Pletal Indication:

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

Pletal Mechanism Of Action:

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

Pletal 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

Pletal 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.

Pletal Generic Name:

Synonyms:

  • Cilostazolum [Inn-Latin]
  • Cilostazole

Drug Type:

Small Molecule; Approved

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 Pletal:

Tablet Oral

Chemical IUPAC Name:

6-[4-(1-cyclohexyltetrazol-5-yl)butoxy]-3,4-dihydro-1H-quinolin-2-one

Organisms Affected:

Humans and other mammals

Pletal to general, pharmacology

General, pharmacology..
General health