Characteristics

Theospirex retard contains 100% of active theophylline. The drug exerts strong and dose-dependent dilatory activity on smooth muscles of the bronchi, broncholi and blood vessels. Theophylline stimulates respiratory center, induces positive ino- and chronotropic activity in myocardium, increases diuresis and decreases edema.

Uniform and pH independent release of the active ingredient from the tablet guarantees constant level of blood theophylline over 12 hours. Thanks to the prolonged action, Theospirex retard allows for avoiding rapid changes in blood theophylline concentration, what leads to better drug tolerance.

The tablet may be divided to adjust the required therapeutic range of blood theophylline concentration.

Continuous drug release throughout the night protects the patients with asthma both against night asthmatic attacks, as well as against worsening of physical condition in the morning.

Therapeutical indications

Mostly as a form of the preventive treatment of asthmatic attacks and dyspnea in patients with:

• bronchial asthma

• spastic bronchitis

• chronic pulmonary emphysema

Contraindications

Theospirex retard should not be used in patients with diagnosed hypersensitivity to theophylline and other xanthine derivatives. The drug should be used with caution in patients with recent myocardial infarction, cardiac arrhythmia, hyperthyreosis, epilepsy, chronic heart failure, diseases of the liver, gastric and duodenal ulcers. Formulations containing theophylline formulations should be used under strict medical supervision in pregnancy, particularly during the first trimester. Administration of the drug in the period of breast-feeding is not recommended.

Interactions with other drugs

Administration of Theospirex simultaneously with other formulations containing xanthine may lead to exacerbation of undesirable effects. Macrolide antibiotics (such as erythromycine), allopurinol, tiabendazl, cimetidine and oral contraceptives may lead to increased blood theophylline concentration.
Smoking, phenobarbital, phenytoin, carbamazepine result in lower blood theophylline concentrations.
Administration of theophylline simultaneously with drugs stimulating the sympathetic nervous system, frusemide, cardiac glycosides and reserpine enhances the activity of these substances. Reduction of the dose of beta-sympathomimetic drug is necessary, particularly when the latter is administrated in a form of aerosol. Theophylline decreases the activity of beta-blockers.

Dosage

The dose of Theospirex retard should be adjusted individually due to differences in its elimination profiles. In the absence of other indications the following doses are used:

• adults: 1 tablet every 12 hours after meals (8-12 mg/kg body weight daily)
  Children above 5 years of age: ½ tablet every 12 hours after meals (10-15 mg/kg body weight daily),

• children above 5 years of age: ½ tablet every 12 hours after meals (10-15 mg/kg body weight daily).

If, after three days of treatment the respiration has not been sufficiently improved and the drug is well-tolerated, the dose may be gradually increased. Adults: up to three tablets daily (max. 15 mg/kg body weight daily). Children: up to 1.5 tablets (max. 20 mg/kg body weight daily). If an undesirable effect occurs, the dose should be immediately decreased. When maximal daily dose has been exceeded, control of blood theophylline concentration is required. Hepatic damage, heart failure, renal function disturbances are the conditions requiring controlling the blood theophylline concentration.

Undesirable effects

In case of overdose or when the patient is hypersensitive to the drug, gastrointestinal disturbances, nausea, vomiting, headache, central nervous system disturbances, tachycardia and palpitation may occur. If such symptoms are present, immediately seek medical advice.

Package

50 coated tablets.