Fenspiride, instructions for use (Method and dosage)
The medicine is prescribed orally. Depending on the age and dosage form, the dosage regimen may vary.
Instructions for Fenspiride tablets
Adults are usually prescribed 80 mg of the drug, 2-3 times a day. The tablets are taken before meals with a sufficient amount of liquid. The duration of treatment depends on the recommendations of the attending physician.
Instructions for Fenspiride in the form of syrup
The daily dosage for adults is 80 mg of the active substance. As a rule, this is from 45 to 90 mg of syrup. The medicine is taken three times a day.
For children, the daily dosage is calculated based on the ratio of 4 mg per kg of child weight. This means that children weighing up to 10 kg can be given 10 to 20 mg of the drug per day. If necessary, the syrup can be dissolved in milk or juice. For children weighing over 10 kg, the daily dosage ranges from 30 to 60 ml. The course of treatment is prescribed by the doctor.
Indications for use
The drug is prescribed:
- for the treatment of laryngitis , bronchitis , nasopharyngitis , otitis , sinusitis or rhinotracheobronchitis ;
- for bronchial asthma as part of maintenance therapy;
- to eliminate unpleasant respiratory symptoms due to influenza , measles or whooping cough ;
- for chronic bronchitis with respiratory failure.
Fenspirid-LF tablets p/o 80 mg No. 10x3
Name
Fenspirid-LF tablet p/o 80 mg in container pack No. 10x3
Description
Round, white, film-coated, biconvex tablets.
Main active ingredient
Fenspiride
Release form
Film-coated tablets.
Dosage
80mg
special instructions
Taking Fenspiride-LF does not replace antibacterial therapy and cannot be a reason for delaying adequate prescription of antibacterial drugs. If symptoms persist or worsen while taking the drug, you should consult a doctor. Prescribe with caution to patients with severe renal failure. Due to the lactose content, the drug is not recommended for patients with congenital galactose intolerance, lactase deficiency or glucose-galactose malabsorption.
Indications for use
Treatment of symptoms of respiratory diseases (cough, sputum production). Treatment with fenspiride does not replace antibacterial therapy and cannot serve as a reason to delay adequate prescription of antibacterial drugs.
Directions for use and doses
For oral administration. Recommended for use by adults. The drug should be taken before meals. In adults: 1 tablet 2-3 times a day. The duration of treatment is determined by the doctor individually and depends on the course of the disease.
Use during pregnancy and lactation
Due to the lack of sufficient data, the use of fenspiride during pregnancy is not recommended. There is no reliable information about the excretion of fenspiride in breast milk. Women who are breastfeeding are not recommended to take the drug.
Use in pediatrics
The drug Fenspirid-LF is not intended for use in children.
Impact on the ability to drive vehicles and operate machinery
Special studies have not been conducted to assess the effect of taking fenspiride on the ability to drive a car and work with potentially dangerous mechanisms. The drug causes drowsiness and may affect the ability to drive vehicles and operate machinery, especially at the beginning of treatment.
Interaction with other drugs
Concomitant use with sedatives is not recommended due to potentiation of the sedative effect. Strengthens the sedative effect of drugs that block H1-histamine receptors (antihistamines). It is not recommended to drink alcohol during treatment.
Contraindications
Hypersensitivity to fenspiride or any of the components of the drug, pregnancy, lactation.
Compound
Each film-coated tablet contains: Active substance: fenspiride hydrochloride – 80 mg. Excipients: hydroxypropyl methylcellulose, magnesium stearate, colloidal silicon dioxide anhydrous, lactose monohydrate, calcium hydrogen phosphate dihydrate, opadry II 85F18422 (white): polyvinyl alcohol, titanium dioxide, polyethylene glycol, talc.
Overdose
When taking a large amount of the drug, the following symptoms may be observed: drowsiness or agitation, nausea, vomiting, sinus tachycardia. Treatment. Symptomatic therapy. It is necessary to perform gastric lavage and ECG monitoring.
Side effect
The frequency of adverse reactions listed below was determined using the following notation: very common (> 1/10), common (> 1/100 - 1/1000 - 1/10000 -
Storage conditions
In a place protected from moisture and light at a temperature not exceeding 25? C. Keep out of the reach of children.
Pharmacodynamics and pharmacokinetics
The medicine is a blocker of H1-antihistamine receptors , an antagonist of specific inflammatory mediators . Fenspiride hydrochloride inhibits the production of serotonin , bradykinin and histamine . When using large dosages of the drug, the intensity of the production of free radicals, cytokines, arachidonic acid metabolites, and tumor necrosis factor alpha decreases.
The drug has an antispasmodic effect similar to papaverine . During experimental studies, it was discovered that the drug has a teratogenic effect and can cause the development of a cleft palate .
In the gastrointestinal tract, Fenspiride is well and almost completely absorbed. It reaches its maximum concentration within 6 hours for the tablet form and 2.5 hours for the medicine in syrup form. The half-life is about 12 hours. The medicine is excreted through the kidneys and, to a much lesser extent, through the intestines.
Chemical properties
Fenspiride is a widely used bronchodilator . Most often it is used as part of the complex treatment of bronchial asthma and infectious and inflammatory diseases of the respiratory tract.
Fenspiride hydrochloride, what is this substance? The drug is most often found in various preparations in the form of hydrochloride. Molecular weight of the compound = 260.3 grams per mole. Fenspiride hydrochloride is available in the form of film-coated tablets or syrup for oral administration.
Fenspiride hydrochloride: experience of use in the treatment of ARI in children
Respiratory diseases account for up to 80% of diseases diagnosed in children. Acute respiratory infections (ARI) and influenza hold the top spot among these pathologies, followed by infectious and ENT diseases. At the same time, according to statistics, 20-25% of children in Russia can be classified as frequently ill, i.e. suffering from 6 to 12 episodes of upper respiratory tract infections per year. The high prevalence of upper respiratory tract infections is partly due to inadequate treatment, incl. simultaneous prescription of an unreasonably large number of drugs, mainly symptomatic therapy. However, it is possible to achieve high efficiency and safety in the treatment of infectious diseases of the upper and lower respiratory tract in children. Fenspiride hydrochloride allows you to solve this problem.
Infectious diseases of the upper and lower respiratory tract are the most common pathological condition in childhood. These diseases pose the greatest danger to a child in the first three years of life.
The main causative agents of ARI in children are various viruses, causing up to 65-95% of all acute respiratory tract infections. In particular, the most common pathogenic microorganisms that cause ARI include adenoviruses, rhinoviruses, respiratory syncytial viruses, influenza and parainfluenza viruses, coronaviruses, etc. In total, about 200 viruses are known to cause ARI. The infection is transmitted by airborne droplets; the incubation period averages two to three days, but can reach five days.
Regardless of the type of pathogen, ARI manifests itself at the level of general and local symptoms. Common manifestations of ARI include fever, chills, loss of appetite, malaise, weakness, etc. Local symptoms of ARI are sneezing, difficulty breathing through the nose, sore throat, runny nose and cough, i.e. various manifestations of inflammatory processes that begin in the mucous membranes of the respiratory tract.
When treating ARI, the main task is to stimulate the body's local immune defense factors. This is necessary to prevent the progression and spread of the disease, as well as the occurrence of complications. In children, prevention of complications of ARI is of particular importance. For example, common complications of upper respiratory tract infections include sinusitis, otitis media and tonsillopharyngitis. Moreover, due to the physiological immaturity of the child’s immune system, a “harmless cold” can cause the development of allergies, airway obstruction, pneumonia, diseases of the cardiovascular system and kidneys.
As a rule, in the treatment of acute respiratory infections in children, symptomatic therapy is used, the effect of which is aimed at reducing the severity of individual symptoms. Practice shows that this approach is wrong. At best, inadequate treatment leads to relapse of the disease. By the way, the prevalence of recurrent ARI in children of preschool and school age is 20-59%.
The most effective treatment regimen is a combination of drugs whose action is aimed at eliminating the cause of the disease and the mechanisms of its development. Thus, in case of ARI, it is necessary to use not only means that help stimulate the body’s immune response, quickly reduce swelling and hyperemia of the mucous membrane of the respiratory tract, but also eliminate cough, regulate the production and improve the discharge of sputum, and also prevent the development of hyperreactivity and irreversible changes in the mucous membrane of the respiratory tract . These drugs include, in particular, fenspiride hydrochloride, which has a complex anti-inflammatory effect on the mucous membrane of the respiratory tract.
The anti-inflammatory effect of fenspiride hydrochloride differs from the effects of non-steroidal anti-inflammatory drugs and glucocorticosteroids. Its action is that the drug blocks the transport of calcium ions into the cell, due to which the transformation cascade of arachidonic acid slows down, and this, in turn, leads to a decrease in the formation of inflammatory mediators such as prostaglandins, leukotrienes and thromboxanes. In addition, fenspiride hydrochloride is an antagonist of histamine H1 receptors and alpha1 adrenergic receptors.
With the use of fenspiride hydrochloride in children, there is a decrease in the formation of sputum and at the same time its faster discharge. This is especially important in childhood, since mucociliary clearance, i.e. removal of mucus from the upper respiratory tract due to the normal functioning of the ciliated (ciliated) epithelium is the main mechanism for cleansing the respiratory tract.
Fenspiride hydrochloride selectively has an anti-inflammatory effect on the upper and lower respiratory tract, helps reduce bronchial hyperreactivity and prevents disruption of their patency. Numerous clinical studies have confirmed the effectiveness of the drug both as monotherapy and in combination with other drugs. Moreover, as practice shows, in more than 70% of cases of ARI in children, monotherapy with fenspiride hydrochloride is possible. Thus, the use of fenspiride hydrochloride for tracheitis and bronchitis in ARI helps reduce the duration of periods of dry and wet cough in children to an average of 2-3 and 5 days, respectively. With the use of fenspiride hydrochloride, a dry cough quickly transforms into a wet cough, and the cough becomes more productive. Therefore, therapy with fenspiride hydrochloride in the vast majority of cases allows one to avoid prescribing additional mucolytics, mucokinetics, bronchodilators and antihistamines to sick children.
The effect of using fenspiride hydrochloride is observed literally from the first days of therapy, reaching a maximum by the 9th day of treatment, and this can be traced at the cellular level. This is evidenced by the results of a study conducted by specialists from the Department of Outpatient, Social Pediatrics and Neonatology of Saratov State Medical University. IN AND. Razumovsky. The researchers analyzed the percentage composition and quality of cells based on samples taken from the throat mucosa of children with ARI at the beginning and end of treatment. Children in one group took fenspiride hydrochloride in the form of syrup (Erespal®), in the second group they received complex therapy, incl. interferon inducers, mucolytics, mucokinetics, mucoregulators and antibiotics. During the analysis, the researchers paid special attention to the level of immune system cells such as neutrophils and macrophages in the mucus, since an increase in this level indicates the presence of an inflammatory reaction in the body. The results of the analysis showed that in the very first days of therapy in children taking Erespal®, the number of neutrophils on the mucous membrane decreased from 17.5 to 9.1%, and macrophages from 15.1 to 3.7%. At the same time, in children who did not receive this drug, the level of these cells, on the contrary, increased, i.e. the development of the inflammatory process continued. By the end of the study, in the group of children taking fenspiride hydrochloride, the number of neutrophils decreased in 92% and macrophages in 84%. This means that inflammation has been suppressed and restoration of the epithelial barrier and, accordingly, mucociliary clearance has begun. At the same time, in about a third of children who did not receive the drug, the number of neutrophils increased over the same period.
The safety of drugs is of particular importance for use in pediatrics, so fenspiride hydrochloride is certainly the drug of choice in the treatment of diseases of the upper and lower respiratory tract, even in newborns. Studies show that when treating ARI in children of different ages, the side effects of fenspiride hydrochloride, unlike other groups of anti-inflammatory drugs, are minimal. Moreover, taking into account all the features and advantages of fenspiride hydrochloride, the drug can be used during vaccination of children prone to an allergic reaction, for example, bronchial obstruction, 7-10 days before, during and 5-6 days after the administration of vaccines.
Reviews
Some reviews about drugs based on Fenspiride:
- "... Cough syrup was prescribed to my child when other standard medications did not help. Despite the “chemical composition” and the abundance of adverse reactions described in the instructions, the drug helped the child a lot. The syrup helped cope not only with a cough, but also with a lingering chronic runny nose. There were no side effects";
- “... After changing the climate and place of residence, I was faced with chronic bronchitis, gradually turning into pneumonia. The doctor prescribed these pills. I drank half the course and the cough and runny nose disappeared without a trace. However, during treatment I had severe weakness, drowsiness, and pain in the chest. After adjusting the dosage, the treatment began to be tolerated better”;
- “... I gave the syrup to my 3-year-old child during the flu to eliminate a cough and runny nose. However, after several days of taking the drug, the general condition noticeably worsened and the child lost consciousness. They didn’t continue the treatment; they didn’t notice any effect.”
Introduction
Respiratory diseases in children consistently occupy first place in the structure of morbidity.
According to the Federal State Statistics Service, in 2010–2013. their share accounted for approximately 63% of the total incidence of children under 14 years of age [1]. At the same time, acute respiratory infections (ARI) accounted for more than half of all acute diseases in childhood, and during epidemics - up to 90%. The main causative agents of ARI are a variety of respiratory viruses (more than 300 species): influenza and parainfluenza viruses, rhinovirus, adenovirus, respiratory syncytial virus, metapneumovirus, reovirus, coronavirus and many others. The possibilities of etiotropic therapy for ARI are limited, and therefore the main role in most cases is played by pathogenetic and symptomatic therapy, in particular anti-inflammatory therapy [2].
Pathogenesis of ARI
The pathogenesis of ARI is based on the inflammatory process in the mucous membrane of the respiratory tract, caused by the action of proinflammatory cytokines and mediators. The main cellular mediators of inflammation include eicosanoids, primarily the products of arachidonic acid metabolism, which occurs along two pathways: the cycloxygenase pathway, leading to the formation of prostaglandins, thromboxane A and prostacyclin, and the lipoxygenase pathway, which leads to the formation of leukotrienes. The biological action of these mediators causes various effects, in particular, expansion and increase in the permeability of microcirculatory vessels, resulting in exudation, leading to swelling of the mucous membrane and submucosal layer of the respiratory tract. As a result of alteration under the influence of viruses, the concentration of free histamine in tissues increases, affecting H1 and H2 receptors. Due to irritation of H-receptors, the influx of sodium and chlorine ions into the cells and, accordingly, the volume of secretion increases. In addition, as a result of cholinergic and α-adrenergic stimulation, the amount of secretion with a high concentration of glycoproteins increases, which causes a violation of the rheological properties of mucus. Also, as a result of the cytotoxic effect of viruses, ultrastructural changes in the cells and cilia of the ciliated epithelium occur. These factors lead to significant disruption of mucociliary transport [2–3]. In infectious diseases caused by certain viruses (rhino-, respiratory syncytial viruses), a key role in pathogenesis is played by pronounced infiltration of the mucous membrane of the respiratory tract with inflammatory cells [2].
Mechanism of action of fenspiride
Medicines that have an anti-inflammatory effect, in most cases, have a narrowly targeted mechanism of action, affecting only individual parts of the inflammatory process. A distinctive feature of fenspiride is that its action is aimed simultaneously at many parts of the inflammatory process [4]. To date, the mechanism of action of the drug has been well studied in experimental studies on cell cultures and laboratory animals.
Fenspiride has a similar effect to corticosteroids, inhibiting the activity of phospholipase A2, but not by enhancing the synthesis of the inhibitor protein, but by blocking the transport of calcium ions into the cell.
In turn, the lack of calcium ions inhibits the activity of phospholipase A2, causing a slowdown in the transformation cascade of arachidonic acid, which ultimately leads to a decrease in the formation of prostaglandins, leukotrienes and thromboxanes. As a result, the state of the microcirculatory system is normalized, and inflammatory changes in the mucous membranes of the respiratory system are reduced [3]. The blocking effect of fenspiride on calcium ion transport was established in studies on laboratory animals [5].
Fenspiride slows down the secretion of many proinflammatory cytokines, primarily tumor necrosis factor α, which stimulates the secretion of mucin by epithelial cells of the respiratory tract [6–7]. The drug reduces the formation of chemotaxis factors and interleukin-8, as a result of which the migration of inflammatory cells is reduced and the process of infiltration of the respiratory epithelium is significantly slowed down [3]. There is also evidence that fenspiride reduces the release of neuropeptides involved in the inflammatory process and bronchoconstriction [8]. It has been established that the drug is an antagonist of histamine H1 receptors and α1-adrenergic receptors, having the same affinity for them [9–10]. Fenspiride, like antihistamines, blocks H1-histamine receptors, as a result of which histamine effects such as spasm of bronchial smooth muscles, swelling of their mucous membrane, catabolism of arachidonic acid and the release of cytokines are reduced [11]. In addition, under the influence of the drug there is a decrease in the content of cyclic nucleotides (cGMP and cAMP) in the cell, which helps to reduce the flow of calcium ions into the cytoplasm. Fenspiride blocks α1-adrenergic receptors, which leads to bronchodilation, inhibition of phospholipases and a decrease in the rate of calcium ions entering the cell, and this in turn reduces the formation of inflammatory mediators [10, 12]. Blockade of α1-adrenergic receptors is accompanied by inhibition of the secretory activity of the mucous glands of the bronchial tree, a decrease in the number of cells secreting sputum, normalization of the volume of tracheal secretions and suppression of the cough reflex [10, 13–15].
The multidirectional effect of fenspiride on the inflammatory process, established in numerous studies, leads to an improvement in mucociliary transport and a decrease in bronchial hyperreactivity, which helps relieve airway obstruction and cough [16–18].
Efficacy and safety of fenspiride in children
Currently, a significant number of clinical studies are presented in the scientific literature, incl. pediatric patients with ARI.
The effectiveness and safety of fenspiride (Erespal) in pediatric practice were determined in a large-scale multicenter controlled study "ELF", conducted in 35 cities of Russia.
The study included more than 5.5 thousand children (average age - 5.2 years) with ARI of mild and moderate severity, who were divided into 2 groups. Patients of the main group received fenspiride in the form of syrup for 7–10 days (daily dose - 4 mg/kg body weight), the control group received symptomatic therapy at the discretion of the doctor. By the 7th day of treatment, recovery occurred in 71.3% of children in the main group and in 53.8% of the control group; significant improvement occurred in 12.2 and 23.4%, respectively. There was a significant difference between the groups in the dynamics of most ARI symptoms (p<0.01). The use of fenspiride has significantly reduced the number of antipyretic and antibacterial drugs. The drug was generally well tolerated, side effects were observed in 2.4% of patients, and only 0.4% of children required discontinuation of fenspiride [19].
Another comparative study examined the effectiveness and safety of fenspiride for young children (under 3 years of age) with ARI: 64 children in the main group received only treatment with fenspiride (Erespal), 30 children in the control group received symptomatic therapy. The initial data of patients in the main and control groups were comparable, in particular, cough was noted in 91% of children. In children receiving fenspiride, improvement was observed significantly faster: by the 4th day after the start of treatment, cough persisted in only 41% of patients in the main group, while in the control group - in 75% (p <0.05). In children with signs of bronchial obstruction, breathing with prolonged exhalation and dry wheezing disappeared by the 7th day of treatment in the main group and only by the 10–14th day in the control group. It should be noted that more than 95% of parents and doctors rated the effectiveness of fenspiride as “good” or “excellent” [20].
Also, the effectiveness of fenspiride was studied in 114 children who were hospitalized with ARI (68 children), community-acquired pneumonia and chronic nonspecific lung diseases. The comparison group included 46 patients who received various mucoactive drugs. Fenspiride therapy for ARI was carried out for 14 days, for other diseases - from 3 weeks to 3 months.
This study specifically examined the effect of fenspiride on the most common symptom of ARI – cough. In patients with ARI in the main group, the duration of cough was significantly shorter than in the comparison group - 3-12 and 7-16 days, respectively. It was noted that the use of fenspiride has a positive effect on both dry and wet cough [21].
In 2013, a study was presented that examined the effectiveness and safety of fenspiride (Erespal) in the complex treatment of acute obstructive bronchitis in hospitalized children.
The study included 60 children aged 2 to 4 years, who were divided into 2 equal groups: in the main group, patients received fenspiride as part of complex therapy from the first day of treatment in the hospital; in the control group, patients also received complex treatment, but without fenspiride. Complex treatment included bronchodilators, mucolytics, antiviral and immunotropic drugs. During the therapy, positive dynamics of clinical manifestations of the disease were noted in both groups. However, in the main group there were significantly shorter periods of reduction in the intensity and duration of cough (p<0.05), manifestations of respiratory failure (p<0.05), persistence of auscultatory changes in the lungs (p<0.01) and duration of hospital stay ( <0.01). When assessing the auscultatory pattern in the lungs, it was noted that on the 3rd day of treatment in children of the main group, the number of dry wheezing decreased significantly and wet rales appeared, whereas in patients of the control group this occurred only on the 5th day of treatment. Children in the main group were discharged from the hospital after 7–8 days, and children in the control group, in most cases, only after 12–14 days [22].
Of great interest is a randomized clinical trial that included 40 children (average age 8.2 years) with acute otitis media, one of the most common complications of ARI in children. Patients in both groups received the antibiotic amoxicillin; patients in the main group also received fenspiride for 10 days. In the main group, the treatment results were significantly better: regression of symptoms (ear pain, fever, etc.) was observed significantly faster, and hearing restoration was observed earlier. However, no side effects were noted during the study. This study showed not only the effectiveness and safety of fenspiride therapy, but also its synergy with an antibacterial drug [23].
Conclusion
Thus, the experimental data presented in the scientific literature indicate that fenspiride has a multidirectional anti-inflammatory effect, which determines the effect on various parts of the pathogenesis of various respiratory diseases, and clinical data confirm the high effectiveness and safety of the drug in children with acute respiratory infections. This allows us to recommend fenspiride for widespread use in everyday pediatric practice.
The original drug fenspiride Erespal is presented on the Russian market, which was used in clinical studies of the effectiveness and safety of use in children. The drug is available in the form of film-coated tablets (80 mg fenspiride) for use in children over 18 years of age and adults, as well as in the form of syrup (2 mg/ml fenspiride) for use in children from 2 to 18 years of age.
