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 congestive heart failure. Cilostazol is contraindicated in patients with congestive heart failure of any severity.
Cilostazol is a quinolinone derivative that inhibits cellular phosphodiesterase (more specific for phosphodiesterase III). Cilostazol USP is 6-[4-(1-cyclohexyl-1 H -tetrazol-5-yl)butoxy]-3,4-dihydro-2(1 H)-quinolinone, CAS-73963-72-1.
Cilostazol tablets are indicated for the reduction of symptoms of intermittent claudication, as indicated by an increased walking distance.
Published Studies Related to Cilostazol
Cilostazol for intermittent claudication. 
CONCLUSIONS: Cilostazol has been shown to be of benefit in improving
Platelet inhibition by adjunctive cilostazol versus high maintenance-dose clopidogrel in patients with acute myocardial infarction according to cytochrome P450 2C19 genotype. [2011.04]
OBJECTIVES: The aim of this study was to assess the degree of platelet inhibition by adjunctive cilostazol in patients with acute myocardial infarction (AMI) according to hepatic cytochrome P450 2C19 (CYP2C19) genotype. BACKGROUND: Although adjunctive cilostazol intensifies platelet inhibition in AMI patients, it is not established whether this regimen can be free from the effect of CYP2C19 loss-of-function variants (*2/*3)... CONCLUSIONS: Compared with high-MD clopidogrel, adjunctive cilostazol significantly enhances platelet inhibition and reduces the rate of HPR, especially in AMI patients with CYP2C19 loss-of-function variants. (Adjunctive Cilostazol Versus High Maintenance-Dose Clopidogrel in Acute Myocardial Infarction (AMI) Patients According to CYP2C19 Polymorphism [ACCELAMI2C19]; NCT00915733). Copyright (c) 2011 American College of Cardiology Foundation. Published by Elsevier Inc. All rights reserved.
Cilostazol attenuates on-treatment platelet reactivity in patients with CYP2C19 loss of function alleles receiving dual antiplatelet therapy: a genetic substudy of the CILON-T randomised controlled trial. [2011.04]
OBJECTIVE: To evaluate whether the addition of cilostazol to dual antiplatelet therapy (DAT, aspirin plus clopidogrel) can attenuate clopidogrel on-treatment platelet reactivity (OPR) in patients with the CYP2C19 loss-of-function (LOF) allele... CONCLUSION: TAT significantly reduced OPR compared with DAT in carriers of the CYP2C19 LOF allele, but not in non-carriers. These data suggest that the addition of cilostazol to DAT may be a good strategy to attenuate CYP2C19 LOF-related high OPR.
A randomized, double-blind, multicenter comparison study of triple antiplatelet therapy with dual antiplatelet therapy to reduce restenosis after drug-eluting stent implantation in long coronary lesions: results from the DECLARE-LONG II (Drug-Eluting Stenting Followed by Cilostazol Treatment Reduces Late Restenosis in Patients with Long Coronary Lesions) trial. [2011.03.15]
OBJECTIVES: The purpose of this study was to determine whether cilostazol reduces intimal hyperplasia in patients undergoing long zotarolimus-eluting stent implantation (stent length: >/= 30 mm) for native long coronary lesions (length: >/= 25 mm). BACKGROUND: Restenosis after drug-eluting stent implantation remains a significant clinical problem in long coronary lesions... CONCLUSIONS: Patients receiving triple antiplatelet therapy after long zotarolimus-eluting stent implantation had decreased extent of late luminal loss, percent intimal hyperplasia volume, and angiographic restenosis, resulting in a reduced risk of 12-month target lesion revascularization compared with patients receiving dual antiplatelet therapy. (Triple Versus Dual Antiplatelet Therapy after ABT578-Eluting Stent; NCT00589927). Copyright (c) 2011 American College of Cardiology Foundation. Published by Elsevier Inc. All rights reserved.
Multicenter randomized trial evaluating the efficacy of cilostazol on ischemic vascular complications after drug-eluting stent implantation for coronary heart disease: results of the CILON-T (influence of CILostazol-based triple antiplatelet therapy ON ischemic complication after drug-eluting stenT implantation) trial. [2011.01.18]
OBJECTIVES: We aimed to test whether cilostazol has beneficial effects in the real-world patients treated with intracoronary drug-eluting stents (DES). BACKGROUND: The addition of cilostazol on the conventional dual antiplatelet therapy has been reported to reduce platelet reactivity and to improve clinical outcomes after percutaneous coronary intervention in previous studies... CONCLUSIONS: Despite the greater reduction of platelet reactivity by addition of cilostazol to conventional DAT, TAT did not show superiority in reducing the composite of adverse cardiovascular outcomes after DES implantation. (The Efficacy of CILostazol ON Ischemic Complications After DES Implantation [CILON-T]; NCT00776828). Copyright A(c) 2011 American College of Cardiology Foundation. Published by Elsevier Inc. All rights reserved.
Clinical Trials Related to Cilostazol
Evaluation of Cilostazol in Combination With L-Carnitine [Completed]
The purpose of this study is to see how safe and effective L carnitine taken with cilostazol
is compared to placebo taken with cilostazol for people with intermittent claudication. A
second purpose of the study is to see if L-carnitine is absorbed into the blood stream.
Overcome Biochemical Aspirin Resistance Through Cilostazol Combination [Completed]
This study will recruit 316 ischemic stroke patients taking aspirin.
They will be randomly assigned into cilostazol group or placebo group. Every patients will
take 200mg of cilostazol a day or placebo for 1 month.
The primary outcome variable of this study is rate of biochemical aspirin resistance on the
Ultra Rapid Platelet Function Assay-ASA.
Trial of Cilostazol in Symptomatic Intracranial Arterial Stenosis II [Completed]
This study will recruit 480 acute stroke patients with symptomatic intracranial stenosis (M1
segment of Middle cerebral artery (MCA) or basilar artery).
They will be randomly assigned into cilostazol group or clopidogrel group. Every patients
will take 100mg of aspirin a day additionally.
The primary outcome variable of this study is Progression rate of symptomatic intracranial
stenosis on magnetic resonance angiogram (MRA).
A Study on the Effect of Cilostazol in Patients With Chronic Tinnitus [Completed]
1. Overview of tinnitus Tinnitus is a noisy sound which is perceived without any external
sound source. According to the survey of the US, 10-20% of adult have the symptom of
tinnitus and 3-5% of tinnitus patients have severe discomfort of daily life. Severe
tinnitus can result in psychiatric problems such as depression and anxiety disorders.
Enhancement of environmental sound, hearing aids, sound generators, cognitive therapy,
transcranial magnetic therapy, and drug therapy have been tried for treatment of
tinnitus. Nitric oxide(NO) is a well-known neurotransmitter acting as a vasodilator
through regulation of production of cyclic guanosine monophosphate(cGMP) and can be
found in various sites of cochlea. It is reported that cGMP enhances activity of
protein kinase A (PKA), a mediator of platelet aggregation inhibition and
vasodilatation and results in increase of vascular flow.
2. Characteristics of the clinical research drug, cilostazol Cilostazol inhibits
phosphodiesterase type 3 (PDE3) selectively and increases amount of cAMP by inhibition
of degradation of cyclic adenosine monophosphate(cAMP). cAMP again by increasing the
active form of PKA suppress the production of blood clots and increase blood flow by
expanding blood vessels. Anti-platelet activity and vasodilatation effect of cilostazol
have been used for improvement of diabetic peripheral vascular disorders and
suppression of stroke recurrence. Previous studies reported that by increasing the
activity of NO and PKA, the blood flow of stria vascularis and cochlear hair cells can
be improved. These studies implies that cilostazol, which causes inhibition of PDE3 and
increase of PKA, can have a potential effect on improvement of tinnitus by increase of
blood flow to peripheral cochlear cells. Thus, we hypothesized that cilostazol, which
has been widely used for enhancing peripheral blood flow, can bring improvement of
tinnitus by causing better peripheral blood flow of cochlea.
3. The aim of the study We planned this study to validate the assumptions of the
background. The aim of our study is whether administration of cilostazol can improve
tinnitus in terms of subjective degree of symptoms in chronic tinnitus patients.
Cilostazol Versus Aspirin for Primary Prevention of Atherosclerotic Events [Active, not recruiting]
This multi-center, randomized controlled study aims to evaluate the efficacy of Cilostazol
versus Aspirin for primary prevention of atherosclerotic events with Korean type 2 Diabetes
Mellitus (DM) patients.
Reports of Suspected Cilostazol Side Effects
Drug Interaction (8),
Myocardial Infarction (5),
Toxic Epidermal Necrolysis (5),
Septic Shock (5),
Acinetobacter Test Positive (4),
Staphylococcus Test Positive (4),
Interstitial Lung Disease (3), more >>
Page last updated: 2015-08-10