Products
Tiagabine was commercially available in the form of film-coated tablets (gabitril). It was approved in many countries in 1996 and went off the market in June 2012.
Structure and properties
Tiagabine (C20H25NO2S2, Mr = 375.5 g/mol) is a piperidine and thiophene derivative. It exists as a white crystalline powder that is sparingly soluble in water.
Effects
Tiagabine (ATC N03AG06) is antiepileptic. It selectively inhibits the reuptake of GABA into presynaptic neurons and into glial cells, resulting in an increase in GABAergic inhibition in the brain. The effects are due to inhibition of the neurotransmitter transporter GAT.
Indications
For add-on treatment with other antiepileptic drugs for partial seizures with or without secondary generalization.
Dosage
According to the SmPC. The drug is administered with meals.
Contraindications
Tiagabine is contraindicated in hypersensitivity and severe hepatic insufficiency. For complete precautions, see the drug label.
Interactions
Tiagabine is metabolized by CYP3A4 and corresponding drug-drug interactions are possible with inducers and inhibitors of the isoenzyme.
Adverse effects
The most common potential adverse effects include fatigue, dizziness, tremor, drowsiness, nervousness, and nausea.
