GABITRIL Product Information

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Important Safety Update

GABITRIL is only indicated as adjunctive therapy in adults and children 12 years and older in the treatment of partial seizures. Cephalon, Inc. does not recommend the use of GABITRIL for any other indication.

GABITRIL Selectively Targets GABA Reuptake in Preclinical Models^1-6


Reuptake of GABA into the presynaptic neuron and glial cell	GABITRIL inhibits reuptake through highly selective binding to the GAT-1 transporter

GABITRIL—A Selective GABA Reuptake Inhibitor (SGRI)

Increases GABA levels in vitro by selectively binding to GAT-1, the predominant GABA uptake transporter
Proven safety profile with a low potential for drug interactions
Linear pharmacokinetics offer predictable systemic exposure
More than 61 million patient days of exposure to GABITRIL therapy³
The precise mechanism by which GABITRIL exerts its effect in humans is unknown

References:
1.	Borden LA, Murali Dhar TG, Smith KE, Weinshank RL, Branchek TA, Gluchowski C. Tiagabine, SK&F 89976-A, CI-966, and NNC-711 are selective for the cloned GABA transporter GAT-1. Eur J Pharmacol. 1994;269:219-224.
2.	GABITRIL package insert, Cephalon, Inc.
3.	Data on file, Cephalon, Inc.
4.	Giardina WJ. Anticonvulsant action of tiagabine, a new GABA-uptake inhibitor. J Epilepsy. 1994;7:161-166.
5.	Schachter SC. Tiagabine: current status and potential clinical applications. Exp Opin Invest Drugs. 1996;5:1377-1387.
6.	Fink-Jensen A, Suzdak PD, Swedberg MDB, Judge ME, Hansen L, Nielsen PG. The g-aminobutyric acid (GABA) uptake inhibitor, tiagabine, increases extracellular brain levels of GABA in awake rats. Eur J Pharmacol. 1992;220:197-201.