Composition, form of production and packaging
Capsules of prolonged action 1 caps.
theophylline 200 mg
[PRING] dibutyl phthalate, silicon dioxide colloidal anhydrous, ammonium methacrylate copolymer type B, ammonium methacrylate copolymer type A, povidone, talc.
Capsule shell composition: gelatin, indigo carmine (E132) dye, titanium dioxide (E171), quinoline yellow dye (E104).
10 pieces. - packings cellular planimetric (4) - packs cardboard.
Capsules of prolonged action 1 caps.
theophylline 350 mg
[PRING] dibutyl phthalate, silicon dioxide colloidal anhydrous, ammonium methacrylate copolymer type B, ammonium methacrylate copolymer type A, povidone, talc.
Capsule shell composition: gelatin, indigo carmine (E132) dye, titanium dioxide (E171), quinoline yellow dye (E104).
10 pieces. - packings cellular planimetric (4) - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2011.
PHARMACHOLOGIC EFFECT
Theotard is a theophylline (a xanthine derivative) in the form of pellets. Theophylline refers to inhibitors of phosphodiesterase, increases accumulation in the tissues of c-AMP, 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, blood vessels (mainly the vessels of the brain, skin and kidneys); has a peripheral vasodilating effect, increases renal blood flow, has a moderate diuretic effect. 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 the respiratory and intercostal muscles, stimulates the respiratory center. 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 heart, has a positive inotropic and chronotropic effect on the heart, increases coronary blood flow and the need for myocardium in oxygen. Reduces the tone of blood vessels (mainly 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. It inhibits platelet augmentation (suppresses the platelet activation factor and PgE2 alpha), increases the resistance of erythrocytes to deformation (improves the rheological properties of the blood), reduces thrombosis and normalizes microcirculation.
Replaced release of active ingredient from prolonged-action capsules ensures the achievement of the therapeutic level of theophylline in the blood 3-5 h after administration and its preservation for 12 h, so that effective theophylline concentrations in the blood during the day are maintained when taking the drug 2 times a day.
The bronchodilator effect of Teotard develops gradually, so the drug is not prescribed for relief of emergency conditions.
PHARMACOKINETICS
After oral administration, Teotard is almost completely absorbed, bioavailability is 88-100%. The delayed release of the active ingredient from prolonged-action capsules of the Teotard preparation ensures maintenance of an even level of theophylline in the serum for 12 hours.
After a single dose of 350 mg of the drug, within 7 hours its C max in plasma is reached, which is 4.4 Ојg / ml. The therapeutic concentration is achieved after a few days and it is 8-20 Ојg / ml. Binding to 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 (in children - 50%).
T 1/2 in non-smoking patients is 7-9 hours. Smoking people are significantly shorter - 4-5 hours. In patients with cirrhosis of the liver, heart failure, renal insufficiency and in patients with alcoholism, T 1/2 is lengthened. The total clearance is reduced in patients with high fever, expressed respiratory insufficiency, in patients with hepatic insufficiency or chronic heart failure (CHF), in viral infections, in patients older than 55 years.
INDICATIONS
- bronchobstructive syndrome of any genesis: bronchial asthma, chronic obstructive bronchitis and COPD;
- pulmonary hypertension, "pulmonary" heart;
- nocturnal respiratory disorders of central genesis (nocturnal apnea).
DOSING MODE
Inside, after eating, squeezed with enough liquid. Capsules of prolonged action can not be opened or chewed.
The dosage of the drug is individual. It is inadmissible to exceed the daily dose of 15 mg / kg in adults in 2 divided doses at an interval of 12 hours, 20 mg / kg inchildren . To select the dose of the drug, it is necessary to determine the concentration of theophylline in the blood serum. As a rule, the concentration of theophylline in the serum from 10 to 15 Ојg / ml provides a therapeutic effect with a minimal risk of side effects. If the concentration exceeds 20 Ојg / ml, then the dose of the drug should be reduced. It is recommended to carry out the control every 6-12 months.
For the first three days, one capsule (200-350 mg) of the drug should be taken every 12 hours. On the third day, the effectiveness of the therapy and the tolerability of the drug should be evaluated. With 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, the age and body weight of the patient.
Morning and evening doses of the drug may be different depending on the time of occurrence of bouts of difficulty breathing, the clinical picture of the disease and the effectiveness of therapy.
Teotard 200 mg is given to children weighing more than 20 kg, as well as adults with low body weight .
Teotard 350 mg is given to adults and children weighing more than 40 kg . The usual maintenance dose for adults with a body weight above 60 kg is 350 mg of Teotard 2 times / day.
For non-smoking adults with a body weight of more than 60 kg, the initial dose is 350 mg / day in 1 evening. Then the dose is subsequently increased by 350 mg to a maintenance dose (an average of -700 mg / day in 1 evening).
For smokers and people with an increased metabolism of the drug, the initial dose is 350 mg, and the supporting dose can be increased to 1.15 g / day (2 tablets in the evening, 1 tablet in the morning).
In people with low clearance of the drug, the initial dose is 200 mg / day, which is then increased 200 mg after 2 days to the maintenance dose 400 mg / day in 1 evening, and in individuals with a body weight of less than 60 kg 200 mg / day.
Children 6-12 years of age are prescribed 200 mg capsules. The daily dose for children 6-8 years (with a body weight of 20-30 kg) - 400 mg, the frequency of the appointment - 2 times / day; for children 8-12 years (with a body weight of 30-40 kg) - 600 mg, multiplicity of appointment - 3 times / day.
Children aged 12-16 years (with a body weight of 40-60 kg) are prescribed capsules 350 mg. The daily dose is 0.7-1.4 g, the multiplicity is 2-3 times / day.
The effect of the drug manifests itself in full 3-4 days after the appointment of treatment.
SIDE EFFECT
On the part of the digestive system: abdominal pain, nausea, vomiting, diarrhea, gastroesophageal reflux, heartburn, peptic ulcer exacerbation, with prolonged use, decreased appetite.
From the central and peripheral nervous system: dizziness, headache, agitation, anxiety, tremor, irritability, vertigo, insomnia.
On the part of the cardiovascular system: palpitation, tachycardia (including the fetus when taking a pregnant woman in the III trimester), arrhythmias, a decrease in blood pressure, cardialgia, an increase in the frequency of angina attacks.
Allergic reactions: skin rash, itching, fever.
Laboratory indicators: hypokalemia and / or hypercalcemia, hyperglycemia and hyperuricemia, albuminuria, hematuria.
Other: chest pain, tachypnea, sensation of "hot flashes" to the skin of the face, increased diuresis, increased sweating.
The incidence of side effects increases if the concentration of the drug in the blood serum exceeds 20 Ојg / ml. Side effects decrease with a decrease in the dose of the drug.
CONTRAINDICATIONS
- epilepsy;
- Acute myocardial infarction, severe arterial hyper- or hypotension, severe arrhythmias, hemorrhagic stroke, hemorrhage into the retina of the eye;
- Stomach ulcer and duodenal ulcer in the stage of exacerbation, gastritis with high acidity, bleeding from the gastrointestinal tract;
- Children under 6 years (for capsules 200 mg), up to 12 years (for capsules 350 mg);
- hypersensitivity to theophylline (including other derivatives of xanthine - caffeine, pentoxifylline, theobromine);
With caution : severe violations of the liver and kidneys, severe coronary insufficiency (unstable angina), widespread atherosclerosis of the vessels, hypertrophic obstructive cardiomyopathy, frequent ventricular extrasystole, CHF, increased convulsive readiness, porphyria, stomach and duodenal ulcer in history, bleeding from the gastrointestinal tract in a recent medical history, uncontrolled hypothyroidism (the possibility of cumulation) or thyrotoxicosis, prolonged hyperthermia, gastroesophageal reflux, hypertrophy prostate cancer, pregnancy and lactation period, elderly age (over 60 years), children's age.
PREGNANCY AND LACTATION
Theophylline penetrates the placental barrier and is excreted into breast milk, so pregnant women can only be used when the expected benefit to the mother exceeds the potential risk to the fetus. If possible, more frequent monitoring (monitoring) of serum theophylline concentration and dose adjustment is recommended. In the III trimester of pregnancy, the appointment of theophylline is not recommended, since it may reduce uterine contractility.
Breastfeeding mothers are encouraged to closely monitor newborns. If irritation develops and sleep disturbances occur in the newborn, it is necessary to consult a doctor.
APPLICATION FOR FUNCTIONS OF THE LIVER
With caution : severe renal dysfunction.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
With caution : severe liver dysfunction.
APPLICATION FOR CHILDREN
Contraindicated:
- Children under 6 years (for capsules 200 mg), up to 12 years (for capsules 350 mg).
APPLICATION IN ELDERLY PATIENTS
With caution appoint the drug to elderly patients (60 years).
SPECIAL INSTRUCTIONS
Persons who have theophylline subjected to rapid metabolism (young people, smokers), one-time intake of the drug per day will be insufficient.
A decrease in the daily dose is required in patients with heart failure, liver failure (especially cirrhosis of the liver), high fever, pneumonia, with viral infections (especially with the flu), thyroid gland hyperfunction, some drugs, elderly patients.
During therapy with Teotard, it is not recommended to take alcohol or a large number of drinks or products containing methylxanthines (coffee, tea, cocoa, chocolate, coca-cola and similar drinks, tonic drinks). the stimulating effect of theophylline on the central nervous system is potentiated.
When receiving theophylline, it is possible to change some of the results of laboratory tests: an increase in the content of fatty acids and the level of catecholamines in the urine.
Impact on the ability to drive vehicles and manage mechanisms
The adverse effect of Teotard on the ability to drive a car and other mechanisms was not reported.
OVERDOSE
Symptoms: decreased appetite, pain in the stomach, diarrhea, nausea, vomiting (including blood), gastrointestinal bleeding, tachypnea, facial skin hyperemia, 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, decreased blood pressure, necrosis of skeletal muscles, confusion, renal insufficiency, and myoglobinuria.
Treatment: withdrawal 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, plasmosorption, hemodialysis (efficacy is low, peritoneal dialysis is ineffective), symptomatic therapy (including metoclopramide, and ondansetron - with vomiting). If seizures occur, maintain airway patency and conduct oxygen therapy. For relief of seizure - iv diazepam, 0.1-0.3 mg / kg (but not more than 10 mg). With severe nausea and vomiting - metoclopramide or ondansetron (IV).
DRUG INTERACTION
Theophylline is not used together with other xanthine derivatives.
Increases the likelihood of side effects of GCS (hypokalemia), 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.
When combined with antibiotics, the group of macrolides, lincomycin, allopurinol, cimetidine, fluoroquinolones (recommended to reduce the theophylline dose by 60%), disulfiram, phenylbutazone, fluvoxamine, imipenem, paracetamol, probenecid, ranitidine, tacrine, thiabendazole, recombinant interferon alpha, methotrexate, mexiletine , nropaphenone, thiabendazole, ticlopidine, verapamil, isoprenaline, oral estrogen-containing contraceptives, phenobarbital, pentobarbital, magnesium hydroxide, morac rinovir or sulphinpyrazone, rifampicin, isoniazid, carbamazepine, primidon, sulphinpyrazone, aminoglutethimide, phenytoin, enoxacin (recommended to reduce theophylline dose by 30%), viloxazine and with influenza vaccination, the intensity of action may increase, which may require a decrease in theophylline dose.
The drug inhibits the therapeutic effects of lithium carbonate, adenosine and beta-adrenoblockers.
Theophylline potentiates the action of beta-adrenostimulants, reserpine and diuretics due to increased glomerular filtration and reduced tubular reabsorption.
Compatible with antispasmodics.
Against the background of a joint admission with alpha-adrenoreceptor blockers, thiazide diuretics, furosemide, the risk of hypokalemia increases.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
Store in a dry, dark place at a temperature of no higher than 25 В° C. Keep out of the reach of children. Shelf life - 5 years.
