Cilostan CR

Cilostan CR

cilostazol

Manufacturer:

Korea United Pharma

Distributor:

Pharma 3
Full Prescribing Info
Contents
Cilostazol.
Description
Each controlled released tablet contains 200 mg cilostazol.
Action
Pharmacology: In subjects with severe renal impairment, the free fraction of Cilostazol was 27% higher and both Cmax and AUC were 29% and 39% lower respectively than in subjects with normal renal function. The Cmax and AUC of the dehydro metabolite were 41% and 47% lower respectively in the severely renally impaired subjects compared to subjects with normal renal function. The Cmax and AUC of 4'-trans-hydroxy cilostazol were 173% and 209% greater in subjects with severe renal impairment. The drug should not be administered to patients with a creatinine clearance <25 mL/min.
In repeated oral administration study with beagle for 13 weeks and 52 weeks, hypertrophic endocardium and coronary arteriography disorder occurred in high dosage. Non- toxic dose is 30 mg/kg/day, 12 mg/kg/day. This change was observed only in dogs and not in rat and monkey. And inhibitor of PDE III and vasodilator have occur same situation.
Indications/Uses
Cilostazol (Cilostan CR) is indicated for the improvement of the maximal and pain-free walking distances in patient with intermittent claudication, who do not have the rest pain and who do not have the evidence of peripheral tissue necrosis (peripheral arterial disease Fontaine stage II). It is for second-line use, in patient whom lifestyle modifications [including stopping smoking and (supervised) exercise programmes] and other appropriate interventions have failed to sufficiently improve their intermittent claudication symptoms.
Dosage/Direction for Use
The recommended dose is 200 mg daily, taken as one dose (every 24 hours).
It should be taken at least 30 minutes before or 2 hours after food.
Overdosage
Information on acute overdose with Cilostazol in humans is limited. The signs and symptoms of an acute overdose can be anticipated to be those of 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 >5.0 g/kg in mice and rats and >2.0 g/kg in dogs.
Contraindications
Patients with any known predisposition to bleeding (e.g. active peptic ulceration, recent (within six months) haemorrhagic stroke, proliferative diabetic retinopathy, poorly controlled hypertension).
Patients with a congestive heart failure.
Patients who have shown hypersensitivity to this product or any of its components.
Pregnant women or women of childbearing potential.
Special Precautions
Patients who are using anticoagulant such as warfarin; platelet aggregation inhibitor including aspirin, ticlopidine, etc.; and thrombolytic including urokinase and alteplase since it may cause bleeding.
Patients who are using prostaglandin E1 or derivative (alprostadile, rimaprodex, alphadex, etc) since bleeding may also occur.
Patients with menstruation.
Severe renal impairment: creatinine clearance of ≤25 mL/min.
Moderate or severe hepatic impairment.
Patients with any known predisposition to bleeding (e.g. active peptic ulceration, recent (within six months) haemorrhagic stroke, proliferative diabetic retinopathy, poorly controlled hypertension).
Patients with any history of ventricular tachycardia, ventricular fibrillation or multifocal ventricular ectopics, whether or not adequately treated, and in patients with prolongation of the QTc interval.
General: Cilostazol (Cilostan CR) may cause dizziness and patients should be warned to exercise caution before they drive or operate machinery.
Taking cilostazol with food has been shown to increase the maximum plasma concentrations (Cmax) of cilostazol, which may be associated with an increased incidence of adverse effects. Cilostazol is an inhibitor of PDE III. It has been reported that in long term administration, comparative experiment of congestive heart failure patient (NYHA class III-IV), survival rate of cardiotonic inhibiting PDE III is lower than placebo as for cardiotonic inhibiting PDE III. Patients should be warned to report any episode of bleeding or easy bruising whilst on therapy. In case of retinal bleeding administration of cilostazol should be stopped.
In addition to reporting episodes of bleeding and easy bruising, patients should be warned to promptly report any other signs which might also suggest the early development of blood dyscrasia such as pyrexia and sore throat. A full blood count should be performed if infection is suspected or there is any other clinical evidence of blood dyscrasia. Cilostazol should be discontinued promptly if there is clinical or laboratory evidence of haematological abnormalities.
Use in Elderly: Particular care should be taken in the elderly since usually their physiologic function may be lowered.
Use in Children: Safety and efficacy in children have not been established.
Use In Pregnancy & Lactation
In animal (rat) studies, low birth weight infant and death have been reported therefore, Cilostazol should not be used in pregnant women or women of childbearing potential.
Transfer of Cilostazol into milk has been reported in experimental animals (rats). Because of the potential risk to nursing infants, a decision should be made to discontinue nursing or to discontinue Cilostazol intake.
Adverse Reactions
Serious Adverse Effects: Encephalorrhagia, pneumorrhagia, fundus bleeding, occasionally, suffusion, or rarely enteral bleeding, nasal hemorrhage, hematuria may occur. If they occur, the administration should be discontinued and appropriate treatment must be done.
Pancytopenia, agranulocytosis, rarely thrombocytopenia may occur. If they occur, the administration should be discontinued and appropriate treatment must be done.
Interstitial pneumonia, accompanied with flush, cough, dyspnea, disorder of chest, eosinophilia may occur. If these symptoms occur, the administration should be discontinued and appropriate treatment must be done including adrenocortical hormone therapy.
Congestive heart failure, cardiac infarction, angina pectoris, ventricular tachycardia, etc. have been reported. If they occur, the administration should be discontinued and/or appropriate therapy instituted.
Occasionally, elevations of AST, ALT, ALP, LDH and icterus may occur, patients should be observed sufficiently. If any symptoms occur, the administration should be discontinued or reduced.
Others: Hypersensitivity: Occasionally eruption, or rarely epidermatomycosis, urticaria, itch, photosensitivity reaction may occur. If they occur, the administration should be discontinued.
Cardiovascular: Arrhythmia such as arterial fibrillation, ventricular tachycardia, premature ventricular contraction, decline blood pressure, occasionally, frequent pulse, ardor, and rarely blood pressure increase may occur. If they occur, dose reduction or discontinuation can be considered.
CNS: Tremors, occasionally headache, dizziness, or rarely, insomnia, drowsiness may occur. If they occur, the administration should be taken such as dose reduction or discontinuation.
Gastrointestinal: Abdominal pain, nausea, vomiting, anorexia, diarrhea may occur occasionally, or brash, abdominal inflation may occur rarely.
Kidney: Increases of BUN, creatinine, uratic value may occur rarely.
Hemic and Lymphatic: Anemia, ecchymosis, iron deficiency anemia, polycythemia, purpura.
Metabolic and Nutritional: Increased creatinine, gout, hyperlipemia, hyperuricemia.
Musculoskeletal: Arthralgia, bone pain, bursitis.
Nervous: Anxiety, insomnia, neuralgia.
Endocrine: Diabetes mellitus.
Respiratory: Asthma, epistaxis, hemoptysis, pneumonia, sinusitis.
Skin and Appendages: Dry skin, furunculosis, skin hypertrophy, urticaria.
Special Senses: Amblyopia, blindness, conjunctivitis, diplopia, ear pain, eye haemorrhage, retinal haemorrhage, tinnitus.
Urogenital: Albuminuria, cystitis, urinary frequency, vaginal haemorrhage, vaginitis.
Other: Pyrexia, occasionally, sweating, edema or rarely, increment blood sugar, chest pain, tinnitus, dolorific, malaise, conjunctivitis, urinary frequency may occur.
Drug Interactions
Cilostazol is extensively metabolised by CYP enzymes, particularly CYP3A4 and CYP2C19. Concomitant administration with anticoagulant drugs such as warfarin; platelet aggregation inhibitors like aspirin, ticlopidine etc.; and thrombolytics including urokinase and alteplase may cause bleeding.
Concomitant intake with prostaglandin E1 or derivative (alprostadile, rimaprodex, alphadex, etc.). May also cause bleeding.
In patients receiving Cilostazol and inhibitors of CYP3A4 (erythromycin, cimetidine, grape fruit juice) concomitantly, increase in blood levels of these drugs may be observed. In these cases, the administration should be reduced or started at lower dosage.
In patients receiving Cilostazol and organic of CYP3A4 (diltiazem) concomitantly, increase in blood levels of these drugs may be observed. If used concomitantly, the administration should be reduced or started at lower dosage.
In patients receiving Cilostazol and inhibitors of CYP3A4 (omeprazole, etc.) concomitantly, blood levels of these drugs may be increased. If used concomitantly, the administration should be reduced or started at lower dosage.
Storage
Store at temperatures not exceeding 30°C.
ATC Classification
B01AC23 - cilostazol ; Belongs to the class of platelet aggregation inhibitors excluding heparin. Used in the treatment of thrombosis.
Presentation/Packing
CR tab 200 mg (white, oblong, engraved with "UT" on one side and "C200" on the other side) x 30's.
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