- Molecular NameBaclofen
- SynonymNA
- Weight213.664
- Drugbank_IDDB00181
- ACS_NO1134-47-0
- Show 2D model
- LogP (experiment)-1.0
- LogP (predicted, AB/LogP v2.0)0.23
- pka3.9, 9.6
- LogD (pH=7, predicted)0.23
- Solubility (experiment)2.09 mg/ml
- LogS (predicted, ACD/Labs)(ph=7)-1.84
- LogSw (predicted, AB/LogsW2.0)8.72
- Sw (mg/ml) (predicted, ACD/Labs)3.11
- No.of HBond Donors3
- No.of HBond Acceptors3
- No.of Rotatable Bonds4
- TPSA63.32
- StatusFDA approved
- AdministrationOral, intrathecal
- PharmacologyA derivative of gamma-aminobutyric acid (GABA) primarily used to treat spasticity. It is an agonist specific to mammalian but not fruit fly (Drosophila) GABAB receptors.
- Absorption_value95.0
- Absorption (description)Baclofen is rapidly absorbed after oral administration.
- Caco_2N/A
- Bioavailability70.0
- Protein binding31.0
- Volume of distribution (VD)0.81 L/kg
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmAbout 15% of a dose is metabolised, mainly to the deaminated derivative
- Half life3.75 h
- ExcretionAbout 80% of a dose is excreted in the urine in 24 h, mostly as unchanged drug; about 20% of a dose may be eliminated in the faeces as unchanged drug and metabolites.
- Urinary Excretion69
- Clerance2.72 ml/min/kg
- ToxicityRecovery has occurred after the ingestion of 1.5 g. A fatality occurred after ingestion of baclofen. Baclofen was detected in serum at a concentration of 17 mg/L and in urine at 760 mg/L which was collected 12 h after ingestion of the drug. [A. D. Fraser et al.,J. Forensic Sci.,1991, 36(5), 1596–1602]. Coma, respiratory failure and severe seizures occurred in a 39-year-old female subject after ingestion of 450 mg of baclofen; following treatment, the patient regained consciousness within 36 h, at which time a plasma concentration of 0.2 mg/L was reported; the plasma half-life was found to be 35 h. [K. Ghose et al.,Postgrad. Med. J.,1980, 56, 865–867].
- LD50 (rat)N/A
- LD50 (mouse)N/A