CILOSTAZOL 100MG TABLETS 56`S

Cilostazol is a medicine used to relieve the leg pain and cramping that occurs when walking in patients with peripheral arterial disease (PAD) — a condition in which narrowed leg arteries reduce blood flow to the leg muscles. The resulting pain on walking that eases with rest is called intermittent claudication.

Cilostazol works by widening the arteries supplying the legs (vasodilation) and preventing blood platelets from clumping together (antiplatelet effect), improving blood flow to the muscles during exercise. With regular treatment, most patients can walk significantly further before experiencing pain. It is typically used as a second-line treatment after lifestyle changes have not adequately improved walking distance.

Approved Uses

•     Improvement of pain-free and maximum walking distance in patients with intermittent claudication (PAD, Fontaine Stage II) — without rest pain or tissue necrosis

•     Also used (in some international guidelines) for secondary prevention of stroke recurrence after non-cardioembolic ischaemic stroke or TIA

Adults

•     100 mg twice daily — best taken at least 30 minutes before or 2 hours after breakfast and dinner

•     Taking with food significantly increases drug absorption and side effects (particularly headache and palpitations) — take on an empty stomach when possible

Dose Reduction to 50 mg Twice Daily — Required With

•     Moderate/strong CYP3A4 inhibitors: clarithromycin, erythromycin, diltiazem, itraconazole, ketoconazole

•     CYP2C19 inhibitors: omeprazole, esomeprazole, fluconazole

Clinical Assessment at 3 Months

If there is no meaningful improvement in walking distance after 3 months of treatment, cilostazol should be discontinued — continued therapy without benefit is not recommended.

Special Populations

•     Renal impairment: No dose adjustment if CrCl >25 mL/min. Use with caution if CrCl ≤25 mL/min

•     Hepatic impairment: Mild — no adjustment. Moderate–severe — insufficient data; use with caution

•     Children: Safety and efficacy not established

Missed Dose

Take as soon as you remember, unless it is almost time for the next dose — skip it and continue normally. Never double up.

Common (may affect more than 1 in 10 patients)

•     Headache: most common side effect, affecting over 30% of patients; usually improves with continued use

•     Diarrhoea and loose stools (affecting over 15%)

•     Palpitations and tachycardia (average increase of 5–8 bpm)

•     Dizziness and peripheral oedema (ankle swelling)

•     Nausea and abnormal stools

Serious — Tell Your Doctor Immediately

•     Cardiac arrhythmias: Palpitations are common and usually benign, but serious arrhythmias can occur in susceptible individuals

•     Significant bleeding: cilostazol inhibits platelet function — report unusual bruising, prolonged bleeding from cuts, blood in urine/stools

•     Rare: agranulocytosis (dangerously low white blood cells) and thrombocytopenia (low platelets) — require immediate medical attention

•     Known hypersensitivity to cilostazol

•     Active pathological bleeding (peptic ulcer, intracranial bleeding)

•     Pregnancy — caused fetal malformations in animal studies

•     Unstable angina or myocardial infarction within the past 6 months

•     History of ventricular tachycardia, ventricular fibrillation, or QTc prolongation

Heart Failure

ABSOLUTE CONTRAINDICATION. PDE-3 inhibitors increase the force of cardiac contraction (positive inotropic effect) — in heart failure, this has been shown to increase mortality. Do NOT use in any patient with a diagnosis of heart failure, regardless of severity.

Pregnancy

CONTRAINDICATED. Cilostazol caused fetal malformations in animal studies. Use effective contraception during treatment.

Breastfeeding

Not recommended — cilostazol and its metabolites pass into breast milk and may affect the nursing infant.

Smoking

Patients with PAD must be strongly encouraged to stop smoking. Smoking significantly constricts blood vessels and greatly limits cilostazol's effectiveness.

Grapefruit Juice

Avoid grapefruit juice during treatment — it inhibits CYP3A4 and increases cilostazol levels by approximately 50%, increasing side effects.

•     CYP3A4 inhibitors — strong (clarithromycin, erythromycin, itraconazole, ketoconazole): Significantly increase cilostazol levels — reduce dose to 50 mg twice daily

•     CYP2C19 inhibitors (omeprazole, esomeprazole): Increase active metabolite levels — reduce dose to 50 mg twice daily

•     CYP3A4 inducers (carbamazepine, rifampicin): Decrease cilostazol levels — may reduce efficacy

•     Grapefruit juice: CYP3A4 inhibitor — increases cilostazol levels ~50%. Avoid.

•     Anticoagulants (warfarin, heparin) and antiplatelet agents (aspirin, clopidogrel): Additive increased bleeding risk — monitor closely

•     Antihypertensives and vasodilators (calcium channel blockers): Additive hypotension and reflex tachycardia

•     Alcohol: Enhances hypotensive effect — advise moderation

•     Store at room temperature (15–25°C), protected from moisture and heat

•     Keep in original packaging, out of reach of children

POM — Prescription Only Medicine.

•     Take on an empty stomach — at least 30 minutes before or 2 hours after meals — for best effect

•     Avoid grapefruit juice during the course of treatment

•     Continue prescribed lifestyle measures: smoking cessation, supervised walking exercise, cholesterol management, and blood pressure control — these are as important as the medication

•     Return for clinical review at 3 months — if your walking distance has not improved meaningfully, your doctor will reassess whether to continue cilostazol

•     Tell your doctor before any procedure or surgery — cilostazol affects platelet function and bleeding risk

•     Heart failure screening: Mandatory before prescribing — check for any history of heart failure, LV dysfunction, or recent hospitalisation for fluid overload. Any doubt warrants an echo or cardiology referral.

•     3-month rule: Build in a clinical review at 3 months — if no objective improvement in maximum or pain-free walking distance, discontinue. Continued prescribing without review is not evidence-based.

•     CYP interactions: Very common in practice — omeprazole (one of the most prescribed drugs) is a CYP2C19 inhibitor that requires a cilostazol dose reduction to 50 mg twice daily

•     Grapefruit juice: Counsel patients explicitly — this is a commonly overlooked interaction that significantly increases drug exposure

•     Aspirin combination: Sometimes co-prescribed for cardiovascular prevention — increased bleeding risk; patient should be aware

•     Pletal comparison: Cilostazol 100 mg BD is the generic equivalent of Pletal® 100 mg BD — bioequivalence established

Q: How long before I start walking further without pain?

A: Many patients notice some improvement within 2–4 weeks, but the full benefit — the maximum increase in walking distance — may take up to 12 weeks of regular treatment. Continue taking it as prescribed even if early improvement is modest.

Q: Can I take aspirin or ibuprofen with cilostazol?

A: Low-dose aspirin is sometimes co-prescribed with cilostazol for cardiovascular protection — this is done under medical supervision as it adds to the antiplatelet effect and increases bleeding risk. Ibuprofen and other NSAIDs should only be taken with caution and are not recommended without medical guidance, as they also increase bleeding risk and can raise blood pressure.

Q: What happens if I stop taking cilostazol?

A: The improvements in walking distance will gradually reverse within 48–96 hours as platelet function and blood vessel tone return to their pre-treatment state. There is no rebound effect or worsening beyond your original baseline — you simply return to where you started.