Cilostazol
Regulatory sources consulted
- openfda-label-1547a408-12a9-fadd-e063-6394a90a4ce0
- aemps-cima-ft-78222
- PubMed PMID:38743805 ↗
- PubMed PMID:35094598 ↗
- PubMed PMID:37511955 ↗
- PubMed PMID:38420850 ↗
- PubMed PMID:34997200 ↗
- OpenFDA · B01AC23
- RxNorm rxcui 21107 ↗
Approved indications
- Reduction of symptoms of intermittent claudication, as demonstrated by an increased walking distance.
- Secondary prevention of non-cardioembolic ischemic stroke, especially in patients intolerant to aspirin or in Asian populations where benefit has been shown. · off-label
Contraindications
Absolute
- Heart failure of any severity.
- Hypersensitivity to cilostazol or any of its components.
- Severe renal impairment (creatinine clearance ≤ 25 ml/min).
- Severe hepatic impairment.
- Active bleeding (e.g., active peptic ulcer or intracranial hemorrhage).
Clinical warnings
- Boxed warning · CONTRAINDICATED IN HEART FAILURE PATIENTS: Cilostazol is contraindicated in patients with heart failure of any severity. Cilostazol and several of its metabolites are inhibitors of phosphodiesterase III. Several drugs with this pharmacologic effect have caused decreased survival compared to placebo in patients with class III-IV heart failure. — FDA
- Major warning · May induce tachycardia, palpitations, and/or hypotension. The increase in heart rate associated with cilostazol is approximately 5 to 7 bpm. — FDA
- Major warning · Cases of thrombocytopenia, leukopenia, agranulocytosis, aplastic anemia, and pancytopenia have been reported. Hematologic monitoring is recommended. — FDA
Drug interactions
- HighKetoconazoleJ02AB02
Mechanism: Strong inhibition of CYP3A4, significantly increasing cilostazol exposure.
Recommendation: Reduce cilostazol dose to 50 mg twice daily when co-administered with strong CYP3A4 inhibitors like ketoconazole.
FDA label
- ModerateOmeprazoleA02BC01
Mechanism: Inhibition of CYP2C19, increasing exposure to cilostazol's active metabolites.
Recommendation: Reduce cilostazol dose to 50 mg twice daily when co-administered with CYP2C19 inhibitors like omeprazole.
FDA label
Adverse events
Common (≥1%)
headache · diarrhea · abnormal stools · palpitations
Rare but serious
agranulocytosis · pancytopenia · aplastic anemia · hemorrhage (gastrointestinal, cerebral) · ventricular tachycardia
Pregnancy and lactation
FDA category: C
Teratogenic in rats at doses >5 times the maximum recommended human dose. There are no adequate studies in pregnant women. Use only if the potential benefit justifies the potential risk to the fetus.
Recent literature (PubMed)
Guía de práctica clínica actualizada que establece las recomendaciones para el manejo de la enfermedad arterial periférica (EAP). Cilostazol se recomienda para mejorar los síntomas y la distancia de caminata en pacientes con claudicación intermitente.
Revisión sobre el uso de antiagregantes en la prevención del ictus isquémico. Señala que cilostazol puede ofrecer beneficios adicionales sobre aspirina y clopidogrel en ciertos grupos raciales, aunque se necesita más investigación en poblaciones diversas.
Revisión de alto impacto que describe la fisiopatología y el tratamiento de la EAP. Confirma que cilostazol, junto con el ejercicio y la revascularización, son las opciones de tratamiento actuales para los síntomas de las extremidades en la EAP.
Revisión sobre la terapia antiplaquetaria dual (DAPT). Menciona que añadir cilostazol puede ser beneficioso para la claudicación en el contexto de la enfermedad arterial periférica, como complemento a la terapia estándar.
Revisión sobre el fenómeno de 'no-reflow' post-recanalización en el ictus isquémico. Cilostazol se menciona como una de las estrategias terapéuticas dirigidas para prevenir o tratar este fenómeno, destacando su rol en la microcirculación.