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Product
Anti-asthmatic Products (Aerocort Inhaler)
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Pletoz (Cilostazol Tablets)
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Aerocort Inhaler
Cilostazol Tablets
COMPOSITION
Pletoz- 50 , 100
•Each tablet contains cilostazol …… 50,100 mg
PHARMACOLOGY
Pharmacodynamics
» Cilostazol and several of its metabolites are cyclic AMP (cAMP),…… phosphodiesterase III inhibitors ( PDE III inhibitors )
» With a resultant increase in cAMP in platelets and blood vessels, leading to inhibition of platelet aggregation, vasodilation and vascular antiproliferative responses in vivo respectively.
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≈ In humans, heart rate increased in a dose-proportional manner by a mean of 5.1 and 7.4 beats per minute in patients treated with 50 and 100 mg b.i.d., respectively.
≈ In 264 cilostazol-treated patients had increases in ventricular premature beats and non-sustained ventricular tachycardia events than did placebo-treated patients; the increases were not dose-related.
≈ In 264 cilostazol-treated patients had increases in ventricular premature beats and non-sustained ventricular tachycardia events than did placebo-treated patients; the increases were not dose-related.
≈ Peak plasma conc: in 3 – 4 hours.
Pharmacokinetics
Absorption & distribution
» Cilostazol is absorbed after oral administration.
» A high fat meal increases absorption, with an approximately 90% increase in C max and a 25% increase in AUC.
» Cilostazol is extensively metabolized by hepatic cytochrome P-450 enzymes, with metabolites largely excreted in urine.
» Pharmacokinetics are approximately dose proportional .
Indications
˜ Cilostazol is indicated for the reduction of symptoms of intermittent claudication.
Dosage & Administration
• The recommended dosage of cilostazol is 100 mg b.i.d. taken at least half an hour before or two hours after breakfast and dinner.
• A dose of 50 mg b.i.d. should be considered during coadministration of such inhibitors of CYP3A4 as ketoconazole, itraconazole, erythromycin and diltiazem, and during coadministration of such inhibitors of CYP2C19 as omeprazole.
• Patients may respond as early as 2 to 4 weeks after the initiation of therapy, but treatment for up to 12 weeks may be needed before a beneficial effect is experienced.
Renal impairment
◊ Special caution should be advised when cilostazol is used in patients with severe renal impairment: estimated creatinine clearance <25 ml/minute.
Hepatic impairment
θ Patients with moderate or severe hepatic impairment have not been studied in clinical trials.
θ Special caution should be advised when cilostazol is used in patients with severe hepatic impairment.
Pregnancy
€ There are no adequate and well-controlled studies in pregnant women.
€ Thus, there is a chance of fetal harm if drug is administered during pregnancy, but the potential benefits may outweigh the potential risk.
Lactation
Ø Because of the potential risk to nursing infants, a decision should be made to discontinue nursing or to discontinue cilostazol.
Pediatric use
Ø The safety and effectiveness of cilostazol in paediatric patients have not been established.
Geriatric Use
Ø 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.
Overdosage
◊ Information on acute overdosage with cilostazol in humans is limited.
◊ The signs and symptoms of an acute overdose ……….severe headache, diarrhoea, hypotension, tachycardia, and possibly cardiac arrhythmias.
◊ The patient should be carefully observed and given supportive treatment.
◊ Since cilostazol is highly protein-bound, it can be efficiently removed by hemodialysis or peritoneal dialysis.
Presentaion
1 strip……….10 tablets
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