Ascoril expectorant, syrup 100 ml

Askoril expectorant – bronchodilator, mucolytic, expectorant.

Pharmacodynamics

A combined drug, has bronchodilator, expectorant and mucolytic action.

Salbutamol is a bronchodilator, stimulates beta₂-adrenoreceptors of the bronchi, blood vessels and myometrium. It prevents or eliminates bronchial spasm, reduces resistance in the airways, increases the vital capacity of the lungs. Causes dilation of the coronary arteries, does not reduce BP.

Bromhexin is a mucolytic agent, has expectorant and anti-cough effect. It increases the serous component of bronchial secretion; it activates the cilia of the atrial epithelium, reduces the viscosity of sputum, increases its volume and improves discharge.

Guifenesin is a mucolytic agent; it reduces surface tension of bronchopulmonary apparatus structures; stimulates secretory cells of the bronchial mucosa producing neutral polysaccharides, depolymerizes acidic mucopolysaccharides, reduces sputum viscosity, activates the bronchial ciliary apparatus, facilitates sputum removal and promotes the transition of non-productive cough into productive one.

Pharmacokinetics

Salbutamol

If ingested, absorption is high. Food intake reduces the absorption rate but does not affect bioavailability. Binding with plasma proteins is 10%. It penetrates through the placenta. It is subjected to presystemic metabolism in liver and intestinal wall and is inactivated to 4-sulfate ester by phenolsulfotransferase. T_1/2 is 3.8-6 h. It is excreted by the kidneys (69-90%), mainly as inactive phenolsulfate metabolite (60%) within 72 hours and with bile (4%). The bioavailability of orally administered salbutamol is about 50%.

Bromhexin

Bromhexin is almost completely (99%) absorbed in the gastrointestinal tract within 30 minutes when administered orally. Bioavailability is low (effect of primary passage through the liver). It penetrates through the placental barrier and the BBB. In the liver it undergoes demethylation and oxidation, metabolized to pharmacologically active ambroxol. T_1/2 – 15 h (due to slow reverse diffusion from tissues). It is excreted by the kidneys. Excretion of metabolites is impaired in CKD. It may cumulate with repeated use.

Gvaifenesin

The absorption from the gastrointestinal tract is fast (25-30 min after oral administration). T_1/2 – 1 h. It penetrates into tissues containing acidic mucopolysaccharides. Approximately 60% of the administered drug is metabolized in the liver. It is excreted with lungs (with sputum) and kidneys both unchanged and as inactive metabolites.

Indications

In the combination therapy of acute and chronic bronchopulmonary diseases, accompanied by the formation of difficult to drain viscous secretion:

Active ingredient

Composition

10 ml of syrup contains:

Active substances:

salbutamol (sulfate form) 2 mg,

bromhexine hydrochloride 4 mg,

guaifenesin 100 mg,

menthol 1 mg;

Associates:

flavorings,

sucrose,

How to take, the dosage

Ingestion.

Adults and children over 12 years of age – 10 ml (2 tsp) 3 times a day.

Children under 6 years of age – 5 ml (1 teaspoon) 3 times a day, 6-12 years – 5-10 ml (1-2 teaspoons) 3 times a day.

Interaction

Other beta2-adrenomimetic agents and theophylline increase the effect of salbutamol and increase the chance of side effects.

Askoril is not prescribed concomitantly with drugs containing codeine and other anti-cough medications, because this makes it difficult to drain the diluted sputum.

The bromhexine in Ascoril promotes penetration of antibiotics (erythromycin, cephalexin, oxytetracycline) into the lung tissue.

Askoril is not recommended for use simultaneously with non-selective beta-adrenoreceptor blockers such as propranololol.

The salbutamol in Ascoril is not recommended for patients who are receiving MAO inhibitors.

Diuretics and GCS drugs increase the hypokalemic effect of salbutamol.

It is not recommended to take alkaline drinking at the same time as Ascoril.

Contraindications

Patients with diabetes mellitus, arterial hypertension, peptic ulcer in remission stage are prescribed with caution.

Side effects

Rarely when used in high doses:

Overdose

Symptoms: increased manifestation of side effects.

Treatment: symptomatic therapy.

Pregnancy use

Contraindicated in pregnancy and children under three years of age

Similarities