Teotard

Theotard has bronchodilatory properties.

Indications Theotaurs

It is used to treat or prevent such conditions:

• bronchial obstruction syndrome, having a different genesis (this includes obstructive bronchitis, asthma and pulmonary pathology in the chronic stage);
• respiratory disturbances at night, having a central etiology (such as sleep apnea);
• pulmonary hypertension  (CPH).

Release form

The release of a substance is realized in capsules having a prolonged form of exposure; inside the pack contains 40 capsules.

Pharmacodynamics

The granules contained in the capsules are pure theophylline anhydrous (xanthine derivative). At the same time, theophylline is a substance that slows down the activity of PDE, as well as increases the accumulation of cAMP within the tissues, as a result of which the contractile activity of smooth muscles is weakened.

The drug has a pronounced bronchodilator effect, prevents or completely eliminates bronchial obstruction. A noticeable increase in pulmonary activity allows an increase in the amount of oxygen entering the arterial blood, due to which CO2 indices decrease.

Theotard stimulates the activity of the respiratory center, weakens the resistance of the pulmonary vessels and the pressure inside the small circle of blood flow. In addition, it has a positive effect on the level of the ICC and has a favorable inotropic and chronotropic effect on the heart muscle. The drug activates the process of diuresis, inhibits platelet aggregation and has a vasodilating effect on the blood vessels (for the most part affects the brain, epidermal and renal vessels).

Pharmacokinetics

Absorption of drugs after oral administration is almost complete. Due to the slow release of the active element from the capsules of drugs, it is possible to maintain uniform blood levels of theophylline in the period of 12 hours.

The development of bronchodilator effects occurs gradually - that is why the drug can not be used for edema in acute conditions.

After 1 single application of 0.35 g of theophylline, after 6.3-8.8 hours, its Cmax is recorded inside the blood plasma, which is 4.4 μg / ml. After several days, the therapeutic values of drugs equal to 8–20 µg / ml are achieved.

The rate of synthesis with protein is 60%. The substance penetrates the placenta and into breast milk. The main metabolic processes take place inside the liver with the help of microsome enzymes.

Excretion occurs through the kidneys (in an adult about 7-13% of the substance has an unchanged state, and in a child this figure is 50%). Half-life ranges from 7-9 hours (for smokers, it is 4-5 hours).

In patients with renal or cardiac insufficiency, hepatic cirrhosis or alcoholism, the half-life of drugs increases. The values of total clearance are reduced in people over the age of 55 years, and in addition, in patients with acute respiratory viral infections, severe fever, insufficiency of heart function, liver or respiratory system, as well as with CHF.

Dosing and administration

Capsules should be used inside in the morning or in the evening, after eating. It is impossible to open or chew the capsules - they are swallowed, washed down with plain water.

Selection of dosage is made by a physician individually. It is forbidden to exceed the daily dose, which for an adult is 15 mg / kg, and for a child - 20 mg / kg, with 2-fold use per day (after a 12-hour period). To choose the dosage necessary for each case, it is first necessary to determine the serum values of theophylline.

The most suitable portion, allowing to achieve high therapeutic efficacy and avoid the development of pronounced negative manifestations, is a dosage in the range of 10-15 μg / ml. At excess of a portion of 20 mkg / ml, it is required to be reduced. Track serum values of theophylline should be at 6-12 months intervals.

In the period of the initial 3 days, it is necessary to use 1 capsule (0.2-0.35 g) of drugs with 12-hour intervals. After this period, it is required to evaluate the effectiveness of the drug and its portability. In the absence of the desired result, the daily portion may increase by 0.2-0.35 g - until the optimal treatment effect is achieved.

If the patient develops side effects, lower the portion until they disappear. The size of the daily dose of drugs is determined by the severity and nature of the pathology, as well as the age and weight of the patient.

Dosages taken in the morning and in the evening can vary in size, taking into account the patient’s temporal susceptibility to the appearance of seizures that make breathing difficult, drug efficacy, and the clinical picture of the disease.

Capsules with a volume of 0.2 g are assigned to people weighing no more than 20 kg (usually children).

Capsules with a volume of 0.35 g are used for persons weighing more than 40 kg. Usually such a portion, used 2 times a day, is supportive in people weighing more than 60 kg.

Non-smoking adults, whose weight is more than 60 kg, must first take 0.35 g of drug, 1 time per day, in the evening. Next, the daily portion is increased by 0.35 g, bringing it to the optimal supporting indicators, which are often 0.7 g with 1-fold use in the evening.

Smokers and those who have a stronger metabolism of theophylline, first also need to take 0.35 g of drugs, and then increase the portion to obtain supporting daily values of 1050 mg (take the scheme - 1 capsule in the morning, and then 2 more in the evening) .

At reduced clearance values, a daily dose of 0.2 g is first used, and then it is increased by 0.2 g at 48-hour intervals. The size of the maintenance dose per day is often 0.4 g (1 time, in the evening), and with a weight below 60 kg it is 0.2 g.

Children in the age range of 6–12 years should use capsules with a volume of 0.2 g. For a weight in the range of 20–30 kg, the daily ration should be 0.4 g (2 times daily intake of 0.2 g). For a weight in the range of 30-40 kg each, it is equal to 0.6 g (3 single intake per day 0.2 g of drug).

Teenagers 12-16 years old (usually their weight is 40-60 kg) should take 0.35 g capsules. Reception occurs 2-3 times a day.

A noticeable drug effect is often noted after 3-4 days of treatment.

[1]

Use Theotaurs during pregnancy

In pregnancy, the appointment of Teothard is allowed only in exceptional cases, especially in the 3rd trimester.

When breastfeeding is necessary to carefully monitor the condition of the newborn. In the event of irritability or the development of sleep disorders, it is necessary to consult a physician.

Contraindications

Main contraindications:

• acute stage of myocardial infarction;
• a strong decrease or increase in blood pressure;
• hemorrhagic stroke;
• arrhythmias with severe severity;
• epilepsy;
• hemorrhages in the region of the eye retina;
• aggravated ulcer;
• bleeding inside the digestive tract;
• hyperacid form of gastritis;
• the presence of intolerance to theophylline (or xanthine derivatives, such as caffeine and theobromine with pentoxifylline).

Extremely careful medicine is used in such cases:

• severe diseases affecting the liver or kidneys;
• CHF;
• vascular form of atherosclerosis, which has a common character;
• unstable form of angina pectoris;
• obstructive cardiomyopathy of hypertrophic type;
• porphyria;
• often observed extrasystole of the ventricles;
• increased convulsive readiness;
• presence of an ulcer in the anamnesis;
• recent bleeding inside the gastrointestinal tract;
• having an uncontrolled nature of hypo-or hyperthyroidism;
• GERD;
• hyperthermia;
• prostate enlargement;
• use in the elderly.

Side effects Theotaurs

The use of the medication may lead to the emergence of individual side effects:

• CNS lesions: feeling of excitement, irritability or anxiety, headaches, tremor, insomnia, dizziness and vertigo;
• allergy symptoms: itching, rash on the epidermis and fever;
• disorders of the digestive system: GERD, diarrhea, abdominal pain, nausea, and in addition, worsening of the ulcer, heartburn, loss of appetite (with prolonged use of drugs) and vomiting;
• cardiovascular dysfunction: tachycardia, (also in the fetus, if treatment is carried out in the 3rd trimester), cardialgia, a decrease in blood pressure, arrhythmias, palpitations and an increase in the number of angina pectoris attacks;
• changes in laboratory data: albuminuria, hematuria, hypercalcemia or hypokalemia, and in addition hyperglycemia and hyperuricemia;
• Other: hot flashes, increased diuresis, hyperhidrosis, pain in the sternum and tachypnea.

The incidence of negative symptoms increases with blood levels of theophylline above 20 μg / ml.

Reducing the portion allows you to reduce the severity of adverse events.

Overdose

In case of poisoning, such manifestations are noted: nausea, tachypnea, facial hyperemia, stomach pain, vomiting (sometimes bloody), loss of appetite, bleeding inside the gastrointestinal tract and diarrhea. In addition, tachycardia, tremor, ventricular arrhythmia, insomnia, motor excitement or anxiety, photophobia and convulsions may develop.

In severe overdose, epileptoid seizures (especially in children), hyperglycemia, a sense of confusion, hypoxia, decreased blood pressure, hypokalemia, and in addition the metabolic form of acidosis, skeletal muscle necrosis and renal insufficiency can be noted.

When such disorders appear, the use of drugs should be discontinued, gastric lavage should be performed (using a combination of polyethylene glycol and electrolytes), and laxatives with activated carbon should be prescribed to the patient.

In addition, procedures of forced diuresis, plasma sorption, hemosorption and hemodialysis (poorly effective) are carried out, and metoclopramide with ondansetron is also prescribed (in case of vomiting).

When convulsions need to monitor the patency of the respiratory ducts and provide oxygen. To stop an incident, you need to enter intravenous diazepam - in a dose of 0.1-0.3 mg / kg (maximum 10 mg).

Interactions with other drugs

Theophylline is compatible with antispasmodics.

You can not combine the drug with other xanthine derivatives.

The drug increases the risk of negative symptoms of mineralocorticosteroids (the appearance of hypernatremia), GCS (the appearance of hypokalemia), means for general anesthesia (the likelihood of ventricular arrhythmias) and drugs that stimulate the activity of the CNS (the appearance of neurotoxicity).

Antidiarrheal drugs and enterosorbents reduce theophylline absorption.

Combined use with allopurinol, cimetidine, and in addition lincomycin, macrolides and fluoroquinolones requires a reduction in dosages of drugs by 60%.

When used together with disulfiram, probenecid, and in addition with fluvoxamine, phenylbutazone, imipenem, paracetamol, tacrine, and at the same time tiabendazole, meksiletin and ranitidine, reduce the dosage of the drug by 30%. The list also includes drugs such as methotrexat, verapamil, recombinant α-interferon, pentobarbital with ticlopidine, phenobarbital, ritonavir with isoprenaline, oestrogenic contraception for ingestion, moracizin, isoniazid with magnesium hydroxide, carbamazepin oxylate, octophysthia, and octophysthylamine. Phenytoin and aminoglutetimid.

Combining with viloxazine, and in addition, parallel vaccination against influenza can cause an increase in the intensity of theophylline effect, which will require a reduction in its dosages.

The drug enhances the properties of diuretics, β-adrenostimulyatorov and reserpina.

The drug inhibits the drug effect of lithium carbonate, adenosine, as well as β-blockers.

When combined with diuretic drugs thiazide character, furosemide and substances that block the activity of α-adrenoreceptors, increases the likelihood of hypokalemia.

[2], [3]

Storage conditions

Theotard is required to be kept in a dry and dark place. Temperature values - maximum 25 ° С.

Shelf life

TeoTard can be used within 5 years from the time of manufacture of the drug.

Application for children

Capsules with a volume of 0.2 g can not be assigned to children under 6 years of age, and capsules with a volume of 0.35 g - children under 12 years of age.

Analogs

Analogues of drugs are medications Aminofillin-Eskom, Eufillin, Diprofillin with Theobromine, as well as Teofedrin-N and Neo-Teofedrin.

Reviews

Teotard receives more positive reviews - they have high bronchodilatory efficacy of drugs with a variety of pulmonary pathologies.

Given that the majority of patients positively assess the effect of the drug, almost everyone notes the appearance of various adverse symptoms after its use. The most frequently mentioned symptoms are tremor in the hands, drowsiness in the morning, dizziness and insomnia.