Orvis Broncho Ambroxol, 7.5 mg/ml 100 ml

Pharmacotherapeutic group: expectorant, mucolytic agent

ATC code: R05CB06

Pharmacological properties

Pharmacodynamics

Ambroxol is the active N-demethylated metabolite of bromhexine.

It has secretomotor, secretolytic and expectorant effects.

Stimulates bronchial glands, increases motor activity of the atomizing epithelium by influencing type 2 pneumocytes in alveoli and Clara cells in bronchioles, increases formation of endogenous surfactant – surfactant that ensures gliding of bronchial secretion in the airway lumen.

Ambroxol increases the proportion of the serous component in the bronchial secretion, improving its structure and contributing to the reduction of viscosity and liquefaction of sputum; as a result, mucociliary transport (mucociliary clearance) is improved.

Augmenting mucociliary clearance improves sputum removal from the bronchial tree and eases coughing.

On average, when taken orally, the action of the drug comes in 30 minutes, the duration of action is 6-12 hours, depending on the dose taken.

Pharmacokinetics

After oral administration, ambroxol is quickly and almost completely absorbed from the gastrointestinal tract.

The maximum concentration (Cmax) in blood plasma with oral administration is reached after 1-3 hours. Distribution volume is 552 l. In the therapeutic range of concentrations, binding to plasma proteins is 80-90 %. The highest concentrations of the active component of the drug are observed in the lungs.

Ambroxol penetrates through the placental and blood-brain barrier, is excreted with the breast milk.

About 30% of the oral dose taken is subject to the effect of primary passage through the liver.

The studies on human liver microsomes have shown that the CYP3A4 isoenzyme is the predominant isoform responsible for metabolizing ambroxol to dibromanthranilic acid.

The remainder of ambroxol is metabolized in the liver by conjugation to form pharmacologically inactive metabolites.

The terminal elimination half-life (T1/2) of ambroxol from blood plasma is 10 hours.

The total half-life of ambroxol and its metabolites is about 22 hours. Excreted by the kidneys: 90% as metabolites, 10% unchanged.

There is no clinically significant effect of age and sex on pharmacokinetics of ambroxol; therefore, there is no reason to adjust the dosage according to these characteristics.

Indications

Active ingredient

Composition

How to take, the dosage

Interaction

Special Instructions

Ambroxol should not be combined with cough suppressants that make it difficult to expectorate sputum.

In order to maintain the secretolytic action during the use of the drug it is necessary to provide the body with sufficient fluid intake.

In patients with bronchial asthma, ambroxol may increase coughing.

The drug contains benzalkonium chloride (a preservative), which when inhaled may cause bronchial spasm in sensitive patients with an overactive airway.

The drug should not be mixed with cromoglycic acid and alkaline solutions.

Patients on a hyponatremic diet should take into account that 1 ml of the drug contains 10 mg of sodium. The maximum daily dose (12 ml) for adults and children over 12 years old contains 120 mg of sodium.

There have been isolated reports of Stevens-Johnson syndrome and Lyell’s syndrome coinciding with the administration of ambroxol, but there is no causal relationship with the intake of the drug.

In most cases, they can be explained by the severity of the underlying disease and/or concomitant therapy.

In patients with Stevens-Johnson or Lyell syndrome, fever, body pain, rhinitis, cough and sore throat may occur in the early phase.

In symptomatic treatment, mucolytic agents such as ambroxol hydrochloride may be mistakenly prescribed.

If the above syndromes develop, it is recommended that ambroxol treatment be discontinued and medical attention sought immediately.

In severe renal failure (creatinine clearance less than 30 ml/min) the risk of cumulation of ambroxol metabolites should be considered.

The effect of the drug on the ability to drive vehicles and mechanisms

The drug has no effect on performance of potentially hazardous activities requiring increased concentration and quick psychomotor reactions (driving, operating moving mechanisms etc.).

Contraindications

Side effects

Overdose

No specific symptoms of ambroxol overdose in humans have been described.

The observed symptoms of overdose were consistent with the known side effects of ambroxol used in the recommended doses (nausea, vomiting, abdominal pain, diarrhea, dyspepsia).

Treatment: artificial vomiting, gastric lavage in the first 1-2 hours after taking the drug; intake of fat-containing foods, symptomatic therapy.

Similarities