Generic Cilostazol

Introduction

Cilostazol is an oral medication approved primarily for the relief of intermittent claudication associated with peripheral arterial disease (PAD). It belongs to the phosphodiesterase-3 (PDE3) inhibitor class and exerts both antiplatelet and vasodilatory actions. The drug is available as a tablet in 50 mg and 100 mg strengths and is marketed worldwide under several brand names, most notably Pletal and Cilostazol-Mylan. It is prescribed to improve walking distance and reduce leg pain in adults with PAD who are not candidates for revascularisation or who require an adjunct to lifestyle measures. In addition to its approved indication, cilostazol has been investigated for a range of off-label conditions, including secondary stroke prevention and pulmonary hypertension.

What is Cilostazol?

Cilostazol is the generic form of the active compound cilostazol, a synthetic quinolinone derivative that inhibits the enzyme phosphodiesterase-3. It is marketed under brand names such as Pletal, Cilostazol-Mylan, and Cilostaz. Our online pharmacy provides this generic alternative as a cost-effective treatment option. The medication is supplied as film-coated tablets, each containing either 50 mg or 100 mg of the active ingredient. Developed in the early s by Boehringer Ingelheim, cilostazol received its first regulatory approval in the United States in 1999 for the management of intermittent claudication.

How Cilostazol Works

Cilostazol blocks phosphodiesterase-3, an enzyme that hydrolyses cyclic adenosine monophosphate (cAMP) in platelets and vascular smooth-muscle cells. By preserving cAMP levels, the drug produces two principal therapeutic effects:

1. Antiplatelet activity - Elevated cAMP inhibits platelet aggregation, reducing the risk of thrombus formation in distal arteries.
2. Vasodilation - In smooth-muscle cells, higher cAMP causes relaxation, widening peripheral arterioles and enhancing blood flow to ischemic muscle tissue.

These mechanisms translate clinically into improved oxygen delivery to the lower limbs, thereby extending walking distance and decreasing the pain that characterises intermittent claudication. The onset of action is typically observed within 2-4 hours after the first dose, while steady-state plasma concentrations are reached after about 2 days of twice-daily dosing. Cilostazol is metabolised primarily by hepatic CYP3A4 and CYP2C19 isoenzymes and has an elimination half-life of approximately 11 hours, supporting a twice-daily dosing schedule.

Conditions Treated with Cilostazol

Approved indication (FDA, EMA, Health Canada):

• Intermittent claudication secondary to peripheral arterial disease - Cilostazol is indicated for adult patients who experience exertional leg pain due to reduced blood flow in the peripheral arteries. By increasing limb perfusion, it helps patients walk farther and experience less pain during activity.

The drug is not approved for the primary prevention of cardiovascular events, stroke, or for use in acute coronary syndromes.

Off-Label and Investigational Uses of Cilostazol

Although regulatory agencies have not formally approved the following applications, several peer-reviewed studies and clinical guidelines have explored cilostazol’s potential benefits:

• Secondary prevention of non-cardioembolic ischemic stroke - Small randomized trials have reported reduced recurrent stroke rates when cilostazol is added to standard antiplatelet therapy, likely due to its combined antiplatelet and vasodilatory actions.
• Pulmonary arterial hypertension - Early-phase trials suggest modest improvements in pulmonary vascular resistance, attributed to pulmonary vasodilation.
• Diabetic foot ulcer healing - Observational data indicate accelerated ulcer closure, possibly related to enhanced microcirculatory flow.
• Coronary artery disease (stable angina) - Cilostazol has been examined as an adjunct to aspirin and clopidogrel, showing modest improvement in exercise tolerance in some studies.
• Erectile dysfunction - The drug’s vasodilatory effect has prompted limited research into its use for men with endothelial-mediated erectile dysfunction.

These off-label uses remain investigational; the evidence base varies in size and quality, and safety has not been established for routine clinical practice. Patients should only consider such applications under direct supervision of a qualified healthcare professional.

Is Cilostazol the Right Medication for You?

Cilostazol is most appropriate for adults with documented PAD who experience intermittent claudication and who are not suitable candidates for surgical revascularisation. Ideal candidates typically have:

• Ankle-brachial index (ABI) between .4 and .9.
• Persistent leg pain limiting ambulation despite supervised exercise and risk-factor modification.

Contraindications and cautionary situations

• Heart failure (NYHA class III/IV) - PDE3 inhibition can exacerbate cardiac dysfunction.
• Severe hepatic impairment - Impaired metabolism increases systemic exposure.
• Active bleeding or recent hemorrhagic stroke - Antiplatelet effect raises bleeding risk.
• Known hypersensitivity to cilostazol or any excipients.

Relative cautions include uncontrolled hypertension, recent myocardial infarction, and concomitant use of potent CYP3A4 inhibitors. In such cases, dose adjustment or alternative therapy may be required.

Risks, Side Effects, and Interactions

Common

• Headache
• Diarrhea or loose stools
• Nausea and dyspepsia
• Abdominal pain or cramping
• Dizziness or light-headedness
• Palpitations

These events occur in more than 1 % of treated patients and are usually mild to moderate in intensity.

Rare

• Rash or pruritus
• Thrombocytopenia
• Mild elevations in liver enzymes (ALT/AST)
• Orthostatic hypotension

Rare adverse reactions are reported in fewer than .1 % of users but may warrant medical evaluation if they persist.

Serious

• Severe or life-threatening bleeding (gastrointestinal, intracranial)
• Cardiac arrhythmias, including ventricular tachycardia, particularly in patients with existing heart disease
• Myocardial infarction - some studies suggest a possible increased risk in patients with severe coronary artery disease
• Acute hepatic failure or severe jaundice
• Anaphylaxis or severe hypersensitivity reactions

Any serious event requires immediate medical attention and discontinuation of therapy.

Drug-drug and drug-food interactions

• CYP3A4 inhibitors (ketoconazole, erythromycin, clarithromycin, protease inhibitors) ↑ cilostazol plasma levels → higher risk of side effects.
• CYP2C19 inhibitors (omeprazole, fluvoxamine) may similarly increase exposure.
• Anticoagulants (warfarin, direct oral anticoagulants) - additive bleeding risk; close monitoring of INR or anti-Xa activity is advisable.
• Concurrent antiplatelet agents (aspirin, clopidogrel) - potentiates antithrombotic effect, increasing hemorrhagic risk.
• Antihypertensives - potential for additive hypotension; blood pressure should be checked after initiation.
• Grapefruit juice - inhibits CYP3A4, potentially raising cilostazol concentrations.
• Alcohol - may exacerbate gastrointestinal irritation and increase bleeding tendency.

Patients should disclose all prescription, over-the-counter, and herbal products before starting cilostazol.

Use: Dosing, Missed Dose, Overdose

Standard dosing - The usual adult regimen is 100 mg taken orally twice daily, at least 30 minutes before or 2 hours after a meal. Food can delay absorption and reduce peak plasma concentrations; therefore, adherence to timing instructions optimises efficacy.

Dose initiation or intolerance - Some clinicians start with 50 mg twice daily for the first 1-2 weeks to improve tolerability, then increase to the full 100 mg dose if the patient tolerates the medication.

Missed dose - If a dose is forgotten and the scheduled time for the next dose is less than 4 hours away, the missed dose should be skipped. Do not double-dose to compensate.

Overdose - Acute overdose may present with severe hypotension, syncope, arrhythmias, and excessive bleeding. Immediate medical evaluation is essential. Supportive care, including monitoring of cardiac rhythm and blood pressure, constitutes the primary treatment; there is no specific antidote.

Practical precautions

• Take the tablets with a full glass of water.
• Avoid simultaneous consumption of grapefruit juice.
• Alcohol should be limited, as it can increase gastrointestinal irritation and bleeding risk.
• Do not operate heavy machinery or drive until you know how cilostazol affects you, especially during the first few weeks.

FAQ

• Can I travel internationally with cilistazol tablets? Yes, cilostazol tablets can be taken while traveling, but keep them in their original packaging with the prescription label (or a copy of the prescription) to avoid customs issues. Carry a brief letter from a healthcare provider if you are crossing borders that require proof of medical necessity.

• How should cilostazol be stored in hot climates? Store the tablets in a cool, dry place away from direct sunlight. If ambient temperatures exceed 30 °C (86 °F) for extended periods, keep the medication in a sealed container inside a refrigerator (2-8 °C) to maintain potency.

• What does the imprint on a 100 mg cilostazol tablet look like? The 100 mg tablet is typically round, film-coated, and bears the imprint “100 CIL” on one side, with “P” on the opposite side. Appearance may vary slightly between manufacturers, but the imprint helps verify authenticity.

• Does cilostazol affect blood sugar levels? Current evidence does not indicate a clinically significant impact of cilostazol on glucose metabolism. Patients with diabetes should continue routine blood-glucose monitoring, as the drug’s primary actions are on platelet aggregation and vascular tone.

• Are there any known drug tests that detect cilostazol? Cilostazol is not a controlled substance and is not included in standard workplace or forensic drug-screening panels. Specialized pharmacokinetic assays can detect it, but such testing is rare and typically limited to clinical research settings.

• Can I consume grapefruit while taking cilostazol? Grapefruit juice inhibits CYP3A4, the enzyme that metabolises cilostazol, potentially raising drug levels and increasing side-effect risk. It is advisable to avoid large amounts of grapefruit or its juice during therapy.

• What is the half-life of cilostazol and how does it affect dosing schedule? Cilostazol has an elimination half-life of roughly 11 hours, which supports twice-daily dosing to maintain steady plasma concentrations. Missing a dose can lead to fluctuations that may reduce efficacy or increase adverse effects.

• How does cilostazol compare to pentoxifylline for intermittent claudication? Both agents improve walking distance, but cilostazol generally shows a greater increase in maximal treadmill walking time and a more favorable side-effect profile. Pentoxifylline, a rheologic agent, is less potent in vasodilation and platelet inhibition.

• Is cilostazol safe for patients with mild liver disease? Mild hepatic impairment (Child-Pugh A) usually does not require dose adjustment, but clinicians should monitor liver function tests periodically because cilostazol is metabolised hepatically. Severe liver disease is a contraindication.

• Why does cilostazol sometimes cause a reddish urine color? Cilostazol and some of its metabolites are excreted renally and can impart a faint reddish-orange hue to urine. This discoloration is harmless and does not indicate hematuria or renal dysfunction.

Glossary

Phosphodiesterase-3 (PDE3)

An enzyme that breaks down cyclic adenosine monophosphate (cAMP) in platelets and vascular smooth-muscle cells; inhibition raises cAMP levels, leading to antiplatelet and vasodilatory effects.

Intermittent Claudication

Exercise-induced muscle pain, typically in the calves, caused by inadequate blood flow due to peripheral arterial narrowing; relief occurs with rest.

Peripheral Arterial Disease (PAD)

A circulation disorder characterized by atherosclerotic narrowing of arteries supplying the limbs, most commonly the lower extremities, leading to symptoms such as claudication.

Half-life

The time required for the plasma concentration of a drug to decrease by 50 %; for cilostazol this is about 11 hours, informing its twice-daily dosing schedule.

Buying Cilostazol from Our Online Pharmacy

Patients who need reliable access to cilostazol can obtain the medication through our online pharmacy. By sourcing directly from licensed international suppliers, we keep prices close to the manufacturer’s cost, making treatment more affordable for individuals without comprehensive insurance coverage. Every batch is verified for authenticity and potency, ensuring that you receive a product that meets stringent quality standards.

Our discreet shipping service protects your privacy: packages are unbranded, and delivery is made through secure carriers with tracking options. Standard international airmail typically arrives within three weeks, while express delivery can be arranged for about a week, depending on the destination. Because we operate as a pharmacy-broker service, we can provide medications that may be unavailable locally, helping bridge gaps in healthcare access.

Choosing our online pharmacy means a reliable, confidential, and cost-effective way to maintain your cilostazol regimen, especially when conventional channels are limited or cost-prohibitive.

Disclaimer

The details presented about cilostazol are intended for general educational purposes only and do not substitute professional medical advice. Treatment decisions, including the use of cilostazol for off-label purposes, must be made under the guidance of a qualified healthcare provider. Readers are assumed to be competent adults who can independently evaluate health information. Our online pharmacy makes generic cilostazol available for individuals facing limited access through traditional pharmacy channels or who are seeking more affordable options. Always discuss any medication changes with a qualified practitioner before initiating, stopping, or altering therapy.