THE INDIAN PHARMACIST Official Circular Pharmacy Logo THE INDIAN PHARMACISTLearn. Explore. Practise. Excel.
MEDICINE MONOGRAPH CODE: [9.15] ID: TIP-MED-000179

Roflumilast

Active Ingredient / Scientific Identity: Roflumilast • Class: Selective Phosphodiesterase-4 (PDE-4) Anti-Inflammatory Inhibitor for Severe COPD (Schedule H)

⚖️ Compare Profile
THE INDIAN PHARMACIST — Educational Reference Sheet
Profile: Roflumilast ([9.15] | ID: TIP-MED-000179) • Last Reviewed: 2026-11-10
Source URL: https://theindianpharmacist.com/medicine/9-15-roflumilast/
Generic / Entity NameRoflumilast ([9.15])
Verified Indian Brands / RefGeneric Compendial Entry (No Commercial Brand Claimed)
Pharmacological ClassSelective Phosphodiesterase-4 (PDE-4) Anti-Inflammatory Inhibitor for Severe COPD (Schedul
Available Dosage FormsTablets: 250 mcg (initiation dose), 500 mcg (maintenance dose)
Regulatory ClassificationSchedule H Prescription Drug (To be sold by retail on the prescription of a Registere
Key Warning & Review DateRenal: No dose adjustment needed in CKD. Hepatic: Moderate-to-Severe (Child–Pugh B or C): STRICTLY CONTRAINDICATED!
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

Roflumilast (TIP-MED-000179, Reference Code [9.15]) is classified under Respiratory, Asthma, COPD & Allergy Medicines (Ch 09) as a Selective Phosphodiesterase-4 (PDE-4) Anti-Inflammatory Inhibitor for Severe COPD (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:
Representative Indian Market Examples (Edition 2.7 Ch 09 [9.15], p. 121): Rofaday (Cipla), Daliresp, Roflupin (Lupin), Fibroventil — Strengths & Dosage Forms: Tablets: 250 mcg (initiation dose), 500 mcg (maintenance dose)
Representative Indian Market Examples (Edition 2.7 Ch 09 [9.15], p. 121): Rofaday (Cipla), Daliresp, Roflupin (Lupin), Fibroventil — Strengths & Dosage Forms: Tablets: 250 mcg (initiation dose), 500 mcg (maintenance dose)
Dosage Forms & Available Strengths:
Tablets: 250 mcg (initiation dose), 500 mcg (maintenance dose)
Routes: Oral / Parenteral / Topical as specified by formulation

3. Mechanism of Action & Pharmacodynamics

Selective Phosphodiesterase-4 (PDE-4) Anti-Inflammatory Inhibitor for Severe COPD (Schedule H) acting on target receptor/enzyme pathways in Respiratory, Asthma, COPD & Allergy Medicines (Ch 09): clinical efficacy is mediated via Selective Phosphodiesterase-4 (PDE-4) Anti-Inflammatory Inhibitor for Severe COPD (Schedule H) for Add-on anti-inflammatory maintenance therapy in Severe-to-Very-Severe COPD (post-bronchodilator FEV1 <50% predicted) associated with chronic bronchitis and a history of frequent exacerbations despite LABA+LAMA(+ICS) therapy (GOLD 2024–2026 Group E).

4. Therapeutic Indications & Evidence-Supported Uses

  • Add-on anti-inflammatory maintenance therapy in Severe-to-Very-Severe COPD (post-bronchodilator FEV1 <50% predicted) associated with chronic bronchitis and a history of frequent exacerbations despite LABA+LAMA(+ICS) therapy (GOLD 2024–2026 Group E)

🇮🇳 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 at 250 mcg PO Once Daily for the first 4 weeks (improves GI tolerability!), then increase to target maintenance dose of 500 mcg PO Once Daily

Administration & Meal Timing: May be taken with or without food at the same time each day | Morning (Once Daily)

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: No dose adjustment needed in CKD. Hepatic: Moderate-to-Severe (Child–Pugh B or C): STRICTLY CONTRAINDICATED!
Elimination & Renal Adjustment:
Renal: No dose adjustment needed in CKD. Hepatic: Moderate-to-Severe (Child–Pugh B or C): STRICTLY CONTRAINDICATED!
Hepatic Impairment Considerations:
Renal: No dose adjustment needed in CKD. Hepatic: Moderate-to-Severe (Child–Pugh B or C): STRICTLY CONTRAINDICATED!

7. Contraindications, Precautions & High-Risk Warnings

Contraindications & Red-Flag Precautions:
  • CONTRAINDICATED in moderate-to-severe hepatic impairment (Child–Pugh B or C) and patients with history of severe depression with suicidal ideation! Not a bronchodilator and NEVER for acute bronchospasm

Key Clinical Precautions: Renal: No dose adjustment needed in CKD. Hepatic: Moderate-to-Severe (Child–Pugh B or C): STRICTLY CONTRAINDICATED!

8. Adverse Effects Profile

Common & Mechanism-Related Adverse Effects:
  • Diarrhoea (10%), unexplained weight loss (5–10% of patients lose 2–4 kg!), nausea, decreased appetite, headache, insomnia, back pain, dizziness
  • Psychiatric adverse events (insomnia, anxiety, new or worsening depression, suicidal ideation/behaviour — boxed warning!), severe cachexia/weight loss in underweight COPD patients (BMI <18.5 kg/m2)
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

  • Strong CYP450 inducers (Rifampicin, Carbamazepine, Phenytoin, Phenobarbital) reduce anti-inflammatory activity by 60% (avoid combination!); CYP1A2/3A4 inhibitors (Fluvoxamine, Enoxacin, Cimetidine, Erythromycin, Ketoconazole) increase systemic exposure; do not combine with Theophylline!

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: Start with 250 mcg daily for 1 month before stepping up to 500 mcg to minimise loose stools and nausea; weigh yourself monthly and inform your doctor if you lose weight or feel persistently sad, anxious, or unable to sleep
  • Meal & Clock Timing Instruction: May be taken with or without food at the same time each day (Morning (Once Daily))
  • Missed Dose Protocol: Take same day if remembered; skip if next day
  • Geriatric Dispensing Pearl: Monitor BMI/weight loss and mood closely in frail elderly COPD patients

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: 250 mcg (initiation dose), 500 mcg (maintenance dose)

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 09 [9.15] (p. 121)

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.

← Back to All 644 Reference Profiles 📖 Explore 40 Knowledge Hub Articles → ✉️ Report Errata / Feedback
Educational Reference Notice: This printout from THE INDIAN PHARMACIST (https://theindianpharmacist.com/medicine/9-15-roflumilast/, 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.