Tiagabine pharmacology in profile

Epilepsia
M J Brodie

Abstract

Tiagabine (TGB) hydrochloride, a nipecotic acid derivative linked to a lipophilic anchor, potently and specifically inhibits uptake of the inhibitory neurotransmitter gamma-aminobutyric acid (GABA) into astrocytes and neurons. With microdialysis, 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 seizure models, including pentylenetetrazol-induced, methyl-6,7-dimethoxy-4-ethyl-beta-carboline-3-carboxylate (DMCM)-induced tonic, amygdala-kindled and picrotoxin-induced convulsions, and maximal electroshock seizures in rodents. In humans, TGB absorption is rapid and complete. It is metabolized in the liver, largely by isoform 3A of the cytochrome P450 family of enzymes. The process of elimination is linear, with a half-life of 5-8 h. TGB does not induce or inhibit metabolic processes, although it provides a target for enzyme inducers that can lower its elimination half-life to 2-3 h. Accordingly, TGB does not alter the concentrations of other antiepileptic drugs (AEDs), with the possible exception of a small decrease in valproate levels. A ...Continue Reading

References

Apr 24, 1991·European Journal of Pharmacology·E B NielsenC Braestrup
Jul 28, 1990·Lancet·B S Meldrum
Jan 1, 1990·British Journal of Pharmacology·J C ReklingA Mosfeldt Laursen
Mar 1, 1987·Epilepsy Research·P Krogsgaard-LarsenA Schousboe
Jun 1, 1995·Seizure : the Journal of the British Epilepsy Association·J P LeachM J Brodie
Oct 14, 1994·European Journal of Pharmacology·L A BordenC Gluchowski
Jan 1, 1994·Epilepsia·H Mengel

❮ Previous
Next ❯

Citations

Jun 29, 2005·Psychopharmacology·Mehmet SofuogluThomas Kosten
Feb 12, 2008·Psychopharmacology·L M McDonaldP H Hutson
Jul 13, 2001·Pharmacology & Therapeutics·P KwanM J Brodie
Jul 11, 2001·Progress in Neuro-psychopharmacology & Biological Psychiatry·U SchmittC Hiemke
May 10, 2003·Clinical Neurophysiology : Official Journal of the International Federation of Clinical Neurophysiology·Carlo Alberto TassinariRoberto Michelucci
Nov 1, 1996·British Journal of Clinical Pharmacology·E Perucca
Jan 1, 1995·Epilepsia·I E Leppik
Nov 24, 1998·Journal of Clinical Pharmacology·M S ThomsenT Kruse
Aug 11, 2000·Pharmacotherapy·J M Pellock
Feb 5, 1998·Lancet·J P Leach, M J Brodie
Oct 13, 2000·Fundamental & Clinical Pharmacology·M S Benedetti
Oct 26, 1999·Epilepsia·J M Pellock, R Appleton
Oct 26, 1999·Epilepsia·S C Schachter
Nov 21, 2007·Emergency Medicine Australasia : EMA·Richard A ForbesFrank F S Daly
Oct 2, 2013·European Neuropsychopharmacology : the Journal of the European College of Neuropsychopharmacology·Xin-Hong XuZhi-Li Huang
Mar 1, 1997·Seminars in Pediatric Neurology·J M Pellock, N Watemberg
Jun 28, 2005·Epilepsy & Behavior : E&B·Thomas N Ferraro, Russell J Buono
May 5, 2001·Expert Opinion on Pharmacotherapy·S C Schachter
Oct 20, 1998·Journal of the American Geriatrics Society·J I Sirven
Dec 7, 2000·Mental Retardation and Developmental Disabilities Research Reviews·J M Pellock, L D Morton
Apr 1, 1997·Cephalalgia : an International Journal of Headache·T J SteinerA W Yuen
Mar 14, 2009·The Neurologist·Rosa Ana Saiz DíazJosé Serratosa
Mar 13, 2002·Epilepsia·S F Berkovic, I E Scheffer
Nov 1, 2002·Expert Review of Neurotherapeutics·Barry E GidalJacqueline A French
Jun 2, 1998·The Annals of Pharmacotherapy·G D Anderson
Nov 24, 1998·The Annals of Pharmacotherapy·M S Luer, D H Rhoney
Jul 3, 2021·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Magdalena KowalskaAlicja Nowaczyk

❮ Previous
Next ❯

Related Concepts

Related Feeds

Astrocytes

Astrocytes are glial cells that support the blood-brain barrier, facilitate neurotransmission, provide nutrients to neurons, and help repair damaged nervous tissues. Here is the latest research.

Amygdala and Midbrain Dopamine

The midbrain dopamine system is widely studied for its involvement in emotional and motivational behavior. Some of these neurons receive information from the amygdala and project throughout the cortex. When the circuit and transmission of dopamine is disrupted symptoms may present. Here is the latest research on the amygdala and midbrain dopamine.

Amygdala: Sensory Processes

Amygdalae, nuclei clusters located in the temporal lobe of the brain, play a role in memory, emotional responses, and decision-making. Here is the latest research on sensory processes in the amygdala.