Theotard 350 mg No. 40 caps. retard

Pharmacological properties of the drug Theotard

Theophylline is a bronchodilator. By relaxing the smooth muscles of the bronchi, it increases the flow of air through the bronchi and thus improves breathing. Because theophylline improves bronchial mucus transport (ciliary epithelial clearance) by increasing mucus and surfactant secretion, it improves expectoration. The anti-inflammatory effect of theophylline consists of inhibiting the proliferation of T-lymphocytes, inhibiting the secretion of cytokines (for example, interleukin-2, tumor necrosis factor), and the activity of eosinophils, macrophages and mast cells. These effects lead to a weakening of inflammation of the bronchial mucosa. Theophylline also affects the smooth muscles of the coronary arteries, blood vessels of the muscles and kidneys, relaxes the muscles of the uterus, cardioesophageal sphincter and bile ducts. Theophylline increases right ventricular ejection fraction, increases cardiac output, decreases pulmonary vascular resistance, and decreases pulmonary hypertension. Theophylline stimulates the respiratory center, increases contraction of the diaphragm and respiratory muscles, increases diuresis, and increases the secretion of catecholamines by the adrenal glands. The capsules contain granules that gradually release theophylline to prevent sudden increases or decreases in its concentration. Theophylline is completely absorbed from the gastrointestinal tract. The highest concentrations in the blood are achieved 7 hours after administration, and steady-state concentrations are achieved within 2-3 days of regular use. Theophylline is distributed to all organs and body fluids; metabolized in the liver. One of its metabolites (3-methylxanthine) also has a bronchodilator effect. Theophylline and its metabolites are excreted by the kidneys. The half-life of theophylline in people who do not smoke is 7–9 hours. In smokers, as well as in children, this time decreases, and in people with impaired liver function and heart failure, it increases.

Use of the drug Theotard

The dose is set individually depending on age, body weight and metabolic characteristics. The usual dose for adults and adolescents weighing 40 kg is 350 mg theophylline 2 times a day. The usual dose for children over 6 years of age and weighing 20 kg, for adolescents is 200 mg theophylline 2 times a day. Patients with nocturnal asthma or sleep-disordered breathing may take a single dose of Theotard at night. On average, a daily dose of 400 to 700 mg of Theotard is sufficient. It is recommended to take the first dose of Theotard in the evening at night. The drug is used after meals with plenty of water. Capsules should be swallowed whole without chewing. The effectiveness of treatment and tolerability of theophylline should be determined on the 3rd day of treatment. If the effectiveness is satisfactory, treatment is continued with the prescribed dose, and if the effectiveness is unsatisfactory, the dose is increased. If side effects occur, reduce the dose. The dosage of theophylline is determined based on clinical effect, serum theophylline concentration and possible side effects. The desired therapeutic concentration of theophylline in serum is from 55 to 110 μmol/L (10–20 mg/L). Therapeutic serum theophylline concentrations are determined in the laboratory. Accurate theophylline concentrations are obtained by drawing blood for analysis 4 hours after the morning dose in a patient taking Theotard twice daily and 12 hours after the evening dose in a patient taking a concurrent daily dose of Theotard. The duration of treatment depends on the course of the disease.

Theotard®

Inside, after meals, with a sufficient amount of liquid.

Extended-release capsules should not be opened or chewed.

The dosage of the drug is individual. It is unacceptable to exceed the daily dose of 15 mg/kg in adults in 2 doses with an interval of 12 hours, 20 mg/kg in children.

To select the dose of the drug, it is necessary to determine the concentration of theophylline in the blood serum. As a rule, serum theophylline concentrations of 5 to 12 mcg/ml provide a therapeutic effect with minimal risk of side effects. Theophylline concentration in blood serum should not exceed 20 mcg/ml. If the concentration exceeds 20 mcg/ml, the dose of the drug should be reduced. It is recommended to carry out monitoring every 6-12 months.

During the first three days, you should take 1 capsule (200-350 mg) of the drug every 12 hours. On the third day, the effectiveness of therapy and tolerability of the drug should be assessed. If there is insufficient effectiveness, the dose can be increased (by 200-350 mg/day) until the maximum therapeutic effect is obtained.

In case of undesirable side effects, the dose should be reduced.

The dose depends on the nature of the disease, age and body weight of the patient.

Morning and evening doses of the drug may be different depending on the time of occurrence of attacks of difficulty breathing, the clinical picture of the disease and the effectiveness of therapy.

Theotard 200 mg is prescribed to children 2 times a day whose body weight exceeds 20 kg, as well as to adults with low body weight.

Theotard 350 mg is prescribed to adults and children 2 times a day whose body weight exceeds 40 kg.

The usual maintenance dose for adults weighing more than 60 kg is 350 mg of Theotard 2 times a day.

For non-smoking adults weighing more than 60 kg, the initial dose is 350 mg/day in 1 dose in the evening. Then the dose is subsequently increased by 350 mg to maintenance (on average 700 mg/day in 1 dose in the evening).

For smoking patients and people with high metabolism, the initial dose is 350 mg, and the maintenance dose can be increased to 1.15 g / day (2 capsules taken in the evening, 1 capsule in the morning).

In persons with reduced clearance of the drug, the initial dose is 200 mg/day, which is then increased by 200 mg every 2 days to a maintenance dose of 400 mg/day in 1 dose in the evening, and in persons with body weight less than 60 kg—200 mg/day .

Children 6-12 years old are prescribed 200 mg capsules. The daily dose for children 6-8 years old (with a body weight of 20-30 kg) is 400 mg, frequency of use is 2 times a day; for children 8-12 years old (with a body weight of 30-40 kg) - 600 mg, frequency of use - 3 times a day.

Children aged 12-16 years (body weight 40-60 kg) are prescribed 350 mg capsules. The daily dose is 0.7-1.4 g, the frequency of use is 2-3 times a day.

The effect of the drug is fully manifested 3-4 days after the start of treatment.

Side effects of the drug Theotard

At the beginning of treatment, mild and temporary side effects may occur, such as headache, increased excitability, irritability, dizziness, insomnia, severe tachycardia and/or an unpleasant feeling of heartbeat (fluttering), abdominal pain, nausea, vomiting, diarrhea and allergic reactions. If the concentration of theophylline in the blood serum exceeds the therapeutic concentration (in hypersensitive patients even earlier), the following side effects may occur: sleep disturbance, large volume of urine excreted, repeated vomiting, tremor, hyperthermia, delirium, heart rhythm disturbances (tachyarrhythmia), sharp decrease Blood pressure and muscle cramps. During treatment with theophylline, the concentration of potassium in the blood serum may decrease (hypokalemia), and the concentration of calcium, creatinine, sugar and uric acid salts may increase (hypercalcemia, hyperglycemia, hyperuricemia).

Special instructions for the use of the drug Theotard

Theotard should be prescribed with caution and only when urgently necessary to patients with unstable angina, heart disease, when tachyarrhythmic disturbances of the heart rhythm are noted, patients with hypertension (arterial hypertension), impaired renal and liver function, porphyria, as well as patients with peptic ulcer disease. history and patients over 60 years of age. The dose of theophylline should be reduced in patients with heart failure, impaired liver function (especially patients with cirrhosis of the liver), with a reduced concentration of oxygen in the blood (hypoxemia), patients with pneumonia, viral infectious diseases (especially influenza). Theophylline can change some laboratory parameters: increase the amount of fatty acids in the blood plasma and increase the level of catecholamines in the urine. During pregnancy and breastfeeding . Theophylline crosses the placenta and is excreted in breast milk. During pregnancy, you can take the drug only if the positive effect for the mother outweighs the risk for the fetus. In pregnant women, serum theophylline concentrations should be determined more frequently and the dose adjusted accordingly. Theophylline should be avoided late in pregnancy as it may inhibit uterine contractions. Breast-feeding women should monitor the infant for theophylline hypersensitivity reactions, agitation, or sleep problems and seek medical advice. Impact on the ability to drive vehicles and operate other machinery. Some side effects (such as dizziness) may affect your ability to drive or operate machines. Patients should be advised not to drive or operate hazardous machinery until they are confident they can tolerate treatment.

Theotard 200 mg No. 40 caps. retard

Instructions for medical use of the drug THEOTARD Trade name THEOTARD International nonproprietary name Theophylline Dosage form Extended release capsules 200 mg or 350 mg Composition: One capsule contains the active substance - theophylline anhydrous 200 mg or 350 mg, excipients: povidone, talc, ammonia copolymer methacrylate, colloidal silicon dioxide, dibutyl phthalate, capsule shell composition: titanium dioxide, quinoline yellow dye, azorubine, crimson dye, patent blue dye, brilliant black, methyl hydroxybenzoate, propyl hydroxybenzoate, gelatin. Description Capsules filled with white granules. The body of the capsule is transparent dark green, the cap of the capsule is opaque dark green. Pharmacotherapeutic group Drugs for the treatment of bronchial asthma. Other drugs for the treatment of bronchial asthma for systemic use. Xanthine derivatives. ATC code R03DA04 Pharmacological properties Pharmacokinetics After oral administration, Theotard is almost completely absorbed. The slow release of the active substance from the retard capsules of the drug Theotard ensures the maintenance of a uniform level of theophylline in the blood serum for 12 hours. The bronchodilator effect of Theotard develops gradually, so the drug is not prescribed for the relief of emergency conditions. After a single dose of 350 mg of the drug, its maximum plasma concentration is reached within 6.3-8.8 hours, which is 4.4 cg/ml. The therapeutic concentration is achieved after a few days and is 8-20 cg/ml. Theotard is metabolized primarily by liver microsomal enzymes. Pharmacodynamics Theotard is a pure anhydrous theophylline (xanthine derivative) in the form of granules. Theophylline is a phosphodiesterase inhibitor and increases the accumulation of c-AMP in tissues, which reduces the contractile activity of smooth muscles. The drug has a pronounced bronchodilator effect, prevents or eliminates bronchial obstruction. Improving lung function allows an increase in the supply of oxygen to the arterial blood, which leads to a decrease in CO2 concentration. Theotard has a stimulating effect on the respiratory center, reduces pulmonary vascular resistance, lowers pressure in the pulmonary circulation, improves mucociliary clearance; has a positive inotropic and chronotropic effect on the heart. The drug stimulates diuresis. Dilates blood vessels (mainly those of the brain, skin and kidneys), inhibits platelet aggregation. Indications for use: treatment and prevention of reversible bronchial obstruction in bronchial asthma, chronic obstructive bronchitis, emphysema; pulmonary hypertension in chronic cor pulmonale; nocturnal breathing disorders of central origin. Directions for use and dosage: Capsules of the drug must not be opened or chewed. The dosage of the drug is individual. It is unacceptable to exceed the daily dose of 15 mg/kg in adults, 20 mg/kg in children. To select the dose of the drug, it is necessary to determine the concentration of theophylline in the blood serum. As a rule, a theophylline concentration in the blood serum of 10 to 15 cg/ml provides a therapeutic effect with minimal risk of side effects. If the concentration exceeds 20 cg/ml, then the dose of the drug should be reduced. During the first three days, one retard capsule of the drug should be taken every 12 hours. On the third day, the effectiveness of therapy and tolerability of the drug should be assessed. If effectiveness is insufficient, the dose may be increased. In case of undesirable side effects, the dose should be reduced. Theotard 200 mg is prescribed to children whose body weight exceeds 20 kg, as well as to adults with low body weight. Theotard 350 mg is prescribed to adults and children whose body weight exceeds 40 kg. Morning and evening doses of the drug may be different depending on the time of occurrence of attacks of difficulty breathing, the clinical picture of the disease and the effectiveness of therapy. Side effects The frequency of side effects increases with increasing concentration of the drug in the blood serum - pain in the stomach, nausea, vomiting, diarrhea - headache, insomnia, tremor, irritability, - heart rhythm disturbances, tachycardia, decreased blood pressure, increased frequency of angina attacks - increased diuresis, hyperglycemia, hypokalemia - skin rash, itching Contraindications - hypersensitivity to theophylline - epilepsy - acute myocardial infarction, acute rhythm disturbances (tachyarrhythmias) - peptic ulcer of the stomach and duodenum in the acute stage - children under 3 years of age Drug interactions Theophylline is not used in combination with other xanthine derivatives. In combination with phenobarbital, diphenin, rifampicin, isoniazid, carbamazepine, sulfinpyrazone, phenytoin, a decrease in the effectiveness of theophylline is observed, which may require an increase in the doses of the drug used. When used simultaneously with macrolide antibiotics, lincomycin, allopurinol, cimetidine, isoprenaline, oral contraceptives, epoxacin and with influenza vaccination, the intensity of action may increase, which may require a reduction in the dose of theophylline. The drug suppresses the therapeutic effects of lithium carbonate and beta-blockers. Theophylline potentiates the effect of diuretics by increasing glomerular filtration and reducing tubular reabsorption. Theophylline should be prescribed with caution concomitantly with anticoagulants. Special instructions The drug is not recommended for use in cases of severe arterial hypertension and widespread vascular atherosclerosis. Use with caution in severe angina, heart failure, serious cardiac arrhythmias, hypertrophic cardiomyopathy, hyperthyroidism, severe liver and kidney dysfunction. In severe diseases of the cardiovascular system, liver, viral infections, as well as in elderly patients, the dose of the drug should be reduced. For persons who metabolize theophylline rapidly (young people, smokers), a single dose of the drug per day will not be sufficient. Pregnancy and lactation The drug should be taken only when the expected benefit to the mother outweighs the risk to the fetus; it should not be taken at the end of pregnancy, as it may stop uterine contractions. Excreted in breast milk, if the baby shows signs of sensitivity or insomnia, consult a doctor. Features of the effect of the drug on the ability to drive a vehicle or operate potentially dangerous mechanisms The drug may have a negative effect on psychomotor reactions, so it is recommended to be careful when driving vehicles and working with potentially dangerous mechanisms. Overdose Symptoms: hand tremors, nausea, vomiting, diarrhea, psychomotor agitation, heart rhythm disturbances, decreased blood pressure, muscle cramps. Treatment: symptomatic treatment. Gastric lavage, taking activated carbon. Release form and packaging 10 capsules in a blister. 4 blisters in a cardboard box along with instructions for use. Storage conditions Store at temperatures up to 25°C, protected from light and moisture. Keep out of the reach of children! Shelf life: 5 years The drug should not be used after the expiration date indicated on the package. Conditions for dispensing from pharmacies By prescription Manufacturer KRKA, d.d., Novo Mesto, Slovenia in collaboration with Astellas Pharma GmbH, Germany

Drug interactions Theotard

During treatment with Theotard, you should not consume alcohol, large amounts of food and drinks that contain methylxanthine (coffee, tea, cocoa, chocolate, Coca-Cola), drugs related to theophylline (caffeine, theobromine, pentoxifylline), as these substances may increase stimulating effect of theophylline on the central nervous system. The effect of theophylline may be enhanced with simultaneous use of allopurinol, cimetidine, disulfiram, phenylbutazone, fluvoxamine, fluoroquinolones, furosemide, imipenem, interferon alpha, isoniazid, calcium antagonists, lincomycin, macrolides, mexiletine, paracetamol, pentoxifylline, oral contraceptives, probenecid, propafenone, pro pranolol, ranitidine, tacrine, thiabendazole, ticlopidine, viloxazine, or influenza vaccine. In patients who are taking one or more of the above drugs in parallel with theophylline, the concentration of theophylline in the blood serum should be monitored and the dose reduced if necessary. When taking ciprofloxacin in combination, the dose of theophylline should be reduced by at least 60%, and when taking enoxacin simultaneously, by 30%. The effect of theophylline may be reduced by concomitant use of antiepileptic drugs (for example, phenytoin, carbamazepine, primidone), barbiturates (especially phenobarbital and pentobarbital), isoprenaline, magnesium hydroxide, moracizine, rifampicin, ritonavir or sulfinpyrazone. The effect of theophylline may also be lower in smokers. In patients who are taking one or more of the above drugs concomitantly with theophylline, the concentration of theophylline in the blood serum should be monitored and the dose increased if necessary. Theophylline may enhance the effect of β-adrenergic agonists, diuretics and reserpine. Theophylline may reduce the effectiveness of adenosine, lithium carbonate and beta-adrenergic antagonists. The simultaneous use of theophylline and β-adrenergic receptor antagonists should be avoided, as theophylline may lose its effectiveness. Halothane anesthesia can cause serious cardiac arrhythmias in patients taking theophylline. During treatment with theophylline, hypokalemia may occur, especially with combined treatment with α-adrenergic receptor agonists, thiazide diuretics, furosemide, corticosteroids, and also with hypoxemia; Therefore, it is recommended to periodically check serum potassium levels.

Overdose of the drug Theotard, symptoms and treatment

It is noted if the concentration of theophylline in the blood serum exceeds 110 µmol/l. Clinical signs of overdose include tremor, nausea, vomiting, diarrhea, delirium, and in especially severe cases, heart rhythm disturbances (tachyarrhythmia), a sharp decrease in blood pressure and muscle cramps. Tachyarrhythmias and seizures may occur suddenly, without the warning symptoms typical of a minor overdose (eg, nausea and vomiting). In most cases, it is sufficient to reduce the dose or temporarily stop using Theotard. Hypotension, restlessness, tremors, delirium, seizures, and more severe cardiac arrhythmias may occur after taking excessive amounts of capsules. In such cases, serum theophylline concentrations should be immediately determined and the dose of Theotard reduced accordingly. Treatment: gastric lavage and use of activated carbon. It is necessary to monitor the patient's condition, especially blood pressure, heart rate, respiration and the concentration of theophylline and potassium in the blood serum. In severe cases, the elimination of theophylline can be accelerated using hemoperfusion or hemodialysis.