Chronic obstructive seizure of a leg, bronchial asthma, emphysema legen, central apnea syndrome. Achievements for systemic stasis in obstructive ganglions of dichal grooms.
active substance: theophylline
1 prolonged-release tablet contains theophylline 300 mg;
auxiliary substances: methacrylate copolymer dispersion, polyacrylate dispersion, microcrystalline cellulose, talc, magnesium stearate.
Dosage form. Extended-release tablets.
Basic physical and chemical properties: round tablets of regular shape, 10 mm in diameter, chamfered and notched on one side, white.
Theophylline’s mechanism of action includes:
- inhibition of the enzyme phosphodiesterase, causing an increase in cAMP levels;
- antagonism towards adenosine receptors;
- inhibition of intracellular calcium release;
- stimulating the release of catecholamines;
- anti-inflammatory effect, which is achieved by inhibiting the activity of T-lymphocytes, eosinophils and neutrophils.
Theophylline has two distinct effects on the airways in patients with reversible obstructive disease: relaxes smooth muscle (bronchodilation) and inhibits airway response to stimulation (non-bronchodilating anti-inflammatory prophylactic effect).
Symptomatic treatment and prevention of bronchial asthma, chronic bronchitis and pulmonary emphysema.
Hypersensitivity to theophylline, other xanthine derivatives (caffeine, pentoxifylline, theobromine) or to any of the excipients; epilepsy; glaucoma; porphyria; the simultaneous use of theophylline and ephedrine in children; acute period of myocardial infarction, acute cardiac arrhythmias (acute tachyarrhythmia), severe arterial hypertension, hyperthyroidism, gastric ulcer and duodenal ulcer in the acute stage, severe liver dysfunction.
Application during pregnancy or lactation
Pregnancy. Theophylline crosses the placental barrier. There are no adequate data from well-controlled studies of pregnant women. It is not recommended to prescribe the drug during pregnancy because its safety has not been proven.
The use of the drug during pregnancy is possible only if there are strict medical indications, careful calculation of the dose and monitoring the condition of the mother and fetus, since theophylline at the end of pregnancy can inhibit uterine contraction.
Lactation. Theophylline passes into breast milk and may cause increased irritability in the newborn. Its use by nursing mothers is allowed only if the intended benefit to the mother outweighs the risk to the newborn.
The ability to influence the reaction rate when driving vehicles or other mechanisms.
Some adverse reactions (for example, dizziness) can affect the ability to drive vehicles and operate machinery. Patients should be advised not to drive or operate hazardous mechanical equipment until they are satisfied that they are responding normally to treatment.
Method of administration and dosage
The drug should be taken orally 30-60 minutes before meals or 2 hours after meals with plenty of liquid. A 300 mg tablet can be halved, but cannot be crushed, chewed, or dissolved in water. In some cases, in order to reduce the irritating effect on the gastric mucosa, the drug must be taken during or immediately after a meal.
The dosage regimen is set individually, depending on the age, body weight of the patient and the characteristics of metabolism.
Adults and children over 12 years old weighing more than 45 kg.
The initial daily dose is 300 mg divided into 2 doses (with an interval of 12 hours) After 3 days, in the absence of serious adverse reactions, the dose can be increased to 600 mg per day, also divided into 2 doses (1 tablet of 300 mg 2 times a day)
Increasing doses is possible only if well tolerated.
Elderly patients with cardiovascular diseases and / or impaired liver and kidney function.
The recommended daily dose of the drug is 8 mg / kg body weight.
The maximum therapeutic effect begins to appear on the 3-4th day after the start of treatment.
Further dose increases are recommended based on the determination of the concentration of theophylline in the blood serum.
The dosage should be selected individually, but usually the tablets are taken 2 times a day. In patients with the most severe clinical symptoms, higher morning or evening doses are appropriate.
For patients whose symptoms persist at night or during the day, regardless of other therapy, or if they have not received theophylline, their therapy may be supplemented with the recommended one-time morning or evening daily dose of theophylline.
The drug should not be used to treat children under 12 years of age.
Severe intoxication can be caused by the use of a dose of more than 3 g in adults (40 mg / kg in children). The lethal dose can be at least 4.5 g in adults (60 mg / kg in children), but it is generally higher.
Symptoms: Severe symptoms may develop 12 hours after an overdose of sustained-release dosage forms.
Gastrointestinal symptoms: nausea, vomiting (often severe), diarrhea, epigastric pain and hematemesis. If the abdominal pain continues, it could be pancreatitis.
Neurological symptoms: anxiety, tremors, muscle hypertension, increased limb reflexes and convulsions, delirium. Coma can develop in very severe cases.
Symptoms from the cardiovascular system: sinus tachycardia is a common reaction, ectopic rhythm, supraventricular and ventricular tachycardia, a sharp decrease in blood pressure, arterial hypotension.
Symptoms of metabolic disorders: hypokalemia (due to the transfer of potassium from plasma to cells), which can develop rapidly and in severe form. Hyperglycemia, hypomagnesemia, metabolic acidosis, and rhabdomyolysis may occur.
Treatment: Activated charcoal or gastric lavage is appropriate for significant overdose within 1–2 hours after application. Multiple doses of orally administered activated charcoal can help eliminate theophylline. Plasma potassium concentration is urgently and repeatedly measured, hypokalemia is corrected. If large amounts of potassium are used, hyperkalemia may develop during recovery. If the plasma potassium level is low, the plasma magnesium concentration should be measured as soon as possible.
When treating ventricular arrhythmias, antiarrhythmic drugs with anticonvulsant effects, such as lidocaine, should be avoided due to the risk of exacerbation of seizures.
In severe poisoning, plasma concentrations of theophylline are measured regularly until the values return to normal. Antiemetics such as metoclopramide or ondansetron should be used to stop vomiting.
In case of tachycardia with adequate cardiac output, it is better not to apply treatment. Beta blockers can be prescribed as a last resort, but not if the patient has asthma. Isolated seizures can be controlled by intravenous diazepam. It is necessary to exclude the presence of hypokalemia.
- Adverse reactions are usually observed with plasma theophylline concentrations> 20 μg / ml. In most cases, they disappear with the use of lower doses.
- Based on the long-term use of theophylline, the following side effects are described, presented by systemic organ classes:
- From the immune system: hypersensitivity, anaphylactic and anaphylactoid reactions.
- From the side of metabolism and nutrition: hyperuricemia, hypokalemia and / or hypercalcemia, hyperglycemia, metabolic acidosis, rhabdomyolysis.
- Mental disorders: agitation, insomnia, especially in children; anxiety, delirium.
- From the nervous system: headache, tremors, confusion, convulsions, irritability, dizziness, sleep disturbances.
- From the gastrointestinal tract: abdominal pain, stomach irritation, gastroesophageal reflux, nausea, vomiting, anorexia, occasional diarrhea, stimulation of gastric acid secretion.
- From the heart: palpitation, arrhythmia, tachycardia.
- From the side of the vessels: lowering blood pressure.
- From the side of the kidneys and urinary tract: increased urine output, especially in children, urinary retention in elderly men.
- Skin and subcutaneous tissue disorders: itching, rash, urticaria, exfoliative dermatitis.
- General disorders: fever, fever, weakness.
The observed adverse reactions in most cases depend on the dose and can be avoided through accurate calculation and individualization of the dosage.
Keep out of the reach of children.
Store in its original packaging (in a dry, dark place) at a temperature not exceeding 25 ° C.