Tilor

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Tilor

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Medically reviewed

Laura Arias

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 Tilor

What is Tilor?

Tilor is a pharmacological agent primarily categorized as an antiviral medication and an interferon inducer. It belongs to the class of low-molecular-weight synthetic compounds known as fluorenones. In clinical practice, it is utilized to stimulate the body's natural production of interferons—proteins that play a critical role in the immune system's response to viral infections.

Mechanism of Action

The primary function of Tilor is to trigger the synthesis of alpha, beta, and gamma interferons. These proteins are produced by various cells, including intestinal epithelial cells, hepatocytes, and T-lymphocytes. By increasing the levels of these interferons, the medication helps the body inhibit the replication of viruses and enhances the overall immune response. This process is often referred to as immunomodulation.

General Characteristics

  • Type: Synthetic interferon inducer.
  • Formulation: Typically available as a tablet for oral administration.
  • Therapeutic Goal: To support the immune system in identifying and neutralizing viral pathogens.

Common Applications

Tilor is often associated with the management of various viral conditions. These may include:

  • Respiratory viral infections such as influenza.
  • Viral hepatitis.
  • Herpetic infections.
  • Cytomegalovirus infections.

In some contexts, it is also used as part of a comprehensive approach to managing certain types of encephalomyelitis or chlamydial infections, where an immune-supportive component is considered beneficial.

What side effects are possible with Tilor?

The safety profile of Tilor, whose active ingredient is Cilostazol, is based on adverse reactions and classifications documented in government regulatory sources, such as FDA and EMA labels.

Adverse Reaction Scope

Adverse reactions are classified by frequency from clinical trials, with the most frequently reported effects involving the nervous system and gastrointestinal tract.

Frequency Category Representative Adverse Reactions System-Organ Class Involved
Very Common (ge 10%) Headache, Diarrhea Nervous System, Gastrointestinal
Common (1% to <10%) Abnormal stools, Palpitation, Dizziness, Tachycardia Gastrointestinal, Cardiac, Nervous System

Serious Adverse Reactions and Safety Restrictions

The regulatory label documents the potential for serious, though less common, events. These include major Hemorrhagic Events (such as intracranial or gastrointestinal hemorrhage) and rare, severe Blood Dyscrasias (including Agranulocytosis or Aplastic anaemia) [Source 1.2, 2.3]. Cardiac events like Heart failure, Myocardial infarction, and Ventricular tachycardia are also documented as serious adverse reactions [Source 1.3, 2.3].

Contraindications define absolute limitations on the use of Tilor and are formally established in official labeling [Source 1.5, 2.3]:

  • Congestive Heart Failure (CHF): Tilor is strictly contraindicated in patients with CHF of any severity [Source 1.5].
  • Severe Organ Impairment: Contraindicated in patients with severe renal impairment or moderate to severe hepatic impairment [Source 2.4].
  • Bleeding Risk: Contraindicated in patients with any known predisposition to bleeding or concurrent use with two or more additional antiplatelet/anticoagulant agents [Source 2.4].

Contextual Safety Notes

Adverse reactions are often concentrated within the first month of treatment [Source 1.8]. Tilor typically causes a small but measurable increase in heart rate [Source 1.5]. Patients receiving strong inhibitors of CYP3A4 or CYP2C19 enzymes require a dose reduction to minimize the risk of increased exposure and subsequent adverse effects [Source 1.5].

Connection to the Overall Safety Profile

These official classifications and contraindications define the safety boundaries of the medicine, emphasizing risks related to bleeding and cardiovascular function. The absolute prohibition against use in congestive heart failure establishes a central constraint on the drug's use, as documented in governmental regulatory information [Source 1.5, 2.3].

Overdose and Emergency Response

Tilor Overdose and When to Seek Help

The official regulatory documents specify that Tilor (Cilostazol) overdose manifests as an exaggeration of its known pharmacological effects.

Domain Documented Overdose Statement
Documented Manifestations Symptoms include severe headache, dizziness, diarrhea, palpitation, and hypotension (low blood pressure).
Physiological Systems Affected Primarily the Cardiovascular System (leading to arrhythmias, tachycardia) and the Gastrointestinal System.
Emergency-Response Statement Treatment is strictly symptomatic and supportive. There is no specific antidote known according to official labeling.

Overdose Classifications

Classification Type Regulatory Statement
Severity Cardiovascular manifestations are the most critical potential severe outcomes, specifically cardiac arrhythmias and tachyarrhythmia.
Overdose-Context The official guidance mandates that management be focused on supporting the patient's vital functions and managing symptomatic presentation.

Official Emergency Actions

  • Seek immediate medical attention for any suspected overdose.
  • Contact a Poison Control center immediately.
  • Call emergency services if the affected person has collapsed, had a seizure, has trouble breathing, or cannot be awakened.

Connection to the Overall Overdose Profile: The regulatory documents define the overdose profile by highlighting the risk of excessive cardiovascular changes, such as hypotension and tachyarrhythmia, which directly mandate the required emergency actions. The official instructions strictly define the conditions under which immediate medical help is necessary (collapse, seizure, respiratory distress), confirming that management is focused solely on supportive treatment due to the lack of a known specific antidote.

Therapeutic Uses of Tilor

What Tilor Treats: Main Uses and Benefits

Tilor is commonly used across therapeutic domains where additional symptomatic support is needed, particularly for conditions associated with acute or disruptive episodes and physiological stress. The substance is used within therapeutic areas involving symptomatic relief for viral diseases, including influenza and acute respiratory viral infection (ARVI). The therapeutic approach is relevant for addressing groups of symptoms that may appear suddenly or intensify over time.

Symptomatic Relief and Patient Support

This medication is applied in clinical settings that involve acute or unstable symptom patterns related to systemic imbalance, such as high fever, chills, muscle aches (myalgia), and headaches. It supports patients during difficult episodes by easing distress and may assist with maintaining functional stability when symptoms are more noticeable. The medication is used for managing symptoms like fever and muscle pain that commonly interfere with daily functioning.

“The medication helps address symptom clusters that may become intense or disruptive, contributing to improved comfort during symptomatic periods.”


Quick Fact: Supportive Relief for Systemic Discomfort

Quick Fact: Supportive Relief for Systemic Discomfort. Tilor is relevant when symptoms create noticeable physiological strain, and may assist with the overall symptom load during acute phases.

Eligibility and Restrictions for Use

Tilor (Cilostazol) is permitted for use only in adults who are managing Intermittent Claudication symptoms and only when non-pharmacological interventions, such as supervised exercise and lifestyle changes, have failed to provide adequate benefit (second-line use).


Contraindicated Populations

Official regulatory labeling dictates that Cilostazol must not be used in patients with the following conditions:

  • Cardiovascular Conditions: Heart failure of any severity, unstable angina pectoris, myocardial infarction or coronary intervention within the last six months, or a history of severe tachyarrhythmia or QTc interval prolongation.
  • Bleeding Risk: Any known predisposition to bleeding, including active peptic ulceration, recent hemorrhagic stroke (within six months), or poorly controlled hypertension.
  • Organ Impairment: Severe renal impairment (creatinine clearance leq 25 ml/min) or moderate or severe hepatic impairment.
  • Concomitant Use: Patients receiving two or more additional antiplatelet or anticoagulant agents (e.g., aspirin and clopidogrel).
  • Pregnancy: Use is contraindicated during pregnancy.

Age and Restriction Status

Population Group Regulatory Status
Pediatric Population Safety and efficacy have not been established
Lactation (Breastfeeding) Use is restricted; a decision to discontinue nursing or discontinue the medicine is required.

Official regulatory documents define the eligible population as adults with stable intermittent claudication who are free from these absolute cardiac, hepatic, renal, or bleeding risk contraindications. Use is further restricted when taken with strong enzyme inhibitors (CYP3A4/CYP2C19).

What should I know about interactions with other medicines?

Pharmacokinetic and Exposure Interactions

The official interaction profile for Tilor (Cilostazol) highlights a reliance on the CYP3A4 and CYP2C19 enzyme systems for metabolism. Co-administration with strong or moderate inhibitors of these enzymes results in increased systemic exposure. For instance, the use of a strong CYP3A4 inhibitor, such as Erythromycin, is documented to raise Cilostazol's overall exposure (AUC) by approximately 73%. This established pharmacokinetic constraint requires consideration of a dose modification when such inhibitors are prescribed concurrently.

Pharmacodynamic Restrictions

The most stringent interaction constraint is based on additive pharmacodynamic effects. Co-administration with two or more additional antiplatelet or anticoagulant agents (e.g., Warfarin, Clopidogrel) is formally contraindicated. This prohibition is explicitly documented in regulatory labeling due to the risk of compounded anti-clotting activity and an increased potential for bleeding. Caution is also noted for co-use with hypotensive agents, as this may result in an additive effect on blood pressure reduction.

Administration and Clearance Constraints

The timing of administration is tied to documented interactions with food. Tilor must be taken 30 minutes before or 2 hours after both breakfast and dinner, as high-fat meals are noted to increase the drug's absorption. Consumption of Grapefruit juice must be avoided, as it is documented to increase the drug's plasma concentration by about 50%. The drug is also formally contraindicated in patients with severe hepatic or severe renal impairment, a restriction directly related to the safe management of drug and metabolite clearance in these specific populations.

Mechanism of Action

Dual Modulation via Selective PDE3 Inhibition

Tilor's mechanism begins at the molecular level with the selective and reversible inhibition of the Phosphodiesterase type 3 (PDE3) enzyme, a target found in both vascular smooth muscle cells (VSMCs) and platelets. By blocking PDE3, the drug prevents the breakdown of the critical intracellular messenger cyclic Adenosine Monophosphate (cAMP). The resulting elevated cAMP levels then activate Protein Kinase A (PKA), initiating the primary dual-action cascade that modulates two key physiological systems: vascular tone and platelet activity.


The Antiplatelet and Vasodilatory Cascade

The increase in cAMP/PKA activity yields two complementary physiological effects. In VSMCs, this cascade leads to the phosphorylation and inhibition of Myosin Light-Chain Kinase (MLCK), which causes the muscle cells to relax, resulting in arterial vasodilation. Simultaneously, in platelets, the same signaling sequence inhibits the aggregation process, reducing their tendency to cluster and form obstructions. This synergy of reducing vessel resistance while limiting cellular blockage is the core mechanism that achieves increased peripheral blood flow in the peripheral vascular bed.

Dosage and Administration Information

How to Use Tilor

The administration of Tilor follows a protocol focusing on dosage, frequency, and timing relative to meals. The medicine is for oral administration as a tablet.

Official Dosing and Administration

Instruction Detail
Route of Administration Oral administration only.
Standard Dosing Schedule The standard maintenance dose is 100 mg taken twice daily (b.i.d.). A reduced dose of 50 mg twice daily is also used in specific circumstances.
Timing in Relation to Meals Dosing must occur on an empty stomach. This is defined as taking the tablet at least 30 minutes before or 2 hours after both breakfast and dinner.
Required Dose Adjustment When Tilor is used concurrently with certain medications that inhibit the CYP3A4 or CYP2C19 enzymes (e.g., diltiazem, omeprazole), the dose is reduced to 50 mg twice daily.

Use Over Time and Population Rules

Treatment duration is characterized by an initial period before full assessment. Patients may require up to 12 weeks of continuous therapy before the full benefit is realized. If no clinically relevant improvement is observed after 3 months of use, the medicine should be discontinued.

Regarding specific populations, no special dosage adjustments are required for older adults with normal kidney and liver function. Furthermore, dose adjustment is not necessary for patients with mild renal impairment (creatinine clearance > 25 ml/min) or mild hepatic impairment. Safety and efficacy have not been established for the pediatric population.

Recent Clinical Evidence

Evidence for Use in Intermittent Claudication

The primary research for Tilor (Cilostazol) was studied for intermittent claudication, the muscle pain associated with Peripheral Artery Disease (PAD). This condition is marked by functional limitations and outcomes related to physical discomfort. Studies explored this area by relying on multiple Randomized Controlled Trials (RCTs) and Systematic Reviews to provide a broader view of the evidence landscape.

In these trials, studies monitored functional outcomes, specifically the distance patients could walk pain-free and the total maximum distance they could cover. Research examined how symptoms evolved in the observed populations during the study period, typically lasting 12 to 24 weeks. Studies reported measurements of functional outcomes, and the findings described patterns observed in the studies when compared to placebo. Research also examined patient-reported outcomes describing perceived discomfort and changes in health-related quality of life.

Research Gaps and Uncertainties

The research included diverse adult populations, often examining patients with co-existing conditions such as diabetes or hypertension. However, the follow-up durations were limited in these primary efficacy trials. According to systematic reviews, the most significant limitation is the lack of statistical power and consistent evidence regarding outcomes related to systemic or functional imbalance, such as rates of amputation, cardiovascular events, and all-cause mortality.

While research findings consistently describe patterns related to functional outcomes, the long-term effects on clinical endpoints or preventing critical events are not well characterized. Evidence quality varies across studies, and the certainty remains low for some patient-reported measures due to inconsistent reporting.

Frequently Asked Questions (FAQ)

Common questions about Tilor (FAQ)

Q: Can Tilor be taken with common over-the-counter medicines like ibuprofen?

Regulatory documents highlight that Tilor already has antiplatelet activity. Combining it with other antiplatelet medicines, such as NSAIDs like ibuprofen, is associated with an increased antiplatelet effect.

Regulatory information indicates that concurrent use may carry an increased risk of bleeding due to the compounded effects of these medications.

Q: How quickly should I expect Tilor to start working?

While the medicine begins its action at the cellular level immediately, the effects on functional outcomes, such as walking distance, take time to be observed.

Official studies indicate that continuous therapy is often assessed after 12 weeks (about three months) to determine if a clinically relevant benefit has been observed.

Q: Is it normal to feel a bit nauseous when first starting Tilor?

Nausea is reported as a common side effect of Tilor, based on official drug information. Other frequently reported issues affecting the digestive system include diarrhea and abnormal stools.

Regulatory data indicates these effects are often most noticeable during the initial month of treatment.

Q: Does Tilor have known interactions with alcohol?

Official information states that it is not fully known if there is a direct interaction between Tilor and alcohol.

However, both alcohol consumption and Tilor commonly list dizziness as a side effect. Combining the two may therefore increase the overall potential for feeling dizzy or lightheaded.

Q: Can Tilor affect sleep or cause insomnia?

Adverse event reporting systems include drowsiness as a reported side effect, though regulatory data suggests it is not a common occurrence.

Insomnia (difficulty sleeping) is not explicitly listed as a common or very common side effect in the official safety profile.

Q: How long does the effect of a Tilor dose typically last?

The duration of a single dose's effect is determined by the drug's half-life. Tilor has an elimination half-life of approximately 11 to 15 hours.

This duration aligns with the official twice-daily dosing regimen used to maintain consistent levels of the medicine in the body.

Q: What does the official patient information say about Tilor and driving?

Official patient information includes warnings because Tilor is known to cause common side effects such as dizziness and headaches.

Caution regarding driving or operating machinery is noted in the patient information until an individual knows how the medicine affects them.

Q: Does Tilor have a risk of causing allergic reactions?

Yes, regulatory data indicates a risk of allergic reactions. Post-marketing safety reports list serious immune system responses, including anaphylaxis (a severe, whole-body allergic reaction) and angioedema (swelling beneath the skin or mucous membranes).

Q: What kind of monitoring might be required while taking Tilor?

The official safety profile outlines that monitoring for certain serious signs is a consideration while using Tilor.

This includes checking for signs of unusual bleeding or bruising. Evaluation for symptoms of serious blood changes (blood dyscrasias) is part of the overall safety management described in official documents.

Q: How is Tilor absorbed into the body?

Tilor is designed to be absorbed best when taken on an empty stomach.

Official pharmacokinetic data shows that the presence of a high-fat meal can increase the amount of Tilor absorbed into the bloodstream. This is why regulatory documents specify strict timing relative to meals.

Q: When was Tilor first approved by regulatory agencies?

Official government records confirm that the active ingredient in Tilor (Cilostazol) was first approved for use by the U.S. Food and Drug Administration (FDA) on January 15, 1999.

Q: How long does Tilor stay in the system after the last dose?

The amount of time Tilor stays in your system is determined by its half-life, which is 11 to 15 hours.

The drug is considered nearly cleared from the body approximately 3 days (or five half-lives) after the last dose.

Q: What is the risk of Tilor overdose according to official documents?

Official documents describe the symptoms of an overdose as generally being an intensification of the drug's known pharmacological effects.

These may include severe headache, intense diarrhea, a drop in blood pressure (hypotension), and a fast heart rate (tachycardia).

Q: What information is available about stopping Tilor use and what happens in the body when it stops working?

Tilor is a reversible acting medicine and is eliminated from the body relatively quickly, typically within 3 days after the last dose. The clearance time assists healthcare providers in planning for procedures that carry a risk of bleeding.

Official documents note that monitoring for potential cardiovascular events may be a consideration for high-risk patients following discontinuation of the therapy.

How should Tilor be stored and disposed of?

Tilor (Cilostazol) must be stored in strict accordance with the instructions provided in its official labeling to maintain potency and stability. The tablets must be kept at Controlled Room Temperature, defined as 20 to 25 C (68 to 77 F), with protection from temperature extremes, light, and moisture. It is explicitly required to keep from freezing and to store the medication in its original container, tightly closed. Per regulatory mandate, all medication must be kept out of the sight and reach of children.

For disposal, official instructions prohibit throwing unused or expired Tilor into wastewater or household waste. The proper procedure is to consult a pharmacist or healthcare professional for guidance on utilizing official medication take-back programs.

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

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