Theotard

Theotard has bronchodilatory properties.

Indications Theotard

It is used for the treatment or prevention of the following conditions:

• bronchial obstruction syndrome of various origins (this includes obstructive bronchitis, bronchial asthma and chronic pulmonary pathologies);
• breathing disorders at night that have a central etiology (such as sleep apnea);
• pulmonary hypertension (PH).

Release form

The substance is released in capsules that have a prolonged effect; the pack contains 40 capsules.

Pharmacodynamics

The granules contained in the capsules are pure anhydrous theophylline (a derivative of xanthine). Theophylline is a substance that slows down the activity of PDE and also increases the accumulation of cAMP inside tissues, which results in weakening the contractile activity of smooth muscles.

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

Teotard stimulates the respiratory center, reduces the resistance of the pulmonary vessels and the pressure inside the pulmonary circulation. In addition, it has a positive effect on the level of the MCC and has a favorable inotropic and chronotropic effect on the heart muscle. The drug activates diuresis processes, inhibits platelet aggregation and has a vasodilating effect on blood vessels (mostly affects the cerebral, epidermal and renal vessels).

Pharmacokinetics

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

The development of the bronchodilatory effect occurs gradually - this is why the drug cannot be used to relieve acute conditions.

After a single use of 0.35 g of theophylline, after 6.3-8.8 hours its Cmax is recorded in the blood plasma, which is 4.4 mcg/ml. After several days, the therapeutic values of the drug are achieved, equal to 8-20 mcg/ml.

The synthesis rate with protein is 60%. The substance penetrates the placenta and into mother's milk. The main metabolic processes occur inside the liver with the help of microsomal enzymes.

Excretion occurs through the kidneys (in an adult, approximately 7-13% of the substance is unchanged, while in a child this figure is 50%). The half-life ranges from 7-9 hours (in smokers it is 4-5 hours).

In people with renal or cardiac insufficiency, liver cirrhosis or alcoholism, the half-life of the drug increases. The values of total clearance decrease in people over 55 years of age, as well as in people with acute respiratory viral infections, severe fever, cardiac, hepatic or respiratory failure, and CHF.

Dosing and administration

The capsules should be taken orally in the morning or evening, after meals. Do not open or chew the capsules – they should be swallowed with plain water.

The dosage is selected by a physician individually. It is prohibited to exceed the daily dose, which is 15 mg/kg for an adult and 20 mg/kg for a child, with 2-times use per day (after a 12-hour interval). In order to select the dosage necessary for each case, it is necessary to first determine the serum values of theophylline.

The most suitable dose, allowing to achieve high therapeutic efficiency and avoid development of pronounced negative manifestations, is a dosage in the range of 10-15 mcg/ml. If the dose exceeds 20 mcg/ml, it should be reduced. Serum theophylline values should be monitored at 6-12-month intervals.

During the initial 3 days, it is necessary to take 1 capsule (0.2-0.35 g) of the drug at 12-hour intervals. After this period, it is necessary to evaluate the effectiveness of the drug and its tolerability. If the desired result is not achieved, the daily dose can be increased by 0.2-0.35 g - until the optimal treatment effect is achieved.

If the patient develops side effects, the dose is reduced until they disappear. The size of the daily portion dose of the drug 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 evening may vary in size, taking into account the patient's temporary predisposition to the occurrence of attacks that make breathing difficult, the drug's effectiveness and the clinical picture of the disease.

Capsules of 0.2 g are prescribed to people weighing no more than 20 kg (usually children).

Capsules of 0.35 g are used for people weighing over 40 kg. Usually, such a portion, taken 2 times a day, is maintenance for people weighing over 60 kg.

Non-smoking adults weighing over 60 kg should first take 0.35 g of the drug, once a day, in the evening. Then the daily dose is increased by 0.35 g, bringing it to the optimal maintenance values, which are often 0.7 g with 1-time use in the evening.

Smokers and those who have an increased metabolism of theophylline should also first take 0.35 g of the drug, and then increase the dose until the daily maintenance value of 1050 mg is reached (take according to the scheme - 1 capsule in the morning, and then 2 more in the evening).

With reduced clearance values, a daily dose of 0.2 g is initially used, and then increased by 0.2 g at 48-hour intervals. The daily maintenance dose is often 0.4 g (once, in the evening), and with a weight below 60 kg - 0.2 g.

Children aged 6-12 years should take capsules of 0.2 g. For a weight of 20-30 kg, the daily dose should be 0.4 g (2 times a day, 0.2 g). For a weight of 30-40 kg, it is 0.6 g (3 times a day, 0.2 g of LS).

Teenagers aged 12-16 (usually weighing 40-60 kg) should take 0.35 g capsules 2-3 times a day.

A noticeable medicinal effect is often observed after 3-4 days of treatment.

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Use Theotard during pregnancy

During pregnancy, Teotard is prescribed only in exceptional cases, especially in the 3rd trimester.

When breastfeeding, it is necessary to closely monitor the condition of the newborn. If irritability or sleep disorders occur, it is necessary to consult a doctor.

Contraindications

Main contraindications:

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

The medicine should be used with extreme caution in the following cases:

• severe forms of diseases affecting the liver or kidneys;
• CHF;
• a vascular form of atherosclerosis that is widespread;
• unstable angina;
• obstructive cardiomyopathy of the hypertrophic type;
• porphyria;
• frequently observed ventricular extrasystole;
• increased convulsive readiness;
• presence of ulcer in the anamnesis;
• recent history of gastrointestinal bleeding;
• uncontrolled hypo- or hyperthyroidism;
• GERD;
• prolonged hyperthermia;
• prostate enlargement;
• use in the elderly.

Side effects Theotard

The use of the drug may lead to the occurrence of certain side effects:

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

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

Reducing the portion size helps to reduce the severity of side effects.

Overdose

In case of poisoning, the following symptoms are observed: 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, a feeling of motor excitement or anxiety, photophobia and convulsions may develop.

In severe overdose, epileptoid seizures (especially in children), hyperglycemia, confusion, hypoxia, decreased blood pressure, hypokalemia, and also metabolic acidosis, skeletal muscle necrosis and renal failure may occur.

If such disorders occur, the use of the drug should be discontinued, gastric lavage should be performed (using a combination of polyethylene glycol with electrolytes), and the patient should be prescribed laxatives with activated charcoal.

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

In case of convulsions, it is necessary to monitor the patency of the respiratory ducts and ensure oxygen supply. To stop the attack, it is necessary to administer diazepam intravenously - in a dose of 0.1-0.3 mg/kg (maximum 10 mg).

Interactions with other drugs

Theophylline is compatible with antispasmodics.

The drug should not be combined with other xanthine derivatives.

The medication increases the risk of developing negative symptoms of mineralocorticosteroids (hypernatremia), GCS (hypokalemia), general anesthetics (increases the likelihood of ventricular arrhythmias) and drugs that stimulate the activity of the central nervous system (neurotoxicity).

Antidiarrheal drugs and enterosorbents reduce the degree of absorption of theophylline.

Combined use with allopurinol, cimetidine, as well as lincomycin, macrolides and fluoroquinolones requires a 60% reduction in drug dosages.

When used together with disulfiram, probenecid, and also with fluvoxamine, phenylbutazone, imipenem, paracetamol, tacrine, and also thiabendazole, mexiletine and ranitidine, the dosage of the drug should be reduced by 30%. This list also includes such drugs as methotrexate, verapamil, recombinant α-interferon, pentobarbital with ticlopidine, phenobarbital, ritonavir with isoprenaline, oral estrogen contraception, moracizine, isoniazid with magnesium hydroxide, carbamazepine with enoxacin, sulfinpyrazone with primidone, rifampicin with phenytoin and aminoglutethimide.

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

The medication enhances the properties of diuretics, β-adrenergic stimulants and reserpine.

The drug suppresses the medicinal effects of lithium carbonate, adenosine, and β-blockers.

When combined with thiazide diuretics, furosemide and substances that block the activity of α-adrenergic receptors, the likelihood of hypokalemia increases.

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Storage conditions

Theotard must be kept in a dry and dark place. Temperature values are maximum 25°C.

Shelf life

Teotard can be used within 5 years from the date of manufacture of the drug.

Application for children

Capsules of 0.2 g should not be prescribed to children under 6 years of age, and capsules of 0.35 g should not be prescribed to children under 12 years of age.

Analogues

Analogues of the drug are the medications Aminophylline-Eskom, Euphyllin, Diprophylline with Theobromine, as well as Theofedrine-N and Neo-Theofedrine.

Reviews

Teotard receives mostly positive reviews, which note the high bronchodilatory effectiveness of the drug in various pulmonary pathologies.

While most patients positively assess the effect of the medication, almost all also note the appearance of various side effects after its use. The most frequently mentioned symptoms are tremors in the hands, a feeling of sleepiness in the morning, dizziness and insomnia.