Eufylline, tablets 150 mg 30 pcs

Pharmacotherapeutic group

The bronchodilator

ATX code[R03DA05]

Pharmacological properties

Pharmacodynamics. Bronchodilator, xanthine derivative; inhibits phosphodiesterase, increases tissue accumulation of adenosine monophosphate (cAMP), blocks adenosine (purine) receptors; reduces calcium ion influx through cell membrane channels, reduces smooth muscle contractile activity.

It relaxes the bronchial musculature, stimulates the respiratory center, increases its sensitivity to carbon dioxide and improves alveolar ventilation, which ultimately leads to a reduction in the severity and frequency of apnea episodes. By normalizing respiratory function, it helps to saturate the blood with oxygen and reduce the concentration of carbon dioxide.

It has a stimulating effect on heart activity, increases the force and number of heartbeats, increases coronary blood flow and increases myocardial oxygen demand. It reduces the tone of the blood vessels (mainly the blood vessels of the brain, skin and kidneys). It has a peripheral venodilator effect, reduces pulmonary vascular resistance, lowers the pressure in the “small” circulatory circle. Increases renal blood flow, has a moderate diuretic effect. It dilates extrahepatic biliary tracts.

Stabilizes the membranes of mast cells, inhibits the release of mediators of allergic reactions.

Inhibits platelet aggregation (inhibits platelet-activating factor and prostaglandin E2 (PgE₂), increases resistance to erythrocyte deformation (improves rheological properties of blood), reduces thrombosis and normalizes microcirculation.

It has a tocolytic effect, increases the acidity of gastric juice. When used in high doses it has epileptogenic effect.

Pharmacokinetics.

After oral administration is quickly and completely absorbed, bioavailability 90-100%. Food reduces the rate of absorption without affecting its magnitude (large volumes of liquid and proteins accelerate the process). The higher the dose taken, the lower the absorption rate. Time to reach maximum concentration is 1-2 hours. Distribution volume is in the range of 0.3-0.7 l/kg (30-70% of the “ideal” body weight), on average 0.45 l/kg. Binding to plasma proteins in adults is 60%, in patients with liver cirrhosis – 36%. It penetrates into breast milk (10% of the dose taken), through the placental barrier (concentration in fetal serum is slightly higher than in the serum of the mother).

The bronchodilator properties of aminophylline occur at concentrations of 10-20 µg/ml. Concentrations over 20 mg/ml are toxic. The excitatory effect on the respiratory center is realized at lower blood concentrations of 5-10 µg/ml.

It is metabolized at physiological pH values with release of free theophylline, which is further metabolized in the liver with the participation of several cytochrome P450 isoenzymes. As a result, caffeine and 1,3-dimethylureic acid (45-55%) are formed, which has pharmacological activity, but is 1-5 times inferior to theophylline. Caffeine is also an active metabolite, but it is formed in small amounts.

In children over 3 years of age and in adults (unlike in younger children) there is no caffeine cumulation phenomenon. Its half-life in children over 6 months is 3.7 hours, in adults 8.7 hours, in smokers (20-40 cigarettes per day) – 4-5 hours (after quitting smoking normalization of pharmacokinetics in 3-4 months); in adults with chronic obstructive pulmonary disease, “pulmonary” heart and pulmonary heart failure – over 24 hours. Metabolites are excreted by the kidneys.

Indications

Bronchoobstructive syndrome of any genesis: bronchial asthma (drug of choice in patients with asthma of physical stress and as an additional agent in other forms), chronic obstructive pulmonary disease, lung emphysema, chronic obstructive bronchitis, pulmonary hypertension, “pulmonary” heart, night apnea.

Active ingredient

Composition

1 tablet contains:

Active substance:

aminophylline 150 mg.

Excipients:

calcium stearate,

potato starch.

How to take, the dosage

The dose should be adjusted according to the individual characteristics of each patient, taking into account clinical response and stable serum eufillin concentrations.

Over the mouth, adults should be prescribed 150 mg 3-4 times a day after meals.

Children over 3 years of age should be prescribed orally at a rate of 7-10 mg/kg per day in 4 doses.

The highest doses of eufillin for adults are single 500 mg; daily 1500 mg.

Higher doses for children over 3 years of age: single dose 7 mg/kg; daily dose 15 mg/kg.

The duration of the course of treatment is from several days to several months, depending on the course of the disease and tolerance of the drug.

In order to reduce toxic effects, it should be prescribed in the lowest effective doses.

Interaction

In concomitant use with sympathomimetics mutual enhancement of action occurs; with beta-adrenoblockers and lithium preparations – action is mutually reduced. Intensity of action of aminophylline may decrease (due to increase of its clearance) during concomitant use with phenobarbital, rifampicin, isoniazid, carbamazepine, sulfinpyrazone, phenytoin and also in smokers.

. The intensity of action of aminophylline may increase (due to decreased clearance) when used concomitantly with macrolide antibiotics, lincomycin, quinolones, allopurinol, beta-adrenoblockers, cimetidine, disulfiram, fluvoxamine, oral hormonal contraceptives, isoprenaline, viloxazine and during flu vaccination.

Xanthine derivatives may potentiate hypokalemia due to the action of β2-adrenoreceptor stimulants, corticosteroids and diuretics.

Antidiarrheals and enterosorbents decrease absorption of aminophylline.

Pharmaceutically incompatible with acid solutions.

Special Instructions

Use with caution in severe coronary artery disease (acute phase of myocardial infarction, angina pectoris), widespread atherosclerosis, hypertrophic obstructive cardiomyopathy, frequent ventricular extrasystole, increased seizure rate, hepatic and/or renal failure, gastric and duodenal ulcers (history), recent GI bleeding, uncontrolled hypothyroidism (possibility of cumulation) or thyrotoxicosis, prolonged hyperthermia, gastroesophageal reflux, prostatic hypertrophy, in elderly patients, in children (especially oral).

The dosing regimen of aminophylline may need to be adjusted for heart failure, liver dysfunction, chronic alcoholism, fever, and acute respiratory infections.

Dose reduction may be required in elderly patients.

If the current dosage form of aminophylline is changed to another dosage form, clinical monitoring and monitoring of plasma theophylline concentrations is necessary.

Aminophylline is not used concomitantly with other xanthine derivatives. During treatment, consumption of food containing xanthine derivatives (strong coffee, tea) should be avoided.

Precaution is used concomitantly with anticoagulants, with other theophylline or purine derivatives.

Concomitant use with beta-adrenoblockers should be avoided.

Aminophylline should not be used concomitantly with glucose solution.

Contraindications

Side effects

CNS disorders: dizziness, sleep disturbances, anxiety, tremors, convulsions.

Cardiovascular system disorders: palpitations, heart rhythm disturbances; with rapid IV administration – occurrence of heart pain, decreased BP, tachycardia (including in the fetus when taken in the III trimester of pregnancy), arrhythmias, BP decrease, cardialgia, increased frequency of angina pectoris attacks.

Digestive system disorders: nausea, vomiting, gastroesophageal reflux, heartburn, aggravation of peptic ulcer disease, diarrhea; with prolonged oral administration – anorexia.

Urinary system disorders: albuminuria, hematuria.

Allergic reactions: skin rash, itching, fever.

Metabolism: rarely – hypoglycemia.

Others: chest pain, tachypnoea, sensation of flushes to the face, albuminuria, hematuria, hypoglycemia, increased diuresis, increased sweating.

Overdose

In case of overdose facial hyperemia, insomnia, motor agitation, anxiety, photophobia, anorexia, diarrhea, nausea, vomiting, epigastric pain, gastrointestinal bleeding, tachycardia, ventricular arrhythmias, tremor, generalized convulsions, hyperventilation, a sharp decrease in blood pressure are observed. Severe poisoning may cause epileptoid seizures (especially in children without any precursors), hypoxia, metabolic acidosis, hyperglycemia, hypokalemia, skeletal muscle necrosis, confusion, renal failure with myoglobinuria.

The treatment of overdose depends on the clinical picture and includes discontinuation of the drug, stimulation of its elimination from the body (forced diuresis, hemosorption, plasma sorption, hemodialysis, peritoneal dialysis) and prescription of symptomatic measures. Diazepam (in injections) is used to relieve seizures. Barbiturates should not be used. Hemodialysis is recommended in severe intoxication (eufillin content over 50 g/l).

Pregnancy use

Theophylline penetrates the placental barrier.

The use of aminophylline in pregnancy can lead to potentially harmful concentrations of theophylline and caffeine in the blood plasma of the newborn. Newborns whose mothers received aminophylline during pregnancy (especially in the third trimester) require medical monitoring to control possible symptoms of theophylline intoxication.

Theophylline is excreted with breast milk. When aminophylline is used in a nursing mother during lactation, irritability may occur in the baby.

Hence, the use of aminophylline during pregnancy and lactation (breastfeeding) is possible in cases when the anticipated benefit of therapy for the mother exceeds the potential risk to the fetus or child.