CILOSTAZOL- cilostazol tablet

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

cilostazol (UNII: N7Z035406B) (cilostazol - UNII:N7Z035406B)

Available from:

Cardinal Health

INN (International Name):

cilostazol

Composition:

cilostazol 100 mg

Administration route:

ORAL

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

Cilostazol is 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 is contraindicated in patients with haemostatic disorders or active pathologic bleeding, such as bleeding peptic ulcer and intracranial bleeding. Cilostazol inhibits platelet aggregation in a reversible manner. Cilostazol is contraindicated in patients with known or suspected hypersensitivity to any of its components.

Product summary:

Cilostazol Tablets, USP 50 mg are white, round, flat-faced, bevelled-edge tablets, engraved "APO" on one side and "CIL" over "50" on the other side. They are supplied as follows: Bottles of 30 NDC 60505-2521-3 Bottles of 60 NDC 60505-2521-1 Bottles of 1000 NDC 60505-2521-8 Cilostazol Tablets, USP 100 mg tablets are white, round, flat-faced, bevelled-edge tablets, engraved "APO" on one side and "CIL" over "100" on the other side. They are supplied as follows: Bottles of 30 NDC 60505-2522-3 Bottles of 60 NDC 60505-2522-1 Bottles of 1000 NDC 60505-2522-8

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

CILOSTAZOL- CILOSTAZOL TABLET
CARDINAL HEALTH
---------- CILOSTAZOL TABLETS, USP
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 is a quinolinone derivative that inhibits cellular
phosphodiesterase (more specific for
phosphodiesterase III). The empirical formula of cilostazol is C
H N O , and its molecular weight
is 369.47. Cilostazol 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:
Cilostazol 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 for oral administration are available in 50 mg and
100 mg round, white tablets. Each
tablet, in addition to the active ingredient, contains the following
inactive ingredients: corn
starch, croscarmellose sodium, magnesium stearate, and silicon
dioxide.
Meets USP Dissolution Test 2
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
with a resultant increase in cAMP in platelets and blood vessels,
leading to inhibition of platelet
aggregation and vasodilation, respectively.
20
27
5
2
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 lipids
have been examined in patients taking cilostazol. After 12 weeks, as
com