Pharmacological properties of the drug Lazolvan
Ambroxol, the active ingredient in Lazolvan, increases the secretion of the glands of the respiratory tract. Ambroxol enhances the secretion of pulmonary surfactant and stimulates ciliary activity. This leads to improved mucus separation and elimination (mucociliary clearance). Activation of fluid secretion and increased mucociliary clearance facilitate the removal of bronchial secretions and reduce cough. The local anesthetic effect of ambroxol can be explained by its sodium channel blocking properties. In vitro studies have demonstrated that ambroxol reversibly and dose-dependently blocks neuronal sodium channels. These pharmacological properties, leading to a rapid reduction in the severity of pain and pain-related discomfort in the nasal cavity and trachea, are consistent with data from additional observation of symptoms in clinical studies of the effectiveness of ambroxol in the treatment of the upper respiratory tract. In vitro studies have demonstrated that the drug reduces the number of cytokines, as well as the number of tissue-associated mononuclear cells and polymorphonuclear cells. Pharmacokinetics. Absorption of all oral forms of ambroxol is rapid and fairly complete, with a linear dependence in the therapeutic range. The maximum level in blood plasma is reached after 0.5–3 hours. In the therapeutic range, about 90% of the drug binds to blood plasma proteins. When administered orally, the distribution of ambroxol from the blood to the tissues is rapid, with a high concentration of the active substance in the lung tissue. Clinical studies have shown that CYP 3A4 is the dominant isoenzyme that metabolizes ambroxol. Ambroxol is metabolized mainly in the liver by conjugation. The half-life from blood plasma is 10 hours. The total clearance is within 660 ml/min, renal clearance is about 8% of the total clearance. No evidence was found that age and gender affect the pharmacokinetics of ambroxol within clinically significant limits, so there is no need for any dose adjustment.
For what diseases is Lazolvan needed?
The medicine is indicated for use:
- for pneumonia;
- acute and chronic bronchitis;
- asthma with difficulty producing sputum;
- bronchial obstruction;
- respiratory distress syndrome;
- other pathologies of the respiratory tract, accompanied by excessive secretion synthesis.
Lazolvan improves well-being and makes breathing easier, but does not affect pathogens. It can only be used as a symptomatic remedy.
Use of the drug Lazolvan
The following dosage regimen is recommended: tablets. Adults and children over 12 years of age: 1 tablet 3 times a day. The therapeutic effect can be increased by using 2 tablets 2 times a day. The tablets should be taken after meals and washed down with water. The duration of treatment depends on the nature of the disease and the effectiveness of the therapy. Syrup. Adults and children over 12 years of age: 10 ml (2 teaspoons) 2 times a day. The syrup is recommended to be consumed with meals. Treatment period is up to 14 days. You should consult your doctor if symptoms of the disease last more than 14 days and/or worsen despite taking Lazolvan syrup. Capsules. Adults: 1 capsule is the daily dose; it should be taken in the morning or evening after meals. Capsules must be swallowed whole, without chewing, with plenty of liquid. Treatment period is up to 14 days. You should consult your doctor if symptoms of the disease last more than 14 days and/or worsen despite taking Lazolvan Retard capsules.
How Lazolvan works
The medicine increases the volume and production of secretions, promoting its liquefaction, stimulates the work of epithelial cilia, helping to move phlegm out. The effect of aerosol particles of the drug begins 20–30 minutes after inhalation. After oral administration, the active substance begins to function within 2–3 hours.
The therapeutic effect lasts from 6 to 12 hours. The components of the drug are metabolized in the liver and leave the body within 10–15 hours. They do not accumulate in blood and tissues.
Side effects of the drug Lazolvan
As a rule, taking Lazolvan is well tolerated. Gastrointestinal disorders: mild manifestations of heartburn, dyspepsia, nausea, vomiting, diarrhea; disorders of the immune system, skin and subcutaneous tissues: skin rash, urticaria, angioedema, anaphylactic reactions (including anaphylactic shock) and allergic reactions. If lesions of the skin or mucous membranes progress, you should immediately consult a doctor and stop treatment with ambroxol. Severe skin lesions, such as Stevens-Johnson and Lyell syndromes, have been reported extremely rarely in association with the use of mucolytic agents such as ambroxol. As a rule, they could be explained by the severity of the underlying disease or the use of concomitant medications.
Special instructions for the use of the drug Lazolvan
Use during pregnancy and lactation. Ambroxol penetrates the placental barrier. Animal studies have not revealed direct or indirect negative effects on pregnancy, embryo/fetal development, childbirth or postnatal development. Extensive clinical experience with use after the 28th week of pregnancy has found no evidence of negative effects on the fetus. Despite this, the usual precautions should be followed when using medications during pregnancy. The use of Lazolvan is not recommended, especially in the first trimester of pregnancy. Ambroxol passes into breast milk. Therefore, Lazolvan is not recommended to be taken during breastfeeding. However, one should not expect a negative effect on an infant if the mother takes Lazolvan during breastfeeding. Lazolvan tablets contain 684 mg of lactose in the maximum recommended daily dose (120 mg). Patients with a rare form of hereditary galactose intolerance, Lapp lactose intolerance or glucose-galactose malabsorption should not take this drug. Lazolvan syrup does not contain sugar, so it can be prescribed to patients with diabetes; the syrup does not contain alcohol. Children under 12 years of age are recommended to use Lazolvan in the form of syrup. Residues of gelatin capsules, sometimes detected in feces, do not indicate the ineffectiveness of the drug (the active substance is released from the capsules during passage through the digestive tract). This dosage form, namely Lazolvan Retard extended-release capsules, should not be prescribed to children.
Lazolvan solution for oral administration and inhalation 7.5 mg/ml 100 ml
Registration Certificate Holder
SANOFI RUSSIA (Russia)
Dosage form
Medicine - Lasolvan® (Lasolvan®)
Description
Solution for oral administration and inhalation
transparent, colorless or slightly brownish.
1 ml
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 mcg, purified water - 989.705 mg.
100 ml - amber glass bottles (1) with a polyethylene dropper and a polypropylene screw cap with first opening control, complete with a measuring cup - cardboard packs.
Indications
Acute and chronic diseases of the respiratory tract, accompanied by the release of viscous sputum and impaired mucociliary clearance:
- acute and chronic bronchitis;
- pneumonia;
- COPD;
- bronchial asthma with difficulty in sputum discharge;
- bronchiectasis.
Contraindications for use
- hypersensitivity to ambroxol or other components of the drug;
- I trimester of pregnancy;
- lactation period (breastfeeding).
Carefully
Lazolvan® should be used during pregnancy (II and III trimesters), in case of renal and/or liver failure.
pharmachologic effect
Studies have shown that ambroxol, the active ingredient in Lazolvan®, increases secretion in the respiratory tract. Enhances the production of pulmonary surfactant and stimulates ciliary activity. These effects lead to increased mucus flow and transport (mucociliary clearance). Increasing mucociliary clearance improves sputum discharge and relieves cough.
In patients with COPD, long-term therapy with Lazolvan® (for at least 2 months) led to 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.
Drug interactions
No clinically significant, undesirable interactions with other drugs have been reported.
Ambroxol increases the penetration of amoxicillin, cefuroxime, and erythromycin into the bronchial secretions.
Dosage regimen
Oral administration (1 ml = 25 drops).
Drops can be diluted in water, tea, juice or milk. The solution can be used regardless of meals.
Adults and children over 12 years old
— 4 ml (100 drops) 3 times/day;
children aged 6 to 12 years
- 2 ml (50 drops) 2-3 times a day;
children aged 2 to 6 years
- 1 ml (25 drops) 3 times a day;
children under 2 years of age
- 1 ml (25 drops) 2 times a day.
Inhalations
Adults and children over 6 years old
— 1-2 inhalations of 2-3 ml of solution/day.
Children under 6 years of age
— 1-2 inhalations of 2 ml solution/day.
Lazolvan® solution for inhalation can be used using any modern equipment for inhalation (except steam inhalers).
To achieve optimal hydration during inhalation, the drug is mixed with 0.9% sodium chloride solution in a 1:1 ratio. Since during inhalation therapy a deep breath can provoke a cough, inhalations should be carried out in normal breathing mode. Before inhalation, it is usually recommended to warm the inhalation solution to body temperature. Patients with bronchial asthma are recommended to carry out inhalation after taking bronchodilators to avoid nonspecific irritation of the respiratory tract and their spasm. If symptoms of the disease persist within 4-5 days from the start of using the drug, it is recommended to consult a doctor.
Overdose
Specific symptoms of overdose in humans have not been described.
There have been reports of accidental overdose and/or medical error resulting in
symptoms
of known side effects of Lazolvan®: nausea, dyspepsia, vomiting, diarrhea, abdominal pain.
Treatment:
provocation of vomiting, gastric lavage in the first 1-2 hours after taking the drug, symptomatic therapy.
Side effect
From the digestive system:
often (1-10%) – dysgeusia (impaired sense of taste), 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%) – dry throat.
For the skin and subcutaneous tissues:
rarely (0.01-0.1%) – rash, itching*.
Allergic reactions:
rarely (0.01-0.1%) – urticaria; anaphylactic reactions (including anaphylactic shock)*, angioedema*, hypersensitivity*.
* these adverse reactions were observed with widespread use of the drug; with a 95% probability, the frequency of these adverse reactions is uncommon (0.1%-1%), but possibly lower; the exact frequency is difficult to estimate, because they were not noted in clinical studies.
special instructions
Should not be used in combination with antitussives that impede the removal of sputum.
The solution contains the preservative benzalkonium chloride, which, when inhaled, may cause bronchospasm in sensitive patients with increased respiratory tract reactivity.
Lazolvan® solution for oral administration and inhalation is not recommended to be mixed with cromoglycic acid and alkaline solutions. An increase in the pH value of the solution above 6.3 may cause precipitation of ambroxol hydrochloride or the appearance of opalescence.
Patients on a low-sodium diet should take into account that Lazolvan® solution for oral administration 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 coincided with the use of expectorants such as ambroxol hydrochloride. In most cases, they are explained by the severity of the underlying disease and/or concomitant therapy. Patients with Stevens-Johnson syndrome or toxic epidermal necrolysis may present with fever, body aches, rhinitis, cough, and sore throat in the early phase. With symptomatic treatment, it is possible to erroneously prescribe anti-cold medications. If new lesions of the skin and mucous membranes develop, the patient should stop treatment with ambroxol and immediately seek medical help.
If renal function is impaired, Lazolvan® should be used only on the recommendation of a doctor.
Effect on the ability to drive vehicles and machinery
There were no cases of the drug influencing the ability to drive vehicles and machinery. 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 conducted.
Storage conditions
The drug should be stored in its original packaging out of the reach of children at a temperature not exceeding 25°C.
Best before date
Shelf life: 5 years.
Use during pregnancy and breastfeeding
Restrictions during pregnancy - With caution. Restrictions when breastfeeding - Contraindicated.
Ambroxol penetrates the placental barrier. Preclinical studies have not revealed direct or indirect adverse effects on pregnancy, embryonic/fetal, postnatal development and labor.
Extensive clinical experience with the use of ambroxol after the 28th week of pregnancy has not found evidence of a negative effect of the drug on the fetus. However, the usual precautions should be taken when using the drug during pregnancy. It is especially not recommended to take Lazolvan® in the first trimester of pregnancy. In the second and third trimesters of pregnancy, the use of the drug is possible only if the expected benefit to the mother outweighs the potential risk to the fetus.
Ambroxol can be excreted in breast milk. Despite the fact that no undesirable effects were observed in breastfed children, it is not recommended to use Lazolvan® solution for oral administration and inhalation during lactation.
Preclinical studies of ambroxol did not reveal any negative effects on fertility.
Use for renal impairment
Restrictions for impaired renal function - With caution.
Carefully
prescribe for renal failure.
Use for liver dysfunction
Restrictions for liver dysfunction - With caution.
Carefully
prescribe for liver failure.
Use in elderly patients
Restrictions for elderly patients - No restrictions.
No clinically significant effect of age on the pharmacokinetics of ambroxol was found, so there is no basis for selecting the dose based on these characteristics.
Use in children
Restrictions for children - No restrictions.
Terms of sale
The drug is available without a prescription.
Contacts for inquiries
SANOFI (Unknown)
Representative office of JSC "Sanofi-aventis group" (France) 125009 Moscow, st. Tverskaya, 22 Tel. Fax
