Drug/Small Molecule:
tiagabine

2D structure

Overview

Generic Names: Tiagabina [INN-Spanish]; Tiagabinum [INN-Latin]
Trade Names: Gabitril
PharmGKB Accession Id: PA451682

Description

Tiagabine is an anti-convulsive medication. It is also used in the treatment for panic disorder as are a few other anticonvulsants. Though the exact mechanism by which tiagabine exerts its effect on the human body is unknown, it does appear to operate as a selective GABA reuptake inhibitor. (source: Drug Bank)

Indication

For the treatment of partial seizures (source: Drug Bank)

ATC Therapeutic Category

  • N03AG:Fatty acid derivatives

Pharmacology, Interactions, and Contraindications

Mechanism Of Action

Though the exact mechanism by which Tiagabine exerts its effect on the human body is unknown, it does appear to operate as a selective GABA reuptake inhibitor. (source: Drug Bank)

Pharmacology

Tiagabine is used primarily as an anticonvulsant for the adjunctive treatment of epilepsy. The precise mechanism by which Tiagabine exerts its antiseizure effect is unknown, although it is believed to be related to its ability to enhance the activity of gamma aminobutyric acid (GABA), the major inhibitory neurotransmitter in the central nervous system. Tiagabine binds to recognition sites associated with the GABA uptake carrier. It is thought that, by this action, Tiagabine blocks GABA uptake into presynaptic neurons, permitting more GABA to be available for receptor binding on the surfaces of post-synaptic cells. (source: Drug Bank)

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Tiagabine is likely metabolized primarily by the 3A isoform subfamily of hepatic cytochrome P450. (source: Drug Bank)

Protein Binding

96% (source: Drug Bank)

Absorption

Tiagabine is nearly completely absorbed (>95%). (source: Drug Bank)

Toxicity

mptoms 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. (source: Drug Bank)

Isomeric SMILES Code:

CC1=C(SC=C1)/C(=C\CCN2C[C@@H](CCC2)C(=O)O)/C3=C(C=CS3)C (source: Drug Bank)

The following genes are in curated knowledge about this drug.

  Gene Relationship Evidence
No phenotype data Genotype Data Available Literature annotations available Not annotated
SLC6A1
  •   
  • PD
  •   
  • FA
  •   
Publications

A list of non-curated publications that mention this drug along with other genes is available.

Drug Targets

Gene Description
ABAT Uncurated Annotation (source: Drug Bank)
SLC6A1 Uncurated Annotation (source: Drug Bank)

A list of non-curated publications that mention this drug along with other drugs is available.

Curated Information

The following diseases are in curated knowledge about this drug.

  Disease Relationship Evidence
No phenotype data No genotype data Literature annotations available Not annotated
Epilepsy
  •   
  • PD
  •   
  •   
  • GN
Publications

Non-Curated Information

A list of non-curated publications that mention this drug along with other diseases is available.

Additional Datasets

These datasets are minimally curated and are sorted alphabetically by title.

  1. Physicochemical determinants of human renal clearance

LinkOuts

Web Resource:
Wikipedia
DrugBank:
DB00906
KEGG Compound ID:
C07503
PubChem Compound ID:
60648
PubChem Substance ID:
196924

Common Searches

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Non-Curated Publications

A list of non-curated publications that mention this drug is available.

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