Cilostazol

Table of contents

  • Brand Names
  • Drug Combinations
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Unlabeled Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Toxicological Effects
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Substrate of
  • Inhibits
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

France: Pletal; Germany: Pletal; Ireland: Pletal; Italy: Pletal; Spain: Ekistol, Pletal; Sweden: Pletal; UK: Pletal.

North America

USA: Cilostazol, Pletal.

Latin America

Argentina: Aclusin, Cibrogan, Cilaal, Cilostal, Cilovas, Licuagen, Pletaal, Policor, Trastocir, Trombonot, Zolplat; Brazil: Cebralat, Vasogard; Mexico: Caudaline.

Asia

Japan: Aitant, Cilosinamin, Ciloslet, Cilosmerck, Cilostate, Ecbarl, Ejennu, Fantezole, Flenied, Gront, Hordazol, Kortrythm, Opetarl, Platemeel, Plestazol, Pletaal, Pletmol, Prelazine, Ranomin, Rotazona.

Drug combinations

Cilostazol and Aspirin

Chemistry

Cilostazol: C~20~H~27~N~5~O~2~. Mw: 369.46. (1) 2(1H)-Quinolinone, 6-[4-(1-cyclohexyl-1H-tetrazol-5-yl)butoxy]-3,4-dihydro-; (2) 6-[4-(1-Cyclohexyl-1H-tetrazol-5-yl)butoxy]-3,4-dihydrocarbostyril. CAS-73963-72-1 (1997).

Pharmacologic Category

Antithrombotic Agents; Platelet-aggregation Inhibitors. Phosphodiesterase Enzyme Inhibitor. (ATC-Code: B01AC23).

Mechanism of action

Appears to inhibit activation of cellular phosphodiesterase type 3, resulting in suppressed degradation and increased concentrations of adenosine 3′,5′-cyclic monophosphate (cAMP) in platelets and blood vessels. Increased cAMP levels appear to mediate arterial vasodilation and inhibition of platelet aggregation. Reduces plasma triglycerides and increases high-density lipoprotein cholesterol concentrations.

Therapeutic use

Symptomatic management of peripheral vascular disease, primarily intermittent claudication.

Pregnancy and lactiation implications

In animal studies, abnormalities of the skeletal, renal and cardiovascular system were increased. Additionally, the incidence of stillbirth and decreased birth weights were increased. Use not recommended during lactation.

Unlabeled use

Adjunct with aspirin and clopidogrel for prevention of stent thrombosis and restenosis after coronary stent placement. Acute coronary syndromes and graft patency improvement in percutaneous coronary interventions with or without stenting.

Contraindications

Hypersensitivity to cilostazol or any component of the formulation. Heart failure. Hemostatic disorders or active bleeding.

Warnings and precautions

Discontinue therapy if leukopenia/thrombocytopenia occurs. Use with caution in underlying heart disease. Use with caution in moderate-to-severe hepatic impairment. Use with caution in severe renal impairment (CrCl <25 mL/minute). Use with caution in patients receiving other platelet aggregation inhibitors. Possible CYP-mediated interactions (use with caution in patients taking strong CYP3A4 inhibitors, moderate or strong CYP3A4 inducers and major CYP3A4 substrates). Withhold for at least 4-6 half-lives prior to elective surgical procedures.

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