TIAGABINE HYDROCHLORIDE tablet film coated

Država: Sjedinjene Američke Države

Jezik: engleski

Izvor: NLM (National Library of Medicine)

Aktivni sastojci:

TIAGABINE HYDROCHLORIDE (UNII: DQH6T6D8OY) (TIAGABINE - UNII:Z80I64HMNP)

Dostupno od:

Avera McKennan Hospital

INN (International ime):

TIAGABINE HYDROCHLORIDE

Sastav:

TIAGABINE HYDROCHLORIDE 4 mg

Tip recepta:

PRESCRIPTION DRUG

Status autorizacije:

New Drug Application Authorized Generic

Svojstava lijeka

TIAGABINE HYDROCHLORIDE- TIAGABINE HYDROCHLORIDE TABLET, FILM COATED
AVERA MCKENNAN HOSPITAL
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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