Included in the formulation
АТХ:R.03.D.A.02 Choline theophylline
Pharmacodynamics:Theophylline salt blocks adenosine α1-receptors of smooth muscle cells, inhibits cAMP phosphodiesterase, which leads to accumulation of cAMP in cells and a decrease in the content of calcium ions. As a result, the interaction of actin and myosin is disturbed due to a decrease in the activity of myosin light chain kinase, which is manifested by an antispasmodic effect on the smooth musculature of the bronchi and blood vessels.
An increase in the concentration of cAMP together with a decrease in the content of calcium ions in mast cells prevents their degranulation, which is accompanied by the release of inflammatory mediators and allergies.
In cardiomyocytes, by decreasing the intracellular concentration of calcium ions, the force of the cardiac contractions increases, which is manifested by tachycardia.
Strengthens the processes of mucociliary clearance, reduces pulmonary vascular resistance, stimulates the respiratory center, helps improve the contraction of respiratory muscles. Has a weak diuretic and antiaggregant effect.
Pharmacokinetics:After oral administration, up to 90% is absorbed in the gastrointestinal tract. The maximum concentration in the blood plasma is reached after 2 hours. The connection with plasma proteins is 55-65%.
Metabolism in the liver.
The half-life is 4.5 hours. Elimination by the kidneys.
Indications:It is used to prevent bronchospasm in chronic obstructive pulmonary diseases, bronchial asthma, pulmonary hypertension and pulmonary emphysema.
X.J40-J47.J40 Bronchitis, not specified as acute or chronic
X.J40-J47.J43 Emphysema
X.J40-J47.J45 Asthma
Contraindications:Ischemic heart disease, peptic ulcer of stomach and duodenum, individual intolerance, children under 10 years old.
Carefully:Severe cardiovascular and pulmonary diseases, hypersensitivity.
Pregnancy and lactation:Recommendations for FDA - Category B. It is used during pregnancy and lactation.
Dosing and Administration:Use in children
at the age of 10-14 years: inside at 15-22 mg / kg per day in 4 divided doses.
Adults
Inside, 200-400 mg 4 times a day.
The highest daily dose: 1600 mg.
The highest single dose: 400 mg.
Side effects:Central and peripheral nervous system: headache, dizziness, nervousness, sleep disorders, convulsions.
Hemopoietic system: anemia, leukopenia, thrombocytopenia.
The cardiovascular system: tachycardia, arterial hypotension.
Digestive system: gastralgia, nausea, vomiting, diarrhea.
Dermatological reactions: pruritus, contact dermatitis
Allergic reactions.
Overdose:Blood vomiting, microhematuria, albuminuria, hyperreflexia, clonic and tonic convulsions, collapse, dehydration, fever.
Treatment is symptomatic.
Interaction:Strengthens the effects of thiazide diuretics and cardiac glycosides.
Reduces the uricosuric effect of pyrazolone derivatives and probenecid.
Erythromycin increases the concentration of choline theophylline to toxic.
Increases the clearance of choline theophylline smoking.
Special instructions:In the treatment of children, simultaneous use, including rectal, with other xanthine derivatives is not recommended.