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

In the studies it was shown that the active ingredient of the drug - ambroxol, increases secretion in the respiratory tract.It increases the production of pulmonary surfactant and stimulates ciliary activity. These effects lead to increased current and transport of mucus (mucociliary clearance). Strengthening mucociliary clearance improves sputum discharge and facilitates coughing. In patients with chronic obstructive pulmonary disease, prolonged therapy with the drug (for at least 2 months) resulted in a significant reduction in the number of exacerbations. There was a significant decrease in the duration of exacerbations and the number of days of antibiotic therapy.

Pharmacokinetics:For all immediate-release ambroxol dosage forms, rapid and almost complete absorption with a linear dose-response in the therapeutic range of concentrations is characteristic. The maximum concentration in plasma (C_m_Oh) with oral intake is achieved after 1-2.5 hours. The volume of distribution is 552 liters. In the therapeutic concentration range, binding to plasma proteins is approximately 90%.

The transfer of ambroxol from the blood to the tissue with oral administration occurs rapidly. The highest concentrations of the active component of the drug are observed in the lungs.Approximately 30% of the administered oral dose is subjected to the effect of a primary pass through the liver. Studies on microsomes of the human liver showed that the isoenzyme CYP3A4 is the predominant isoform responsible for the metabolism of ambroxol to dibromoanthranilic acid. The rest of the ambroxol is metabolized in the liver, mainly by glucuronidation and by partial cleavage of dibromantranilic acid (approximately 10% of the administered dose), as well as a small number of additional metabolites. The period of terminal half-life of ambroxol is about 10 hours. The total clearance is within 660 ml / min, the renal clearance accounts for about 8% of the total clearance. With the radioactive label method, it is estimated that after taking a single dose of the drug for the next 5 days, about 83% of the dose taken is excreted in the urine.

There is no clinically significant effect of age and sex on the pharmacokinetics of ambroxol, so there is no reason for choosing a dose for these symptoms.

Indications:Acute and chronic diseases of the respiratory tract with the release of viscous sputum: acute and chronic bronchitis, pneumonia,chronic obstructive pulmonary disease, bronchial asthma with difficulty in sputum discharge, bronchiectasis.

Contraindications:

Hypersensitivity to ambroxol or other components of the drug, pregnancy (I trimester), the period of lactation.

Carefully:

In renal and / or hepatic insufficiency, during pregnancy (II-III trimester).

Pregnancy and lactation:

Ambroxol penetrates the placental barrier. Pre-clinical studies are not revealed a direct or indirect adverse effect on pregnancy, embryonic / fetal, postnatal development and on generic activities.

The extensive clinical experience of using ambroxol after the 28th week of pregnancy found no evidence of a negative effect of the drug on the fetus.

However, the usual precautions should be followed when using the drug during pregnancy. It is especially not recommended to take the drug in the I trimester of pregnancy. In the II and III trimesters of pregnancy, the drug can be used only if the potential benefit to the mother exceeds the potential risk to the fetus.

Ambroxol can excrete with human milk. Despite the fact that undesirable effects in children receiving breastfeeding were not observed, during lactation it is not recommended to use Ambroxol solution for ingestion and inhalation.

Preclinical studies of ambroxol showed no adverse effects on fertility.

Dosing and Administration:

Application of the solution inside (1 ml = 25 drops):

adults and children over 12 years: 4 ml (= 100 drops) 3 times a day;

children from 6 to 12 years: 2 ml (= 50 drops) 2-3 times a day;

children from 2 to 6 years: 1 ml (= 25 drops) 3 times a day;

children under 2 years: 1 ml (= 25 drops) 2 times a day.

Drops can be diluted in water, tea, juice or milk. You can apply the solution regardless of food intake.

Application of the solution in the form of inhalation:

adults and children over 6 years of age: 1-2 inhalations for 2-3 ml of solution per day; children under 6 years: 1-2 inhalations of 2 ml of solution per day.

The drug solution can be used using any modern equipment for inhalation (except for steam inhalers). To achieve optimal humidification during inhalations, the preparation is mixed with a solvent (sodium chloride 0.9%) in a ratio of 1: 1. Since inhalation therapy can cause a deep inhalation of a cough, inhalation should be performed in the usual breathing mode. Before inhalation it is recommended to warm the inhalation solution to body temperature.

Patients with bronchial asthma should be given inhalation after taking bronchodilators, in order to avoid nonspecific irritation respiratory tract and their spasm.

If the symptoms persist for 4-5 days after the start of the procedure, it is recommended that you consult a doctor.

Side effects:

Disorders from the gastrointestinal tract:

Often (1,0- 10,0%) - nausea, decreased sensitivity in the oral cavity or pharynx; Infrequent (0,1-1,%) - dyspepsia, vomiting, diarrhea, abdominal pain, dry mouth;

Rarely (0.01 - 0.1%) - dryness in the throat.

Disorders of the immune system, lesions of the rut and subcutaneous tissues:

Rare (0.01 - 0.1%) - rash, hives; angioedema, anaphylactic reactions (including anaphylactic shock) *, itching *, hypersensitivity *.

Disorders from the nervous system:

Often (1,0 - 10,0%) - dysgeusia (a violation of taste sensations).

* These adverse reactions were observed with a wide application of the drug; with 95% probability, the incidence of these adverse reactions is infrequent (0.1-1.0%),but possibly lower; the exact frequency is difficult to assess, as they were not noted in clinical trials.

Overdose:

Specific symptoms of an overdose in humans are not described.

There are reports of accidental overdose and / or medical error, which resulted in symptoms of known side effects of the drug: nausea, dyspepsia, vomiting, diarrhea, abdominal pain. In this case, the need for symptomatic therapy.

Treatment: artificial vomiting, gastric lavage in the first 1-2 hours after taking the drug, symptomatic therapy.

Interaction:

Clinically significant, undesirable interactions with other drugs have not been reported.

With simultaneous use with amoxicillin, cefuroxime, erythromycin, ambroxol increases their concentration in the bronchial secretion.

Special instructions:

Ambroxol should not be taken concomitantly with antitussive drugs that hamper the excretion of sputum.

The solution contains a preservative benzalkonium chloride, which, when inhaled, can cause bronchospasm in sensitive patients with increased respiratory reactivity ways.

Ambroxol solution for ingestion and inhalation should not be mixed with cromoglycic acid and alkaline solutions. An increase in the pH of the solution above 6.3 can cause precipitation of ambroxol hydrochloride or the appearance of opalescence.

Patients who observe a hyponatric diet should take into account that the drug contains 42.8 mg of sodium in the recommended daily dose (12 ml) for adults and children over 12 years.

There are isolated reports of severe skin lesions, such as Stevens-Johnson syndrome and Lyell's syndrome, coinciding with the appointment of expectorants such as ambroxol chloride. In most cases, they can be explained by the severity of the underlying disease and / or concomitant therapy. Patients with Stevens-Johnson syndrome or Lyell syndrome in the early phase may experience fever, body pain, rhinitis, cough and sore throat. With symptomatic treatment, it is possible to erroneously prescribe anti-cold remedies. When new lesions of the skin and mucous membranes appear, it is recommended to stop treatment with the drug and immediately seek medical help.

If the kidney function is impaired, the drug should be used only on the advice of a doctor.

Effect on the ability to drive transp. cf. and fur:

There were no cases of drug effects on the ability to drive vehicles and mechanisms. Studies on the effect of the drug on the ability to drive vehicles and engage in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions have not been carried out.

Form release / dosage:

Solution for ingestion and inhalation 7.5 mg / ml.

Packaging:

To 4 ml in a tube-dropper with a valve.

To 50 ml, 100 ml in bottles of dark glass with a screw mouth, sealed with stoppers, droppers, polyethylene and screw caps, with the control of the first opening of polymeric materials.

Set:

10 tubes of IV drops with a drug, 10 tubes of IV drops with a solvent (sodium chloride 0.9%), with instructions for use are placed in a pack of cardboard.

A bottle of 50 ml, 100 ml with instructions for use and a measuring cup is placed in a pack of cardboard.

Storage conditions:

In a pack at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

5 years.

Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:Without recipe

Registration number:LP-004481

Date of registration:28.09.2017

Expiration Date:28.09.2022

The owner of the registration certificate:UPDATE OF PFC, CJSC UPDATE OF PFC, CJSC Russia

Manufacturer: & nbsp

UPDATE, PFC CJSC Russia

Information update date: & nbsp18.10.2017

Illustrated instructions

Instructions

Ambroxol (Ambroxol)