Cilostazol, also known as Sisetazole, Pletal, OPC-13013, Cilosrazol, etc., is a novel antiplatelet agent with marked inhibitory effects on platelet aggregation and vasodilatory properties.
Drug Properties
Chinese Name: 西洛他唑
English Name: Cilostazol
CAS Number: 73963-72-1
Alternative Names: Sisetazole, Pletal, OPC-13013, Cilosrazol, etc.
Appearance: White or almost white crystalline powder, odorless. Easily soluble in glacial acetic acid or chloroform, slightly soluble in methanol or anhydrous ethanol, and practically insoluble in water, 0.1M hydrochloric acid, or 0.1M sodium hydroxide solution.
Pharmacological Effects
Cilostazol primarily inhibits the activity of phosphodiesterase (PDE), particularly PDE III, on platelets and smooth muscle, thereby expanding blood vessels and inhibiting platelet aggregation induced by thromboxane A2.
It inhibits both primary and secondary aggregation induced by ADP or adrenaline without affecting platelet arachidonic acid metabolism.
Cilostazol does not interfere with the synthesis of prostacyclin (PGI2) by vascular endothelial cells and can increase tissue blood flow in the feet and calf muscles, leading to an increase in ankle-brachial pressure index, cutaneous blood flow, and skin temperature of the extremities, thus improving symptoms such as intermittent claudication.
Clinical Applications
Cilostazol is widely used in the treatment of chronic arterial occlusive diseases caused by atherosclerosis, aortitis, thromboangiitis obliterans, and diabetes.
It improves symptoms such as chronic ulcers, pain, cold sensation, and intermittent claudication caused by limb ischemia.
It can also be used as adjunctive therapy after angioplasty, vascular grafting, or sympathectomy to alleviate symptoms, improve circulation, and inhibit thrombus formation in grafted vessels.
