Instructions for use Salbroxol tablets blister pack No. 20
Composition
active ingredients: ambroxol hydrochloride, salbutamol sulfate;
1 tablet contains ambroxol hydrochloride (calculated as 100% substance) – 15 mg, salbutamol sulfate (calculated as 100% substance) – 4 mg;
Excipients: lactose monohydrate, crospovidone, calcium stearate, colloidal anhydrous silicon dioxide.
Dosage form
Pills.
Main physicochemical properties: round tablets, white in color, with a flat surface with beveled edges and a score.
Pharmacotherapeutic group
Drugs affecting the respiratory system. Drugs used in obstructive airway diseases. Salbutamol, combinations. ATX code R03A K04.
Pharmacological properties
Pharmacodynamics
A combined medicinal product, the therapeutic effect of which is due to the pharmacological properties of the active components that make up its composition.
Ambroxol is a secretolytic and secretomotor agent from the benzylamine group.
Normalizes pathologically altered formation of bronchial secretions by stimulating serous cells of the glands of the bronchial mucosa, resulting in an increase in the content of mucous secretions and a change in the ratio of mucous and serous components of sputum. Ambroxol activates hydrolyzing enzymes and enhances the release of lysosomes from Clark cells, changes the structure of bronchial secretions by reducing and fragmenting mucopolysaccharide fibers, selectively inhibits the absorption of sodium by the respiratory tract epithelium, which leads to a decrease in sputum viscosity. Enhances the movement of cilia of the ciliated epithelium of the bronchi, increasing mucociliary transport of sputum, which facilitates its discharge. In addition, ambroxol stimulates the synthesis of surfactant phospholipids by alveolar pneumocytes, has an antioxidant effect. Ambroxol penetrates well through the placental barrier and improves the synthesis of surfactant during intrauterine development of the fetus.
Salbutamol is a selective agonist of b2-adrenergic receptors. It has a bronchodilator effect, prevents and relieves bronchospasm, reduces airway resistance, increases vital capacity of the lungs. It increases the resistance of mast cells and basophils to degranulation upon contact with an allergen, thereby preventing the release of histamine, a slowly reacting substance of anaphylaxis, and neutrophil chemotaxis factor. Compared with other b2-adrenergic agonists, salbutamol has a less pronounced positive chrono- and inotropic effect on the myocardium, and practically does not change blood pressure and heart rate.
Pharmacokinetics
Ambroxol is rapidly and completely absorbed from the gastrointestinal tract after oral administration.
The pharmacological effect occurs 30 minutes after taking the drug, the maximum concentration in the blood plasma is detected after 1-3 hours and is maintained for 6-12 hours. The bioavailability of ambroxol is 30%. This is due to the effect of "first pass" through the liver. Binding to blood plasma proteins is approximately 85%.
Approximately 90% of ambroxol is excreted from the body as metabolites in the urine, less than 10% is excreted unchanged.
Salbutamol is poorly bound to plasma proteins, its oral bioavailability is 40-50%. The half-life of salbutamol and its active metabolite is 6 hours. Salbutamol metabolites are conjugated sulfates (42%), the main of which is salbutamol ester sulfate, which has a b2-adrenostimulating effect. Conjugated sulfates are excreted mainly in the urine and in small quantities in the bile.
Salbutamol and ambroxol penetrate the placental barrier and into breast milk.
Indication
Bronchial asthma; chronic obstructive bronchitis; pulmonary emphysema.
Contraindication
Hypersensitivity to the active substances or to any other components of the drug; severe tachyarrhythmia; severe arterial hypertension; acute heart failure, heart defects, myocarditis; convulsive syndrome; gastric and duodenal ulcer; glaucoma; pheochromocytoma; thyrotoxicosis; simultaneous use of β-blockers, especially non-selective ones; threat of abortion.
Interaction with other medicinal products and other types of interactions
Interactions related to ambroxol
Antitussives (e.g. codeine): suppress sputum discharge and excessive mucus accumulation while reducing cough. Therefore, such a combination is possible only after a careful assessment by a doctor of the ratio of the expected benefit and the possible risk of use.
Antibiotics (amoxicillin, cefuroxime, erythromycin, doxycycline): improving the delivery of antibiotics to the lung tissue.
Theophylline: increased plasma theophylline concentration.
Compatible with agents that inhibit labor activity (hexoprenaline, terbutaline).
Possible use with cardiac glycosides, diuretics, corticosteroids.
Interactions related to salbutamol
MAO inhibitors, ergotamine, tetracyclines, antidepressants, methylxanthines, furazolidone, procarbazine: simultaneous use is not indicated due to possible potentiation of adrenomimetic effects.
Antidiabetic agents: possible reduction of the hypoglycemic effect.
Halothane, methoxyflurane or enflurane: Salbutamol therapy should be discontinued at least 6 hours before anaesthesia with halogenated anaesthetics.
Adrenergic drugs, including sympathomimetics: use with caution to prevent cardiac dysfunction.
Diuretics, corticosteroids: possible development of serious hypokalemia.
Cardiac glycosides (e.g. digoxin): increased risk of arrhythmias; possibility of hypokalemia due to salbutamol use; decreased serum digoxin concentration.
Application features
When using mucolytic agents, including ambroxol hydrochloride, isolated cases of severe skin lesions, such as Stevens-Johnson syndrome and Lyell's syndrome (toxic epidermal necrolysis), have been reported. In most cases, these could be explained by the severity of the underlying disease and/or concomitant therapy. In addition, in the initial stage of Stevens-Johnson syndrome or Lyell's syndrome, patients may experience flu-like non-specific prodromal symptoms such as fever, body aches (malaise), rhinitis, cough, sore throat. As a result of their erroneous assessment, patients may have received drugs for the symptomatic treatment of cough and cold. For this reason, if skin and/or mucous membrane lesions occur during the use of ambroxol hydrochloride, the drug should be discontinued immediately and medical attention should be sought.
Increasing the dose or reducing the intervals between doses of the drug should be carried out under the supervision of a doctor. Reducing the interval is possible only in exceptional cases and must be strictly justified.
The drug should be used with caution in patients with renal and/or hepatic insufficiency (due to the possibility of accumulation of metabolites in the liver), risk factors for the development of arterial hypertension, ischemic heart disease or significant risk factors for the development of coronary heart disease, arrhythmia, tachycardia, chronic heart failure.
There is evidence of isolated cases of myocardial ischemia associated with the use of salbutamol. Attention should be paid to the assessment of symptoms such as shortness of breath and chest pain, which may be due to both cardiac and respiratory disease.
Potentially serious hypokalemia may result from agonist therapy
β2-adrenergic receptors. Particular caution is recommended in severe bronchial asthma, as this effect may be enhanced by hypoxia, concomitant use of xanthine derivatives such as theophylline, steroids, diuretics, cardiac glycosides. In this situation, it is recommended to monitor the level of potassium in the blood serum.
Salbroxol should be used with caution in patients with diabetes mellitus and blood sugar levels should be closely monitored. Like other β2-adrenoceptor agonists, salbutamol may cause an increase in blood glucose levels. In patients with diabetes mellitus, this may lead to the development of ketoacidosis. Concomitant use of corticosteroids may exacerbate this condition.
It should be remembered that the drug contains an active substance that may lead to a positive result in doping control.
The drug contains lactose, therefore patients with rare hereditary disorders of carbohydrate tolerance (congenital galactosemia, glucose-galactose malabsorption syndrome, lactase deficiency) should not take it.
Ability to influence reaction speed when driving vehicles or other mechanisms
During treatment, caution should be exercised when driving or operating machinery. Given that patients with hypersensitivity may experience adverse reactions (dizziness, drowsiness) when using the drug, while taking the drug, you should refrain from driving vehicles and performing other work that requires concentration.
Use during pregnancy or breastfeeding
The drug penetrates the placental barrier. Use in the first trimester of pregnancy is contraindicated. Despite the lack of reliable data on the negative impact on the fetus and infant, use in the second and third trimesters of pregnancy is possible if the expected positive effect for the mother outweighs the potential risk to the fetus/child.
The drug penetrates into breast milk, therefore it is not recommended for use during breastfeeding. If necessary, use of the drug should be discontinued.
Method of administration and doses
For internal use. Adults and children over 14 years of age should take 1 tablet.
3-4 times a day.
The drug should be taken between meals. The intervals between doses should be at least 6 hours.
For adults, if necessary, the dose of the drug can be increased to 2 tablets 4 times a day. The duration of treatment is determined by the doctor depending on the clinical picture of the disease.
Children
There is no experience with the use of the drug in children under 14 years of age.
Overdose
Symptoms: tachycardia, arrhythmia, sleep disturbances, chest pain, rapid heartbeat, tremor of the hands and whole body, agitation, increased fatigue, reactions from the digestive tract, including nausea and vomiting, salivation.
Severe complications are possible: arterial hypertension or hypotension, collapse, angioedema.
In some cases, hypokalemia may occur, so it is necessary to check the serum potassium level.
Treatment: symptomatic. Perform gastric lavage, use activated charcoal and laxatives to reduce unwanted absorption of the drug.
If necessary, use β1-blockers, but avoid high doses (in sensitive patients this may cause bronchospasm). Heart rate should be monitored. Antidote unknown.
Adverse reactions
Adverse reactions that may be associated with ambroxol
Digestive tract: dyspepsia, heartburn, nausea, vomiting, anorexia, abdominal pain, feeling of fullness of the stomach, diarrhea/constipation, hypersalivation, dry mouth, hypoesthesia of the oral and/or pharyngeal mucosa.
Respiratory system: rhinorrhea, dryness of the mucous membrane of the upper respiratory tract, shortness of breath (as a symptom of a hypersensitivity reaction).
Urinary system: dysuria.
Nervous system: dysgeusia (taste disorder).
Immune system, skin and subcutaneous tissue: hypersensitivity reactions, including pruritus, skin rash, urticaria, angioedema, anaphylactic reactions (including anaphylactic shock), drug fever, chills, other allergic reactions. Very rarely, erythema, severe skin lesions such as Stevens-Johnson syndrome and Lyell's syndrome may occur. In most cases, their occurrence could be explained by the severity of the underlying disease or the simultaneous use of another drug.
Other: reactions from the mucous membranes.
Adverse reactions that may be associated with salbutamol
Immune system: anaphylactic reactions, including urticaria, angioedema, bronchospasm, hypotension, collapse.
Skin and subcutaneous tissue: skin rash, itching, sweating.
Digestive tract: nausea, vomiting.
Metabolic disorders: hypokalemia (potentially the use of β2-adrenoceptor agonists can cause severe hypokalemia), increased blood glucose levels.
Nervous system: headache, dizziness, hyperactivity.
Cardiac disorders: tachycardia, palpitations, cardiac arrhythmias including fibrillation, supraventricular tachycardia and extrasystole; myocardial ischemia.
Vascular disorders: peripheral vasodilation.
Musculoskeletal system: tension, tremor of skeletal muscles (usually hands), muscle cramps.
Urinary system: difficulty urinating.
Expiration date
3 years.
Storage conditions
In the original packaging at a temperature not exceeding 25 ° C. Keep out of the reach of children.
Packaging
10 tablets in a blister, 2 blisters in a pack.
Vacation category
According to the recipe.
Producer
Public Joint Stock Company "Research and Production Center "Borshchagov Chemical and Pharmaceutical Plant".
Limited Liability Company "Agropharm".
Location of the manufacturer and its business address
Ukraine, 03134, Kyiv, Myru St., 17.
Ukraine, 08200, Kyiv region, Irpin city, Centralna st., 113-A.
