Each tablet contains Cilostazol 50 mg or 100 mg.
Pletaxol (Cilostazol) is a quinoline derivative that inhibits cellular phosphodiesterase (more specific for phosphodiesterase III). The empirical formula of cilostazol is C20H27N5O2, and its molecular weight is 369.46. Cilostazol is 6[4[(1-cyclohexyl-1H-tetra- zol-5-yl)butoxy]-3,4-dihydro-2(1H)-quinolinone, CAS-73963-72-1.
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.
Pharmacology: Pharmacokinetics: Cilostazol is absorbed after oral doses and absorption is increased if taken with a high fat meal. Cilostazol is extensively metabolized in the liver by cytochrome P450 isoenzymes, mainly CYP3A4 and to a lesser extent CYP2C19, to both active and inactive metabolites; these are predominantly excreted in the urine (74%) with the remainder in the faeces (20%). The active metabolites have apparent elimination half-lives of 11 to 13 hours. Cilostazol is 95 to 98% protein bound.
It is used in the management of peripheral vascular disease; often used for atherosclerotic or occlusive arterial disease but in its widest sense covers both arterial and venous disorders and may be due to atherosclerosis, vasospasm, or thromboembolism.
50 mg Tablet: The usual dose is 50 mg twice daily, at least 30 minutes before meal or 2 hours after meal; doses should be reduced in patients taking enzyme inhibitors. Response to treatment may occur in 2 to 4 weeks, but up to 12 weeks may be required. Or as prescribed by the physician.
100 mg Tablet: The usual dose is 100 mg twice daily, at least 30 minutes before meal or 2 hours after meal; doses should be reduced in patients taking enzyme inhibitors. Response to treatment may occur in 2 to 4 weeks, but up to 12 weeks may be required. Or as prescribed by the physician.
Information on acute overdosage with Cilostazol in humans is limited. The signs and symptoms of an acute overdose can be anticipated to be those excessive pharmacologic effect: severe headache, diarrhea, hypotension, tachycardia, and possibly cardiac arrhythmias. The patient should be carefully observed and given supportive treatment. Since cilostazol is highly protein-bound, it is unlikely that it can be efficiently removed by hemodialysis or peritoneal dialysis. The oral LD50 of cilostazol is greater than 5 g per kg in mice and rats and greater than 2 g per kg in dogs.
Cilostazol is contraindicated in patients with congestive heart failure of any severity. It is also contraindicated in patients with a known predisposition to bleeding, a history of ventricular arrhythmias, QT interval prolongation, severe renal impairment, or moderate to severe hepatic impairment.
Cilostazol Tablet is contraindicated in patients with known or suspected hypersensitivity to any of its components.
Contraindicated in heart failure patients: PLETAXOL is contraindicated in patients with heart failure of any severity. 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 heart failure.
Cilostazol should be avoided or used in reduced doses in patients taking inhibitors of the cytochrome P450 isoenzymes CYP3A4 or CYP2C19.
Teratogenic Effects: Pregnancy Category C, Cilostazol has been shown to be teratogenic in rats at doses that are greater than 5-times the human MRHD on a body surface area basis. There are no adequate and well-controlled studies in pregnant women.
In a rat development toxicity study, oral administration of 1000 mg cilostazol/kg/day was associated with decreased fetal weight, and increased incidences of cardiovascular, renal, and skeletal anomalies (ventricular septal, aortic arch and subclavian artery abnormalities, renal pelvic delation, 14th rib, and retarded ossification). At this dose, systemic exposure to unbound cilostazol in nonpregnant rats was about 5 times exposure in humans given the MRHD. Increased incidences of ventricular septal defect and retarded ossification were also noted at 150 mg/kg/day (5 times the MRHD on a systemic exposure basis). In a rabbit developmental toxicity study, an increased incidence of retardation of ossification of the sternum was seen at doses as low as 150 mg/kg/day. In nonpregnant rabbits given 150 mg/kg/day, exposure to unbound cilostazol was considerably lower than that seen in humans given the MRHD, and exposure to 3,4-dehydro- cilostazol was barely detectable. When cilostazol was administered to rats during late pregnancy and lactation, an increased incidence of stillborn and decreased birth weights of offspring was seen at doses of 150 mg/kg/day (5 times the MRHD on a systemic exposure basis).
Adverse effects of Cilostazol include headache, dizziness, palpitations, and diarrhoea; oedema, nausea and vomiting, other cardiac arrhythmias, chest pain, rhinitis, ecchymosis, and skin rashes have also been reported. Cardiovascular toxicity has been reported in animal studies of Cilostazol, and prolonged oral use of other phosphodiesterase inhibitors for the treatment of heart failure has been associated with increased mortality.
Cilostazol is extensively metabolized to active and inactive metabolites by cytochrome P450 isoenzymes, mainly CYP3A4 and to a lesser extent CYP2C19. Therefore, use with other drugs that inhibit or are metabolized by these hepatic enzymes may result in changes in plasma concentrations of either drug and, possibly, adverse effects. Cilostazol should therefore be used with caution in patients taking drugs metabolised by these enzymes; in patients taking enzyme inhibitors it should be avoided or a reduced dose of 50 mg twice daily should be considered.
Store at temperatures not exceeding 30°C.
B01AC23 - cilostazol ; Belongs to the class of platelet aggregation inhibitors excluding heparin. Used in the treatment of thrombosis.
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