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MEDICINE MONOGRAPH CODE: [3.20] ID: TIP-MED-000020

Cilostazol

Active Ingredient / Scientific Identity: Cilostazol • Class: Phosphodiesterase-3 (PDE-3) Inhibitor; Antiplatelet & Direct Arterial Vasodilator

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THE INDIAN PHARMACIST — Educational Reference Sheet
Profile: Cilostazol ([3.20] | ID: TIP-MED-000020) • Last Reviewed: 2026-11-10
Source URL: https://theindianpharmacist.com/medicine/3-20-cilostazol/
Generic / Entity NameCilostazol ([3.20])
Verified Indian Brands / RefGeneric Compendial Entry (No Commercial Brand Claimed)
Pharmacological ClassPhosphodiesterase-3 (PDE-3) Inhibitor; Antiplatelet & Direct Arterial Vasodilator
Available Dosage FormsOral Uncoated Tablets: 50 mg, 100 mg; Sustained-Release: 100 mg SR
Regulatory ClassificationSchedule H Prescription Drug (To be sold by retail on the prescription of a Registere
Key Warning & Review DateRenal: Dosing depends on severe renal impairment—contraindicated if CrCl ≤25 mL/min (active metabolites accumulate). Hepatic:
Reviewed: 2026-11-10
Safety Matrix:⚖️ Legal Status: Schedule H Prescription Drug (To be sold by retail o✔️ Standard Clinical Dispensing Precautions

1. Clinical & Scientific Overview

Cilostazol (TIP-MED-000020, Reference Code [3.20]) is classified under Cardiovascular & Antithrombotic Medicines (Ch 03) as a Phosphodiesterase-3 (PDE-3) Inhibitor; Antiplatelet & Direct Arterial Vasodilator. Within the Indian regulatory and compendial framework, it is governed under Schedule H Prescription Drug (To be sold by retail on the prescription of a Registered Medical Practitioner only — Drugs Rules 1945).

Verified Indian Market Examples / Compendial Status:
Representative Indian Market Examples (Edition 2.7 Ch 03 [3.20], p. 30): Pletoz (Cipla), Cilodoc (Lupin), Stiloz (Glenmark), Pletal — Strengths & Dosage Forms: Oral Uncoated Tablets: 50 mg, 100 mg; Sustained-Release: 100 mg SR
Representative Indian Market Examples (Edition 2.7 Ch 03 [3.20], p. 30): Pletoz (Cipla), Cilodoc (Lupin), Stiloz (Glenmark), Pletal — Strengths & Dosage Forms: Oral Uncoated Tablets: 50 mg, 100 mg; Sustained-Release: 100 mg SR
Dosage Forms & Available Strengths:
Oral Uncoated Tablets: 50 mg, 100 mg; Sustained-Release: 100 mg SR
Routes: Oral / Parenteral / Topical as specified by formulation

3. Mechanism of Action & Pharmacodynamics

Phosphodiesterase-3 (PDE-3) Inhibitor; Antiplatelet & Direct Arterial Vasodilator acting on target receptor/enzyme pathways in Cardiovascular & Antithrombotic Medicines (Ch 03): clinical efficacy is mediated via Phosphodiesterase-3 (PDE-3) Inhibitor; Antiplatelet & Direct Arterial Vasodilator for Intermittent claudication in peripheral arterial disease (PAD—increases pain-free walking distance in patients without rest pain); off-label/specialist use in secondary stroke prevention or sinoatrial node dysfunction..

4. Therapeutic Indications & Evidence-Supported Uses

  • Intermittent claudication in peripheral arterial disease (PAD—increases pain-free walking distance in patients without rest pain)
  • off-label/specialist use in secondary stroke prevention or sinoatrial node dysfunction

🇮🇳 Jurisdiction & Indication Note: Indications and schedules reflect Indian compendial and regulatory records (CDSCO / Indian Pharmacopoeia & NFI / NLEM 2022). Where international reference labels (US FDA DailyMed / NCBI StatPearls) are cited for pharmacokinetic or mechanistic parameters, international approvals do not automatically imply CDSCO approval in India.

5. Educational Dosage Context, Formulations & Administration

Educational Dosing & Regimen Summary: General Adult Reference: 100 mg twice daily. Reduced dose: 50 mg twice daily when co-administered with CYP3A4 or CYP2C19 inhibitors. Follow physician prescription.

Administration & Meal Timing: Strictly on an EMPTY STOMACH: at least 30 minutes BEFORE or 2 hours AFTER breakfast and dinner. Taking cilostazol with a high-fat meal increases peak plasma levels (Cmax) by ~90%, precipitating severe headache, tachycardia, and palpitations. | Twice daily (30 minutes before breakfast and 30 minutes before dinner).

6. Pharmacokinetics, Metabolism & Renal/Hepatic Adjustment

Absorption & Disposition:
Absorption, distribution, metabolism, and excretion follow class pharmacokinetic profile; verify patient renal/hepatic function.
Metabolism & Biotransformation:
Renal: Dosing depends on severe renal impairment—contraindicated if CrCl ≤25 mL/min (active metabolites accumulate). Hepatic: Contraindicated in moderate-to-severe hepatic impairment (Child-Pugh B or C).
Elimination & Renal Adjustment:
Renal: Dosing depends on severe renal impairment—contraindicated if CrCl ≤25 mL/min (active metabolites accumulate). Hepatic: Contraindicated in moderate-to-severe hepatic impairment (Child-Pugh B or C).
Hepatic Impairment Considerations:
Renal: Dosing depends on severe renal impairment—contraindicated if CrCl ≤25 mL/min (active metabolites accumulate). Hepatic: Contraindicated in moderate-to-severe hepatic impairment (Child-Pugh B or C).

7. Contraindications, Precautions & High-Risk Warnings

Contraindications & Red-Flag Precautions:
  • Strictly contraindicated in Congestive Heart Failure (CHF) of any severity (PDE-3 inhibitors decrease survival in heart failure), unstable angina, recent MI/PCI (within 6 months), active bleeding, and severe tachyarrhythmias.

Key Clinical Precautions: Renal: Dosing depends on severe renal impairment—contraindicated if CrCl ≤25 mL/min (active metabolites accumulate). Hepatic: Contraindicated in moderate-to-severe hepatic impairment (Child-Pugh B or C).

8. Adverse Effects Profile

Common & Mechanism-Related Adverse Effects:
  • Throbbing headache (25–30%, due to cerebral vasodilation—often improves after 1–2 weeks), palpitations, resting tachycardia (heart rate increases by 5–10 bpm), loose stools/diarrhoea, dizziness.
  • Ventricular or supraventricular tachyarrhythmias, worsening angina pectoris, exacerbation of heart failure, severe bleeding, leukopenia/thrombocytopenia.
Serious / Dose-Limiting Adverse Effects:
  • Monitor for severe hypersensitivity, organ toxicity, or dose-limiting adverse events.

9. Major Drug–Drug, Drug–Food & Drug–Herb Interactions

  • CYP3A4 inhibitors (diltiazem, erythromycin, clarithromycin, ketoconazole, itraconazole) and CYP2C19 inhibitors (omeprazole, fluconazole) double cilostazol exposure—reduce cilostazol dose to 50 mg BD
  • Additive bleeding risk with dual antiplatelets (aspirin + clopidogrel) or anticoagulants

10. Clinical Monitoring, Patient Counselling & Storage

Clinical & Laboratory Monitoring: Monitor clinical response, baseline renal/hepatic parameters, and relevant serum biomarkers.

Pharmacist Patient Counselling Points:

  • Patient Counselling Checklist: Emphasise taking cilostazol 30 minutes before breakfast and dinner, never right after food (taking after food causes pounding headaches and racing heart). Reassure that mild headache in the first week can be managed with paracetamol and usually subsides; report chest pain or racing palpitations.
  • Meal & Clock Timing Instruction: Strictly on an EMPTY STOMACH: at least 30 minutes BEFORE or 2 hours AFTER breakfast and dinner. Taking cilostazol with a high-fat meal increases peak plasma levels (Cmax) by ~90%, precipitating severe headache, tachycardia, and palpitations. (Twice daily (30 minutes before breakfast and 30 minutes before dinner).)
  • Missed Dose Protocol: Take if remembered at least 30 minutes before a meal or 2 hours after eating; if close to the next dose, skip. Never double.
  • Geriatric Dispensing Pearl: Before dispensing to an elderly vascular patient, always screen the prescription for heart failure drugs (sacubitril/valsartan, carvedilol, furosemide + spironolactone) and verify left ventricular ejection fraction, as cilostazol is contraindicated in heart failure.

Storage, Stability & Dispensing Safeguards: Store below 25°C–30°C in original moisture- and light-resistant packaging out of reach of children. Available forms: Oral Uncoated Tablets: 50 mg, 100 mg; Sustained-Release: 100 mg SR

11. Visual Pharmacology & Mechanism Diagram (svg-v339-01-adme-12-step-journey)

THE 12-STEP ORAL DRUG JOURNEY THROUGH THE HUMAN BODY (LADME) Note: IV bolus enters Step 6 directly (F = 100%); Sublingual & Transdermal routes bypass Step 4–5 Portal First-Pass Metabolism 1. Oral Administration • Tablet / Capsule swallowed • Gastric emptying to duodenum pH 1.5–3.5 (Stomach) 2. Disintegration & Dissolution • Tablet breaks into granules • API dissolves in GI fluid Noyes-Whitney Dissolution Rate 3. GI Epithelial Absorption • Crosses intestinal villi • Passive / Active / P-gp efflux Small Intestine (Large Surface Area) 4. Portal Circulation • Mesenteric veins → Portal vein • Delivers blood to liver sinusoids Pre-systemic Venous Conduit 5. First-Pass Metabolism • Gut & hepatic CYP450 extraction • High: GTN, Propranolol, Morphine Determines Bioavailability (F = f_a × (1-E_H)) 6. Systemic Circulation • Hepatic vein → IVC → Heart • Unbound vs Albumin-bound drug Only FREE drug is active 7–8. Tissue Distribution (Vd) • Capillary permeation to organs • Blood-Brain & Placental barriers Vd = Dose / C_0 (L or L/kg) 9. Target Site of Action • Receptors (GPCR, Ion channel) • Enzymes & Carrier Transporters Pharmacodynamic Effect (E_max, EC50) 10. Hepatic Biotransformation • Phase I (CYP450 Oxidation/Hydrolysis) • Phase II (Glucuronidation/Sulfation) Converts lipophilic drug → hydrophilic metabolite 11. Renal & Biliary Elimination • Nephron: Filtration + Secretion − Reabsorption • Biliary excretion & Enterohepatic recycling Total Clearance CL_tot = CL_renal + CL_hepatic 12. Excretion from the Body • Urine (Primary polar metabolite route) • Bile/Faeces, Expired Air, Sweat, Milk Elimination Half-Life t1/2 = (0.693 × Vd) / CL
svg-v339-01-adme-12-step-journey — 8.1 Complete 12-Step Journey of an Orally Administered Drug (ADME): Figure 8.1: The 12-step physiological journey of a typical orally administered solid dosage form through Liberation, Absorption, Distribution, Metabolism, and Excretion (LADME). Note: Parenteral (IV), sublingual, and inhalational routes bypass gastrointestinal absorption and/or hepatic first-pass metabolism.

12. Authoritative References, Regulatory Sources & Editorial Disclaimer

Primary Compendial & Guideline Reference: Indian Pharmacist Desk Reference — Professional Edition 2.7 (2026–27) • Ch 03 [3.20] (p. 30)

Official Verification Portals: Indian Pharmacopoeia Commission (IPC) & National Formulary of India (NFI) • Central Drugs Standard Control Organization (CDSCO) • Ministry of Health & Family Welfare — NLEM 2022 • NCBI Bookshelf / StatPearls Pharmacology Reference • DailyMed (US FDA Official Prescribing Reference)

Last Medically & Pharmaceutically Reviewed: 2026-11-10 • Verification Status: HANDBOOK_SOURCE_CONTENT

Educational & Clinical Disclaimer: This reference profile is published solely for pharmacy education, academic study, and professional clinical reference. It does not substitute for patient-specific clinical judgement, qualified specialist oncology/medical supervision, or official CDSCO/IP prescribing information. Never self-medicate with prescription, Schedule H/H1/X, NDPS, or oncology medicines.

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Educational Reference Notice: This printout from THE INDIAN PHARMACIST (https://theindianpharmacist.com/medicine/3-20-cilostazol/, Last Reviewed: 2026-11-10) is an educational reference sheet for students and healthcare learners. It is NOT an official prescribing guideline or patient-specific treatment order.