Ascoril tablets, No. 20

As part of the combined therapy of acute and chronic bronchopulmonary diseases, accompanied by the formation of a viscous secretion that is difficult to separate:

-bronchial asthma;

-tracheobronchitis;

-obstructive bronchitis;

-pneumonia;

- pulmonary emphysema;

-whooping cough;

-pneumoconiosis;

-pulmonary tuberculosis.

Inside. Adults and children over 12 years old - 1 table. 3 times a day; children from 6 to 12 years old - 1/2 or 1 table. 3 times a day.

For children under 6 years of age, the use of Ascoril Expectorant syrup is recommended.

Pills

1 tab.

active substances:

salbutamol sulfate (equivalent to salbutamol) 2 mg

bromhexine hydrochloride 8 mg

guaifenesin 100 mg

excipients: calcium hydrogen phosphate; corn starch; methyl parahydroxybenzoate (methylparaben); propyl parahydroxybenzoate (propylparaben); talcum powder; colloidal silicon dioxide; magnesium stearate

-Hypersensitivity to the components of the drug;

-achyarrhythmia, myocarditis;

- heart defects;

-decompensated diabetes mellitus;

-thyrotoxicosis;

-glaucoma;

-hepatic or renal failure;

- peptic ulcer of the stomach and duodenum in the acute stage;

-gastric bleeding;

-arterial hypertension;

-pregnancy;

- lactation period;

-Children under 6 years old.

With care: diabetes mellitus; peptic ulcer of the stomach and duodenum in remission.

pharmachologic effect

Combined drug with bronchodilator, expectorant and mucolytic action.

Bromhexine is a mucolytic agent. Increases the serous component of bronchial secretions and activates the cilia of the ciliated epithelium, thereby providing the expectorant effect of the drug: reducing the viscosity of sputum, increasing its volume and improving discharge.

Guaifenesin is a mucolytic and expectorant agent that reduces the viscosity of sputum, facilitates its removal and promotes the transition of an unproductive cough into a productive one.

Salbutamol is a bronchodilator, is a selective agonist of ? 2 -adrenergic receptors. In therapeutic doses, the drug acts on the ?2-adrenergic receptors of the smooth muscles of the bronchi, preventing and / or eliminating bronchospasm, thus reducing the resistance in the airways and increasing the vital capacity of the lungs. The bronchodilatory effect of salbutamol (with reversible airway obstruction) lasts from 4 to 5 hours.

Pharmacokinetics

Bromhexine

Absorption and distribution

When ingested, it is almost completely (99%) absorbed from the gastrointestinal tract within 30 minutes. Bromhexine exhibits dose-proportional linear pharmacokinetics when taken orally over a dose range of 8 mg to 32 mg. Bioavailability - low (as it undergoes a 'first pass' effect through the liver). Penetrates the placental barrier and the BBB.

Metabolism and excretion

In the liver, it undergoes demethylation and oxidation, metabolized to pharmacologically active ambroxol. T1 / 2 - 15 hours (due to slow reverse diffusion from tissues). It is excreted by the kidneys.

In chronic renal failure, the excretion of metabolites is impaired. May cumulate with repeated use.

Guaifenesin

Absorption and distribution

Absorption from the gastrointestinal tract is fast (25-30 minutes after ingestion). Penetrates into tissues containing acidic mucopolysaccharides.

Metabolism and excretion

Approximately 60% of the administered drug is metabolized in the liver by oxidation to beta- (2-methoxy-phenoxy) -lactic acid.

T1 / 2 - 1 hour. It is excreted by the lungs (with sputum) and kidneys both unchanged and in the form of inactive metabolites.

Salbutamol

Absorption and distribution

When taken orally, absorption is high. The oral bioavailability of salbutamol is about 50%. Food intake reduces the rate of absorption, but does not affect bioavailability. Cmax of salbutamol and its metabolites in blood plasma is 5.1Ц11.7 mcg% 2.5 hours after oral administration at a dose of 4 mg.

Plasma protein binding - 10%. Penetrates the placental barrier.

Metabolism and excretion

Undergoes significant metabolism during the 'first pass' through the liver, converting to phenolic sulfate.

T1 / 2 - 3.8-6 hours. Unchanged salbutamol and metabolite are excreted mainly by the kidneys (69-90%).

Application during pregnancy and lactation

The drug is contraindicated during pregnancy and during breastfeeding.

Application for violations of liver function

The use of the drug is contraindicated in liver failure.

Application for impaired renal function

The use of the drug is contraindicated in renal failure.

Application in children

The use of the drug is contraindicated in children under 6 years of age.

special instructions

Bromhexine

Should be used with caution in patients with gastric ulcer.

Patients should be warned about possible increased mucus secretion.

Only a few cases of severe skin lesions, such as Stevens-Johnson syndrome and toxic epidermal necrolysis (TEN), were reported, which were associated in time with the use of expectorants, in particular bromhexine hydrochloride. Most of them can be explained by the severity of the underlying disease and / or the use of concomitant medications. In addition, at an early stage, Stevens-Johnson syndrome or TEN may present with nonspecific flu-like prodromal symptoms such as fever, aches, rhinitis, cough, and sore throat. Diagnostic errors associated with these nonspecific flu-like prodromal symptoms may lead to symptomatic treatment with cough and cold medications.Therefore, if skin or mucous membrane lesions occur, you should immediately seek medical attention and, as a precautionary measure, stop taking bromhexine hydrochloride.

Guaifenesin

Do not use concomitantly with cough suppressants or combined cough medicines.

Guaifenesin stains urine pink.

When used in excess, guaifenesin can cause kidney stones.

If urine is collected within 24 hours after taking guaifenesin, its metabolite can change the color of urine, and 5-hydroxyindoleacetic acid (5-HIAA) and vanillin mandelic acid (VMC) can be detected in the laboratory.

Salbutamol

Bronchodilators should not be used as the only or main drug in the treatment of patients with severe or unstable asthma. In severe bronchial asthma, regular assessment of the condition is necessary, including the determination of lung function, because patients are at risk of severe seizures and even death. The attending physicians of such patients should decide on the appointment of oral corticosteroids and / or the maximum recommended dose of inhaled corticosteroids.

With the use of sympathomimetics, including salbutamol, cardiovascular effects may be observed. Based on some data obtained in the period of post-registration use, as well as published data, rare cases of myocardial ischemia associated with salbutamol were noted. Patients with underlying severe heart disease (eg, coronary artery disease, arrhythmias, or severe heart failure) using salbutamol should be advised to seek medical attention if chest pain or other symptoms indicate worsening heart disease. Consideration should be given to assessing symptoms such as shortness of breath or chest pain, as they can be of respiratory or cardiac origin.

Salbutamol should not cause difficulty in urinating, because it does not stimulate ?-adrenergic receptors, unlike sympathomimetic agents such as ephedrine. However, difficulty in urinating has been reported in patients with prostatic hypertrophy.

Like other ?-adrenergic receptor agonists, salbutamol can cause reversible metabolic changes, for example, an increase in blood glucose concentration. Patients with diabetes mellitus may be unable to compensate for increased blood glucose levels, and ketoacidosis has been reported in such patients. Concomitant use of corticosteroids may enhance this effect.

Influence on the ability to drive vehicles and mechanisms

Given the profile of side effects (dizziness, drowsiness and others), it is recommended during treatment to refrain from driving vehicles and mechanisms, engaging in other potentially hazardous activities that require increased concentration of attention and speed of psychomotor reactions.

Overdose

Bromhexine

Currently, there are no specific symptoms of overdose in humans. Based on reports of accidental overdose and / or misuse of the drug, the observed symptoms correspond to the known side effects of bromhexine when used in the recommended doses, and symptomatic therapy is carried out if necessary.

Guaifenesin

Symptoms

The acute toxicity effects of guaifenesin include digestive discomfort, nausea, and drowsiness.

Treatment

Symptomatic therapy is performed.

Salbutamol

Symptoms

The most common signs and symptoms of salbutamol overdose are transient phenomena pharmacologically mediated by stimulation of ?-adrenergic receptors. These include tachycardia, tremors, hyperactivity, and metabolic changes including hypokalemia.

An overdose of salbutamol can lead to hypokalemia (abnormally low concentration of potassium in the blood). Therefore, it is necessary to control the concentration of potassium in the blood serum.

When used in high doses, as well as in case of overdose with short-acting beta-agonists, the development of lactic acidosis was noted. Therefore, in case of an overdose, control over an increase in serum lactate and the subsequent development of metabolic acidosis may be shown (especially if tachypnea persists or worsens, despite the elimination of other signs of bronchospasm, such as wheezing).

Nausea, vomiting and hyperglycemia have been reported predominantly in children and in cases where salbutamol overdose has occurred after oral administration.

Treatment

The drug should be discontinued and appropriate symptomatic therapy should be prescribed. Cardioselective beta-blockers (atenolol, bisoprolol, metoprolol) in patients with cardiac symptoms (eg, tachycardia, palpitations) should be used with caution because of the risk of bronchospasm.

Drug interactions

Salbutamol

The effects of salbutamol can be altered by guanethidine, reserpine, methyldopa, tricyclic antidepressants and MAO inhibitors.

With the simultaneous use of high-dose theophylline or high-dose corticosteroids with higher doses of salbutamol, the risk of hypokalemia increases.

Halogenated anesthetics

Due to the additional antihypertensive effect, the risk of developing weakness of labor with the development of bleeding increases. In addition, there have been reported cases of severe ventricular arrhythmias due to increased cardiac reactivity when the drug interacts with halogen-containing anesthetics. Therapy should be discontinued at least 6 hours prior to any planned anesthesia with halogenated anesthetics.

Antidiabetic drugs

The use of beta-agonists is accompanied by an increase in the concentration of glucose in the blood, which can be interpreted as a decrease in the effectiveness of hypoglycemic therapy. In this case, correction of individual hypoglycemic therapy may be required.

Drugs that lower the concentration of potassium in the blood

Due to the hypokalemic effect of beta-agonists, the simultaneous use of other drugs that increase the risk of hypokalemia (such as diuretics, digoxin, methylxanthines, corticosteroids) should be used with caution, after a careful assessment of the balance of benefits and risks, taking into account the increased risk of cardiac arrhythmias due to hypokalemia ...

The risk of hypokalemia increases with concomitant use with diuretics.

The combined drug Ascoril is not prescribed simultaneously with drugs containing codeine and other antitussives, because this makes it difficult for the liquefied sputum to pass.

Bromhexine, which is part of the drug, promotes the penetration of antibiotics (erythromycin, cephalexin, oxytetracycline) into the lung tissue.

It is not recommended to use the combined drug Ascoril simultaneously with non-selective ?-adrenoreceptor blockers, such as propranolol.