Long acting theophyllines. Theophylline: instructions for use

I capsule with modified release 100 mg contains: theophylline anhydrous 100 mg excipients: neutral micropellets (sucrose and corn starch), bleached shellac, talc, gelatin, azorubine (E122).
1 capsule with modified release 200 mg contains: theophylline anhydrous 200 mg,
excipients: neutral micropellets (sucrose and corn starch), bleached shellac, talc, gelatin, indigo carmine (E132). .,
1 capsule with modified release 300 mg contains: theophylline anhydrous 300 mg,
excipients: neutral micropellets (sucrose and corn starch), bleached shellac, talc, gelatin, quinoline yellow (E104), patent blue V (E131).

Description

Capsules 100 mg
Hard gelatin capsules No. 3 consisting of a colorless body and a pink cap.
Capsules 200 mg
Hard gelatin capsules No. 2 consisting of a colorless body and a dark blue cap.
Capsules 300 mg
Hard gelatin capsules No. 1 consisting of a colorless body and a green cap.

Indications for use

TEOPHIL SR® is used as a bronchodilator for symptomatic treatment and prevention of attacks of bronchial asthma, reversible bronchospasm with chronic bronchitis and bronchial asthma
-treatment and prevention of attacks of difficulty breathing in patients with chronic obstructive pulmonary diseases;

Contraindications

Age up to 6 years;
- increased sensitivity to the components of the drug;
-epilepsy;
- stomach ulcer and duodenum in the acute phase

Pregnancy and lactation

The use of theophylline during pregnancy should only be considered if safe options are not available. alternative methods treatment. Theophylline crosses the placenta; the safety of its use during pregnancy has not been established.
Theophylline is excreted in breast milk and should not be administered to nursing mothers.

Directions for use and doses

Doses of the drug are set individually. Since theophylline is not distributed in adipose tissue, the dose of the drug is calculated based on ideal body weight. The recommended doses are as follows.
Adults: 200-300 mg 2 times a day.
Children over 6 years of age: 100-200 mg 2 times a day.

Age	Dose
6-9 years	24 mg/kg/day
9-12 years	20 mg/kg/day
12-16 years old	18 mg/kg/day
Over 16 years old	13 mg/kg/day or 900 mg/day

Capsules should be taken whole, without chewing, with a sufficient amount of liquid.
The total dose should usually not exceed 24 mg/kg body weight
for children and 13 mg/kg for adults. Bioequivalence cannot be guaranteed between various drugs containing theophylline. If an effective dose has been selected for the patient once, then he should not replace Theofil with another drug containing xanthines without repeated selection. effective dose and clinical supervision.

Side effect

Side effects are closely related to serum theophylline concentrations and are therefore rare with extended-release formulations. The following side effects were noted:
Gastrointestinal tract: nausea, vomiting, abdominal pain, diarrhea.
Central nervous system: headache, irritation, fatigue, insomnia, reflex hyperexcitability, muscle twitching, clonic and tonic generalized convulsions.
Cardiovascular system: flutter, tachycardia, extrasystole, hot flashes, hypotension, circulatory collapse, ventricular arrhythmia.
Respiratory system: tachypnea.
Urinary system: potentiation of diuresis Others: alopecia, hypertriglyceridemia, rash.

Overdose

Signs and symptoms, headache, nausea, vomiting, fatigue, hypotension, tachycardia, arrhythmia (usually supraventricular tachyarrhythmia), possible seizures.
Treatment: empty the stomach by washing or inducing vomiting. Purpose activated carbon. If seizures develop, the patient is administered diazepam 0.1 - 0.3 mg/kg to 10 mg.
For adults, doses greater than 3 g may have serious effects (40 mg/kg for children). The lethal dose for adults may be as low as 4.5 g (60 mg/kg in a child), but is usually higher.
Symptoms
Caution: Severe symptoms may develop within 12 hours of overdose.
Digestive disorders: nausea, vomiting (often severe forms),
pain in the epigastric region
Metabolic functions: Hypokalemia due to the transition of potassium from
plasma in cells is common occurrence, can develop quickly and is severe
character. Hyperglycemia, hypomagnesemia, metabolic
acidosis and rhabdomyolysis.
Treatment:
In case of significant overdose, you should drink activated charcoal within 1-2 hours or do a gastric lavage. .
After a repeated dose of activated charcoal, the removal of theophylline from the body may increase. Measure plasma potassium concentrations promptly and repeat measurements frequently to correct hypokalemia.
ATTENTION! With large doses of potassium during the recovery period, severe hyperkalemia can develop. If plasma potassium concentration is low, magnesium concentration should be measured immediately.
Proconvulsants should be avoided when treating ventricular arrhythmia. antiarrhythmic drugs, such as lidocaine, so as not to cause or aggravate an attack.
If theophylline poisoning is suspected, its plasma concentration should be measured regularly until it drops.-
Vomiting should be treated with antiemetic drugs such as metoclopramide or ondansetron.
Tachycardia with normal cardiac output does not require specific treatment. Beta blockers may be given in extreme cases, provided the patient is not asthmatic. For seizures (provided that they are not caused by hypokalemia), diazepam is administered intravenously.

Interaction with other drugs

With the simultaneous administration of theophylline and furosemide, beta-agonists, and other methylxanthines, the effect of theophylline is enhanced.
Ephedrine and ephedrine-containing drugs can increase both direct and side effects
effects of theophylline.

Theophylline is a phosphodiesterase inhibitor; bronchodilator.

Release form and composition

The dosage form of Theophylline is long-acting tablets (10 pcs. in blister packs, 2, 3 or 5 packs in a cardboard pack; 20, 30 or 50 pcs. in polymer jars, 1 jar in a cardboard pack).

The active ingredient of the drug is theophylline. 1 tablet contains 100, 200 or 300 mg.

Indications for use

• Broncho-obstructive syndrome of various origins: chronic obstructive disease lungs (chronic obstructive bronchitis and emphysema), bronchial asthma(exertional asthma is the drug of choice, other forms of bronchial asthma are an additional remedy);
• Edema syndrome of renal origin (as an auxiliary drug in the composition combination therapy);
• Pulmonary hypertension and cor pulmonale;
• Sleep apnea.

Contraindications

Theophylline is contraindicated in the following conditions/diseases:

• Retinal hemorrhage;
• Hemorrhagic stroke;
• Epilepsy;
• Severe tachyarrhythmias;
• Severe arterial hypo- and hypertension;
• Bleeding from gastrointestinal tract in recent history;
• Gastritis with high acidity;
• Exacerbation peptic ulcer stomach and duodenum;
• Children under 12 years of age;
• Hypersensitivity to the components of the drug or to other xanthine derivatives (theobromine, pentoxifylline, caffeine).

Theophylline should be used with caution and under special medical supervision in the following cases:

• Children and old age;
• Severe coronary insufficiency (angina pectoris and acute phase of myocardial infarction);
• Hypertrophic obstructive cardiomyopathy;
• Common vascular atherosclerosis;
• Hepatic and/or renal failure;
• Increased convulsive readiness;
• Uncontrolled hypothyroidism and thyrotoxicosis;
• Chronic heart failure;
• Ventricular extrasystole;
• Prolonged hyperthermia;
• Hypertrophy prostate gland;
• Gastroesophageal reflux;
• History of gastric and duodenal ulcers.

During pregnancy, the drug can only be used if the expected benefit for the expectant mother exceeds possible risks for the fetus.

If it is necessary to carry out treatment with Theophylline during lactation, it should be taken into account that the substance is excreted in breast milk.

Directions for use and dosage

Theophylline is taken orally with water and without chewing, after meals. The dose for each patient is determined individually.

The initial dose is usually 400 mg per day. If well tolerated, it is increased every 2-3 days by approximately 25% of the initial dose until the optimal therapeutic effect is achieved.

Without monitoring the concentration of theophylline in blood plasma, the following maximum doses can be used:

• Adults and adolescents over 16 years of age – 13 mg/kg or 900 mg per day;
• Children 12-16 years old – 18 mg/kg/day;
• Children 9-12 years old – 20 mg/kg/day;
• Children 3-9 years old – 24 mg/kg/day.

If, when taking the drug in recommended doses, symptoms of toxic effects appear or there is a need to further increase the dose due to insufficient effect, the content of theophylline in the blood plasma should be monitored. The optimal therapeutic concentration of the substance is 0.01-0.02 mg/ml. In the case of a lower level, the therapeutic effect is weakly expressed, however, with a higher concentration, a significant increase in the effect is not observed, but the risk of developing side effects.

Elderly people, patients with viral infections and diseases of cardio-vascular system Theophylline dose is reduced.

Side effects

• Digestive system: exacerbation of peptic ulcer, nausea, diarrhea, vomiting, gastralgia, heartburn, gastroesophageal reflux; with long-term therapy – loss of appetite;
• Allergic reactions: itching, skin rash, fever;
• Cardiovascular system: decrease blood pressure, cardialgia, palpitations, increased frequency of angina attacks, arrhythmias, as well as tachycardia, including in the fetus, if the pregnant woman took the drug in the third trimester;
• Central nervous system: agitation, headache, anxiety, insomnia, dizziness, tremor, irritability;
• Other: increased diuresis, hematuria, albuminuria, hypoglycemia, flushing, chest pain, increased sweating, tachypnea.

The severity of side effects decreases after reducing the dose of Theophylline.

special instructions

Intensity therapeutic action the drug in smoking patients may decrease.

Theophylline should not be used in combination with other xanthine derivatives.

Drug interactions

Effect on theophylline in case of simultaneous use of other medicines:

• Propranolol, cimetidine, allopurinol, isoprenaline, lincomycin, macrolide antibiotics, oral contraceptives reduce the clearance of theophylline;
• Beta-blockers, especially non-selective ones, reduce the bronchodilatory effect of theophylline due to narrowing of the bronchi;
• Furosemide, caffeine, beta2-adrenoreceptor stimulants enhance the effect of theophylline;
• Aminoglutethimide increases the excretion of theophylline from the body, thereby reducing its effectiveness;
• Acyclovir, verapamil, nifedipine, disulfiram increase the concentration of theophylline, enhance its side effects or contribute to the development of toxic reactions;
• Phenobarbital, carbamazepine, isoniazid, sulfinpyrazone, rifampicin increase the clearance of theophylline, thereby reducing the intensity of its action;
• Enoxacin and other fluoroquinolones increase plasma theophylline concentrations.

Theophylline reduces the effectiveness of beta-blockers and lithium salts.

In the case of simultaneous use of phenytoin, there is a mutual decrease in plasma concentrations and, as a consequence, a decrease in therapeutic effectiveness.

Terms and conditions of storage

Store in a place protected from light at a temperature not exceeding 25 °C.

Shelf life – 5 years.

Theophylline is a derivative of xanthine, a natural product from the group of purine alkaloids. Refers to pharmacological group. The name comes from the tea leaves from which Albrecht Kossel isolated a small amount of theophylline in 1888.

Tea leaves from which theophylline was isolated.

Theophylline is found in small quantities in coffee beans. Used to treat bronchial asthma and other bronchial diseases. In addition, theophylline improves heart performance and acts as a.

Theophylline is used for acute attacks bronchial asthma and other obstructive diseases respiratory tract, can also be used to treat status asthmaticus resistant to standard therapy. For this purpose, theophylline is administered intravenously.

In extended-release oral dosage forms (extended-release tablets or capsules), theophylline is approved for the long-term treatment and prevention of asthmatic attacks and other obstructive airway diseases. It is used as a reserve remedy for severe bronchial asthma, both as long-term therapy and for the relief of attacks.

In pediatrics, theophylline can be used to treat idiopathic respiratory arrest in premature newborns, accompanied by other therapeutic measures to stimulate breathing. Similarly, theophylline is approved for the secondary prevention of life-threatening apnea in infancy (ALTE), although there is limited reliable data on mortality reduction.

The use of off-label theophylline to prevent kidney damage caused by contrast media is controversial. Its use as a diuretic and its earlier use in the treatment of angina are considered obsolete.

Contraindications

Theophylline should not be used in cases of known hypersensitivity to it, after recent myocardial infarction or acute tachysystolic arrhythmia.

With great caution and strictly according to indications, the drug can be used in patients with:

• unstable angina,
• tendency to tachysystolic arrhythmias,
• severe arterial hypertension,
• hypertrophic obstructive cardiomyopathy,
• hyperthyroidism,
• epilepsy,
• stomach and duodenal ulcers,
• porphyria.

Hepatic and renal dysfunction are not contraindications, but require dosage adjustment and control.

Theophylline during pregnancy and lactation

Theophylline should be avoided during the first trimester of pregnancy as there is insufficient data on its use at this stage of pregnancy. active substance. During the second and third trimesters, theophylline can be used only after a competent assessment of the need and the risk of consequences.

Theophylline goes into breast milk and can reach therapeutically effective levels in serum in infants. Therefore, a health risk assessment should also be carried out, the dosage should be chosen as low as possible and the child may need to be weaned if theophylline is used by the mother.

Interactions

Drugs and other exogenous substances (xenobiotics) that lead to a decrease or increase in the concentration of theophylline in the body can easily lead to either ineffectiveness of the theophylline administered or to toxic reactions. Enzyme inducers such as barbiturates, carbamazepine, phenytoin, primidone, rifampicin and sulfinpyrazone, as well as smoking, lead to accelerated degradation of theophylline.

Inhibitors of the cytochrome P450 system, in particular inhibitors of CYP-1A2, on the contrary, lead to a decrease in the degradation of theophylline, which can lead to its accumulation in the body. Significant interactions are possible with (for example, with), fluoroquinolones (for example, ciprofloxacin, enoxacin), thiabendazole, cimetidine and allopurinol.

The concentration of theophylline also increases when used simultaneously with birth control pills, imipenem, isoniazid, calcium antagonists, propranolol, mexiletine, propafenone, ticlopidine, interferon alpha and influenza vaccines. Interaction with ranitidine is also possible but not guaranteed.

Due to its synergism, theophylline can enhance the effects of other methylxanthines, including caffeine. The effect is similarly enhanced when joint use with beta-2 and diuretics.

The effect of beta blockers and lithium drugs can be mitigated by the use of theophylline. An increase in cardiac side effects from inhalational anesthesia may be observed when used concomitantly with halothane.

Side effects

In 10% of cases, theophylline may affect nervous system, this can manifest itself as headaches, tremors, anxiety, and insomnia. The drug can also affect the metabolism and electrolyte balance of the body, which manifests itself as hypokalemia, hypoglycemia, hyperuricemia, an increase in serum calcium (hypercalcemia) and creatinine.

Also very common side effects are: genitourinary system and, most often, in the form of increased diuresis. This side effect has previously been used to treat theophylline as a diuretic. Very rarely (0.1 - 1%) hypersensitivity reactions to theophylline may occur, requiring replacement of the drug.

Recipe in Latin

The theophylline prescription in Latin is written out, like any other, in the form and. If you want to read in more detail and step by step how to prescribe a specific dosage form, click on the previous links. Find even more examples in ours. An example of theophylline capsule prescription:

Rp.: Theophyllini 200 mg
D.t.d. N 20 in caps.

in tablets:

Rp.: Theophyllini 200 mg
D.t.d. N 50 in tab.
S. Orally, 1 capsule 2 times a day.

Theophylline is most often used for complex treatment asthma. This option is one of the cheapest today.

Side effects when using the drug occur regularly. This fact slightly weakens the popularity of Theophylline.

Patients with severe asthma mostly take this drug.

The use of Theophylline in small portions can play the role of an immunomodulator and also reduce inflammatory processes. It is most effective when paired with inhaled steroid hormones.

Indications for use

This is broncho-obstructive syndrome of various types:

• bronchial asthma (both the main medicine and additionally administered);
• obstructive bronchitis;
• asthmatic status;
• emphysema;
• sleep apnea;
• pulmonary hypertension;
• pulmonary heart syndrome (pathology of the right side of the heart);
• edema syndrome.

Mode of application

Ingestion. The mode is set individually. It all depends on the patient’s age, body weight, and the nature of the disease. Typically, adults are prescribed 0.1 or 0.2 grams two or four times a day. If the dynamics of treatment are positive, the dose is increased by a quarter every two days.

Maximum daily dose for an adult- 1.2 grams, no more than 0.4 grams of the drug can be taken at a time. For children from 3 to 9 years old, the daily dose is 0.2 grams.

If while taking the medication there are toxic factors, it is recommended to periodically analyze the level of theophylline in the blood. The normal level is considered to be 15 mcg/ml.

If the examination reveals a lower level of concentration, then its effect is not pronounced. If the level is sharply increased, then there is a high probability of side effects.

Release form, composition

The drug is available in the form of tablets, capsules, suppositories and powder. You can also buy theophylline in the form of an elixir at the pharmacy.

Ingredients: theophylline 300 mg.

The effect of this drug is significantly reduced when used with drugs Propranolol, Isoprenaline tablets, Lincomycin, Cimetidine, oral contraceptives.

Simultaneous use of non-selective beta-blockers leads to narrowing of the bronchi. This negatively affects the effectiveness of theophylline.

Caffeine and Furosemide enhance the effect of theophylline.

Aminoglutethimide has the ability to remove theophylline from the body. This significantly reduces the effect of taking the drug.

Acyclovir increases the concentration of theophylline in the blood. The risk of side effects increases.

Side effects

For patients suffering from asthma attacks, intravenous aminophylline gives less effect than nebulized β2-agonists. It is used to treat patients who do not respond to β2-agonists.

A drug regularly causes in patients side effects . Theophylline is very quickly and completely absorbed from the gastrointestinal tract, but there are some factors that affect its plasma clearance.

Side effects: restlessness, loss of control of consciousness, convulsive syndrome, deterioration of visual acuity, scotoma, angina pectoris, arrhythmia, tachycardia, hypotension, pain in the trachea, tickling, lack of smell, xerostomia, sudden weight loss, nausea, gag reflex, heartburn, cholestatic hepatitis, increased levels of liver enzymes, intestinal atony, allergies, leukopenia, pancytopenia, hypofibrinogenemia, thrombocytopenia.

Contraindications

Contraindications include:

The drug is used very carefully in the following cases:

• bearing a child and breast-feeding;
• advanced age;
• coronary insufficiency (acute phase of myocardial infarction);
• vascular atherosclerosis;
• renal failure.

Overdose

When the dose of the drug was significantly exceeded, the following reactions were observed:

• intestinal disorder;
• reduction or complete absence appetite;
• nausea and vomiting (possibly with blood or blood clots);
• bleeding from the gastrointestinal tract;
• anxious and restless states;
• increased physical activity, convulsions;
• fear of bright light.

In case of acute overdose, epilepsy attacks may occur. This is especially true for children. In rare cases, a lack of oxygen, loss and confusion of spatial orientation, hyperglycemia, and necrosis of skeletal muscles may occur. Low blood pressure also appears.

As a treatment, it is necessary to urgently stop the medicine and rinse the stomach. Then it is recommended to use the maximum possible dose of laxatives and activated carbon.

In the hospital, the intestines are washed with an electrolyte. If the patient suffers from vomiting, ondansetron or metoclopramide should be given intravenously.

If a convulsive syndrome occurs, it is imperative to monitor the airway and provide oxygen therapy. At the same time, 0.2 mg/kg Diazepam is injected into a vein. Its daily dose does not exceed 10 mg.

During pregnancy

During pregnancy, the drug should be used with extreme caution. The risk of taking theophylline should be much greater less danger for mother and fetus. The drug is prescribed exclusively by the attending physician and in very rare cases.

The drug is able to penetrate the placenta to the fetus and is also excreted in mother's milk.

Storage conditions and periods

The medicine should be stored at a temperature not exceeding 20 degrees in a dark place. The drug is valid for three years from the date of manufacture.

Price

average price in Russia:

• Tablets, form 100 mg 50 pieces - 80 rubles;
• Tablets 200 mg 50 pieces - 130 rubles;
• Tablets 300 mg pieces - 170 rubles.

average cost in Ukraine:

• Tablets, form 100 mg 50 pieces - 130 hryvnia;
• Tablets 200 mg 50 pieces - 183 hryvnia;
• Tablets 300 mg pieces - 250 hryvnia.

Analogs

Analogs of Theophylline are:

• neo-theophedrine;
• theobromine;
• diprophylline;
• theophedrine-N.

Dosage form:  extended release tablets Compound:

1 tablet contains:active substance:

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

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

Description: pills white with a yellowish tint, flat-cylindrical shape with a chamfer (for a dosage of 0.1 g), with a chamfer and a notch (for dosages of OD g and 0.3 g). Pharmacotherapeutic group:bronchodilator. ATX:  

R.03.D.A.04 Theophylline

Pharmacodynamics:

Antispasmodic, purine derivative: Blocks adenosine receptors and inhibits phosphodiesterase. Causes a pronounced bronchodilator effect due to a direct effect on the bronchial muscles. Stabilizes the membrane 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. Normalizing respiratory function, helps saturate the blood with oxygen and reduce the concentration of carbon dioxide; stimulates the breathing centers. Strengthens ventilation of the lungs in conditions of hypokalemia.

It has a stimulating effect on the activity of the heart, increases the strength and frequency of heart contractions, increases coronary blood flow and myocardial oxygen demand. Reduces tone blood vessels(mainly brain vessels, skin and kidneys). Reduces pulmonary vascular resistance, lowers pressure in the pulmonary circulation. Increases renal blood flow and has a moderate diuretic effect. Expands extrahepatic bile ducts.

Slow release active substance from tablets ensures the achievement of a therapeutic level of theophylline in the blood 3-5 hours after administration and its maintenance for 10-12 hours, so effective concentrations theophylline levels in the blood during the day are maintained when taking the drug 2 times a day.

Pharmacokinetics:

Absorbed quite well from the gastrointestinal tract, bioavailability is 88-100%. Time to reach maximum concentration in blood plasma is 6 hours.

Communication with plasma proteins is about 60%. Penetrates the placental barrier and is found in breast milk. Metabolized in the liver (90%) with the participation of several cytochrome P450 enzymes (the most important CYP1A2). Main metabolites: 1.3-dimethyluric acid and 3-methylxanthine.

Excretion of metabolites by the kidneys along with 7-13% of unchanged active substance. The half-life in non-smoking patients is 6-12 hours. smoking people significantly shorter - 4-5 hours. In patients with liver cirrhosis, renal failure and in patients with alcoholism, the half-life is extended. Total clearance is reduced in patients with high fever, severe respiratory failure, in patients with liver failure or chronic heart failure, with viral infections, in patients over 55 years of age.

Indications:

Broncho-obstructive syndrome of any origin: bronchial asthma (drug of choice in patients with exercise-induced asthma and as an additional remedy for other forms), chronic obstructive diseases (chronic obstructive bronchitis, pulmonary emphysema).

Pulmonary hypertension, cor pulmonale, edematous syndrome of renal origin (as part of combination therapy), sleep apnea.

Contraindications:

Hypersensitivity (including to other xanthine derivatives - caffeine, pentoxifylline, theobromine), epilepsy, peptic ulcer of the stomach and duodenum, gastritis with high acidity, bleeding from the gastrointestinal tract, severe arterial hyper- or hypotension, severe tachyarrhythmias, hemorrhagic stroke, retinal hemorrhage, childhood up to 12 years old.

Carefully:Use with caution in severe coronary insufficiency (acute phase of myocardial infarction, angina pectoris), widespread vascular atherosclerosis, hypertrophic obstructive cardiomyopathy, frequent ventricular extrasystole, chronic heart failure, increased convulsive readiness, liver and/or kidney failure, gastric ulcer and 12- duodenal ulcer (history), bleeding from the gastrointestinal tract in a recent history, uncontrolled hypothyroidism (possibility of cumulation) or thyrotoxicosis, prolonged hyperthermia, gastroesophageal reflux, prostatic hypertrophy, pregnancy, lactation, old age. Pregnancy and lactation:

During pregnancy (especially in the first trimester) it is prescribed only if the expected benefit to the mother exceeds possible risk for the fetus. Prescription of the drug during pregnancy (first trimester and last weeks) is possible only according to strict indications.

When prescribing the drug during lactation, one should take into account what is excreted in breast milk; It is not recommended to take the drug during lactation. If necessary, take the drug during lactation, the woman should stop breastfeeding.

Directions for use and dosage:

Inside, with a sufficient amount of liquid.

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

In patients weighing less than 60 kg initial single dose- 100 mg in the evening, then 100 mg 2 times a day.

Treatment begins with smaller doses, which are gradually, with an interval of 1-2 days, increased (by 100-200 mg/day) until the maximum therapeutic effect, if poorly tolerated - reduce.

The dose depends on the nature of the disease, age and body weight of the patient. If it is necessary to prescribe in large doses, treatment is carried out under the control of the concentration of theophylline in the blood (therapeutic concentration - in the range of 10-15 mcg/ml): at a concentration of 20-25 mcg/ml, it is necessary to reduce the daily dose by 10%; 25-30 mcg/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 the patient's condition stabilizes while taking high doses, it is necessary to carry out monitoring every 6-12 months.

Maintenance dose for adults weighing over 60 kg- 600 mg/day, less than 60 kg - 400 mg/day.

Forsmokerswith body weight more than 60 kg The daily dose of the drug is 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 cardiovascular diseases and liver dysfunction: with a body weight of more than 60 kg, the daily dose is 400 mg, with a body weight of less than 60 kg - 200 mg. Decrease daily dose required in patients with severe damage to the heart, liver, viral infections, and in elderly patients.

Children weighing up to 30 kg- 10-20 mg/kg/day (in 2 doses).

Side effects:

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

From the cardiovascular system:palpitations, tachycardia (including in the fetus when taken by a pregnant woman in the third trimester), arrhythmias, decreased blood pressure, cardialgia, increased frequency of angina attacks.

From the outside digestive system: gastralgia, nausea, vomiting, gastroesophageal reflux, heartburn, exacerbation of peptic ulcer, diarrhea, with long-term use - loss of appetite.

Allergic reactions: skin rash, itching, fever.

Other: chest pain, tachypnea, flushing, albuminuria, hematuria, hypoglycemia, increased diuresis, increased sweating.

Side effects decrease with decreasing dosage of the drug.

Overdose:

Symptoms:

loss of appetite, gastralgia, diarrhea, nausea, vomiting (including blood), gastrointestinal intestinal bleeding, tachypnea, facial skin flushing, tachycardia, ventricular arrhythmias, insomnia, motor agitation, anxiety, photophobia, tremor, convulsions.

In case of severe poisoning, epileptoid seizures may develop (especially in children without any warning signs), hypoxia, metabolic acidosis, hyperglycemia, hypokalemia, decreased blood pressure, necrosis skeletal muscles, confusion, renal failure with myoglobinuria.

Treatment:

drug withdrawal, gastric lavage, administration of activated charcoal, laxatives, intestinal lavage with a combination of polyethylene glycol and electrolytes, forced diuresis, hemosorption, plasma sorption, hemodialysis (low efficiency, peritoneal dialysis is ineffective), symptomatic therapy (including vomiting).

If convulsions occur, maintain airway patency and administer oxygen therapy. To stop a seizure - intravenously, 0.1-0.3 mg/kg (no more than 10 mg). At severe nausea and vomiting - or (intravenously).

Interaction:

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

Antidiarrheal drugs and enterosorbents reduce the absorption of theophylline. , sulfinpyrazone, oral estrogen-containing contraceptives and moracizine, being 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 antibiotics, lincomycin, allopurinol, cimetidine, fluoroquinolones), isoprenaline, enoxacin, disulfiram, recombinant interferon alpha, methotrexate, mexiletine, propafenone, thiabendazole, ticlopidine, verapamil and with influenza vaccination, the potency of theophylline may increase and require a reduction in its dose.

Strengthens the effect of beta-agonists and diuretics (by increasing glomerular filtration), reduces the effectiveness of lithium drugs and beta-blockers. Compatible with antispasmodics, do not use in combination with other xanthine derivatives.

Prescribe with caution simultaneously with anticoagulants.

Special instructions:

At serious illnesses cardiovascular system, liver, viral infections, as well as in elderly patients, the dose of the drug should be reduced. The effect of theophylline may be reduced in patients who smoke.

If it is necessary to use theophylline during lactation, it is recommended to stop breastfeeding, since the drug passes into breast milk. If used at the end of pregnancy, tachycardia in the fetus is possible.

The drug is not intended for relief emergency conditions. Treatment with prolonged forms is carried out with periodic monitoring of theophylline concentration in the blood. If asthma is well controlled and there are no side effects or factors that may alter dosage requirements, theophylline concentrations are measured at 6-12 month intervals.

Use caution when consuming large amounts of caffeine-containing foods or drinks during treatment.

Impact on the ability to drive vehicles. Wed and fur.: Release form/dosage:

Extended-release tablets 100 mg, 200 mg and 300 mg.

10 tablets in a blister pack made of polyvinyl chloride film and printed varnished aluminum foil.

5 blister packs along with instructions for use are placed in a cardboard pack. Package: (10) - contour cell packaging (2) - cardboard packs

(10) - contour cell packaging (3) - cardboard packs

(10) - contour cell packaging (5) - cardboard packs

(20) - polymer cans (1) - cardboard packs

(30) - polymer cans (1) - cardboard packs

(50) - polymer cans (1) - cardboard packs

Storage conditions:List B. In a dry place, protected from light, at a temperature not exceeding 25 ° C. Keep out of the reach of children. Best before date:

3 years. Do not use after expiration date.

Conditions for dispensing from pharmacies: On prescription Registration number: LSR-001948/09 Registration date: 16.03.2009 Owner of the Registration Certificate: VALENTA FARM, JSC Russia Manufacturer:   Information update date:   17.09.2015 Illustrated instructions