Doxofillin - instructions for use, dose, side effects, contraindications

Clinical and pharmacological group: & nbsp

Included in the formulation

АТХ:

R.03.D.A.11 Doxophylline

Pharmacodynamics:

Doxofillin is a derivative of xanthine, an antiasthmatic agent. Pharmacological action - bronchodilator, bronchodilator.

Doxofillin only affects the smooth muscles of the pulmonary vessels and bronchi, causing bronchodilation. This is due to the ability to inhibit the enzyme phosphodiesterase, which is accompanied by an increase in the intracellular content of cAMP. Accumulation in cAMP cells inhibits the myosin binding to actin, which reduces the contractile activity of smooth muscles and contributes, in particular, to relaxing the muscles of the bronchi and eliminating bronchospasm. Unlike other methylxanthines, doxophylline does not block adenosine receptors and does not affect the transport of calcium ions. Thus, the drug does not have a stimulating effect on the central nervous system and does not affect the functioning of the heart, blood vessels and kidneys.

Pharmacokinetics:

The half-life of doxophyllin is more than 6 hours, so the use of the drug 2-3 times a day is possible until a constant and effective concentration in the blood plasma is achieved. After oral administration, the maximum concentration in the blood plasma is reached after 60 minutes. Bioavailability for oral use is about 62.6%; at a pH of 7.4, the amount of the drug that binds to plasma proteins is about 48%.

Indications:

Treatment and prevention of bronchial obstructive syndrome in bronchial asthma; chronic obstructive bronchitis; emphysema of the lungs.

ICD-10

X.J40-J47.J42 Chronic bronchitis, unspecified

X.J40-J47.J40 Bronchitis, not specified as acute or chronic

X.J40-J47.J43 Emphysema

X.J40-J47.J44 Other chronic obstructive pulmonary disease

X.J40-J47.J45 Asthma

Contraindications:

Hypersensitivity to the drug; acute myocardial infarction; arterial hypotension; hyperthyroidism; extrasystole; peptic ulcer of the stomach and duodenum in the stage of exacerbation; pregnancy; the period of breastfeeding; epilepsy; increased convulsive activity; children's age till 18 years.

Carefully:

With caution should be used in patients with low blood pressure, suffering from cardiopathy, elderly patients and patients with severe hypoxemia, hyperthyroidism, chronic pulmonary heart disease, liver disease, peptic ulcer, with severe renal failure.

Particular care should be taken in patients with circulatory failure.

Such factors as age, circulatory insufficiency in the stage of decompensation, chronic obstructive pulmonary diseases, severe liver diseases, concomitant infections lead to a decrease in the hepatic clearance of xanthine derivatives and an increase in the content of doxophylline in the blood (the dose of the drug should be reduced).

Pregnancy and lactation:

When pregnancy is contraindicated. For the duration of treatment, breastfeeding should be discontinued.

Dosing and Administration:

Inside, adults 1 tablet (400 mg) 2-3 times a day.

Intravenously (in acute conditions), adults - the contents of 2 ampoules (200 mg) after preliminary dilution with saline, inject slowly (for 15-20 minutes), in the "lying" position; if necessary, it can be repeated every 12 hours. An increase in the dose is possible only when the content of the drug is monitored in the blood (the therapeutic level is 10 μg / ml).

Side effects:

Nausea, vomiting, epigastric pain, headache, irritability, insomnia, tachycardia, extrasystole, tachypnea; in rare cases - hyperglycemia, albuminuria.

Overdose:

Symptoms: severe arrhythmias, convulsive seizures (tonic, clonic).

Treatment: symptomatic therapy. There is no specific antidote. After the disappearance of all manifestations of intoxication, therapy can be resumed in a sparing regimen.

Interaction:

The intake of food and drinks containing caffeine.

In combination with phenobarbital, phenytoin, rifampin, isoniazid, carbamazepine, sulfinpyrazone, phenytoin decrease in efficiency is observed xanthine derivatives that may require increasing doses of the drug used.

While the use of macrolide antibiotics, lincomycin, allopurinol, cimetidine, isoprenaline, beta-blockers, oral contraceptives, and proksatsinom vaccination anti-influenza drugs may increase the intensity of the action, which may require dose reduction doksofillina.

The drug suppresses the therapeutic effects of lithium carbonate and beta-adrenoblockers.

Xanthine derivatives potentiate the action of diuretics by increasing glomerular filtration and reducing tubular reabsorption.

With care, xanthine derivatives are prescribed together with anticoagulants.

Doxofillin should not be used with other xanthine derivatives.

Care should be taken when using ephedrine or other sympathomimetics at the same time.

If side effects occur, treatment may need to be discontinued.

Special instructions:

Does not affect the ability to drive a car and work with technical means.

In case of side effects it is necessary to stop using the drug. Treatment to them can be resumed at lower doses after the complete disappearance of side effects.

Instructions

Doxophylline (Doxophyllinum)