- Molecular NameTiagabine
- SynonymTiagabina [INN-Spanish]; Tiagabinum [INN-Latin]
- Weight375.557
- Drugbank_IDDB00906
- ACS_NO115103-54-3
- Show 2D model
- LogP (experiment)N/A
- LogP (predicted, AB/LogP v2.0)4.83
- pka3.3, 9.4 (tiagabine hydrochloride)
- LogD (pH=7, predicted)2.33
- Solubility (experiment)N/A
- LogS (predicted, ACD/Labs)(ph=7)-4.3
- LogSw (predicted, AB/LogsW2.0)0.02
- Sw (mg/ml) (predicted, ACD/Labs)0.02
- No.of HBond Donors1
- No.of HBond Acceptors3
- No.of Rotatable Bonds6
- TPSA97.02
- StatusFDA approved
- AdministrationN/A
- PharmacologyAn anti-convulsive medication.The medication is also used in the treatment of panic disorder, as are a few other anticonvulsants.
- Absorption_value95.0
- Absorption (description)Tiagabine is nearly completely absorbed (>95%).
- Caco_2N/A
- Bioavailability90.0
- Protein binding96.0
- Volume of distribution (VD)1.3 L/kg
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmMetabolized primarily by UGT and CYP3A.
- Half life7~9 h. May be reduced to 2~3 h by the concomitant administration of liver enzyme inducing drugs.
- ExcretionFecal and renal
- Urinary Excretion1~2
- Clerance2.0 ml/min/kg
- ToxicitySmptoms most often accompanying tiagabine overdose, alone or in combination with other drugs, have included: seizures including status epilepticus in patients with and without underlying seizure disorders, nonconvulsive status epilepticus, coma, ataxia, confusion, somnolence, drowsiness, impaired speech, agitation, lethargy, myoclonus, spike wave stupor, tremors, disorientation, vomiting, hostility, and temporary paralysis. Respiratory depression was seen in a number of patients, including children, in the context of seizures.
- LD50 (rat)N/A
- LD50 (mouse)N/A