Theopec, 200 mg 50 pcs.

Theophylline refers to phosphodiesterase inhibitors. It increases accumulation of c-AMP in tissues, which reduces the contractile activity of smooth muscles.

Theophylline dilates bronchi, blood vessels (mainly brain, skin and kidney vessels). It reduces pulmonary vascular resistance, lowers pressure in the small circle of the circulation. Increases renal blood flow. It has a moderately pronounced diuretic effect. It inhibits platelet aggregation.

It has a stimulating effect on the respiratory center, increases the frequency and strength of heart contractions. Delayed release of the active ingredient from the tablet ensures that the therapeutic level of theophylline in the blood reaches 3-5 hours after taking Theopec and persists for 10-12 hours.

Twice administration of the drug allows obtaining effective concentrations of theophylline in blood within 24 hours. Because of the long-term action of the drug, one of the important indications for use is to prevent nocturnal and pre-morning bronchospasm phenomena.

Pharmacokinetics

After oral administration, theophylline is completely absorbed (90% bioavailability). In blood 40-60% bound to proteins. It penetrates through histohematic barriers. It is bioreformed in liver with formation of inactive metabolites. It is excreted from the body mainly by the kidneys, partially with breast milk.

Indications

Chronic Obstructive Pulmonary Disease, Cough, Bronchospasm, Bronchitis, Bronchial Asthma

Treatment and prevention of bronchoobstructive syndrome in bronchial asthma, chronic obstructive bronchitis, pulmonary emphysema, dermatorespiratory syndrome and other respiratory diseases.

Active ingredient

Theophylline

Composition

Active ingredient:

Theophylline 200 mg.

How to take, the dosage

It is set individually. The initial dose is on average 400 mg/day. If well tolerated, the dose can be increased by approximately 25% of the initial dose every 2-3 days until optimal therapeutic effect is achieved.

The maximum doses that can be used without monitoring plasma theophylline concentrations are: children aged 3-9 years – 24 mg/kg/day, 9-12 years – 20 mg/kg/day, 12-16 years – 18 mg/kg/day; patients aged 16 years and older – 13 mg/kg/day or 900 mg/day.

If symptoms of toxic effect occur during use in the indicated doses or if there is a need for further dose increase (due to insufficient therapeutic effect), it is recommended to monitor plasma theophylline concentration. Optimal therapeutic concentrations of theophylline are 10-20 µg/ml.

In lower concentrations the therapeutic effect is poorly expressed, in high concentrations no significant enhancement of the therapeutic effect is noted, while the risk of side effects increases significantly. The frequency of administration depends on the dosage form.

Interaction

Concomitant use with antibiotics of the macrolide group, allopurinol, cimetidine, oral contraceptives, isoprenaline, lincomycin decreases clearance of theophylline.

In concomitant use beta-adrenoblockers, especially non-selective, may cause bronchoconstriction, which reduces the bronchodilator effect of theophylline. The effectiveness of beta-adrenoblockers may be reduced.

Theophylline action is enhanced with concomitant use of β₂-adrenoreceptor stimulants, caffeine, furosemide.

Concomitant use with aminoglutethimide may decrease the effectiveness of theophylline due to increased excretion.

Concomitant use with acyclovir may increase the plasma concentration of theophylline and increase adverse reactions.

Concomitant use with verapamil, diltiazem, nifedipine, felodipine usually slightly or moderately changes the plasma concentration of theophylline with no changes in bronchodilator action. There have been described cases of increased plasma concentration of theophylline and increased adverse effects in patients receiving verapamil or nifedipine concomitantly.

Concomitant use of disulfiram increases plasma concentration of theophylline and develops toxic reactions.

The concomitant use of lithium salts may decrease their effectiveness.

Concomitant use with propranolol decreases clearance of theophylline.

Concomitant use with phenytoin decreases plasma concentrations of theophylline and phenytoin and decreases their therapeutic effectiveness.

Concomitant use with phenobarbital, rifampicin, isoniazid, carbamazepine, sulfinpyrazone may decrease the intensity of action of theophylline due to its increased clearance.

Concomitant use with enoxacin or other fluoroquinolones may significantly increase plasma concentrations of theophylline.

Special Instructions

In severe diseases of the cardiovascular system, liver, viral infections, as well as in elderly patients, the drug dose should be reduced.

The efficacy of Theophylline may decrease in smokers. Because the bronchodilator effect of Theopec develops gradually in 3-6 hours after administration, the drug is not prescribed to relieve acute conditions.

Caution should be exercised when consuming large amounts of caffeine-containing products or beverages during treatment.

Contraindications

• Hypersensitivity (including. to other xanthine derivatives – caffeine, pentoxifylline, theobromine),
• acute myocardial infarction,
• severe arterial hyper- or hypotension,
• severe cardiac rhythm disorders (severe tachyarrhythmias, extrasystoles),
• hyperfunction of the thyroid,
• gastric and duodenal ulcer in the acute stage,
• gastritis with hyperacidity,
• bleeding from the gastrointestinal tract,
• epilepsyepilepsy,
• high seizure activity,
• hemorrhagic stroke,
• pregnancy,
• children under 3 years of age.

. Caution should be used with severe angina pectoris, heart failure, hypertrophic cardiomyopathy, marked liver and renal dysfunction, gastric and duodenal ulcer (in anamnesis), bleeding from the gastrointestinal tract in recent history, prolonged hyperthermia, gastroesophageal reflux, prostate hypertrophy.

Side effects

Nervous system disorders: dizziness, headache, insomnia, agitation, anxiety, irritability, tremor.

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

Digestive system disorders: gastralgia, nausea, vomiting, gastroesophageal reflux, heartburn, aggravation of peptic ulcer disease, diarrhea, with prolonged use – loss of appetite.

Allergic reactions: skin rash, itching, fever.

Other: chest pain, tachypnoea, sensation of flushes to the face, albuminuria, hematuria, hypoglycemia, increased diuresis, increased sweating. The side effects decrease with lowering the dose of the drug.

Overdose

Symptoms: decreased appetite, gastralgia, diarrhea, nausea, vomiting (including blood), gastrointestinal bleeding, tachypnea, facial hyperemia, tachycardia, ventricular arrhythmias, insomnia, motor agitation, anxiety, photophobia, tremors, seizures. In severe poisoning epileptoid seizures, hypoxia, metabolic acidosis, hyperglycemia, hypokalemia, decreased blood pressure, confusion, renal failure with myoglobinuria may develop.

Treatment: withdrawal of the drug, gastric lavage, administration of activated charcoal, laxative drugs, bowel lavage with a combination of polyethylene glycol and electrolytes, forced diuresis, hemosorption, plasma sorption, hemodialysis (effectiveness is not high, peritoneal dialysis is not effective), symptomatic therapy (includingincluding metoclopramide and ondansetron for vomiting). Maintain airway patency and oxygen therapy if seizures occur. For seizure management, intravenous diazepam 0.1-0.3 mg/kg (but no more than 10 mg). For severe nausea and vomiting – metoclopramide or ondansetron (IV).