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Cilostazol information from DrugsUpdate  

See Available Brands of Cilostazol in India

P - Caution when used during pregnancy
L - Caution when used during lactation

Cilostazol is a medication used in the alleviation of the symptom of intermittent claudication in individuals with peripheral vascular disease. It is manufactured by Otsuka Pharmaceutical Co. under the trade name Pletal. Although drugs similar to cilostazol have increased the risk of death in patients with congestive heart failure, studies of significant size have not addressed people without the disease.

Cilostazol is a selective PDE3 phosphodiesterase inhibitor with therapeutic focus on cAMP. It inhibits platelet aggregation and is a direct arterial vasodilator. Its main effects are dilation of the arteries supplying blood to the legs and decreasing platelet coagulation.

Pharmacodynamics

Pharmacokinetics

Cilostazol is a reversible, selective inhibitor of phosphodiesterase-III (PDE-III), thereby suppressing cyclic adenosine monophosphate (cAMP) degradation. Increase in cAMP in platelets and blood vessels leads to inhibition of platelet aggregation and vasodilation. Cilostazol also inhibits adenosine uptake into cells, which augments the cAMP-elevating effect of PDE-III inhibition.


Absorption
Absorbed from the GI tract after oral admin.

Distribution
95-98% bound to plasma proteins.

Metabolism
Extensively metabolised hepatically by CYP450 isoenzymes, mainly CYP3A4.


Excretion
Mainly excreted in the urine, remainder excreted in the faeces.

Cilostazol Indications / Cilostazol Uses

Information Not Available

Cilostazol Adverse Reactions / Cilostazol Side Effects

Headache, dizziness, palpitations, diarrhoea, abnormal stools; pain, infection; peripheral oedema, nausea, vomiting, other cardiac arrhythmias, chest pain, rhinitis, pharyngitis, ecchymosis and skin rash.

Precautions

Warnings
Contraindicated for use in CHF patients of any severity. Cilostazol and metabolites are inhibitors of phosphodiesterase III. Such activity has been shown to decrease survival of patients with class III to IV CHF.

Monitor
Monitor patient for signs and symptoms of bleeding, especially those concurrently on other anticoagulants. Assess patient for adverse cardiac signs and symptoms and for signs of CHF.

Renal Function
Use with caution in patients with severe renal function impairment (Ccr less than 25 mL/minute).

Hepatic Function
Use with caution.

Hematologic toxicity
Thrombocytopenia or leukopenia progressing to agranulocytosis has been reported; however, agranulocytosis was reversible on immediate discontinuation of cilostazol.

Overdosage
Symptoms
Cardiac arrhythmias, diarrhea, hypotension, severe headache, tachycardia.

Special Precautions

Congestive heart disease. Concurrent therapy with clopidogrel has not been studied for safety or efficacy. Pregnancy and lactation.

Other Drug Interactions

Co-admin with drugs that affect CYP3A4 (erythromycin, other macrolides, diltiazem) or CYP2C19 (omeprazole) may influence the pharmacokinetics of cilostazol.

Other Interactions

Information Not Available

Dosage

Oral Peripheral vascular disease Adult: 100 mg bid. May reduce dose in patients taking enzyme inhibitors concurrently.

Food(before/after)

Should be taken on an empty stomach. (Take at least ½ an hour before or 2 hours after meals.)

List of Contraindications

Cilostazol and Pregnancy

Caution when used during pregnancy.


Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.

Cilostazol and Lactation

Caution when used during lactation

Cilostazol and Children

The safety and effectiveness of Cilostazol in pediatric patients have not been established

Cilostazol and Geriatic

Of the total number of subjects (n=2274) in clinical studies of Cilostazol, 56 percent were 65-years-old and over, while 16 percent were 75-years-old and over. No overall differences in safety or effectiveness were observed between these subjects and younger subjects and other reported clinical experience has not identified differences in responses between the elderly and younger patients, but greater sensitivity of some older individuals cannot be ruled out. Pharmacokinetic studies have not disclosed any age-related effects on the absorption, distribution, metabolism and elimination of Cilostazol and its metabolites.

Cilostazol and Other Contraindications

Heart failure; known predisposition to bleeding; history of ventricular arrhythmias; QT interval prolongation; severe renal impairment; moderate to severe hepatic impairment.

Storage

Oral
Store at 25°C.

Lab interference

Oral
Store at 25°C.

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