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Quibron-T (Theophylline) is a bronchodilator used to treat the symptoms of asthma, chronic bronchitis, and emphysema.

Brand: Theophylline

Availability: In Stock
Average Delivery Time: 9 Days
Exp. Date: June 2024
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Product description

Drug Name

Quibron-T (Theophylline)

Pharmacological action

Phosphodiesterase inhibitor, methylxanthine. Increases accumulation of CAMP in tissues, blocks adenosine (purine) receptors; reduces influx of calcium ions through cell membrane channels, reduces smooth muscle contractile activity. Relaxes muscles of bronchi, blood vessels (mainly brain, skin and kidney vessels); has a peripheral vasodilator effect, increases renal blood flow, has a moderately pronounced diuretic effect. Stabilizes the membrane of mast cells, inhibits the release of mediators of allergic reactions. Increases mucociliary clearance, stimulates contraction of the diaphragm, improves the function of respiratory and intercostal muscles, stimulates the respiratory center. Normalizes respiratory function, promotes blood oxygenation and reduces carbon dioxide concentration; stimulates respiratory centers. Enhances lung ventilation in conditions of hypokalemia.

Has a stimulating effect on cardiac activity, increases the force of heart contractions and heart rate, increases coronary blood flow and myocardial oxygen demand. Reduces the tone of blood vessels (mainly vessels of the brain, skin and kidneys). Reduces pulmonary vascular resistance, lowers the pressure in the small circle of circulation.

Increases renal blood flow, has a moderate diuretic effect. Dilates extrahepatic biliary tracts. Inhibits platelet aggregation (inhibits platelet activation factor and PgE2α), increases resistance of erythrocytes to deformation (improves rheological properties of blood), reduces thrombosis and normalizes microcirculation.


When administered orally, theophylline is quickly and completely absorbed from the gastrointestinal tract. The presence of food in the stomach may affect the rate (but not the degree) of absorption of theophylline as well as its clearance. When using the usual dosage form, Cmax in plasma is reached after 1-2 hours.

Absorption is slow and incomplete after intravenous injection.

Binding to plasma proteins is approximately 40%; in neonates as well as in adults with disease, binding is reduced.

Theophylline is metabolized in the liver with the participation of several cytochrome P450 isoenzymes, the most important of which is CYP1A2. During metabolism 1,3-dimethylureic acid, 1-methylureic acid and 3-methylxanthine are formed. These metabolites are excreted in the urine. In adults, 10% is excreted unchanged. In newborns a significant portion is excreted as caffeine (due to the immaturity of its further metabolic pathways), unchanged - 50%.

Significant individual differences in the rate of hepatic metabolism of theophylline cause marked variability in clearance values, plasma concentrations, T1/2. Such factors as age, tobacco smoking habits, diet, diseases, and concomitant drug therapy affect hepatic metabolism.

T1/2 of theophylline in non-smoking patients with bronchial asthma practically without pathological changes from other organs and systems is 6-12 h, in children - 1-5 h, in smokers - 4-5 h, in newborns and premature babies - 10-45 h.

T1/2 of theophylline is increased in elderly people and patients with heart failure or liver diseases.

Clearance decreases in heart failure, liver dysfunction, chronic alcoholism, pulmonary edema, COPD.

Contraindications to use

Epilepsy, gastric and duodenal ulcer in the acute phase, gastritis with hyperacidity, recent gastrointestinal bleeding, severe arterial hyper- or hypotension, severe tachyarrhythmias, hemorrhagic stroke, retinal haemorrhage, childhood age (under 3 years, for prolonged oral forms - under 12 years), hypersensitivity to theophylline and to other xanthine derivatives (caffeine, pentoxifylline, theobromine).

Use during pregnancy and lactation

Theophylline penetrates the placental barrier and is excreted with breast milk.

During pregnancy, theophylline is used only if the estimated benefit to the mother exceeds the possible risk to the fetus.

If it is necessary to use during lactation, it should be taken into account that theophylline is excreted with breast milk.

Administration in liver dysfunction

In severe liver disease, the dose of theophylline should be reduced.

Administration in children

Contraindicated in children (under 3 years of age, for prolonged oral forms under 12 years of age).

Administration in elderly patients

Use with caution in elderly patients.

Indications of active substances of Theophylline

Bronchoobstructive syndrome of various genesis: bronchial asthma (drug of choice for exertional asthma and as adjunctive treatment for other forms of bronchial asthma), COPD (chronic obstructive bronchitis, pulmonary emphysema). Pulmonary hypertension, pulmonary heart, edema syndrome of renal genesis (as part of the combined therapy), nocturnal apnea.

Dosing regimen

 The optimal dosing regimen is determined by the doctor. Should be strictly in accordance with the dosage form used by a particular drug indications for use and the dosing regimen.

The dosing regimen shall be established individually. The initial dose is on average 400 mg/day. In case of good tolerance, the dose can be increased by about 25% of the initial one every 2-3 days until the optimal therapeutic effect is achieved.

Maximum doses that can be used without monitoring of plasma theophylline concentration: 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 during use in indicated doses symptoms of toxic effect appear or if there is a necessity of further dose increase (due to insufficient therapeutic effect), it is recommended to monitor theophylline concentration in plasma. Optimal therapeutic concentrations of theophylline are 10-20 µg/ml. At lower concentrations, the therapeutic effect is poorly expressed, at higher concentrations, no significant increase in therapeutic effect is noted, while the risk of side effects increases significantly. The frequency of administration depends on the dosage form.