Страна: САЩ
Език: английски
Източник: NLM (National Library of Medicine)
TIAGABINE HYDROCHLORIDE (UNII: DQH6T6D8OY) (TIAGABINE - UNII:Z80I64HMNP)
Avera McKennan Hospital
TIAGABINE HYDROCHLORIDE
TIAGABINE HYDROCHLORIDE 4 mg
PRESCRIPTION DRUG
New Drug Application Authorized Generic
TIAGABINE HYDROCHLORIDE- TIAGABINE HYDROCHLORIDE TABLET, FILM COATED AVERA MCKENNAN HOSPITAL ---------- TIAGABINE HYDROCHLORIDE TABLETS RX ONLY DESCRIPTION Tiagabine hydrochloride is an antiepilepsy drug available as 2 mg and 4 mg tablets for oral administration. Its chemical name is (-)-(R)-1-[4,4-Bis(3-methyl-2-thienyl)-3-butenyl]nipecotic acid hydrochloride, its molecular formula is C H NO S HCl, and its molecular weight is 412.0. Tiagabine HCl is a white to off-white, odorless, crystalline powder. It is insoluble in heptane, sparingly soluble in water, and soluble in aqueous base. The structural formula is: INACTIVE INGREDIENTS Tiagabine HCl tablets contain the following inactive ingredients: Ascorbic acid, colloidal silicon dioxide, crospovidone, hydrogenated vegetable oil wax, hydroxypropyl cellulose, hypromellose, lactose, magnesium stearate, microcrystalline cellulose, pregelatinized starch, stearic acid, and titanium dioxide. In addition, individual tablets contain: CLINICAL PHARMACOLOGY MECHANISM OF ACTION The precise mechanism by which tiagabine exerts its antiseizure effect is unknown, although it is believed to be related to its ability, documented in _in vitro_ experiments, to enhance the activity of gamma aminobutyric acid (GABA), the major inhibitory neurotransmitter in the central nervous system. These experiments have shown that tiagabine binds to recognition sites associated with the GABA uptake carrier. It is thought that, by this action, tiagabine blocks GABA uptake into presynaptic neurons, permitting more GABA to be available for receptor binding on the surfaces of post-synaptic cells. Inhibition of GABA uptake has been shown for synaptosomes, neuronal cell cultures, and glial cell cultures. In rat-derived hippocampal slices, tiagabine has been shown to prolong GABA-mediated inhibitory post-synaptic potentials. Tiagabine increases the amount of GABA available in the extracellular space of the globus pallidus, ventral palladum, and substantia nigra in rats at the ED and ED doses for inhibiti Прочетете целия документ