II. Indications

  1. Intermittent Claudication
    1. Adjunct while taking other antiplatelet medication (e.g. Aspirin, Clopidogrel)

III. Contraindications

  1. Congestive Heart Failure (increased mortality)
  2. Caution in severe hepatic insufficiency
  3. Caution in GFR <25 ml/min

IV. Mechanism

  1. Quinolinone derivative
  2. Inhibits phosphodiesterase 3 (PDE3) leading to higher levels of cAMP within Platelets and vessels
  3. Inhibits Platelet aggregation
  4. Also promotes vasodilation

V. Dosing

  1. Take 100 mg orally twice daily on an empty Stomach
  2. Indications for half dose (50 mg orally twice daily)
    1. Use of strong CYP3A4 Inhibitors (e.g. Itraconazole, Erythromycin)
    2. Use of strong CYP2C19 Inhibitors (e.g. Omeprazole)

VI. Adverse Effects

  1. Headache
  2. Palpitations
  3. Left Ventricular Outflow Obstruction
    1. Increased risk in patients with sigmoid shaped interventricular septum

VII. Safety

  1. Pregnancy Category C
  2. Unknown safety in Lactation

VIII. Drug Interactions

  1. CYP3A4 Inhibitors (e.g. Itraconazole, Erythromycin)
  2. CYP2C19 Inhibitors (e.g. Omeprazole)
  3. Grapefruit juice
    1. Increases Cilostazol levels

IX. Efficacy

  1. Full effect may be delayed for 12 weeks

XI. References

  1. Balinski (2023) Cilostazol, StatPearls, Treasure Island
    1. https://www.ncbi.nlm.nih.gov/books/NBK544363/
  2. Hamilton (2020) Tarascon Pocket Pharmacopoeia

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Related Studies

Cost: Medications

cilostazol (on 12/21/2022 at Medicaid.Gov Survey of pharmacy drug pricing)
CILOSTAZOL 100 MG TABLET Generic $0.13 each
CILOSTAZOL 50 MG TABLET Generic $0.11 each

Ontology: cilostazol (C0055729)

Definition (NCI) A quinolinone derivative and cellular phosphodiesterase inhibitor, more specific for phosphodiesterase III (PDE III). Although the exact mechanism of action of is unknown, cilostazol and its metabolites appears to inhibit PDE III activity, thereby suppressing cyclic adenosine monophosphate (cAMP) degradation. This results in an increase in cAMP in platelets and blood vessels, leading to inhibition of platelet aggregation and vasodilation.
Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH C045645
SnomedCT 395239000, 116087001
English 6-(4-(1-cyclohexyl-1H-tetrazol-5-yl)butoxy)-3,4-dihydro-2(1H)-quinolinone, cilostazol, 6-[4-(1-cyclohexyl-1H-tetrazol-5-yl)butoxy]-3,4-dihydro-2(1H)-quinolinone, cilostazol (medication), CILOSTAZOL, cilostazol [Chemical/Ingredient], Cilostazol (product), Cilostazol (substance), Cilostazol
Spanish cilostazol (producto), cilostazol (sustancia), cilostazol

Ontology: Pletal (C0722654)

Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH C045645
English Pletal, cilostazol (Pletal), pletal, Otsuka brand of cilostazol