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QuickView for Cilostazol (compound)


PubChem
Name: cilostazol
PubChem Compound ID: 2754
Molecular formula: C20H27N5O2
Molecular weight: 369.461 g/mol
Synonyms:
EU-0100218; OPC 21; 6-(4-(1-Cyclohexyl-1H-tetrazol-5-yl)butoxy)-3,4-dihydro-2(1H)-quinolinone; Cilostazole; KBio3_002259; SPBio_001256; Pletal; 3,4-Dihydro-6-(4-(1-cyclohexyl-1H-tetrazol-5-yl)butoxy)-2(1H)-quinolinone; KBioGR_001184; 2(1H)-Quionlinone, 6-(4-(1-cyclohexyl-1H-tetrazol-5-yl)butoxy)-3,4-dihydro-.
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DrugBank
Identification
Name: cilostazol
Name (isomeric): DB01166
Drug Type: small molecule
Synonyms:
Cilostazolum [INN-Latin]; Cilostazole
Brand: Pletaal, Pletal
Category: Vasodilator Agents, Phosphodiesterase Inhibitors, Fibrinolytic Agents, Platelet Aggregation Inhibitors, Neuroprotective Agents, Bronchodilator Agents
CAS number: 73963-72-1
Pharmacology
Indication: 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: 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: 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.
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.
Route of elimination: Cilostazol is extensively metabolized by hepatic cytochrome P-450 enzymes, mainly 3A4, and, to a lesser extent, 2C19, with metabolites largely excreted in urine. Cilostazol is eliminated predominately by metabolism and subsequent urinary excretion of metabolites. The primary route of elimination was via the urine (74%), with the remainder excreted in feces (20%). No measurable amount of unchanged cilostazol was excreted in the urine, and less than 2% of the dose was excreted as 3,4-dehydro-cilostazol. About 30% of the dose was excreted in urine as 4'-trans-hydroxy-cilostazol.
Half Life: 11-13 hours.
Toxicity: 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.
Affected organisms: Humans and other mammals
Interactions
Food interaction:
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.
Drug interaction:
SertralineSertraline increases the effect of cilostazol
OmeprazoleOmeprazole increases the effect of cilostazol
TelithromycinTelithromycin may reduce clearance of Cilostazol. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Cilostazol if Telithromycin is initiated, discontinued or dose changed.
ItraconazoleItraconazole may increase the effect of cilostazol.
TreprostinilThe prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the antiplatelet agent, Cilostazol. Monitor for increased bleeding during concomitant thearpy.
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