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MEDICINE MONOGRAPH CODE: [9.14]-C92 ID: TIP-MED-000362

Doxofylline

Active Ingredient / Scientific Identity: Doxofylline • Class: Airway Muco-Regulator / Surfactant Stimulator & Novelly Substituted Xanthine Bronchodilator (Schedule H)

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THE INDIAN PHARMACIST — Educational Reference Sheet
Profile: Doxofylline ([9.14]-C92 | ID: TIP-MED-000362) • Last Reviewed: 2026-11-10
Source URL: https://theindianpharmacist.com/medicine/9-14-c92-doxofylline/
Generic / Entity NameDoxofylline ([9.14]-C92)
Verified Indian Brands / RefGeneric Compendial Entry (No Commercial Brand Claimed)
Pharmacological ClassAirway Muco-Regulator / Surfactant Stimulator & Novelly Substituted Xanthine Bronchodilato
Available Dosage FormsAcebrophylline Capsules: 100 mg IR (BD); SR Tablets: 200 mg (OD); Syrup: 50 mg/5mL. Doxofylline Tablets: 400 m
Regulatory ClassificationSchedule H Prescription Drug (To be sold by retail on the prescription of a Registere
Key Warning & Review DateRenal & Hepatic: Reduce dose (Doxofylline 200 mg BD or Acebrophylline 100 mg OD) in significant hepatic cirrhosis, congestive
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

Doxofylline (TIP-MED-000362, Reference Code [9.14]-C92) is classified under Respiratory, Asthma, COPD & Allergy Medicines (Ch 09) as a Airway Muco-Regulator / Surfactant Stimulator & Novelly Substituted Xanthine Bronchodilator (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 [9.14] (Acebrophylline & Doxofylline). Representative Indian Market Examples (Edition 2.7 Ch 09 [9.14], p. 120): Acebrophylline: AB Phylline / AB Phylline SR (Sun), Macphylline (Macleods), Ascoril AB. Doxofylline: Doxolin (Zydus), Doxovent (Glenmark), Synasma (Ranbaxy) — Strengths & Dosage Forms: Acebrophylline Capsules: 100 mg IR (BD); SR Tablets: 200 mg (OD); Syrup: 50 mg/5mL. Doxofylline Tablets: 400 mg IR (BD), 650 mg SR (OD); Syrup: 100 mg/5mL
Co-indexed constituent under primary monograph [9.14] (Acebrophylline & Doxofylline). Representative Indian Market Examples (Edition 2.7 Ch 09 [9.14], p. 120): Acebrophylline: AB Phylline / AB Phylline SR (Sun), Macphylline (Macleods), Ascoril AB. Doxofylline: Doxolin (Zydus), Doxovent (Glenmark), Synasma (Ranbaxy) — Strengths & Dosage Forms: Acebrophylline Capsules: 100 mg IR (BD); SR Tablets: 200 mg (OD); Syrup: 50 mg/5mL. Doxofylline Tablets: 400 mg IR (BD), 650 mg SR (OD); Syrup: 100 mg/5mL
Dosage Forms & Available Strengths:
Acebrophylline Capsules: 100 mg IR (BD); SR Tablets: 200 mg (OD); Syrup: 50 mg/5mL. Doxofylline Tablets: 400 mg IR (BD), 650 mg SR (OD); Syrup: 100 mg/5mL
Routes: Oral / Parenteral / Topical per formulation

3. Mechanism of Action & Pharmacodynamics

Airway Muco-Regulator / Surfactant Stimulator & Novelly Substituted Xanthine Bronchodilator (Schedule H) acting on target receptor/enzyme pathways in Respiratory, Asthma, COPD & Allergy Medicines (Ch 09): clinical efficacy is mediated via Airway Muco-Regulator / Surfactant Stimulator & Novelly Substituted Xanthine Bronchodilator (Schedule H) for Add-on maintenance therapy for COPD and chronic bronchitis with tenacious mucus hypersecretion (Doxofylline has minimal adenosine A1/A2 receptor affinity and a wider therapeutic window than conventional Theophylline!).

4. Therapeutic Indications & Evidence-Supported Uses

  • Add-on maintenance therapy for COPD and chronic bronchitis with tenacious mucus hypersecretion (Doxofylline has minimal adenosine A1/A2 receptor affinity and a wider therapeutic window than conventional Theophylline!)

🇮🇳 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: Acebrophylline: 100 mg IR PO BD after meals, or 200 mg SR PO OD after dinner. Doxofylline: 400 mg PO BD (200 mg BD in frail elderly), or 650 mg SR OD

Administration & Meal Timing: Take WITH or after meals to minimise epigastric discomfort; swallow SR tablets whole | Morning & Evening after meals (BD) or Evening after dinner (200 mg / 650 mg SR OD)

6. Pharmacokinetics, Metabolism & Renal/Hepatic Adjustment

Absorption & Disposition:
Follows class pharmacokinetic profile detailed in parent monograph [9.14].
Metabolism & Biotransformation:
Renal & Hepatic: Reduce dose (Doxofylline 200 mg BD or Acebrophylline 100 mg OD) in significant hepatic cirrhosis, congestive heart failure, or severe renal impairment
Elimination & Renal Adjustment:
Renal & Hepatic: Reduce dose (Doxofylline 200 mg BD or Acebrophylline 100 mg OD) in significant hepatic cirrhosis, congestive heart failure, or severe renal impairment
Hepatic Impairment Considerations:
Renal & Hepatic: Reduce dose (Doxofylline 200 mg BD or Acebrophylline 100 mg OD) in significant hepatic cirrhosis, congestive heart failure, or severe renal impairment

7. Contraindications, Precautions & High-Risk Warnings

Contraindications & Red-Flag Precautions:
  • Contraindicated in acute myocardial infarction, severe hypotension, uncontrolled tachyarrhythmias, active peptic ulcer, severe renal/hepatic failure, and lactation. NEVER combine Acebrophylline, Doxofylline, and Theophylline/Deriphyllin together!

Key Clinical Precautions: Renal & Hepatic: Reduce dose (Doxofylline 200 mg BD or Acebrophylline 100 mg OD) in significant hepatic cirrhosis, congestive heart failure, or severe renal impairment

8. Adverse Effects Profile

Common & Mechanism-Related Adverse Effects:
  • Mild epigastric pain, nausea, headache, dizziness, occasional palpitations or insomnia (significantly lower incidence of tachyarrhythmias, seizures, and gastric hyperacidity on Doxofylline compared with Theophylline!)
  • Supraventricular tachycardia, severe vomiting, hypokalaemia, or seizures in massive overdose
Serious / Dose-Limiting Adverse Effects:

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

    • Unlike Theophylline, Doxofylline has minimal CYP1A2 inhibition interactions with Ciprofloxacin or Clarithromycin, though caution is still advised with ephedrine/high-dose SABA, caffeine excess, Allopurinol, and Cimetidine

    10. Clinical Monitoring, Patient Counselling & Storage

    Clinical & Laboratory Monitoring: Monitor clinical parameters per parent monograph [9.14].

    Pharmacist Patient Counselling Points:

    • Patient Counselling Checklist: Take after food; verify patient is NOT also taking Deriphyllin or Unicontin (Theophylline); cut back on strong coffee/tea if you feel shaky or have a fast heartbeat
    • Meal & Clock Timing Instruction: Take WITH or after meals to minimise epigastric discomfort; swallow SR tablets whole (Morning & Evening after meals (BD) or Evening after dinner (200 mg / 650 mg SR OD))
    • Missed Dose Protocol: Take after next meal if remembered; never double dose
    • Geriatric Dispensing Pearl: Doxofylline (200–400 mg BD) is much safer than Theophylline in older COPD patients because it avoids narrow-therapeutic-index arrhythmias and Ciprofloxacin interactions

    Storage, Stability & Dispensing Safeguards: Store below 25°C–30°C in original moisture- and light-resistant packaging out of reach of children. Available forms: Acebrophylline Capsules: 100 mg IR (BD); SR Tablets: 200 mg (OD); Syrup: 50 mg/5mL. Doxofylline Tablets: 400 mg IR (BD), 650 mg SR (OD); Syrup: 100 mg/5mL

    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/9-14-c92-doxofylline/, 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.