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MEDICINE MONOGRAPH CODE: [4.19] ID: TIP-MED-000063 ⚠️ HIGH-ALERT / SPECIALIST SUPERVISION

Repaglinide

Active Ingredient / Scientific Identity: Repaglinide • Class: Short-Acting Meglitinide Prandial Insulin Secretagogue (Schedule H)

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THE INDIAN PHARMACIST — Educational Reference Sheet
Profile: Repaglinide ([4.19] | ID: TIP-MED-000063) • Last Reviewed: 2026-11-10
Source URL: https://theindianpharmacist.com/medicine/4-19-repaglinide/
Generic / Entity NameRepaglinide ([4.19])
Verified Indian Brands / RefGeneric Compendial Entry (No Commercial Brand Claimed)
Pharmacological ClassShort-Acting Meglitinide Prandial Insulin Secretagogue (Schedule H)
Available Dosage FormsTablets: 0.5 mg, 1 mg, 2 mg; FDCs with Metformin or Voglibose
Regulatory ClassificationSchedule H & Schedule G Prescription Drug ('Caution: It is dangerous to take this pre
Key Warning & Review DateRenal: >90% hepatobiliary excretion — safe in CKD Stage 3–5 (start at 0.5 mg pre-meal and titrate slowly). Hepatic: Contraind
Reviewed: 2026-11-10
Safety Matrix:⚖️ Legal Status: Schedule H & Schedule G Prescription Drug ('Caution:🚨 Clinically High-Alert: Independent Dose & Route Verification Required

1. Clinical & Scientific Overview

Repaglinide (TIP-MED-000063, Reference Code [4.19]) is classified under Antidiabetic Medicines, Insulins & GLP-1 Agonists (Ch 04) as a Short-Acting Meglitinide Prandial Insulin Secretagogue (Schedule H). Within the Indian regulatory and compendial framework, it is governed under Schedule H & Schedule G Prescription Drug ('Caution: It is dangerous to take this preparation except under medical supervision' — Drugs Rules 1945).

Verified Indian Market Examples / Compendial Status:
Representative Indian Market Examples (Edition 2.7 Ch 04 [4.19], p. 54): Eurepa (Torrent), Novonorm (Novo Nordisk), Regan (Sun) — Strengths & Dosage Forms: Tablets: 0.5 mg, 1 mg, 2 mg; FDCs with Metformin or Voglibose
Representative Indian Market Examples (Edition 2.7 Ch 04 [4.19], p. 54): Eurepa (Torrent), Novonorm (Novo Nordisk), Regan (Sun) — Strengths & Dosage Forms: Tablets: 0.5 mg, 1 mg, 2 mg; FDCs with Metformin or Voglibose
Dosage Forms & Available Strengths:
Tablets: 0.5 mg, 1 mg, 2 mg; FDCs with Metformin or Voglibose
Routes: Oral / Parenteral / Topical as specified by formulation

3. Mechanism of Action & Pharmacodynamics

Short-Acting Meglitinide Prandial Insulin Secretagogue (Schedule H) acting on target receptor/enzyme pathways in Antidiabetic Medicines, Insulins & GLP-1 Agonists (Ch 04): clinical efficacy is mediated via Short-Acting Meglitinide Prandial Insulin Secretagogue (Schedule H) for Type 2 Diabetes Mellitus with predominant postprandial hyperglycaemia, irregular meal schedules, or CKD Stage 3b–5 where Sulfonylureas (Glimepiride/Glibenclamide) cause prolonged hypoglycaemia.

4. Therapeutic Indications & Evidence-Supported Uses

  • Type 2 Diabetes Mellitus with predominant postprandial hyperglycaemia, irregular meal schedules, or CKD Stage 3b–5 where Sulfonylureas (Glimepiride/Glibenclamide) cause prolonged hypoglycaemia

🇮🇳 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: Start 0.5 mg PO 15 minutes before each main meal (1–2 mg if transferring from another OAD); titrate to max 4 mg per meal (Max 16 mg/day)

Administration & Meal Timing: Take 15–30 minutes BEFORE each main meal. GOLDEN RULE: '1 Meal = 1 Dose; Skip Meal = SKIP Dose!' | 15 Minutes Before Breakfast, Lunch & Dinner (Prandial TDS)

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: >90% hepatobiliary excretion — safe in CKD Stage 3–5 (start at 0.5 mg pre-meal and titrate slowly). Hepatic: Contraindicated in severe liver disease
Elimination & Renal Adjustment:
Renal: >90% hepatobiliary excretion — safe in CKD Stage 3–5 (start at 0.5 mg pre-meal and titrate slowly). Hepatic: Contraindicated in severe liver disease
Hepatic Impairment Considerations:
Renal: >90% hepatobiliary excretion — safe in CKD Stage 3–5 (start at 0.5 mg pre-meal and titrate slowly). Hepatic: Contraindicated in severe liver disease

7. Contraindications, Precautions & High-Risk Warnings

Contraindications & Red-Flag Precautions:
  • ABSOLUTELY CONTRAINDICATED with Gemfibrozil! Contraindicated in Type 1 DM, DKA, and severe hepatic impairment (Child–Pugh C)

Key Clinical Precautions: Renal: >90% hepatobiliary excretion — safe in CKD Stage 3–5 (start at 0.5 mg pre-meal and titrate slowly). Hepatic: Contraindicated in severe liver disease

8. Adverse Effects Profile

Common & Mechanism-Related Adverse Effects:
  • Mild hypoglycaemia (significantly shorter and less frequent than Glibenclamide/Glimepiride), slight weight gain, URI
  • Severe hypoglycaemia (especially if taken without eating or combined with CYP2C8 inhibitors!)
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

  • CRITICAL CONTRAINDICATED INTERACTION: Gemfibrozil (CYP2C8 inhibitor) increases Repaglinide AUC 8-fold and Clopidogrel (CYP2C8 inhibitor via glucuronide metabolite) increases Repaglinide AUC 4–5-fold -> severe prolonged hypoglycaemia! (Limit Repaglinide to max 0
  • 5 mg pre-meal if on Clopidogrel; never combine with Gemfibrozil!)
  • Cyclosporine and Trimethoprim also increase levels

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: Follow the strict rule: 'Eat a meal = Take a tablet; Skip a meal = Skip the tablet!' Carry glucose tablets/sugar sachets; verify patient is NOT taking Clopidogrel or Gemfibrozil
  • Meal & Clock Timing Instruction: Take 15–30 minutes BEFORE each main meal. GOLDEN RULE: '1 Meal = 1 Dose; Skip Meal = SKIP Dose!' (15 Minutes Before Breakfast, Lunch & Dinner (Prandial TDS))
  • Missed Dose Protocol: If forgotten before a meal and meal is already finished, SKIP that dose completely! Never take between meals
  • Geriatric Dispensing Pearl: Safer than long-acting Sulfonylureas in elderly CKD patients, provided Clopidogrel interaction is screened

Storage, Stability & Dispensing Safeguards: Store below 25°C–30°C in original moisture- and light-resistant packaging out of reach of children. Available forms: Tablets: 0.5 mg, 1 mg, 2 mg; FDCs with Metformin or Voglibose

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 04 [4.19] (p. 54)

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/4-19-repaglinide/, 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.