Tiagabine Pharmacology in Profile

  title={Tiagabine Pharmacology in Profile},
  author={Martin J Brodie},
  • M. Brodie
  • Published 1 June 1995
  • Biology
  • Epilepsia
Summary: Tiagabine (TGB) hydrochloride, a nipecotic acid derivative linked to a lipophilic anchor, potently and specifically inhibits uptake of the inhibitory neurotransmitter γ‐aminobu‐tyric acid (GABA) into astrocytes and neurons. With microdial‐ysis, TGB has been shown to increase extracellular overflow of GABA in the midbrain of awake rats. TGB administration prolongs neuronal depolarization induced by iontophoretically applied GABA in hippocampal slices. TGB is effective in a wide range of… 

Tiagabine in the Management of Epilepsy

Tiagabine (TGB) is a new antiepileptic drug (AED) that uniquely reduces the uptake of the inhibitory neurotransmitter ‐γ‐aminobutyric acid into presynaptic neuronal and glial cells that will find an enduring place in the management of epilepsy.


Tiagabine (TGB) is a recently approved antiepileptic drug (AED) that inhibits γ‐aminobutyric acid (GABA) reuptake into neurons and glia, a mechanism of action that is specific and unique among the

Tiagabine: A Novel Antiepileptic Drug

Tiagabine has demonstrated a good safety profile and, while it has not been demonstrated to be superior to other second-line AEDs for partial seizures, its safety and select mechanism of action warrant its further evaluation in the clinical setting.

Pharmacology and clinical experience with tiagabine

Open studies confirm that patients with medically refractory partial epilepsy can be successfully converted to TGB monotherapy and that TGB may be effective for other seizure types, such as infantile spasms.

Metabolism and Excretion of Mood Stabilizers and New Anticonvulsants

Several of the newer anticonvulsants lack the problematic drug-drug interactions seen with older agents, and some may even (based on their mechanisms of action and preliminary preclinical and clinical data) ultimately prove to have novel psychotropic effects.

Deliberate self‐poisoning with tiagabine: An unusual toxidrome

A 44‐year‐old woman presented after deliberate self‐poisoning with 100 tiagabine 15 mg tablets and was associated with the rapid onset of coma and an unusual toxidrome, and recovery was complicated by agitated delirium.

Tiagabine: The Safety Landscape

Tiagabine (TGB) hydrochloride is a potential new antiepileptic drug (AED) undergoing clinical development and was found to be tolerated in an integrated safety analysis of five double‐blind, add‐on therapy trials involving approximately 1,000 patients with epilepsy with difficult‐to‐control seizures with existing AEDs.

Enzyme induction and inhibition by new antiepileptic drugs: a review of human studies

  • M. Benedetti
  • Biology, Medicine
    Fundamental & clinical pharmacology
  • 2000
The aim of this paper is to review a number of new antiepileptic agents for their inducing and/or inhibitory properties in humans, mainly considering the interactions where they are involved as the cause rather than the object of such interactions.

Antiepileptic Drug Tiagabine Does Not Directly Target Key Cardiac Ion Channels Kv11.1, Nav1.5 and Cav1.2

It was found that tachycardia and other tiagabine-induced cardiac complications are not due to a direct effect of this drug on ventricular depolarization and repolarization.



Pharmacokinetics of Tiagabine, a γ‐Aminobutyric Acid‐Uptake Inhibitor, in Healthy Subjects After Single and Multiple Doses

Tiagabine (TGB) HC1, a new antiepileptic compound, is a potent and specific inhibitor of γ‐aminobutyric acid (GABA) uptake and indicated that TGB does not induce or inhibit hepaticmicrosomal enzyme systems.

The effect of two lipophilic γ‐aminobutyric acid uptake blockers in CA1 of the rat hippocampal slice

It is found that NO–05–0328 and NO‐05‐0329, at least in vitro, are more effective than older GABA uptake inhibitors such as nipecotic acid and they therefore deserve consideration for clinical use.

Blockade of GABA Uptake with Tiagabine Inhibits Audiogenic Seizures and Reduces Neuronal Firing in the Inferior Colliculus of the Genetically Epilepsy-Prone Rat

The blockade of GABA uptake by tiagabine may act to inhibit audiogenic seizures, in part, by intensifying these naturally occurring forms of acoustically evoked inhibition in inferior colliculus neurons.

(R)‐N‐[4,4‐Bis(3‐Methyl‐2‐Thienyl)but‐3‐en‐1‐yl]Nipecotic Acid Binds with High Affinity to the Brain γ‐Aminobutyric Acid Uptake Carrier

It is concluded that NO 328 is a potent and selective inhibitor of neuronal and glial GABA uptake and that [3H]NO 328 are a useful radioligand for labeling the GABA uptake carrier in brain membranes.