Cilostazol

What it is and how it works

Mechanism of Action Cilostazol and several of its metabolites inhibit phosphodiesterase III activity and suppress cAMP degradation with a resultant increase in cAMP in platelets and blood vessels, leading to inhibition of platelet aggregation and vasodilation, respectively. Cilostazol reversibly inhibits platelet aggregation induced by a variety of stimuli, including thrombin, ADP, collagen, arachidonic acid, epinephrine, and shear stress. Cardiovascular effects: Cilostazol affects both vascular beds and cardiovascular function. It produces heterogeneous dilation of vascular beds, with greater dilation in femoral beds than in vertebral, carotid or superior mesenteric arteries.

Mechanism class: Phosphodiesterase 3 Inhibitors

Indications

Cilostazol tablets are indicated for the reduction of symptoms of intermittent claudication, as demonstrated by an increased walking distance. Cilostazol tablets are a phosphodiesterase III inhibitor (PDE III inhibitor) indicated for the reduction of symptoms of intermittent claudication, as demonstrated by an increased walking distance

Dosage and administration (summary)

The recommended dosage of cilostazol tablets is 100 mg twice daily taken at least half an hour before or two hours after breakfast and dinner Reduce the dose to 50 mg twice daily when coadministered with CYP3A4 inhibitors such as ketoconazole, itraconazole, erythromycin, and diltiazem, or CYP2C19 inhibitors such as ticlopidine, fluconazole, and omeprazole Recommended Dosage The recommended dosage of cilostazol tablets is 100 mg twice daily taken at least half an hour before or two hours after breakfast and dinner. Patients may respond as early as 2 to 4 weeks after the initiation of therapy, but treatment for up to 12 weeks may be needed before a beneficial effect is experienced.

Contraindications

Cilostazol tablets are 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.

Warnings and precautions

Risks of tachycardia, palpitation, tachyarrhythmia or hypotension. Risks of exacerbations of angina pectoris or myocardial infarction in patients with a history of ischemic heart disease Left ventricular outflow tract obstruction has been reported in patients with sigmoid shaped interventricular septum Risks of thrombocytopenia or leukopenia progressing to agranulocytosis-monitor platelets and white blood cell counts Avoid use in patients with hemostatic disorders or active pathologic bleeding Tachycardia Cilostazol may induce tachycardia, palpitation, tachyarrhythmia or hypotension.

Pregnancy

Pregnancy Teratogenic Effects Cilostazol has been shown to be teratogenic in rats at doses that are greater than 5-times the human MRHD on a body surface area basis. There are no adequate and well-controlled studies in pregnant women.

Storage and supply

100 mg - white to off-white, round tablets, debossed with “TEVA” on one side and “7231” on the other, available in bottles of 60 (NDC 63629-8795-01) Store at 20° to 25°C (68° to 77°F) . Dispense in a tight, light-resistant container as defined in the USP, with a child-resistant closure (as required).

Source: Cilostazol (Cilostazol) — US FDA prescribing information, 2024-01-11, DailyMed. Summarised and shortened; the full label governs. Iranian registration, indications and labelling may differ.