TIZANIDINE tablet

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

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

Available from:

St. Mary's Medical Park Pharmacy

INN (International Name):

TIZANIDINE HYDROCHLORIDE

Composition:

TIZANIDINE 2 mg

Administration route:

ORAL

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

Tizanidine tablet is a short-acting drug for the management of spasticity. Because of the short duration of effect, treatment with tizanidine should be reserved for those daily activities and times when relief of spasticity is most important (see DOSAGE AND ADMINISTRATION). Concomitant use of tizanidine with fluvoxamine or with ciprofloxacin, potent inhibitors of CYP1A2, is contraindicated. Significant alterations of pharmacokinetic parameters of tizanidine including increased AUC, t1/2, C max , increased oral bioavailability and decreased plasma clearance have been observed with concomitant administration of either fluvoxamine or ciprofloxacin. This pharmacokinetic interaction can result in potentially serious adverse events (See WARNINGS and CLINICAL PHARMACOLOGY: Drug Interactions). Tizanidine tablets is contraindicated in patients with known hypersensitivity to Tizanidine tablets or its ingredients. Abuse potential was not evaluated in human studies. Rats were able to distinguish tizanidine fr

Product summary:

Tizanidine tablets USP are available as white to off-white, round, flat, beveledged uncoated tablets containing 2 mg or 4 mg of tizanidine.Tizanidine tablets USP 2 mg are debossed with "U" and "168" on one side and bisecting score on other side. NDC 60760-782-04 BOTTLES OF 4 60760-782-15 BOTTLES OF 15 60760-782-30 BOTTLES OF 30 60760-782-90 BOTTLES OF 90 Dispense in tight, light-resistant container [see USP]. Rx Only

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

TIZANIDINE- TIZANIDINE TABLET
ST. MARY'S MEDICAL PARK PHARMACY
----------
TIZANIDINE TABLETS USP
PHARMACOKINETIC DIFFERENCES BETWEEN TIZANIDINE CAPSULES AND
TIZANIDINE TABLETS:
TIZANIDINE CAPSULES ARE NOT BIOEQUIVALENT TO TIZANIDINE TABLETS IN
THE FED STATE. THE PRESCRIBER SHOULD BE THOROUGHLY FAMILIAR WITH
THE COMPLEX EFFECTS OF FOOD ON TIZANIDINE PHARMACOKINETICS (SEE
PHARMACOKINETICS AND DOSAGE AND ADMINISTRATION).
DESCRIPTION
Tizanidine hydrochloride is a centrally acting α
-adrenergic agonist. Tizanidine HCl
(tizanidine) 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 and 4 mg tablets for oral
administration.
Tizanidine tablets USP are composed of the active ingredient,
tizanidine hydrochloride
USP (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, stearic acid,
microcrystalline cellulose and anhydrous lactose.
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,
2
9
8
5
2
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 similar