Ascoril expectorant
Bromhexine
Should be used with caution in patients with gastric ulcers.
Patients should be warned about the possible increase in mucus secretion.
Only isolated cases of severe skin lesions, such as Stevens-Johnson syndrome and toxic epidermal necrolysis (TEN), have been reported in association with the use of expectorants, particularly bromhexine hydrochloride. Most of them can be explained by the severity of the underlying disease and/or the use of concomitant medications. In addition, at an early stage, Stevens-Johnson syndrome or TEN may manifest with nonspecific flu-like prodromal symptoms such as fever, aches, rhinitis, cough and sore throat. Diagnostic errors associated with these nonspecific influenza-like prodromal symptoms may lead to symptomatic treatment with cough and cold medications. Therefore, if skin or mucous membrane lesions occur, seek immediate medical attention and stop taking bromhexine hydrochloride as a precaution.
Guaifenesin
Do not use concomitantly with cough suppressants or combination cold medications.
Guaifenesin turns urine pink.
When used in excess, guaifenesin can cause the formation of kidney stones.
If urine is collected within 24 hours of taking guaifenesin, its metabolite may change the color of the urine, and 5-hydroxyindoleacetic acid (5-HIAA) and vanillylmandelic acid (VMA) may be detected in the laboratory.
Salbutamol
Bronchodilators should not be used as the sole or primary drug in the treatment of patients with severe or unstable bronchial asthma. In severe asthma, regular assessment of the condition, including testing of lung function, is necessary, as patients are at risk of severe attacks and even death. Physicians treating such patients should consider prescribing oral corticosteroids and/or the maximum recommended dose of inhaled corticosteroids.
If treatment becomes ineffective, patients should seek medical attention.
The dose or frequency of use should be increased only as recommended by a physician.
Patients taking salbutamol may also take short-acting bronchodilators to relieve symptoms.
An increased need for bronchodilators, especially short-acting inhaled beta2-agonists, to relieve asthma symptoms indicates worsening disease control. Patients should be instructed to seek medical attention if treatment with short-acting bronchodilators becomes less effective or if they require more inhalations than usual.
In such a situation, the patient's condition should be re-evaluated and the need for an enhanced course of anti-inflammatory therapy (for example, higher doses of inhaled glucocorticosteroids or a course of oral glucocorticosteroid therapy) should be decided. Treatment of severe exacerbations of bronchial asthma should be carried out in the general manner.
Patients should be warned that if the effect of the usual treatment of an attack is weakened, as well as if the usual time of action of the drug decreases, they should not increase the dose or frequency of use, but seek medical help.
Salbutamol causes peripheral vasodilation, which may be accompanied by reflex tachycardia and increased cardiac output. It should be used with caution in patients suffering from angina pectoris, severe forms of tachycardia or thyrotoxicosis.
Cardiovascular effects may be observed with the use of sympathomimetics, including salbutamol. Based on some data obtained during post-marketing use, as well as published data, rare cases of myocardial ischemia associated with salbutamol have been noted. Patients with underlying severe heart disease (eg, coronary artery disease, arrhythmia, or severe heart failure) using salbutamol should be warned to seek medical attention if chest pain or other symptoms suggestive of worsening heart disease occur. Care must be taken to evaluate symptoms such as shortness of breath or chest pain, as they may be of either respiratory or cardiac origin.
Treatment of severe exacerbations of bronchial asthma should be carried out in the usual way.
Use with caution in conjunction with anesthetics such as chloroform, cyclopropane, halothane and other halogen-containing drugs.
Salbutamol should not cause difficulty urinating, since it does not stimulate alpha-adrenergic receptors, unlike sympathomimetic drugs such as ephedrine. However, difficulty urinating has been reported in patients with prostatic hypertrophy.
Potentially serious hypokalemia may occur when beta2-agonists are administered primarily parenterally or via nebulizer. It is recommended to use special caution when treating severe exacerbations of bronchial asthma, since hypokalemia may be exacerbated by hypoxia and the simultaneous use of xanthine derivatives and corticosteroids. In such situations, it is recommended to monitor the concentration of potassium in the blood serum.
Like other beta-adrenergic agonists, salbutamol can cause reversible metabolic changes, such as an increase in blood glucose concentrations. Patients with diabetes mellitus may be unable to compensate for increased blood glucose concentrations, and ketoacidosis has been reported in such patients. Concomitant use of corticosteroids may enhance this effect.
Use of the combined mucoregulator Ascoril for respiratory diseases
The formation of tracheobronchial secretion is an important protective mechanism that is disrupted when the mucous membrane of the respiratory tract is exposed to various infectious, chemical, physical and other factors. The removal of sputum is ensured by the movement of the cilia of the ciliated epithelium and the cough reflex. The source of tracheobronchial mucus formation is the bronchial glands, goblet cells, and the epithelium of terminal bronchioles and alveoli. The number of cells and glands producing secretions increases in the direction from the alveoli to the large bronchi. The ciliated epithelium of the respiratory tract ensures the constant movement of this secretion towards the oral cavity, due to which the evacuation of cellular debris, foreign particles and pathological agents occurs. Tracheobronchial secretion is one of the first lines of defense of the body from the effects of inhaled gases, dust, and microorganisms [1]. In its structure, tracheobronchial secretion consists of two phases: gel and sol. The gel, which is denser and more viscous, is located superficially and normally only touches the eyelashes. Sol is a more liquid layer, lies periciliary under the gel layer, in which the cilia of the ciliated epithelium move. The sol consists of gland secretions, capillary transudate, interstitial fluid and is an aqueous solution of various chemical compounds. This liquid has a viscosity similar to that of plasma. The thickness of the sol layer is 5 µm and is stable, since it provides good vibrations of the cilia immersed in it, which have a length of 5–6 µm. The composition of the gel layer of the secretion includes glycoproteins that are secreted by goblet cells. In addition, the secretion includes other proteins (lysozyme, albumin, a1-antitrypsin, etc.), secretory immunoglobulin class A (sIgA), a lipid complex, and surfactant, which play an important role in the adhesion of the secretion and affect the structure of the mucus. All elements of the gel layer are connected by disulfide, ionic and other bonds. The gel layer is located, as it were, on a “mat” of cilia immersed in liquid sol. The bronchial mucosa contains a large number of ciliated cells that make up the ciliated epithelium, which provide mucociliary transport. The effective beating of the cilia of the ciliated epithelium in the proximal direction occurs 2–3 times faster than their return movement. All cilia make about 1000 coordinated oscillatory movements per minute, which ensures the forward movement of mucus from bottom to top, while the speed of mucus movement increases with increasing distance from the alveoli. The function of the ciliated epithelium is negatively affected by many factors: tobacco smoke paralyzes the movement of cilia, inhalation of pure oxygen, ammonia, formaldehyde, hot air has an adverse effect, and the action of toxins of viruses and bacteria is damaging. In these cases, the coordination of the movement of cilia, the bioenergetics of cells and the efficiency of the ciliary impulse are disrupted. The function of cilia is also impaired in a sensitized organism. In addition to the coordinated work of cilia, effective mucociliary clearance requires appropriate rheological parameters of the secretion, primarily its viscosity and elasticity. Removing both too viscous and too liquid secretions is difficult. The viscosity and elasticity of the secretion depend on the amount of water in it and its constituent glycoproteins - mucins. It should be noted that secret mucins belong to two different subtypes: acidic (sialo- and sulfomucins) and neutral (fucomucins). During inflammation, the secretory function of the bronchial glands and goblet cells increases significantly, and the content of cell decay products, waste products and decay of microorganisms, and exudate in the bronchial secretion increases. The ratio of fucomucins and sialomucins increases, which leads to an increase in mucus viscosity. The latter inevitably leads to its stagnation, which in turn promotes the proliferation of bacteria. Under these conditions, the ciliated epithelium works with excessive load, but is not able to provide the necessary transport of mucus. Long-term overload leads to depletion of the functional capabilities of the mucociliary apparatus, dystrophy and atrophy of the ciliated epithelium. Bacterial enzymes and lysosomal proteases of destroyed cells can secondarily modify sialomucins and lead to their loss of the ability to form fibrous structures, which makes the secretion liquid and can cause it to flow down the bronchial wall due to loss of elasticity. Thus, the result of any irritative, infectious or allergic inflammation of the bronchial mucosa is a change in the amount and rheological properties of sputum, a violation of the drainage function of the bronchi [5]. Under different pathological conditions, the viscosity and elasticity of the secretion can change in different ways, which requires an individual approach to each patient and the choice of one or another drug that can affect the secretory function of the mucous membrane or the secretion itself. Summarizing the above, we can schematically depict the pathogenesis of mucostasis (Fig. 1). Thus, at the beginning of an acute inflammatory process accompanied by a dry cough, drugs that stimulate secretion are indicated; for an unproductive wet cough, drugs that dilute sputum are indicated; and for a productive wet cough, mucoregulators that normalize mucus formation and secretion composition are indicated. Therefore, the normalization of mucus formation and evacuation of bronchial secretions in most respiratory diseases is of great importance. The positive results obtained by normalizing mucus formation and overcoming mucostasis are presented in Figure 2. In many clinical situations, improvement in mucus formation occurs as a result of the use of the main means of treating each specific disease: antibiotics, corticosteroids, bronchodilators, etc. However, often the main means are not enough for quick and complete elimination of mucostasis. In such situations, in addition to the main drugs, mucolytic (secretolytic) agents are prescribed that improve the processes of mucus formation and sputum evacuation. In practice, doctors of various schools (classical medicine, homeopathy, oriental medicine, various branches of so-called “traditional medicine”) use more than a hundred remedies that have mucolytic properties. In principle, this large group of drugs is difficult to classify due to its heterogeneity. Conventionally, all drugs are divided according to their source of origin: herbal or synthetic, or according to the main mechanisms of their action: expectorants, thinning sputum, reducing the viscosity of sputum, stimulating secretion with new properties [4]. Drugs that facilitate the removal of mucus from the bronchi are traditionally divided into the following groups: 1. Drugs that stimulate expectoration. Cause irritation of stomach receptors and reflexively enhance the secretion of bronchial glands. 2. Mucolytics - drugs that depolymerize mucopolysaccharide and mucoprotein fibers in sputum and break the disulfide bonds of sputum proteins. 3. Mucoregulators - agents that regulate the production of secretions by glandular cells and act directly on the glandular cell. 4. Mucohydrants - drugs that promote hydration of secretions. 5. Bronchoroics - drugs that enhance transepithelial secretion of water. 6. Combination drugs that combine several drugs with different mechanisms of action to facilitate the removal of mucus from the bronchi. There are very few combination drugs that can affect several mechanisms of mucostasis at once. One of them is Ascoril (pharmaceutical company Glenmark) [6,7], which has a dual effect: bronchodilator and expectorant. Ascoril syrup contains salbutamol sulfate, bromhexine hydrochloride, guaifenesin and menthol. Salbutamol sulfate is a short-acting β2 agonist with pronounced bronchodilator and antispasmodic effects. Eliminates and prevents bronchospasm, reduces bronchial resistance. In some chronic respiratory diseases (BA, COPD, bronchiectasis, cystic fibrosis), along with the symptoms of mucostasis, bronchial obstruction is expressed, which significantly affects the speed and quality of sputum production. Viscous sputum aggravates bronchial obstruction, which in turn prevents the free separation of sputum. A combination of bronchodilator and mucolytic properties of β2-agonists can successfully “cut the Gordian knot”. In addition to its bronchodilator effect, salbutamol can have a direct effect on mucociliary transport, stimulating β2 receptors present in mucosecreting cells, and thereby leading to an increase in bronchial secretion. They also affect the ciliary apparatus of the bronchial epithelium, increasing their vibrations, which improves the evacuation of sputum. It should be remembered that orally taken salbutamol has slightly different pharmacokinetic properties than that used in aerosol form. Salbutamol taken orally has a high absorption rate. Eating reduces its rate, but does not affect bioavailability. 10% of salbutamol is bound to plasma proteins. The drug penetrates the placenta. The bioavailability of orally taken salbutamol is 50% (!). In this regard, Ascoril should be prescribed with caution to patients taking methylxanthines, MAO inhibitors and tricyclic antidepressants (possibility of tachyarrhythmia, drop in blood pressure). It is not recommended to take simultaneously with non-selective β-blockers. Another active component of Ascoril is guaifenesin. Guaifenesin is a unique substance that combines mucolytic and reflex actions, irritating the stomach receptors and thereby stimulating the gastropulmonary reflex, thereby increasing the secretion of the bronchial glands and the activity of the cilia of the ciliated epithelium. Another property of guaifenesin is its ability to reduce the surface tension of the structures of the bronchopulmonary apparatus and stimulate secretory cells of the bronchial mucosa that produce neutral polysaccharides. It depolymerizes acidic mucopolysaccharides and reduces the viscosity of sputum. This diverse mechanism of action of guaifenesin facilitates the removal of phlegm and promotes the transition of a nonproductive cough to a productive one. Absorption from the gastrointestinal tract is rapid (25–30 minutes after oral administration). T1/2 – 1 hour. Penetrates tissues containing acidic mucopolysaccharides. Approximately 60% of the administered drug is metabolized in the liver. It is excreted by the lungs (with sputum) and the kidneys, both unchanged and in the form of inactive metabolites. It is recommended to drink enough fluids while taking guaifenesin. The drug should not be used if you have a cough with copious sputum discharge. The third component of Ascoril is bromhexine, a mucolytic agent that has an expectorant and antitussive effect. Bromhexine is a “classic”, long-known mucolytic drug, which is a derivative of the alkaloid vasicine. Its mucolytic effect is associated with the depolymerization of mucoprotein and mucopolysaccharide fibers. Increases the serous component of bronchial secretions, activates the cilia of the ciliated epithelium, reduces the viscosity of sputum, increases its volume and improves discharge. One of the unique properties of bromhexine is the stimulation of the synthesis of endogenous surfactant and the penetration of the antibiotic into the lung tissue. Such unique qualities of bromhexine often make it the drug of choice for the treatment of pneumonia and brochiectasis. When taken orally, it is almost completely (99%) absorbed from the gastrointestinal tract within 30 minutes. Bioavailability is low (first pass effect through the liver). Penetrates through the placental and blood-brain barriers. In the liver, the drug undergoes demethylation and oxidation, and is metabolized to the pharmacologically active ambroxol. T1/2 – 15 hours (due to slow reverse diffusion from tissues). Excreted by the kidneys. In chronic renal failure, the elimination of metabolites is impaired. May accumulate with repeated use. The fourth component of Ascoril syrup is menthol, which contains essential oils that have a soothing, mild antispasmodic and antiseptic effect. Thus, Ascoril is a unique combination of substances that simultaneously have a bronchodilator, expectorant and mucolytic effect. Indications. As part of combination therapy for acute and chronic bronchopulmonary diseases, accompanied by the formation of difficult-to-separate viscous secretions: • BA; • tracheobronchitis; • COPD; • pneumonia; • emphysema; • whooping cough; • pneumoconiosis; • pulmonary tuberculosis. Contraindications: • hypersensitivity to the components of the drug; • pregnancy; • lactation period; • tachyarrhythmia; • myocarditis; • heart defects; • decompensated diabetes mellitus; • thyrotoxicosis; • glaucoma; • liver or kidney failure; • peptic ulcer of the stomach and duodenum in the acute stage; • stomach bleeding; • arterial hypertension; • children under 6 years of age. Prescribe with caution to patients with diabetes mellitus, gastric and duodenal ulcers in remission. Dosage regimen. Inside. Adults and children over 12 years of age are prescribed 1 tablet 3 times a day. Drug interactions. Other β2-adrenergic agonists and theophylline enhance the effect of salbutamol and increase the likelihood of side effects. Ascoril is not prescribed simultaneously with drugs containing codeine and other antitussives, as this makes it difficult to clear liquefied sputum. Bromhexine, which is part of Ascoril, promotes the penetration of antibiotics (erythromycin, cephalexin, oxytetracycline) into the lung tissue. It is not recommended to use Ascoril simultaneously with non-selective β-adrenergic receptor blockers, such as propranolol. Salbutamol, which is part of Ascoril, is not recommended for patients receiving MAO inhibitors. Diuretics and corticosteroids enhance the hypokalemic effect of salbutamol. It is not recommended to take alkaline drinks at the same time as Ascoril. Such diversity and multiplicity of action of Ascoril determine the advisability of its use in almost all diseases of the respiratory system with symptoms of mucostasis. Acute respiratory diseases. The term “acute respiratory diseases” (acute respiratory infections) combines influenza and a large group of diseases characterized by predominant damage to the respiratory tract. These diseases are caused by various, mainly viral etiological agents and are widespread in all countries of the world. On average, every adult gets sick with influenza or other acute respiratory diseases 2 times a year, a schoolchild – 3 times, a preschool child – 6 times. Mucostasis is a common occurrence in acute respiratory infections. In such cases, the use of Ascoril is an effective and safe method of correcting therapy [8–12]. Acute bronchitis. The diagnosis of “acute bronchitis” is made in the presence of an acute cough that lasts no more than 3 weeks, regardless of the presence of sputum, in the absence of signs of pneumonia and chronic lung diseases that may be the cause of the cough. The diagnosis is made by exclusion and is based on the clinical picture. For patients with acute bronchitis with a debilitating, unproductive cough, the administration of Ascoril helps alleviate symptoms and is a prevention of secondary bacterial complications [11,13]. Pneumonia. Bacterial pneumonia is a classic example of an infection of the alveoli involving the lower respiratory tract. In almost all pneumonias, the surfactant system is disrupted, and the severity of its damage is directly proportional to the severity of the pneumonia. The unique properties of Ascoril, aimed at correcting the synthesis of surfactant, significantly increase the effectiveness of the treatment of pneumonia. Chronic non-obstructive bronchitis is a very common disease among smokers, workers in hot shops and people working in dusty conditions. The main symptom of the disease is chronic cough (both without exacerbation and during exacerbation). Moreover, in the overwhelming majority of these patients, signs of mucostasis are detected, which are successfully compensated by the administration of Ascoril. COPD is one of the most insidious and widespread diseases of the respiratory system. Among the pathogenetic mechanisms of this disease, mucostasis occupies an important place, and it is not always possible to compensate for its phenomena with classical means of basic therapy. Some medications, such as corticosteroids, may worsen mucostasis. Among the many sanogenetic mechanisms of action of Ascoril, its ability to enhance the synthesis of sIgA, the level of which decreases as COPD progresses, is very important. At the same time, sIgA deficiency as a manifestation of local immunodeficiency is the most important factor favoring the colonization of pathogenic microorganisms and the progression of the disease. And if earlier the advisability of using mucoregulators for COPD was questioned, today, with obvious signs of mucostasis, the appointment of such a multifunctional mucoregulator as Ascoril is pathogenetically justified and brings positive results during exacerbation of the disease. So, in 2012 [18], the results of an open comparative study of the use of ascoril and the combination of salbutamol with bromhexin in the complex therapy of exacerbations of COPD were published, which showed a distinct advantage of the therapy using Ascoril. The authors showed that the speed of reducing the intensity of cough in the group of patients taking ascoril was statistically reliably higher than in patients of the comparison group. The use of ascoril is effective in stable COPD [6,14,15]. A special place among the indications for the purpose of ascoril is occupied by bronchiectatic disease and cystic fibrosis. The drug has an effective therapeutic effect on the drainage function of the airways, its use, especially in inhalations, is one of the means of treating these diseases. BA - a disease in which any drug should be prescribed with caution due to possible phenomena of paradoxical bronchospasm and aggravation of the severity of patients. Ascoril in numerous controlled studies showed its safety from the standpoint of aggravation of bronchial obstruction, therefore, in case of phenomena of mucosmostasis in patients with BA (and this is often observed with infectious complications), it is the drug of choice [16,17]. Pulmonary tuberculosis. In recent years, an interest in the pathogenetic therapy of patients with pulmonary tuberculosis has been revived in phthisitic practice. It is proved, for example, that compensation for bronchial obstruction, and its component is mucostasis, significantly increases the effectiveness of therapy for patients with tuberculosis. Fibrosting alveolitis is a heterogeneous group of diffuse lung diseases, in the chronic course of which the syndrome of the “cellular lung” with diffuse pneumosclerosis and bronchiectasis, which are characterized by fluent, are formed. Ascoria, along with other mucoregoers, is an integral component of the complex therapy of these pathological conditions. Thus, due to the multiplicity of the mechanisms of therapeutic effect on the basic pathogenetic mechanisms of respiratory diseases, regardless of their etiology, ascoria is a means of choosing in the complex therapy of diseases and syndromes accompanied by mucostasis.
Literature 1. Chuchalin A.G., Abrosimov V.N. Cough. Ryazan, 2002. 103 p. 2. Fedoseev G.B., Emelyanov A.V., Timchik V.G. Expectorant drugs as a means for the treatment of obstructive pulmonary diseases // New St. Petersburg Medical Gazette. 1997. No. 2. P. 60–61. 3. Belousov Yu.B., Moiseev V.S., Lepakhin V.K. Clinical pharmacology and pharmacotherapy. M.: Universum, 1993. 395 p. 4. Sinopalnikov A.I., Klyachkina I.L. Mucolytic therapy for chronic obstructive bronchitis / In the book: Chronic obstructive pulmonary diseases. M.: Binom, 1998. pp. 275–290. 5. Abrosimov V.N. Pulmonary clearance, breathing technique and kinesitherapy for patients with COPD. Ryazan, 2010. 6. Fedoseev G.B., Zinakova M.K., Rovkina E.I. Clinical aspects of the use of Ascoril in a pulmonology clinic // New St. Petersburg Medical Gazette. 2002. No. 2. P. 64–67. 7. Rovkina E.I. Efficacy and safety of the expectorant drug Ascoril. // New St. Petersburg Medical Gazette. 2000. No. 4. P. 54–55. 8. Okovity S.V., Anisimova N.A. Pharmacological approaches to antitussive therapy. RMJ. Respiratory tract diseases. 2011. No. 23. 9. Belousov Yu.B., Omelyanovsky V.V. Clinical pharmacology of respiratory diseases in children. Guide for doctors. M., 1996. 176 p. 10. Geppe N.A., Seliverstova N.A., Beraia T.T. and others. Improving cough therapy in children. // Issues of practical pediatrics. 2009. No. 4. pp. 20–25. 11. Samsygina G.A., Zaitseva O.V. Bronchitis in children. Expectorant and mucolytic therapy. A manual for doctors. M., 1999. 36 p. 12. Meshcheryakov V.V., Sinevich O.Yu., Pavlinova E.B. and others. Efficacy and safety of the oral form of salbutamol (using the example of the drug Ascoril) in the treatment of exacerbations of bronchial asthma in children // Pediatrics. 2003. No. 6. P. 68–70. 13. Okovity S.V., Gaivoronskaya V.V., Kulikov A.N., Shulenin S.N. Clinical pharmacology. Selected lectures. M., 2008. P. 608. 14. Ainapure SS, Desai A., Korde K. Efficacy and safety of Ascoril in the management of cough – National Study Group report // J Indian Med Assoc. 2001. Vol. 99. R. 111, 114. 15. Jayaram S., Desai A. Efficacy and safety of Ascoril expectorant and other cough formula in the treatment of cough management in pediatric and adult patients – a randomized double–blind comparative trial // J Indian Med Assoc. 2000. Vol. 98. R. 68–70. 16. Prabhu Shankar S., Chandrashekharan S., Bolmall CS, Baliga V. Efficacy, safety and tolerability of salbutamol + guaiphenesin + bromhexine (Ascoril) expectorant versus expectorants containing salbutamol and either guaiphenesin or bromhexine in productive cough: a randomized controlled comparative study // J Indian Med Assoc. 2010. Vol. 108. R. 313–314, 316–318, 320. 17. Korzh A.N., Krasnokutsky S.V., Vaskiv N.N. Use of the drug Ascoril in the treatment of patients with chronic obstructive pulmonary disease // Consilium Medicum Ukraine. 2007. No. 4. 18. Klyachkina I.L., Dmitriev Yu.K. Treatment of mild exacerbations of chronic obstructive pulmonary disease // Clinical medicine. 2012. No. 3. pp. 79–82.
Cofasma syrup 200ml fl
Pharmacological properties:
The combined drug has a bronchodilator, expectorant and mucolytic effect. Salbutamol is a bronchodilator that stimulates beta-2 adrenergic receptors in the bronchi, blood vessels and myometrium. Prevents or eliminates bronchospasm, reduces resistance in the respiratory tract, and increases vital capacity of the lungs (VC). Causes expansion of the coronary arteries, does not reduce blood pressure (BP).
Bromhexine is a mucolytic agent that has an expectorant effect. Increases the serous component of bronchial secretions; activates the cilia of the ciliated epithelium, reduces the viscosity of sputum, increases its volume and improves discharge.
Guaifenesin is a mucolytic agent that reduces the surface tension of the structures of the bronchopulmonary apparatus; stimulates secretory cells of the bronchial mucosa that produce neutral polysaccharides, depolymerizes acidic mucopolysaccharides, reduces the viscosity of sputum, activates the ciliary apparatus of the bronchi, facilitates the removal of sputum and promotes the transition of an unproductive cough to a productive one.
Pharmacokinetics:
Salbutamol.
Absorption and distribution: after oral administration, absorption is high. The bioavailability of salbutamol taken orally is about 50%. Eating reduces the rate of absorption but does not affect bioavailability.
Communication with plasma proteins - 10%. Penetrates through the placental barrier.
Metabolism and excretion: undergoes first-pass metabolism in the liver and intestinal wall, and is inactivated by phenolsulfotransferase to 4-o-sulfate ester. The half-life (T1/2) is 3.8-6 hours. It is excreted in the urine (69-90%), mainly in the form of an inactive phenol sulfate metabolite (60%) within 72 hours and in bile (4%).
Bromhexine.
Absorption and distribution: when taken orally, it is almost completely (99%) absorbed in the gastrointestinal tract within 30 minutes. Bioavailability is low (first pass effect through the liver). Penetrates the placental barrier and the blood-brain barrier (BBB).
Metabolism and excretion: in the liver it undergoes demethylation and oxidation, metabolized to the pharmacologically active ambroxol. T1/2 -15 hours (due to slow reverse diffusion from tissues). Excreted by the kidneys. In chronic renal failure, the excretion of metabolites is impaired. May accumulate with repeated use.
Guaifenesin.
Absorption and distribution: absorption from the gastrointestinal tract is rapid (25-30 minutes after oral administration). Penetrates into tissues containing acidic mucopolysaccharides.
Metabolism and excretion: approximately 60% of the administered drug is metabolized in the liver.
T 1/2 - 1 hour. Excreted by the lungs (with sputum) and the kidneys, both unchanged and in the form of inactive metabolites.
