Name:
Amoxicillin. Forms of releasetablets МННАmoxicillin FTGAntibiotic; semi-synthetic penicillin
Description:
Round, biconvex, film-coated tablets from white to almost white, with a slight characteristic odor (for tablets containing 125 mg of amoxicillin); oval biconvex tablets, coated from white to almost white, scored on both sides, with a slight characteristic odor (for tablets containing 250 mg, 500 mg, 750 mg, 1000 mg amoxicillin). Composition Each coated tablet contains: tablet core: active ingredient: amoxicillin (as amoxicillin trihydrate) – 125 mg, or 250 mg, or 500 mg, or 750 mg, or 1000 mg; excipients: povidone, sodium starch glycolate (type A), magnesium stearate, microcrystalline cellulose; tablet shell: hypromellose, talc, titanium dioxide, macrogol 400. Pharmacotherapeutic group Antibacterial agents for systemic use. Beta-lactam antibiotics, penicillins. Broad spectrum penicillins. ATC code: J01CA04. Pharmacological properties Amoxicillin is a broad-spectrum semi-synthetic penicillin (beta-lactam antibiotic) that inhibits one or more enzymes involved in the biosynthesis of peptidoglycan in bacteria. Peptidoglycan is an integral structural component of the bacterial cell wall. Inhibition of peptidoglycan synthesis leads to weakening of the strength of the cell wall, which usually results in cell lysis and death. Thus, amoxicillin has a bactericidal effect. Amoxicillin can be broken down by beta-lactamases, enzymes produced by antibiotic-resistant bacteria. Therefore, the spectrum of action of amoxicillin (when used in monotherapy) does not include microorganisms that are capable of producing these enzymes. The main mechanisms that provide bacterial resistance to amoxicillin are: inactivation by bacterial beta-lactamases; a change in the structure of penicillin-binding proteins, which reduces the affinity of the antibiotic for the target. Bacterial impermeability or efflux mechanisms may cause or promote bacterial resistance, especially in Gram-negative bacteria. Minimum inhibitory concentration (MIC) values for amoxicillin according to the European Committee for Antimicrobial Susceptibility Testing (EUCAST). Microorganism MIC values (mg/l) Sensitive Resistant >Enterobacteriaceae 81 8 Staphylococcus spp. Note2 Note2 Enterococcus spp. 4 8 Streptococcus groups A, B, C and G Note 4 Note 4 Streptococcus pneumoniae Note 5 Note 5 Group of green streptococci 0.5 2 Haemophilus influenzae 26 26 Moraxella catarrhalis Note 7 Note 7 Neisseria meningitidis 0.125 1 Gram-positive anaerobes, except Clostridium difficile8 4 8 Gram-negative anaerobes 8 0 .5 2 Helicobacter pylori 0.1259 0.1259 Pasteurella multocida 1 1 Breakpoints regardless of species10 2 8 1 Wild-type Enterobacteriaceae are characterized as susceptible to aminopenicillins. Some countries prefer to characterize wild-type isolates of E. coli and P. mirabilis as intermediate susceptibility. If necessary, the MIC value for sensitive microorganisms S ≤ 0.5 mg/l is used. 2 Most staphylococci produce penicillinase, which makes them resistant to amoxicillin. Methicillin-resistant isolates, with rare exceptions, are resistant to all beta-lactam drugs. 3 Amoxicillin susceptibility can be determined from ampicillin data. 4 Group A, B, C, and G streptococcal susceptibility to penicillins is determined from benzylpenicillin susceptibility data. 5 Breakpoints apply only to “non-meningitis” isolates. For isolates with intermediate susceptibility to ampicillin, oral amoxicillin should be avoided. Sensitivity is determined by the MIC for ampicillin.6 Values are based on intravenous data. Beta-lactamase producing isolates should be considered resistant.7 Beta-lactamase producers should be considered resistant.8 Amoxicillin susceptibility can be determined from benzylpenicillin data. values regardless of species are based on data obtained with the introduction of at least 0.5 g 3 or 4 times a day (1.5-2 g per day). The prevalence of resistance may vary by geographic location and over time for certain species. It is desirable to focus on local information on resistance, especially when treating severe infections. If necessary, qualified advice should be sought if the local prevalence of resistance is such that the effectiveness of the drug in the treatment of specific types of infections is doubtful. In vitro sensitivity of microorganisms to amoxicillin Usually sensitive microorganisms are gram-positive aerobes: Enterococcus faecalis, beta-hemolytic streptococci (groups A, B, C and G), Listeria monocytogenes. 2. Microorganisms, the acquired resistance of which may be a problem in the treatment of infection: gram-negative aerobes: Escherichia coli, Haemophilus influenzae, Helicobacter pylori, Proteus mirabilis, Salmonella typhi, Salmonella paratyphi, Pasteurella multocida; gram-positive aerobes: coagulase-negative staphylococci, Staphylococcus aureus1, Streptococcus pneumoniae, a group of green streptococci; gram-positive anaerobes: Clostridium spp.; gram-negative anaerobes: Fusobacterium spp.; other microorganisms: Borrelia burgdorferi. 3. Microorganisms with natural resistance2: Gram-positive aerobes: Enterococcus faecium2; gram-negative aerobes: Acinetobacter spp., Enterobacter spp., Klebsiella spp., Pseudomonas spp.; gram-negative anaerobes: Bacteroides spp. (many strains of Bacteroides fragilis are resistant); other microorganisms: Chlamydia spp., Mycoplasma spp., Legionella spp. 1Almost all Staphylococcus aureus are resistant to amoxicillin due to penicillinase production. In addition, all methicillin-resistant strains are resistant to amoxicillin. 2Natural intermediate susceptibility in the absence of acquired resistance mechanisms. Simultaneous food intake does not affect the absorption of amoxicillin. Hemodialysis can be used to remove amoxicillin from the circulation. In animal studies, no significant retention of drug derivatives in body tissues was found. Amoxicillin, like most penicillins, can be found in breast milk (see section “Use during pregnancy and lactation”). Amoxicillin crosses the placental barrier (see section “Use during pregnancy and lactation”). The main route of elimination of amoxicillin is through the kidneys. In every child in the first week of life (including premature newborns), the interval between injections should be at least 12 hours (2 times a day) due to the immaturity of the renal excretion pathway. Since the elderly may experience a decrease in renal function, in this category of patients it is necessary to carefully select the dose and periodically monitor renal function. Indications for use Amoxicillin may be used in children and adults to treat the following infections: acute bacterial sinusitis; acute otitis media; acute streptococcal tonsillitis and pharyngitis; exacerbation of chronic bronchitis; community-acquired pneumonia; acute cystitis; asymptomatic bacteriuria in pregnant women; acute pyelonephritis; typhoid and paratyphoid; peridental abscess with spreading cellulitis; prosthetic joint infections; eradication of Helicobacter pylori; Lyme disease. Amoxicillin can also be used to prevent endocarditis. When deciding whether to prescribe the drug AMOXICILLIN, one should rely on the general principles of antibiotic therapy and on the information provided in official guidelines for the appropriate use of antibacterial drugs. Dosing and Administration Method of administration Amoxicillin is intended for oral administration. Eating does not affect the absorption of amoxicillin. Therefore, the tablet can be taken regardless of the meal. Treatment can be started with parenteral (intravenous) amoxicillin (at the doses recommended for this route of administration) and continued with oral amoxicillin tablets. Doses When prescribing a specific dose of amoxicillin for the treatment of a specific infection, one should take into account: the type of suspected pathogen and the characteristic profile of sensitivity / resistance to antibacterial agents for this pathogen (see section “Special Instructions and Precautions”); severity and localization of the infectious process; age, body weight, kidney function status of the patient. The duration of the course of treatment should be determined based on the type of infection, the individual reactions of the patient to the drug. In general, the duration of the course should be as short as possible. Some infections require long-term therapy with amoxicillin (see the “Special instructions and precautions” section of the relative prolonged treatment). When deciding whether to prescribe the drug AMOXICILLIN, one should rely on the general principles of antibiotic therapy and on the information provided in official guidelines for the appropriate use of antibacterial drugs. Adults and children weighing >40 kg Indication* Dose* Acute bacterial sinusitis 250-500 mg every 8 hours or 750-1000 mg every 12 hours For severe infections 750-1000 mg every 8 hours For acute cystitis may the following treatment regimen should be used: 3 g of amoxicillin 2 times a day, the course of treatment is 1 day. Asymptomatic bacteriuria in pregnant women Acute pyelonephritis Peritoneal abscess with spreading cellulitis Acute cystitis Acute otitis media 500 mg every 8 hours, 750-1000 mg every 12 hours In severe infections – 750-1000 mg every 8 hours for 10 days. Acute streptococcal tonsillitis and pharyngitis Exacerbation of chronic bronchitis Community-acquired pneumonia 500–1000 mg every 8 hours Typhoid fever and paratyphoid fever 500–2000 mg every 8 hours Prosthetic joint infections 500–1000 mg every 8 hours Prophylaxis of endocarditis A single dose of 2 g should be given after 30-60 minutes before the procedure. Helicobacter pylori eradication 750–1000 mg twice daily in combination with a proton pump inhibitor (eg, omeprazole, lansoprazole) and another antibacterial (eg, clarithromycin, metronidazole); course of treatment – 7 days. Lyme disease (see section “Special instructions and precautions”) Early stage: 500-1000 mg every 8 hours; the daily dose can be increased to 4 g (maximum daily dose), it should be divided into several doses; course of treatment – 14 days (10-21 days). Late stage (systemic disorders): 500-2000 mg every 8 hours; the daily dose can be increased to 6 g (maximum daily dose), it should be divided into several doses; course of treatment – 10-30 days *The official treatment recommendations for each indication should be taken into account. Children weighing <40 kg Indication* Dose* Acute bacterial sinusitis 20-90 mg/kg/day; the daily dose should be divided into several doses**. Acute otitis media Community-acquired pneumonia For more accurate and convenient dosing of the drug, as well as due to possible difficulties in swallowing tablets, in children (especially young children) it may be advisable to use amoxicillin in the form of a suspension or in other dosage forms. In children under 6 months of age, amoxicillin suspension is recommended. Acute cystitis Acute pyelonephritis Peritoneal abscess with spreading cellulitis Acute streptococcal tonsillitis and pharyngitis 40-90 mg/kg/day; the daily dose should be divided into several doses**. Typhoid and paratyphoid 100 mg/kg/day; The daily dose should be divided into 3 doses. Prevention of endocarditis A single dose of 50 mg/kg of body weight should be taken 30-60 minutes before the procedure. Lyme disease (see section "Special instructions and precautions") Early stage: 25-50 mg / kg / day; the daily dose should be divided into 3 doses; course of treatment - 10-21 days. Late stage (systemic disorders): 100 mg / kg / day; the daily dose should be divided into 3 doses; course of treatment - 10-30 days. *The official treatment recommendations for each indication should be taken into account. **Twice daily recommended only for doses approaching the upper limit of the indicated range. Elderly patients Correction of the dosing regimen is not required. Patients with impaired renal function Glomerular filtration rate ml/min Adults and children weighing ≥40 kg Children weighing <40 kg* More than 30 No correction required. No correction required. 10-30 Maximum 500 mg 2 times a day. 15 mg/kg 2 times a day (maximum 500 mg 2 times a day). Less than 10 Maximum 500 mg per day. 15 mg/kg once daily (maximum 500 mg). * In most cases, parenteral amoxicillin should be preferred. Patients on hemodialysis During hemodialysis, amoxicillin may be removed from the circulating blood. Hemodialysis Adults and children weighing ≥40 kg 500 mg every 24 hours. One additional dose of 500 mg is prescribed for hemodialysis. To restore the concentration of the drug in the blood, another dose of 500 mg is given after hemodialysis. Children weighing < 40 kg 15 mg/kg/day once (maximum 500 mg). For hemodialysis, one additional dose of 15 mg/kg is prescribed. To restore the drug concentration in the blood, another dose of 15 mg/kg is administered after hemodialysis. Patients on peritoneal dialysis The maximum daily dose of amoxicillin is 500 mg. Patients with impaired liver function In the presence of this pathology, the dosage regimen should be selected with caution and regular monitoring of the state of liver function during treatment should be carried out (see sections "Special Instructions and Precautions" and "Side Effects"). Attention!!! If the patient has forgotten to take the next dose of the drug Amoxicillin, it must be taken as soon as possible. The next scheduled dose should be taken at least 4 hours after the missed dose. Do not take a double dose to make up for a missed dose! Side effects The most frequently reported adverse reactions were diarrhea, nausea and skin rash. The frequency of occurrence of adverse reactions is estimated according to the following classification: very often (≥1 / 10); often (≥1/100 to <1/10); infrequently (≥1/1000 to <1/100); rarely (≥1/10000 to <1/1000); very rarely (<1/10000); frequency unknown (frequency cannot be determined from available data). Also, adverse reactions are distributed by organ systems. The information is presented in the form of a table. 1 Infections and invasions Very rarely Candidiasis of the skin and mucous membranes 2 Blood and lymphatic system disorders Very rarely Reversible leukopenia (including severe neutropenia or agranulocytosis), reversible thrombocytopenia and hemolytic anemia, prolongation of bleeding time and prothrombin time (see section "Special instructions and precautions") 3 Immune system disorders Very rarely Severe allergic reactions, including angioedema, anaphylaxis, serum sickness and allergic vasculitis (see section "Special instructions and precautions") Frequency unknown Jarisch-Herksheimer reaction (see section "Special precautions") instructions and precautions") 4 Nervous system disorders Very rare Hyperkinesia, dizziness, convulsions (see section "Special instructions and precautions") 5 Gastrointestinal disorders Clinical trial data *Common Diarrhea, nausea *Uncommon Vomiting Post-marketing data Very rare Antibi otitis-associated colitis (including pseudomembranous colitis and hemorrhagic colitis; 6 Hepatic and biliary tract disorders Very rare Hepatitis, cholestatic jaundice, mild elevation of aspartate aminotransferase and/or alanine aminotransferase 7 Skin and subcutaneous tissue disorders Clinical trial data *Common Skin rash **Uncommon Urticaria , itching Post-marketing data Very rarely other severe skin reactions such as skin discoloration, blistering, pustules, skin flaking, redness, pain. They may be associated with fever, headache, and pain throughout the body; drug reaction with eosinophilia and systemic symptoms (DRESS syndrome: flu-like symptoms with rash, fever, swollen lymph nodes, and abnormal blood test results, including elevated white blood cells (eosinophilia), and liver enzymes) (see section "Special Instructions and precautions). 8 Renal and urinary tract disorders Very rare Interstitial nephritis, crystalluria (see sections "Special instructions and precautions" and "Overdose") * The frequency of these adverse reactions is determined based on the results of clinical trials in which they were included ) about 6,000 adults and children taking amoxicillin. Reporting adverse reactions If you experience any adverse reactions, it is recommended that you consult your doctor. This recommendation applies to any possible adverse reactions, including those not listed in the leaflet for the use of the drug. You can also report adverse reactions to the adverse drug reactions (actions) information database, including reports of drug failures. By reporting adverse reactions, you help to get more information about the safety of the drug. Contraindications The appointment and use of the drug AMOXICILLIN is contraindicated in the following situations: known increased individual sensitivity to amoxicillin and / or to any of the auxiliary components of the drug; known increased individual sensitivity to any antibiotic from the penicillin series; a history of severe immediate-type hypersensitivity reaction (eg, anaphylaxis) associated with another beta-lactam drug (eg, cephalosporins, carbapenems, or monobactams). OverdoseSymptoms In case of an overdose of amoxicillin, obvious disorders of the gastrointestinal tract (nausea, vomiting, diarrhea), obvious disturbances in water and electrolyte balance can be observed. Crystalluria has been reported with the use of amoxicillin, in some cases leading to renal failure. In patients with impaired renal function or in those patients who take amoxicillin in high doses, convulsions may occur (see sections "Special Instructions and Precautions" and "Side Effects"). Treatment In violation of the function of the gastrointestinal tract, symptomatic treatment is indicated. Particular attention should be paid to the normalization of water and electrolyte balance. Amoxicillin can be removed from the vascular bed by hemodialysis. Interaction with other medicinal products and other forms of interaction Probenecid Concomitant use of probenecid is not recommended. Probenecid reduces tubular secretion of amoxicillin in the kidneys. Simultaneous administration of probenecid can lead to an increase in the concentration of amoxicillin and a prolongation of its plasma half-life. Allopurinol The combined use of amoxicillin and allopurinol may increase the likelihood of allergic skin reactions. Tetracyclines Tetracyclines and other bacteriostatic agents may interfere with the bactericidal effects of amoxicillin. Oral anticoagulants Oral anticoagulants and antibiotics from the penicillin group are widely used in clinical practice, with no evidence of interaction between drugs. However, the literature describes cases of an increase in the international normalized ratio (INR) in patients undergoing course treatment with amoxicillin while taking acenocoumarol or warfarin. If the combined use of oral anticoagulants and amoxicillin is considered necessary, careful monitoring of the value of prothrombin time or INR should be carried out with an increase in the dose of amoxicillin and after stopping treatment with amoxicillin. Moreover, dose adjustment of oral anticoagulants may be required (see sections "Special instructions and precautions" and "Side effects"). Methotrexate Penicillins can reduce the excretion of methotrexate, which will increase the likelihood of manifestation of the toxic properties of the latter. Special instructions and precautions Hypersensitivity reactions Before starting treatment with amoxicillin, it is imperative to find out if the patient had previously had hypersensitivity reactions, the occurrence of which was associated with taking any antibiotic from the group of penicillins, cephalosporins or other beta-lactam (see sections "Contraindications" and side effects). There are reports of the development of serious hypersensitivity reactions, sometimes fatal, (including anaphylactoid and severe skin adverse reactions) in patients receiving penicillin therapy. These reactions are more common in people with a history of hypersensitivity to penicillin and atopy. If an allergic reaction develops, stop taking amoxicillin and consult a doctor. Non-susceptible organisms Amoxicillin should be used to treat infections only if one of the following conditions is met: the pathogen has been identified and found to be susceptible to amoxicillin; the suspected causative agent is very likely to be sensitive to amoxicillin (see section "Pharmacological properties"). This information is especially important to take into account when deciding whether to prescribe amoxicillin to patients with a urinary tract infection or a severe infection of the ear, nose, or pharynx. Convulsions Convulsions may occur in patients: with impaired renal function; taking amoxicillin in high doses; with the presence of predisposing factors (for example, a history of seizures, treated epilepsy or meningeal disorders) (see section "Side effects"). Impaired renal function In patients with impaired renal function, the dose should be selected in accordance with the severity of the pathology (see section "Method of application and doses"). Skin reactions Generalized erythema with fever and pustules that occurs at the beginning of treatment with amoxicillin may be a symptom of acute generalized exanthematous pustulosis (see section "Side effect"). If such a reaction occurs, you should immediately stop taking amoxicillin; in the future, the appointment of amoxicillin is contraindicated in any case. Amoxicillin should be avoided if infectious mononucleosis is suspected. Taking amoxicillin with infectious mononucleosis can lead to a measles-like rash. The Jarisch-Herxheimer reaction The Jarisch-Herxheimer reaction (fever, chills, headache, muscle pain and skin rash) has been noted with the use of amoxicillin for the treatment of Lyme disease (see section "Side Effects"). Its appearance is a direct consequence of the bactericidal activity of amoxicillin against the bacterium that is the causative agent of Lyme disease (spirochete Borrelia burgdorferi). Patients should be aware that this reaction is common, usually resolves on its own, and is considered a natural consequence of antibiotic therapy for Lyme disease. Overgrowth of non-susceptible organisms Long-term use of amoxicillin can sometimes lead to overgrowth of non-susceptible organisms. When taking almost all antibacterial drugs, cases of antibiotic-associated colitis have been reported. Its severity can vary from mild to life-threatening (see section "Side effect"). If a patient develops diarrhea during or after treatment with any antibiotic, this diagnosis should always be assumed. If antibiotic-associated colitis is suspected or confirmed, amoxicillin should be stopped immediately and appropriate treatment instituted. In this situation, antiperistaltic drugs are contraindicated. Long-term treatment With long-term treatment with amoxicillin, it is recommended to regularly monitor the function of organ systems, including kidney function, liver function, hematopoiesis function. When taking amoxicillin, there have been cases of increased activity of liver enzymes and changes in the cellular composition of the blood (see section "Side Effects"). Anticoagulants Prolongation of prothrombin time has been reported in rare cases in patients treated with amoxicillin. Appropriate monitoring should be carried out if the patient is taking amoxicillin with anticoagulants. It may be necessary to adjust the dose of oral anticoagulant in order to maintain the level of anticoagulation at the desired level (see sections "Interaction with other medicinal products and other forms of interaction" and "Side effect"). Crystalluria In patients with reduced urine output (diuresis), crystalluria has been observed in very rare cases, mainly with the introduction of an antibiotic parenterally. When prescribing amoxicillin in high doses, it is recommended to ensure the introduction of an adequate amount of fluid and maintain a sufficient level of urine output in order to reduce the likelihood of crystalluria associated with taking amoxicillin. In patients with urinary catheters, it is necessary to regularly check the patency of the urinary tract (see sections "Side Effects" and "Overdose"). Interference with laboratory tests Elevated serum and urinary concentrations of amoxicillin may interfere with the results of certain laboratory tests. Due to high concentrations of amoxicillin in the urine, false positive results are often observed when using chemical diagnostic methods. In the course of treatment with amoxicillin, if it is necessary to determine the concentration of glucose in the urine, it is recommended to use enzymatic glucose oxidase methods. In the presence of amoxicillin, the results of determining the concentration of estriol in pregnant women may be distorted. Use during pregnancy and lactation Pregnancy In animal studies, no direct or indirect negative effects have been identified, which are manifestations of reproductive toxicity. Limited data on the use of amoxicillin during pregnancy in humans do not indicate an increased risk of congenital malformations. Amoxicillin should only be used in pregnant women if the expected benefit outweighs the potential risks. Breast-feeding Amoxicillin is excreted in small amounts into breast milk, which creates a possible risk of sensitization. Consequently, in children who are breastfed, diarrhea and fungal infections of the mucous membranes may occur; therefore, before starting amoxicillin, breastfeeding should be suspended. Amoxicillin should only be used during lactation after careful benefit/risk assessment by a physician. Fertility There are no data on the effect of amoxicillin on human fertility. Animal reproduction studies have shown no effect on fertility. Use in children In children under 6 months of age, it is recommended to use amoxicillin in the form of a suspension. In children weighing ≥40 kg, the amoxicillin dosing regimen is similar to that in adults. Influence on the ability to drive vehicles and work with mechanisms Special studies of the effect of amoxicillin on the ability to drive vehicles or other moving mechanisms have not been conducted. However, it should be borne in mind that during the treatment with amoxicillin, side effects may occur that may affect the indicated ability (for example, allergic reactions, dizziness, convulsions) (see section "Side Effects"). Release form and packagingCoated tablets, 125 mg each in blisters No. 10×1, No. 10×2, in jars No. 20; 250 mg each in blisters No. 12×1, No. 12×2, in jars No. 20 and in blisters No. 6×2, No. 6×3, No. 6×4, No. 10×1, No. 10×2 , No. 10×3; 500 mg each in blisters No. 12×1, No. 12×2, in jars No. 10, No. 20 and in blisters No. 6×2, No. 6×3, No. 6×4, No. 10×1, No. 10×2; 750 mg each in blisters No. 6×1, No. 6×2, in jars No. 10 and in blisters No. 6×2, No. 6×3, No. 6×4, No. 10×1, No. 10×2 ; 1000 mg in blisters No. 6×2, in jars No. 10 and in blisters No. 6×2, No. 6×3, No. 6×4 in package No. 1. Together with the leaflet, 1 or 2 blisters, 1, 2, 3 or 4 blisters or a can are placed in a carton pack. Storage conditionsKeep in a place protected from light at a temperature not exceeding 25°C. Keep out of the reach of children. Shelf life 2 years. Do not use after the expiry date stated on the packaging. Conditions of release By prescription .p/o 1000mg
INN | AMOXICILLIN |
---|---|
The code | 140 492 |
Barcode | 4 810 183 013 904 |
Dosage | 1000mg |
Active substance | Amoxicillin |
Manufacturer | Pharmtekhnologiya LLC, Belarus |
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