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Details

Stereochemistry RACEMIC
Molecular Formula C10H12ClNO2
Molecular Weight 213.6611
Optical Activity ( + / - )
Defined Stereocenters 0 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of BACLOFEN

SMILES

c1cc(ccc1C(CC(=O)O)CN)Cl

InChI

InChIKey=KPYSYYIEGFHWSV-UHFFFAOYSA-N
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)

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

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
Status epilepticus complicating intrathecal baclofen overdose.
1992 Feb 8
Effects of nitrendipine, chlordiazepoxide, flumazenil and baclofen on the increased anxiety resulting from alcohol withdrawal.
1992 Jan
Effects of some GABAergic agents on quinine-induced seizures in mice.
1992 Jul 15
A case of mania associated with high-dose baclofen therapy.
1992 Jun
Indication, efficiency and complications of intrathecal pump supported baclofen treatment in spinal spasticity.
1992 Jun
Prolonged seizure activity after baclofen withdrawal.
1992 Mar
[Baclofen intoxication in chronic hemodialysis and kidney transplantation].
1992 May 8
Death after acute withdrawal of intrathecal baclofen: case report and literature review.
1999 Dec
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
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
GABA enhances transmission at an excitatory glutamatergic synapse.
2001 Aug 15
Cloning and functional expression of GABA(B) receptors from Drosophila.
2001 Feb
Modification of d-amphetamine-induced responses by baclofen in rats.
2001 Jan
Long-term intrathecal Baclofen infusion in supraspinal spasticity of adulthood.
2002 Feb
Baclofen decreases methamphetamine self-administration in rats.
2002 Jul 2
A possible baclofen-induced neurotoxicity in a CAPD patient who recovered with long-duration hemodialysis.
2002 Mar-Apr
Deep venous thrombosis as a result of hypotonia secondary to intrathecal baclofen therapy: a case report.
2002 Sep
Baclofen attenuates conditioned locomotion to cues associated with cocaine administration and stabilizes extracellular glutamate levels in rat nucleus accumbens.
2003
Pharmacological characterisation of a cell line expressing GABA B1b and GABA B2 receptor subunits.
2003 Apr 1
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
Intrathecal baclofen withdrawal mimicking sepsis.
2003 May
Pharmacological sensitivity and gene expression analysis of the tibial nerve injury model of neuropathic pain.
2003 May 30
Pharmacological complications of the chronic baclofen infusion in the severe spinal spasticity. Personal experience and review of the literature.
2004 Dec
Baclofen as adjunctive treatment for a patient with cocaine dependence and schizoaffective disorder.
2004 Oct
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
Prolonged intrathecal baclofen withdrawal syndrome. Case report and discussion of current therapeutic management.
2005 Jun
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
[Baclofen-associated encephalopathy in a hemodialysis patient with hiccups].
2006
Intrathecal baclofen toxicity and deep coma in minutes.
2006
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
GABAB1 receptor subunit isoforms exert a differential influence on baseline but not GABAB receptor agonist-induced changes in mice.
2006 Dec
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
Antinociceptive and behavioral effects of ribavirin in mice.
2006 Feb
Aseptic meningitis after intrathecal baclofen injection.
2006 May
GABAergic network activation of glial cells underlies hippocampal heterosynaptic depression.
2006 May 17
Baclofen-induced neurotoxicity in chronic renal failure patients with intractable hiccups.
2006 Nov
Baclofen-induced psychosis.
2006 Nov
Genomic and functional conservation of sedative-hypnotic targets in the zebrafish.
2007 Apr
GABA(B) receptor-positive modulation decreases selective molecular and behavioral effects of cocaine.
2007 Feb
Experience with external pump trial prior to implantation for intrathecal baclofen in ambulatory patients with spastic cerebral palsy.
2007 Jan-Mar
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
Name Type Language
BACLOFEN
EP   INN   MART.   MI   ORANGE BOOK   USAN   USP   USP-RS   VANDF   WHO-DD  
USAN   INN  
Official Name English
KEMSTRO
Brand Name English
BACLOFEN [JAN]
Common Name English
BACLOFEN [USP MONOGRAPH]
Common Name English
OZOBAX
Brand Name English
BACLOFEN [MI]
Common Name English
BA-34647
Code English
BACLOFEN [USAN]
Common Name English
BACLOFEN [WHO-DD]
Common Name English
BACLOFEN [ORANGE BOOK]
Common Name English
BACLOFEN [USP-RS]
Common Name English
4-AMINO-3-(4-CHLOROPHENYL)BUTANOIC ACID
Systematic Name English
BACLOFEN [INN]
Common Name English
BACLOFEN [MART.]
Common Name English
GABLOFEN
Brand Name English
BUTANOIC ACID, 4-AMINO-3-(4-CHLOROPHENYL)-
Common Name English
BA-34,647
Code English
BACLOFEN [EP MONOGRAPH]
Common Name English
NSC-755906
Code English
BACLOFEN [VANDF]
Common Name English
(RS)-BACLOFEN
Common Name English
LIORESAL
Brand Name English
.BETA.-(AMINOMETHYL)-P-CHLOROHYDROCINNAMIC ACID
Common Name English
Classification Tree Code System Code
WHO-ATC M03BX01
Created by admin on Fri Jun 25 21:05:38 UTC 2021 , Edited by admin on Fri Jun 25 21:05:38 UTC 2021
EU-Orphan Drug EU/3/14/1260
Created by admin on Fri Jun 25 21:05:38 UTC 2021 , Edited by admin on Fri Jun 25 21:05:38 UTC 2021
NDF-RT N0000000196
Created by admin on Fri Jun 25 21:05:38 UTC 2021 , Edited by admin on Fri Jun 25 21:05:38 UTC 2021
FDA ORPHAN DRUG 174703
Created by admin on Fri Jun 25 21:05:38 UTC 2021 , Edited by admin on Fri Jun 25 21:05:38 UTC 2021
FDA ORPHAN DRUG 23987
Created by admin on Fri Jun 25 21:05:38 UTC 2021 , Edited by admin on Fri Jun 25 21:05:38 UTC 2021
FDA ORPHAN DRUG 80494
Created by admin on Fri Jun 25 21:05:38 UTC 2021 , Edited by admin on Fri Jun 25 21:05:38 UTC 2021
WHO-VATC QM03BX01
Created by admin on Fri Jun 25 21:05:38 UTC 2021 , Edited by admin on Fri Jun 25 21:05:38 UTC 2021
FDA ORPHAN DRUG 493915
Created by admin on Fri Jun 25 21:05:38 UTC 2021 , Edited by admin on Fri Jun 25 21:05:38 UTC 2021
FDA ORPHAN DRUG 685619
Created by admin on Fri Jun 25 21:05:38 UTC 2021 , Edited by admin on Fri Jun 25 21:05:38 UTC 2021
FDA ORPHAN DRUG 480215
Created by admin on Fri Jun 25 21:05:38 UTC 2021 , Edited by admin on Fri Jun 25 21:05:38 UTC 2021
NDF-RT N0000175759
Created by admin on Fri Jun 25 21:05:38 UTC 2021 , Edited by admin on Fri Jun 25 21:05:38 UTC 2021
LIVERTOX 87
Created by admin on Fri Jun 25 21:05:38 UTC 2021 , Edited by admin on Fri Jun 25 21:05:38 UTC 2021
FDA ORPHAN DRUG 422914
Created by admin on Fri Jun 25 21:05:38 UTC 2021 , Edited by admin on Fri Jun 25 21:05:38 UTC 2021
NDF-RT N0000000116
Created by admin on Fri Jun 25 21:05:38 UTC 2021 , Edited by admin on Fri Jun 25 21:05:38 UTC 2021
NCI_THESAURUS C29696
Created by admin on Fri Jun 25 21:05:38 UTC 2021 , Edited by admin on Fri Jun 25 21:05:38 UTC 2021
FDA ORPHAN DRUG 64091
Created by admin on Fri Jun 25 21:05:38 UTC 2021 , Edited by admin on Fri Jun 25 21:05:38 UTC 2021
Code System Code Type Description
WIKIPEDIA
BACLOFEN
Created by admin on Fri Jun 25 21:05:38 UTC 2021 , Edited by admin on Fri Jun 25 21:05:38 UTC 2021
PRIMARY
CAS
1134-47-0
Created by admin on Fri Jun 25 21:05:38 UTC 2021 , Edited by admin on Fri Jun 25 21:05:38 UTC 2021
PRIMARY
DRUG CENTRAL
282
Created by admin on Fri Jun 25 21:05:38 UTC 2021 , Edited by admin on Fri Jun 25 21:05:38 UTC 2021
PRIMARY
RXCUI
1292
Created by admin on Fri Jun 25 21:05:38 UTC 2021 , Edited by admin on Fri Jun 25 21:05:38 UTC 2021
PRIMARY RxNorm
DRUG BANK
DB00181
Created by admin on Fri Jun 25 21:05:38 UTC 2021 , Edited by admin on Fri Jun 25 21:05:38 UTC 2021
PRIMARY
PUBCHEM
2284
Created by admin on Fri Jun 25 21:05:38 UTC 2021 , Edited by admin on Fri Jun 25 21:05:38 UTC 2021
PRIMARY
INN
2956
Created by admin on Fri Jun 25 21:05:38 UTC 2021 , Edited by admin on Fri Jun 25 21:05:38 UTC 2021
PRIMARY
IUPHAR
1084
Created by admin on Fri Jun 25 21:05:38 UTC 2021 , Edited by admin on Fri Jun 25 21:05:38 UTC 2021
PRIMARY
MERCK INDEX
M2200
Created by admin on Fri Jun 25 21:05:38 UTC 2021 , Edited by admin on Fri Jun 25 21:05:38 UTC 2021
PRIMARY Merck Index
NCI_THESAURUS
C28858
Created by admin on Fri Jun 25 21:05:38 UTC 2021 , Edited by admin on Fri Jun 25 21:05:38 UTC 2021
PRIMARY
USP_CATALOG
1048200
Created by admin on Fri Jun 25 21:05:38 UTC 2021 , Edited by admin on Fri Jun 25 21:05:38 UTC 2021
PRIMARY USP-RS
LACTMED
Baclofen
Created by admin on Fri Jun 25 21:05:38 UTC 2021 , Edited by admin on Fri Jun 25 21:05:38 UTC 2021
PRIMARY
EPA CompTox
1134-47-0
Created by admin on Fri Jun 25 21:05:38 UTC 2021 , Edited by admin on Fri Jun 25 21:05:38 UTC 2021
PRIMARY
EVMPD
SUB05667MIG
Created by admin on Fri Jun 25 21:05:38 UTC 2021 , Edited by admin on Fri Jun 25 21:05:38 UTC 2021
PRIMARY
FDA UNII
H789N3FKE8
Created by admin on Fri Jun 25 21:05:38 UTC 2021 , Edited by admin on Fri Jun 25 21:05:38 UTC 2021
PRIMARY
ChEMBL
CHEMBL701
Created by admin on Fri Jun 25 21:05:38 UTC 2021 , Edited by admin on Fri Jun 25 21:05:38 UTC 2021
PRIMARY
MESH
D001418
Created by admin on Fri Jun 25 21:05:38 UTC 2021 , Edited by admin on Fri Jun 25 21:05:38 UTC 2021
PRIMARY
ECHA (EC/EINECS)
214-486-9
Created by admin on Fri Jun 25 21:05:38 UTC 2021 , Edited by admin on Fri Jun 25 21:05:38 UTC 2021
PRIMARY