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MEDICINE MONOGRAPH CODE: [3.40]-C5 ID: TIP-MED-000275

Ranolazine

Active Ingredient / Scientific Identity: Ranolazine • Class: Potassium-Channel Opener / Late INa Blocker / Metabolic Anti-Ischaemic Agents (Schedule H)

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THE INDIAN PHARMACIST — Educational Reference Sheet
Profile: Ranolazine ([3.40]-C5 | ID: TIP-MED-000275) • Last Reviewed: 2026-11-10
Source URL: https://theindianpharmacist.com/medicine/3-40-c5-ranolazine/
Generic / Entity NameRanolazine ([3.40]-C5)
Verified Indian Brands / RefGeneric Compendial Entry (No Commercial Brand Claimed)
Pharmacological ClassPotassium-Channel Opener / Late INa Blocker / Metabolic Anti-Ischaemic Agents (Schedule H)
Available Dosage FormsNicorandil: 5 mg, 10 mg, 20 mg SR. Ranolazine: 500 mg, 1000 mg ER. Trimetazidine: 35 mg MR BD / 60 mg OD
Regulatory ClassificationSchedule H Prescription Drug (To be sold by retail on the prescription of a Registere
Key Warning & Review DateRenal: If eGFR 30–60 mL/min, halve Trimetazidine to 35 mg MR OD; if eGFR <30 mL/min, avoid Trimetazidine and Ranolazine. Hepa
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

Ranolazine (TIP-MED-000275, Reference Code [3.40]-C5) is classified under Cardiovascular & Antithrombotic Medicines (Ch 03) as a Potassium-Channel Opener / Late INa Blocker / Metabolic Anti-Ischaemic Agents (Schedule H). 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:
Co-indexed constituent under primary monograph [3.40] (Nicorandil, Ranolazine & Trimetazidine (Second-Line Antianginals)). Representative Indian Market Examples (Edition 2.7 Ch 03 [3.40], p. 40): Nicorandil: Nikoran (Torrent), Korandil (Sun). Ranolazine: Ranozex (Sun), Cartinex. Trimetazidine: Flavedon MR (Servier), Cytogard OD — Strengths & Dosage Forms: Nicorandil: 5 mg, 10 mg, 20 mg SR. Ranolazine: 500 mg, 1000 mg ER. Trimetazidine: 35 mg MR BD / 60 mg OD
Co-indexed constituent under primary monograph [3.40] (Nicorandil, Ranolazine & Trimetazidine (Second-Line Antianginals)). Representative Indian Market Examples (Edition 2.7 Ch 03 [3.40], p. 40): Nicorandil: Nikoran (Torrent), Korandil (Sun). Ranolazine: Ranozex (Sun), Cartinex. Trimetazidine: Flavedon MR (Servier), Cytogard OD — Strengths & Dosage Forms: Nicorandil: 5 mg, 10 mg, 20 mg SR. Ranolazine: 500 mg, 1000 mg ER. Trimetazidine: 35 mg MR BD / 60 mg OD
Dosage Forms & Available Strengths:
Nicorandil: 5 mg, 10 mg, 20 mg SR. Ranolazine: 500 mg, 1000 mg ER. Trimetazidine: 35 mg MR BD / 60 mg OD
Routes: Oral / Parenteral / Topical per formulation

3. Mechanism of Action & Pharmacodynamics

Potassium-Channel Opener / Late INa Blocker / Metabolic Anti-Ischaemic Agents (Schedule H) acting on target receptor/enzyme pathways in Cardiovascular & Antithrombotic Medicines (Ch 03): clinical efficacy is mediated via Potassium-Channel Opener / Late INa Blocker / Metabolic Anti-Ischaemic Agents (Schedule H) for Add-on antianginal therapy for chronic stable angina inadequately controlled by or intolerant to Beta-blockers, CCBs, and Nitrates.

4. Therapeutic Indications & Evidence-Supported Uses

  • Add-on antianginal therapy for chronic stable angina inadequately controlled by or intolerant to Beta-blockers, CCBs, and Nitrates

🇮🇳 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: Nicorandil: 5–10 mg PO BD (max 20 mg BD). Ranolazine: 500 mg ER PO BD (max 1000 mg BD). Trimetazidine: 35 mg MR PO BD with meals

Administration & Meal Timing: Swallow Ranolazine ER and Trimetazidine MR whole; keep Nicorandil strips sealed with desiccant until the moment of swallowing (moisture-sensitive!) | Morning & Evening (12-hourly BD)

6. Pharmacokinetics, Metabolism & Renal/Hepatic Adjustment

Absorption & Disposition:
Follows class pharmacokinetic profile detailed in parent monograph [3.40].
Metabolism & Biotransformation:
Renal: If eGFR 30–60 mL/min, halve Trimetazidine to 35 mg MR OD; if eGFR <30 mL/min, avoid Trimetazidine and Ranolazine. Hepatic: Ranolazine contraindicated in Child–Pugh B/C
Elimination & Renal Adjustment:
Renal: If eGFR 30–60 mL/min, halve Trimetazidine to 35 mg MR OD; if eGFR <30 mL/min, avoid Trimetazidine and Ranolazine. Hepatic: Ranolazine contraindicated in Child–Pugh B/C
Hepatic Impairment Considerations:
Renal: If eGFR 30–60 mL/min, halve Trimetazidine to 35 mg MR OD; if eGFR <30 mL/min, avoid Trimetazidine and Ranolazine. Hepatic: Ranolazine contraindicated in Child–Pugh B/C

7. Contraindications, Precautions & High-Risk Warnings

Contraindications & Red-Flag Precautions:
  • Nicorandil: ABSOLUTELY CONTRAINDICATED with PDE-5 inhibitors (Sildenafil/Tadalafil); causes painful mucosal/GI/perianal ulcers! Ranolazine: Contraindicated in cirrhosis, eGFR <30 mL/min, QTc prolongation, and strong CYP3A4 inhibitors. Trimetazidine: Contraindicated in Parkinson's disease, tremors, and eGFR <30 mL/min!

Key Clinical Precautions: Renal: If eGFR 30–60 mL/min, halve Trimetazidine to 35 mg MR OD; if eGFR <30 mL/min, avoid Trimetazidine and Ranolazine. Hepatic: Ranolazine contraindicated in Child–Pugh B/C

8. Adverse Effects Profile

Common & Mechanism-Related Adverse Effects:
  • Nicorandil: Headache, dizziness. Ranolazine: Constipation, dizziness, nausea. Trimetazidine: GI upset, dizziness
  • Nicorandil: Severe persistent oral, corneal, ileal, or anal ulceration (STOP drug permanently!). Ranolazine: QTc prolongation. Trimetazidine: Drug-induced Parkinsonism, resting tremor, gait instability
Serious / Dose-Limiting Adverse Effects:

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

    • Nicorandil + PDE-5i = fatal hypotension; Nicorandil + Aspirin/NSAIDs/Steroids = GI perforation
    • Ranolazine + Clarithromycin/Ketoconazole = contraindicated; Ranolazine + Diltiazem/Verapamil = cap Ranolazine at 500 mg BD; Ranolazine increases Simvastatin (max 20 mg) & Metformin (max 1000 mg/d)

    10. Clinical Monitoring, Patient Counselling & Storage

    Clinical & Laboratory Monitoring: Monitor clinical parameters per parent monograph [3.40].

    Pharmacist Patient Counselling Points:

    • Patient Counselling Checklist: For Nicorandil: keep tablet in foil with silica desiccant until swallowing and report any mouth ulcers immediately; for Trimetazidine: report any hand tremor or stiffness immediately
    • Meal & Clock Timing Instruction: Swallow Ranolazine ER and Trimetazidine MR whole; keep Nicorandil strips sealed with desiccant until the moment of swallowing (moisture-sensitive!) (Morning & Evening (12-hourly BD))
    • Missed Dose Protocol: Skip if close to next BD dose; never crush ER/MR tablets
    • Geriatric Dispensing Pearl: Closely monitor older adults on Trimetazidine for drug-induced Parkinsonism (never misdiagnose as idiopathic Parkinson's!)

    Storage, Stability & Dispensing Safeguards: Store below 25°C–30°C in original moisture- and light-resistant packaging out of reach of children. Available forms: Nicorandil: 5 mg, 10 mg, 20 mg SR. Ranolazine: 500 mg, 1000 mg ER. Trimetazidine: 35 mg MR BD / 60 mg OD

    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 Pharmacopoeia (IP 2022) • NFI • CDSCO

    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: VERIFIED_EDUCATIONAL_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/3-40-c5-ranolazine/, 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.