Tiagabine
- Atc Codes:N03AG06
- CAS Codes:145821-59-6#115103-54-3
- PHARMGKB ID:145821-59-6#115103-54-3
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Substrate of
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Gabitril; Belgium: Gabitril; Bulgaria: Gabitril; Czech Republic: Gabitril; Denmark: Gabitril; Finland: Gabitril; France: Gabitril; Germany: Gabitril; Greece: Gabitril; Ireland: Gabitril; Italy: Gabitril; Latvia: Gabitril; Lithuania: Gabitril; Poland: Gabitril; Portugal: Gabitril; Slovakia: Gabitril; Slovenia: Gabitril; Spain: Gabitril; UK: Gabitril.
North America
USA: Gabitril.
Drug combinations
Chemistry
Tiagabine Hydrochloride: C~20~H~25~NO~2~S~2~ HCl. Mw: 412.01. (1) 3-Piperidinecarboxylic acid, 1-[4,4-bis(3-methyl-2-thienyl)-3-butenyl]-, hydrochloride, (R)-; (2)(-)-(R)-1-[4,4-Bis(3-methyl-2-thienyl)-3-butenyl]nipecotic acid, hydrochloride. CAS-145821-59-6; CAS-115103-54-3 (tiagabine)(1996).
Pharmacologic Category
Anticonvulsants, Miscellaneous. (ATC-Code: N03AG06).
Mechanism of action
Exact mechanism not definitively known; however, in vitro experiments demonstrate that it enhances activity of gamma-aminobutyric acid (GABA). It is thought that binding to GABA uptake carrier inhibits uptake of GABA into presynaptic neurons, allowing availability of increased amount of GABA to postsynaptic neurons. Based on in vitro studies, tiagabine does not inhibit uptake of dopamine, norepinephrine, serotonin, glutamate, or choline.
Therapeutic use
Adjunctive therapy in adults and children ≥12 years of age in treatment of partial seizures.
Pregnancy and lactiation implications
Use with caution in pregnancy. Enters breast milk (not recommended in nursing women).
Unlabeled use
Contraindications
Hypersensitivity to tiagabine or any component of the formulation.
Warnings and precautions
May cause CNS depression. Severe reactions, including toxic epidermal necrolysis and Stevens-Johnson syndromes, although rarely reported, resulted in fatalities. Use with caution in hepatic impairment. Caution should be used in treating any patient not receiving one of these medications. Effects with other sedative drugs or ethanol may be potentiated. Anticonvulsants should not be discontinued abruptly due to possibility of increasing seizure frequency.