Eufylline, tablets 150 mg 30 pcs

Pharmacotherapeutic group: Bronchodilator – phosphodiesterase inhibitor.

ATX code: R03DA05

Pharmacological action

Eufylline is a bronchodilator, a xanthine derivative; It inhibits phosphodiesterase, increases the accumulation of cyclic adenosine monophosphate in tissues, blocks adenosine (purine) receptors; reduces the flow of calcium ions through cell membrane channels, reduces the contractile activity of smooth muscles.
Relaxes bronchial muscles, increases mucociliary clearance, stimulates diaphragm contraction, improves respiratory and intercostal muscles function, stimulates respiratory center, increases its sensitivity to carbon dioxide and improves alveolar ventilation, which finally leads to decrease of 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 heart contractions, increases coronary blood flow and myocardial oxygen demand. It reduces the tone of blood vessels (mainly blood vessels of the brain, skin and kidneys).

It has a peripheral venodilator effect, reduces pulmonary vascular resistance, reduces the pressure in the “small” circle of the circulation. Increases renal blood flow, has a moderate diuretic effect. Dilates extrahepatic biliary tracts. Inhibits platelet aggregation (inhibits platelet activation factor and PgE2 alpha), increases resistance of erythrocytes to 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 enileptogenic effect.

Pharmacokinetics

After oral administration is quickly and completely absorbed, bioavailability – 90 – 100%. Food reduces the absorption rate without affecting its magnitude (large amounts of liquid and proteins accelerate the process). The higher the dose taken, the lower the absorption rate. Time to reach Cmax 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 above 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, 1,3-Dimethylureic acid (45-55%) is formed, which has pharmacological activity, but is 1-5 times inferior to theophylline.

Caffeine is an active metabolite and is formed in small amounts. There is no caffeine cumulation phenomenon in children over 3 years of age and in adults (unlike in younger children). Half-life in children over 6 months – 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. It is excreted by the kidneys.

Indications

Active ingredient

Composition

Composition per 1 tablet:

Active ingredients: aminophylline 150 mg.

Excipients: potato starch – 48.0 mg, calcium
stearate – 2.0 mg.

How to take, the dosage

Interaction

Increases the likelihood of side effects of glucocorticosteroids, mineralocorticosteroids (hypernatremia), drugs for general anesthesia (increases the risk of ventricular arrhythmias), xanthines and drugs that excite the central nervous system (increases neurotoxicity), beta-adrenostimulants. Antidiarrheals and enterosorbents reduce absorption of aminophylline. Rifampicin, phenobarbital, phenytoin, isoniazid, carbamazepine, sulfinpyrazone, aminoglutethimide, oral estrogen-containing contraceptives and morazine, being inducers of liver microsomal enzymes, increase clearance of aminophylline, which may require increasing its dose.

. Concomitant use with antibiotics of the group of macrolides, lincomycin, allopurinol, cimetidine, isoprenaline, enoxacin, small doses of ethanol, disulfiram, fluoroquinolones, recombinant interferon-alpha, methotrexate, mexiletine, propafenone, thiabendazole, ticlopidine, verapamil, and during influenza vaccination, the intensity of action of aminophylline may increase, which may require reducing its dose. Increases the effect of beta-adrenergic stimulants and diuretics (including by increasing glomerular filtration), reduces the effectiveness of lithium drugs and beta-adrenoblockers. Compatible with antispasmodics, do not use with other xanthine derivatives.

Special Instructions

Caution should be exercised when drinking large amounts of caffeinated products or beverages.

Impact of the drug on the ability to drive vehicles, machinery

At the time of treatment, it is necessary to refrain from driving and engaging in other potentially dangerous activities requiring increased concentration and rapid psychomotor reactions.

Synopsis

Contraindications

Hypersensitivity (including to other xanthine derivatives: caffeine, pentoxifylline, theobromine), epilepsy, gastric and duodenal ulcer (acute stage), gastritis with hyperacidity, severe arterial hyper- or hypotension, tachyarrhythmias, hemorrhagic stroke, retinal hemorrhage, childhood age (under 3 years).

With caution.

. Severe coronary artery disease (acute phase of myocardial infarction, angina pectoris), widespread vascular atherosclerosis, hypertrophic obstructive cardiomyopathy, frequent ventricular extrasystole, increased seizure readiness, hepatic and/or renal failure, gastric and 12 duodenal ulcer (history), gastrointestinal bleeding in recent history, uncontrolled hypothyroidism (possibility of cumulation) or thyrotoxicosis, prolonged hyperthermia, gastroesophageal reflux, prostatic hyperplasia, pregnancy, lactation, old age, childhood. Administration simultaneously with anticoagulants.

Side effects

Nervous system disorders: dizziness, headache, insomnia, agitation, anxiety, irritability, tremor.

Cardiovascular system disorders: palpitations, tachycardia (including in the fetus when taken by a pregnant woman in the III trimester), arrhythmias, cardialgia, decreased blood pressure, increased frequency of angina attacks.

Digestive system disorders: gastralgia, nausea, vomiting, gastroesophageal reflux, heartburn, aggravation of peptic ulcer disease, diarrhea; with prolonged use – loss of appetite.

Allergic reactions: skin rash, itching, fever.

Others: chest pain, tachypnoea, sensation of hot flashes in the face, albuminuria, hematuria, hypoglycemia, increased diuresis, increased sweating.

Overdose

Symptoms: decreased appetite, gastralgia, diarrhea, nausea, vomiting (including with blood), gastrointestinal bleeding, tachypnoea, facial hyperemia, tachycardia, ventricular arrhythmias, insomnia, motor agitation, anxiety, photophobia, tremors, seizures. Severe poisoning may cause epileptoid seizures (especially in children without any precursors), hypoxia, metabolic acidosis, hyperglycemia, hypokalemia, decreased blood pressure, skeletal muscle necrosis, confusion, renal failure with myoglobinuria.

Treatment: Withdrawal of the drug, gastric lavage, use of activated charcoal, laxatives, bowel lavage with a combination of polyethylene glycol and electrolytes, forced diuresis, hemosorption, plasma sorption, hemodialysis (effectiveness is not high, peritoneal dialysis is not effective), symptomatic therapy (including metoclopramide and ondansetron for vomiting). If seizures occur, maintain airway patency and administer oxygen therapy. For seizure management – intravenous diazepam 0.1-0.3 mg/kg (but no more than 10 mg). For severe nausea and vomiting – metoclopramide or ondansetron (IV).

Pregnancy use