Theopec, sustained release pills 200mg, 50pcs

Composition

Active ingredient:

theophylline 200 mg

Pharmacological action

Theophylline is a phosphodiesterase inhibitor. Increases the accumulation of c-AMP in the tissues, which reduces the contractile activity of smooth muscles.

Theophylline dilates the bronchi and blood vessels (mainly those of the brain, skin, and kidneys). Reduces pulmonary vascular resistance, lowers pressure in the small circle of blood circulation. Increases renal blood flow. It has a moderate diuretic effect. Inhibits platelet aggregation.

It has a stimulating effect on the respiratory center, increases the frequency and strength of heart contractions. The delayed release of the Active ingredient from the tablet ensures that the therapeutic level of theophylline in the blood is reached 3-5 hours after taking Teopec and persists for 10-12 hours.

A two-time dose of the drug allows you to get effective concentrations of theophylline in the blood during the day. Due to the long-term effect of the drug, one of the important indications for use is the prevention of night and pre-morning phenomena of bronchospasm.

Pharmacokinetics

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

Indications

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

Contraindications

• Hypersensitivity (including to other xanthine derivatives – caffeine pentoxifylline, the theobromine),
• acute myocardial infarction,
• severe arterial Hyper – or hypotension,
• widespread atherosclerosis,
• a serious irregular heart rhythm (tachyarrhythmia heavy, arrythmia),
• hyperthyroidism,
• peptic ulcer of stomach and duodenum in the acute stage,
• gastritis with high acidity,
• bleeding from the gastrointestinal tract,
• epilepsy,
• increased seizure activity,
• hemorrhagic stroke,
• bleeding in the retina of the eye,
• pregnancy,
• children’s age up to 3 years.

It should be used with caution in patients with severe angina, heart failure, hypertrophic cardiomyopathy, severe liver and kidney dysfunction, gastric and duodenal ulcers (in the anamnesis), bleeding from the gastrointestinal tract in the recent anamnesis, prolonged hyperthermia, gastroesophageal reflux, prostatic hypertrophy.

Side effects

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

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

From the digestive system: gastralgia, nausea, vomiting, gastroesophageal reflux, heartburn, exacerbation of peptic ulcer disease, diarrhea, with prolonged use – decreased appetite.

Allergic reactions: skin rash, pruritus, fever.

Others: chest pain, tachypnea, flushing of the face, albuminuria, hematuria, hypoglycemia, increased diuresis, increased sweating. Side effects decrease with a lower dose of the drug.

Interaction

When used concomitantly with macrolide antibiotics, allopurinol, cimetidine, oral contraceptives, isoprenaline, lincomycin, theophylline clearance decreases.

When used concomitantly, beta-blockers, especially non-selective ones, can cause narrowing of the bronchi, which reduces the bronchodilating effect of theophylline. It is possible to reduce the effectiveness of beta-blockers.

With the simultaneous use of beta_-2-adrenergic stimulants, caffeine, furosemide, the effect of theophylline is enhanced.

When used concomitantly with aminoglutetimide, it is possible to reduce the effectiveness of theophylline due to an increase in its excretion from the body.

When used concomitantly with acyclovir, it is possible to increase the concentration of theophylline in blood plasma and increase adverse reactions.

When used concomitantly with verapamil, diltiazem, nifedipine, felodipine, the concentration of theophylline in blood plasma usually changes slightly or moderately in the absence of changes in the bronchodilator effect. Cases of increased plasma concentrations of theophylline and increased side effects of theophylline have been reported in patients receiving concomitant treatment with verapamil or nifedipine.

With simultaneous use of disulfiram, the concentration of theophylline in the blood plasma increases and toxic reactions develop.

With the simultaneous use of lithium salts, their effectiveness may decrease.

When used concomitantly with propranolol, theophylline clearance decreases.

When used concomitantly with phenytoin, the concentrations of theophylline and phenytoin in blood plasma decrease and their therapeutic effectiveness decreases.

When used concomitantly with phenobarbital, rifampicin, isoniazid, carbamazepine, sulfinpyrazone, the intensity of theophylline action may decrease due to an increase in its clearance.

When used concomitantly with enoxacin or other fluoroquinolones, a significant increase in the concentration of theophylline in blood plasma is possible.

How to take, course of use and dosage

They are installed 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 the optimal therapeutic effect is achieved.

The maximum doses that can be used without controlling the concentration of theophylline in blood plasma: 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 effects appear when used in these doses or there is a need to further increase the dose (due to insufficient therapeutic effect), it is recommended to monitor the concentration of theophylline in the blood plasma. Optimal therapeutic concentrations of theophylline are 10-20 mcg / ml.

At lower concentrations, the therapeutic effect is weak, at high concentrations, there is no significant increase in the therapeutic effect, while the risk of side effects increases significantly. The frequency of use depends on the dosage form.

Overdose

Symptoms: decreased appetite, gastralgia, diarrhea, nausea, vomiting (including blood), gastrointestinal bleeding, tachypnea, facial flushing, tachycardia, ventricular arrhythmias, insomnia, motor agitation, anxiety, photophobia, tremor, convulsions. Severe poisoning can lead to epileptoid seizures, hypoxia, metabolic acidosis, hyperglycemia, hypokalemia, low blood pressure, confusion, and kidney failure with myoglobinuria.

Treatment: withdrawal of the drug, gastric lavage, use of activated charcoal, laxatives, intestinal lavage with a combination of polyethylene glycol and electrolytes, forced diuresis, hemosorption, plasma sorption, hemodialysis (the effectiveness is not high, peritoneal dialysis is not effective), symptomatic therapy (including metoclopramide and ondansetron-for vomiting). If convulsions occur, maintain airway patency and perform oxygen therapy. To stop a seizure – IV diazepam,0.1-0.3 mg / kg (but not more than 10 mg). For severe nausea and vomiting – metoclopramide or ondansetron (IV).

Special instructions

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

The effectiveness of theophylline may decrease in smokers. Since the bronchodilatory effect of Teopec develops gradually in 3-6 hours after use, the drug is not prescribed for the relief of emergency conditions.

Use caution when consuming large amounts of caffeinated foods or beverages during treatment.

Form of production

Tablets

Storage conditions

Store in a dry place, protected from light, at room temperature

Shelf life

5 years

Active ingredient

Theophylline

Conditions of release from pharmacies

By prescription

Dosage form

long-acting tablets

Purpose

Children as prescribed by a doctor, Adults as prescribed by a doctor, Children over 3 years of age

Indications

Bronchitis, Bronchospasm, Chronic Obstructive pulmonary disease, Bronchial asthma