Teopek - instructions for use. Theophylline use and possible contraindications Presence of side effects

Gross formula

Pharmacological group of the substance Theophylline

Nosological classification (ICD-10)

CAS code

Characteristics of the substance Theophylline

White crystalline powder, slightly soluble in cold water (1:180), easily hot (1:85), soluble in acids and alkalis. Molecular weight 180.17.

Pharmacology

Binds to adenosine receptors. It also blocks phosphodiesterase, stabilizes cAMP and reduces the concentration of intracellular calcium. It relaxes the smooth muscles of the internal organs (bronchus, gastrointestinal tract and uterus), inhibits the degranulation of mast cells and reduces the level of allergy mediators (serotonin, histamine, etc.) in the blood (anti-allergic effect). Increases the tone of the respiratory muscles (intercostal muscles and diaphragm); dilates the vessels of the lungs and improves blood oxygenation; inhibits platelet aggregation (inhibits platelet activating factor and PGF 2alpha), increases the resistance of erythrocytes to deformation (improves the rheological properties of blood), reduces thrombosis and normalizes microcirculation. The antianginal effect (increase in oxygen delivery to the myocardium) is due to the expansion of the coronary arteries.

After oral administration, it is completely absorbed (bioavailability over 90%). Cmax in the blood is achieved within 2 hours (normal form) and 6 hours (prolonged form). In the blood, 40-60% is associated with proteins. Penetrates through histohematic barriers. Undergoes biotransformation in the liver with the formation of inactive metabolites. It is excreted mainly by the kidneys (up to 13% in adults and up to 50% in children - unchanged); partially excreted in breast milk.

The use of theophylline

Bronchial asthma, status asthmaticus, obstructive bronchitis, pulmonary emphysema, sleep apnea.

Contraindications

Hypersensitivity, incl. to other xanthine derivatives (caffeine, pentoxifylline, theobromine), hemorrhagic stroke, retinal hemorrhage, acute myocardial infarction, severe atherosclerosis of the coronary arteries, bleeding in a recent history.

Use during pregnancy and lactation

Side effects of theophylline substance

Anxiety, impaired consciousness, convulsions, visual disturbances, scotoma, angina attacks, arrhythmias, tachycardia, hypotension, laryngitis, sore throat, flu-like syndrome, nasal congestion, xerostomia, anorexia, nausea, vomiting, heartburn, exacerbation of cholecystitis, cholestatic hepatitis, increased concentrations of liver enzymes (AST, ALT, alkaline phosphatase, LDH), intestinal atony, leukopenia, hypofibrinogenemia, pancytopenia, thrombocytopenia, allergic reactions.

Interaction

Cimetidine, allopurinol, cyclosporine A, macrolide antibiotics, oral contraceptives, anti-influenza serum, a diet low in protein and high in carbohydrates - reduce clearance and increase the risk of side effects.

Phenobarbital, phenytoin, xanthines, smoking - accelerate biotransformation (induce microsomal liver enzymes). Beta-blockers reduce bronchodilator activity. Adsorbents, enveloping agents, antacids, oxidizing agents slow down absorption and reduce Cmax, while alkalizing substances increase it. Enhances the effects of diuretics, reduces - NSAIDs (from the group of pyrazolone derivatives), beta-blockers, probenecid.

Overdose

Symptoms: agitation, confusion, convulsions, tachycardia, arrhythmia, hypotension, nausea, diarrhea, bloody vomiting, hyperglycemia, hypokalemia, metabolic acidosis.

Treatment: the appointment of activated charcoal, irrigation of the intestines with a combination of polyethylene glycol and salts; with severe nausea and vomiting - metoclopramide or ondansetron (in / in), convulsions - benzodiazepines, phenobarbital (or sodium thiopental) and peripheral muscle relaxants; if necessary - hemoperfusion.

Routes of administration

inside.

Theophylline Substance Precautions

Treatment with retard forms is carried out with periodic monitoring of the concentration of the drug in the blood (should not exceed 20 μg / ml).

Interactions with other active substances

Trade names

pharmachologic effect

Indications for use

Mode of application

Side effects

Contraindications

Release form

Storage conditions

Active substance:

Additionally

The authors

Links

• The official instructions for the drug Theophylline.
• Modern drugs: a complete practical guide. Moscow, 2000. S. A. Kryzhanovsky, M. B. Vititnova.

Instructions for medical use

medicinal product

Theophylline

Tradename

Theophylline

International non-proprietary name

Dosage form

Extended release capsules 350 mg

Compound

One capsule contains

active substance- theophylline pellet 500.0 mg

(equivalent to theophylline 350.0 mg),

Excipients: talc,

composition of gelatin capsules: gelatin, titanium dioxide (E 171).

Description

Hard gelatin capsules: white body and cap. Capsule size #0. The contents of the capsules are white or almost white pellets.

Pharmacotherapistscal group

Drugs for the treatment of obstructive respiratory diseases.

Other drugs for the treatment of obstructive airways disease for systemic use. Xanthines. Theophylline

ATX code R03DA04

Pharmacological properties

Pharmacokinetics

When taken orally, theophylline is rapidly and completely absorbed from the gastrointestinal tract.

The maximum concentration in the blood plasma after taking the drug inside is reached after 4-8 hours. The bioavailability of theophylline is approximately 90%. Plasma protein binding - 60%, in patients with liver disease - 20-40%. Theophylline moderately penetrates into tissues, the volume of distribution is about 0.5 l / kg.

It penetrates well through the blood-brain barrier, the placenta and into breast milk.

The duration of maintaining the therapeutic concentration in the blood after a single dose of the drug ranges from 4 to 5 hours.

Theophylline is metabolized in the liver with the participation of microsomal enzymes. In the process of metabolism, 1,3-dimethyluric acid, 1-methyluric acid and 3-methylxanthine are formed. These metabolites are excreted in the urine. In unchanged form, 10% of theophylline is excreted in adults.

The elimination half-life averages 6-12 hours.

Theophylline clearance is reduced in the elderly, patients with impaired liver function, heart failure.

Pharmacodynamics

The mechanism of action of the drug is to block the phosphodiesterase enzyme, which leads to increased accumulation of cAMP, blocking adenosine receptors, stimulating the synthesis of endogenous catecholamines, inhibiting intracellular calcium release, which leads to a decrease in 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 vasodilatory effect, increases renal blood flow, has a moderately pronounced diuretic effect.

Theophylline, expanding the pulmonary vessels, reduces pressure in the pulmonary circulation (reduces transient hypertension in the pulmonary circulation during an attack of bronchial asthma), improves the pumping function of the right and left ventricles of the heart.

Stabilizes the mast cell membrane, inhibits the release of inflammatory mediators, increases mucociliary clearance.

It has a stimulating effect on the respiratory center, which leads to increased ventilation of the lungs by increasing the contractility of the intercostal muscles and the diaphragm.

Indications for use

- broncho-obstructive syndrome in bronchial asthma, chronic obstructive bronchitis, emphysema

- pulmonary hypertension in chronic cor pulmonale

Dosage and administration

The drug is taken orally with a sufficient amount of liquid.

Capsules should be swallowed whole, without opening or chewing.

The dosage regimen is set individually by the attending physician.

Initial daily dose for adults and children over 12 years of age weighing more than 45 kg is 350 mg (1 capsule 1 time per day). The daily dose can be increased after 3 days to 700 mg (1 capsule 2 times a day) with good tolerability of the drug. The maximum daily dose should not exceed 13 mg/kg.

In patients weighing less than 45 kg the daily dose of the drug is 10 mg / kg.

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 blood serum from 10 to 15 μg / ml provides a therapeutic effect with a minimal risk of side effects. If the concentration exceeds 20 mcg / ml, then the dose of the drug should be reduced.

The effect of the drug is fully manifested 3-4 days after the start of treatment.

Side effects

- heartburn, nausea, vomiting, epigastric pain, diarrhea, gastroesophageal

reflux, exacerbation of peptic ulcer of the stomach and duodenum in

patients suffering from this disease

- headache, dizziness, agitation, insomnia, anxiety, irritability

- hand tremor, convulsions

- sinus tachycardia, arrhythmias, arterial hypotension

- chest pain, increased frequency of angina attacks in patients with coronary heart disease

• increased diuresis (especially in children)
• hypokalemia, hypoglycemia
• allergic reactions, skin rash, itching, hyperthermia

Contraindications

• hypersensitivity to theophylline and other xanthine derivatives or other components of the drug
• co-administration with ephedrine in children
• porphyria
• epilepsy and other convulsive conditions
• myocardial infarction in the acute and subacute period, cardiac arrhythmias
• hemorrhagic stroke, retinal hemorrhage
• severe arterial hyper- and hypotension
• peptic ulcer of the stomach and duodenum in the acute stage
• pregnancy and lactation
• children's age up to 12 years

Drug Interactions

Theophylline potentiates the bronchodilator action of beta 2-agonists, which allows the use of the latter in smaller doses.

Theophylline increases the clearance of lithium and pyridoxine when co-administered, so their effectiveness is reduced at a constant concentration of the drug in the blood plasma.

The concentration of theophylline in the blood may decrease with simultaneous use with phenobarbital, rifampicin, carbamazepine, sulfinpyrazone, phenytoin, ritonavir, primidone, St. John's wort, as well as in smokers.

Plasma concentrations of theophylline may be reduced while taking St. John's wort.

Theophylline concentration in the blood may increase when used simultaneously with antibiotics from the macrolide group, allopurinol, beta-blockers, cimetidine, hormonal oral contraceptives, isoprenaline, lincomycin, ciprofloxacin, norfloxacin, diltiazem, verapamil, furosemide, isoniazid, fluconazole, mexiletine, di, profexiletine , interferon-alpha, corticosteroids.

When taken simultaneously with ketamine, a decrease in the convulsive threshold is possible, with doxapram - increased stimulation of the central nervous system, with beta-blockers - a decrease in the bronchodilating effect.

Theophylline can potentiate hypokalemia due to the action of β 2 -adrenergic stimulants, corticosteroids and diuretics.

The drug should not be used together with drugs containing xanthine derivatives (caffeine, theobromine, pentoxifylline), fluvoxamine.

special instructions

This dosage form is not intended for the relief of emergency conditions.

Treatment is carried out with periodic monitoring of theophylline concentration in the blood.

Theophylline should be used with caution in patients with severe coronary insufficiency (angina pectoris), widespread vascular atherosclerosis, due to a possible increase in angina attacks, the appearance of cardialgia, chronic heart failure, liver and / or kidney failure, chronic alcoholism, peptic ulcer of the stomach and duodenum (possible exacerbation), gastritis with high acidity, hyperthyroidism (due to the possibility of cumulation), hyperthermia, prostatic hypertrophy, urinary tract obstruction due to the possibility of urinary retention.

The half-life of theophylline may be prolonged in the elderly and in patients with heart failure, hepatic impairment, or viral infection. Toxic cumulation may develop, and therefore a dose reduction is necessary in elderly patients.

Application in pediatrics

Pregnancy and lactation

Theophylline penetrates the placental barrier, excreted in breast milk.

During pregnancy theophylline used only if the expected benefit to the mother outweighs the possible risk to the fetus.

If it is necessary to prescribe the drug during lactation, it is recommended to stop breastfeeding.

Features of the influence of the drug on the ability to drive a vehicle or potentially dangerous mechanisms

Care should be taken when driving vehicles and working with potentially dangerous mechanisms, taking into account the possibility of developing dizziness.

Overdose

Symptoms: nausea, vomiting, epigastric pain, anxiety, hand tremor, convulsions, psychomotor agitation, sinus tachycardia, supraventricular and ventricular extrasystole, lowering blood pressure, hypokalemia, hyperglycemia, hypomagnesemia, metabolic acidosis, rhabdomyolysis, renal failure with myoglobinuria.

Treatment: drug withdrawal, gastric lavage, activated charcoal, laxatives, elimination of electrolyte imbalance, symptomatic therapy (for vomiting - metoclopramide, ondansetron, for the relief of seizures - intravenous diazepam 0.1-0.3 mg / kg).

Release form and packaging

10 capsules in a blister pack made of PVC or imported film, and aluminum or imported foil.

4 blister packs, together with the approved instructions for medical use in the state and Russian languages, are placed in a pack of cardboard for consumer packaging or chrome-ersatz.

It is allowed to apply information from the instructions for medical use in the state and Russian languages ​​to the pack.

Packs are placed in boxes made of boxed or corrugated cardboard.

Storage conditions

Store in a dry, dark place at a temperature not exceeding 25ºС.

Keep out of the reach of children!

Shelf life

Do not use the drug after the expiration date.

Terms of dispensing from pharmacies

On prescription

Manufacturer

Chimpharm JSC, Republic of Kazakhstan,

Shymkent, st. Rashidova, b / n, tel / f: 560882

Registration certificate holder

Chimpharm JSC, Republic of Kazakhstan

Address of the organization hosting on the territory of the Republic of Kazakhstan claims from consumers on the quality of products (goods)

JSC "Khimfarm", Shymkent, REPUBLIC OF KAZAKHSTAN,

st. Rashidova, b / n, tel / f: 560882

Phone number 7252 (561342)

Fax number 7252 (561342)

E-mail address [email protected]

THEOPHIL® SR 200 THEOPHIL® SR 300

International non-proprietary name

Dosage form

Extended release capsules 200 mg, 300 mg

Compound

One capsule contains

active substance - theophylline micropellets 273.96 mg and 410.94 mg (equivalent to 200 mg and 300 mg theophylline, respectively),

composition of the capsule shell: capsule body - gelatin, cap of the capsule indigo carmine FD&C blue 2 (E 132) and gelatin (for THEOPHIL ® CP 200); patent blue V (E 131), quinoline yellow and gelatin (E 104) (for THEOPHIL ® SR 300).

Description

Size "2" hard gelatin capsules with a transparent, colorless body and a dark blue transparent cap. ® SR 200).

Size "1" hard gelatin capsules with a transparent, colorless body and a transparent green cap. The contents of the capsule are whitish spherical micropellets. (for THEOPHIL ® SR 300).

Pharmacotherapistscal group

Other drugs for the treatment of obstructive airways disease for systemic use. Xanthines.

ATX code R03DA04

Pharmacological properties

Pharmacokinetics

When taken orally, theophylline is rapidly and completely absorbed from the gastrointestinal tract. The presence of food in the stomach can affect the rate of absorption of theophylline, as well as its clearance.

The maximum concentration in plasma after oral administration is reached after 6-9 hours. Plasma protein binding is 60%, in people with liver disease - 20-40%. Theophylline moderately penetrates into tissues, the volume of distribution is about 0.5 l / kg. However, it penetrates well through the blood-brain barrier, the placenta and into breast milk.

Theophylline is metabolized in the liver by 90%. The elimination half-life of theophylline in non-smoking patients with bronchial asthma and without pathological changes in other organs and systems is 6-12 hours, in smokers - 4-5 hours. The elimination half-life is increased in elderly patients and in patients with heart failure and liver disease. The half-life of the drug for children is 1.5 hours. Mainly excreted in the urine. The duration of maintaining a therapeutic concentration in the blood ranges from 4 to 5 hours.

Pharmacodynamics

Theophylline inhibits the activity of specific phosphodiesterases (PDE), stabilizes the intracellular concentration of cyclic adenosine monophosphate (cAMP). Theophylline blocks adenosine receptors and relaxes the smooth muscles of the bronchi and blood vessels of the lungs.

Theophylline stimulates the respiratory center of the medulla oblongata, increasing sensitivity to the stimulating effects of carbon dioxide.

Theophylline may reduce airway hyperreactivity associated with the late phase reaction caused by inhaled allergens.

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

Theophylline also dilates peripheral, coronary and renal vessels, has a moderate diuretic effect, inhibits platelet aggregation, and inhibits the release of allergy mediators from mast cells. Theophylline has a stimulating effect on the heart muscle and on the central nervous system, causes vasoconstriction of the brain, increases the contractility of the diaphragm, reduces the total peripheral vascular resistance, incl. resistance of the pulmonary vessels, causes an increase in the secretion of acid in the stomach.

Indications for use

• bronchial asthma
• symptomatic treatment of bronchospasm of various etiologies (including chronic obstructive pulmonary disease, chronic bronchitis, pulmonary emphysema)
• pulmonary hypertension
• cor pulmonale
• nocturnal paroxysmal apnea

Dosage and administration

The drug is taken orally with a sufficient amount of liquid. The dosing regimen is set individually. Capsules should be swallowed whole, without opening or chewing.

The maximum daily dose in adults is 15 mg/kg.

For non-smoking adults with a body weight of 60 kg and above, the initial dose is 200 mg per day, then 200 mg 2 times a day. In patients weighing less than 60 kg, the initial single dose is 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 is obtained, with poor tolerance - reduced. 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 theophylline concentration in the blood (therapeutic concentration - in the range of 10-15 μg / ml): at a concentration of 20-25 μg / 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. Re-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 monitor every 6-12 months.

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

For smokers weighing over 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 impaired liver function: 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. Reducing the daily dose is required in patients with severe lesions of the heart, liver, with viral infections, in elderly patients.

Side effects

• heartburn, nausea, vomiting, exacerbation of peptic ulcer, epigastric pain, diarrhea, with prolonged use - loss of appetite
• headache, dizziness, irritability, anxiety, restlessness, insomnia, increased reflex excitability, clonic and tonic convulsions, tremor
• palpitations, tachycardia, arrhythmia, extrasystole, flushing, hypotension, circulatory disorders, ventricular arrhythmia, increased frequency of angina attacks, pain in the heart
• tachypnea

increased diuresis, hematuria, albuminuria

alopecia

hypoglycemia, hypokalemia;

skin itching, rash

Contraindications

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

epilepsy and other convulsive conditions

hyperthyroidism

acute myocardial infarction

subaortic stenosis

extrasystole, severe tachyarrhythmias, severe arterial hyper- or hypotension

hemorrhagic stroke

gastritis with high acidity, bleeding from the gastrointestinal tract in a recent history

peptic ulcer of the stomach and duodenum in the acute phase

retinal hemorrhage

children and adolescents up to 18 years of age

pregnancy

Drug Interactions

Theophylline potentiates the bronchodilator action of beta2-agonists, which allows the use of the latter in smaller doses. Theophylline increases the clearance of lithium and pyridoxine when co-administered, so their effectiveness is reduced at a constant concentration of the drug in the blood plasma. The concentration of theophylline in the blood decreases with simultaneous use with phenobarbital, rifampicin, isoniazid, carbamazepine, sulfinpyrazone, phenytoin, and also in smokers. The concentration of theophylline in the blood increases with simultaneous use with macrolide antibiotics, allopurinol, beta-blockers, cimetidine, hormonal oral contraceptives, isoprenaline, lincomycin.

Theophylline can potentiate hypokalemia due to the action of β2-adrenergic stimulants, corticosteroids and diuretics.

special instructions

Extended release tablets are not intended for emergency management. Treatment with prolonged forms is carried out with periodic monitoring of theophylline concentration in the blood.

Theophylline should be used with caution in patients with: severe coronary insufficiency (angina pectoris), widespread vascular atherosclerosis, hypertrophic obstructive cardiomyopathy, frequent ventricular extrasystole, CHF, liver and / or kidney failure, gastric ulcer and 12 duodenal ulcer (history), uncontrolled hypothyroidism (possibility of cumulation), prolonged hyperthermia, prostatic hypertrophy.

The drug should not be used together with drugs containing xanthine derivatives (caffeine, theobromine, pentoxifylline).

lactation period

It should be borne in mind that theophylline is excreted in breast milk. If it is necessary to prescribe the drug during lactation, the question of stopping breastfeeding is raised.

Features of the influence of the drug on the ability to drive a vehicle or potentially dangerous mechanisms

In connection with undesirable effects on the central nervous system, theophylline should be used with caution.

Overdose

Symptoms: loss of appetite, gastralgia, diarrhea, nausea, vomiting (including with blood), gastrointestinal bleeding, tachypnea, flushing of the skin of the face, tachycardia, ventricular arrhythmia, insomnia, motor agitation, anxiety, photophobia, tremor, convulsions. In severe poisoning, epileptoid seizures, hypoxia, metabolic acidosis, hyperglycemia, hypokalemia, lowering blood pressure, skeletal muscle necrosis, confusion, renal failure with myoglobinuria may develop.

Treatment: discontinuation of the drug, gastric lavage, the appointment of activated charcoal, laxatives, forced diuresis, hemosorption, plasma sorption, symptomatic therapy (including metoclopramide and ondansetron - with vomiting). For the relief of a seizure - in / in diazepam, 0.1-0.3 mg / kg (but not more than 10 mg). For severe nausea and vomiting, metoclopramide or ondansetron (iv).

Release form and packaging

10 capsules are placed in a blister pack made of polyvinyl chloride film and printed aluminum foil.

3 contour packs, together with instructions for medical use in the state and Russian languages, are placed in a cardboard pack with a hologram of the manufacturer.

Storage conditions

Store at a temperature not exceeding 25 ºС, in a dry, dark place.

Keep out of the reach of children!

Shelf life

Do not use after the expiry date stated on the packaging.

Terms of dispensing from pharmacies

On prescription

Manufacturer

The Republic of Kazakhstan,

Almaty, st. Shevchenko 162 E.

Registration certificate holder

JSC "Nobel Almaty Pharmaceutical Factory"

The Republic of Kazakhstan

Address of the organization that accepts claims from consumers on the quality of products (goods) on the territory of the Republic of Kazakhstan:

JSC Nobel Almaty Pharmaceutical Factory»

Theophylline is a phosphodiesterase inhibitor; bronchodilator.

Release form and composition

Dosage form of Theophylline - prolonged-release tablets (10 pcs in blisters, in a carton pack of 2, 3 or 5 packs; 20, 30 or 50 pcs in polymer cans, in a carton pack of 1 can).

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

Indications for use

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

Contraindications

Theophylline is contraindicated in the following conditions/diseases:

• Hemorrhage in the retina;
• hemorrhagic stroke;
• Epilepsy;
• Severe tachyarrhythmias;
• Severe arterial hypo- and hypertension;
• Bleeding from the gastrointestinal tract in a recent history;
• Gastritis with high acidity;
• Exacerbation of peptic ulcer of the stomach and duodenum;
• Children's age up to 12 years;
• 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 such cases:

• Childhood and old age;
• Severe coronary insufficiency (angina pectoris and acute phase of myocardial infarction);
• Hypertrophic obstructive cardiomyopathy;
• Widespread vascular atherosclerosis;
• Liver and / or renal failure;
• Increased convulsive readiness;
• Uncontrolled hypothyroidism and thyrotoxicosis;
• Chronic heart failure;
• Ventricular extrasystole;
• Prolonged hyperthermia;
• prostatic hypertrophy;
• Gastroesophageal reflux;
• Peptic ulcer of the stomach and 12 duodenal ulcer in history.

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

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

Method of application and dosage

Theophylline is taken orally, washed down with water and not chewed, after a meal. The dose for each patient is determined individually.

The initial dose is usually 400 mg per day. In the case of good tolerance, every 2-3 days it is increased by about 25% of the initial one until the optimal therapeutic effect is achieved.

Without monitoring the concentration of theophylline in 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 a toxic effect appear or there is a need for a further increase in the dose due to an 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, at a higher concentration, a significant increase in the action is not observed, but the risk of side effects increases significantly.

For the elderly, patients with viral infections and diseases of the cardiovascular system, the dose of Theophylline 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: lowering blood pressure, cardialgia, palpitations, an increase in the frequency of angina attacks, arrhythmias, and 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;
• Others: increased diuresis, hematuria, albuminuria, hypoglycemia, flushing, chest pain, increased sweating, tachypnea.

The severity of side effects decreases after the dose of Theophylline is reduced.

special instructions

The intensity of the therapeutic effect of the drug in smoking patients may decrease.

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

drug interaction

Influence on theophylline in case of simultaneous use of other drugs:

• Propranolol, cimetidine, allopurinol, isoprenaline, lincomycin, macrolide antibiotics, oral contraceptives reduce the clearance of theophylline;
• Beta-blockers, especially non-selective ones, reduce the bronchodilating effect of theophylline due to bronchial constriction;
• Furosemide, caffeine, beta2-adrenergic stimulants enhance the effect of theophylline;
• Aminoglutethimide increases the excretion of theophylline from the body, which reduces its effectiveness;
• Acyclovir, verapamil, nifedipine, disulfiram increase the concentration of theophylline, increase 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 the concentration of theophylline in plasma.

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 result, a decrease in therapeutic efficacy.

Terms and conditions of storage

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

Shelf life - 5 years.