A fixed-dose combination of two methylxanthine derivatives, Etofylline and Theophylline, used primarily as a bronchodilator and respiratory stimulant. Etofylline is a theophylline derivative with improved solubility and a more favorable side effect profile. The combination provides synergistic bronchodilation and is widely used in India for the management of reversible airway obstruction.
Adult: One tablet (Etofylline 77mg + Theophylline 23mg) two to three times daily. Maximum: 3 tablets per day. Dosage must be individualized based on response and serum levels.
Note: Administer with or after food to minimize gastric irritation. Tablets should be swallowed whole with a full glass of water. Avoid taking with high-fat meals as it can increase absorption rate. Maintain consistent timing of doses.
The combination exerts bronchodilation through multiple mechanisms. Primarily, they act as non-selective phosphodiesterase (PDE) inhibitors, increasing intracellular cyclic AMP (cAMP) and cyclic GMP (cGMP) in bronchial smooth muscle cells, leading to relaxation. They are also non-selective adenosine receptor antagonists (A1, A2a, A2b, A3), which prevents adenosine-induced bronchoconstriction. Additionally, they may increase diaphragmatic contractility and stimulate the respiratory center in the medulla.
Pregnancy: Category C: Animal studies show risk, human data limited. Use only if potential benefit justifies potential fetal risk. Theophylline crosses the placenta. Neonatal tachycardia, irritability, and apnea have been reported. Monitor serum levels.
Driving: May impair ability to drive or operate machinery due to potential for dizziness, nervousness, or visual disturbances. Patients should be cautioned until their individual response is known.
| Ciprofloxacin/Enoxacin | Markedly decreases Theophylline clearance, leading to toxicity | Major |
| Erythromycin/Clarithromycin | Decreases Theophylline clearance, increases serum levels | Major |
| Phenytoin/Carbamazepine/Phenobarbital | Increases Theophylline clearance, decreases serum levels and efficacy | Major |
| Cimetidine | Decreases Theophylline clearance, increases serum levels | Major |
| Fluvoxamine | Potent inhibitor of CYP1A2, significantly increases Theophylline levels | Major |
| Beta-blockers (e.g., Propranolol) | Antagonize bronchodilator effect; may cause bronchospasm | Moderate |
| Lithium | Theophylline increases renal lithium excretion, decreasing lithium levels | Moderate |
| Warfarin | Theophylline may potentiate anticoagulant effect | Moderate |
Same composition (Etofylline (77mg) + Theophylline (23mg)), different brands: