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Active ingredient: Cilostazol - Brands, Medical Use, Clinical Data

Brands, Medical Use, Clinical Data

Drug Category

  • Neuroprotective Agents
  • Vasodilator Agents
  • Fibrinolytic Agents
  • Bronchodilator Agents

Dosage Forms

  • Not Available

Brands / Synonyms

Cilostazol; Cilostazol [Inn:Jan]; Cilostazole; Cilostazolum [Inn-Latin]; Pletaal; Pletal; Pletal

Indications

For the reduction of symptoms of intermittent claudication (pain in the legs that occurs with walking and disappears with rest)

Pharmacology

Cilostazol 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.

Mechanism of Action

The mechanism of the effects of Cilostazol on the symptoms of intermittent claudication is not fully understood. Cilostazol 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.

Absorption

Not Available

Toxicity

Not Available

Biotrnasformation / Drug Metabolism

Hepatic

Contraindications

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.

Drug Interactions

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.

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