Properties
What is it?
DANOBIN General Description: International Nonproprietary Name: Doxofylline; Main physical and chemical properties: Light orange syrup with a pleasant aroma. Composition: 5 ml of syrup contains: Doxofylline – 100 mg; Excipients: Acrysol K-150 (PEG-40 hydrogenated castor oil), sucrose, sodium methylparaben, sodium propylparaben, sodium saccharin, aspartame, disodium edetate, citric acid monohydrate, Sunset Yellow FCF (E 110) dye, orange liquid flavor, mint liquid flavor, bitter taste masking liquid flavor, purified water. Dosage form: Syrup. Pharmacological group: Bronchodilators; Phosphodiesterase inhibitors. Pharmacological properties: Pharmacodynamic properties. Doxofylline (7-(1,3-dioxolan-2-methyl) theophylline) is a new type of xanthine-series bronchodilator, which differs from theophylline in that the dioxolane group is located at the seventh position. Like theophylline, the mechanism of action of doxofylline is related to phosphodiesterase inhibition. However, unlike theophylline, it is characterized by lower affinity for adenosine A1 and A2 receptors, which increases the safety of the drug. Clinical observations have revealed the bronchodilating properties of doxofylline in patients with bronchial asthma and chronic obstructive pulmonary disease. Doxofylline reduces the number of asthma attacks and the frequency of beta-2-agonist use. Based on safety data, the drug shows better tolerance towards the cardiovascular, digestive, and central nervous systems. No correlation between serum doxofylline levels and any side effects has been observed. During clinical studies, no sleep disturbances, chronotropic effect on the heart, or increased gastric secretion were observed. Pharmacokinetic properties. The half-life of doxofylline is over 6 hours, so a constant effective level in plasma can be maintained with three-times-daily dosing. The kinetics of oral administration have been studied in humans to determine the distribution and absorption of the drug. In the distribution phase, plasma AUC was only a small fraction of the total AUC. Plasma clearance was high, with values ranging from 444 to 806 ml/min, and the volume of distribution was approximately 1 L/kg. The drug is rapidly absorbed, with maximum plasma concentration reached within 30 minutes. Absolute bioavailability upon oral administration is approximately 62.6%; at pH 7.4, the protein binding of the product in plasma is approximately 48%. Less than 4% of the oral dose is excreted unchanged in the urine. Indications: • Bronchial asthma and chronic obstructive pulmonary disease. Method of administration and dosage: Children up to 12 years old: The recommended daily dose of doxofylline is 12 mg/kg per day, divided into two doses. If the result is insufficient, the dose can be increased to 18 mg/kg under medical supervision. From 12 to 18 years old: 1 measuring cup = 10 ml (200 mg) 2-3 times a day. Adults: 2 measuring cups = 20 ml (400 mg) 2 times a day. Elderly: 1 measuring cup = 10 ml (200 mg) 2 times a day. Side effects: Rarely observed: nausea, vomiting, headache, irritability, insomnia, palpitations, and tachycardia. In case of any side effect not listed in the instructions for use, the patient should consult their doctor. Contraindications: Contraindicated in patients with hypersensitivity to the active substance or any ingredient of the preparation. Interactions with medicinal products and other types of interactions: Doxofylline should not be administered with other xanthine derivatives. Cases of toxic synergism between xanthines and ephedrine have been described. Some drugs inhibit the elimination of xanthines (including doxofylline) from the body, for example: erythromycin, troleandomycin, lincomycin (and other antibiotics of this group), allopurinol, cimetidine, ranitidine, propranolol, influenza vaccine. No correlation between serum doxofylline levels and side effects has been observed. Overdose: Although serious cardiac rhythm disturbances have not been confirmed with the use of doxofylline, they cannot be completely ruled out in case of overdose of xanthine compounds. In case of significant overdose, palpitations may occur, which is its main symptom. In case of development of side effects, it is necessary to discontinue treatment. Resumption of treatment at a lower dose is permissible only after consulting a doctor. Pregnancy and lactation: Animal studies have shown that doxofylline does not cause fetal damage and does not affect reproductive capacity. Nevertheless, it is prescribed during pregnancy only in cases of extreme necessity. Doxofylline is contraindicated in nursing mothers. Special instructions: The half-life of doxofylline may increase in cases of severe liver and heart failure. Some drugs inhibit the elimination of xanthines (including doxofylline) from the body, for example: erythromycin, troleandomycin, lincomycin (and other antibiotics of this group), allopurinol, cimetidine, propranolol, influenza vaccine. In this case, a reduction in the dose of doxofylline is necessary. Phenytoin, like other anticonvulsants, and smoking increase the elimination and half-life of doxofylline: in this case, an increase in dose may be necessary. Doxofylline should be prescribed with caution in patients with gastric or duodenal ulcer disease and in the elderly with impaired liver function. Effect of the preparation on the ability to drive and operate machinery: The preparation does not affect the ability to drive vehicles and operate machinery. Packaging: 100 ml polymer bottle with a 10 ml measuring cap. Storage conditions: Store at a temperature not exceeding 25°C in the original packaging. Keep out of reach of children. The preparation should not be used if any visible defects are detected upon visual inspection. Shelf life: 2 years. The preparation should not be used after the expiry date indicated on the packaging. Pharmacy dispensing condition: Pharmaceutical product group III, dispensed without a prescription.