Amoxiclav instructions for use of tablets for adults 500. Antibiotic Amoxiclav: instructions for use, pharmacological properties, indications, dosage

Amoxiclav
Buy Amoxiclav in pharmacies

DOSAGE FORMS
coated tablets 875mg/125mg
film-coated tablets 875mg+125mg

MANUFACTURERS
Lek d.d. (Slovenia)

GROUP
Combined antimicrobials

COMPOSITION
Active substances: 875 mg of amoxicillin in the form of trihydrate and 125 mg of clavulanic acid in the form of potassium salt.

INTERNATIONAL NON-PROPRIETARY NAME
Amoxicillin + Clavulanic acid

SYNONYMS
Amoxiclav Quiktab, Arlet, Augmentin, Augmentin EC, Augmentin SR, Klamosar, Medoklav, Panklav, Ranklav, Rapiclav, Sinulox, Sinulox RTU, Flemoclav Solutab, Ecoclave

PHARMACHOLOGIC EFFECT
The drug is a combination of amoxicillin and clavulanic acid. Amoxicillin is a semi-synthetic penicillin (beta-lactam antibiotic) that inhibits one or more enzymes (often referred to as penicillin-binding proteins, PBPs) in the biosynthesis pathway of peptidoglycan, which is an integral structural component of the bacterial cell wall. Inhibition of peptidoglycan synthesis leads to a loss of cell wall strength, which usually leads to lysis and death of microorganism cells. Amoxicillin is destroyed by the action of beta-lactamases produced by resistant bacteria, thus, the spectrum of activity of amoxicillin alone does not include microorganisms that produce these enzymes. Clavulanic acid is a beta-lactam structurally related to penicillins. It inhibits some beta-lactamases, thereby preventing the inactivation of amoxicillin and extending its spectrum of activity to include bacteria normally resistant to amoxicillin as well as to other penicillins and cephalosporins. By itself, clavulanic acid does not have a clinically significant antibacterial effect. The drug has a bactericidal effect in vivo on the following microorganisms: Gram-positive aerobes. Staphylococcus aureus, Streptococcus pneumoniae, Streptococcus pyogenes. Gram-negative aerobes. Enterobacter spp, Escherichia coli, Haemophilus influenza, Species of the genus Klebsiella, Moraxella catarrhalis (Branhamella catarrhalis). The drug has a bactericidal effect in vitro on the following microorganisms (however, the clinical dependence is still unknown). Gram-positive aerobes. Bacil Hs anthracis. Species of the genus Corynebacterium, Enterococcus faecalis, Enterococcus faecium, Listeria monocytogenes, Nocardia asteroids, Coagulase-negative staphylococci (including Staphylococcus epidermidis) Streptococcus agalaciiae. Other species of the genus Streptococcus Streptococcus viridians. Gram-positive anaerobes. Species of the genus Clostridium, Species of the genus Peptococcus, Species of the genus Peptostreptococcus. Gram-negative aerobes. Bordetella pertussis, Species of the genus Brucella, Gardnerella vaginalis, Helicobacter pylori, Species of the genus Legionella, Neisseria gonorrhoeae, Neisseria meningitides, Pasteurella multocida, Proteus mirabilis, Proteus vulgaris, Species of the genus Salmonella, Species of the genus Shigella, Vibrio cholerae, Yersinia enterocolitica. Gram-negative anaerobes. Species of the genus Bacteroides (including Bacteroides fragilis), Species of the genus Fusobacterium. Others: Borrella burgdorferi, Chlamydia spp., Leptospira icterohaemorrhagiae, Treponema pallidum. Some strains of these bacterial species produce beta-lactamase, which contributes to their insensitivity to amoxicillin monotherapy. Pharmacokinetics. The main pharmacokinetic parameters of amoxicillin and clavulanic acid are similar. Amoxicillin and clavulanic acid are highly soluble in aqueous solutions with a physiological pH value and after taking the drug inside, they are quickly and completely absorbed from the gastrointestinal tract (GIT). The absorption of the active substances of amoxicillin and clavulanic acid is optimal if taken at the beginning of a meal. The bioavailability of amoxicillin and clavulanic acid after oral administration is about 70%. Peak plasma concentrations are reached approximately 1 hour after ingestion. The maximum concentration values ​​​​are for amoxicillin (depending on the dose) 3-12 μg / ml, for clavulanic acid - about 2 μg / ml. When using the drug, plasma concentrations of amoxicillin / clavulanic acid are similar to those with oral administration of the corresponding doses of amoxicillin or clavulanic acid separately in equivalent doses. Both components are characterized by a good volume of distribution in various organs, tissues and body fluids (including lungs, abdominal organs; adipose, bone and muscle tissues; pleural, synovial and peritoneal fluids; skin, bile, urine, purulent discharge, sputum, interstitial fluid). Plasma protein binding is moderate: 25% for clavulanic acid and 18% for amoxicillin. The volume of distribution is about 0.3-0.4 l/kg for amoxicillin and about 0.2 l/kg for clavulanic acid. Amoxicillin and clavulanic acid do not cross the blood-brain barrier in non-inflamed meninges. Amoxicillin (like most penicillins) is excreted in breast milk. IN breast milk trace amounts of clavulanic acid were also found. Amoxicillin and clavulanic acid cross the placental barrier. Amoxicillin is excreted primarily by the kidneys, while clavulanic acid is eliminated via both renal and extrarenal mechanisms. After a single oral administration of one tablet of 250 mg / 125 mg or 500 mg / 125 mg, approximately 60-70% of amoxicillin and 40-65% of clavulanic acid are excreted unchanged in the urine during the first 6 hours. About 10-25% of the initial dose of amoxicillin is excreted in the urine as inactive penicillic acid. Clavulanic acid in the human body undergoes intensive metabolism with the formation of 2,5-dihydro-4-(2-hydroxyethyl)-5-oxo-1H-pyrrole-3-carboxylic acid and 1-amino-4-hydroxy-butan-2-one and is excreted in urine and feces. The mean half-life of amoxicillin/clavulanic acid is approximately one hour, and the mean total clearance is approximately 25 L/h in healthy patients. In the course of various studies, it was found that the excretion of amoxicillin in the urine within 24 hours is approximately 50-85%, clavulanic acid - 27-60%. The greatest amount of clavulanic acid is excreted during the first 2 hours after ingestion. Patients with impaired liver function. In patients with severe kidney failure the half-life increases to 7.5 hours for amoxicillin and up to 4.5 hours for clavulanic acid. For patients with impaired liver function, the dose of the drug should be selected with caution, constant monitoring of the state of the liver is necessary. Both components are removed by hemodialysis and minor amounts by peritoneal dialysis.

INDICATIONS FOR USE
Infections caused by susceptible strains of microorganisms: infections of the upper respiratory tract and ENT organs (including acute and chronic sinusitis, acute and chronic otitis media, retropharyngeal abscess, tonsillitis, pharyngitis); lower respiratory tract infections (incl. acute bronchitis with bacterial superinfection, Chronical bronchitis, pneumonia); infections urinary tract; infections in gynecology; infections of the skin and soft tissues, as well as wounds from human and animal bites; bone and connective tissue infections; infections biliary tract(cholecystitis, cholangitis); odontogenic infections.

CONTRAINDICATIONS
Hypersensitivity to the components of the drug; a history of hypersensitivity to penicillins, cephalosporins and other beta-lactam antibiotics, cholestatic jaundice and / or other liver dysfunction caused by taking amoxicillin / clavulanic acid in history; Infectious mononucleosis and lymphocytic leukemia.

SIDE EFFECT
From the digestive system: loss of appetite, nausea, vomiting, diarrhea, abdominal pain, gastritis, stomatitis, glossitis, black "hairy" tongue, darkening of tooth enamel, hemorrhagic colitis (may also develop after therapy), enterocolitis, pseudomembranous colitis, violation liver function, increased activity of alanine aminotransferase, aspartate aminotransferase, alkaline phosphatase and / or plasma bilirubin levels, liver failure (more often in the elderly, men, with long-term therapy), cholestatic jaundice, hepatitis. Allergic reactions: itching, urticaria, erythematous rashes, multiforme exudative erythema, angioedema, anaphylactic shock, allergic vasculitis, exfoliative dermatitis, Stevens-Johnson syndrome, acute generalized exanthematous pustulosis, a syndrome similar to serum sickness, toxic epidermal necrolysis. From the hematopoietic system and lymphatic system: reversible leukopenia "(including neutropenia), thrombocytopenia, hemolytic anemia, reversible increase in prothrombin in time (when used together with anticoagulants), reversible increase in bleeding time, eosinophilia, pancytopenia, thrombocytosis, agranulocytosis. From the side of the central nervous system: dizziness, headache, convulsions (may occur in patients with impaired renal function when taking high doses of the drug), hyperactivity. Feelings of anxiety, insomnia, behavioral changes, agitation. From the urinary system: interstitial nephritis, crystalluria, hematuria. Other: candidiasis and other types of superinfection.

INTERACTION
Antacids, glucosamine, laxatives, aminoglycosides slow absorption, ascorbic acid increases absorption. Diuretics, allopurinol, phenylbutazone; non-steroidal anti-inflammatory drugs and other drugs that block tubular secretion (probenecid) increase the concentration of amoxicillin (clavulanic acid is excreted mainly by glomerular filtration). The simultaneous use of the drug and methotrexate increases the toxicity of methotrexate. Appointment in conjunction with allopurinol increases the incidence of exanthema. Avoid concomitant use with disulfiram. Reduces the effectiveness of drugs, during the metabolism of which para-aminobenzoic acid is formed, ethinyl estradiol - the risk of bleeding "breakthrough". The literature describes rare cases of an increase in the international normalized ratio (MNR) in patients with the combined use of acenocoumarol or warfarin and amoxicillin. If necessary, simultaneous use with anticoagulants and prothrobin time or MHO should be carefully iterated when prescribing or discontinuing the drug. The combination with rifampicin is antagonistic (mutual weakening of the antibacterial effect). The drug should not be used simultaneously in combination with bacteriostatic antibiotics (macrolides, tetracyclines), sulfonamides due to a possible decrease in the effectiveness of the drug. The drug reduces the effectiveness of oral contraceptives.

METHOD OF APPLICATION AND DOSAGE
inside. The dosage regimen is set individually depending on the age, body weight, kidney function of the patient, as well as the severity of the infection. The drug is recommended to be taken at the beginning of a meal for optimal absorption and to reduce possible side effects from the digestive system. The course of treatment is 5 - 14 days. The duration of the course of treatment is determined by the attending physician. The course should not last more than 14 days without a second medical examination. Children under 12 years old. The dose is prescribed depending on age and body weight. Recommended dosage regimen: 40 mg/kg/day in 3 divided doses. Children weighing 40 kg or more should be given the same doses as adults. For children under the age of 6 years, it is more preferable to take a suspension of the drug. Adults and children over 12 years of age (or over 40 kg body weight). The usual dose for mild to moderate infections is 1 tablet every 12 hours, for severe infections and respiratory tract infections, 1 tablet every 8 hours. Since the 250mg + 125mg and 500mg-125mg tablets of the combination of amoxicillin and clavulanic acid contain the same amount of clavulanic acid -125mg, then 2 tablets of 250mg + 125mg are not equivalent to 1 tablet of 500mg + 125mg. Dosage for odontogenic infections: 1 tablet every 12 hours for 5 days. Patients with impaired renal function. Dose adjustments are based on the maximum recommended dose of amoxicillin and are based on creatinine clearance (CC) values. Adults and children over 12 years of age (or over 40 kg body weight). QC> 30 ml / min: dose adjustment is not required. With anuria, the interval between dosing should be increased to 48 hours or more. Tablets 875 mg + 125 mg should only be used in patients with CC> 30 ml / min. Patients with impaired liver function. The drug should be taken with caution. It is necessary to conduct regular monitoring of liver function.

OVERDOSE
There are no reports of death or life-threatening side effects due to an overdose of the drug. In most cases, overdose symptoms include gastrointestinal disorders (abdominal pain, diarrhea, vomiting). Anxiety, insomnia, dizziness, and in isolated cases, convulsive seizures are also possible. In case of an overdose, the patient should be under the supervision of a physician, treatment is symptomatic. In case of recent intake (less than 4 hours), it is necessary to perform gastric lavage and prescribe activated charcoal to reduce absorption. Amoxicillin/clavulanic acid is removed by hemodialysis.

SPECIAL INSTRUCTIONS
Carefully. Pseudomembranous colitis in history, diseases of the gastrointestinal tract, liver failure, severe renal dysfunction, pregnancy, lactation, while used with anticoagulants. Use during pregnancy and during breastfeeding. During pregnancy and lactation, the drug is used only if the intended benefit to the mother outweighs the potential risk to the fetus and child. During the course of treatment, it is necessary to monitor the state of the function of the hematopoietic organs, liver, kidneys. In patients with severely impaired renal function, an adequate dose adjustment or an increase in the intervals between doses is required. In order to reduce the risk of side effects from the gastrointestinal tract, the drug should be taken with food. It is possible to develop superinfection due to the growth of microflora insensitive to it, which requires an appropriate change. antibiotic therapy. In patients with hypersensitivity to penicillins, cross-allergic reactions with cephalosporin antibiotics are possible. In women with premature rupture of membranes, it has been found that prophylactic therapy with amoxicillin + clavulanic acid may be associated with an increased risk of neonatal necrotizing colitis. In patients with reduced diuresis, crystalluria very rarely occurs. During the use of large doses of amoxicillin, it is recommended to take a sufficient amount of fluid and maintain adequate diuresis to reduce the likelihood of amoxicillin crystal formation. Laboratory tests: High concentrations of amoxicillin give a false positive reaction to urine glucose when using Benedict's reagent or Fehling's solution. Enzymatic reactions with glucosidase are recommended. Special precautions for the disposal of unused medicinal product. There is no need for special precautions when destroying an unused drug. Influence on the ability to drive vehicles and engage in other activities that require concentration and speed of psychomotor reactions. Due to the possibility of developing side effects from the central nervous system, such as: dizziness, headache, convulsions, during treatment, care should be taken when driving and engaging in other activities that require concentration and speed of psychomotor reactions.

STORAGE CONDITIONS
Store in a dry place, out of the reach of children, at a temperature not exceeding 25 C.

Amoxiclav 500/125 belongs to the group antibacterial agents penicillin series, used to combat many diseases caused by infection of a bacterial nature. This is a complex drug preparation, consisting of two components with antibacterial activity.

Amoxiclav is a product of an Austrian pharmaceutical company.

The medication is available in the following forms:

  • in tablets with a dosage of 250 mg / 125 mg with a thin shell soluble in the intestine;
  • in tablets with a dosage of 500 mg / 125 mg with an enteric coating;
  • in the form of tablets for resorption, dissolution in water - Amoxiclav Quiktab with a dosage of 500 mg / 125 mg;
  • in the form of a powder that allows you to prepare a suspension for children;
  • in the form of a powder, for the preparation of intravenous injections.

The tablet form of Amoxiclav includes the following components that actively affect the body:

  • amoxicillin 500 mg;
  • clavulanic acid 125 mg.

Tablets, in addition to active substances, consist of the following auxiliary components that do not have a therapeutic effect:

  • cellulose;
  • silicon dioxide;
  • polysorbate;
  • titanium dioxide;
  • magnesium stearate.

Amoxiclav Quiktab tablets, in addition to active ingredients, consist of the following auxiliary ingredients:

  • aspartame;
  • silicon dioxide;
  • iron oxide;
  • castor oil;
  • flavors.

The suspension, along with the active ingredients, includes in its composition substances that do not have a therapeutic effect on bacteria:

  • mannitol;
  • sodium citrate;
  • sodium saccharin;
  • sodium benzoate.

For your information. The injection powder contains only active ingredients.

Pharmacological action, pharmacodynamics and pharmacokinetics


Instructions for use indicate the presence of the following pharmacological activity of Amoxiclav:

  • penicillin-derived drug has a bactericidal effect, disrupts cell synthesis. Thus destroying pathogenic microorganisms;
  • clavulanic acid enhances the effectiveness of amoxicillin. The second active component of Amoxiclav also has an antimicrobial effect;
  • the drug is active against gram-positive anaerobes;
  • the medicine is effectively taken with gram-negative anaerobes.

Amoxiclav quickly acts on pathogenic microorganisms. Already 60 minutes after its administration, the highest concentration of active components in plasma is determined. The active component of the antibiotic is absorbed into circulatory system from the intestines, from where it spreads throughout the body. The drug is excreted through the urinary system within an hour.

In what cases is Amoxiclav prescribed?

Indications for prescribing medication are:

  • infectious ENT diseases;
  • urinary infections;
  • pathology of the bronchi, lungs caused by infections;
  • bacterial processes of the upper respiratory tract;
  • gynecological infections, postpartum inflammation;
  • infectious processes of connective tissues;
  • diseases of bone tissue;
  • skin infectious diseases, post-burn conditions;
  • inflammatory processes of bones, joints;
  • infected processes of the abdominal cavity;
  • odotogenic infections;
  • infection of the teeth, jaw;
  • preoperative, postoperative period.

Important! Amoxiclav is taken only to eliminate an infection that marks sensitivity to the penicillin series.

Instructions for use and dosage

It is recommended to drink a penicillin-containing drug after consulting a doctor. It is important to find out the presence of sensitivity of bacteria to antibiotics by conducting bacteriological studies. Recommendations for dosage, frequency of administration, duration of the treatment course are given individually. An assessment is made of the patient's condition, age, type of disease, its severity. Before starting treatment, it is necessary to make sure that there is no hypersensitivity to Amoxiclav. It is advisable to do an allergy test.

Tablets 500 mg + 125 mg

The tableted form of Amoxiclav is prescribed for adults, children over 12 years of age. In this case daily dose should not exceed 600 mg.

  • uncomplicated pathology - 1 tab. four times a day;
  • mild infection - 1 tab. twice a day;
  • complicated course of the disease - 1 tab. up to 6 times a day;
  • odotogenic infection - 1 tab. four times or twice a day.

If treatment is required for a patient who suffers from liver failure, then between doses it is necessary to increase the break to 12 hours. In severe kidney disease, the interval between doses is recommended to be increased to 24 hours, provided intravenous administration Amoxiclav.

Therapy of the child population is carried out by Amoxiclav in suspension, diluted to measure with distilled water. Permissible dosage per day is up to 45 mg of a penicillin preparation per 1 kg of the child's weight.

Amoxiclav in injections

Amoxiclav injections are usually given intravenously. In exceptional situations, intramuscular injection is allowed, taking into account the following dose:

  • older than 12 years, the antibiotic is administered 1.2 g 3 times a day. Severe course is treated with a four-time injection;
  • up to 12 years, the dosage is calculated individually, based on the weight of the child. For 1 kg of weight there are 30 mg of Amoxiclav four times a day;
  • for babies up to 3 months, the dosage is calculated from 30 mg per 1 kg of the child's weight twice a day.

Important! The prepared injection powder must be administered within 15 minutes. The prepared solution must not be frozen.

If after 2-3 days after the start of treatment the expected result is not observed, then it is necessary to change the therapeutic tactics with a change in the drug group. Amoxiclav has proven effective only against bacterial infections.

During pregnancy and lactation

The appointment of Amoxiclav to pregnant women is made only if the expected benefit to the expectant mother is higher than the expected harm to the child. It is especially harmful to carry out antibiotic therapy in the first trimester.

In the second, third trimester, the medication is prescribed subject to the exact observance of the dose. During breastfeeding, the drug is not used. This is due to the fact that its active components enter the child's body through breast milk.

drug interaction

With the parallel use of Amoxiclav with some groups of medicines, the following undesirable reactions may occur:

  • with ascorbic acid, the absorption of the antibiotic is accelerated;
  • with laxatives, there is a slowdown in absorption;
  • with non-steroidal anti-inflammatory drugs, an increased concentration of Amoxiclav is observed;
  • with anticoagulants, the effectiveness of antithrombotic agents decreases;
  • with Rifampicin, the antibacterial effect is weakened;
  • with tetracyclines, the effectiveness of antibiotic therapy is reduced;
  • with oral contraceptives, their effectiveness may be reduced.

Can I drink alcohol while taking the drug

It is forbidden to take Amoxiclav simultaneously, even with low-alcohol drinks. This can lead to an increase in the negative impact on the liver, an increase in the number of side effects.

Contraindications, side effects and overdose

Before starting the use of Amoxiclav, it is necessary to take into account the presence of the following contraindications:

  • jaundice;
  • lymphocytic leukemia;
  • mononucleosis;
  • allergic reaction to penicillin-containing drugs;
  • liver diseases;
  • kidney diseases.

If there is hypersensitivity to active ingredients, the recommended dosage is exceeded, the frequency of Amoxiclav use is increased, then side effects may develop in the form of:

  • nausea;
  • decreased appetite;
  • diarrhea;
  • vomiting;
  • abdominal pain;
  • itching;
  • skin rash;
  • puffiness;
  • anaphylactic shock;
  • dermatitis;
  • jade;
  • headache;
  • dizziness;
  • convulsive state;
  • dysbacteriosis causing a fungal infection;
  • bacterial resistance.

Cases of overdose lead to an increase in side effects, the severity of their manifestations increases. Usually, an incorrectly calculated dose of Amoxiclav causes vomiting, diarrhea, and nervous overexcitation. More severe situations are accompanied by convulsions. If symptoms of an overdose appear after taking, then you should call a doctor, do a gastric lavage, take activated charcoal.

To replace the recommended intake of the following drugs with a wide spectrum of action:

  • Renklava;
  • Amoxivana;
  • Flemoklava;
  • Augmentina;
  • Panclava.

The replacement of Amoxiclav should be carried out by a doctor, as well as the calculation of the recommended dosage and frequency of administration.

Antibiotic therapy with Amoxiclav helps fight various infections. The drug is usually well tolerated by patients of different age categories.

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Amoxiclav: instructions for use and reviews

Amoxiclav is a combined antibiotic medication.

Release form and composition

Amoxiclav is produced in the form of:

  • Coated tablets containing 250 mg, 500 mg or 875 mg of amoxicillin, 125 mg of clavulanic acid and excipients: colloidal silicon dioxide, crospovidone, croscarmellose sodium, magnesium stearate, talc, MCC. In blisters and dark glass bottles;
  • Powder for suspension for oral administration containing 5 ml of the finished suspension of amoxicillin and clavulanic acid in the ratio of 125 mg / 31.25 mg, 250 mg / 62.5 mg, 400 mg / 57 mg and excipients: citric acid, sodium citrate , MCC and carmellose sodium, xanthan gum, colloidal silicon dioxide, wild cherry flavor and lemon flavor, sodium saccharinate, mannitol. In dark glass bottles;
  • Powder for solution for injection containing 1 vial of amoxicillin and clavulanic acid in the ratio of 500 mg / 100 mg, 1000 mg / 200 mg.

Pharmacological properties

Pharmacodynamics

Amoxicillin is a semi-synthetic penicillin that affects many gram-negative and gram-positive microorganisms. It inhibits the biosynthesis of peptidoglycan, a component that is part of the structure of the bacterial cell wall. A decrease in the production of peptidoglycan causes a decrease in the strength of cell walls, which further leads to lysis and death of cells of pathogens. At the same time, amoxicillin is sensitive to the action of beta-lactamases, which destroy it, so its spectrum of antibacterial activity does not include microorganisms that synthesize this enzyme.

Clavulanic acid is a beta-lactamase inhibitor whose structure is similar to that of penicillin. It has the ability to inactivate numerous beta-lactamases that produce microorganisms with proven resistance to cephalosporins and penicillins. The relative effectiveness of clavulanic acid against plasmid beta-lactamases, which most often cause antibiotic resistance in bacteria, has been proven. However, the substance does not act on chromosomal type I beta-lactamases that are not inhibited by clavulanic acid.

The presence of clavulanic acid in Amoxiclav prevents the destruction of amoxicillin by special enzymes - beta-lactamases - and expands the spectrum of antibacterial activity of amoxicillin.

Clinical studies in vitro prove high sensitivity to the action of Amoxiclav of the following microorganisms:

  • gram-negative anaerobes: varieties of the genus Prevotella, Bacteroides fragilis, other subspecies of the genus Bacteroides, varieties of the genus Porphyromonas, varieties of the genus Capnocytophaga, varieties of the genus Fusobacterium, Fusobacterium nucleatum, Eikenella corrodens;
  • gram-positive anaerobes: varieties of the genus Peptostreptococcus, Peptostreptococcus magnus, Peptostreptococcus micros, Peptococcus niger, varieties of the genus Clostridium;
  • gram-negative aerobes: Vibrio cholerae, Bordetella pertussis, Pasteurella multocida, Haemophilus influenza, Neisseria gonorrhoeae, Moraxella catarrhalis, Helicobacter pylori;
  • gram-positive aerobes: coagulase-negative staphylococci (showing sensitivity to methicillin), Staphylococcus saprophyticus (strains sensitive to methicillin), Staphylococcus aureus (strains sensitive to methicillin), Bacillus anthracis, Streptococcus agalactiae, Streptococcus pyogenes and other streptococci of the beta-hemolytic group, Enterococcus faecalisoccus , Nocardia asteroids, Listeria monocytogenes;
  • others: Treponema pallidum, Leptospira icterohaemorrhagiae, Borrelia burgdorferi.

The following microorganisms are characterized by acquired resistance to the active components of Amoxiclav:

  • gram-positive aerobes: streptococci of the Viridans group, Streptococcus pneumoniae, Enterococcus faecium, bacteria of the genus Corynebacterium;
  • gram-negative aerobes: bacteria of the genus Shigella, Escherichia coli, bacteria of the genus Salmonella, bacteria of the genus Klebsiella, Klebsiella pneumoniae (clinical studies confirm the effectiveness of the active ingredients of Amoxiclav in relation to this microorganism, also its strains do not synthesize beta-lactamase), Klebsiella oxytoca, bacteria of the genus Proteus , Proteus vulgaris, Proteus mirabilis.

Natural resistance to the combination of amoxicillin and clavulanic acid is demonstrated by such microorganisms:

  • gram-negative aerobes: bacteria of the genus Acinetobacter, Yersinia enterocolitica, Citrobacter freundii, Stenotrophomonas maltophilia, bacteria of the genus Enterobacter, bacteria of the genus Pseudomonas, Hafnia alvei, bacteria of the genus Serratia, Legionella pneumophila, bacteria of the genus Providencia, Morganella morganii;
  • others: bacteria of the genus Mycoplasma, Chlamydophila psittaci, Chlamydophila pneumoniae, bacteria of the genus Chlamydia, Coxiella burnetii.

The sensitivity of bacteria to amoxicillin monotherapy most often means similar sensitivity to the combination of amoxicillin and clavulanic acid.

Pharmacokinetics

The main pharmacokinetic parameters of amoxicillin and clavulanic acid are largely similar. Both substances show a good ability to dissolve in aqueous solutions having a physiological pH value, and after oral administration of Amoxiclav, they are rapidly and almost completely absorbed from the gastrointestinal tract. The degree of absorption of clavulanic acid and amoxicillin is considered optimal if the drug is taken at the beginning of a meal.

After oral administration, the bioavailability of the active components of Amoxiclav reaches 70%.

When appointed medicinal product at various doses, the pharmacokinetic parameters of amoxicillin and clavulanic acid are as follows:

  • at a dosage of 875 mg / 125 mg 2 times a day for amoxicillin: the maximum concentration in blood plasma is 11.64 ± 2.78 μg / ml, the time to reach it is 1.5 hours (range is from 1 to 2.5 hours) , area under the concentration-time curve (AUC) - 53.52 ± 12.31 μg h / ml, half-life - 1.19 ± 0.21 hours; for clavulanic acid: maximum plasma concentration - 2.18 ± 0.99 μg / ml, time to reach it - 1.25 hours (range is from 1 to 2 hours), area under the concentration-time curve (AUC) – 10.16 ± 3.04 µg×h/ml, elimination half-life – 0.96 ± 0.12 hours;
  • at a dosage of 500 mg / 125 mg 2 times a day for amoxicillin: the maximum concentration in blood plasma is 7.19 ± 2.26 μg / ml, the time to reach it is 1.5 hours (range is from 1 to 2.5 hours) , area under the concentration-time curve (AUC) - 53.5 ± 8.87 μg h / ml, half-life - 1.15 ± 0.2 hours; for clavulanic acid: maximum plasma concentration - 2.4 ± 0.83 μg / ml, time to reach it - 1.5 hours (range is from 1 to 2 hours), area under the concentration-time curve (AUC) – 15.72 ± 3.86 µg×h/ml, elimination half-life – 0.98 ± 0.12 hours;
  • at a dosage of 250 mg / 125 mg 3 times a day for amoxicillin: the maximum plasma concentration is 3.3 ± 1.12 μg / ml, the time to reach it is 1.5 hours (range is from 1 to 2 hours), the area under curve "concentration - time" (AUC) - 26.7 ± 4.56 μg h / ml, half-life - 1.36 ± 0.56 hours; for clavulanic acid: maximum plasma concentration - 1.5 ± 0.7 μg / ml, time to reach it - 1.2 hours (range is from 1 to 2 hours), area under the concentration-time curve (AUC) - 12.6 ± 3.25 μg h / ml, half-life - 1.01 ± 0.11 hours.

All the above values ​​are obtained as a result clinical research in which healthy volunteers participated.

Amoxicillin and clavulanic acid are characterized by a high volume of distribution in various tissues, organ systems and body fluids (including muscle, bone and adipose tissue, abdominal organs, lungs, interstitial, peritoneal, synovial and pleural fluids, sputum, bile, purulent discharge, urine and skin).

Active ingredients moderately bind to plasma proteins: amoxicillin in the amount of 18% and clavulanic acid in the amount of 25% of the dose taken. The volume of distribution is approximately 0.2 L/kg for clavulanic acid and 0.3–0.4 L/kg for amoxicillin. Both substances do not cross the blood-brain barrier in the absence of inflammation of the meninges. Amoxicillin, like many penicillins, passes into breast milk, which also contains clavulanic acid in trace concentrations. The active components of Amoxiclav penetrate the placental barrier.

Approximately 10-25% of the initial dose of amoxicillin is excreted in the urine as penicillic acid, which has no pharmacological activity. Clavulanic acid is extensively metabolized in the body, forming 1-amino-4-hydroxy-butan-2-one and 2,5-dihydro-4-(2-hydroxyethyl)-5-oxo-1H-pyrrole-3-carboxylic acid, which excreted through the gastrointestinal tract, kidneys, as well as with exhaled air (turning into the form of carbon dioxide).

Amoxicillin is eliminated predominantly by renal filtration, while clavulanic acid is eliminated by both renal and extrarenal mechanisms. After a single oral dose of 1 tablet of 500 mg / 125 mg or 250 mg / 125 mg, about 40-65% of clavulanic acid and 60-70% of amoxicillin are excreted unchanged in the urine during the first 6 hours.

On average, the half-life of the active components of Amoxiclav is approximately 1 hour, and the average total clearance is approximately 25 l / h in healthy patients. Most of the clavulanic acid is excreted from the body during the first 2 hours after ingestion.

In patients with renal dysfunction, the total clearance of clavulanic acid and amoxicillin decreases in proportion to the decrease in renal function. The decrease in clearance is more pronounced with amoxicillin than with clavulanic acid, since most of the dose of amoxicillin is excreted through the kidneys. In renal insufficiency, the dose of Amoxiclav should be selected taking into account the undesirability of amoxicillin accumulation against the background of a stable concentration of clavulanic acid that meets the standards. In patients with severe renal insufficiency, the half-life of amoxicillin increases to 7.5 hours, and clavulanic acid - up to 4.5 hours.

In patients with liver dysfunction, Amoxiclav is prescribed with caution, and constant monitoring of liver function is also recommended. Both amoxicillin and clavulanic acid are removed by hemodialysis, and in small concentrations by peritoneal dialysis.

Indications for use

According to the instructions, Amoxiclav is prescribed for the treatment of infectious and inflammatory diseases caused by drug-sensitive microorganisms. The drug is indicated for gynecological, odontogenic infections, as well as infections:

  • ENT organs and upper respiratory tract, including acute and chronic sinusitis, otitis media, tonsillitis, pharyngeal abscess, pharyngitis;
  • Connective and bone tissue;
  • Lower respiratory tract, including chronic bronchitis, acute bronchitis with bacterial superinfection, pneumonia;
  • urinary tract;
  • Skin and soft tissues, including animal and human bites;
  • bile ducts.

The use of Amoxiclav in the form of injections is indicated:

  • With infections of the abdominal cavity;
  • With sexually transmitted infections - gonorrhea, soft chancre;
  • To prevent the development of infections after surgical interventions.

Contraindications

Amoxiclav is not prescribed for cholestatic jaundice and hepatitis associated with the use of penicillin antibiotics. In addition, the remedy is contraindicated in:

  • Sensitivity to penicillin drugs, clavulanic acid, amoxicillin, other components of Amoxiclav;
  • infectious mononucleosis;
  • Lymphoid leukemia.

Amoxiclav is prescribed with caution when:

  • History of pseudomembranous colitis;
  • liver failure;
  • Severe impairment of kidney function.

The possibility of using Amoxiclav by pregnant and lactating women should be decided individually with the doctor.

Instructions for use Amoxiclav: method and dosage

Tablets and solution for suspension for oral administration

The regimen of taking the drug and the duration of therapy is determined depending on the severity of the infection, the age, kidney function of the patient and body weight. In tablets and suspensions, Amoxiclav is recommended to be taken with food, which will reduce the risk of side effects from the digestive system.

The average course of treatment is from 5-14 days. Longer treatment is possible only after a second medical examination.

The recommended dosage regimen for Amoxiclav tablets for children under 12 years of age is 40 mg / kg per day, which is divided into 3 doses. Children weighing more than 40 kg are shown adult dosages of the drug. For children under 6 years of age, it is preferable to use Amoxiclav suspension.

There are two schemes for taking Amoxiclav by adults with mild and moderate infections:

  • Every 8 hours, 1 tablet 250+125 mg;
  • Every 12 hours, 1 tablet 500+125 mg.

Against the background of a severe course of infection and with infections of the respiratory tract, one tablet of 500 + 125 mg should be taken every 8 hours or every 12 hours, 1 tablet of 875 + 125 mg.

For odontogenic infections, 1 tablet Amoxiclav 250+125 mg every 8 hours or 1 tablet 500+125 mg every 12 hours is indicated for 5 days.

Newborns and children under 3 months of age Amoxiclav is prescribed as a suspension at the rate of 30 mg / kg per day (according to amoxicillin). The medicine is taken every 12 hours. To comply with the dosage, use the dosing pipette supplied with the package.

The daily dosage of Amoxiclav for children older than 3 months is:

  • With mild and moderate severity of the course of the disease - from 20 mg / kg per day;
  • In severe infections and in the treatment of infections of the lower respiratory tract, otitis media, sinusitis - up to 40 mg / kg (amoxicillin) per day.

It should be borne in mind that when calculating dosages, it is necessary to rely not on the age of the child, but on his body weight and the severity of the course of the disease.

Injection

Amoxiclav in the form of a solution for injection is administered exclusively intravenously.

For children under 3 months, the dose is calculated based on the following information:

  • body weight less than 4 kg: Amoxiclav is administered at a dosage of 30 mg / kg (taking into account the conversion to the entire drug) every 12 hours;
  • body weight over 4 kg: Amoxiclav is administered at a dosage of 30 mg / kg (taking into account the conversion to the entire drug) every 8 hours.

Children who have not reached 3 months, the solution for injection should be administered only slowly by infusion over 30-40 minutes.

For children whose body weight does not exceed 40 kg, the dose is selected based on body weight.

For children aged 3 months to 12 years, the drug is administered at a dosage of 30 mg / kg of body weight (in terms of the entire drug) every 8 hours, and in the case of a severe course of an infectious disease - every 6 hours.

In children with diagnosed renal dysfunction, dose adjustments may be required based on the maximum recommended dose of amoxicillin. If in such patients the creatinine clearance exceeds 30 ml / min, a dose change is optional. In other cases, in children whose body weight does not exceed 40 kg, it is recommended to use Amoxiclav in the following dosages:

  • CC 10-30 ml / min: 25 mg / 5 mg per 1 kg of body weight every 12 hours;
  • CC less than 10 ml / min: 25 mg / 5 mg per 1 kg of body weight every 24 hours;
  • hemodialysis: 25 mg/5 mg per 1 kg of body weight every 24 hours in combination with an additional dose of 12.5 mg/2.5 mg per 1 kg of body weight at the end of the dialysis session (associated with a decrease in the concentrations of clavulanic acid and amoxicillin in blood serum).

Each 30 mg of the drug contains 25 mg of amoxicillin and 5 mg of clavulanic acid.

Adults and children over 12 years of age or weighing more than 40 kg Amoxiclav is administered at a dosage of 1200 mg of the drug (1000 mg + 200 mg) every 8 hours, and in the case of an acute course of an infectious disease - every 6 hours.

Amoxiclav is also prescribed for surgical interventions at a prophylactic dose, which is usually 1200 mg during induction anesthesia in cases where the operation lasts less than 2 hours. With longer surgical interventions, the patient receives the drug at a dose of 1200 mg up to 4 times for 1 day.

In patients suffering from renal insufficiency, the dose and / or time interval between injections of Amoxiclav should be adjusted depending on the degree of impaired renal function in accordance with the following instructions:

  • CC more than 30 ml / min: there is no need for dose adjustment;
  • CC 10-30 ml / min: the first dose is 1200 mg (1000 mg + 200 mg), after which the drug is administered intravenously at a dose of 600 mg (500 mg + 100 mg) every 12 hours;
  • CC less than 10 ml / min: the first dose is 1200 mg (1000 mg + 200 mg), after which the drug is administered intravenously at a dose of 600 mg (500 mg + 100 mg) every 24 hours;
  • anuria: the interval between injections of the drug should be increased to 48 hours or more.

Since up to 85% of the administered dose of Amoxiclav is removed during the hemodialysis procedure, the usual dose of the injection solution should be administered at the end of each session. With peritoneal dialysis, there is no need for dose adjustment.

The duration of the course of treatment is from 5 to 14 days (its exact duration can only be determined by the attending physician). With a decrease in the severity of symptoms, a transition to oral forms of Amoxiclav is recommended as a continuation of therapy.

When preparing a solution for injection, the contents of the vial in an amount of 600 mg (500 mg + 100 mg) are dissolved in 10 ml of water for injection, and in an amount of 1200 mg (1000 mg + 200 mg) in 20 ml of water for injection (this volume is not recommended exceed). The drug is administered intravenously slowly (over 3-4 minutes), and the introduction should be carried out within 20 minutes after the preparation of the solution.

Amoxiclav solution can also be used for intravenous infusion. In this case, prepared solutions containing 1200 mg (1000 mg + 200 mg) or 600 mg (500 mg + 100 mg) of the drug are further diluted in 100 ml or 50 ml of the infusion solution, respectively. The duration of the infusion reaches 30-40 minutes.

The use of the following liquids in the recommended volumes allows you to maintain the necessary concentrations of amoxicillin in the infusion solutions. Their periods of stability vary and are:

  • for water for injection: 4 hours at 25 °C and 8 hours at 5 °C;
  • for solutions of sodium chloride and calcium chloride for intravenous infusion: 3 hours at 25 ° C;
  • for Ringer's lactate solution for intravenous infusion: 3 hours at 25 °C;
  • for sodium chloride solution 0.9% for intravenous infusion: 4 hours at 25 °C and 8 hours at 5 °C.

Amoxiclav solution should not be mixed with solutions of sodium bicarbonate, dextran or dextrose. Only clear solutions are to be administered. The prepared solution must not be frozen.

Side effects

The use of Amoxiclav can lead to the development of side effects:

  • Hematopoietic system: anemia, eosinophilia, thrombocytopenia, agranulocytosis, leukopenia;
  • Digestive system: diarrhea, flatulence, gastritis, nausea, dyspepsia, glossitis, stomatitis, anorexia, enterocolitis, vomiting;
  • Nervous system: anxiety, inappropriate behavior, overexcitation, convulsions, confusion, insomnia, hyperactivity, dizziness, headache;
  • Skin: urticaria, edema, rash; less often - exfoliative dermatitis, epidermal toxic necrolysis, Stevens-Johnson syndrome, erythema multiforme;
  • Urinary system: interstitial nephritis, hematuria.

It is also possible to develop superinfection (including candidiasis).

In most cases, side effects against the background of the use of Amoxiclav are mild and transient.

Overdose

There are no reports that an overdose of Amoxiclav provokes serious side effects that threaten life or death.

Most often, an overdose is manifested by such symptoms as disorders of the water and electrolyte balance and dysfunction of the gastrointestinal tract (vomiting, diarrhea, pain in the abdomen). Sometimes taking amoxicillin can lead to the development of crystalluria, and in the future - renal failure. In patients with renal dysfunction or those receiving the drug in high doses, convulsive seizures are possible.

In case of an overdose of Amoxiclav, the patient should be under the supervision of a specialist who, if necessary, prescribes symptomatic therapy. If Amoxiclav was taken less than 4 hours ago, it is recommended to perform a gastric lavage and take activated charcoal to reduce absorption. The active components of the drug are well excreted from the body through hemodialysis.

special instructions

Taking Amoxiclav with meals reduces the likelihood of side effects from the gastrointestinal tract.

During course therapy, it is necessary to control the functions of the liver, hematopoiesis and kidneys.

Against the background of severe renal impairment, the doctor should adjust the dosing regimen or increase the interval between taking the medication.

Influence on the ability to drive vehicles and complex mechanisms

If during treatment with the drug the patient is diagnosed with adverse reactions from the central nervous system (for example, convulsions or dizziness), it is recommended to refrain from driving and performing work that requires increased concentration and immediate psychomotor reactions.

Use during pregnancy and lactation

In the course of animal experiments, the harm of taking Amoxiclav during pregnancy and the effect of the drug on embryonic development fetuses have not been confirmed. In a single study in women with premature rupture of the membranes, it was found that the prophylactic use of the combination of amoxicillin and clavulanic acid may increase the risk of neonatal necrotizing enterocolitis.

During pregnancy and lactation, the use of Amoxiclav is recommended only if the potential benefit of treatment for the mother significantly outweighs the possible risks to the health of the fetus and child. Clavulanic acid and amoxicillin in small concentrations are found in breast milk. Breastfed infants may develop diarrhea, sensitization, candidiasis of the mucous membranes oral cavity therefore, if treatment with the drug is necessary, it is advisable to stop breastfeeding.

For impaired renal function

Patients with moderate renal insufficiency (CC varies from 10 to 30 ml / min) are recommended to take Amoxiclav 1 tablet (dose 500 mg / 125 mg or 250 mg / 125 mg, depending on the severity of the disease) every 12 hours, and with severe renal insufficiency (CC is less than 10 ml / min) - 1 tablet (dose 500 mg / 125 mg or 250 mg / 125 mg, depending on the severity of the disease) every 24 hours.

The first dose of solution for intravenous administration with CC 10-30 ml / min is 1000 mg / 200 mg, then 500 mg / 100 mg every 12 hours. With CC less than 10 ml / min, the first dose of the solution for intravenous administration is 1000 mg / 200 mg, then 500 mg / 100 mg every 24 hours.

With anuria, the interval between doses of Amoxiclav is increased to 48 hours or more.

For impaired liver function

Patients with impaired liver function should take Amoxiclav with caution. During therapy, it is necessary to regularly monitor liver function.

Use in the elderly

Elderly patients do not need to adjust the dosing regimen.

drug interaction

Taking ascorbic acid together with Amoxiclav enhances the absorption of its active ingredients, and taking aminoglycosides, antacids, laxatives, glucosamine reduces their absorption. The use of non-steroidal anti-inflammatory drugs (NSAIDs), diuretics, phenylbutazone, allopurinol and other drugs that block tubular secretion (probenecid) increases the level of amoxicillin in the body (clavulanic acid is eliminated mainly through glomerular filtration). The combination of Amoxiclav and probenecid can lead to an increase and persistence in the blood concentration of amoxicillin, but not clavulanic acid, so the simultaneous use of drugs is prohibited.

The combination of amoxicillin, clavulanic acid and methotrexate enhances the toxic properties of methotrexate. The use of the drug in conjunction with allopurinol can provoke the development of skin allergic reactions. It is not recommended to prescribe Amoxiclav together with disulfiram.

The combination of amoxicillin and clavulanic acid reduces the effectiveness of drugs whose metabolism leads to the formation of para-aminobenzoic acid, and when taken with ethinyl estradiol, the risk of breakthrough bleeding increases.

In the literature, there are isolated reports of an increase in the international normalized ratio (INR) in patients while taking amoxicillin and warfarin or acenocoumarol. If it is necessary to combine Amoxiclav with anticoagulants, regular monitoring of INR or prothrombin time is recommended when canceling or starting treatment with the drug, since dose adjustment of oral anticoagulants may be required.

Co-administration of amoxicillin / clavulanic acid with rifampicin can lead to mutual weakening of the antibacterial action. Amoxiclav is not recommended for use even once in combination with bacteriostatic antibiotics (tetracyclines, macrolides) and sulfonamides due to the likely decrease in the effectiveness of amoxicillin / clavulanic acid.

Taking the drug leads to a decrease in the effectiveness of oral contraceptives. In patients taking mycophenolate mofetil, after the start of treatment with Amoxiclav, there is a decrease in the content of the active metabolite in the body - mycophenolic acid - by about 50% before taking the next dose of the drug. Variation in its concentration may not accurately reflect overall changes in exposure to a given metabolite.

Analogues

Analogues of Amoxiclav are:

  • By active substance- Bactoclav, Klamosar, Arlet, Panklav, Medoklav, Liklav, Augmentin, Rapiclav, Fibell, Ecoclave, Amovikomb, Amoksivan;
  • According to the mechanism of action - Libaktsil, Oksamp, Santaz, Ampioks, Tazotsin, Timentin, Sulacillin, Ampisid.

Terms and conditions of storage

The shelf life of tablets and solution is 2 years. Store in a dry place, at a temperature not exceeding 25°C. Keep away from children.

The shelf life of the finished suspension is 7 days. The finished suspension is stored at a temperature of 2-8°C.