U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry RACEMIC
Molecular Formula C10H12ClNO2.ClH
Molecular Weight 250.122
Optical Activity ( + / - )
Defined Stereocenters 0 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of BACLOFEN HYDROCHLORIDE

SMILES

Cl.NCC(CC(O)=O)C1=CC=C(Cl)C=C1

InChI

InChIKey=WMNUVYYLMCMHLU-UHFFFAOYSA-N
InChI=1S/C10H12ClNO2.ClH/c11-9-3-1-7(2-4-9)8(6-12)5-10(13)14;/h1-4,8H,5-6,12H2,(H,13,14);1H

HIDE SMILES / InChI

Description
Curator's Comment: description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/18221197 https://www.ncbi.nlm.nih.gov/pubmed/15486423

Baclofen (brand names Kemstro, Lioresal, and Gablofen) is a derivative of gamma-aminobutyric acid (GABA). Baclofen is a muscle relaxer and an antispastic agent and is used to treat muscle symptoms caused by multiple sclerosis, including spasm, pain, and stiffness. It is primarily used to treat spasticity and is under investigation for the treatment of alcoholism. 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. 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 intersubjective variation in absorption and/or elimination. Baclofen is a direct agonist at GABA-B 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.

CNS Activity

CNS Penetrant
2554
Curator's Comment: Baclofen is a GABA-like drug which passes through the blood-brain barrier and which reduces the neuroleptic-induced increase of dopamine turn-over

Originator

Keberle. H. at Ciba-Geigy
2
Curator's Comment: It was synthesized for the first time in Ciba-Geigy by the Swiss chemist Heinrich Keberle in 1962

Approval Year

1977
44
Targets

Targets

Primary TargetPharmacologyConditionPotency
Agonist
2678
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Approved
8429
GABLOFEN

Approved Use

Gablofen (baclofen injection) is indicated for use in the management of severe spasticity in adult and pediatric patients age 4 years and above. Patients should first respond to a screening dose of intrathecal baclofen prior to consideration for long term infusion via an implantable pump. For spasticity of spinal cord origin, chronic infusion of Gablofen via an implantable pump should be reserved for patients unresponsive to oral baclofen therapy, or those who experience intolerable CNS side effects at effective doses. Patients with spasticity due to traumatic brain injury should wait at least one year after the injury before consideration of long term intrathecal baclofen therapy. Gablofen is intended for use by the intrathecal route in single bolus test doses (via spinal catheter or lumbar puncture) and, for chronic use, only with the Medtronic SynchroMed® II Programmable Pump or other pumps labeled for intrathecal administration of Gablofen

Launch Date

2010
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
0.2 μg/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/2336342/
10 mg 4 times / day steady-state, oral
dose: 10 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
BACLOFEN plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
178 ng/mL
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2003/21589_kemstro_lbl.pdf
10 mg single, oral
dose: 10 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
BACLOFEN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
1.1 μg × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/2336342/
10 mg 4 times / day steady-state, oral
dose: 10 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
BACLOFEN plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
3.75 h
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2003/21589_kemstro_lbl.pdf
10 mg single, oral
dose: 10 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
BACLOFEN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
70%
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2003/21589_kemstro_lbl.pdf
10 mg single, oral
dose: 10 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
BACLOFEN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
500 mg 1 times / day single, oral
Studied dose
Dose: 500 mg, 1 times / day
Route: oral
Route: single
Dose: 500 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2003/021589s000_Kemstro_MedR.pdf
Page: nda/2003/021589s000_Kemstro_MedR.pdf - p.36
healthy, 25 years
n = 1
Health Status: healthy
Age Group: 25 years
Sex: F
Population Size: 1
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2003/021589s000_Kemstro_MedR.pdf
Page: nda/2003/021589s000_Kemstro_MedR.pdf - p.36
Other AEs: Hypertension, Respiratory depression...
Other AEs:
Hypertension
Respiratory depression
Coma
Hypotonia
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2003/021589s000_Kemstro_MedR.pdf
Page: nda/2003/021589s000_Kemstro_MedR.pdf - p.36
800 mg 1 times / day single, oral
Studied dose
Dose: 800 mg, 1 times / day
Route: oral
Route: single
Dose: 800 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2003/021589s000_Kemstro_MedR.pdf
https://pubmed.ncbi.nlm.nih.gov/9711203/
unhealthy, 42 years
n = 1
Health Status: unhealthy
Condition: spasticity
Age Group: 42 years
Sex: M
Population Size: 1
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2003/021589s000_Kemstro_MedR.pdf
https://pubmed.ncbi.nlm.nih.gov/9711203/
Other AEs: Hypotension...
Other AEs:
Hypotension
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2003/021589s000_Kemstro_MedR.pdf
https://pubmed.ncbi.nlm.nih.gov/9711203/
800 mg 1 times / day single, oral
Studied dose
Dose: 800 mg, 1 times / day
Route: oral
Route: single
Dose: 800 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2003/021589s000_Kemstro_MedR.pdf
Page: nda/2003/021589s000_Kemstro_MedR.pdf - p.36
unhealthy, 42 years
n = 1
Health Status: unhealthy
Condition: spasticity
Age Group: 42 years
Sex: M
Population Size: 1
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2003/021589s000_Kemstro_MedR.pdf
Page: nda/2003/021589s000_Kemstro_MedR.pdf - p.36
Other AEs: Hypotonia, Bradycardia...
Other AEs:
Hypotonia
Bradycardia
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2003/021589s000_Kemstro_MedR.pdf
Page: nda/2003/021589s000_Kemstro_MedR.pdf - p.36
10 mg 3 times / day multiple, oral
Recommended
Dose: 10 mg, 3 times / day
Route: oral
Route: multiple
Dose: 10 mg, 3 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/3912190/
unhealthy, 69-81 years
n = 12
Health Status: unhealthy
Condition: stroke
Age Group: 69-81 years
Sex: M+F
Population Size: 12
Sources:
https://pubmed.ncbi.nlm.nih.gov/3912190/
Disc. AE: Drowsiness...
AEs leading to
discontinuation/dose reduction:
Drowsiness (grade 3, 41.7%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/3912190/
30 mg 1 times / day multiple, oral
Recommended
Dose: 30 mg, 1 times / day
Route: oral
Route: multiple
Dose: 30 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/15597084/
unhealthy, mean age 42 years
n = 12
Health Status: unhealthy
Condition: alcohol dependence
Age Group: mean age 42 years
Sex: M+F
Population Size: 12
Sources:
https://pubmed.ncbi.nlm.nih.gov/15597084/
Disc. AE: Drowsiness, Fatigue...
AEs leading to
discontinuation/dose reduction:
Drowsiness (grade 1-2, 16.7%)
Fatigue (grade 1-2, 8.3%)
Confusion (grade 1-2, 8.3%)
Dizziness (grade 1-2, 8.3%)
Insomnia (grade 1-2, 8.3%)
Constipation (grade 1-2, 8.3%)
Depression (grade 1-2, 8.3%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/15597084/
10 mg 3 times / day steady, oral
Dose: 10 mg, 3 times / day
Route: oral
Route: steady
Dose: 10 mg, 3 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01008280
unhealthy
n = 88
Health Status: unhealthy
Condition: Hepatitis C
Population Size: 88
Sources:
https://clinicaltrials.gov/ct2/show/NCT01008280
Other AEs: Confusion, Dizziness...
Other AEs:
Confusion (below serious, 20 patients)
Dizziness (below serious, 23 patients)
Drowsiness (below serious, 34 patients)
Hallucinations (below serious, 5 patients)
Headache (below serious, 22 patients)
Hypotension (below serious, 7 patients)
Itching (below serious, 13 patients)
Loss of consciousness (below serious, 4 patients)
Paresthesia (below serious, 11 patient)
Rash (below serious, 8 patients)
Slurred speech (below serious, 9 patients)
Sources:
https://clinicaltrials.gov/ct2/show/NCT01008280
10 mg 3 times / day steady, oral
Dose: 10 mg, 3 times / day
Route: oral
Route: steady
Dose: 10 mg, 3 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01751386
unhealthy
n = 20
Health Status: unhealthy
Condition: Alcoholism
Population Size: 20
Sources:
https://clinicaltrials.gov/ct2/show/NCT01751386
Other AEs: Increased appetite, Insomnia...
Other AEs:
Increased appetite (below serious, 1 patient)
Insomnia (below serious, 3 patients)
Depression (below serious, 1 patient)
Sources:
https://clinicaltrials.gov/ct2/show/NCT01751386
10 mg 3 times / day steady, oral
Dose: 10 mg, 3 times / day
Route: oral
Route: steady
Dose: 10 mg, 3 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01980706
unhealthy
n = 43
Health Status: unhealthy
Condition: Alcohol Dependence
Population Size: 43
Sources:
https://clinicaltrials.gov/ct2/show/NCT01980706
Other AEs: Sedation, Dizziness...
Other AEs:
Sedation (below serious, 25 patients)
Dizziness (below serious, 12 patients)
Nausea (below serious, 5 patients)
Constipation (below serious, 4 patients)
Headache (below serious, 5 patients)
Sources:
https://clinicaltrials.gov/ct2/show/NCT01980706
30 mg 3 times / day steady, oral
Dose: 30 mg, 3 times / day
Route: oral
Route: steady
Dose: 30 mg, 3 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01980706
unhealthy
n = 37
Health Status: unhealthy
Condition: Alcohol Dependence
Population Size: 37
Sources:
https://clinicaltrials.gov/ct2/show/NCT01980706
Other AEs: Drowsiness, Sedation...
Other AEs:
Drowsiness (serious, 1 patient)
Sedation (below serious, 20 patients)
Dizziness (below serious, 8 patients)
Headache (below serious, 4 patients)
Sources:
https://clinicaltrials.gov/ct2/show/NCT01980706
AEs

AEs

AESignificanceDosePopulation
Coma
500 mg 1 times / day single, oral
Studied dose
Dose: 500 mg, 1 times / day
Route: oral
Route: single
Dose: 500 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2003/021589s000_Kemstro_MedR.pdf
Page: nda/2003/021589s000_Kemstro_MedR.pdf - p.36
healthy, 25 years
n = 1
Health Status: healthy
Age Group: 25 years
Sex: F
Population Size: 1
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2003/021589s000_Kemstro_MedR.pdf
Page: nda/2003/021589s000_Kemstro_MedR.pdf - p.36
Hypertension
500 mg 1 times / day single, oral
Studied dose
Dose: 500 mg, 1 times / day
Route: oral
Route: single
Dose: 500 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2003/021589s000_Kemstro_MedR.pdf
Page: nda/2003/021589s000_Kemstro_MedR.pdf - p.36
healthy, 25 years
n = 1
Health Status: healthy
Age Group: 25 years
Sex: F
Population Size: 1
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2003/021589s000_Kemstro_MedR.pdf
Page: nda/2003/021589s000_Kemstro_MedR.pdf - p.36
Hypotonia
500 mg 1 times / day single, oral
Studied dose
Dose: 500 mg, 1 times / day
Route: oral
Route: single
Dose: 500 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2003/021589s000_Kemstro_MedR.pdf
Page: nda/2003/021589s000_Kemstro_MedR.pdf - p.36
healthy, 25 years
n = 1
Health Status: healthy
Age Group: 25 years
Sex: F
Population Size: 1
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2003/021589s000_Kemstro_MedR.pdf
Page: nda/2003/021589s000_Kemstro_MedR.pdf - p.36
Respiratory depression
500 mg 1 times / day single, oral
Studied dose
Dose: 500 mg, 1 times / day
Route: oral
Route: single
Dose: 500 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2003/021589s000_Kemstro_MedR.pdf
Page: nda/2003/021589s000_Kemstro_MedR.pdf - p.36
healthy, 25 years
n = 1
Health Status: healthy
Age Group: 25 years
Sex: F
Population Size: 1
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2003/021589s000_Kemstro_MedR.pdf
Page: nda/2003/021589s000_Kemstro_MedR.pdf - p.36
Hypotension
800 mg 1 times / day single, oral
Studied dose
Dose: 800 mg, 1 times / day
Route: oral
Route: single
Dose: 800 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2003/021589s000_Kemstro_MedR.pdf
https://pubmed.ncbi.nlm.nih.gov/9711203/
unhealthy, 42 years
n = 1
Health Status: unhealthy
Condition: spasticity
Age Group: 42 years
Sex: M
Population Size: 1
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2003/021589s000_Kemstro_MedR.pdf
https://pubmed.ncbi.nlm.nih.gov/9711203/
Bradycardia
800 mg 1 times / day single, oral
Studied dose
Dose: 800 mg, 1 times / day
Route: oral
Route: single
Dose: 800 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2003/021589s000_Kemstro_MedR.pdf
Page: nda/2003/021589s000_Kemstro_MedR.pdf - p.36
unhealthy, 42 years
n = 1
Health Status: unhealthy
Condition: spasticity
Age Group: 42 years
Sex: M
Population Size: 1
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2003/021589s000_Kemstro_MedR.pdf
Page: nda/2003/021589s000_Kemstro_MedR.pdf - p.36
Hypotonia
800 mg 1 times / day single, oral
Studied dose
Dose: 800 mg, 1 times / day
Route: oral
Route: single
Dose: 800 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2003/021589s000_Kemstro_MedR.pdf
Page: nda/2003/021589s000_Kemstro_MedR.pdf - p.36
unhealthy, 42 years
n = 1
Health Status: unhealthy
Condition: spasticity
Age Group: 42 years
Sex: M
Population Size: 1
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2003/021589s000_Kemstro_MedR.pdf
Page: nda/2003/021589s000_Kemstro_MedR.pdf - p.36
Drowsiness grade 3, 41.7%
Disc. AE
10 mg 3 times / day multiple, oral
Recommended
Dose: 10 mg, 3 times / day
Route: oral
Route: multiple
Dose: 10 mg, 3 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/3912190/
unhealthy, 69-81 years
n = 12
Health Status: unhealthy
Condition: stroke
Age Group: 69-81 years
Sex: M+F
Population Size: 12
Sources:
https://pubmed.ncbi.nlm.nih.gov/3912190/
Drowsiness grade 1-2, 16.7%
Disc. AE
30 mg 1 times / day multiple, oral
Recommended
Dose: 30 mg, 1 times / day
Route: oral
Route: multiple
Dose: 30 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/15597084/
unhealthy, mean age 42 years
n = 12
Health Status: unhealthy
Condition: alcohol dependence
Age Group: mean age 42 years
Sex: M+F
Population Size: 12
Sources:
https://pubmed.ncbi.nlm.nih.gov/15597084/
Confusion grade 1-2, 8.3%
Disc. AE
30 mg 1 times / day multiple, oral
Recommended
Dose: 30 mg, 1 times / day
Route: oral
Route: multiple
Dose: 30 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/15597084/
unhealthy, mean age 42 years
n = 12
Health Status: unhealthy
Condition: alcohol dependence
Age Group: mean age 42 years
Sex: M+F
Population Size: 12
Sources:
https://pubmed.ncbi.nlm.nih.gov/15597084/
Constipation grade 1-2, 8.3%
Disc. AE
30 mg 1 times / day multiple, oral
Recommended
Dose: 30 mg, 1 times / day
Route: oral
Route: multiple
Dose: 30 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/15597084/
unhealthy, mean age 42 years
n = 12
Health Status: unhealthy
Condition: alcohol dependence
Age Group: mean age 42 years
Sex: M+F
Population Size: 12
Sources:
https://pubmed.ncbi.nlm.nih.gov/15597084/
Depression grade 1-2, 8.3%
Disc. AE
30 mg 1 times / day multiple, oral
Recommended
Dose: 30 mg, 1 times / day
Route: oral
Route: multiple
Dose: 30 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/15597084/
unhealthy, mean age 42 years
n = 12
Health Status: unhealthy
Condition: alcohol dependence
Age Group: mean age 42 years
Sex: M+F
Population Size: 12
Sources:
https://pubmed.ncbi.nlm.nih.gov/15597084/
Dizziness grade 1-2, 8.3%
Disc. AE
30 mg 1 times / day multiple, oral
Recommended
Dose: 30 mg, 1 times / day
Route: oral
Route: multiple
Dose: 30 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/15597084/
unhealthy, mean age 42 years
n = 12
Health Status: unhealthy
Condition: alcohol dependence
Age Group: mean age 42 years
Sex: M+F
Population Size: 12
Sources:
https://pubmed.ncbi.nlm.nih.gov/15597084/
Fatigue grade 1-2, 8.3%
Disc. AE
30 mg 1 times / day multiple, oral
Recommended
Dose: 30 mg, 1 times / day
Route: oral
Route: multiple
Dose: 30 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/15597084/
unhealthy, mean age 42 years
n = 12
Health Status: unhealthy
Condition: alcohol dependence
Age Group: mean age 42 years
Sex: M+F
Population Size: 12
Sources:
https://pubmed.ncbi.nlm.nih.gov/15597084/
Insomnia grade 1-2, 8.3%
Disc. AE
30 mg 1 times / day multiple, oral
Recommended
Dose: 30 mg, 1 times / day
Route: oral
Route: multiple
Dose: 30 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/15597084/
unhealthy, mean age 42 years
n = 12
Health Status: unhealthy
Condition: alcohol dependence
Age Group: mean age 42 years
Sex: M+F
Population Size: 12
Sources:
https://pubmed.ncbi.nlm.nih.gov/15597084/
Paresthesia below serious, 11 patient
10 mg 3 times / day steady, oral
Dose: 10 mg, 3 times / day
Route: oral
Route: steady
Dose: 10 mg, 3 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01008280
unhealthy
n = 88
Health Status: unhealthy
Condition: Hepatitis C
Population Size: 88
Sources:
https://clinicaltrials.gov/ct2/show/NCT01008280
Itching below serious, 13 patients
10 mg 3 times / day steady, oral
Dose: 10 mg, 3 times / day
Route: oral
Route: steady
Dose: 10 mg, 3 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01008280
unhealthy
n = 88
Health Status: unhealthy
Condition: Hepatitis C
Population Size: 88
Sources:
https://clinicaltrials.gov/ct2/show/NCT01008280
Confusion below serious, 20 patients
10 mg 3 times / day steady, oral
Dose: 10 mg, 3 times / day
Route: oral
Route: steady
Dose: 10 mg, 3 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01008280
unhealthy
n = 88
Health Status: unhealthy
Condition: Hepatitis C
Population Size: 88
Sources:
https://clinicaltrials.gov/ct2/show/NCT01008280
Headache below serious, 22 patients
10 mg 3 times / day steady, oral
Dose: 10 mg, 3 times / day
Route: oral
Route: steady
Dose: 10 mg, 3 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01008280
unhealthy
n = 88
Health Status: unhealthy
Condition: Hepatitis C
Population Size: 88
Sources:
https://clinicaltrials.gov/ct2/show/NCT01008280
Dizziness below serious, 23 patients
10 mg 3 times / day steady, oral
Dose: 10 mg, 3 times / day
Route: oral
Route: steady
Dose: 10 mg, 3 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01008280
unhealthy
n = 88
Health Status: unhealthy
Condition: Hepatitis C
Population Size: 88
Sources:
https://clinicaltrials.gov/ct2/show/NCT01008280
Drowsiness below serious, 34 patients
10 mg 3 times / day steady, oral
Dose: 10 mg, 3 times / day
Route: oral
Route: steady
Dose: 10 mg, 3 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01008280
unhealthy
n = 88
Health Status: unhealthy
Condition: Hepatitis C
Population Size: 88
Sources:
https://clinicaltrials.gov/ct2/show/NCT01008280
Loss of consciousness below serious, 4 patients
10 mg 3 times / day steady, oral
Dose: 10 mg, 3 times / day
Route: oral
Route: steady
Dose: 10 mg, 3 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01008280
unhealthy
n = 88
Health Status: unhealthy
Condition: Hepatitis C
Population Size: 88
Sources:
https://clinicaltrials.gov/ct2/show/NCT01008280
Hallucinations below serious, 5 patients
10 mg 3 times / day steady, oral
Dose: 10 mg, 3 times / day
Route: oral
Route: steady
Dose: 10 mg, 3 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01008280
unhealthy
n = 88
Health Status: unhealthy
Condition: Hepatitis C
Population Size: 88
Sources:
https://clinicaltrials.gov/ct2/show/NCT01008280
Hypotension below serious, 7 patients
10 mg 3 times / day steady, oral
Dose: 10 mg, 3 times / day
Route: oral
Route: steady
Dose: 10 mg, 3 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01008280
unhealthy
n = 88
Health Status: unhealthy
Condition: Hepatitis C
Population Size: 88
Sources:
https://clinicaltrials.gov/ct2/show/NCT01008280
Rash below serious, 8 patients
10 mg 3 times / day steady, oral
Dose: 10 mg, 3 times / day
Route: oral
Route: steady
Dose: 10 mg, 3 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01008280
unhealthy
n = 88
Health Status: unhealthy
Condition: Hepatitis C
Population Size: 88
Sources:
https://clinicaltrials.gov/ct2/show/NCT01008280
Slurred speech below serious, 9 patients
10 mg 3 times / day steady, oral
Dose: 10 mg, 3 times / day
Route: oral
Route: steady
Dose: 10 mg, 3 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01008280
unhealthy
n = 88
Health Status: unhealthy
Condition: Hepatitis C
Population Size: 88
Sources:
https://clinicaltrials.gov/ct2/show/NCT01008280
Depression below serious, 1 patient
10 mg 3 times / day steady, oral
Dose: 10 mg, 3 times / day
Route: oral
Route: steady
Dose: 10 mg, 3 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01751386
unhealthy
n = 20
Health Status: unhealthy
Condition: Alcoholism
Population Size: 20
Sources:
https://clinicaltrials.gov/ct2/show/NCT01751386
Increased appetite below serious, 1 patient
10 mg 3 times / day steady, oral
Dose: 10 mg, 3 times / day
Route: oral
Route: steady
Dose: 10 mg, 3 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01751386
unhealthy
n = 20
Health Status: unhealthy
Condition: Alcoholism
Population Size: 20
Sources:
https://clinicaltrials.gov/ct2/show/NCT01751386
Insomnia below serious, 3 patients
10 mg 3 times / day steady, oral
Dose: 10 mg, 3 times / day
Route: oral
Route: steady
Dose: 10 mg, 3 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01751386
unhealthy
n = 20
Health Status: unhealthy
Condition: Alcoholism
Population Size: 20
Sources:
https://clinicaltrials.gov/ct2/show/NCT01751386
Dizziness below serious, 12 patients
10 mg 3 times / day steady, oral
Dose: 10 mg, 3 times / day
Route: oral
Route: steady
Dose: 10 mg, 3 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01980706
unhealthy
n = 43
Health Status: unhealthy
Condition: Alcohol Dependence
Population Size: 43
Sources:
https://clinicaltrials.gov/ct2/show/NCT01980706
Sedation below serious, 25 patients
10 mg 3 times / day steady, oral
Dose: 10 mg, 3 times / day
Route: oral
Route: steady
Dose: 10 mg, 3 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01980706
unhealthy
n = 43
Health Status: unhealthy
Condition: Alcohol Dependence
Population Size: 43
Sources:
https://clinicaltrials.gov/ct2/show/NCT01980706
Constipation below serious, 4 patients
10 mg 3 times / day steady, oral
Dose: 10 mg, 3 times / day
Route: oral
Route: steady
Dose: 10 mg, 3 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01980706
unhealthy
n = 43
Health Status: unhealthy
Condition: Alcohol Dependence
Population Size: 43
Sources:
https://clinicaltrials.gov/ct2/show/NCT01980706
Headache below serious, 5 patients
10 mg 3 times / day steady, oral
Dose: 10 mg, 3 times / day
Route: oral
Route: steady
Dose: 10 mg, 3 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01980706
unhealthy
n = 43
Health Status: unhealthy
Condition: Alcohol Dependence
Population Size: 43
Sources:
https://clinicaltrials.gov/ct2/show/NCT01980706
Nausea below serious, 5 patients
10 mg 3 times / day steady, oral
Dose: 10 mg, 3 times / day
Route: oral
Route: steady
Dose: 10 mg, 3 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01980706
unhealthy
n = 43
Health Status: unhealthy
Condition: Alcohol Dependence
Population Size: 43
Sources:
https://clinicaltrials.gov/ct2/show/NCT01980706
Sedation below serious, 20 patients
30 mg 3 times / day steady, oral
Dose: 30 mg, 3 times / day
Route: oral
Route: steady
Dose: 30 mg, 3 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01980706
unhealthy
n = 37
Health Status: unhealthy
Condition: Alcohol Dependence
Population Size: 37
Sources:
https://clinicaltrials.gov/ct2/show/NCT01980706
Headache below serious, 4 patients
30 mg 3 times / day steady, oral
Dose: 30 mg, 3 times / day
Route: oral
Route: steady
Dose: 30 mg, 3 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01980706
unhealthy
n = 37
Health Status: unhealthy
Condition: Alcohol Dependence
Population Size: 37
Sources:
https://clinicaltrials.gov/ct2/show/NCT01980706
Dizziness below serious, 8 patients
30 mg 3 times / day steady, oral
Dose: 30 mg, 3 times / day
Route: oral
Route: steady
Dose: 30 mg, 3 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01980706
unhealthy
n = 37
Health Status: unhealthy
Condition: Alcohol Dependence
Population Size: 37
Sources:
https://clinicaltrials.gov/ct2/show/NCT01980706
Drowsiness serious, 1 patient
30 mg 3 times / day steady, oral
Dose: 30 mg, 3 times / day
Route: oral
Route: steady
Dose: 30 mg, 3 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01980706
unhealthy
n = 37
Health Status: unhealthy
Condition: Alcohol Dependence
Population Size: 37
Sources:
https://clinicaltrials.gov/ct2/show/NCT01980706
Sourcing

Sourcing

Vendor/AggregatorIDURL
ChEBI
CHEBI:2972
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:2972
ChemicalBook
CB8669450
https://www.chemicalbook.com/ChemicalProductProperty_EN_CB8669450
MolPort
MolPort-002-051-370
https://www.molport.com/shop/molecule-link/MolPort-002-051-370
eMolecules
535235
https://www.emolecules.com/cgi-bin/more?vid=535235
PubMed

PubMed

TitleDatePubMed
Involvement of GABAergic mechanisms in chloroquine-induced seizures in mice.
1992 Mar
[Baclofen intoxication in chronic hemodialysis and kidney transplantation].
1992 May 8
Effect of baclofen on cocaine self-administration in rats reinforced under fixed-ratio 1 and progressive-ratio schedules.
2000 Feb
Continuous intrathecal pump infusion of baclofen with antibiotic drugs for treatment of pump-associated meningitis. Case report.
2000 Feb
The human GABA(B1b) and GABA(B2) heterodimeric recombinant receptor shows low sensitivity to phaclofen and saclofen.
2000 Nov
The effect of GABA receptor ligands in experimental spina bifida occulta.
2001
GABA enhances transmission at an excitatory glutamatergic synapse.
2001 Aug 15
Long-term intrathecal Baclofen infusion in supraspinal spasticity of adulthood.
2002 Feb
A possible baclofen-induced neurotoxicity in a CAPD patient who recovered with long-duration hemodialysis.
2002 Mar-Apr
Different actions of gabapentin and baclofen in hippocampus from weaver mice.
2003
Baclofen attenuates conditioned locomotion to cues associated with cocaine administration and stabilizes extracellular glutamate levels in rat nucleus accumbens.
2003
Gamma-aminobutyric acid B receptor 1 mediates behavior-impairing actions of alcohol in Drosophila: adult RNA interference and pharmacological evidence.
2003 Apr 29
Lithium-induced periodic alternating nystagmus.
2003 Jan 28
Intrathecal baclofen for stiff-person syndrome: life-threatening intermittent catheter leakage.
2003 Jun 24
Evaluation of interaction between gabapentin and baclofen in the formalin test in mice.
2003 Sep-Oct
GABAB receptor stimulation decreases amphetamine-induced behavior and neuropeptide gene expression in the striatum.
2004 Apr 9
Pharmacological modulation of GABA(B) receptors affects cocaine-induced seizures in mice.
2004 Jul
Suppression of GABA(B) receptor function in vivo by disulfide reducing agent, DL-dithiothreitol (DTT).
2004 Jul
GABA(B) receptor modulators potentiate baclofen-induced depression of dopamine neuron activity in the rat ventral tegmental area.
2005 Apr
Attenuation of d-amphetamine self-administration by baclofen in the rat: behavioral and neurochemical correlates.
2005 Feb
Different sensitivity to the motor incoordinating effects of gamma-hydroxybutyric acid (GHB) and baclofen in GHB-sensitive and GHB-resistant rats.
2005 Feb 1
Injections of baclofen into the ventral medial prefrontal cortex block the initiation, but not the expression, of cocaine sensitization in rats.
2005 Jul
Pruritus after intrathecal baclofen withdrawal: A retrospective study.
2005 Mar
An unusual cause of overdose after baclofen pump implantation: case report.
2005 Mar
Severe seizures during propofol induction in a patient with syringomyelia receiving baclofen.
2005 May
Intracerebral baclofen administration decreases amphetamine-induced behavior and neuropeptide gene expression in the striatum.
2005 May
Intrathecal baclofen overdose followed by withdrawal: clinical and EEG features.
2005 Nov
Effects of baclofen on cocaine self-administration: opioid- and nonopioid-dependent volunteers.
2006 Aug
GABAB1 receptor subunit isoforms exert a differential influence on baseline but not GABAB receptor agonist-induced changes in mice.
2006 Dec
[Radiculopathy following intrathecal baclofen pump implantation].
2006 Jun
Aseptic meningitis after intrathecal baclofen injection.
2006 May
Baclofen-induced sexual dysfunction.
2006 Sep 26
Genomic and functional conservation of sedative-hypnotic targets in the zebrafish.
2007 Apr
Baclofen alters flash-evoked potentials in Long-Evans rats.
2007 Apr
Interactions of the basolateral amygdala with the dorsal hippocampus and dorsomedial prefrontal cortex regulate drug context-induced reinstatement of cocaine-seeking in rats.
2007 Jul
Attenuation of cocaine-seeking by GABA B receptor agonists baclofen and CGP44532 but not the GABA reuptake inhibitor tiagabine in baboons.
2007 Jul 10
Effects of GABA(B) receptor agents on cocaine priming, discrete contextual cue and food induced relapses.
2007 Oct 1
Patents

Patents

08242145
4
JP2002511777A
414
JP2011079841A
5

Sample Use Guides

In Vivo Use Guide
Gablofen is approved only for use with the Medtronic SynchroMed® II Programmable Pump or other pumps labeled 34 for intrathecal administration of Gablofen (baclofen injection). Lowest dose with an optimal response should be used, generally 300 to 800 mcg/day for spasticity of spinal cord origin and 90 to 700 mcg/day for spasticity of cerebral origin; Titrate Gablofen to maintain some degree of muscle tone and allow occasional spasms
Route of Administration: Other
In Vitro Use Guide
Curator's Comment: In vitro, baclofen reduces chemotaxis of human peripheral blood mononuclear cells towards CCL2, CCL5, CXCL10, CXCL2 and CX3CL1 in a dose-dependant manner. Protein kinase C inhibitors calphostin C and G0 6976 could reverse this effect, pointing towards the involvement of both calcium-dependent and -independent protein kinase C in baclofen-induced inhibition of chemokine receptors.
Unknown
Name Type Language
BACLOFEN HYDROCHLORIDE
MI  
Common Name English
4-AMINO-3-(4-CHLOROPHENYL)BUTANOIC ACID HYDROCHLORIDE
Systematic Name English
(±)-4-AMINO-3-(4-CHLOROPHENYL)BUTANOIC ACID HYDROCHLORIDE
Systematic Name English
BACLOFEN HYDROCHLORIDE [MI]
Common Name English
BENZENEPROPANOIC ACID, .BETA.-(AMINOMETHYL)-4-CHLORO-, HYDROCHLORIDE
Common Name English
BACLOFEN HCL
Common Name English
(±)-BACLOFEN HYDROCHLORIDE
Common Name English
Classification Tree Code System Code
NCI_THESAURUS C29696
Created by admin on Fri Dec 15 17:34:23 GMT 2023 , Edited by admin on Fri Dec 15 17:34:23 GMT 2023
Code System Code Type Description
PUBCHEM
6602720
Created by admin on Fri Dec 15 17:34:23 GMT 2023 , Edited by admin on Fri Dec 15 17:34:23 GMT 2023
PRIMARY
CAS
70206-22-3
Created by admin on Fri Dec 15 17:34:23 GMT 2023 , Edited by admin on Fri Dec 15 17:34:23 GMT 2023
SUPERSEDED
CAS
28311-31-1
Created by admin on Fri Dec 15 17:34:23 GMT 2023 , Edited by admin on Fri Dec 15 17:34:23 GMT 2023
PRIMARY
NCI_THESAURUS
C90887
Created by admin on Fri Dec 15 17:34:23 GMT 2023 , Edited by admin on Fri Dec 15 17:34:23 GMT 2023
PRIMARY
FDA UNII
64OSE3996V
Created by admin on Fri Dec 15 17:34:23 GMT 2023 , Edited by admin on Fri Dec 15 17:34:23 GMT 2023
PRIMARY
MERCK INDEX
m2200
Created by admin on Fri Dec 15 17:34:23 GMT 2023 , Edited by admin on Fri Dec 15 17:34:23 GMT 2023
PRIMARY Merck Index
DRUG BANK
DBSALT002256
Created by admin on Fri Dec 15 17:34:23 GMT 2023 , Edited by admin on Fri Dec 15 17:34:23 GMT 2023
PRIMARY
ACTIVE MOIETY
Structure of BACLOFEN
NIH
NCATS
PRIVACY ACT
ACCESSIBILITY
DISCLAIMER
HHS VULNERABILITY DISCLOSURE
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