Mucosol

International nonproprietary name

Carbocisteine.

Pharmatherapeutic Group

Expectorant drugs. Mucolytic agents.

Formulation

Syrup: every 5 g of syrup contains 250 mg of carbocisteine.

Pharmacological Action

Pharmacodynamics

Mucolytic and expectorant drug which effect is stipulated by activation of sialic transferase         (goblet cells enzyme of bronchi mucous membrane). It normalizes quantitative ratio of acidic and neutral sialomucins of bronchial secret: reduces the quantity of neutral glycopeptides, increases the quantity of hydroxysialoglycopeptides. It decreases ductility of bronchial secret and secret separated from sinus, alleviates discharge of sputum and mucus, relieves cough. It promotes regeneration of mucous membrane, normalizes its structure, reduces number of goblet cells, especially in terminal bronchi and, as a sequence, reduces generation of mucus. It restores secretion of immunologically active IgA (specific protection), improves mucociliary clearance.

Pharmacokinetics

Absorption being rapid and practically complete. Bioavailability being low ( less than 10% of the taken dose). TCmax in blood and in mucous membrane – 1.5 – 2 hours, therapeutic concentration is preserved in blood within 8 hours. It is longer of all detained in blood, liver and middle ear. High concentration of the drug is accumulated in bronchial secret (17.5% of taken dose). It is metabolized in liver (having effect of “first passage” through liver). It is excreted by kidneys (60-90% - unchanged, the rest – in the form of metabolites). T ½ is 2-3.5 hours. Full excretion occurs in 3 days.

Therapeutic Indications

Acute and chronic bronchopulmonary diseases accompanied by formation of viscous hardly-secreted sputum (tracheitis, bronchitis, tracheobronchitis, bronchial asthma, multiple bronchiectasis) and mucus (inflammatory diseases of middle ear, nose and paranasal sinus -  rhinitis, adenoiditis, otitis media, sinusitis); preparation to bronchoscopy and/or bronchography.

Direction for Use and Dosage Schedule

The preparation is intended for intake. 1 teaspoon (5 ml) of syrup contains 0.25 g of carbocisteine.

Children from 1 month to 2 years are prescribed to take 1/5 of teaspoon (1.25 ml of syrup, or 0.05 g of carbocisteine) two times a day.

Children from 2 to 5 years are prescribed to take 1/2 of teaspoon (2.5 ml of syrup, or 0.125 g of carbocisteine) 2-3 times a day.

Children from 5 to12 years are prescribed to take 1 teaspoon (5 ml of syrup, or 0.25 g of carbocisteine) 2-3 times a day.

Adults are prescribed to take 3 teaspoons (15 ml of syrup, or 0.75 g of carbocisteine) 2-3 times a day, at amelioration dose is recommended to be reduced up to 2 teaspoons a day.

Duration of treatment should not exceed 8-10 days.

Particular Indications

It should be considered that 1 tablespoon of syrup contains 6 g of saccharose.

Adverse Reaction

Mucosol is usually well tolerable. In separate cased appearance of skin eruption is possible.

There are occasional reports of initiation of gastrointestinal hemorrhage during carbocisteine therapy.

Contraindications

Increased individual sensitivity to components of the preparation, ulcer of stomach and  duodenum ( in the phase of  exacerbation), impaired function of kidneys, acute glomerulonephritis,  cystitis, pregnancy (the first trimester), lactation period, infancy under

1 month.

Precautions

The preparation intake is not recommended at impaired function of kidneys, acute glomerulonephritis, cystitis. Mucosol is prescribed with care at ulcer of stomach and duodenum

in anamnesis.

Using during pregnancy: it may be taken with care during IId and IIId trimester of pregnancy under strict doctor’s control.

Interaction with other drugs

It enhances efficiency of glucocorticoid (mutually) and antibacterial therapy of inflammatory diseases of upper air passages and lower air passages. It potentiates broncholytic action of theophillin. Activity of carbocisteine is relieved by antitussive and atropine-like drugs.

Form of  Production

Syrup. 80ml in vials.

Mucosol is produced in collaboration with “CTS Chemical Industries Ltd.” company, Israel.