CILOSTAZOL- cilostazol tablet

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

CILOSTAZOL (UNII: N7Z035406B) (CILOSTAZOL - UNII:N7Z035406B)

Available from:

NCS HealthCare of KY, Inc dba Vangard Labs

INN (International Name):

CILOSTAZOL

Composition:

CILOSTAZOL 100 mg

Administration route:

ORAL

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

Cilostazol tablets USP are indicated for the reduction of symptoms of intermittent claudication, as indicated by an increased walking distance. Cilostazol and several of its metabolites are inhibitors of phosphodiesterase III. Several drugs with this pharmacologic effect have caused decreased survival compared to placebo in patients with class III-IV congestive heart failure. Cilostazol is contraindicated in patients with congestive heart failure of any severity. Cilostazol tablets are contraindicated in patients with hemostatic disorders or active pathologic bleeding, such as bleeding peptic ulcer and intracranial bleeding. Cilostazol inhibits platelet aggregation in a reversible manner. Cilostazol tablets are contraindicated in patients with known or suspected hypersensitivity to any of their components.

Product summary:

Cilostazol tablets USP are available as follows: 50 mg - white to off-white, pillow-shaped tablets, debossed with “TEVA” on one side and “7230” on the other, available in blisterpacks of 30. 100 mg - white to off-white, round tablets, debossed with “TEVA” on one side and “7231” on the other, available in blisterpacks of 30.

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

CILOSTAZOL- CILOSTAZOL TABLET
NCS HEALTHCARE OF KY, INC DBA VANGARD LABS
----------
CILOSTAZOL TABLETS USP
RX ONLY
REV. K 6/2012
CONTRAINDICATION
Cilostazol and several of its metabolites are inhibitors of
phosphodiesterase III. Several drugs
with this pharmacologic effect have caused decreased survival compared
to placebo in patients
with class III-IV congestive heart failure. Cilostazol is
contraindicated in patients with congestive
heart failure of any severity.
DESCRIPTION
Cilostazol, USP is a quinolinone derivative that inhibits cellular
phosphodiesterase (more specific for
phosphodiesterase III). Cilostazol, USP is
6-[4-(1-cyclohexyl-1_H_-tetrazol-5-yl)butoxy]-3,4-dihydro-
2(1_H_)-quinolinone, CAS-73963-72-1.
The structural formula is:
C
H N O M. W. 369.46
Cilostazol, USP occurs as white to off-white crystals or as a
crystalline powder that is slightly soluble
in methanol and ethanol, and is practically insoluble in water, 0.1 N
HCl, and 0.1 N NaOH.
Cilostazol tablets USP for oral administration are available in 50 mg
pillow-shaped and 100 mg round,
white to off-white debossed tablets. Each tablet, in addition to the
active ingredient, contains the
following inactive ingredients: colloidal silicon dioxide,
crospovidone, magnesium stearate,
microcrystalline cellulose, povidone, and starch.
Meets USP Dissolution Test 3.
CLINICAL PHARMACOLOGY
MECHANISM OF ACTION
The mechanism of the effects of cilostazol on the symptoms of
intermittent claudication is not fully
understood. Cilostazol and several of its metabolites are cyclic AMP
(cAMP) phosphodiesterase III
inhibitors (PDE III inhibitors), inhibiting phosphodiesterase activity
and suppressing cAMP degradation
20
27
5
2
with a resultant increase in cAMP in platelets and blood vessels,
leading to inhibition of platelet
aggregation and vasodilation, respectively.
Cilostazol reversibly inhibits platelet aggregation induced by a
variety of stimuli, including thrombin,
ADP, collagen, arachidonic acid, epinephrine, and shear stress.
Effects on circulating plasma lipi