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| Clinical data | |
|---|---|
| Pronunciation | /sɪˈlɒstəzɒl/ sil-OS-tə-zol |
| Trade names | Pletal |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a601038 |
| License data | |
| Routes of administration | By mouth (tablets) |
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| Pharmacokinetic data | |
| Protein binding | 95–98% |
| Metabolism | Liver (CYP3A4- andCYP2C19-mediated) |
| Eliminationhalf-life | 11–13 hours |
| Excretion | Kidney |
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| IUPHAR/BPS | |
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| CompTox Dashboard(EPA) | |
| ECHA InfoCard | 100.215.897 |
| Chemical and physical data | |
| Formula | C20H27N5O2 |
| Molar mass | 369.469 g·mol−1 |
| 3D model (JSmol) | |
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Cilostazol, sold under the brand namePletal among others, is amedication used to help the symptoms ofintermittent claudication inperipheral vascular disease.[1] It may also be used to preventstroke.[1] It is taken by mouth.[1]
Common side effects include headache, diarrhea, dizziness, and cough.[1] Serious side effects may include decreased survival in those withheart failure,low platelets, andlow white blood cells.[1] Cilostazol is aphosphodiesterase 3 inhibitor which works byinhibiting platelet aggregation and dilating arteries.[1]
Cilostazol was approved for medical use in the United States in 1999.[1] It is available as ageneric medication.[2] In 2019, it was the 347th most commonly prescribed medication in the United States, with more than 800 thousand prescriptions.[3]
Cilostazol is approved for the treatment of intermittent claudication in the United States and United Kingdom.[1][4] If no improvement is seen after 3 months, stopping the medication is reasonable.[2]
Cilostazol is also used for secondary stroke prevention,[1] though to date no regulatory body has approved it specifically for that indication.
Cilostazol is dangerous for people with severe heart failure. Cilostazol has been studied in people without heart failure, without evidence of harm, but much more data would be needed to determine no risk exists. Although cilostazol would not be approvable for a trivial condition the Cardio-Renal Advisory Committee and FDA concluded that fully informed patients and physicians should be able to choose to use it to treat intermittent claudication. Patient and physician labeling will describe the basis for concern and the incomplete information available.[5]
Possible side effects of cilostazol use includeheadache (the most common),diarrhea, severeheat intolerance, abnormalstools,increased heart rate, andpalpitations.[6]
Cilostazol is metabolized byCYP3A4 andCYP2C19, twoisoenzymes of thecytochrome P450 system. Drugs thatinhibit CYP3A4, such asitraconazole,erythromycin,ketoconazole, anddiltiazem, are known tointeract with cilostazol. Theproton pump inhibitoromeprazole, an inhibitor of CYP2C19, increases exposure to the activemetabolite of cilostazol.[6][7]
A single report has been made ofgrapefruit juice possibly increasing the effects of cilostazol;[8] some drug information sources list this as a possible interaction.[9][10][11] The FDA-approved labeling of cilostazol notes that grapefruit juice (which is a CYP3A4 inhibitor) increases the drug'smaximum concentration by around 50%.[6]
Cilostazol is a selective inhibitor of phosphodiesterase type 3 (PDE3) with therapeutic focus on increasing cAMP. An increase in cAMP results in an increase in the active form ofprotein kinase A (PKA), which is directly related with an inhibition in platelet aggregation. PKA also prevents the activation of an enzyme (myosin light-chain kinase) that is important in the contraction of smooth muscle cells, thereby exerting its vasodilatory effect.
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