Aerofillin of the tab. of 400 mg No. 20

Pharmacological properties

Pharmacodynamics. doxofillin affects only unstriated muscles of pulmonary vessels and bronchial tubes, causing a bronkhodilatation. it is connected with ability to inhibit enzyme fde that is followed by increase in intracellular contents tsamf. accumulation in cages tsamf slows down compound of myosin with actin which reduces sokratitelny activity of unstriated muscles and promotes, in particular, relaxation of muscles of bronchial tubes and elimination of a bronchospasm. unlike other methylxanthines, doxofillin does not block adenosine receptors and does not influence transport of calcium ions. thus, medicine has no promoting effect on central nervous system and does not influence performance of cardiac, vessels and kidneys.

Pharmacokinetics. T _½ doxofillina makes 6 h therefore use of medicine 3 times a day is allowed that provides constant and effective concentration of medicine in blood plasma. After intake of medicine in the form of the tablets C _max in blood plasma it is reached in 60 min. The absolute bioavailability at oral administration is about 62.6%; at value rn 7.4 amount of medicine which contacts proteins of blood plasma are about 48%.

At oral administration of 4% of a doxofillin it is removed with urine in not changed look.

Indication

Oh, diseases of lungs with a bronchial spastic component (hobl).

Use

Dose of medicine is established by the doctor individually depending on age, body weight and features of metabolism of the patient. the average daily dose for adults and children is aged more senior than 12 years makes 800–1200 mg (1 tablet 2–3 times a day). to children at the age of 6–12 years appoint ½ tablets 2–3 times a day (12–18 mg/kg of body weight a day).

Contraindication

Hypersensitivity to a doxofillin or other components of medicine and also other derivatives of xanthine, a sharp myocardial infarction, arterial hypotension.

Side effects

from a GIT: nausea, vomiting, pain in epigastric area, a gastroesophagal reflux, are seldom possible diarrhea, dyspepsia.

from nervous system: irritability, headache, insomnia, dizziness, tremor.

from a cardiovascular system: premature ventricular contraction, heart consciousness.

from a respiratory system: tachypnea.

from the system of blood: in isolated cases — a hyperglycemia, an albuminuria.

Allergic reactions: are seldom possible an acute anaphylaxis (Quincke's disease).

Special instructions

With care should use medicament for treatment of patients with a cardiopathy, ag, elderly people and patients with a severe form of a hypoxia, a hyper thyroidism, chronic right ventricular insufficiency, stagnant heart failure, diseases of a liver and kidneys, a round ulcer and also at the increased body temperature, cardiac arrhythmias, alcoholism. the extra care should be observed at treatment of patients with chronic heart failure as they reduce removal of medicine from blood which lasts throughout the long period, even after the end of treatment.

in the presence of the factors influencing removal of derivatives of xanthine monitoring of concentration of medicine to blood for therapy control.

Drug contains lactose therefore patients with rare hereditary forms of intolerance have galactoses, insufficiency of lactase or a syndrome of glyukozo-galaktozny malabsorption it is not necessary to apply it.

Period of pregnancy and feeding by a breast. In view of limited experience of use of medicine during pregnancy doxofillin it is possible to appoint only taking into account a ratio advantage for mother/risk for a fruit. Doxofillin is contraindicated during feeding by a breast.

Children. Drug is used at children aged 6 years are more senior.

Ability to influence speed of response at control of vehicles and work with other mechanisms. Does not influence.

Interaction

consumption of the foodstuff and drinks containing caffeine. it is not necessary to apply along with other medicines containing xanthines. it is necessary to be careful at the combined application of an aerofillin and sympathomimetics. simultaneous use of such medicines as erythromycin, troleandomitsin, lincomycin, clindamycin, Allopyrinolum, Cimetidinum, the vaccine against flu, propranolol and also in interaction of xanthines with Disulfiramum, fluvoksaminy, interferon an alpha, oral contraceptives can slow down removal of derivatives of xanthine, at the same time medicine level in blood plasma can increase. in such cases it is necessary to lower a medicine dose.

At use of Phenytoinum, other anticonvulsants and tobacco smoking and also in interaction of xanthines with rifampicin, ritonaviry, Sulfinpyrazonum elimination of derivatives of xanthine can accelerate, at this T _½ decreases. In these cases it is necessary to raise a medicine dose.

At xanthines noted toxic synergism with ephedrine, a halothane or ketamine, also it can counteract action of adenosine and other blockers of neuromuscular transfer.

Elimination of lithium can increase with the subsequent reduction of expressiveness of effect.

Xanthines can strengthen the hypopotassemia caused by a hypoxia or connected with application of stimulators β ₂ - adrenoceptors (agonists β ₂ - adrenoceptors), corticosteroids and diuretic medicines.

Considering the pharmacological reasons, it is necessary to avoid simultaneous use of xanthines and blockers of β-adrenoceptors as the last lead to emergence of a bronchospasm.

Overdose

Symptoms: cardiac arrhythmias, spasms (tonic, clonic), agitation, strengthening of a diuresis, strengthening of expressiveness of manifestations of side effects.

Treatment: as there is no specific antidote, in case of overdose carry out symptomatic therapy of heart failure, anticonvulsant therapy. After disappearance of symptoms of intoxication the use of medicine can be resumed.

Storage conditions

At a temperature not above 25 °C.