Theothard Retard Capsules 200mg N40
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Active ingredients
Theophylline
Composition
Capsules of the prolonged action 1 caps. theophylline 200 mg. Excipients: dibutyl phthalate, colloidal anhydrous silicon dioxide, ammonium methacrylate copolymer type B, ammonium methacrylate copolymer type A, povidone, talc.
Pharmacological effect
Theotard is a theophylline (xanthine derivative) in the form of pellets. Theophylline belongs to phosphodiesterase inhibitors, increases accumulation of c-AMP in tissues, blocks adenosine (purine) receptors; reduces the entry of calcium ions through the channels of cell membranes, reduces the contractile activity of smooth muscles. It relaxes the muscles of the bronchi, blood vessels (mainly the brain, skin and kidneys); has a peripheral vasodilating effect, increases renal blood flow, has a moderate diuretic effect. Stabilizes the mast cell membrane, inhibits the release of mediators of allergic reactions. Increases mucociliary clearance, stimulates contraction of the diaphragm, improves the function of the respiratory and intercostal muscles, stimulates the respiratory center. Normalizing the respiratory function, helps to saturate the blood with oxygen and reduce the concentration of carbon dioxide; stimulates the respiratory centers. Strengthens ventilation of the lungs in the conditions of a hypokalemia. It has a stimulating effect on the activity of the heart, has a positive inotropic and chronotropic effect on the heart, 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 blood pressure in the pulmonary circulation. Increases renal blood flow, has a moderate diuretic effect. Expands extrahepatic biliary tract. It inhibits platelet regression (inhibits platelet activating factor and PgE2 alpha), increases erythrocyte resistance to deformation (improves the rheological properties of blood), reduces blood clots and normalizes microcirculation. Replaced release of the active substance from the capsules of a prolonged action ensures the achievement of a therapeutic level of theophylline in the blood within 3-5 hours after administration and its preservation for 12 hours,so that the effective concentration of theophylline in the blood during the day is maintained when taking the drug 2 times a day. Teothard's bronchodilator effect develops gradually, so the drug is not indicated for the relief of emergency conditions.
Pharmacokinetics
After oral administration Teotard is almost completely absorbed, bioavailability - 88-100%. Slow release of the active substance from the capsules of the prolonged action of the drug Teotard ensures the maintenance of a uniform level of theophylline in the blood serum for 12 hours. After a single dose of 350 mg of the drug, plasma Cmax is reached in 7 hours, which is 4.4 μg / ml. Therapeutic concentration is reached in a few days and it is 8-20 μg / ml. Plasma protein binding is about 60%. It penetrates the placental barrier, is found in breast milk. Metabolized in the liver (90%) with the participation of several cytochrome P450 enzymes (the most important CYP1A2). The major metabolites are 1,3-dimethyl uric acid and 3 methylxanthine. Excretion of metabolites by the kidneys, together with 7-13% of the unchanged active substance (in children - 50%). T1 / 2 in non-smoking patients is 7-9 hours. In smoking people, significantly shorter - 4-5 hours. In patients with cirrhosis of the liver, heart failure, renal failure, and in patients with alcoholism, T1 / 2 is lengthened. Total clearance is reduced in patients with high fever, severe respiratory failure, in patients with hepatic insufficiency or chronic heart failure (CHF), in viral infections, in patients over 55 years of age.
Indications
Broncho-obstructive syndrome of various genesis: bronchial asthma (a drug of choice for physical stress asthma and as an additional remedy for other forms of bronchial asthma), COPD (chronic obstructive bronchitis, pulmonary emphysema). Pulmonary hypertension, pulmonary heart, edematous syndrome of renal genesis (as part of combination therapy), sleep apnea.
Contraindications
Epilepsy, peptic ulcer of the stomach and duodenum in the acute phase, gastritis with increased acidity, recent hemorrhage from the gastrointestinal tract, severe arterial hyper- or hypotension, severe tachyarrhythmias, hemorrhagic stroke, hemorrhage into the retina of the eye, children (up to 3 years old, for prolonged periosis forms - up to 12 years), hypersensitivity to theophylline and to other xanthine derivatives (caffeine, pentoxifylline, theobromine).
Use during pregnancy and lactation
Theophylline penetrates the placental barrier, is excreted in breast milk. In pregnancy, theophylline is used only if the intended benefit to the mother exceeds the possible risk to the fetus. If necessary, use during lactation should be aware that theophylline is excreted in breast milk.
Dosage and administration
Install individually. The initial dose is an average of 400 mg / day. With good tolerance, the dose can be increased by approximately 25% from the initial every 2-3 days until the optimum therapeutic effect is achieved. The maximum dose that can be used without controlling the concentration of theophylline in the 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, when used in the indicated doses, symptoms of toxic action appear or the need arises to further increase the dose (due to insufficient therapeutic effect), it is recommended to control the concentration of theophylline in the blood plasma. The optimal therapeutic concentration of theophylline - 10-20 mg / ml. At lower concentrations, the therapeutic effect is mild, at large concentrations, there is no significant increase in the therapeutic effect, while the risk of side effects increases significantly. The frequency of administration depends on the dosage form.
Side effects
From the side of the central nervous system: dizziness, headache, insomnia, agitation, anxiety, irritability, tremor. Since the cardiovascular system: heartbeat, tachycardia (including the fetus when taken in the third trimester), arrhythmias, decreased blood pressure, cardialgia, increased frequency of strokes. On the part of the digestive system: gastralgia, nausea, vomiting, gastroesophageal reflux, heartburn, exacerbation of peptic ulcer, diarrhea, with prolonged use - loss of appetite. Allergic reactions: skin rash, itching, fever. Other: pain in the chest, tachypnea, sensation of hot flashes to the face, albuminuria, hematuria, hypoglycemia, increased diuresis, increased sweating. Side effects decrease with decreasing dose.
Interaction with other drugs
Theophylline is not used in conjunction with other xanthine derivatives.Increases the likelihood of side effects of GCS (hypokalemia), mineralocorticosteroids (hypernatremia), means for general anesthesia (increases the risk of ventricular arrhythmias), means of stimulating the central nervous system (increases neurotoxicity). Antidiarrheal drugs and enterosorbents reduce theophylline absorption. With simultaneous use of antibiotics, macrolides, lincomycin, allopurinol, cimetidine, and fluoroquinamone are recommended. , nropafenone, thiabendazole, ticlopidine, verapamil, isoprenaline, oral estrogen-containing contraceptives, phenobarbital, pentobarbital, magnesium hydroxide, morac isin, ritonavir or sulfinpirazon, rifampicin, isoniazid, carbamazepine, primidone, sulfinpyrazon, aminogutetimid, phenytoin, enoxacin (it is recommended to reduce theophylline doses by 30%), viloxazine and, if the flu is vaccinated, can be used by an increase in the flow ratio, it is possible to increase a figure, if it is working, it can increase, if it is in a position, it is, if it is, it is, if it is, it will be in trouble, it can be a figure, it can be a figure, if it is a woman, it is in a cell The drug inhibits the therapeutic effects of lithium carbonate, adenosine and beta-blockers. Theophylline potentiates the action of beta-adrenostimulants, reserpine and diuretics by increasing glomerular filtration and reducing tubular reabsorption. Compatible with antispasmodics. Against the background of joint use with alpha-adrenoreceptor blockers, thiazide diuretics, furosemide, the risk of hypokalemia increases.
special instructions
Use with caution in severe coronary insufficiency (acute phase of myocardial infarction, angina), widespread vascular atherosclerosis, hypertrophic obstructive cardiomyopathy, ventricular extrasystole, chronic heart failure, increased seizure readiness, in case of heart failure, and had to have heart disease and had to have a simple case, in case of heart disease, and had to have a simple case, it is unacceptable, in case of heart disease, and had to have heart disease and had to have heart disease and had to have a heart disease, he had heart disease, he had heart disease, and he had heart disease, he had heart disease, and he had heart disease, he had heart disease, and he had heart disease, he had heart disease, and he had heart disease, he had heart disease, and he had heart disease, he had heart disease, he had heart disease, he had heart disease, he was ill, he had heart disease, he had a heart failure, he had heart disease, he had a heart failure, he had a heart disease history), with uncontrolled hypothyroidism (the possibility of cumulation) or thyrotoxicosis, prolonged hyperthermia, gastroesophageal reflux, prostatic hypertrophy, during pregnancy, during lactation, in elderly patients, in children (especially for oral forms). Use with caution rectal with diarrhea and diseases of the rectum.The intensity of theophylline may decrease in smokers. Theophylline is not used simultaneously with other xanthine derivatives. In severe diseases of the cardiovascular system, liver, viral infections, as well as in elderly patients, the dose of theophylline should be reduced.