TIZANIDINE HYDROCHLORIDE tablet

Land: USA

Sprog: engelsk

Kilde: NLM (National Library of Medicine)

Aktiv bestanddel:

TIZANIDINE HYDROCHLORIDE (UNII: B53E3NMY5C) (TIZANIDINE - UNII:6AI06C00GW)

Tilgængelig fra:

Clinical Solutions Wholesale

INN (International Name):

TIZANIDINE HYDROCHLORIDE

Sammensætning:

TIZANIDINE 4 mg

Recept type:

PRESCRIPTION DRUG

Autorisation status:

Abbreviated New Drug Application

Produktets egenskaber

TIZANIDINE HYDROCHLORIDE- TIZANIDINE HYDROCHLORIDE TABLET
CLINICAL SOLUTIONS WHOLESALE
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TIZANIDINE TABLETS USP
DESCRIPTION
Tizanidine hydrochloride is a centrally acting α -adrenergic agonist.
Tizanidine hydrochloride is a
white to off-white, fine crystalline powder, which is odorless or with
a faint characteristic odor.
Tizanidine is slightly soluble in water and methanol; solubility in
water decreases as the pH increases.
Its chemical name is
5-chloro-4-(2-imidazolin-2-ylamino)-2,1,3-benzothiodiazole
hydrochloride.
Tizanidine’s molecular formula is C H CIN S•HCl, its molecular
weight is 290.2 and its structural
formula is:
Tizanidine tablets USP are supplied as 2 mg and 4 mg tablets for oral
administration. Tizanidine tablets
USP are composed of the active ingredient, tizanidine hydrochloride
(2.288 mg equivalent to 2 mg
tizanidine base and 4.576 mg equivalent to 4 mg tizanidine base), and
the inactive ingredients, colloidal
silicon dioxide, lactose monohydrate, microcrystalline cellulose and
stearic acid.
CLINICAL PHARMACOLOGY
MECHANISM OF ACTION
Tizanidine is an agonist at α -adrenergic receptor sites and
presumably reduces spasticity by increasing
presynaptic inhibition of motor neurons. In animal models, tizanidine
has no direct effect on skeletal
muscle fibers or the neuromuscular junction, and no major effect on
monosynaptic spinal reflexes. The
effects of tizanidine are greatest on polysynaptic pathways. The
overall effect of these actions is
thought to reduce facilitation of spinal motor neurons.
The imidazoline chemical structure of tizanidine is related to that of
the anti-hypertensive drug
clonidine and other α -adrenergic agonists. Pharmacological studies
in animals show similarities
between the two compounds, but tizanidine was found to have one-tenth
to one-fiftieth (1/50) of the
potency of clonidine in lowering blood pressure.
PHARMACOKINETICS
Absorption and Distribution
Following oral administration, tizanidine is essentially completely
absorbed. The absolute oral
bioavailabilit