Antiplat

Quick links to important sections

Antiplat

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 Antiplat

This foundational section defines the core identity of Antiplat, establishing its composition, class, and general mechanism without detailing clinical applications or usage instructions.


Quick Facts

Property Description
Active ingredient Cilostazol
Form Oral tablets
Pharmacological class Phosphodiesterase Type 3 (PDE3) Inhibitor, Antiplatelet agent
General use Supports improved peripheral circulation
Origin Synthetic compound (Quinolinone derivative)

Antiplat: Definition and Core Identity

Antiplat is a prescription-only synthetic medicine supplied as an oral dosage form (tablets), containing the single active pharmaceutical ingredient, Cilostazol. The substance is chemically identified as a quinolinone derivative, a structure that confirms its origin as a chemically synthesized compound. The primary function of Cilostazol is to support and improve blood circulation in the body, which is a pharmacological property of the substance. The drug is designed for systemic absorption following ingestion, differentiating it from topical preparations.


Pharmacological Classification and Composition

Antiplat belongs to the distinct class of Phosphodiesterase Type 3 (PDE3) Inhibitors, which is its central mechanism of action, and is concurrently categorized as an Antiplatelet agent. The product contains only Cilostazol as its active component, making it a single-ingredient product, and is formulated with solid excipients suitable for oral administration. The specific inhibition of the PDE3 enzyme regulates internal cellular signaling, which is key to achieving its subsequent beneficial effects on the vascular system. Cilostazol's pharmacological actions involve both antiplatelet and vasodilatory properties, providing a unique dual benefit to the vascular system.


General Purpose and Action Principle

The general purpose of Antiplat is to promote better and more sustained blood flow by reducing resistance within the peripheral arteries. This support for circulation addresses issues related to restricted blood flow in the extremities. This is achieved through a dual action: vasodilation (widening of the blood vessels) and the inhibition of specific blood cell aggregation. By combining these two effects, Cilostazol supports improved circulation, a beneficial function for individuals requiring vascular support. This medicine works to facilitate smoother, less obstructed movement of blood throughout the affected arteries.

What side effects are possible with Antiplat?

Possible Side Effects and Safety Information

The safety profile of Antiplat is strictly based on data documented in governmental regulatory sources, such as FDA Prescribing Information and the EMA Summary of Product Characteristics (SmPC). The most prominent safety concern is the risk of bleeding.

Adverse Reactions by Frequency and System-Organ Class

Adverse reactions are formally categorized based on their incidence:

  • Very Common (Affecting 1 in 10 or more): Hemorrhage/Bleeding (e.g., minor bleeding events).
  • Common (Affecting 1 in 100 to less than 1 in 10): Non-major bleeding events, gastrointestinal disturbances (e.g., dyspepsia, diarrhea), and epistaxis.
  • Uncommon (Affecting 1 in 1,000 to less than 1 in 100): Gastrointestinal ulcers, thrombocytopenia, and rash.

Serious Adverse Reactions

The following are designated by regulators as rare but clinically critical events:

  • Major Hemorrhage: Includes life-threatening or fatal events such as Intracranial Hemorrhage and severe gastrointestinal bleeding.
  • Thrombotic Thrombocytopenic Purpura (TTP): A potentially fatal condition characterized by blood cell changes, which is explicitly noted in official warnings.

Safety Constraints and Population Notes

The official labeling defines specific restrictions and necessary precautions:

  • Contraindications: Antiplat is strictly contraindicated in patients with active pathological bleeding (e.g., peptic ulcer) and in those with severe hepatic impairment.
  • Surgical Use: Regulatory guidance requires the medicine to be temporarily discontinued (typically 5 to 7 days) prior to elective surgery that poses a major risk of bleeding.
  • Geriatric Use: An increased risk of major bleeding is explicitly documented in certain older adult populations (e.g., those 75 years and older), requiring caution or alternative dosing based on the regulatory label. Note: Premature discontinuation of Antiplat can increase the risk of serious cardiovascular events.

Overdose and Emergency Response

Antiplat Overdose and when to seek help

Overdose with Antiplat (Cilostazol) may present with manifestations consistent with an exaggerated level of its pharmacological effects, as described in regulatory documents. The documented clinical signs include severe headache, dizziness, diarrhea, and syncope (fainting). Critically, overdose can lead to signs of severe cardiovascular toxicity, such as tachycardia (fast heart rate), palpitation, and profound hypotension (low blood pressure), which represent the serious outcomes reported in regulatory labeling.


Immediate Action Required

If an overdose is suspected, seek emergency medical treatment right away. Immediate contact with emergency services is mandated if the affected individual has collapsed, had a seizure, has trouble breathing, or can't be awakened. Guidance should also be sought from a Poison Control Center.


Management and Monitoring

Management of an overdose involves general symptomatic and supportive measures, as no specific antidote is known. Close observation and continuous monitoring are required, with the primary focus directed toward assessing for signs of cardiovascular toxicity. Procedural steps, such as considering gastric lavage or administration of activated charcoal, may be initiated soon after ingestion to reduce systemic absorption.

Therapeutic Uses of Antiplat

What Antiplat Treats: Main Uses and Benefits

Antiplat (Cilostazol) is generally used to address symptoms related to physical discomfort and conditions presenting with systemic or localized discomfort. The medication is applied across therapeutic domains where additional symptomatic support is needed.

Symptomatic Relief for Restricted Peripheral Blood Flow

Antiplat is commonly used to help with the symptoms of intermittent claudication, a condition characterized by exertional leg pain. The indications for use include intermittent claudication and supporting specific patient groups who require vascular stability. This is applied in addressing symptoms that become more disruptive during flare-ups of activity and are associated with acute or episodic changes.

Improving Functional Mobility and Walking Capacity

The core therapeutic benefit may assist with improving day-to-day comfort during periods of heightened symptoms associated with walking. This action addresses functional mobility limitations and contributes to easing the overall symptom load that interferes with routine activities.

Use in Secondary Vascular Event Prevention

The medicine may be part of symptomatic management in other clinical settings, notably being considered relevant for supporting stability in patients following a non-cardioembolic stroke or transient ischemic attack (TIA).


Therapeutic Quick Reference

Focus Description
Primary Indication Intermittent Claudication
Symptom Relieved Pain, cramping, or weakness in legs caused by walking
Core Benefit Helps improve day-to-day comfort during symptomatic periods
Clinical Context Applied in chronic symptomatic episodes

Regulatory References

  1. MedlinePlus Drug Information

Eligibility and Restrictions for Use

Eligibility Profile: Official Regulatory Information

Antiplat is intended for use in adult patients. Eligibility is strictly governed by a series of absolute exclusions derived from official regulatory documents. Use is primarily restricted due to the potential for adverse effects related to the heart and blood clotting function, rather than general safety summaries.


Contraindicated Populations (Must Not Use) Regulatory Status
Heart Failure (of any severity) CONTRAINDICATED (FDA Boxed Warning)
Severe Renal Impairment (CrCl le 25 mL/min) CONTRAINDICATED
Moderate or Severe Hepatic Impairment CONTRAINDICATED
Pregnancy and Lactation CONTRAINDICATED
Recent CV Events (MI/PCI within 6 months) CONTRAINDICATED
Concomitant use of ge 2 additional antiplatelet/anticoagulant agents CONTRAINDICATED
Patients with any known predisposition to bleeding (e.g., active ulceration) CONTRAINDICATED

Population-Specific Limitations

  • Pediatric Use: Safety and efficacy have not been established in children.
  • Organ Function: Patients with mild hepatic or renal impairment may be eligible, as no dosage adjustment is necessary for these conditions.

Connection to the overall eligibility profile: The official regulatory structure defines who can and cannot use Antiplat almost entirely through absolute exclusions, which mandate non-eligibility based on pre-existing cardiac instability, specific organ function thresholds, or a heightened risk of hemorrhage.

What should I know about interactions with other medicines?

Interactions with other medicines and products

The official interaction profile of Antiplat (Cilostazol) is defined by its antiplatelet activity and metabolism, establishing mandatory constraints documented by government regulatory sources.


Interaction Scope

Property Description (Strictly Regulatory-Based)
Medicinal product categories with documented interactions: Antiplatelet agents, Anticoagulant agents, Strong/Moderate CYP3A4 Inhibitors, CYP2C19 Inhibitors.
Mechanistic basis of interactions: Inhibition of hepatic CYP3A4 and CYP2C19 (Pharmacokinetic); Additive inhibition of platelet function (Pharmacodynamic).
Timing-based interaction rules: Must be administered on an empty stomach (30 minutes before or 2 hours after meals) due to documented increased exposure with food.
Interaction-related restrictions: Contraindicated with two or more additional antiplatelet or anticoagulant agents. Avoid concurrent use of Grapefruit Juice.

Interaction Classifications (High-Level)

Property Classification (Strictly Regulatory-Based)
Interaction severity classification: Contraindicated Combinations (e.g., Two or more antiplatelet/anticoagulants; Heart Failure of any severity). Clinically Significant Interactions (CYP inhibitors).
Population-specific interaction notes: Severe Renal Impairment alters protein binding. Caution advised in Moderate or Severe Hepatic Impairment due to lack of study data.

Resulting Interaction Structure

Official interaction statements:

  • Co-administration with CYP3A4 or CYP2C19 inhibitors (e.g., Erythromycin, Diltiazem, Omeprazole) results in a significant increase in systemic exposure of Antiplat and/or its active metabolites.
  • Additive pharmacodynamic effects occur with other agents that inhibit platelet function or coagulation, officially increasing the risk of haemorrhagic events.
  • The formal constraint of taking Antiplat with CYP enzyme inhibitors requires a procedural dose adjustment to manage exposure.

The regulatory documents establish Antiplat's interaction structure based on mandatory restrictions for pharmacodynamic and pharmacokinetic interactions, defining which combinations are contraindicated and when procedural adjustments are required to manage increased systemic exposure.

Mechanism of Action

Enzyme Inhibition and the cAMP Signaling Cascade

Antiplat (Cilostazol) executes a dual pharmacodynamic mechanism centered on the selective inhibition of the Phosphodiesterase Type 3 ( PDE3) enzyme. This enzyme is critically expressed in vascular smooth muscle cells ( VSMC) and platelets. By blocking PDE3, the drug prevents the breakdown of the intracellular messenger cyclic adenosine monophosphate ( cAMP), causing a subsequent increase in its concentration. This elevated cAMP level initiates a signaling sequence that governs the drug's effects.


Modulation of Arterial Tone and Fluidity

This cAMP increase leads to two primary physiological changes. In VSMCs, the cascade causes muscle relaxation, resulting in peripheral arterial vasodilation (widening of the vessels) and reduced resistance. Concurrently, in platelets, the cAMP elevation suppresses activation signals, which leads to the inhibition of aggregation (clustering). This combined action of vessel widening and reduced cellular obstruction results in a reduction of peripheral vascular resistance and cellular clustering.


Inherent Mechanistic Constraint

The mechanism of PDE3 inhibition introduces a physiological constraint due to the enzyme's expression in cardiac tissue. The resulting cAMP elevation in the heart can cause an increase in cardiac contractility and heart rate.

Dosage and Administration Information

How to Use Antiplat: Official Administration Guidelines

Antiplat (Cilostazol) is an oral medication supplied as tablets in two standard strengths, 50 mg and 100 mg. The official instructions for use are governed by precise rules regarding route, frequency, timing with meals, and dose adjustment, ensuring proper systemic absorption of the drug.


Core Administration Protocol

The medicine is intended for use twice daily (b.i.d.) on a consistent schedule. The standard recommended adult dose for the main indication is 100 mg taken twice daily. Standard guidelines specify that this regimen should be maintained for at least three months before a decision is made to discontinue the treatment if insufficient symptomatic improvement is observed.

Timing and Dosage Adjustments

Proper use dictates that Antiplat must be taken on an empty stomach. This means the tablet must be administered either at least 30 minutes before or 2 hours after both the morning and evening meals. This specific timing is required to prevent an undesirable increase in the blood concentration of the drug, which occurs if taken with food.

Specific dosage changes are mandated when certain other medicines are co-administered. If the patient is concurrently taking strong or moderate inhibitors of the CYP3A4 or CYP2C19 enzymes, the Antiplat dose must be reduced to 50 mg twice daily. Furthermore, the official protocol advises against consuming grapefruit juice, as it may affect the drug's metabolism. In cases of a missed dose, the patient should simply skip the forgotten dose and return to the normal schedule with the next planned dose, without taking a double amount.

Recent Clinical Evidence

Research Evidence / Overview of Studies for Antiplat

Evidence for Use in Intermittent Claudication

The body of research for Antiplat includes numerous placebo-controlled Randomized Controlled Trials (RCTs). These trials involved comparing the observations of Antiplat against an inactive substance (placebo) in similar groups of patients. Research explored how symptoms change over time, with studies aiming to measure changes in walking ability in participants who are adults with Peripheral Artery Disease (PAD). The main focus was on outcomes reflecting daily functioning or activity level, specifically the standardized distance a person could walk before pain began, and the maximum total distance they could walk.

The initial short-to-intermediate term trials, generally lasting between 12 and 24 weeks, reported measurements of change in both pain-free walking distance and maximum walking distance in the group receiving Antiplat compared to the placebo group. Research highlights changes measured during the study period, which were generally noted in the primary regulatory studies. The body of evidence for this indication includes multiple RCTs focusing on functional measures, and is broadly supported by the available data.


Research in Secondary Vascular Event Prevention

Research also examined Antiplat for a different context: evaluation in patients who had experienced a prior non-cardioembolic stroke or Transient Ischemic Attack (TIA). The evidence for this use was primarily evaluated in large, long-term Randomized Controlled Trials (RCTs) that often spanned one to five years of observation. These studies explored whether taking Antiplat was associated with differences in the rate of recurrent vascular events, such as a second stroke.

Studies monitored outcomes related to systemic or functional imbalance by focusing on major event recurrence. Findings describe patterns related to the rate of stroke recurrence in the groups receiving Antiplat within the specific populations studied. However, it is important to note that the largest and most influential trials supporting this area were predominantly conducted in Asian populations.


Uncertainty and Gaps in the Research Record

Despite the body of RCTs for Intermittent Claudication, the long-term effects are not fully established regarding the maintenance of functional changes or the overall impact on major clinical endpoints like heart attack or stroke in this population. In the area of secondary stroke prevention, while the large trials provided data, the fact that the results apply only to the populations studied means that comparative evidence is lacking for broader global use. Studies contribute to the broader evidence landscape, but current findings describe group patterns, not personal outcomes, and research does not determine whether an individual will respond similarly.

Frequently Asked Questions (FAQ)

Common questions about Antiplat (FAQ)


Q: What is Antiplat used for?

Antiplat is a prescription medication approved for use in patients who have peripheral artery disease (PAD). Its main purpose, based on regulatory approvals, is to help relieve the symptoms of leg pain or cramping—a condition known as intermittent claudication—that occurs while walking.


Q: How long do I have to take Antiplat before it works?

Regulatory data indicates that improvement in walking symptoms may begin within 2 to 4 weeks after starting treatment. However, the full expected benefit, such as a significant increase in the distance a patient can walk without pain, may take up to 12 weeks (three months) to be observed.


Q: Who should NOT take Antiplat (contraindications)?

Official drug documents state that this medicine is strictly contraindicated (must not be used) in patients with certain conditions. These include heart failure of any severity, active pathological bleeding (such as a peptic ulcer), severe kidney or moderate to severe liver impairment. The medicine is also contraindicated if a patient is concurrently taking two or more additional blood thinner or antiplatelet medications.


Q: Where in the body does Antiplat primarily work?

Antiplat is designed to support peripheral circulation. It primarily works in the arteries of the body by performing a dual action. It helps relax the blood vessel walls (vasodilation) and helps prevent blood cells from clustering together (antiplatelet action), which is intended to improve overall blood flow.


Q: What are the symptoms of a serious allergic reaction to Antiplat?

A serious allergic reaction is possible but rare. If symptoms such as hives, significant swelling of the face, lips, tongue, or throat, or sudden difficulty breathing occur, emergency medical attention may be required. These signs are listed in official drug information.


Q: How long does Antiplat stay in your system after you stop taking it?

Official pharmacological data indicates that the elimination half-life of the active ingredient (Cilostazol) is approximately 11 to 13 hours. The half-life is the time it takes for the amount of drug in the body to be reduced by half. A drug is generally considered cleared from the body after four to five times its half-life.


Q: What is the chemical name of the active ingredient?

The active ingredient in Antiplat is Cilostazol. Its formal chemical name, as defined in regulatory and scientific registries, is 6-[4-(1-Cyclohexyl-1H-tetrazol-5-yl)butoxy]-3,4-dihydro-2(1H)-quinolinone.


Q: Can Antiplat cause an irregular or fast heart rate?

Yes, official safety information states that an increased heart rate (tachycardia) or a pounding or irregular heartbeat (palpitations) are reported as common side effects. Due to the drug’s mechanism of action, it may cause a small, expected increase in heart rate in some patients.


How should Antiplat be stored and disposed of?

The official storage and disposal requirements for Antiplat (Cilostazol) tablets are strictly defined in regulatory documents to ensure product stability.

Storage Requirements

The tablets must be stored at Controlled Room Temperature, specifically between 20 C and 25 C (68 F and 77 F). The product must be protected from excess heat, moisture, and freezing (Do not freeze). Keep the medication in the original container and ensure the container is tightly closed.

For safety, the tablets must be kept out of the sight and reach of children.

Disposal Instructions

Expired or unused Cilostazol must not be thrown away via wastewater or household waste, as specified in regulatory labeling. To protect the environment, the official instruction is to ask a pharmacist or healthcare professional for the proper local disposal procedure.

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

Available in countries:

Equivalent of Antiplat found in:

A-Z Index: