Cilostazol

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Cilostazol

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Medically reviewed

Marina Burgos

Last updated on 22/12/2025

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 Cilostazol

Property Description
Active ingredient Cilostazol
Form Oral Tablet
Pharmacological class Phosphodiesterase III (PDE3) Inhibitor
Common use Improving limb circulation
Origin Synthetic compound (Quinolinone derivative)

What Type of Medicine is Cilostazol?

Cilostazol is a synthetic prescription medication that belongs to the Quinolinone derivative chemical family. It is pharmacologically classified as both a Platelet-Aggregation Inhibitor and a Vasodilator, with its primary mechanism defining it as a Phosphodiesterase III (PDE3) Inhibitor.

This single-ingredient product is defined by its role in addressing circulatory issues. Cilostazol provides both the widening of blood vessels and the reduction of platelet stickiness. This dual ability to improve blood flow by physically opening arteries and thinning the blood makes it clinically recognized for its specific application in improving walking performance in adults.


Composition and Available Form

The medication is based entirely on the active ingredient, Cilostazol, which is provided for oral administration exclusively in the tablet dosage form. The tablet structure utilizes standard pharmaceutical excipients as the base, which serve to bind the pill and facilitate its controlled release within the digestive system.

As a synthetic compound, its purity and consistency are highly controlled during manufacturing. Agents like Cilostazol are specifically studied for their effects on leg pain caused by poor circulation. The requirement for a prescription reinforces its status as a drug for specialized cardiovascular management under medical guidance.


General Therapeutic Purpose

The overall goal of Cilostazol is to significantly enhance the movement of blood through the peripheral vascular system, particularly to the limbs. It achieves this by reducing the natural tendency of platelets to become sticky and by actively promoting the relaxation of the muscular walls in peripheral arteries.

By maximizing blood flow and reducing the risk of obstruction within the vessels, the medication supports the general physiological objective of increasing oxygen and nutrient delivery to tissues. This combined effect aids the primary therapeutic purpose of augmenting physical capacity in individuals where peripheral circulation is a limiting factor, such as those experiencing discomfort when walking.

What side effects are possible with Cilostazol?

Possible Side Effects and Safety Information

The safety profile for Cilostazol, a Phosphodiesterase III (PDE3) inhibitor, is rigorously classified by government regulatory authorities, detailing potential adverse reactions by frequency and physiological system affected.

Adverse Reactions by Frequency

Adverse reactions that are frequently documented include those categorized as Very Common (reported in ge 10% of patients) and Common (reported in 1% to 10% of patients). The most frequently reported events are Headache, Diarrhea, and Abnormal stools.

Common reactions span multiple System-Organ Classes and include Palpitations, Tachycardia, Dizziness, Nausea, Vomiting, Abdominal pain, and Peripheral oedema.

Serious Safety Constraints and Contraindications

The official labeling includes a critical safety constraint that Cilostazol is contraindicated in patients with any degree of Heart Failure, a restriction based on risks identified with the drug's pharmacological class. This constraint defines a major limitation for its use.

Additionally, the medication is contraindicated in individuals with a known predisposition to bleeding, such as those with active pathological bleeding or hemostatic abnormalities. It is also contraindicated in cases of severe renal impairment or moderate to severe hepatic impairment, as drug clearance is substantially reduced in these populations.

Less frequent but serious adverse reactions documented in regulatory sources include major cardiovascular events like Myocardial infarction and Stroke, as well as severe Hematological Abnormalities such as Agranulocytosis and Aplastic Anemia. Regulatory texts advise that blood cell counts should be monitored periodically due to the risk of these hematological complications.

Overdose and Emergency Response

The official regulatory documents define the Cilostazol overdose profile based on the risk of an excessive pharmacologic effect of the medication. Symptoms associated with acute overdose are generally documented as an exaggeration of the drug’s known actions. Clinical manifestations include severe headache, diarrhea, tachycardia (fast heartbeat), and hypotension (low blood pressure). The most serious documented concern is the potential for cardiac arrhythmias (irregular heartbeats), which reflects the medication's impact on the cardiovascular system.

Emergency Actions and Required Care

It is mandated by regulatory authorities that individuals who suspect an overdose must seek immediate medical attention by contacting a Poison Control Center or proceeding to an emergency room at once. Urgent medical assistance is required if the affected person has collapsed, experienced a seizure, or has trouble breathing.

Official Management Strategy

The management of Cilostazol overdose is described as symptomatic and supportive. As no specific antidote is listed in the official prescribing information, care focuses on maintaining vital functions. Procedural steps, such as gastric lavage or induced vomiting, may be considered by medical professionals as appropriate to empty the stomach. Due to the medication's high protein binding, elimination through hemodialysis is stated by the regulator as being unlikely to be efficient.

Therapeutic Uses of Cilostazol

Main Uses and Benefits of Cilostazol

Cilostazol is a medication primarily prescribed to manage the symptoms of intermittent claudication. This condition is characterized by muscle pain, cramping, or fatigue in the legs that occurs during physical activity, such as walking, and typically subsides with rest.

Treatment of Intermittent Claudication

Intermittent claudication is a symptom of peripheral artery disease, where the arteries that supply blood to the legs become narrowed or blocked. This reduced blood flow prevents muscles from receiving enough oxygen during exertion. Cilostazol works by helping to open the blood vessels and reducing the stickiness of platelets in the blood.

Improving Walking Distance

The primary benefit of this treatment is the improvement of a patient's functional mobility. Clinical observations show that consistent use of the medication can lead to:

  • Increased Pain-Free Walking Distance: Patients may find they can walk further before the onset of leg pain begins.
  • Increased Absolute Walking Distance: The total distance a person can walk before the pain becomes too severe to continue is often improved.
  • Enhanced Quality of Life: By improving the ability to perform daily activities and exercise, the medication helps patients maintain a more active lifestyle.

Mechanism of Action

Cilostazol belongs to a class of drugs known as phosphodiesterase III inhibitors. It serves two main functions that contribute to its therapeutic effects:

  1. Vasodilation: It promotes the relaxation of the smooth muscles in the arterial walls, which allows the blood vessels to widen and improves overall circulation to the limbs.
  2. Antiplatelet Activity: It inhibits the aggregation of platelets, which are the components of blood responsible for clotting. By reducing the likelihood of minor clot formations, it helps maintain smoother blood flow through narrowed passages.

While the medication addresses the symptoms of leg pain, it is often utilized as part of a broader management plan to improve circulatory health and physical endurance.

Eligibility and Restrictions for Use

Cilostazol is eligible for use only in the adult population (18 years and older) who have Intermittent Claudication due to Peripheral Artery Disease. Safety and efficacy have not been established in pediatric patients.

Populations for Whom Use is Contraindicated

Cilostazol is strictly contraindicated for several populations, based on official regulatory labeling, including a US FDA Black Box Warning for patients with:

  • Heart failure of any severity (Congestive Heart Failure).
  • Active pathologic bleeding or a known predisposition to hemorrhage (e.g., active peptic ulceration, recent haemorrhagic stroke).
  • Unstable angina pectoris, a recent myocardial infarction (within six months), or a recent coronary intervention.
  • Severe Renal Impairment (creatinine clearance le 25 ml/min) or Moderate to Severe Hepatic Impairment.
  • Pregnancy and is not recommended for nursing mothers.

Condition-Based Eligibility Restrictions

Use is restricted for patients taking two or more additional antiplatelet or anticoagulant agents concurrently. Furthermore, when the medicine is co-administered with strong inhibitors of CYP3A4 or CYP2C19 enzymes, regulatory labels require a dose reduction to 50 mg twice daily. No special dosage requirements are noted for the elderly.

What should I know about interactions with other medicines?

Interactions with other medicines and products

Official regulatory documents define the interaction profile of Cilostazol based on its metabolic pathways and its pharmacodynamic effects on blood clotting.

Documented Pharmacokinetic Interactions

Cilostazol is metabolized by CYP3A4 and CYP2C19 enzymes. Co-administration with strong or moderate inhibitors of these enzymes significantly increases the plasma concentration of Cilostazol and its active metabolite. For instance, strong CYP3A4 inhibitors (like ketoconazole and erythromycin) and strong CYP2C19 inhibitors (like omeprazole) require a mandated dose adjustment, as defined in the official prescribing information, to manage this increased exposure.

Pharmacodynamic and Food Interactions

Due to the medicine’s effect on platelet function, the official label imposes strict constraints on co-administration with other antiplatelet and anticoagulant agents. Combining Cilostazol with two or more additional antiplatelet or anticoagulant agents (such as warfarin or clopidogrel) is officially contraindicated due to the high risk of hemorrhagic events. Furthermore, administration is dependent on timing: Cilostazol must be taken on an empty stomach (one-half hour before or two hours after a meal) to prevent the documented food-mediated increase in drug exposure. Consumption of grapefruit juice is also listed as an interaction that increases plasma concentration.

Mechanism of Action

Molecular Mechanism: Selective PDE3 Enzyme Inhibition

Cilostazol operates as a selective inhibitor of the enzyme Phosphodiesterase Type 3 ( PDE3), which is responsible for breaking down the cellular messenger cyclic adenosine monophosphate ( cAMP) in various cells, including platelets and arterial smooth muscle. By blocking this enzyme, Cilostazol prevents the degradation of cAMP, consequently altering the cyclic nucleotide concentration within these cellular systems.


Dual Physiological Action: Vasodilation and Antiplatelet Activity

The elevated cAMP levels initiate two critical and concurrent cascades. In the arterial smooth muscle, increased cAMP leads to muscle relaxation and subsequent vasodilation (vessel widening), which modulates vascular resistance. Concurrently, in platelets, the cAMP increase suppresses their activation pathway, which reduces their capacity for aggregation and adhesion. The combined physiological consequence is an increase in the potential for blood flow and oxygen delivery to the tissues.


️ Mechanism Limitations and Regional Specificity

The vasodilatory component of the mechanism is not uniformly expressed throughout the body; rather, the effect is mechanistically more pronounced in the peripheral arteries compared to central vessels. This difference is consistent with the distribution and activity of the PDE3 enzyme in different vascular territories, resulting in the most pronounced physiological response in the peripheral circulation.

Dosage and Administration Information

The use of Cilostazol tablets involves specific parameters regarding dosage, frequency, and timing. The medication is available in 50 mg and 100 mg oral tablets and is administered via the oral route.

Dosing and Administration

The standard recommended dosage is 100 mg twice daily (b.i.d.). This frequency is important to maintaining therapeutic levels of the active substance. To facilitate optimal absorption, the tablets are taken on an empty stomach. This involves taking the dose at least 30 minutes before or 2 hours after both breakfast and the evening meal.

Dose Adjustments and Treatment Course

A dose reduction to 50 mg twice daily is indicated when Cilostazol is co-administered with certain other medications that strongly inhibit the CYP3A4 or CYP2C19 enzymes (e.g., omeprazole or diltiazem). These parameters provide a structured approach to administration in the context of concurrent therapies.

Regarding the treatment course, it may require up to 12 weeks before the full beneficial effect is experienced. If symptoms show no improvement after a duration of 3 months of therapy, the treatment is typically discontinued. If a single dose is missed, the instruction is to skip the missed dose and continue with the regular schedule, rather than taking a double dose.

Recent Clinical Evidence

Research evidence / Overview of Studies for Cilostazol

Evidence for Use in Intermittent Claudication (IC) and Walking Function

The main research exploring this medication's use in individuals with Intermittent Claudication (IC)—a condition marked by functional limitations and outcomes related to physical discomfort during activity—centers around a series of short-term, randomized controlled trials (RCTs). These RCTs were complemented by subsequent Meta-analyses. This body of evidence was applied in studies examining patient-reported experiences, with research exploring outcomes related to physical discomfort and daily functioning or activity level.

The studies monitored functional capacity by measuring the distance walked to the onset of symptoms (Pain-Free Walking Distance) and the total distance walked (Maximum Walking Distance), assessed via standardized treadmill tests. Findings describe patterns observed in the studies where research highlights changes measured during the study period for these functional outcomes, in comparison to the placebo group. The evidence level for this specific research area has been broadly categorized as High.


Research on Preventing Vessel Re-narrowing (Restenosis)

This medication was studied for research contexts involving artery health and patency, primarily after procedures used to open narrowed arteries. This research includes randomized trials and meta-analyses that studies explored outcomes measured after the medication was added to standard antiplatelet therapy following stenting or endovascular therapy (EVT).

The studies examined angiographic endpoints such as the rate of restenosis (the re-narrowing of the treated vessel) and the amount of late lumen loss (change in vessel width). The evidence level for this research area has been broadly categorized as Moderate.


What Remains Uncertain in the Research Landscape

The primary limitation is that the research exploring short-term symptom changes was conducted over follow-up durations that were limited (12–24 weeks). As a result, the certainty remains low regarding the long-term progression of the underlying condition and the impact on critical outcomes like the need for amputation or cardiovascular events over long periods. Research indicates long-term effects are not fully established, and data for certain patient groups remain insufficient.

Key Studies & References

  1. Effect of cilostazol on in-stent restenosis after drug-eluting stent implantation: a systematic review and meta-analysis of randomized controlled trials

Frequently Asked Questions (FAQ)

Common questions about Cilostazol (FAQ)


Q: Is Cilostazol a blood thinner, and how is it different from aspirin?

Official documents classify the medicine as a Platelet-Aggregation Inhibitor and a Vasodilator. This dual classification describes the drug's properties to help reduce platelet clumping and relax blood vessels, which is consistent with the goal of improving blood flow.


Q: How quickly does Cilostazol start working for walking distance?

Official product information suggests that some individuals may notice a response as early as 2 to 4 weeks after beginning therapy. However, the research supporting authorization indicates that a full assessment of the medicine's effect is typically made after a course of up to 12 weeks.


Q: Does Cilostazol have a common interaction with grapefruit?

Yes, regulatory information lists an interaction with grapefruit or grapefruit juice. This interaction may result in increased exposure to the medicine, potentially raising the likelihood of experiencing adverse effects.


Q: Can I take Cilostazol if I am also taking medicine for high blood pressure?

Official information does not forbid the combination with all blood pressure medications. However, the medicine's potential to cause hypotension (low blood pressure) is noted. Official information suggests informing a healthcare provider of all other medications being taken.


Q: Does taking Cilostazol require special monitoring or blood tests?

Yes, regulatory information advises that platelet and white blood cell counts should be monitored periodically. This advice is based on the potential for hematological complications, such as agranulocytosis.


Q: What research is available on Cilostazol use in younger adults?

Cilostazol is only authorized for use in the adult population. The official label notes that safety and effectiveness have not been established in pediatric patients (children).


Q: Can Cilostazol help with leg pain besides walking?

The medicine is specifically authorized in regulatory documents for use in individuals with intermittent claudication. This condition is characterized by pain or cramping in the legs that occurs during activity and typically subsides when the patient is resting.


Q: Is it normal to feel a rapid heartbeat or palpitations when starting Cilostazol?

Official regulatory documents list palpitations (feeling your heart beat quickly) and tachycardia (a rapid heart rate) as common adverse reactions. The change in heart rate is approximated in official documents.


Q: Can Cilostazol be used by people with diabetes?

Diabetes itself is not listed as a restriction in the official product information. Studies used for authorization included individuals with diabetes. However, the use of the medicine is subject to its official contraindications, such as the presence of heart failure.


Q: Are there any specific foods or drinks I should avoid while on this medication?

Yes, the official label advises that the medicine must be taken on an empty stomach. This requirement prevents food-mediated increases in drug exposure. Additionally, regulatory documents list grapefruit juice as a product that should be avoided.


Q: Can older people safely use Cilostazol?

Official documentation states that there are no special dosage recommendations required for elderly patients. The safety and effectiveness profile observed in this population is generally consistent with that seen in younger adults.


Q: Does Cilostazol cause headaches, and if so, how long do they usually last?

Headache is reported as a Very Common adverse reaction, meaning it occurs in 10% or more of patients. Regulatory documents, however, do not specify the typical duration or expected resolution time for this side effect.


Q: Is Cilostazol known to interact with herbal supplements like St. John's Wort?

Yes, St. John's Wort is specifically mentioned in some regulatory documents. This is because it may interact with the enzyme systems in the body that are responsible for breaking down the medicine.


Q: How long can a person expect to be on Cilostazol treatment?

Official information states that if symptoms do not show improvement after 3 months of therapy, the medicine should be discontinued. The decision to continue treatment beyond this initial assessment period is made by a healthcare provider on an individual basis.


Q: Will Cilostazol interfere with sleep or cause insomnia?

Insomnia (difficulty falling or staying asleep) has been reported as an adverse reaction in postmarketing experience with the drug, according to official regulatory documents.


Q: Are there any known interactions between Cilostazol and alcohol?

Regulatory documents do not strictly prohibit alcohol consumption, but caution may be advised. Alcohol can potentially increase the risk of side effects such as dizziness or lightheadedness, which are also known effects of the medication.


Q: What are the research findings regarding Cilostazol's effect on quality of life?

Research cited in authoritative sources indicates that, in addition to improving walking function, the medicine has been shown in clinical studies to improve health-related quality of life (QoL) for individuals with intermittent claudication.


Q: Is Cilostazol used for conditions other than peripheral artery disease (PAD)?

Cilostazol is only approved for use for one condition: the reduction of symptoms of intermittent claudication in people with peripheral artery disease. Official documentation does not authorize its use for any other conditions.


Q: Is it normal for me to feel dizzy or lightheaded while on this medication?

Dizziness is listed in official regulatory documents as a Common adverse reaction, meaning it is reported in 1% to 10% of patients. Lightheadedness may be a related side effect.


Q: Are there long-term side effects associated with continuous Cilostazol use?

Because the primary clinical trials were short-term (12–24 weeks), regulatory documents indicate that the certainty remains low regarding the long-term effects on major cardiovascular events and the underlying condition's progression.


Q: Is there a known interaction between Cilostazol and acid reflux medications?

Yes, some acid reflux medications, such as omeprazole, are known to interact with Cilostazol. Official documents note that a dose adjustment is specified when the medicine is taken alongside strong inhibitors of the CYP2C19 enzyme.


Q: Can Cilostazol interact with anxiety or depression medications?

Regulatory documents state that certain medications used for anxiety or depression, such as SSRIs, have the potential to interact. This combination may be associated with an increased risk of bleeding due to effects on platelet function.


Q: Does Cilostazol require being taken with food, or can it be taken on an empty stomach?

The medication is required to be taken on an empty stomach to prevent a food-mediated increase in the drug's exposure. This means taking the dose at least 30 minutes before or 2 hours after breakfast and the evening meal.


Q: How is Cilostazol eliminated from the body?

The medicine is broken down primarily in the liver. Official documents state that the primary route of elimination for the resulting breakdown products is via the urine (about 74%), with the rest excreted in feces.


Q: Is Cilostazol similar to Pentoxifylline, and how do they differ?

Pentoxifylline is a separate medication that is also used for intermittent claudication. Clinical research referenced by authoritative sources has examined the two agents in relation to walking function.


Q: Does Cilostazol cause any change in vision?

Official documents report less common adverse reactions, including retinal hemorrhage and conjunctivitis (pink eye). These reports indicate the potential for vision- or eye-related effects.


Q: Are stomach upset or nausea common when first starting the drug?

Nausea, vomiting, and abdominal pain are all listed as Common adverse reactions in official documents, meaning they are reported in 1% to 10% of patients. The commonality of these effects includes the period when treatment is initiated.


Q: Are there any specific populations where Cilostazol has been less studied?

Regulatory documents indicate that data for certain patient groups remain insufficient, with limited certainty regarding the long-term effects on major cardiovascular outcomes and the progression of the underlying condition.


Q: Is there a link between Cilostazol and changes in liver function tests?

Yes, official regulatory texts include hepatic dysfunction (poor liver function) and abnormal liver function tests among the documented serious adverse reactions.


Q: How long does it take for side effects like diarrhea to go away after starting Cilostazol?

Diarrhea is listed as a Very Common adverse reaction, occurring in 10% or more of patients. Regulatory documents confirm this high frequency, but do not specify the typical duration or expected resolution time for this side effect.


Q: Is Cilostazol known to cause any skin reactions or rashes?

Yes, official regulatory documents report the occurrence of urticaria (hives) and rash as documented adverse reactions, confirming the potential for skin-related effects.


Q: Does the time of day matter when taking Cilostazol?

Yes, the official dosing instructions require the medicine to be taken twice daily in relation to mealtimes: before or after breakfast and before or after the evening meal.

How should Cilostazol be stored and disposed of?

Cilostazol is a medicine that must be stored and discarded according to official regulatory guidelines to maintain its stability and ensure safety.

Official Storage Requirements

Condition Regulatory Standard
Temperature Store at Controlled Room Temperature, typically 20 C to 25 C (68 F to 77 F), with temporary excursions permitted up to 30 C.
Container Keep the tablets in the original container and ensure it is tightly closed.
Protection Store the container away from excess heat and moisture.
Safety Keep out of the sight and reach of children at all times.

Disposal Instructions

Unused or expired Cilostazol should be disposed of via an authorized drug take-back program where available. The product is not recommended for disposal down the sink or toilet. If take-back options are not accessible, the medication should be mixed with an undesirable substance, sealed in a bag, and then placed in household trash, as specified by government guidelines.

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

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