- Molecular NameCilostazol
- SynonymCilostazole; Cilostazolum [INN-Latin]
- Weight369.469
- Drugbank_IDDB01166
- ACS_NO73963-72-1
- Show 3D model
- LogP (experiment)2.686
- LogP (predicted, AB/LogP v2.0)3.15
- pkaN/A
- LogD (pH=7, predicted)3.15
- Solubility (experiment)N/A
- LogS (predicted, ACD/Labs)(ph=7)-4.86
- LogSw (predicted, AB/LogsW2.0)0.21
- Sw (mg/ml) (predicted, ACD/Labs)0.01
- No.of HBond Donors1
- No.of HBond Acceptors7
- No.of Rotatable Bonds7
- TPSA81.93
- StatusFDA approved
- AdministrationN/A
- PharmacologyA medication used in the alleviation of the symptom of intermittent claudication in individuals with peripheral vascular disease.
- Absorption_valueN/A
- Absorption (description)Cilostazol is absorbed at a moderate rate after oral administration. Absorption is increased if the drug is administered with a high fat meal.
- Caco_2N/A
- BioavailabilityN/A
- Protein binding96.5
- Volume of distribution (VD)2.76 L/kg
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmHepatic (CYP3A4- and CYP2C19-mediated). The drug is extensively metabolised by hepatic cytochrome P450 enzymes (mainly 3A4). A number of metabolites are produced, two of which are active; 3,4-dehydrocilostazol (the most active metabolite accounting for at least 50% of the pharmacological activity) and 4′-trans-hydroxycilostazol.
- Half life11~13 h
- ExcretionIn plasma, 56% of the dose is detected as the unchanged drug, 15% 3,4-dehydrocilostazol and 4% 4′-trans-hydroxycilostazol. The primary elimination route is urine with 74% of the dose excreted in this way; <2% as the 3,4-dehydrocilostazol metabolite and 30% 4′-trans-hydroxycilostazol. No unchanged drug is detected in urine. It is extensively distributed in tissues.
- Urinary ExcretionN/A
- CleranceOral, 0.18 L/h/kg. Relatively low plasma clearance.
- ToxicityN/A
- LD50 (rat)N/A
- LD50 (mouse)N/A