Theophylline (Theophylline)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceTheophyllineTheophylline
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    VALENTA PHARM, PAO     Russia
    • Dosage form: & nbspsustained-release tablets
    Composition:

    1 tablet contains: active substance:

    theophylline (in terms of 100% substance) - OD g, 0.2 g or 0.3 g; Excipients:

    kollidone SR: polyvinyl acetate - 80%, povidone - 19%, sodium lauryl sulfate - 0.8%, silicon dioxide - 0.2%; microcrystalline cellulose, calcium stearate.

    Description:white tablets with a yellowish tinge of flat-cylindrical shape with a bevel (for a dosage of 0.1 g), with a facet and a risk (for dosages of OD g and 0.3 g).
    Pharmacotherapeutic group:bronchodilator.
    ATX: & nbsp

    R.03.D.A.04   Theophylline

    Pharmacodynamics:

    Spasmolytic agent, Purine Derivative: Blocks adenosine receptors and inhibits phosphodiesterase. Causes a pronounced bronchodilator effect, caused by a direct effect on the bronchial musculature. Stabilizes the membrane of mast cells, inhibits the release of mediators of allergic reactions, increases mucociliary clearance, stimulates contraction of the diaphragm, improves the function of respiratory and intercostal muscles.Normalizing the respiratory function, promotes the saturation of blood with oxygen and a decrease in the concentration of carbon dioxide; stimulates the centers of respiration. Strengthens lung ventilation in hypokalemia.

    Has a stimulating effect on the activity of the heart, increases the strength and heart rate, increases coronary blood flow and the need for myocardium in oxygen. Reduces the tone of blood vessels (mainly, the vessels of the brain, skin and kidneys). Reduces pulmonary vascular resistance, lowers pressure in a small circle of blood circulation. Increases renal blood flow, has a moderate diuretic effect. Expands extrahepatic biliary tract.

    The delayed release of the active substance from the tablets ensures the therapeutic level of theophylline in the blood 3-5 h after administration and maintained for 10-12 h, so that effective theophylline concentrations in the blood during the day are maintained when taking the drug 2 times a day.

    Pharmacokinetics:

    Sufficiently absorbed from the gastrointestinal tract, bioavailability - 88-100%. Time to reach the maximum concentration in blood plasma for 6 hours.

    The connection with plasma proteins is about 60%.Penetrates through the placental barrier, is found in breast milk. Metabolised in the liver (90%) with the participation of several cytochrome P450 enzymes (the most important CYP1A2). The main metabolites are: 1,3-dimethylurea and 3-methylxanthine.

    Excretion of metabolites by the kidneys together with 7-13% of the unchanged active substance. The half-life period in non-smoking patients is 6-12 hours. Smoking people are significantly shorter - 4-5 hours. In patients with cirrhosis of the liver, kidney failure and alcoholism patients, the half-life period is prolonged. The overall clearance is lower in patients with high fever, expressed respiratory insufficiency, in patients with hepatic insufficiency or chronic heart failure, in viral infections, in patients older than 55 years.

    Indications:

    Bronchoobstructive syndrome of any genesis: bronchial asthma (a drug of choice in patients with asthma of physical stress and as an adjunct in other forms), chronic obstructive diseases (chronic obstructive bronchitis, emphysema of the lungs).

    Pulmonary hypertension, pulmonary heart, edematous syndrome of renal genesis (as part of combination therapy), nocturnal apnea.

    Contraindications:

    Hypersensitivity (including other derivatives of xanthine-caffeine, pentoxifylline, theobromine), epilepsy, peptic ulcer and duodenal ulcer, gastritis with high acidity, bleeding from the gastrointestinal tract, severe arterial hyper- or hypotension, severe tachyarrhythmias, hemorrhagic stroke, hemorrhage in the retina of the eye, children under 12 years.

    Carefully:With caution should be used for severe coronary insufficiency (acute phase of myocardial infarction, angina pectoris), widespread atherosclerosis of the vessels, hypertrophic obstructive cardiomyopathy, frequent ventricular extrasystole, chronic heart failure, increased convulsive alertness, hepatic and / or renal insufficiency, stomach ulcer and 12- (history), bleeding from the gastrointestinal tract in a recent history, uncontrolled hypothyroidism (the possibility of cumulation), or ireotoksikoz, prolonged pyrexia, gastroesophageal reflux disease, prostatic hypertrophy, pregnancy, lactation, old age.
    Pregnancy and lactation:

    During pregnancy (especially in the first trimester) theophylline appoint only if the intended benefit to the mother exceeds the possible risk to the fetus. The appointment of the drug during pregnancy (first trimester and last weeks) is possible only on strict indications.

    When prescribing the drug during lactation, it should be borne in mind that theophylline excreted in breast milk; it is not recommended to take the drug during lactation. If necessary, take the drug during lactation, a woman should stop breastfeeding.

    Dosing and Administration:

    Inside, squeezed with enough liquid.

    The average dose for adults and children over 12 years of age - 300 mg twice a day (at the rate of 10-15 mg / kg / day for 2 divided doses with an interval of 12 hours), if necessary 300 mg 3 times a day or 500 mg once, before bed (in the case of predominantly nocturnal and morning seizures). Non-smoking adult patients with a body weight of 60 kg or more, the initial dose is 200 mg, taken in the evening, then 200 mg twice a day.

    Patients weighing less than 60 kg the initial single dose is 100 mg in the evening, then 100 mg twice a day.

    Treatment begins with smaller doses,which gradually, with an interval of 1-2 days, increase (by 100-200 mg / day) to obtain the maximum therapeutic effect, with poor tolerance - reduce.

    The dose depends on the nature of the disease, the age and body weight of the patient. If it is necessary to administer in large doses, the treatment is controlled by the concentration of theophylline in the blood (therapeutic concentration is within 10-15 μg / ml): at a concentration of 20-25 μg / ml, the daily dose should be reduced by 10%; 25-30 μg / ml - by 25%; above 30 mcg / ml - the daily dose is reduced by 2 times. Repeated control is carried out after 3 days. If the concentration is too low, the daily dose is increased by 25% at 3-day intervals. When stabilizing the patient's condition against the background of taking in high doses, it is necessary to carry out a control every 6-12 months.

    Adherent dose for adults with a body weight above 60 kg - 600 mg / day, less than 60 kg - 400 mg / day.

    For smokers with a body weight of more than 60 kg daily dose of the drug - 600 mg in the evening and 300 mg in the morning, with a body weight of less than 60 kg - 400 mg in the evening and 200 mg in the morning.

    For patients with diseases of the cardiovascular system and a violation of the liver: with a body weight of more than 60 kg daily dose of 400 mg, with a body weight of less than 60 kg - 200 mg.A decrease in the daily dose is required in patients with severe heart, liver, and viral infections, and in elderly patients.

    Children with body weight up to 30 kg - 10-20 mg / kg / day (in 2 divided doses).

    Side effects:

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

    From the cardiovascular system: palpitations, tachycardia (including the fetus when taking a pregnant woman in the third trimester), arrhythmias, lowering blood pressure, cardialgia, an increase in the frequency of angina attacks.

    From the digestive system: gastralgia, nausea, vomiting, gastroesophageal reflux, heartburn, peptic ulcer, diarrhea, with prolonged admission - a decrease in appetite.

    Allergic reactions: skin rash, itching, fever.

    Other: pain in the chest, tachypnea, sensation of hot flashes to the face, albuminuria, hematuria, hypoglycemia, increased diuresis, increased sweating.

    Side effects decrease with a decrease in the dose of the drug.

    Overdose:

    Symptoms:

    a decrease in appetite, gastralgia, diarrhea, nausea, vomiting (including with blood), gastrointestinal bleeding, tachypnea,hyperemia of the facial skin, tachycardia, ventricular arrhythmias, insomnia, motor excitement, anxiety, photophobia, tremor, convulsions.

    In severe poisoning, epileptic seizures may develop (especially in children without any precursors), hypoxia, metabolic acidosis, hyperglycemia, hypokalemia, lowering blood pressure, necrosis of skeletal muscles, confusion, renal insufficiency with myoglobinuria.

    Treatment:

    cancellation of the drug, gastric lavage, the appointment of activated carbon, laxative drugs, washing the intestine with a combination of polyethylene glycol and electrolytes, forced diuresis, hemosorption, plasmasorption, hemodialysis (efficacy is low, peritoneal dialysis is ineffective), symptomatic therapy (including metoclopramide and ondansetron - when vomiting).

    If seizures occur, maintain airway patency and conduct oxygen therapy. To stop the seizure - intravenously diazepam, 0.1-0.3 mg / kg (not more than 10 mg). With severe nausea and vomiting - metoclopramide or ondansetron (intravenously).

    Interaction:

    Increases the likelihood of side effects of glucocorticosteroids, mineralocorticosteroids (hypernatremia), funds for general anesthesia (increases the risk of ventricular arrhythmias), drugs that excite the central nervous system (increases neurotoxicity).

    Antidiarrhoeal drugs and enterosorbents reduce the absorption of theophylline. Rifampicin, phenobarbital, phenytoin, isoniazid, carbamazepine, sulfinpyrazone, aminoglutethimide, oral estrogen-containing contraceptives and moracisin, as inducers of microsomal oxidation, increase the clearance of theophylline, which may require an increase in its dose.

    When used simultaneously with P450 inhibitors (including macrolide group antibiotics, lincomycin, allopurinol, cimetidine, fluoroquinolones), isoprenaline, enoxacin, disulfiram, recombinant interferon alpha, methotrexate, mexiletine, propafenone, thiabendazole, ticlopidine, verapamil and for vaccination against the force of action of theophylline may increase and require a reduction in its dose.

    Strengthens the action of beta-adrenostimulators and diuretics (due to increased glomerular filtration), reduces the effectiveness of lithium and beta-blockers.Compatible with antispasmodics, do not use together with other xanthine derivatives.

    With caution appoint simultaneously with anticoagulants.

    Special instructions:

    In severe diseases of the cardiovascular system, liver, viral infections, as well as in elderly patients, the dose of the drug should be reduced. The severity of the effect of theophylline may decrease in smokers.

    If it is necessary to use theophylline during lactation, it is recommended to stop breastfeeding, as the drug penetrates into breast milk. In case of application at the end of pregnancy, tachycardia in the fetus is possible.

    The drug is not intended for relief of emergency conditions. Treatment with prolonged forms is carried out with periodic monitoring of theophylline concentration in the blood. If bronchial asthma is well controlled and there are no side effects or factors that can change the need for a dose, the measurement of theophylline concentration is carried out at intervals of 6-12 months.

    Be careful when consuming large quantities of caffeine-containing foods or drinks during the treatment period.

    Effect on the ability to drive transp. cf. and fur:
    Form release / dosage:

    Tablets of prolonged action of 100 mg, 200 mg and 300 mg.

    For 10 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

    5 contour mesh packages together with the instruction for use are placed in a pack of cardboard.
    Packaging:(10) - packings, cellular, outline (2) - packs, cardboard
    (10) - packings, cellular, outline (3) - packs, cardboard
    (10) - packings, cellular planimetric (5) - packs cardboard
    (20) - polymer cans (1) - cardboard packs
    (30) - polymer cans (1) - packs of cardboard
    (50) - polymer cans (1) - cardboard packs
    Storage conditions:List B. In a dry, the dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.
    Shelf life:

    3 years. Do not use after the expiration date.

    Terms of leave from pharmacies:On prescription
    Registration number:LSR-001948/09
    Date of registration:16.03.2009
    The owner of the registration certificate:VALENTA PHARM, PAO VALENTA PHARM, PAO Russia
    Manufacturer: & nbsp
    Information update date: & nbsp17.09.2015
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