[Durgical](https://durgical.com/en/) › [DurgiPedia](https://durgical.com/en/durgipedia/) › [Pharmacology](https://durgical.com/en/pharmacology/) › [Antiseizure medicines](https://durgical.com/en/pharmacology/classes/antiseizure-medicines/) › Tiagabine

[Pharmacology](https://durgical.com/en/pharmacology/) · [Antiseizure medicines](https://durgical.com/en/pharmacology/classes/antiseizure-medicines/)

# Tiagabine

An add-on medicine for focal seizures that blocks the GABA transporter GAT-1, so GABA stays longer in the synapse.

Updated 2026-11-01

- Class: [Antiseizure medicines](https://durgical.com/en/pharmacology/classes/antiseizure-medicines/)
- Transporter: GABA transporter 1 (GAT-1)
- ATC code: N03AG06

⇄**GABA transporter 1 (GAT-1)**Tiagabine

ⓘ The figure shows tiagabine bound to the human GABA transporter GAT-1 in its inward-open state.

**Target in 3D:** GABA transporter 1 (GAT-1). PDB structure 7SK2 (RCSB PDB, public domain). [View the structure at RCSB PDB](https://www.rcsb.org/structure/7SK2) · Drag to rotate · pinch to zoom

## Mechanism of action

Tiagabine blocks GAT-1, the transporter that takes GABA back into neurons and glia after release. GABA stays longer in the synaptic cleft and inhibits neurons more strongly.

- Binds the GABA transporter GAT-1
- GABA reuptake into neurons and glia is blocked
- GABA stays longer in the synapse
- Inhibition is stronger and seizures less frequent

## Pharmacokinetics

**Absorption**
Well absorbed by mouth; food slows absorption but not the amount

**Distribution**
Highly bound to plasma proteins

**Metabolism**
In the liver, mainly by CYP3A

**Half-life**
About 7 to 9 hours; about 2 to 5 hours with enzyme-inducing antiseizure medicines

## Indications

- Add-on treatment of focal seizures in adults and adolescents [Epilepsy and seizures →](https://durgical.com/en/conditions/epilepsy-and-seizures/)

## Adverse effects

### Common

- Dizziness and lack of energy
- Sleepiness
- Nausea and abdominal pain
- Nervousness, irritability and tremor
- Difficulty concentrating

### Serious (rare, important)

- New seizures and status epilepticus in people without epilepsy (off-label use)
- Worsening of EEG abnormalities in people with a history of spike-and-wave discharges
- Suicidal thoughts

## Contraindications

- Hypersensitivity to tiagabine

## Key interactions

**Enzyme-inducing antiseizure medicines (carbamazepine, phenytoin, phenobarbital)**
Much faster clearance and lower tiagabine levels

**Other highly protein-bound drugs**
Possible displacement

**Alcohol and other sedatives**
More sleepiness and dizziness

## What is monitored

- Seizure control and any new seizure type
- Dizziness and concentration
- Mood and suicidal thoughts

## Administration and safety

- Given by mouth
- Not used outside epilepsy: in people without epilepsy it has caused seizures
- Withdrawn gradually

## Nursing care

- Check whether the patient also takes enzyme inducers, which change its effect
- Warn about dizziness and sleepiness before driving
- Teach to report new or different seizures

## Pregnancy and breastfeeding

Human data are limited; benefits and risks are weighed with specialist care.

## Memory aid

Tiagabine: «Tie up GAT» – it ties up the GABA transporter so GABA lingers.

## Test yourself

Think of the answer, then tap the question to see it.

## What is the target of tiagabine?

GAT-1, the GABA transporter that takes GABA back into neurons and glia.

## Why can tiagabine be dangerous in people without epilepsy?

Off-label use has been linked to new seizures and status epilepticus in people without epilepsy.

## How do enzyme inducers change tiagabine?

Carbamazepine, phenytoin and phenobarbital speed its clearance and shorten its half-life.

[Add to my cards (3)](https://durgical.app/estudiar/?add=/en/pharmacology/tiagabine/)

## Related drugs

- [Vigabatrin](https://durgical.com/en/pharmacology/vigabatrin/)

## Related conditions

- [Epilepsy and seizures](https://durgical.com/en/conditions/epilepsy-and-seizures/)

[← Back to the class: Antiseizure medicines](https://durgical.com/en/pharmacology/classes/antiseizure-medicines/)

Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.

Sources: [Tiagabine: MedlinePlus Drug Information](https://medlineplus.gov/druginfo/meds/a698014.html) (MedlinePlus (U.S. National Library of Medicine), 2026); [DailyMed - TIAGABINE HYDROCHLORIDE tablet, film coated](https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=953ef3cc-e3cb-480f-b9ea-256520fd62b8) (DailyMed (U.S. National Library of Medicine), 2026); [ATCDDD - ATC/DDD Index](https://atcddd.fhi.no/atc_ddd_index/?code=N03AG06) (WHO Collaborating Centre for Drug Statistics Methodology, 2026).

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Representative model, for educational purposes only.

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Source: https://durgical.com/en/pharmacology/tiagabine/
License: CC BY 4.0 (https://creativecommons.org/licenses/by/4.0/). Cite as: DurgiPedia (durgical.com), https://durgical.com/en/pharmacology/tiagabine/