hydroxybutyric acid

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

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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.

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.

• Approved
• Vet approved
• Nutraceutical
• Illicit
• Withdrawn
• Investigational
• Experimental
• All Drugs

Drug	Interaction
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1,2-Benzodiazepine	The risk or severity of adverse effects can be increased when Baclofen is combined with 1,2-Benzodiazepine.
Abacavir	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.

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Food Interactions

• Avoid alcohol.
• Take with food. Take with food or milk to reduce gastric irritation.

Products

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Product Ingredients

Ingredient	UNII	CAS	InChI Key
Baclofen hydrochloride	64OSE3996V	28311-31-1	WMNUVYYLMCMHLU-UHFFFAOYSA-N

Product Images

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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
Baclofen	Tablet	10 mg/1	Oral	Caraco Pharmaceutical Laboratories, Ltd.	2007-03-30	Not applicable
Baclofen	Tablet	10 mg/1	Oral	Vintage Pharmaceuticals, LLC	2007-05-17	2007-05-17
Baclofen	Tablet	20 mg	Oral	Apotex Corporation	1994-12-31	2014-08-23
Baclofen	Tablet	20 mg	Oral	Sanis Health Inc	2010-02-25	Not applicable
Baclofen	Tablet	20 mg/1	Oral	Caraco Pharmaceutical Laboratories, Ltd.	2007-03-30	Not applicable
Baclofen	Tablet	10 mg	Oral	Apotex Corporation	1994-12-31	2014-08-23
Baclofen	Tablet	20 mg/1	Oral	Vintage Pharmaceuticals, LLC	2007-05-17	2007-05-17
Baclofen	Tablet	10 mg	Oral	Sanis Health Inc	2010-02-25	Not applicable
Baclofen Injection	Solution		Intrathecal	Sterimax Inc	2014-06-06	Not applicable
Baclofen Injection	Solution		Intrathecal	Teligent Pharma, Inc	2017-08-25	Not applicable

Generic Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End	Region	Image
Apo-baclofen	Tablet		Oral	Apotex Corporation	1994-12-31	Not applicable
Apo-baclofen	Tablet		Oral	Apotex Corporation	1994-12-31	Not applicable
Ava-baclofen	Tablet		Oral	Avanstra Inc	2011-10-11	2014-08-21
Ava-baclofen	Tablet		Oral	Avanstra Inc	2011-10-11	2014-08-21
Baclofen	Tablet	20 mg/1	Oral	Rebel Distributors	2004-07-01	Not applicable
Baclofen	Tablet	20 mg/1	Oral	REMEDYREPACK INC.	2020-03-30	Not applicable
Baclofen	Tablet	20 mg/1	Oral	Nucare Pharmaceuticals,inc.	1988-07-21	Not applicable
Baclofen	Tablet	10 mg/1	Oral	AvPAK	2021-03-02	Not applicable
Baclofen	Tablet	10 mg/1	Oral	Preferred Pharmaceuticals, Inc.	2020-02-28	Not applicable
Baclofen	Tablet	20 mg/1	Oral	Aphena Pharma Solutions - Tennessee, LLC	2005-08-30	Not applicable

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
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
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

Categories

ATC Codes

M03BX01 — Baclofen

• M03BX — Other centrally acting agents
• M03B — MUSCLE RELAXANTS, CENTRALLY ACTING AGENTS
• M03 — MUSCLE RELAXANTS
• M — MUSCULO-SKELETAL SYSTEM

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 / Organic oxides / Monoalkylamines / Hydrocarbon derivatives / Carbonyl compounds

show 4 more

Substituents

3-phenylpropanoic-acid / Amine / Amino acid / Amino fatty acid / Aralkylamine / Aromatic homomonocyclic compound / Aryl chloride / Aryl halide / Benzenoid / Carbonyl group / Carboxylic acid / Chlorobenzene / Fatty acyl / Gamma amino acid or derivatives / Halobenzene / Hydrocarbon derivative / Monocarboxylic acid or derivatives / Monocyclic benzene moiety / Organic nitrogen compound / Organic oxide / Organic oxygen compound / Organochloride / Organohalogen compound / Organonitrogen compound / Organooxygen compound / Organopnictogen compound / Primary aliphatic amine / Primary amine

show 18 more

Molecular Framework

Aromatic homomonocyclic compounds

External Descriptors

monocarboxylic acid, primary amino compound, monochlorobenzenes, gamma-amino acid (CHEBI:2972)

Affected organisms

• Humans and other mammals

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

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. [Article]
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. [Article]
3. See S, Ginzburg R: Skeletal muscle relaxants. Pharmacotherapy. 2008 Feb;28(2):207-13. doi: 10.1592/phco.28.2.207. [Article]
4. 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. [Article]
5. Liu J, Wang LN: Baclofen for alcohol withdrawal. Cochrane Database Syst Rev. 2017 Aug 20;8:CD008502. doi: 10.1002/14651858.CD008502.pub5. [Article]
6. Liu J, Wang LN: Baclofen for alcohol withdrawal. Cochrane Database Syst Rev. 2013 Feb 28;(2):CD008502. doi: 10.1002/14651858.CD008502.pub3. [Article]
7. 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. [Article]
8. 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. [Article]
9. 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. [Article]
10. 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. [Article]
11. 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. [Article]
12. 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. [Article]
13. 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. [Article]
14. Baclofen tablets [Link]
15. Baclofen powder, DailyMed [Link]
16. Pacifen Medsafe NZ [File]
17. Lioresal (intrathecal) FDA label [File]
18. 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

RxNav

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	Supportive Care	Cerebral Palsy (CP) / Crying	1
4	Completed	Supportive Care	Spasticity, Muscle	1
4	Completed	Treatment	Alcohol Dependency	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

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
Tablet	Oral	25 MG
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
Injection, solution	Parenteral
Solution	Parenteral
Injection	Parenteral
Injection, solution
Injection	Intrathecal
Tablet	Oral	10 mg/1
Tablet	Oral	20 mg/1
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
Injection	Intrathecal	10 mg/5mL
Tablet	Oral
Solution	Intrathecal
Solution	Oral	5 mg/5mL
Tablet	Oral	10 mg

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
US6221392	No	2001-04-24	2018-04-09
US6024981	No	2000-02-15	2018-04-09
US10610502	No	2019-08-30	2039-08-30

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

ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)

Not Available

Spectra

Spectrum	Spectrum Type	Splash Key
Predicted GC-MS Spectrum - GC-MS	Predicted GC-MS	Not Available
Mass Spectrum (Electron Ionization)	MS	splash10-000i-2900000000-963f049a4367a1d5a5f5
Predicted MS/MS Spectrum - 10V, Positive (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)	Predicted LC-MS/MS	Not Available
LC-MS/MS Spectrum - LC-ESI-QTOF , negative	LC-MS/MS	splash10-03dr-0950000000-33d21cbb6740c1f1aee1
LC-MS/MS Spectrum - LC-ESI-QQ , positive	LC-MS/MS	splash10-03di-1590000000-8a64733764308ba98f9a
LC-MS/MS Spectrum - LC-ESI-QQ , positive	LC-MS/MS	splash10-0f6t-0900000000-6647c58db763b4df68a0
LC-MS/MS Spectrum - LC-ESI-QQ , positive	LC-MS/MS	splash10-0udi-0900000000-72d6d878c9c2f29d846a
LC-MS/MS Spectrum - LC-ESI-QQ , positive	LC-MS/MS	splash10-014i-1900000000-18f69033596a03ee643a
LC-MS/MS Spectrum - LC-ESI-QQ , positive	LC-MS/MS	splash10-014i-1900000000-997473c303f07afcdf4e
LC-MS/MS Spectrum - LC-ESI-IT , positive	LC-MS/MS	splash10-0002-0900000000-d1da4625d180fe0af521
LC-MS/MS Spectrum - LC-ESI-QTOF , positive	LC-MS/MS	splash10-03di-0190000000-bd0fff49defde62ed0fa
LC-MS/MS Spectrum - LC-ESI-QTOF , positive	LC-MS/MS	splash10-0ik9-0790000000-1a50b0b7f24aaaf6a87e

Targets

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Binding Properties

×

Property	Measurement	pH	Temperature (°C)	References
EC 50 (nM)	1000	N/A	N/A	A27350
EC 50 (nM)	1700	N/A	N/A	A27350
IC 50 (nM)	15	N/A	N/A	A27349
IC 50 (nM)	1770	N/A	N/A	A27349
IC 50 (nM)	35	N/A	N/A	A27349

Details

Binding Properties1. Gamma-aminobutyric acid type B receptor subunit 1

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

1. Bowery NG: GABAB receptor pharmacology. Annu Rev Pharmacol Toxicol. 1993;33:109-47. [Article]
2. 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. [Article]
3. 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. [Article]
4. 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. [Article]
5. 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. [Article]
6. 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. [Article]
7. Pittman QJ: The action is at the terminal. J Physiol. 1999 Nov 1;520 Pt 3:629. [Article]
8. 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. [Article]
9. 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. [Article]
10. 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. [Article]

Details2. Gamma-aminobutyric acid type B receptor subunit 2

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

1. 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. [Article]
2. Bowery NG: GABAB receptor pharmacology. Annu Rev Pharmacol Toxicol. 1993;33:109-47. [Article]
3. 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. [Article]
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. [Article]
5. 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. [Article]
6. Pittman QJ: The action is at the terminal. J Physiol. 1999 Nov 1;520 Pt 3:629. [Article]
7. 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. [Article]
8. 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. [Article]

×

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Drug created on June 13, 2005 13:24 / Updated on May 07, 2021 21:05