Cilostal

Quick links to important sections

Cilostal

Medically reviewed

Marina Burgos

Last updated on 10/01/2026

This page provides general, reference-level information compiled from official medical sources. It is not a substitute for professional medical advice, diagnosis, or treatment. For decisions about your health, please consult a qualified healthcare professional.

Overview of Cilostal

Quick Facts: Cilostal (Cilostazol)

Property Description
Active ingredient Cilostazol
Form Oral tablet
Pharmacological class Selective Phosphodiesterase 3 (PDE3) Inhibitor, Antiplatelet Agent
Common purpose To improve circulation and reduce platelet stickiness
Origin Synthetic (a 2-oxo-quinoline derivative)

Cilostal: Definition, Chemical Identity, and Class

Cilostal is the trade name for the pharmaceutical agent whose active ingredient is Cilostazol (INN), a synthetic molecule classified as a 2-oxo-quinoline derivative. This distinct chemical structure differentiates it from other common cardiovascular medications. Cilostazol is placed within the pharmacological category of a selective Phosphodiesterase 3 (PDE3) inhibitor, a key enzyme regulator. This mechanism is crucial to its function as an Antiplatelet Agent, a primary therapeutic group it belongs to. Cilostazol is a quinolinone derivative used orally for its specific mechanism of action.


What Type of Medicine Is Cilostal and How Is It Formulated?

Cilostazol is formulated exclusively as a single-agent product for oral administration, typically available as an oral tablet. This solid, systemic formulation requires the active substance, Cilostazol, to be combined with various solid excipients necessary for stability and proper absorption. The preparation is designed to be swallowed, absorbed through the digestive tract, and then circulated throughout the body's vascular network, establishing it as a prescription drug (Rx).


General Purpose: Why Cilostazol Improves Circulation

The primary general purpose of Cilostazol is to improve circulation by exerting two simultaneous physiological effects: vasodilation (widening of blood vessels) and inhibition of platelet aggregation (reducing the tendency of blood components to clump together). By achieving both effects, Cilostazol enhances the flow of blood through the arteries while also preventing platelets from forming restrictive blockages. This drug is associated with enhancing walking capacity in patients with compromised peripheral blood flow. This coordinated dual action is the general benefit it is designed to deliver.

Regulatory References

  1. DailyMed Label for Cilostazol (NIH)

What side effects are possible with Cilostal?

Possible side effects and safety information

The official safety profile for Cilostazol (Cilostal) documents adverse reactions according to frequency classifications and the physiological systems affected, based on data from regulatory bodies like the FDA and EMA.

Documented Adverse Reactions and Frequencies

Adverse reactions are classified into frequency tiers. Those reported as Very Common (1/10) include Headache and Diarrhea. Effects classified as Common (1/100 to <1/10) often involve the Cardiac, Nervous System, and Gastrointestinal domains, such as Palpitation, Tachycardia, Dizziness, Vomiting, and Nausea.

Reactions affecting the Blood and Lymphatic System, such as Thrombocytopenia and Leukopenia, are classified as Rare (1/10,000 to <1/1,000). The official label notes that frequently observed effects, such as Headache, are typically experienced at the start of treatment and may diminish with continued use.

Serious Safety Restrictions and Contraindications

The labeling defines specific, mandatory use restrictions. Cilostazol is officially contraindicated in patients with Heart Failure of any severity, a limitation documented in the FDA's Boxed Warning due to the PDE III inhibitor class effect. The medicine is also contraindicated in individuals with Severe Renal Impairment or Moderate to Severe Hepatic Impairment, as well as in those with a history of unstable angina, recent myocardial infarction, or an active predisposition to bleeding (e.g., active peptic ulceration).

Serious adverse reactions documented in postmarketing reports include severe hemorrhagic events (e.g., Intracranial Hemorrhage), Agranulocytosis, Aplastic Anemia, and severe bullous dermatological reactions.

Overdose and Emergency Response

Cilostal Overdose and When to Seek Help

Official regulatory information describes that the manifestations of an acute Cilostazol overdose are anticipated to be those of excessive pharmacologic effect.

Documented Overdose Presentations

System Affected Regulatory-Listed Manifestations
Cardiovascular Hypotension (low blood pressure), tachycardia (fast heart rate), and cardiac arrhythmias (irregular heartbeat).
General/Gastrointestinal Severe headache, diarrhea, dizziness, and fainting.

In cases of an overdose, regulators note that severe outcomes may involve an increase in heart rate and the risks associated with the drug's antiplatelet action, such as intracranial hemorrhage.

Emergency Actions Mandated by Regulators

If an overdose is suspected, immediate medical attention is required. Official instructions advise individuals to contact a poison control center or emergency room at once.

Urgent medical help must be sought immediately if the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened.

Management procedures detailed in regulatory documents emphasize that the patient should be carefully observed and given supportive treatment. Given the drug's high protein-binding nature, clearance methods such as hemodialysis or peritoneal dialysis are officially noted as being unlikely to be efficient in removing Cilostazol from the body.

Therapeutic Uses of Cilostal

Cilostal (Cilostazol) is indicated for the symptomatic management of Intermittent Claudication (IC) in patients with Peripheral Arterial Disease (PAD) whose symptoms are primarily lifestyle-limiting. This medication is used to help with symptoms related to physical discomfort, specifically the pain, aching, or cramping in the legs that occurs during walking and interferes with daily functioning.

The key therapeutic benefit may be to increase the distance a patient can walk before discomfort begins and to support general well-being during symptomatic phases. It is typically used in settings where symptoms have not sufficiently improved despite lifestyle modifications, such as supervised exercise programs, and it supports the patient by easing the overall symptom burden during periods of heightened discomfort.

Cilostal is used for easing lifestyle-limiting leg pain and is applied in clinical contexts that involve the secondary prevention of vascular events. It plays a role in managing chronic conditions characterized by recurrent claudication symptoms.

“Cilostal is generally applied in situations requiring supportive relief to manage chronic lower limb pain related to walking.”

Quick Fact: Relief for Lifestyle-Limiting Pain
Primary Symptom Domain Activity-related muscle discomfort (cramping, aching)
Key Therapeutic Benefit Supports improved walking distance before discomfort begins
Typical Context of Use Symptomatic management for Peripheral Arterial Disease (PAD)

Regulatory References

  1. European Medicines Agency's public assessment report on Cilostazol

Eligibility and Restrictions for Use

Who Can and Cannot Use Cilostal?

The official eligibility for Cilostazol is strictly defined by regulatory documents. Use is restricted to adult patients whose intermittent claudication symptoms have not sufficiently improved after appropriate lifestyle changes, such as supervised exercise programs.


Absolute Contraindications

Cilostazol is formally prohibited in several patient populations:

  • Cardiac Status: Patients with heart failure of any severity (a major regulatory prohibition). It is also forbidden for patients with unstable angina or those who have had a myocardial infarction or coronary intervention within the last six months.
  • Bleeding Risk: Individuals with active pathological bleeding, established haemostatic defects, or those taking two or more antiplatelet/anticoagulant agents concurrently.
  • Organ Function: Patients with severe renal impairment or moderate to severe hepatic impairment, as use in these groups is not established or prohibited.

Special Population Eligibility

  • Pregnancy & Lactation: The medication is contraindicated during pregnancy and is not recommended while breastfeeding.
  • Pediatric Use: Safety and effectiveness have not been established in children under 18 years of age.
  • Geriatric Use: Regulatory data indicates no significant differences, and no special restrictions apply for older adult use.

What should I know about interactions with other medicines?

The official prescribing information for Cilostazol documents several clinically significant interaction patterns, primarily affecting its systemic exposure and its effect on blood clotting.

Metabolic and Exposure-Altering Interactions

Cilostazol is metabolized by liver enzymes, notably CYP3A4 and CYP2C19. Co-administration with strong or moderate inhibitors of these enzymes, such as ketoconazole or erythromycin, causes a pharmacokinetic interaction that increases the plasma concentration (exposure) of Cilostazol or its active metabolites. This regulatory finding requires that the dose be adjusted downward when Cilostazol is combined with these specific enzyme inhibitors.

Pharmacodynamic Interactions and Restrictions

Due to its antiplatelet activity, Cilostazol has an additive pharmacodynamic effect when combined with other antiplatelet agents (e.g., aspirin) or anticoagulants (e.g., warfarin). This combination is officially associated with an increased risk of hemorrhage. Consequently, the co-administration of Cilostazol with two or more additional antiplatelet or anticoagulant medicines is a formal contraindication documented in regulatory labels.

Interaction with Food and Conditions

A significant drug-food interaction is documented, where high-fat meals and grapefruit juice substantially increase the drug's absorption and exposure. To mitigate this effect, the label specifies that Cilostazol must be taken on an empty stomach—at least 30 minutes before or 2 hours after a meal. Furthermore, use is formally restricted in patients with moderate or severe hepatic impairment due to the potential for excessive drug exposure.

Mechanism of Action

Selective Enzyme Inhibition and Signal Amplification

Cilostazol's core action is the selective competitive inhibition of the Phosphodiesterase Type 3 (PDE3) enzyme, preventing it from degrading the vital cell messenger, cyclic AMP (cAMP). This inhibition results in an increase in intracellular cAMP levels, which acts as the molecular trigger that influences downstream signaling in key vascular cells. This domain results in the sustained activity of the cAMP/Protein Kinase A ( PKA) pathway, influencing the regulation of smooth muscle tone and platelet function.


Dual Regulation of Vascular Tone and Hemostasis

The increased cAMP signal modulates two simultaneous physiological processes. In Vascular Smooth Muscle Cells (VSMCs), the elevated cAMP leads to muscle relaxation, causing arterial vasodilation (widening). In platelets, the same signal suppresses activation, resulting in an antiplatelet effect that reduces the components' tendency to aggregate. This coordinated vascular and hemostatic effect influences the dynamics of peripheral circulation.


Secondary Mechanisms and Systemic Constraints

Beyond PDE3 inhibition, Cilostazol also inhibits the cellular uptake of Adenosine, a natural signaling molecule, thereby promoting the duration of action of local adenosine. However, because PDE3 is also present in the heart, the drug's core mechanism can lead to an increase in myocardial contractility and heart rate (functional consequence), indicating a lack of target exclusivity outside of the intended peripheral vasculature.

Dosage and Administration Information

How Cilostal (Cilostazol) is Used: Administration Guidelines

Cilostal is approved for use as an oral tablet and is administered according to guidelines concerning dosing, timing, and duration. It is not available or approved for administration via any other route, such as intravenous or topical.


Standard Dosage and Timing Protocol

The standard adult dosing regimen is 100 mg twice daily.

Administration Component Instruction
Route of Administration Oral tablet only.
Standard Dosing Frequency Twice daily (e.g., morning and evening).
Food Relationship Taken on an empty stomach, specifically 30 minutes before or 2 hours after a meal, as food impacts its absorption.

Usage Duration and Special Conditions

Treatment with Cilostazol typically requires a minimum duration before efficacy can be assessed. The regimen is generally continued for up to 12 weeks (3 months) to determine whether the medicine is providing a satisfactory benefit. If no symptomatic improvement is observed after this period, the medication is usually discontinued.

Dose Adjustment: A lower dose of 50 mg twice daily is utilized if the patient is simultaneously taking other medications known to significantly inhibit the CYP3A4 or CYP2C19 liver enzymes. No special dose adjustment is required for older adults or individuals with mild to moderate kidney impairment. If a dose is missed, the instructions are to skip that dose and resume the regular schedule; a double dose should not be taken.

Recent Clinical Evidence

Research Evidence / Overview of Studies


Phase III Clinical Trials

Studies have examined whether the drug has an effect on pain reduction and evaluated whether it was associated with an improvement in quality of life in patients with intermittent claudication (IC). Clinical trials designed to assess walking performance showed that participants receiving the drug experienced an increase in both pain-free and maximal walking distances compared to placebo.

Specific studies examined the safety profile of the drug in participant groups. Adverse events reported by participants were documented in the trial findings, with commonly reported events including headache and diarrhea. Researchers noted specific observations regarding liver enzyme levels, which were monitored throughout the trials.

  • Trial 1: Efficacy and Safety

    • The primary goal of this trial was to assess changes in specific symptom scores using standardized treadmill testing over periods typically ranging from 12 to 24 weeks. The trial design required participants to adhere to a specific administration protocol.
  • Trial 2: Long-term Analysis

    • This study extended over periods up to two years, focusing on sustained observation of participants. Researchers also investigated whether the drug was associated with a change in the frequency of flare-ups.

Subgroup Analysis and Combination Therapy

Specific analyses were conducted to examine outcomes in distinct groups, including elderly individuals and those with certain mild to moderate impairments. The effect on walking distance was generally observed across various subgroups, including patients with and without diabetes.

  • Combination Therapy
    • Preliminary data compared outcomes of participants receiving combination therapy (the drug plus other antiplatelet agents) against those receiving monotherapy in trials for secondary stroke prevention. Studies documented that individuals with severe kidney issues were excluded from specific trials.

Summary of Findings

Overall research has explored whether the drug is associated with changes in specific disease biomarkers and whether the profile of adverse events was consistent across the study populations. The evidence remains limited regarding studies performed in pediatric populations.

Key Studies & References

  1. National Institute for Health and Care Excellence (NICE) Guideline: Peripheral arterial disease: diagnosis and management (Used for clinical context and treatment options)

Frequently Asked Questions (FAQ)

Common questions about Cilostal (FAQ)

Q: How long does it typically take to notice the effects of Cilostal?

Studies and official information indicate that the full efficacy of Cilostal cannot be formally assessed until the regimen is completed for up to 12 weeks (3 months). Based on study results, the benefits of the medication are typically assessed after approximately 60 to 90 days.

Q: Is Cilostal intended to be a long-term or permanent medication?

Treatment with Cilostal is typically initiated for a minimum of 12 weeks to assess improvement. Official documents indicate that long-term studies have been conducted for up to two years, particularly in research contexts like secondary stroke prevention. The determination of long-term use is based on the evaluation of sustained benefit, as noted in clinical practice.

Q: Is a generic version of the drug Cilostal readily available?

The active ingredient, Cilostazol, is available as a generic medication. The availability of generic alternatives is consistent with general drug information provided by regulatory bodies.

Q: Is Cilostal used to prevent blood clots?

Cilostazol is classified as an antiplatelet agent. Its mechanism involves the reversible inhibition of platelet aggregation (clumping), which contributes to its therapeutic goal of improving blood flow. This action is part of the therapeutic goal of influencing blood flow dynamics.

Q: Can Cilostal be taken at the same time as common over-the-counter pain relievers?

Cilostazol is an antiplatelet agent, and combining it with other platelet inhibitors, such as aspirin, may increase the risk of bleeding (hemorrhage). Regulatory documents advise caution when combining this medicine with any other substance that increases bleeding risk.

Q: Is it safe to take Cilostal if I am already taking a daily low-dose aspirin regimen?

The coadministration of Cilostazol and a single antiplatelet agent, such as aspirin, results in an additive antiplatelet effect, which is officially associated with an increased risk of hemorrhage. The official label strictly contraindicates the use of Cilostazol with two or more additional antiplatelet or anticoagulant agents. The official documentation emphasizes that combining the medications requires close monitoring for bleeding risk.

Q: Is it safe to take Cilostal with non-steroidal anti-inflammatory drugs (NSAIDs)?

Non-steroidal anti-inflammatory drugs (NSAIDs) may increase the risk of bleeding. Regulatory documents emphasize that caution is necessary when combining the medication with other antiplatelet agents or substances that increase bleeding risk.

Q: Does Cilostal have an impact on a person's blood pressure readings?

The drug's mechanism of action includes vasodilation (widening of blood vessels), which can lead to a mild reduction in blood pressure. Low blood pressure has been observed in some clinical data. This is typically a mild effect, reported in less than 1% of patients in trials.

Q: What are the potential effects of stopping Cilostal abruptly?

Cilostazol’s mechanism of action on platelets is reversible, meaning its effects resolve within a predictable time frame. For procedures that require stopping the drug to reduce bleeding risk, discontinuation approximately three days prior to a procedure is noted in regulatory information.

Q: Is there a withdrawal period when stopping Cilostal?

Cilostazol is cleared from the body within a few days of stopping, as its effects are reversible. This rapid clearance means that the medication reaches adequate systemic clearance relatively quickly after discontinuation, as documented by elimination half-life data.

Q: Can I drive while taking Cilostal?

Official patient information sheets state that Cilostazol may cause dizziness. If dizziness occurs after taking this medicine, activities requiring full alertness, such as driving or using heavy machinery, should be avoided.

Q: Is the feeling of increased heart rate a sign of a serious side effect from Cilostal?

An increase in heart rate, known as tachycardia, is a common, expected side effect due to the drug’s mechanism of action. This cardiac effect is usually managed but is not listed as a severe safety restriction in the same way as conditions like Heart Failure or severe hemorrhage.

Q: What is the current research on the long-term safety profile of Cilostal?

Long-term safety has been evaluated in studies lasting up to two years. Long-term data suggests the drug does not appear to increase the risk of major bleeding when used alone. Patient discontinuation is most often due to common side effects like headache, diarrhea, and palpitations.

Q: Are there known interactions between Cilostal and common vitamin or herbal supplements?

There are no general statements covering all vitamins or herbal supplements in official documents. However, the regulatory label advises caution with any substance that affects the CYP3A4 or CYP2C19 liver enzyme systems, as this may change the drug’s concentration in the body.

Q: Does Cilostal interact with common medications used to treat heartburn or reflux (antacids)?

The drug interaction profile notes a specific interaction with omeprazole, a common gastric acid reducer, which can increase the systemic exposure of Cilostazol’s active metabolites. Dose adjustment of Cilostazol may be necessary when taken with this type of inhibitor, as noted in the drug interaction profile.

Q: Does Cilostal have any interactions with psychiatric medications?

Some medications used to treat depression, such as fluoxetine, fluvoxamine, and sertraline, are known inhibitors of the CYP enzyme system. Official documentation indicates that a dose adjustment of Cilostazol may be necessary when combined with these specific types of inhibitors.

Q: Can taking Cilostal affect my eyesight?

Adverse events documented in postmarketing reports include less common or rare reports of visual disturbances. These effects may include blurred vision and temporary blindness.

How should Cilostal be stored and disposed of?

Official Storage and Disposal Instructions

Cilostazol must be stored under specific, officially documented conditions to maintain its integrity.

Storage Detail Requirement
Temperature Store at Controlled Room Temperature, 20 C to 25 C (68 F to 77 F).
Protection Keep the container tightly closed to protect from moisture.
Packaging Store in the original container or as dispensed.
Safety Keep out of the sight and reach of children.

Disposal of unused or expired Cilostazol must follow regulatory requirements. The product should be discarded according to local regulations, typically through an authorized collection system or special waste collection point.

Attention! Always consult to a doctor or pharmacist before using pills or medicines.

Available in countries:

Equivalent of Cilostal found in:

A-Z Index: