Dilsatan

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Dilsatan

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 Dilsatan

Dilsatan: What is it?

Property Description
Active ingredient Cilostazol
Form Tablets (Oral preparation)
Pharmacological class Selective Phosphodiesterase 3 (PDE3) Inhibitor
General purpose Improving blood flow and circulation in the extremities
Origin Synthetic compound

Identity and Classification: What Type of Medicine is Dilsatan?

Dilsatan is a prescription-only medicine whose fundamental identity is defined by its active ingredient, Cilostazol, which belongs to the Selective Phosphodiesterase 3 (PDE3) Inhibitor pharmacological class. This classification identifies it as a synthetic compound used in the long-term management of chronic vascular conditions. Cilostazol is used for improving walking ability in patients with circulatory impairment. The distinguishing feature of Cilostazol is its dual-action mechanism, which differentiates it from general antiplatelet agents that lack the strong vasodilatory component.

Composition, Form, and Origin: Is Dilsatan a Natural or Synthetic Compound?

The active core of Dilsatan is the Cilostazol molecule, which is a synthetic compound manufactured through chemical processes, not derived from natural sources. It is formulated as an oral preparation in the standard dosage form of tablets. The preparation is a single active ingredient product, combining Cilostazol with necessary solid pharmaceutical excipients required to create the final tablet structure. This form is intended for reliable, sustained maintenance therapy.

General Purpose: How Does Dilsatan Function at a High Level?

Dilsatan's high-level purpose is to improve overall blood flow by combining two primary actions: widening blood vessels (vasodilation) and reducing the stickiness of blood platelets (antiplatelet action). Cilostazol is primarily utilized for its vascular effects, promoting blood flow, especially to the lower extremities. This integrated circulatory effect is generally intended to relieve the mechanical constraints of chronic vascular impairment, supporting better circulation and oxygenation.

What side effects are possible with Dilsatan?

Possible side effects and safety information

The safety profile of Dilsatan, defined by its active ingredient Cilostazol, is formally categorized by regulatory agencies based on the frequency and type of documented adverse reactions. These classifications are used to structure the understanding of the medicine's risk profile, focusing on affected organ systems and specific populations.


Adverse Reaction Classifications

Adverse reactions are grouped by incidence, according to regulatory standards:

  • Very Common (ge 1/10): Reactions noted at the highest frequency include headache, diarrhea, abnormal stools, and palpitation. These effects often relate to the drug's vasodilatory and gastrointestinal activity.
  • Common (ge 1/100 to < 1/10): This frequency range includes dizziness, tachycardia, peripheral edema, and general gastrointestinal discomfort like nausea and dyspepsia.
  • Rare/Very Rare: This category includes serious events such as severe blood disorders (e.g., aplastic anaemia, agranulocytosis, pancytopenia) and the potential for serious bleeding events, including intracranial hemorrhage.

Adverse reactions are also classified by System-Organ-Classes (SOC), including Cardiac Disorders, Nervous System Disorders, and Blood and Lymphatic System Disorders.


Safety Constraints and Serious Reactions

Official labeling defines critical constraints on the use of Dilsatan. The medicine is contraindicated in patients with congestive heart failure (CHF) of any severity due to the risk of serious cardiac adverse reactions. It is also restricted in patients with severe renal impairment (creatinine clearance le 25 ml/min) and those with moderate or severe hepatic impairment. Additionally, use is restricted in patients with a known predisposition to bleeding (e.g., recent hemorrhagic stroke or active peptic ulceration), reflecting the documented risk of hemorrhage. Adverse reactions are generally observed to be more concentrated within the first month of treatment.

Overdose and Emergency Response

The official regulatory documentation for Dilsatan (Cilostazol) overdose outlines specific signs and mandates immediate emergency actions resulting from excessive pharmacologic effect.

Documented Overdose Manifestations

An overdose may present with an exaggeration of the drug's intended action on the circulatory system. Documented clinical manifestations include severe headache, dizziness, and gastrointestinal distress such as diarrhea. More serious signs involve the cardiovascular system, including a pronounced drop in blood pressure (hypotension), a sustained increase in heart rate (tachycardia), palpitations, and the potential for severe, non-routine changes to heart rhythm, such as cardiac arrhythmias.

When to Seek Immediate Help

Government regulatory guidance specifies that a patient must receive immediate medical attention if more Dilsatan tablets than the prescribed dose are taken. Contact a doctor or local hospital immediately. Furthermore, urgent emergency services (e.g., 911) must be called if the individual exhibits signs of a severe, life-threatening event, including collapse, a seizure, significant trouble breathing, or inability to be awakened.

Official Management and Monitoring

Management of Dilsatan overdose is strictly symptomatic and supportive. Regulatory instructions mandate that the patient should be carefully observed and monitored due to the risk of severe cardiovascular outcomes. Procedures such as induced vomiting or gastric lavage may be employed to aid in stomach emptying, as deemed medically appropriate. Due to the drug's high level of protein binding (95–98%), official documents indicate that the removal of Cilostazol by dialysis is unlikely to be efficient.

Therapeutic Uses of Dilsatan

What Dilsatan Treats: Main Uses and Benefits

Dilsatan is a medication primarily prescribed for the management of cardiovascular conditions. It belongs to a class of drugs known as angiotensin II receptor blockers (ARBs), which work by modulating specific hormonal pathways that regulate blood pressure and fluid balance in the body.

Essential Hypertension

The primary use of Dilsatan is the treatment of essential hypertension, also known as high blood pressure. Hypertension occurs when the force of the blood against the artery walls is consistently too high, which can lead to long-term damage to the heart and blood vessels.

Dilsatan works by blocking the action of angiotensin II, a substance in the body that causes blood vessels to tighten and narrow. By inhibiting this process, the medication helps blood vessels relax and widen, which facilitates easier blood flow and reduces the overall pressure within the circulatory system.

Cardiovascular Protection

Beyond the immediate reduction of blood pressure, Dilsatan is utilized for its role in long-term cardiovascular protection. Reducing high blood pressure is a critical step in lowering the risk of serious health complications, including:

  • Stroke: By maintaining lower pressure levels, the strain on the vessels supplying the brain is reduced.
  • Myocardial Infarction (Heart Attack): Lowering the workload on the heart muscle helps prevent damage over time.
  • Renal Function Preservation: Controlled blood pressure is essential for protecting the small blood vessels in the kidneys, which can be damaged by chronic hypertension.

Therapeutic Benefits

The benefit of Dilsatan lies in its ability to provide sustained blood pressure control throughout a 24-hour period. Because it targets the underlying mechanism of vessel constriction rather than simply slowing the heart rate, it allows for a physiological approach to managing hypertension. This management is a key component in the prevention of chronic heart failure and other vascular diseases associated with prolonged high blood pressure.

Regulatory References

  1. NIH MedlinePlus Drug Information

Eligibility and Restrictions for Use

The official regulatory profile for Dilsatan, which contains Cilostazol, establishes strict eligibility criteria, primarily restricting its use to adult patients with chronic circulatory impairment (peripheral arterial disease).

Populations for Whom Use is Contraindicated

Category Official Regulatory Statement
Cardiovascular Risk Contraindicated in patients with heart failure of any severity, as noted in the FDA's Boxed Warning. European labeling also prohibits use in unstable angina or after a recent myocardial infarction or coronary intervention (within six months).
Bleeding Risk Contraindicated with any active pathologic bleeding or known predisposition to bleeding, such as active peptic ulceration or recent hemorrhagic stroke.
Organ Function Contraindicated in patients with severe renal impairment (creatinine clearance leq 25 mL/min) and moderate or severe hepatic impairment.
Co-Medication Contraindicated for patients receiving two or more additional antiplatelet or anticoagulant agents (e.g., aspirin and clopidogrel).

Age and Reproductive Eligibility

Group Eligibility Status
Pediatric Patients Safety and efficacy have not been established.
Pregnancy Contraindicated (European labeling). In the US, it is classified as Pregnancy Category C.
Lactation Not recommended; a decision must be made to discontinue the drug or discontinue nursing.

Treatment should also be discontinued if a clinically relevant benefit is not observed after three months of use, as stated in regulatory guidelines.

What should I know about interactions with other medicines?

Interactions with other medicines and products

This section outlines documented interactions based on official regulatory information and is not a substitute for professional medical advice.

Dilsatan is principally metabolized by the enzyme Cytochrome P450 3A4 (CYP3A4) and transported by P-glycoprotein (P-gp). It also acts as an inhibitor of CYP2C9 and P-gp, leading to the following officially identified interaction domains:


Interacting Product Category Regulatory Constraint/Requirement
Strong CYP3A4 Inhibitors (e.g., Ketoconazole, Itraconazole) Co-administration is generally not recommended or contraindicated due to significantly increased Dilsatan plasma levels.
Moderate CYP3A4/P-gp Inhibitors (e.g., Erythromycin, Diltiazem) Requires use of a reduced starting dose of Dilsatan to manage systemic exposure.
CYP3A4 Inducers (e.g., Rifampin) Concurrent use is expected to substantially decrease Dilsatan concentrations, which may diminish its documented effect.
CYP2C9 Substrates (e.g., Warfarin) Requires careful monitoring of Prothrombin Time/INR and potential dose adjustment for the co-administered drug due to Dilsatan's moderate inhibition of CYP2C9.
P-gp Substrates (e.g., Digoxin) Requires monitoring of plasma levels for the co-administered drug due to Dilsatan's inhibition of P-gp, which increases the systemic exposure of the substrate.

The overall interaction profile for Dilsatan mandates caution with other medications that significantly affect the CYP3A4 enzyme system or P-glycoprotein transport. This requires either avoidance of certain strong inhibitors or dose adjustments when moderate inhibitors or inducers are co-administered. Additionally, close clinical and laboratory monitoring is necessary when Dilsatan is combined with drugs having a narrow therapeutic index, such as Warfarin and Digoxin.

Mechanism of Action

How Dilsatan Works: Mechanism of Action

Dilsatan exerts its effect through the modulation of key enzyme-mediated signaling pathways within the vascular tissues and blood components. Its mechanistic action results in two primary, distinct physiological consequences. The core mechanism is defined by its influence on the cellular second messenger system.

Dilsatan works by acting as a selective inhibitor of the enzyme Phosphodiesterase Type 3 (PDE3). This enzyme is crucial for hydrolyzing the intracellular signaling molecule cyclic adenosine monophosphate (cAMP) in target cells. By blocking PDE3, Dilsatan prevents the degradation of cAMP, causing its concentration to rise and amplify the downstream signaling cascade.

The resulting high concentration of cAMP produces a dual physiological consequence:

  • Vascular Smooth Muscle Relaxation: Elevated cAMP activates Protein Kinase A (PKA), which inactivates the contractile proteins, leading to smooth muscle relaxation (vasodilation), which manifests as a reduction in vessel tension and increase in vascular lumen size.
  • Anti-Aggregatory Effect: In blood platelets, the boosted cAMP levels limit the cell's responsiveness to aggregating signals. This targeted interference with the platelet signaling pathway reduces the cellular responsiveness to aggregating signals and limits the potential for aggregation.

Dosage and Administration Information

Dilsatan is an oral medicine (Cilostazol) formulated as a tablet. Its administration involves specific parameters concerning dosage, frequency, and timing relative to food intake.

The standard regimen is 100 mg twice daily (bid). This dose serves as the primary maintenance schedule.

Timing and Administration

Dilsatan is taken on an empty stomach to ensure consistent absorption. Each dose is separated from meals by being taken at least 30 minutes before or 2 hours after both breakfast and dinner.

Dose Adjustment for Interactions: A reduced dose of 50 mg twice daily is utilized when the medicine is co-administered with strong inhibitors of the CYP3A4 or CYP2C19 enzymes, such as certain antibiotics or stomach acid-reducing medications.

Treatment Duration and Missed Doses

Treatment is managed as a course with an initial assessment period. The response is reassessed after 3 months of consistent use. If no adequate or beneficial effect is observed on symptoms after this period, the medicine is typically discontinued.

If a scheduled dose is missed, the regular schedule is resumed by taking the next dose at the usual time. Two doses are not taken simultaneously to make up for a missed one.

Special Populations: No specific dose adjustment is required for older adults.

Recent Clinical Evidence

Research Evidence: Overview of Studies


Evidence for Functional Capacity in PAD

Research on Dilsatan explored its use in people with symptomatic Peripheral Arterial Disease (PAD) and intermittent claudication. Studies included numerous short-term, randomized controlled trials (RCTs) and meta-analyses that examined changes in functional capacity. The primary focus was on objective, measurable outcomes, such as the patient's pain-free and maximum walking distances on standardized tests. Studies reported measurements that indicated changes in these walking distances in observed populations compared to placebo groups. These findings describe patterns related to outcomes reflecting daily functioning, typically monitored over defined short-term intervals of 3 to 6 months. Follow-up durations were limited in these core efficacy trials, meaning evidence concerning long-term symptom changes over many years is not fully established.


Post-Revascularization and Research Gaps

Dilsatan was also studied as an add-on therapy following certain vascular procedures like stenting. Research examined outcomes related to the treated blood vessel, specifically the rate of vessel re-narrowing (restenosis) and the need for a repeat procedure (Target Lesion Revascularization). Trials spanning one to two years reported measurements related to these outcomes, with some describing lower rates of vessel re-narrowing compared to controls. The research also monitored certain special populations, such as older adults (ge65 years old) and individuals with diabetes.

A key uncertainty remains the definitive characterization of the drug's long-term effect on major cardiovascular events (heart attack, stroke). The evidence for the effect on reducing these events over time remains limited. Comparative evidence against other studied or comparable treatments is also sometimes lacking across all outcomes.

Key Studies & References

  1. Systematic review and meta-analysis of randomized clinical trials appraising the impact of cilostazol after percutaneous coronary intervention

Frequently Asked Questions (FAQ)

Common questions about Dilsatan (FAQ)

Q: What is the main reason Dilsatan is prescribed?

A: Regulatory documents state that Dilsatan is approved to reduce the symptoms of intermittent claudication—which is leg pain experienced during walking—in individuals who have Peripheral Arterial Disease (PAD).


Q: Is Dilsatan used for blood pressure or just for blood flow issues?

A: The medicine is primarily intended to help with blood flow issues related to Peripheral Arterial Disease. Because the medicine works by relaxing blood vessel muscles (vasodilation), official product information notes that it may also lead to a minor reduction in systolic blood pressure.


Q: How quickly does Dilsatan usually start working for the intended condition?

A: It takes time for the medicine to achieve its full response to symptoms. Official regulatory guidelines indicate that a patient's response is formally evaluated after a period of 3 months of consistent use.


Q: What happens if a person stops taking Dilsatan suddenly?

A: Observations from clinical studies indicated that the improvement in walking distance experienced by patients was lost when the treatment was discontinued. The medicine’s effect is generally reversed when use is stopped.


Q: Is a headache a common side effect of Dilsatan?

A: Yes, headache is reported with high frequency. Official product safety data categorizes headache as a 'Very Common' side effect, meaning it has been noted in one out of every 10 people or more in clinical studies.


Q: Can Dilsatan cause changes in sleep patterns or insomnia?

A: Yes, official adverse event reports list insomnia (difficulty falling or staying asleep) as a reported side effect of the medicine.


Q: Does Dilsatan have any known food or drink interactions, like with grapefruit juice?

A: Official information specifically states that taking Dilsatan alongside grapefruit juice is generally not recommended. This is due to the expectation that grapefruit juice significantly increases the systemic exposure of Dilsatan, requiring caution.


Q: Is it safe to take Dilsatan with over-the-counter pain relievers like ibuprofen or acetaminophen?

A: Official warnings emphasize the need for caution when Dilsatan is co-administered with other antiplatelet or anticoagulant medicines. The concomitant use of these categories of medication carries a potential increase in the risk of bleeding events.


Q: Does Dilsatan have potential interactions with common supplements or herbal products?

A: Dilsatan is processed by specific liver enzymes (CYP3A4 and CYP2C19). If any herbal or supplement product is known to strongly affect these enzymes, it may change the levels of Dilsatan in the body. The decision to use Dilsatan with any specific herbal or supplement product should be discussed with a healthcare provider.


Q: Is Dilsatan safe to use during pregnancy?

A: Safety has not been definitively established for use during human pregnancy. Because official regulatory authorities generally advise against its use during this time, alternative options may be considered.


Q: Can Dilsatan be safely used by women who are breastfeeding?

A: It is not known whether Dilsatan is transferred into human breast milk. Due to the unknown effects this may have on the infant, official documentation states that a decision must be made to either discontinue nursing or discontinue the drug.


Q: Does Dilsatan affect blood sugar levels, which would be a concern for people with diabetes?

A: Official safety data includes reported adverse events of increased blood sugar levels. Official documentation notes that monitoring of blood glucose levels may be necessary for individuals with diabetes.


Q: Does Dilsatan interact with medications used for acid reflux or heartburn?

A: Official product information notes that certain strong inhibitors of the CYP2C19 enzyme—including some stomach acid-reducing medicines—can interact with Dilsatan. Official prescribing information mandates that when taken together, Dilsatan requires a dosage adjustment.


Q: How does Dilsatan affect a person's ability to drive or operate machinery?

A: Official warnings note that due to side effects such as dizziness, caution is advised regarding activities requiring full mental alertness, such as driving or operating machinery.


Q: Is Dilsatan a medicine that requires regular blood tests or monitoring?

A: Yes, official regulatory information indicates that regular monitoring of complete blood counts (also called a full blood count) may be necessary. This is especially important if infection or any signs of blood abnormality are suspected.


Q: What types of medications are listed as major interactions with Dilsatan?

A: Official documentation identifies strong inhibitors of the CYP3A4 enzyme as having a major interaction. These include certain antifungal medications, and co-administration with these types of medicines is restricted or considered contraindicated by regulatory bodies.


Q: Can taking Dilsatan cause joint or muscle pain?

A: Official safety data includes reports of arthralgia (joint pain) as an adverse event. Additionally, bone pain has also been reported in official documents.


Q: Can Dilsatan cause skin rashes or itching?

A: Official adverse event reports include several skin-related reactions. These reactions include reports of general skin rash, pruritus (itching), and urticaria (hives).


Q: Does Dilsatan interact with common anti-depressant or anxiety medications?

A: The medicine interacts with the liver's CYP450 enzyme system. If an anti-depressant or anxiety medication is known to strongly inhibit the CYP3A4 or CYP2C19 enzymes, the regulatory guidelines specify that a dosage adjustment may be necessary for Dilsatan.


Q: Is Dilsatan safe to take if I am scheduled for surgery or a dental procedure?

A: Due to the antiplatelet effect of Dilsatan and its potential to increase the risk of bleeding, caution is necessary before any procedure. Guidance on the temporary interruption of Dilsatan before a procedure is usually determined by the treating healthcare provider.


Q: What is the official information regarding Dilsatan and its effect on bone health?

A: Official safety data includes reports of bone pain as an adverse event in a small number of patients.


Q: Does Dilsatan increase or decrease the effect of other medications?

A: Dilsatan is described as an inhibitor of the CYP2C9 enzyme and the P-glycoprotein (P-gp) transporter. This can potentially increase the systemic exposure and effects of other medicines that rely on these two systems for processing or transport.


Q: How long does Dilsatan stay in the body after the last dose?

A: The time it takes for the amount of medicine in the body to be reduced by half—known as the terminal elimination half-life—is approximately 11 to 13 hours, according to official pharmacokinetics data.


Q: Why is Dilsatan sometimes used alongside another medicine?

A: In certain medical contexts, such as after specific vascular procedures, research has examined Dilsatan as an add-on therapy. This approach reflects the drug’s established effects of promoting vasodilation and reducing platelet aggregation.


Q: Do you need to take Dilsatan with food, or does it matter?

A: Official regulatory guidance is specific on this point: Dilsatan should be taken on an empty stomach. This means taking it at least 30 minutes before or 2 hours after a meal to ensure the amount of medicine absorbed into the body remains consistent.

How should Dilsatan be stored and disposed of?

Storage Conditions and Requirements

Dilsatan (Cilostazol tablets) must be stored at Controlled Room Temperature, defined by regulators as 25 C (77 F), with allowed temperature excursions between 15 C and 30 C (59 F and 86 F). The product must be protected from environmental extremes; it should be kept away from excess heat and moisture, and it must not be frozen. For stability, the medicine must be kept in its original container, which should be tightly closed.

Child-Safety and Disposal Rules

It is an official requirement that Dilsatan tablets must be stored out of the sight and reach of children; using a locked safety cap and placing the product in a secure location is mandatory. For disposal, the medicine should not be thrown away in household waste or wastewater. Expired or unused tablets should be disposed of by taking them to a dedicated medicine take-back program or following specific instructions from the pharmacist in accordance with local and national regulations.

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

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