TIAGABINE HYDROCHLORIDE tablet

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

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

Available from:

Northstar Rx LLC

Administration route:

ORAL

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

Tiagabine hydrochloride tablet is indicated as adjunctive therapy in adults and children 12 years and older in the treatment of partial seizures. Tiagabine hydrochloride is contraindicated in patients who have demonstrated hypersensitivity to the drug or its ingredients. The abuse and dependence potential of tiagabine hydrochloride have not been evaluated in human studies.

Product summary:

Tiagabine hydrochloride tablets are available in four dosage strengths. 2 mg light orange-peach colored, round shaped, biconvex film-coated tablets debossed with “MT”  on one side and “3” on the other side, are available in bottles of 30 (NDC 16714-151-01). 4 mg yellow colored, round shaped, biconvex film-coated tablets debossed with “MT” on one side and “4” on the other side, are available in bottles of 30 (NDC 16714-152-01). 12 mg green colored, capsule shaped, biconvex film-coated tablets debossed with “MT” on one side and “5” on the other side, are available in bottles of 30 (NDC 16714-153-01). 16 mg blue colored, capsule shaped, biconvex film-coated tablets debossed with “MT” on one side and “6” on the other side, are available in bottles of 30  (NDC 16714-154-01). Recommended Storage: Store at 20° to 25°C (68° to 77°F). [See USP Controlled Room Temperature]. Protect from light and moisture.

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

TIAGABINE HYDROCHLORIDE - TIAGABINE HYDROCHLORIDE TABLET
NORTHSTAR RX LLC
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DESCRIPTION
Tiagabine hydrochloride USP is an antiepilepsy drug available as 2 mg,
4 mg, 12 mg,
and 16 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 412.01. Tiagabine HCl, USP is a
white to
off-white powder. It is freely soluble in methanol and in alcohol,
soluble in 5% Water in
isopropanol, very slightly soluble in chloroform, sparingly soluble in
water and practically
insoluble in n-Heptane. The structural formula is:
INACTIVE INGREDIENTS
Tiagabine hydrochloride tablets contain the following inactive
ingredients: Butylated
hydroxyanisole, colloidal silicon dioxide, crospovidone, hydrogenated
vegetable oil
(cottonseed oil), hydroxypropyl cellulose, hypromellose, lactose
anhydrous, magnesium
stearate, microcrystalline cellulose, pregelatinized starch, stearic
acid and titanium
dioxide.
In addition, individual tablets contain:
2 mg tablets: FD&C yellow No. 6 aluminum lake
4 mg tablets: D&C yellow No. 10 aluminum lake
12 mg tablets: D&C yellow No. 10 aluminum lake and FD&C Blue No. 1
aluminum lake
16 mg tablets: FD&C blue No. 2 aluminum lake
CLINICAL PHARMACOLOGY
20
25
2 2
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