Included in the formulation
АТХ:R.03.D.A.04 Theophylline
Pharmacodynamics:It 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, the empty stomach is completely absorbed in the gastrointestinal tract. The maximum concentration in the blood plasma is reached after 2 hours. The connection with plasma proteins is 40-60%.
Penetrates through the blood-brain and placental barrier, is found in breast milk. Metabolism in the liver to inactive metabolites.
The half-life is 6-12 hours. Elimination by the kidneys.
Indications:It is used for the treatment of chronic obstructive pulmonary diseases, bronchial asthma, pulmonary hypertension, emphysema. Used in combination therapy with edematous syndrome, pulmonary hypertension, nocturnal apnea.
X.J40-J47.J43 Emphysema
X.J40-J47.J43.9 Emphysema (lung) (pulmonary)
X.J40-J47.J45 Asthma
VI.G40-G47.G47.3 Apnea in a dream
IX.I26-I28.I27.9 Pulmonary heart disease, unspecified
X.J40-J47.J46 Asthmatic status [status asthmaticus]
IX.I26-I28.I27.0 Primary pulmonary hypertension
X.J40-J47.J42 Chronic bronchitis, unspecified
X.J40-J47.J44 Other chronic obstructive pulmonary disease
X.J40-J47.J44.9 Chronic obstructive pulmonary disease, unspecified
XIV.N00-N08.N04 Nephrotic syndrome
Contraindications:Stomach ulcer and duodenal ulcer, epilepsy, tachyarrhythmia, bleeding from the gastrointestinal tract,hemorrhage into the retina of the eye, individual intolerance, children under 3 years old.
Carefully:Severe cardiovascular and pulmonary diseases, porphyria, prostatic hypertrophy, convulsive alertness, hypersensitivity.
Pregnancy and lactation:Recommendations for FDA - Category C. It is used with caution during pregnancy and lactation in cases where the intended benefit exceeds the risk to the fetus and newborn.
Dosing and Administration:Use in children
Contraindicated up to three years of age.
Inside, depending on age:
3-9 years - 24 mg / kg per day;
9-12 years - 20 mg / kg each per day;
12-16 years old - 18 mg / kg per day;
16-18 years old - 13 mg / kg per day or 900 mg per day.
The frequency of admission depends on the clinical picture of the disease.
Adults Inside, 100-200 mg 2-4 times a day.
The highest daily dose: 1.2 g.
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 theophylline to toxic.
Increases the clearance of theophylline smoking.
β2-adrenomimetics, caffeine and furosemide increase the effect of theophylline.
Aminoglutethimide enhances the excretion of theophylline.
Special instructions:When treating with retard forms, periodic monitoring of the theophylline concentration in blood plasma is necessary - it should not exceed 20 μg / ml.