Doxofylline (400mg) + Ambroxol (30mg)

Clinical Pharmacologist's Monograph

⚠️ Prescription Only: This medicine is Schedule H/H1. Do not self-medicate.

1. Clinical Overview

A fixed-dose combination (FDC) of a methylxanthine bronchodilator (Doxofylline) and a mucolytic agent (Ambroxol) used for the management of chronic obstructive pulmonary disease (COPD) and bronchial asthma with associated productive cough. Doxofylline is a selective phosphodiesterase-4 (PDE4) inhibitor with a better safety profile than theophylline, while Ambroxol facilitates expectoration by increasing mucus clearance.

OnsetDurationBioavailability
Doxofylline: 1-2 hours; Ambroxol: 30-60 minutes.Doxofylline: Approximately 12 hours; Ambroxol: 6-12 hours.Doxofylline: ~62.6%; Ambroxol: ~70-80%.

2. Mechanism of Action

Doxofylline acts as a bronchodilator and anti-inflammatory agent by selectively inhibiting phosphodiesterase-4 (PDE4), leading to increased intracellular cAMP. This relaxes bronchial smooth muscle and inhibits the release of pro-inflammatory mediators. Ambroxol is a mucolytic and expectorant that stimulates surfactant production, depolymerizes acid mucopolysaccharide fibers in sputum, and enhances ciliary beat frequency, facilitating mucus clearance.

3. Indications & Uses

  • Chronic Obstructive Pulmonary Disease (COPD) - maintenance therapy
  • Bronchial Asthma - for relief of bronchospasm and associated productive cough

4. Dosage & Administration

Adult Dosage: One tablet (Doxofylline 400mg + Ambroxol 30mg) twice daily, preferably after meals.

Administration: Swallow the tablet whole with a glass of water, after food to minimize gastric irritation. Do not crush or chew. Maintain adequate hydration to aid mucolytic action.

5. Side Effects

Common side effects may include:

  • Nausea
  • Epigastric discomfort/Heartburn
  • Headache
  • Mild dizziness
  • Diarrhea

6. Drug Interactions

DrugEffectSeverity
Ciprofloxacin/EnoxacinMarkedly increases Doxofylline levels (CYP1A2 inhibition), risk of toxicity.Major
Phenobarbital, Phenytoin, RifampicinDecreases Doxofylline levels (CYP450 induction), may reduce efficacy.Moderate
Beta-2 Agonists (Salbutamol, Terbutaline)Additive bronchodilation; may potentiate hypokalemia and tachycardia.Moderate
Diuretics (especially Loop Diuretics)Increased risk of hypokalemia with Doxofylline.Moderate
WarfarinAmbroxol may slightly increase bleeding risk; monitor INR.Minor
Antitussives (e.g., Codeine)Counteracts the expectorant action of Ambroxol; avoid concurrent use.Moderate

7. Patient Counselling

  • DO take the tablet after meals with a full glass of water.
  • DO maintain regular dosing intervals.
  • DO inform your doctor about all other medicines you are taking.
  • DO keep yourself well-hydrated to help loosen mucus.
  • DONT crush, break, or chew the tablet.
  • DONT take an extra dose if you miss one. Skip it and take the next scheduled dose.
  • DONT start or stop any other medication without consulting your doctor.
  • DONT consume excessive caffeine (tea, coffee, cola) while on this medication.

8. Toxicology & Storage

Overdose: Primarily due to Doxofylline: Severe nausea/vomiting, hematemesis, tremors, agitation, tachycardia, arrhythmias, hypotension, seizures, metabolic acidosis. Ambroxol overdose: GI distress, salivation, nausea.

Storage: Store below 30°C, in a cool, dry place, protected from light and moisture. Keep out of reach of children.