Cilostazol Tablets

Mechanism

Cilostazol inhibits phosphodiesterase‑3, increasing intracellular cAMP levels. This leads to vasodilation, inhibition of platelet aggregation, and improved blood flow in peripheral arteries.

Pharmacokinetics

• Absorption: Rapidly absorbed after oral administration; peak plasma concentration reached in 2–4 hours.
• Bioavailability: Food (especially high‑fat meals) increases absorption significantly.
• Distribution: Extensively protein bound (~95–98%).
• Metabolism: Extensively metabolized in the liver via CYP3A4 and CYP2C19 into active metabolites.
• Excretion: Eliminated mainly via urine (~74%) and feces (~20%).
• Half-life: Terminal elimination half-life ~11–13 hours, supporting twice‑daily dosing.

Side Effects

• Headache
• Palpitations
• Dizziness
• Diarrhea
• Peripheral edema

Contraindication

• Congestive heart failure
• Hypersensitivity to Cilostazol
• Severe renal or hepatic impairment

Interaction

• CYP3A4 inhibitors (ketoconazole, erythromycin increase plasma levels)
• CYP2C19 inhibitors (omeprazole increase exposure)
• Other antiplatelet/anticoagulants (additive bleeding risk)

Warning and Precautions

• Use under medical supervision only
• Monitor for bleeding complications
• Not recommended in patients with heart failure

Dosage

As directed by the Physician.