Composition, form of production and packaging
? The solution for ingestion and inhalation is clear, colorless or slightly brownish in color.
Ambroxol hydrochloride 7.5 mg
Excipients: citric acid monohydrate - 2 mg, sodium hydrogen phosphate dihydrate - 4.35 mg, sodium chloride - 6.22 mg, benzalkonium chloride - 225 Ојg, purified water - 989.705 mg.
100 ml - bottles of amber glass (1) with a dropper of polyethylene and a screw cap made of polypropylene with control of the first opening, complete with a measuring cup - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2017.
Mucolytic and expectorant drug.
Studies have shown that ambroxol, the active ingredient of LazolvanВ®, increases secretion in the respiratory tract. Strengthens 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 COPD, long-term therapy with LazolvanВ® (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.
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. C max when ingested is achieved in 1-2.5 hours.
V d 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 dose taken internally, is subjected to the effect of "first passage" through the liver. Studies on microsomes of human liver showed that the isoenzyme CYP3A4 is the predominant isoform responsible for the metabolism of ambroxol to dibromoanthranilic acid. The remaining part of ambroxol is metabolized in the liver, mainly by glucuronization and by partial cleavage to dibromantranilic acid (approximately 10% of the administered dose), as well as a small number of additional metabolites.
The terminal T 1/2 ambroxol is about 10 hours. The total clearance is within 660 ml / min, the renal clearance accounts for about 8% of the total clearance. Using the method of introducing a radioactive label, it was 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.
Pharmacokinetics in specific patient groups
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.
Acute and chronic diseases of the respiratory tract, accompanied by the release of viscous sputum and violation of mucociliary clearance:
- Acute and chronic bronchitis;
- bronchial asthma with difficulty of sputum discharge;
Ingestion (1 ml = 25 drops).
Drops can be diluted in water, tea, juice or milk. You can apply the solution regardless of food intake.
Adults and children over 12 years of age - 4 ml (100 drops) 3 times / day; children aged 6 to 12 years - 2 ml (50 drops) 2-3 times / day; children aged 2 to 6 years- 1 ml (25 drops) 3 times / day; Children under the age of 2 years - 1 ml (25 drops) 2 times / day.
Adults and children older than 6 years - 1-2 inhalations of 2-3 ml of solution / day.
Children under the age of 6 years - 1-2 inhalations of 2 ml of solution / day.
LazolvanВ® solution for inhalation can be used using any modern equipment for inhalation (except for steam inhalers). To achieve optimal moistening with inhalations, the preparation is mixed with 0.9% sodium chloride solution 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 usually 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 of the respiratory tract and their spasm.
If the symptoms persist for 4-5 days after the beginning of the drug, it is recommended to consult a doctor.
On the part of the digestive system: often (1-10%) - dysgeusia (a violation of taste sensations), nausea, decreased sensitivity in the oral cavity or pharynx; infrequently (0.1-1%) - dyspepsia, vomiting, diarrhea, abdominal pain, dry mouth; rarely (0.01-0.1%) - dryness in the throat.
From the skin and subcutaneous tissues: rarely (0.01-0.1%) - rash, itching *.
Allergic reactions: rarely (0.01-0.1%) - hives; anaphylactic reactions (including anaphylactic shock) *, angioedema, * hypersensitivity *.
* - these adverse reactions were observed with a wide application of the drug; with 95% probability, the frequency of these adverse reactions is infrequent (0.1% -1%), but possibly lower; the exact frequency is difficult to estimate; they were not noted during clinical trials.
- I trimester of pregnancy;
- the period of lactation (breastfeeding);
- Hypersensitivity to ambroxol or other components of the drug.
With caution should be prescribed in the II and III trimesters of pregnancy, patients with renal and / or liver failure.
PREGNANCY AND LACTATION
Ambroxol penetrates the placental barrier. Preclinical studies showed no direct or indirect adverse effects on pregnancy, fetal / 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. Nevertheless, it is necessary to observe the usual precautions when applying the drug during pregnancy. Especially it is not recommended to take Lazolvan В® in the first trimester of pregnancy. In the II and III trimesters of pregnancy, the drug is only possible if the expected benefit to the mother exceeds the potential risk to the fetus.
Ambroxol can be excreted in breast milk. Despite the fact that undesirable effects in children who are breastfed were not observed, during lactation it is not recommended to use Lazolvan В® solution for ingestion and inhalation.
Preclinical studies of ambroxol showed no adverse effects on fertility.
APPLICATION FOR FUNCTIONS OF THE LIVER
With caution appoint with kidney failure.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
With caution appoint with liver failure.
APPLICATION IN ELDERLY PATIENTS
There is no clinically significant effect of age on the pharmacokinetics of ambroxol, so there is no reason to select a dose for these symptoms.
Do not use in combination with antitussive drugs that make it difficult to remove phlegm.
The solution contains benzalkonium chloride preservative, which, when inhaled, can cause bronchospasm in sensitive patients with increased reactivity of the respiratory tract.
Lazolvan В® 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 follow a diet with a reduced sodium content should take into account that Lazolvan В® solution for ingestion and inhalation contains 42.8 mg of sodium in the recommended daily dose (12 ml) for adults and children over 12 years of age.
There are isolated reports of severe skin lesions (Stevens-Johnson syndrome and toxic epidermal necrolysis) that coincide with the use of expectorants such as ambroxol hydrochloride. In most cases, they are due to the severity of the underlying disease and / or concomitant therapy. In patients with Stevens-Johnson syndrome or toxic epidermal necrolysis, fever, body pain, rhinitis, cough and sore throat may appear in the early phase. With symptomatic treatment, it is possible to erroneously prescribe anti-cold remedies. When developing new lesions of the skin and mucous membranes, the patient should stop treatment with ambroxol and immediately seek medical help.
If renal dysfunction is disturbed, LazolvanВ® should be used only on the advice of a physician.
Impact on the ability to drive vehicles and manage mechanisms
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.
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 Lazolvan В® : nausea, dyspepsia, vomiting, diarrhea, abdominal pain.
Treatment: provocation of vomiting, gastric lavage in the first 1-2 hours after taking the drug, symptomatic therapy.
No clinically relevant, undesirable interactions with other drugs have been reported.
Ambroxol increases penetration into the bronchial secret of amoxicillin, cefuroxime, erythromycin.
TERMS OF RELEASE FROM PHARMACY
The drug is approved for use as a means of OTC.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored out of reach of children, protected from light at a temperature of no higher than 25 В° C. Shelf life - 5 years.