KRKA #Colds_and_flu #Bronchial #HEALTH_CARE
Pharmacological properties
Pharmacodynamics. 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. since theophylline improves the transport of bronchial mucus (ciliated epithelial clearance) by increasing mucus and surfactant secretion, it improves expectoration. the anti-inflammatory effect of theophylline consists in inhibiting the proliferation of t-lymphocytes, inhibition of the secretion of cytokines (for example, interleukin-2, tumor necrosis factor), the activity of eosinophilic granulocytes, macrophages and mast cells. these effects lead to a weakening of the inflammation of the bronchial mucosa.
Theophylline also affects the smooth muscles of the coronary arteries, muscle blood vessels and kidneys, relaxes the muscles of the uterus, cardioesophageal sphincter and bile ducts. Theophylline increases the right ventricular ejection fraction, increases cardiac output, decreases resistance in pulmonary blood vessels, and decreases pulmonary hypertension.
Theophylline stimulates the respiratory center, increases the contraction of the diaphragm and respiratory muscles, increases diuresis, and increases the secretion of catecholamines by the adrenal glands.
Pharmacokinetics. The preparation is manufactured according to a special technological scheme. The capsules contain granules from which theophylline is gradually released to prevent a sharp increase or decrease in its concentration.
Theophylline is completely absorbed in the gastrointestinal tract. The highest blood concentrations are reached 7 hours after ingestion, and stationary concentrations are reached 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 bronchodilatory effect. Theophylline and its metabolites are excreted by the kidneys.
T½ of theophylline in nonsmokers is 7-9 hours. In smokers, as well as in children, this period decreases, and in persons with impaired liver function and heart failure, it increases.
Indications
All types of BA in children and adults, hoble, pulmonary emphysema, pulmonary hypertension in chronic pulmonary heart disease, central breathing disorders during sleep (nocturnal paroxysmal apnea).
Application
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 of theophylline 2 times a day.
The usual dose for children over 6 years old and weighing 20 kg, for adolescents is 200 mg of theophylline 2 times a day.
Patients with nocturnal asthma or breathing problems during sleep can take a single dose of Theotard at night. On average, a daily dose of 400 to 700 mg of Teotard is sufficient. It is recommended to take the first dose of Teotard in the evening before going to bed. The preparation is used after meals with plenty of water. The capsules are swallowed whole without chewing.
The effectiveness of treatment and the tolerability of theophylline should be determined on the 3rd day of treatment. If the efficacy is satisfactory, the treatment is continued with the prescribed dose, and if the efficacy is unsatisfactory, the dose is increased. If side effects appear, the dose is reduced.
The dose of theophylline is determined based on the clinical effect, serum theophylline concentration and potential side effects. The desired therapeutic concentration of theophylline in the blood serum is from 55 to 110 µmol / l (10–20 mg / l).
Therapeutic serum concentrations of theophylline are determined in the laboratory. The exact values of theophylline concentration are obtained by taking blood for analysis 4 hours after the morning dose from a patient who takes Teotard 2 times a day, and 12 hours after the evening dose from a patient who takes a single daily dose of Theotard. The duration of treatment depends on the course of the disease.
Contraindications
Hypersensitivity to any ingredient of the preparation, as well as to xanthine preparations (for example, caffeine, theobromine, pentoxifylline), acute period of myocardial infarction, tachyarrhythmia, hypertrophic obstructive cardiomyopathy, severe arterial hypertension, epilepsy, hyperthyroidism, gastric ulcer and duodenal ulcer liver; children under 6 years of age or weighing 20 kg.
Side effects
At the beginning of treatment, there may be moderate and temporary side effects such as headache, irritability, irritability, dizziness, insomnia, severe tachycardia and / or an unpleasant palpitations (palpitations), abdominal pain, nausea, vomiting, diarrhea, and allergic reactions.
If the concentration of theophylline in the blood serum exceeds the therapeutic value (even earlier in hypersensitive patients), the following side effects may occur: sleep disturbance, large volume of urine excreted, repeated vomiting, tremor, hyperthermia, delirium, heart rhythm disturbance (tachyarrhythmia), a sharp decrease in 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, glucose and uric acid salts may increase (hypercalcemia, hyperglycemia, hyperuricemia).
special instructions
Teotard should be used with caution and only if there is an urgent need to prescribe to patients with unstable angina pectoris, with heart disease, when tachyarrhythmic heart rhythm disturbances are noted, patients with arthritis, impaired renal and liver function, porphyria, as well as patients with a history of peptic ulcer disease and persons aged over 60 years old.
The dose of theophylline should be reduced in patients with heart failure, impaired liver function (especially patients with cirrhosis of the liver), with reduced oxygen concentration in the blood (hypoxemia), patients with pneumonia, viral infectious diseases (especially with influenza).
Theophylline can alter 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 preparation only if the positive effect for the mother outweighs the risk for the fetus. In pregnant women, the concentration of theophylline in the blood serum should be determined more often and the dose should be adjusted accordingly. The use of theophylline at the end of pregnancy should be avoided as it can inhibit uterine contraction.
Breastfeeding women should watch for a baby's hypersensitivity to theophylline reaction, agitation or sleep problems and seek medical advice.
Influence on the ability to drive vehicles and work with other mechanisms. Some side effects (for example, dizziness) can affect the ability to drive vehicles and operate other mechanisms. Patients should be advised not to drive or operate hazardous mechanical equipment until they are satisfied that they can tolerate treatment.
Interactions
During treatment with theotard, one should not consume alcohol, large amounts of food and drinks that contain methylxanthine (coffee, tea, cocoa, chocolate, Coca-Cola), preparations related to theophylline (caffeine, theobromine, pentoxifylline), since these substances can enhance the stimulant the effect of theophylline on the central nervous system.
The effect of theophylline can be enhanced with the simultaneous use of allopurinol, cimetidine, disulfiram, phenylbutazone, fluvoxamine, fluoroquinolones, furosemide, imipenem, interferon alpha, isoniazid, calcium antagonists, lincomycin, macrolides, mexiletin, paracetifranzepilin, propoxyphenol, propoxyphenol, propylene, propoxyfenol ranitidine, tacrine, thiabendazole, ticlopidine, viloxazine, or influenza vaccine. In patients who take one or more of the above preparations in parallel with theophylline, the concentration of theophylline in the blood serum should be monitored and the dose should be reduced if necessary.
With the combined administration of ciprofloxacin, the dose of theophylline must be reduced by at least 60%, and with the simultaneous administration of enoxacin - by 30%.
The effect of theophylline may be reduced with the combined use of antiepileptic preparations (for example, phenytoin, carbamazepine, primidone), barbiturates (especially phenobarbital and pentobarbital), isoprenaline, magnesium hydroxide, moracizin, rifampicin, ritonavir, or sulfinpyrazone. The effect of theophylline may also be lower in smokers. In patients who simultaneously take one or more of the above preparations with theophylline, the concentration of theophylline in the blood serum should be monitored and the dose increased, if necessary.
Theophylline can enhance the effectiveness of β-adrenergic receptor agonists, diuretics and reserpine.
Theophylline may reduce the effectiveness of adenosine, lithium carbonate, and β-adrenergic receptor antagonists.
The simultaneous use of theophylline and β-adrenergic receptor antagonists should be avoided, since theophylline may lose its effectiveness.
Anesthesia with halothane can cause serious heart rhythm disturbances in patients taking theophylline.
During treatment with theophylline, hypokalemia may occur, especially with combined treatment with α-adrenergic receptor agonists, thiazide diuretics, furosemide, GCS, as well as with hypoxemia; it is therefore recommended that serum potassium levels be checked periodically.
Overdose
It is noted if the concentration of theophylline in the blood serum is 110 μmol / l.
Clinical signs of overdose include tremors, nausea, vomiting, diarrhea, delirium, in especially severe cases - also cardiac arrhythmias (tachyarrhythmia), a sharp decrease in blood pressure and muscle cramps. Tachyarrhythmias and seizures can occur suddenly, without warning symptoms typical of minor overdose (eg nausea and vomiting). In most cases, it is sufficient to reduce the dose or temporarily stop using Theotard.
After taking an excessive number of capsules, arterial hypotension, anxiety, tremors, delirium, convulsions and more severe heart rhythm disturbances may occur. In such cases, the concentration of theophylline in serum should be determined immediately and the dose of Theotard should be reduced accordingly.
Treatment: gastric lavage and the 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 serum. In severe cases, theophylline excretion can be accelerated by hemoperfusion or hemodialysis.
Storage conditions
At temperatures up to 25 ° C.
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