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Cilostazol

PLETAL

What it isPDE3 inhibitor with antiplatelet and vasodilator effects; intermittent claudication.

Why this oneIt is the only oral drug with consistent walking-distance benefit in claudication; pentoxifylline is ineffective.

What limits itContraindicated in heart failure of any severity — PDE3 inhibitors raised mortality. Headache is common; CYP3A4 and CYP2C19 dependent.

FDA-approved for

FDA label

BOXED WARNING Contraindicated in patients with heart failure of any severity — PDE III inhibitors have decreased survival in class III–IV heart failure.
FDA dosingPopulationStartTargetMax
Intermittent claudicationAdults100 mg BID100 mg BID100 mg BID
Intermittent claudication — with CYP3A4 or CYP2C19 inhibitorsAdults50 mg BID50 mg BID50 mg BID

Renal Undefined

Hepatic Undefined

Reduce to 50 mg BID with strong/moderate CYP3A4 inhibitors (ketoconazole, itraconazole, erythromycin, diltiazem) or CYP2C19 inhibitors (ticlopidine, fluconazole, omeprazole)

Instructions

Contraindications

Cautions

Adverse reactions

Pregnancy Category C; teratogenic/fetotoxic in animals — no adequate human studies

Lactation Transferred into milk in animals — discontinue nursing or the drug

⚠ BOXED WARNING

Cost, est. cash$4–$300/month

Generic entry2004

Classes and tags

Clinical profile

Therapeutic safety burden2 / 4
Overdose danger3 / 4
Weight-gain liability0 / 4
Sedation liability0 / 4
QT / Torsades3 / 4
Direct muscarinic antagonism0 / 4
Embryofetal risk2 / 4

Legacy pregnancy categoryB

Defining liabilityGI or intracranial bleeding, especially with anticoagulants, NSAIDs or serotonergic antidepressants.

Mechanism of action: Cilostazol ballicule

Cilostazol ballicule: receptor binding, kinetics and half-life diagram

Open Cilostazol in the interactive console ↗

Memory aids: mascots and interaction avatars

Cilostazol PLETAL mascot mnemonic cartoon
“Plates, all CeeLo style”
Plate-lets
Cilostazol CYP2C19 substrate avatar
CYP2C19 substrate
Cilostazol CYP3A4 substrate avatar
CYP3A4 substrate

Open Cilostazol in the interactive console ↗