Teotard - instructions for use, doses, side effects, contraindications

Excipients: povidone, silicon dioxide colloidal, anhydrous, triethyl citrate, methyl methacrylate, trimethylammonioethyl methacrylate chloride and ethyl acrylate copolymer [1: 2: 0.1], methyl methacrylate, trimethylammonioethyl methacrylate chloride and ethyl acrylate copolymer [1: 2: 0.2], talc.

Capsule shell composition: gelatin, titanium dioxide E171, dye quinoline yellow E104, indigo carmine dye E132.

Description:

Hard, gelatin capsules. The capsule body is a transparent dark green color, the cap of the capsule is an opaque dark green color. The contents of capsules are pellets of white color. Capsules 200 mg - №2, capsules 350 mg - №1.

Pharmacotherapeutic group:Bronchodilator

ATX: & nbsp

R.03.D.A.04 Theophylline

Pharmacodynamics:

Theotard is a theophylline (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 the "small" circle of blood circulation. Increases renal blood flow, has a moderate diuretic effect. Expands extrahepatic biliary tract. It inhibits platelet aggregation (suppresses the platelet activation factor and PgE2 alpha), increases the resistance of erythrocytes to deformation (improves the rheological properties of the blood), reduces thrombus formation and normalizes microcirculation.

The delayed release of the active ingredient from prolonged-action capsules ensures the therapeutic level of theophylline in the blood 3-5 hours after ingestion and its preservation for 12 hours, 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 - 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 is reached its maximum concentration (TC_mOh) in the plasma, which is 4.4 μg / ml. The therapeutic concentration is achieved after a few days and it is 8-20 μg / ml. 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 (in children - 50%).

The half-life (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 lengthens. The overall clearance is lower in patients with high fever, expressed respiratory failure,in patients with hepatic insufficiency or chronic heart failure (CHF), in viral infections, in patients older than 55 years.

Indications:

- Bronchobstructive syndrome of any origin: bronchial asthma, chronic obstructive bronchitis and COPD.

- Pulmonary hypertension, pulmonary heart.

- Night respiratory disorders of central origin (nocturnal apnea).

Contraindications:

- Hypersensitivity to theophylline (including other derivatives of xanthine - caffeine, pentoxifylline, theobromine);

- epilepsy;

- acute myocardial infarction, severe arterial hyper- or hypotension, severe arrhythmias, hemorrhagic stroke, hemorrhage into the retina of the eye;

- peptic ulcer of the stomach and duodenum in the stage of exacerbation, gastritis with high acidity, bleeding from the gastrointestinal tract (GIT);

- Children under 6 years (for capsules 200 mg), up to 12 years (for capsules 350 mg).

Carefully:

Severe violations of liver and kidney function, severe coronary insufficiency (unstable angina), widespread atherosclerosis of the vessels, hypertrophic obstructive cardiomyopathy, frequent ventricular extrasystole, CHF,increased convulsive readiness, porphyria, peptic ulcer of the stomach and duodenum, history of bleeding from the gastrointestinal tract in recent history, uncontrolled hypothyroidism (possibility of cumulation) or thyrotoxicosis, prolonged hyperthermia, gastroesophageal reflux, prostatic hypertrophy, pregnancy and lactation, elderly age 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 third 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, the newborn should consult a doctor.

Dosing and Administration:

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 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, the concentration of theophylline in the serum from 10 to 15 μg / ml provides a therapeutic effect with a minimal risk of side effects. If the concentration exceeds 20 μg / 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 therapy and the tolerability of the drug should be assessed. 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 a 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 (on average, 700 mg / day in 1 evening).

For smokers and people with 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 are taken 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 a day; for children 8-12 years (with a body weight of 30-40 kg) - 600 mg, the frequency of the appointment - 3 times a 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 in knocking.

The effect of the drug manifests itself in full 3-4 days after the appointment of treatment.

Side effects:

From the gastrointestinal tract: abdominal pain, nausea, vomiting, diarrhea, gastroesophageal reflux, heartburn, peptic ulcer exacerbation, with prolonged admission - a decrease in appetite.

From the central and peripheral nervous system: dizziness, headache, agitation, anxiety, tremor, irritability, vertigo, insomnia.

From the cardiovascular system: palpitations, palpitations, tachycardia (including the fetus when taking a pregnant woman in the III trimester), arrhythmias, lowering blood pressure (BP), 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: pain in the chest, tachypnea, a 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 μg / ml. Side effects decrease with a decrease in the dose of the drug.

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, epileptoid seizures (especially in children without any precursors), hypoxia, metabolic acidosis, hyperglycemia, hypokalemia, decreased blood pressure, necrosis of skeletal muscles, confusion, renal insufficiency, and 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. For seizure seizure - in / in diazepam, 0.1-0.3 mg / kg (but not more than 10 mg).With severe nausea and vomiting - metoclopramide or ondansetron (w / w).

Interaction:

Theophylline is not used together with other xanthine derivatives.

Increases the likelihood of side effects of glucocorticosteroids (GCS) (hypokalemia), mineralocorticosteroids (MKS) (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 , propafenone, tiabendazole, ticlopidine, verapamil, isoprenaline, oral estrogen-containing contraceptives, phenobarbital, pentobarbital, magnesium hydroxide, morac izine, ritonavir or sulphinpyrazone, rifampicin, isoniazid, carbamazepine,primidon, sulphinpyrazone, aminoglutethimide, phenytoin, enoxacin (it is recommended to reduce the theophylline dose by 30%), viloxazine and during influenza vaccination, the intensity of action may increase, which may require a decrease in the 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-receptor blockers, thiazide diuretics, furosemide, the risk of hypokalemia increases.

Special instructions:

Persons with whom theophylline is subject 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 liver cirrhosis), high fever, pneumonia, with viral infections (especially with the flu), thyroid gland hyperfunction, with some medications (see p."Interaction with other drugs"), in 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.

Effect on the ability to drive transp. cf. and fur:

The adverse effect of Teotard on the ability to drive a car and other mechanisms was not reported.

Form release / dosage:

Capsules of prolonged action, 200 mg and 350 mg.

Packaging:

10 capsules in a blister pack.

4 blisters in a cardboard box together with instructions for use.

Storage conditions:

Store at a temperature not exceeding 30 ° C.

Keep out of the reach of children.

Shelf life:

5 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:П N014325 / 01

Date of registration:01.07.2008

Expiration Date:Unlimited

The owner of the registration certificate:KRKA, dd, Novo mesto, AOKRKA, dd, Novo mesto, AO

Manufacturer: & nbsp

KRKA-RUS, LLC Russia

VECTOR-MEDICA, CJSC Russia

KRKA, d.d. Slovenia

Representation: & nbspKRKA, dd, Novo mesto, AOKRKA, dd, Novo mesto, AO

Information update date: & nbsp31.01.2017

Illustrated instructions

Instructions

Theotard (Theotard®)