Euphyllin tablets 150mg, No. 30

• Broncho-obstructive syndrome of any genesis;

• bronchial asthma (drug of choice in patients with exercise asthma and as an additional remedy for other forms),

• chronic obstructive pulmonary disease (chronic obstructive bronchitis, pulmonary emphysema),

• hypertension in the pulmonary circulation,

• Pulmonary heart,

• sleep apnea.

The dose should be selected in accordance with the individual characteristics of each patient, taking into account the clinical response and the stable concentration of aminophylline in the blood serum.

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

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

Higher doses of aminophylline for adults: single 500 mg; daily - 1500 mg.

Higher doses for children over 3 years old: 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 the tolerability of the drug.

To reduce toxic effects, it should be prescribed in the minimum effective doses.

Active ingredient: aminophylline (aminophylline) - 150.0 mg.

Excipients: potato starch - 48.5 mg, calcium stearate - 1.5 mg .

• Hypersensitivity to the drug (including to other xanthine derivatives: caffeine, pentoxifylline, theobromine),

• epilepsy,

• peptic ulcer and 12 duodenal ulcer (in the acute stage),

• gastritis with high acidity,

• severe arterial hyper- and hypotension,

• tachyarrhythmias,

• hemorrhagic stroke,

• retinal hemorrhage,

• children's age (up to 3 years).

CAREFULLY

Ischemic heart disease (acute phase of myocardial infarction, angina pectoris), common vascular atherosclerosis, hypertrophic obstructive cardiomyopathy, frequent ventricular premature beats, increased convulsive readiness, hepatic and / or renal failure, gastric ulcer and duodenal ulcer (in history) recent history of intestinal bleeding, uncontrolled hypothyroidism (the possibility of cumulation) or thyrotoxicosis, prolonged hyperthermia, gastroesophageal reflux, prostate adenoma, pregnancy, lactation, old age, childhood.

Trade name: Euphyllin

International non-proprietary name: Aminophylline

Dosage form Tablets

Composition for one tablet

Active ingredient: aminophylline (aminophylline) - 150.0 mg.

Excipients: potato starch - 48.5 mg, calcium stearate - 1.5 mg .

Description

Tablets are white or white with a yellowish tinge, round, flat-cylindrical.

Pharmacotherapeutic group

Bronchodilator

ATX code [R03DA05]

Pharmacological properties

Pharmacodynamics. Bronchodilator, xanthine derivative; inhibits phosphodiesterase, increases the accumulation of adenosine monophosphate (cAMP) in tissues, blocks adenosine (purine) receptors; reduces the flow of calcium ions through the channels of cell membranes, reduces the contractile activity of smooth muscles.

Relaxes the muscles of the bronchi, stimulates the respiratory center, increases its sensitivity to carbon dioxide and improves alveolar ventilation, which ultimately leads to a decrease in the severity and frequency of apnea episodes. By normalizing the respiratory function, it contributes to the saturation of blood with oxygen and a decrease in the concentration of carbon dioxide.

It has a stimulating effect on the activity of the heart, increases the strength and number of heart contractions, increases coronary blood flow and increases myocardial oxygen demand. Reduces the tone of blood vessels (mainly the vessels of the brain, skin and kidneys). It has a peripheral venodilating effect, reduces pulmonary vascular resistance, lowers pressure in the 'small' circle of blood circulation. Increases renal blood flow, has a moderate diuretic effect. Expands the extrahepatic biliary tract.

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

Inhibits platelet aggregation (inhibits platelet activation factor and prostaglandin E2 (PgE2), increases the resistance of erythrocytes to deformation (improves the rheological properties of blood), reduces thrombus formation and normalizes microcirculation.

Has a tocolytic effect, increases the acidity of gastric juice. When used in large doses, it has an epileptogenic effect.

Pharmacokinetics. After oral administration, it is rapidly and completely absorbed, bioavailability is 90-100%. Food reduces the rate of absorption without affecting its value (large volumes of liquid and proteins accelerate the process). The higher the dose taken, the lower the rate of absorption. The time to reach maximum concentration is 1-2 hours. The volume of distribution is in the range of 0.3-0.7 l / kg (30-70% of the 'ideal' body weight), an average of 0.45 l / kg. Communication with plasma proteins in adults - 60%, in patients with liver cirrhosis - 36%. Penetrates into breast milk (10% of the dose taken), through the placental barrier (the concentration in the fetal serum is slightly higher than in the mother's serum).

Aminophylline exhibits bronchodilating properties at concentrations of 10-20 ?g / ml. Concentrations over 20 mg / ml are toxic. The stimulating effect on the respiratory center is realized with a lower content of the drug in the blood - 5-10 ?g / ml.

It is metabolized at physiological pH values ??with the 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-dimethyl uric 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 produced in small quantities.

In children over 3 years of age and in adults (as opposed to younger children), the phenomenon of caffeine accumulation is absent. 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, pharmacokinetics are normalized after 3-4 months); in adults with chronic obstructive pulmonary disease, pulmonary heart disease and pulmonary heart disease - over 24 hours. The metabolites are excreted by the kidneys.

INDICATIONS

• Broncho-obstructive syndrome of any genesis;

• bronchial asthma (drug of choice in patients with exercise asthma and as an additional remedy for other forms),

• chronic obstructive pulmonary disease (chronic obstructive bronchitis, pulmonary emphysema),

• hypertension in the pulmonary circulation,

• Pulmonary heart,

• sleep apnea.

CONTRAINDICATIONS

• Hypersensitivity to the drug (including to other xanthine derivatives: caffeine, pentoxifylline, theobromine),

• epilepsy,

• peptic ulcer and 12 duodenal ulcer (in the acute stage),

• gastritis with high acidity,

• severe arterial hyper- and hypotension,

• tachyarrhythmias,

• hemorrhagic stroke,

• retinal hemorrhage,

• children's age (up to 3 years).

CAREFULLY

Ischemic heart disease (acute phase of myocardial infarction, angina pectoris), common vascular atherosclerosis, hypertrophic obstructive cardiomyopathy, frequent ventricular premature beats, increased convulsive readiness, hepatic and / or renal failure, gastric ulcer and duodenal ulcer (in history) recent history of intestinal bleeding, uncontrolled hypothyroidism (the possibility of cumulation) or thyrotoxicosis, prolonged hyperthermia, gastroesophageal reflux, prostate adenoma, pregnancy, lactation, old age, childhood.

APPLICATION DURING PREGNANCY AND DURING BREASTFEEDING

The use of the drug during pregnancy is possible only if the intended benefit to the mother outweighs the risk to the fetus.

If necessary, the appointment of the drug during lactation should stop breastfeeding.

DOSAGE AND APPLICATION

The dose should be selected in accordance with the individual characteristics of each patient, taking into account the clinical response and the stable concentration of aminophylline in the blood serum.

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

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

Higher doses of aminophylline for adults: single 500 mg; daily - 1500 mg.

Higher doses for children over 3 years old: 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 the tolerability of the drug.

To reduce toxic effects, it should be prescribed in the minimum effective doses.

SIDE EFFECT

From the nervous system: dizziness, headache, insomnia, agitation, anxiety, irritability, tremor.

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

From the digestive system: gastralgia, nausea, vomiting, gastroesophageal reflux, heartburn, exacerbation of gastric ulcer and 12 duodenal ulcer, diarrhea, with prolonged use - loss of appetite.

Allergic reactions: skin rash, itching, fever.

Others: chest pain, tachypnea, a feeling of 'hot flashes' to the face, albuminuria, hematuria, hypoglycemia, increased urine output, increased sweating.

OVERDOSE

Symptoms: decreased appetite, gastralgia, diarrhea, nausea, vomiting (including blood), gastrointestinal bleeding, tachypnea, facial flushing, tachycardia, ventricular arrhythmias, insomnia, motor agitation, anxiety, photophobia, tremors, convulsions. In severe poisoning, epileptiform seizures may develop (especially in children without precursors), hypoxia, metabolic acidosis, hyperglycemia, hypokalemia, decreased blood pressure, skeletal muscle necrosis, confusion, renal failure with myoglobinuria.

Treatment: drug withdrawal, gastric lavage, administration of activated charcoal, laxatives, forced diuresis, hemosorption, plasmasorption, hemodialysis (efficiency is not great, peritoneal dialysis is not effective), symptomatic therapy (including metoclopramide and ondansetron - with vomiting). If seizures occur, maintain airway patency and oxygen therapy. For relief of seizures, intravenous administration of diazepam at a dose of 0.1-0.3 mg / kg (no more than 10 mg). For severe nausea and vomiting, metoclopramide and ondansetron (intravenously).

INTERACTION WITH OTHER DRUGS

Increases the likelihood of developing side effects of glucocorticosteroids and mineralocorticosteroids (hypernatremia), agents for general anesthesia (there is a risk of ventricular arrhythmias), agents that excite the central nervous system (increases neurotoxicity).

Antidiarrheal drugs and enterosorbents reduce the absorption of aminophylline.

Rifampicin, phenobarbital, phenytoin, isoniazid, carbamazepine, sulfinpyrazone, aminoglutethimide, oral estrogen-containing contraceptives and moracizin, being inducers of microsomal oxidation, increase the clearance of aminophylline, which may require an increase in its dose.

With simultaneous use with antibiotics of the macrolide group, lincomycin, allopurinol, cimetidine, isoprenaline, enoxacin, small doses of ethanol, disulfiram, fluoroquinolones, recombinant interferon alfa, methotrexate, mexiletine, propafenone, thiabendazole, vierapamiline against influenza increase, which may require a decrease in its dose.

Increases the effect of beta-adrenostimulants and diuretics (including by increasing glomerular filtration), reduces the effectiveness of lithium preparations and beta-blockers.

Compatible with antispasmodics, not used in conjunction with other xanthine derivatives. It is prescribed with caution at the same time as anticoagulants.

SPECIAL INSTRUCTIONS

Exercise caution when consuming large amounts of caffeinated foods and beverages during treatment.

INFLUENCE ON ABILITY TO DRIVE VEHICLES, MECHANISMS

During the period of drug treatment, care must be taken when administering

vehicles and engaging in other potentially hazardous activities that require increased concentration of attention and speed of psychomotor reactions.

RELEASE FORM

Tablets 150 mg.

On 10, 15 or 20 tablets in a blister strip packaging from a film of polyvinyl chloride and printed aluminum foil varnished.

1, 2, 3 or 5 blisters together with instructions for use are placed in a cardboard box.

STORAGE CONDITIONS

Store at a temperature not exceeding 25 ? —.

Keep out of the reach of children.

SHELF LIFE

5 years. Do not use after the expiration date.

HOLIDAY TERMS

Dispensed by prescription.

Name and address of manufacturer / organization accepting claims

JSC 'Pharmstandard-Leksredstva', 305022, Russia, Kursk, st. 2nd Aggregatnaya, 1a / 18, tel./fax: (4712) 34-03-13, www.pharmstd.ru

OJSC 'Pharmstandard-Leksredstva'