Tiagabine
Tiagabine. Selective GAT-1 GABA-reuptake inhibitor — increases synaptic GABA dwell time → enhanced inhibitory tone in cortex / hippocampus.… Oral half-life 5.7 h.
Selective GAT-1 GABA-reuptake inhibitor — increases synaptic GABA dwell time → enhanced inhibitory tone in cortex / hippocampus. FDA-approved for partial seizures (adjunct). Off-label for anxiety + sleep architecture studies. Highly protein-bound (~96%); extensive CYP3A4 metabolism.
PK: F 0.96 WAS A PROTEIN-BINDING FRACTION — the source sentence is that tiagabine "is highly (96%) bound to plasma proteins", one clause away from the 7 h half-life that was also taken from it. The record now carries one internally consistent population fit (PMID:11042231, 130 monotherapy patients): "1.25 /h" absorption, "62.0 L" apparent volume and "5.72 h" half-life, with F pinned to 1 because that volume is apparent. This is one of only two genuine published human absorption rate constants found across the whole audit. The healthy-subject half-life of 7 h is also real (PMID:9118850) but must not be mixed with a volume and rate fitted at 5.72 h. V 70 L was a shared default.
Pharmacokinetics
- Oral — t½ 5.7 h · F 100% · ka 1.25 h⁻¹ · Vd 62 L
Sources: PMID:2299358, PMID:11042231, PMID:9118850, PMID:8827398