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.
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.
Absorbed from the GI tract after oral admin.
95-98% bound to plasma proteins.
Extensively metabolised hepatically by CYP450 isoenzymes, mainly CYP3A4.
Mainly excreted in the urine, remainder excreted in the faeces.
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Headache, dizziness, palpitations, diarrhoea, abnormal stools; pain, infection; peripheral oedema, nausea, vomiting, other cardiac arrhythmias, chest pain, rhinitis, pharyngitis, ecchymosis and skin rash.
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 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.
Use with caution in patients with severe renal function impairment (Ccr less than 25 mL/minute).
Use with caution.
Thrombocytopenia or leukopenia progressing to agranulocytosis has been reported; however, agranulocytosis was reversible on immediate discontinuation of cilostazol.
Cardiac arrhythmias, diarrhea, hypotension, severe headache, tachycardia.
Congestive heart disease. Concurrent therapy with clopidogrel has not been studied for safety or efficacy. Pregnancy and lactation.
Co-admin with drugs that affect CYP3A4 (erythromycin, other macrolides, diltiazem) or CYP2C19 (omeprazole) may influence the pharmacokinetics of cilostazol.
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Oral Peripheral vascular disease Adult: 100 mg bid. May reduce dose in patients taking enzyme inhibitors concurrently.
Should be taken on an empty stomach. (Take at least ½ an hour before or 2 hours after meals.)
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.
Caution when used during lactation
The safety and effectiveness of Cilostazol in pediatric patients have not been established
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.
Heart failure; known predisposition to bleeding; history of ventricular arrhythmias; QT interval prolongation; severe renal impairment; moderate to severe hepatic impairment.
Store at 25°C.
Store at 25°C.