Tiagabin

GABAergic transmission, tiagabine has sedative side effects. 

GABA transporter GAT1 (SLC6A1) GABAergic neurons in CNS <10 Clearance of interstitial neurotransmitter, reuptake into neurons Tiagabine, an antiepileptic drug... 

QH15NO2 5006-62-2) see Tiagabine a-ethyl-4-nitrobenzeneacetic acid (C (,H, N04 7463-53-8) see Indobufen ethyl 4-nitrobenzoate (C9H9NO4 99-77-4) see Benzocaine ethyl 3-nitro-benzylideneacetoacetate (CijHijNO, 39562-16-8) see Nitrendipine ethyl At-(2-nitro-6-chlorobenzyl)glycinate... 

Vigabatrin (not marketed in United States), tiagabine, topiramate, gabapentin, carbamazepine, lamotrigine... 

Gonzalez G, Sevarino K, Sofuoglu M, et al Tiagabine increases cocaine-free urines in cocaine-dependent methadone-treated patients results of a randomized pilot study. Addiction 98 1625-1632, 2003... 

In parallel with the identification of distinct transporters for GABA there has been continued interest in the development of selective blockers of these transporters and the therapeutic potential that could result from prolonging the action of synaptically released GABA. It has been known for a long time that certain pro-drugs of nipecotic add (e.g. nipecotic acid ethyl ester) are able to cross the blood-brain barrier and are effective anticonvulsants in experimental models of epilepsy. More recently, several different systemically active lipophillic compounds have been described that act selectively on GAT-1, GAT-2 or GAT-3 (Fig. 11.4). Of these, tiagabine (gabitiil), a derivative of nipecotic acid that acts preferentially on GAT -1, has proved clinically useful in cases of refractory epilepsy. 

Thompson, SM and Gahwiler, BH (1992) Effects of the GABA uptake inhibitor tiagabine on inhibitory synaptic potentials in rat hippocampal slice cultures. J. Neurophysiol. 67 1698-1701. 

Outside of the evidence-based guidelines, other pharmacologic treatments are commonly used or avoided. For initial treatment of absence seizures, ethosuximide and valproate are commonly used, not only in the United Kingdom, but also in the United States. Zonisamide may be also used for initial treatment of absence and myoclonic seizures. In absence and myoclonic seizures, carbamazepine, oxcarbazepine, gabapentin, tiagabine, and pregabalin should be avoided, as they have been associated with an exacerbation of these types of seizures. 

Phenobarbital Phenytoin Topiramate Valproate Oxcarbazepine Topiramate Second-line Clobazam6 Gabapentin Levetiracetam Phenytoin Tiagabine... 

Winhusen T.M., Somoza E.C., Harrer J.M. et al. A placebo-controlled screening trial of tiagabine, sertraline and donepezil as cocaine dependence treatments. Addiction. 100(Suppl. 1) 68, 2005. 

Carbamazepine, phenytoin, valproate, gabapentin, lamotrigine, levetiracetam, tiagabine, topiramate, zonisamide... 

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