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Manufacturers: Beaufour Ipsen International
Active ingredients
- Oxeladine
Disease class
- Acute pharyngitis, unspecified
- Acute laryngitis and tracheitis
- Influenza caused by an identified influenza virus
- Pneumonia without specifying the pathogen
- Bronchitis, not specified as acute or chronic
- Cough
- Whooping cough
Clinical and pharmacological group
- Not indicated. See instructions
Pharmacological action
- Antitussive (inhibiting the cough reflex)
Pharmacological group
- Antitussives
Pharmacological properties of the drug Paxeladin
Oxeladine citrate is an antitussive agent that has no chemical affinity for opioids and their derivatives, as well as antihistamines. Paxeladin selectively acts at the level of cough nerve centers. At a dose that has an antitussive effect, it does not depress the respiratory center, but, on the contrary, has a weak effect of normalizing breathing. Paxeladine does not have a hypnotic effect and does not affect psychomotor activity. Capsules: the maximum concentration in the blood plasma after taking the capsules is achieved after 4-6 hours, after which the drug is still in the bloodstream for 4 hours. Syrup: the maximum concentration of the drug in the blood is reached 1 hour after administration and remains for 4 hours.
On the possibilities of using acetylcysteine in therapeutic practice
In inflammatory diseases of the paranasal sinuses and middle ear, the success of treatment primarily depends on the adequacy of the evacuation of pathological secretions. Of great importance in the treatment of sinusitis and otitis is the dilution of viscous and thick secretions, which can help normalize the condition of the mucous membrane and enhance local phagocytosis [4,5]. Mucolytic drugs in most cases are optimal in the treatment of respiratory diseases and are used to treat diseases of the upper and lower respiratory tract, accompanied by impaired sputum discharge, such as tracheitis, bronchitis, pneumonia, chronic bronchitis, bronchial asthma, cystic fibrosis, lung abscess. Also, drugs in this group are used for various ENT diseases (rhinitis, laryngotracheitis, sinusitis, otitis). Mucolytic drugs act on bronchial secretions and effectively dilute sputum without significantly increasing its quantity. In therapeutic practice, mucolytics based on acetylcysteine (AC) are quite widespread. This is due to the fact that AC is a highly effective mucolytic with antioxidant and antitoxic properties with a good safety profile, which determines the indications for its use in patients with bronchopulmonary pathology [6]. The structure of AC contains sulfhydryl groups, which contribute to the rupture of disulfide bonds of acidic mucopolysaccharides of sputum, which leads to a decrease in the viscosity of mucus. This is the main mechanism of action of the drug; in addition, the drug has a stimulating effect on mucosal cells, the secretion of which has the ability to lyse fibrin [7]. AC also helps to liquefy pus and thereby improve its evacuation from the respiratory tract. Thus, for bacterial infections, AC can be used as a drug of first choice. AC has the ability to inhibit bacterial adhesion to the epithelium of the upper respiratory tract, significantly reducing the incidence of infectious complications by reducing colonization of mucous membranes with bacteria and viruses. Thus, AC has three main effects: mucolytic, antioxidant and antitoxic. The anti-oxidant effect is associated with the presence of acetylcysteine nucleophilic thiol SH-group, which easily donates hydrogen, neutralizing oxidative radicals. The drug promotes the synthesis of glutathione, the main antioxidant system of the body, which increases the protection of cells from the damaging effects of free radical oxidation, characteristic of an intense inflammatory reaction [8]. Maintaining an adequate concentration of glutathione in the intercellular fluid is necessary to prevent the damaging effects of toxic agents, and its synthesis, which occurs in the liver and lungs, is determined by the availability of cysteine. With a decrease in concentration or an increased need for glutathione, its level can be increased due to the delivery of cysteine from exogenous AC. As a result, inflammation of the bronchi and the severity of clinical symptoms are reduced, and the effectiveness of treatment of inflammatory diseases of the bronchopulmonary system is increased. On the other hand, the direct antioxidant effect of AC has a significant protective effect against aggressive agents entering the body through respiration (tobacco smoke, urban smog, toxic fumes and other air pollutants). The antioxidant properties of AC provide additional protection of the respiratory system from the damaging effects of free radicals, endo- and exotoxins formed during inflammatory diseases of the respiratory tract. The drug does not cause “lung swamping” syndrome - stagnation of a large amount of sputum in the lungs, since it does not increase the volume of bronchial secretions, but makes it less viscous, thereby improving evacuation. The only exception is children in the first months of life: with inhalation administration of the drug it is quite rare, but an increase in the volume of sputum may be observed. Its use in combination with drugs that inhibit the cough reflex (codeine, oxeladine, prenoxdiazine and others) is not recommended. The drug should be used especially carefully in children of the first year of life who have an imperfect cough reflex and are prone to a rapid deterioration in mucociliary clearance. It should be noted that when using mucolytics, this is an extremely rare occurrence. AC is most often prescribed orally, as it is well absorbed and effective concentrations of the drug quickly reach the lungs. In surgical and endoscopic practice, AC is used endotracheally, through slow instillations, and, if necessary, parenterally - intramuscularly and intravenously. The effect of the drug begins in 30–60 minutes and lasts up to 4 hours. The effectiveness of AC use in patients with various pathologies of the bronchopulmonary system has been proven in many studies. Thus, according to the results of the randomized placebo-controlled multicenter BRONCUS study conducted in 2003, patients with COPD took AC for 3 years. A slowdown in the decline in FEV1 and vital capacity was found, especially in patients with severe disease [9]. Another study of oral AC conducted by the Swedish Lung Society showed that the drug was able to reduce the number of exacerbations in patients with COPD [10]. Another study assessed the incidence of hospitalization due to exacerbation of COPD - with AC use, 4 of 258 patients (1.6%) had to be hospitalized during the 24-week study period, and with placebo, 9 of 268 (3.4%) were hospitalized. When analyzing the effectiveness of AC treatment in patients with COPD, it was shown that while using the drug, 61.4% of patients reported an improvement in their condition, and only 34.6% when using placebo; the difference in favor of AC was statistically significant [11]. Another study revealed that there was no decrease in FEV1 during AC therapy, while patients’ assessment of their well-being showed significant positive dynamics [12]. Also, positive results were obtained when using AC as part of complex therapy in patients with interstitial lung diseases. Thus, the results of a randomized, double-blind, placebo-controlled study on the effectiveness of AC in patients with idiopathic interstitial pneumonia, IFIGENIA, demonstrated the advantages of adding AC to standard glucocorticosteroid therapy. In this study, idiopathic fibrosing alveolitis was morphologically verified in 155 patients (80 AC group and 75 placebo group). After 12 months, a slowdown in the decline in vital capacity and lung diffusion capacity was noted with AC intake compared with placebo (9 and 24%, respectively). In the AC group, mortality was 9% versus 11% in the placebo group [13]. Another comparative study of certain expectorants and mucolytic drugs in children suffering from acute and chronic bronchopulmonary diseases included 259 patients and was followed for 3 years [3]. The study included children from the first days of life to 15 years. Patients with acute and chronic bronchopulmonary pathology were included, of which 92 children received acetylcysteine granulate (trade name ACC-100, 200), 117 children received ambroxol in the form of tablets, syrup, inhalation and injection, 50 patients made up the comparison group (of which 30 patients were prescribed bromhexine, 20 – mucaltin). The timing of the appearance of a productive cough, a decrease in its intensity, and the timing of recovery were assessed. In addition, sputum viscosity was assessed. As a result of the observations, it was found that on the 2nd day after the appointment of AC, the cough increased somewhat, but became more productive; on the 3rd day of treatment, a weakening of the cough was noted and its disappearance on the 4-5th day of using the drug. Thus, as a result of the study, it was revealed that in children with acute bronchitis the best clinical effect was achieved when using AC. When prescribing bromhexine and ambroxol, a pronounced mucolytic effect was also noted, but at a later date than AC, from the start of treatment. Mucaltin had the least clinical effectiveness. The use of AC is limited not only to bronchopulmonary pathology and otolaryngology. The positive effect of AC in patients with nephropathy with the introduction of a contrast agent (in particular, during coronary angiography) has been shown. Thus, in the AC group, the probability of an increase in serum creatinine (by more than 25%) within 2 days after contrast administration was 68% lower than in the placebo group. In addition, when taking the drug, mean serum creatinine levels were significantly lower (p = 0.006) [14]. AC also has pronounced nonspecific antitoxic activity - the drug is effective against poisoning with various organic and inorganic compounds, where its detoxifying properties are used. Thus, AC is the main antidote for an overdose of paracetamol. Timely use of AC in case of paracetamol poisoning is necessary to stimulate the formation of glutathione in the liver, which prevents the development of liver necrosis. AC is effective if this therapy is started no later than 10–12 hours after taking the drug, but after 16–20 hours the effect is doubtful [15,16]. AC is also used for poisoning with dichloroethane, which is used as an organic solvent for the extraction of fats, waxes, paraffins, dry cleaning and as a starting product in the synthesis of certain compounds [17]. Regarding the safety profile of AC, it has been shown that in patients with respiratory tract diseases, the incidence of side effects requiring discontinuation of therapy is no higher than that of placebo [18]. The high safety of AC is associated with its composition - the drug is an amino acid derivative. In long-term clinical practice in both adults and children, the drug acetylcysteine - ACC - has proven itself well and is widely used. ACC compares favorably with other mucolytics not only by its properties that reduce viscosity and improve sputum drainage, but also by its antioxidant effects. ACC can be used in children from 2 years of age without a doctor's prescription. The drug is available in granules and effervescent tablets for preparing drinks, incl. hot, in dosages of 100, 200 and 600 mg and used 2-3 times a day. ACC in dosage form - granules for the preparation of syrup (100 mg of ACC per 5 ml of syrup) can be widely used in pediatric practice. This dosage form does not contain sugar or alcohol, has pleasant organoleptic properties and can be dosed with ACC for children under 2 years of age. The duration of the course depends on the nature and course of the disease and ranges from 3 to 14 days for acute pathologies, and 2–3 weeks for chronic diseases. If necessary, courses of treatment can be repeated. Injection forms of ACC can be used for intravenous, intramuscular, inhalation and endobronchial administration. In conclusion, it should be noted that the use of ACC in the complex treatment of respiratory diseases is a rational approach from the standpoint of modern medicine. The drug has a pronounced mucolytic effect, a good safety profile and a convenient dosage regimen. References 1. Principi N., Zavattini G. Possibility of interaction among antibiotics and mucolytics in children. // Int. J. Pharm.Res. – 1996. – VI. – No. 5. – R. 369–372. 2. Belousov Yu.B., Omelyanovsky V.V. Clinical pharmacology of respiratory diseases in children. Guide for doctors. Moscow, 1996, 176 p. 3. Samsygina G.A., Zaitseva O.V. Bronchitis in children. Expectorant and mucolytic therapy. A manual for doctors. Moscow, 1999, 36 p. 4. Piskunov S.Z. Russian rhinology. – 1993; 1:19–39. 6. Ryazantsev S.V. News of otorhinolaryngology and logopathology 1998; 4:90–92. 5. Tarasov D.I., Fedorova O.K., Bykova V.P. Diseases of the middle ear M. –1988. 6. Geppe N.A., Snegotskaya M.N., Nikitenko A.A. Acetylcysteine in the treatment of cough in children. // Pediatrics. Consilium medicum application. – 2007. – No. 2. – P. 43–47. 7. Zaitseva O.V. Mucolytics in the treatment of respiratory diseases in children. Consilium provisorum. vol. 3, no. 1, 2005. 8. Samsygina G.A. Antitussive therapy: a rational choice. In the world of drugs. No. 2, 1999. 9. Zuin R, Palamidese A, Negrin R, Catozzo L, Scarda A, Balbinot M High-dose N-acetylcysteine in patients with exacerbations of chronic obstructive pulmonary disease Clin Drug Investig. 2005;25(6):401–8. 10. Avdeev S.N., Chuchalin A.G. Conservative therapy for exacerbation of chronic obstructive pulmonary disease breast cancer, v. 5, no. 17, 1997. 11. Voznesensky N.A. based on materials: Dekhuijzen PNR // Eur. Respira. J. 2004. V. 23. No. 4. R. 629. Antioxidant properties and clinical effectiveness of Fluimucil (M-acetylcysteine) in COPD. Atmosphere. Pulmonology and Allergology No. 3, 2004. 12. Novikov Yu.K., Belevsky A.S. Mucolytics in the complex treatment of COPD. Attending doctor. No. 2, 2001. 13. Yachnik A.I., Monogarova N.E. Efficacy of acetylcysteine in the complex treatment of patients with COPD and idiopathic interstitial pneumonia https://www.medicusamicus.com/3. 14. Shamkhalova M.Sh., Zaitseva N.V., Kurumova K.O., Shestakova M.V. contrast-induced nephropathy in patients with diabetes mellitus Journal "Difficult Patient". Archive. No. 4, 2007. 15. Bennet PN, Brown MJ Clinical Pharmacology Tenth edition. 2008. P. 132 16. Sule AA, Tai DY, Tze CC, Deepa B, Leow MK. Potentially fatal paracetamol overdose and successful treatment with 3 days of intravenous N–acetylcysteine regime–a case report. Ann Acad Med Singapore. 2006 Feb;35(2):108–11. 17. Petrenko E.P. Military toxicology, radiobiology and medical defense. Tutorial. 18. Balyasinskaya G.L., Bogomilsky M.R., Lyumanova S.R., Volkov I.K. Use of Fluimucil® (N-acetylcysteine) for lung diseases Pediatrics. 2005. No. 6.
