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

Molecular Formula ClH
Molecular Weight 36.461
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Molecular Formula C10H12ClNO2
Molecular Weight 213.661
Charge 0
Count
Stereochemistry RACEMIC
Additional Stereochemistry No
Defined Stereocenters 0 / 1
E/Z Centers 0
Optical Activity ( + / - )

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

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

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

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
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

1.29012479E12
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
0.2 μg/mL
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
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
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
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%
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: 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: Page: nda/2003/021589s000_Kemstro_MedR.pdf - p.36
Other AEs: Hypertension, Respiratory depression...
Other AEs:
Hypertension
Respiratory depression
Coma
Hypotonia
Sources: 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:
unhealthy, 42 years
n = 1
Health Status: unhealthy
Condition: spasticity
Age Group: 42 years
Sex: M
Population Size: 1
Sources:
Other AEs: 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: 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: Page: nda/2003/021589s000_Kemstro_MedR.pdf - p.36
Other AEs: Hypotonia, Bradycardia...
Other AEs:
Hypotonia
Bradycardia
Sources: 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:
unhealthy, 69-81 years
n = 12
Health Status: unhealthy
Condition: stroke
Age Group: 69-81 years
Sex: M+F
Population Size: 12
Sources:
Disc. AE: Drowsiness...
AEs leading to
discontinuation/dose reduction:
Drowsiness (grade 3, 41.7%)
Sources:
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:
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:
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:
10 mg 3 times / day steady, oral
Dose: 10 mg, 3 times / day
Route: oral
Route: steady
Dose: 10 mg, 3 times / day
Sources:
unhealthy
n = 88
Health Status: unhealthy
Condition: Hepatitis C
Population Size: 88
Sources:
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:
10 mg 3 times / day steady, oral
Dose: 10 mg, 3 times / day
Route: oral
Route: steady
Dose: 10 mg, 3 times / day
Sources:
unhealthy
n = 20
Health Status: unhealthy
Condition: Alcoholism
Population Size: 20
Sources:
Other AEs: Increased appetite, Insomnia...
Other AEs:
Increased appetite (below serious, 1 patient)
Insomnia (below serious, 3 patients)
Depression (below serious, 1 patient)
Sources:
10 mg 3 times / day steady, oral
Dose: 10 mg, 3 times / day
Route: oral
Route: steady
Dose: 10 mg, 3 times / day
Sources:
unhealthy
n = 43
Health Status: unhealthy
Condition: Alcohol Dependence
Population Size: 43
Sources:
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:
30 mg 3 times / day steady, oral
Dose: 30 mg, 3 times / day
Route: oral
Route: steady
Dose: 30 mg, 3 times / day
Sources:
unhealthy
n = 37
Health Status: unhealthy
Condition: Alcohol Dependence
Population Size: 37
Sources:
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:
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: 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: 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: 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: 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: 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: 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: 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: 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:
unhealthy, 42 years
n = 1
Health Status: unhealthy
Condition: spasticity
Age Group: 42 years
Sex: M
Population Size: 1
Sources:
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: 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: 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: 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: 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:
unhealthy, 69-81 years
n = 12
Health Status: unhealthy
Condition: stroke
Age Group: 69-81 years
Sex: M+F
Population Size: 12
Sources:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
unhealthy
n = 88
Health Status: unhealthy
Condition: Hepatitis C
Population Size: 88
Sources:
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:
unhealthy
n = 88
Health Status: unhealthy
Condition: Hepatitis C
Population Size: 88
Sources:
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:
unhealthy
n = 88
Health Status: unhealthy
Condition: Hepatitis C
Population Size: 88
Sources:
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:
unhealthy
n = 88
Health Status: unhealthy
Condition: Hepatitis C
Population Size: 88
Sources:
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:
unhealthy
n = 88
Health Status: unhealthy
Condition: Hepatitis C
Population Size: 88
Sources:
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:
unhealthy
n = 88
Health Status: unhealthy
Condition: Hepatitis C
Population Size: 88
Sources:
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:
unhealthy
n = 88
Health Status: unhealthy
Condition: Hepatitis C
Population Size: 88
Sources:
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:
unhealthy
n = 88
Health Status: unhealthy
Condition: Hepatitis C
Population Size: 88
Sources:
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:
unhealthy
n = 88
Health Status: unhealthy
Condition: Hepatitis C
Population Size: 88
Sources:
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:
unhealthy
n = 88
Health Status: unhealthy
Condition: Hepatitis C
Population Size: 88
Sources:
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:
unhealthy
n = 88
Health Status: unhealthy
Condition: Hepatitis C
Population Size: 88
Sources:
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:
unhealthy
n = 20
Health Status: unhealthy
Condition: Alcoholism
Population Size: 20
Sources:
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:
unhealthy
n = 20
Health Status: unhealthy
Condition: Alcoholism
Population Size: 20
Sources:
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:
unhealthy
n = 20
Health Status: unhealthy
Condition: Alcoholism
Population Size: 20
Sources:
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:
unhealthy
n = 43
Health Status: unhealthy
Condition: Alcohol Dependence
Population Size: 43
Sources:
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:
unhealthy
n = 43
Health Status: unhealthy
Condition: Alcohol Dependence
Population Size: 43
Sources:
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:
unhealthy
n = 43
Health Status: unhealthy
Condition: Alcohol Dependence
Population Size: 43
Sources:
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:
unhealthy
n = 43
Health Status: unhealthy
Condition: Alcohol Dependence
Population Size: 43
Sources:
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:
unhealthy
n = 43
Health Status: unhealthy
Condition: Alcohol Dependence
Population Size: 43
Sources:
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:
unhealthy
n = 37
Health Status: unhealthy
Condition: Alcohol Dependence
Population Size: 37
Sources:
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:
unhealthy
n = 37
Health Status: unhealthy
Condition: Alcohol Dependence
Population Size: 37
Sources:
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:
unhealthy
n = 37
Health Status: unhealthy
Condition: Alcohol Dependence
Population Size: 37
Sources:
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:
unhealthy
n = 37
Health Status: unhealthy
Condition: Alcohol Dependence
Population Size: 37
Sources:
PubMed

PubMed

TitleDatePubMed
A case of mania associated with high-dose baclofen therapy.
1992 Jun
Prolonged seizure activity after baclofen withdrawal.
1992 Mar
Reversible akinetic mutism possibly induced by baclofen.
1999 Apr
Cerebellar Ataxia.
2000 May
The human GABA(B1b) and GABA(B2) heterodimeric recombinant receptor shows low sensitivity to phaclofen and saclofen.
2000 Nov
Involvement of GABAergic neurotransmission in the neurobiology of the apomorphine-induced aggressive behavior paradigm, a model of psychotic behavior in rats.
2000 Oct
Inhibition of baclofen on morphine-induced hyperactivity, reverse tolerance and postsynaptic dopamine receptor supersensitivity.
2001 Apr
Cholinergic transmission via central synapses in the locust nervous system.
2001 Dec
Cloning and functional expression of GABA(B) receptors from Drosophila.
2001 Feb
Modification of d-amphetamine-induced responses by baclofen in rats.
2001 Jan
Neuroleptic malignant-like syndrome after abrupt withdrawal of baclofen.
2001 Mar
Baclofen decreases methamphetamine self-administration in rats.
2002 Jul 2
DM235 (sunifiram): a novel nootropic with potential as a cognitive enhancer.
2002 Jun
Different actions of gabapentin and baclofen in hippocampus from weaver mice.
2003
Changes in GABA(A) receptor gene expression associated with selective alterations in receptor function and pharmacology after ethanol withdrawal.
2003 Dec 17
Lithium-induced periodic alternating nystagmus.
2003 Jan 28
Intrathecal baclofen for stiff-person syndrome: life-threatening intermittent catheter leakage.
2003 Jun 24
[Parkinsonian dystonia].
2003 Oct
Oral baclofen in cerebral palsy: possible seizure potentiation?
2003 Sep
Effects of positive allosteric modulators of the GABAB receptor on cocaine self-administration in rats.
2004 Apr
GABAB receptor stimulation decreases amphetamine-induced behavior and neuropeptide gene expression in the striatum.
2004 Apr 9
Baclofen as adjunctive treatment for a patient with cocaine dependence and schizoaffective disorder.
2004 Oct
Involvement of G protein betagamma-subunits in diverse signaling induced by G(i/o)-coupled receptors: study using the Xenopus oocyte expression system.
2004 Oct
GABA(B) receptor modulators potentiate baclofen-induced depression of dopamine neuron activity in the rat ventral tegmental area.
2005 Apr
Possible azithromycin-associated hiccups.
2005 Aug
Injections of baclofen into the ventral medial prefrontal cortex block the initiation, but not the expression, of cocaine sensitization in rats.
2005 Jul
Incidence of seizures in patients with multiple sclerosis treated with intrathecal baclofen.
2005 Mar 22
Intrathecal baclofen overdose followed by withdrawal: clinical and EEG features.
2005 Nov
Cocaine-induced locomotor activity and Fos expression in nucleus accumbens are sensitized for 6 months after repeated cocaine administration outside the home cage.
2006 Aug
Differential effects of chronic amphetamine and baclofen administration on cAMP levels and phosphorylation of CREB in distinct brain regions of wild type and monoamine oxidase B-deficient mice.
2006 Dec 15
Aseptic meningitis after intrathecal baclofen injection.
2006 May
Ethanol blocks nicotine-induced seizures in mice: comparison with midazolam and baclofen.
2006 Nov
Genomic and functional conservation of sedative-hypnotic targets in the zebrafish.
2007 Apr
Experience with external pump trial prior to implantation for intrathecal baclofen in ambulatory patients with spastic cerebral palsy.
2007 Jan-Mar
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
Effects of GABA(B) receptor agents on cocaine priming, discrete contextual cue and food induced relapses.
2007 Oct 1
Patents

Sample Use Guides

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
Substance Class Chemical
Created
by admin
on Fri Dec 16 22:31:01 UTC 2022
Edited
by admin
on Fri Dec 16 22:31:01 UTC 2022
Record UNII
64OSE3996V
Record Status Validated (UNII)
Record Version
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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 16 22:31:01 UTC 2022 , Edited by admin on Fri Dec 16 22:31:01 UTC 2022
Code System Code Type Description
PUBCHEM
6602720
Created by admin on Fri Dec 16 22:31:01 UTC 2022 , Edited by admin on Fri Dec 16 22:31:01 UTC 2022
PRIMARY
CAS
70206-22-3
Created by admin on Fri Dec 16 22:31:01 UTC 2022 , Edited by admin on Fri Dec 16 22:31:01 UTC 2022
SUPERSEDED
CAS
28311-31-1
Created by admin on Fri Dec 16 22:31:01 UTC 2022 , Edited by admin on Fri Dec 16 22:31:01 UTC 2022
PRIMARY
NCI_THESAURUS
C90887
Created by admin on Fri Dec 16 22:31:01 UTC 2022 , Edited by admin on Fri Dec 16 22:31:01 UTC 2022
PRIMARY
FDA UNII
64OSE3996V
Created by admin on Fri Dec 16 22:31:01 UTC 2022 , Edited by admin on Fri Dec 16 22:31:01 UTC 2022
PRIMARY
MERCK INDEX
M2200
Created by admin on Fri Dec 16 22:31:01 UTC 2022 , Edited by admin on Fri Dec 16 22:31:01 UTC 2022
PRIMARY Merck Index
DRUG BANK
DBSALT002256
Created by admin on Fri Dec 16 22:31:01 UTC 2022 , Edited by admin on Fri Dec 16 22:31:01 UTC 2022
PRIMARY
Related Record Type Details
PARENT -> SALT/SOLVATE
Related Record Type Details
ACTIVE MOIETY