Pletaal - General Information:Pletaal 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. [Wikipedia]
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Pharmacology:Pletaal is a quinolinone derivative indicated for the reduction of symptoms of intermittent claudication, as indicated by an increased walking distance. Intermittent claudication is pain in the legs that occurs with walking and disappears with rest. The pain occurs due to reduced blood flow to the legs.
Pletaal for patients
Since PLETAL is extensively metabolized by cytochrome P-450 isoenzymes, caution should be exercised when PLETAL is coadministered with inhibitors of C.P.A. such as ketoconazole and erythromycin or inhibitors of CYP2C19 such as omeprazole. Pharmacokinetic studies have demonstrated that omeprazole and erythromycin significantly increased the systemic exposure of cilostazol and/or its major metabolites. Population pharmacokinetic studies showed higher concentrations of cilostazol among patients concurrently treated with diltiazem, an inhibitor of C.P.A.. Pletal does not, however, appear to cause increased blood levels of drugs metabolized by CYP3A4, as it had no effect on lovastatin, a drug with metabolism very sensitive to C.P.A. inhibition.
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 congestive heart failure. PLETAL is contraindicated in patients with congestive heart failure of any severity.
PLETAL is contraindicated in patients with haemostatic disorders or active pathologic bleeding, such as bleeding peptic ulcer and intracranial bleeding. PLETAL inhibits platelet aggregation in a reversible manner.
PLETAL is contraindicated in patients with known or suspected hypersensitivity to any of its components.
Additional information about PletaalPletaal Indication: For the reduction of symptoms of intermittent claudication (pain in the legs that occurs with walking and disappears with rest).
Mechanism Of Action: The mechanism of the effects of cilostazol on the symptoms of intermittent claudication is not fully understood. Pletaal and several of its metabolites are cyclic AMP (cAMP) phosphodiesterase III inhibitors (PDE III inhibitors), inhibiting phosphodiesterase activity and suppressing cAMP degradation with a resultant increase in cAMP in platelets and blood vessels, leading to inhibition of platelet aggregation and vasodilation.
Drug Interactions: Diltiazem Diltiazem increases the effect of cilostazol
Erythromycin Erythromycin increases the effect of cilostazol
Josamycin Erythromycin increases the effect of cilostazol
Fluconazole Fluconazole decreases the effect of cilostazol
Fluoxetine Fluoxetine increases the effect of cilostazol
Fluvoxamine Fluvoxamine increases the effect of cilostazol
Itraconazole The imidazole increases the effect of cilostazol
Ketoconazole The imidazole increases the effect of cilostazol
Nefazodone Nefazodone increases the effect of cilostazol
Omeprazole Omeprazole increases the effect of cilostazol
Sertraline Sertraline increases the effect of cilostazol
Food Interactions: Take on an empty stomach, a lipid rich meal will increase absorption.
Grapefruit and grapefruit juice should be avoided throughout treatment, grapefruit can significantly increase serum levels of this product.
Generic Name: Cilostazol
Synonyms: Cilostazolum [Inn-Latin]; Cilostazole
Drug Category: Neuroprotective Agents; Vasodilator Agents; Fibrinolytic Agents; Bronchodilator Agents
Drug Type: Small Molecule; Approved
Other Brand Names containing Cilostazol: Pletaal; Pletal;
Absorption: Cilostazol is absorbed after oral administration. A high fat meal increases absorption, with an approximately 90% increase in Cmax and a 25% increase in AUC. Absolute bioavailability is not known.
Toxicity (Overdose): Information on acute overdosage 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 oral LD50 of cilostazol is >5.0 g/kg in mice and rats and >2.0 g/kg in dogs.
Protein Binding: 95-98%
Biotransformation: Hepatic. Cilostazol is extensively metabolized by hepatic cytochrome P-450 enzymes, mainly 3A4, and, to a lesser extent, 2C19, with metabolites largely excreted in urine. Two metabolites are active, with one metabolite appearing to account for at least 50% of the pharmacologic (PDE III inhibition) activity after administration of cilostazol.
Half Life: 11-13 hours.
Dosage Forms of Pletaal: Tablet Oral
Chemical IUPAC Name: 6-[4-(1-cyclohexyltetrazol-5-yl)butoxy]-3,4-dihydro-1H-quinolin-2-one
Chemical Formula: C20H27N5O2
Cilostazol on Wikipedia: http://en.wikipedia.org/wiki/Cilostazol
Organisms Affected: Humans and other mammals
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