Doxophylline is used to treat the following indications:

• Bronchial asthma
• Bronchospasm
• Chronic obstructive pulmonary disease (COPD)
• Pulmonary disease with spastic bronchial component

Doxophylline is a novel bronchodilator. It structurally differs from theophylline due to the presence of a dioxolane group in position 7. Doxophylline selectively inhibits phosphodiesterase 4, thereby relaxing bronchial smooth muscle. However, unlike theophylline, doxophylline appears to have decreased affinity toward adenosine A1 and A2 receptors, which may account for the better safety profile of the drug. Doxophylline is reported to inhibit platelet activating factor (PAF) and the generation of leukotriene production.

Elderly: 200 mg tablet two or three times daily.

Adults: 400 mg tablet two or three times daily, or as prescribed by the physician.

Children:

• 12 years of age: 10 ml syrup or 200 mg tablet two or three times daily.

• 6–12 years of age: 6–9 mg per kg body weight two times daily. For example, if body weight is 10 kg, give 3 ml (60 mg) two times daily, or as prescribed by the physician.

If the required daily dose of doxophylline is 400 mg, then doxophylline SR tablet should be taken once daily, or as prescribed by the physician.

Doxophylline should not be administered with other xanthine preparations. It is recommended to limit consumption of beverages and food containing caffeine. Caution should be exercised when administering doxophylline together with ephedrine or other sympathomimetic drugs. The concurrent administration of many drugs such as erythromycin, TAO (troleandomycin), lincomycin, clindamycin, allopurinol, cimetidine, influenza vaccine, and propranolol may reduce the hepatic clearance of xanthine derivatives, leading to an increase in the plasmatic levels of the drug. Phenytoin, other anticonvulsants, and cigarette smoking may increase the clearance of xanthine derivatives with a reduction in plasmatic half-life. In these cases, it may be necessary to increase the dosage of the drug.

Doxophylline is contraindicated in individuals with known hypersensitivity to the drug or other xanthine derivatives. It is also contraindicated in patients with acute myocardial infarction, hypotension, and during lactation.

Patients treated with xanthine derivatives may experience nausea, vomiting, epigastric pain, headache, irritability, insomnia, tachycardia, extrasystoles, tachypnea, and, in rare cases, hyperglycemia or albuminuria. In case of overdose, severe cardiac arrhythmias and tonic-clonic seizures may occur. These effects may represent the first signs of intoxication. The appearance of side effects may require discontinuation of the treatment. If necessary, at the physician's discretion, treatment may be resumed at lower doses after all signs and symptoms of toxicity have subsided.

Pregnancy and Lactation: Animal tests have shown that the active ingredient of doxophylline does not interfere with pre- and postnatal growth. However, as there is not sufficient clinical evidence about the effects of the drug during pregnancy, use of the drug during pregnancy should be evaluated carefully on a case-by-case basis according to the risk-benefit ratio. The drug is contraindicated during lactation.

Effects on ability to drive and use machines: The product does not affect the patient's alertness and therefore does not interfere with his/her ability to drive and use machines.

Numerous factors may reduce the hepatic clearance of xanthine derivatives, leading to increased plasma levels of the drug. These factors include age, congestive cardiac decompensation, chronic obstructive pulmonary disease (COPD), severe liver disease, concomitant infections, and the concurrent administration of several drugs such as erythromycin, TAO (troleandomycin), lincomycin, clindamycin, allopurinol, cimetidine, influenza vaccine, and propranolol. In these cases, it may be necessary to reduce the dosage of the drug. In the presence of factors that may influence the clearance of xanthine derivatives, monitoring of blood levels of the drug is recommended to control the therapeutic range.

Caution should be taken when administering the product to patients with cardiac disease, hypertension, in the elderly, in patients with severe hypoxemia, hyperthyroidism, chronic cor pulmonale, congestive heart failure, liver disease, peptic ulcer, and in those with renal impairment. In particular, it should be used with caution in patients with congestive heart failure, since the clearance of the drug is considerably slower in these patients, in whom high blood levels may persist for long periods even after discontinuation of treatment. There is no risk of addiction or any other form of dependence.

In case of overdose, severe cardiac arrhythmias and tonic-clonic seizures may occur. These effects may represent the first signs of intoxication. The appearance of side effects may require discontinuation of treatment. If necessary, at the physician's discretion, treatment may be resumed at lower doses after all signs and symptoms of toxicity have subsided. As there is no specific antidote, in case of overdose, symptomatic treatment of cardiovascular collapse should be instituted.

Bronchodilator, Methylxanthine derivatives

Keep in a dry place away from light and heat. Keep out of the reach of children. Doxophylline should be used only on prescription of a specialist physician.