OBJECTIVE Cilostazol is a Biopharmaceutical Classification System class II drug with low solubility and high permeability, so its oral absorption is variable and incomplete. The aim of this study was to prepare two sulfonate salts of cilostazol to increase the dissolution and hence the oral bioavailability of cilostazol. METHODS Cilostazol mesylate and cilostazol besylate were synthesized fro...

AIM The vascular endothelium plays a key role in the pathophysiology of atherosclerosis. Flow-mediated dilation (FMD) is a novel way of assessing endothelial function. Cilostazol is a unique antiplatelet drug that also has the potential to improve endothelial function. The objective of this present study was to investigate the effects of cilosatzol on endothelial function as assessed by FMD. ...

A aterosclerose é uma doença inflamatória crônica de origem multifatorial que ocorre em resposta à agressão endotelial, acometendo principalmente a camada íntima artérias médio e grande calibres. O diabetes mellitus tipo 2 está associado alta taxa cardiovascular aterosclerótica. Esse estudo visa analisar o impacto, pelo tratamento medicamentoso do Cilostazol, um medicamento antiplaquetário, na ...

Cilostazol, a selective type III phosphodiesterase inhibitor, has antiplatelet and vasodilating effects. In this study, the effects of cilostazol on lipid metabolism and lipoprotein lipase (LPL) activity were studied in rats. Cilostazol was administered orally at doses of 30 or 100 mg/kg twice a day for 1-2 weeks to rats. Cilostazol decreased the serum triglyceride level in normolipidemic rats....

This study aimed to evaluate the transporter-mediated renal excretion mechanism for cilostazol and to characterize the mechanism of drug–drug interaction (DDI) between cilostazol and aspirin or probenecid. Concentrations of cilostazol and its metabolites OPC-13015 [6-[4-(1-cyclohexyl-1H-tetrazol-5-yl)butoxy]-2(1H)quinolinone] and OPC-13213 [3,4-dihydro-6-[4-[1-(trans-4-hydroxycyclohexyl)-1H-tet...

Patients with essential hypertension undergo endothelial dysfunction, particularly in the conduit arteries. Cilostazol, a type III phosphodiesterase inhibitor, serves a role in the inhibition of platelet aggregation and it is widely used in the treatment of peripheral vascular diseases. Previous studies have suggested that cilostazol suppresses endothelial dysfunction; however, it remains unkno...

abstract reactive oxygen species and oxidative stress impair β-cell function and reduce insulin secretion. it has been shown that progesterone and cilostazol possess antioxidant properties. the present study was aimed to investigate in vitro pretreatment effect of progesterone and cilostazol on insulin secretion as well as their protective effects against hydrogen peroxide-induced oxidative str...

Cilostazol is a selective inhibitor of phosphodiesterase 3 that increases intracellular cAMP levels and activates protein kinase A, thereby inhibiting vascular smooth muscle cell (VSMC) proliferation. We investigated whether AMP-activated protein kinase (AMPK) activation induced by heme oxygenase-1 (HO-1) is a mediator of the beneficial effects of cilostazol and whether cilostazol may prevent c...

This study was designed to investigate the effects of cilostazol on the pharmacokinetics of carvedilol following oral or intravenous administration of carvedilol in rats. Clinically carvedilol and cilostazol can be prescribed for treatment of cardiovascular diseases. Carvedilol and cilostazol are all substrates of CYP2C9 enzymes. Carvedilol was administered orally or intravenously without or wi...

Purpose: To study the effect of Cilostazol on rat thromboangiitis obliterans (TAO), and mechanism action involved.
 Methods: Rats (N = 45) were injected with sodium laurate to establish model TAO, then divided into Sham group (n 15), TAO 15) + cilostazol 15). After administration cilostazol, lesions in rats graded, femoral arteries stained by hematoxylin-eosin (H&E) determine degree va...