Product Name

Cilostazol

CAS Number

73963-72-1

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Product Name:
Cilostazol
CAS Number:
73963-72-1
Indication:
For the reduction of symptoms of intermittent claudication (pain in the legs that occurs with walking and disappears with rest).
Mode 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.

Pharmacodynamics:

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.

Metabolism:

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.

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.

IUPAC:
6-[4-(1-cyclohexyl-1H-1, 2, 3, 4-tetrazol-5-yl)butoxy]-1, 2, 3, 4-tetrahydroquinolin-2-one
ATC:
B01AC23
PubChem:
2754
DrugBank:
DB01166 (APRD00155)
Formula:
C19H27ClO2
Molecular Mass:
369.4607
Synonyms:
Cilostazole Cilostazolum [INN-Latin]
SMILES:
O=C1CCC2=C(N1)C=CC(OCCCCC1=NN=NN1C1CCCCC1)=C2
InChi:
RRGUKTPIGVIEKM-UHFFFAOYSA-N

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