Теофил® WEDNESDAY

General characteristics. Structure:

Active ingredient: 136,98 mg of theophylline of a micropellet (100 mg of theophylline are equivalent).

Structure of a cover of the capsule: the capsule case – gelatin, a capsule lid – a pace red (Е 129), gelatin.

Broncholitic drug.

Pharmacological properties:

Pharmacodynamics. Theophylline suppresses activity of specific phosphodiesterases (FDE), stabilizes intracellular concentration of cyclic adenosinemonophosphate (tsAMF). Theophylline blocks receptors of adenosine and relaxes smooth muscles of bronchial tubes and blood vessels of lungs.

Theophylline stimulates a respiratory center of a myelencephalon, increasing sensitivity to a promoting effect of carbon dioxide.

Theophylline can reduce the hyperreactivity of respiratory tracts connected with a late phase of the reaction caused by inhalation of allergens.

Theophylline increases number and activity of T-suppressors in peripheral blood.

Theophylline also expands peripheral, coronary and renal vessels, has moderate diuretic effect, inhibits aggregation of thrombocytes, slows down release from mast cells of mediators of an allergy. Theophylline exerts the stimulating impact on a cardiac muscle and on the central nervous system, causes brain vasoconstriction, increases contractility of a diaphragm, reduces the general peripheric resistance of vessels, including resistance of pulmonary vessels, causes increase in secretion of acid in a stomach.

Pharmacokinetics. At intake theophylline is quickly and completely soaked up from digestive tract. Presence of food at a stomach can influence theophylline absorption speed, and also its clearance.

The maximum concentration in plasma after administration of drug inside, is reached 6-9 hours later. Protein-binding of plasma makes 60%, people with a disease of a liver have 20-40%. Theophylline moderately gets into fabrics, distribution volume near 0,5l/kg. However well gets through a blood-brain barrier, a placenta and into breast milk.

Theophylline is metabolized in a liver for 90%. The theophylline elimination half-life at non-smoking patients with bronchial asthma and without pathological changes from other bodies and systems makes 6-12 hours, smokers have 4-5 hours. The elimination half-life increases at elderly patients and at patients with heart failure and diseases of a liver. The drug elimination half-life for children makes 1,5 hours. It is generally removed by urine. Duration of preservation of therapeutic concentration in blood fluctuates from 4 to 5 hours.

Indications to use:

- bronchial asthma;
- simtomatichesky treatment of a bronchospasm of various etiology (including at chronic obstructive pulmonary diseases, chronic bronchitis, emphysema of lungs);
- pulmonary hypertensia;
- pulmonary heart;
- night paroxysmal apnoea.

Route of administration and doses:

Drug is used orally, washing down with enough liquid. The mode of dosing are established individually. To swallow capsules entirely, without opening and without chewing.

To children 12 years and to teenagers are more senior. A single dose - 100 mg; a daily dose - 200 mg. Maximum single dose-200 of mg; the maximum daily dose - 400 mg.

If improvement of a state is not observed, then the dose can be increased approximately by 25% each 3 days during time so far drug normally is transferred.

Increase in a dose has to be made to the maximum doses provided below:
Age Dosage

12-16 years: 18 mg/kg a day

16 years are also more senior: 13 mg/kg a day or on 900 mg a day.

For non-smoking adult patients with the body weight of 60 kg and the initial dose - 200 mg a day, then on 200 mg 2 times a day is higher. Patients with body weight have less than 60 kg an initial single dose - 100 mg in the evening, then on 100 mg 2 times a day. Treatment is begun with smaller doses which gradually, at an interval of 1-2 days, increase (by 100-200 mg/days) before obtaining the maximum therapeutic effect, at bad portability - reduce. The dose depends on the nature of a disease, age and body weight of the patient. In need of appointment in high doses treatment is carried out under control of concentration of theophylline to blood (therapeutic concentration - within 10-15 mkg/ml): at concentration of 20-25 mkg/ml it is necessary to lower a daily dose by 10%; 25-30 mkg/ml - for 25%; it is higher than 30 mkg/ml - the daily dose is reduced twice. Repeated control is carried out in 3 days. At too low concentration the daily dose is increased by 25% with 3-day intervals. At stabilization of a condition of the patient against the background of reception in high doses it is necessary to carry out control every 6-12 month.

The maximum daily dose for not smoking adults makes 1200/kg.

The maximum daily dose for the smoking adults makes 900-1250/kg.

The maintenance dose for adults with body weight is higher than 60 kg - 600 mg/days, less than 60 kg - 400 mg/days.

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

For patients with diseases warmly – vascular system and an abnormal liver function: with body weight more than 60 kg a daily dose - 400 mg, with body weight less than 60 kg - 200 mg. Reduction of a daily dose is required from patients with severe damages of heart, liver, with viral infections, from patients of advanced age.

Features of use:

Tablets with the prolonged release are not intended for stopping of medical emergencies. Treatment by the prolonged forms is carried out at periodic control of concentration of theophylline to blood.

Theophylline has to be applied with care at patients with: heavy coronary insufficiency (stenocardia), widespread atherosclerosis of vessels, a hypertrophic subaortic stenosis, frequent ventricular premature ventricular contraction, HSN, a liver and/or renal failure, a peptic ulcer of a stomach and a 12-perstny gut (in the anamnesis), an uncontrollable hypothyroidism (a possibility of cumulation), a long hyperthermia, a prostatauxe.

Drug should not will be applied together with the drugs containing xanthine derivatives (caffeine, theobromine, пентоксифиллин).

Lactation period. It is necessary to consider that theophylline is emitted with breast milk. In case of need purposes of drug in the period of a lactation the question of the breastfeeding termination is raised.

Features of influence of medicine on ability to manage the vehicle or potentially dangerous mechanisms. Due to the undesirable effects on the central nervous system – it is necessary to apply theophylline with care.

Side effects:

- heartburn, nausea, vomiting, an aggravation of a peptic ulcer, pain in epigastriums, diarrhea, at long reception - a loss of appetite;

- a headache, dizziness, irritability, uneasiness, concern, sleeplessness, the increased reflex irritability, clonic and tonic convulsions, a tremor;

- heartbeat, tachycardia, arrhythmia, premature ventricular contraction, rushes of blood, hypotension, blood circulation disturbance, ventricular arrhythmia, increase in frequency of attacks of stenocardia, pain in heart;

- tachypnea;

- increase in a diuresis, hamaturia, albuminuria;

- alopecia;

- hypoglycemia, hypopotassemia;

- skin itch, rash.

Interaction with other medicines:

Theophylline exponentiates broncholitic action of beta2-adrenomimetik that allows to use the last in smaller doses.

Theophylline increases clearance of lithium and a pyridoxine at joint appointment therefore their efficiency decreases at invariable concentration of drug in a blood plasma.

Concentration of theophylline in blood to decrease at simultaneous use with phenobarbital, rifampicin, an isoniazid, carbamazepine, Sulfinpyrazonum, Phenytoinum, and also at smokers.

Concentration of theophylline in blood increases at simultaneous use with antibiotics from group of macroleads, Allopyrinolum, beta adrenoblockers, Cimetidinum, hormonal oral contraceptives, izoprenaliny, lincomycin.

Theophylline can exponentiate the hypopotassemia caused by action of stimulators β2-адренорецепторов, corticosteroids and diuretics.

Contraindications:

- hypersensitivity to theophylline (including to other derivatives of xanthine) or to drug components;

- epilepsy and other convulsive states;

- hyperfunction of a thyroid gland;

- acute myocardial infarction;

- subaortal stenosis;

- premature ventricular contraction, heavy tachyarrhythmias, heavy arterial hyper - or hypotension;

- hemorrhagic stroke;

- gastritis with a hyperoxemia, bleeding from digestive tract in the recent anamnesis;

- a peptic ulcer of a stomach and duodenum in an aggravation phase;

- eye retinal apoplexy;

- children's age up to 12 years;

- pregnancy.

Overdose:

Symptoms: a loss of appetite, a gastralgia, diarrhea, nausea, vomiting (including with blood), gastrointestinal bleeding, a tachypnea, a dermahemia of the person, tachycardia, ventricular arrhythmia, sleeplessness, motive excitement, uneasiness, a photophobia, a tremor, spasms. At a serious poisoning epileptoidny attacks, a hypoxia, a metabolic acidosis, a hyperglycemia, a hypopotassemia, a lowering of arterial pressure, a necrosis of skeletal muscles, confusion of consciousness, a renal failure with a myoglobinuria can develop.

Treatment: drug withdrawal, a gastric lavage, purpose of absorbent carbon, laxative medicines, an artificial diuresis, hemosorption, a plazmosorbtion, symptomatic therapy (including Metoclopramidum and ондансетрон - at vomiting). For stopping of an attack - in/in diazepam, 0.1-0.3 mg/kg (but no more than 10 mg). At severe nausea and vomiting - Metoclopramidum or ондансетрон (in/in).

Storage conditions:

To store at a temperature not over 25 ºС, in the dry, protected from light place. To store in the place, unavailable to children! Period of storage 3 years. Not to apply after a period of validity, specified on packaging.

Issue conditions:

According to the recipe

Packaging:

On 10 capsules place in a blister strip packaging from a film of polyvinyl chloride and printing aluminum foil.

On 3 planimetric packagings together with the instruction on a medical use in the state and Russian languages place in a pack cardboard with the hologram of firm – producer.