Pharmacological properties: Amoxicillin is a broad-spectrum bactericidal acid-resistant antibiotic from the group of semi-synthetic penicillins. It is active against gram-positive and gram-negative microorganisms, such as Streptococcus pyogenes, Streptococcus pneumoniae, Clostridium tetani, Clostridium welchii, Neisseria gonorrhoeae, Neisseria meningitidis, Staphylococcus aureus(not producing betalactamases), Bacillus anthracis, Listeria monocytogenes, Helicobacter pylori. Less active against Enterococcus faecalis, Escherichia coli, Proteus mirabilis, Salmonella typhi, Shigella sonnei, Vibrio cholerae.
Inactive against microorganisms producing beta-lactamases Pseudomonas spp., Indole-positive Proteus spp., Serratia spp., Enterobacter spp.
In combination with metronidazole, it is active against Helicobacter pylori.
Pharmacokinetics: After oral administration, amoxicillin is absorbed rapidly and almost completely (about 93%), acid-resistant. Eating practically does not affect the absorption of the drug. The maximum concentration of the active substance in the plasma is observed after 1-2 hours. After oral administration of 500 mg of amoxicillin, the maximum concentration of the active substance, 5 μg / ml, is observed in the blood plasma after 2 hours. With an increase or decrease in the dose of the drug by 2 times, the maximum concentration in the blood plasma also changes by 2 times. About 20% of amoxicillin binds to plasma proteins. Amoxicillin penetrates well into the mucous membranes, bone tissue, intraocular fluid and sputum in therapeutically effective concentrations. The concentration of amoxicillin in bile exceeds its concentration in blood plasma by 2-4 times. In amniotic fluid and umbilical vessels, the concentration of amoxicillin is 25-30% of its level in the blood plasma of a pregnant woman. Amoxicillin penetrates poorly through the BBB; however, with inflammation of the meninges, the concentration in the cerebrospinal fluid is about 20% of the concentration in the blood plasma.
Amoxicillin is partially metabolized in the liver; most of its metabolites do not have microbiological activity. About 60% of the oral dose of amoxicillin is eliminated unchanged by the kidneys (about 80% by tubular excretion, 20% by glomerular filtration). In the absence of impaired renal function, the half-life dreeding period of amoxicillin is 1-1.5 hours. In premature infants, newborns, and children under 6 months of age. – 3-4 hours
Pharmacokinetics in special clinical cases: The half-life breeding period of amoxicillin does not change with impaired liver function.
In case of impaired renal function (creatinine clearance <15 ml / min), the half-life breeding period of amoxicillin can increase and reaches 8.5 hours with anuria.
Indications for use: Infectious and inflammatory diseases caused by microorganisms sensitive to the drug:
– respiratory infections;
– infections of the genitourinary system;
– gastrointestinal tract infections;
– infections of the skin and soft tissues;
– endocarditis (prevention)
Infections associated with Helicobacter pylori in chronic gastritis, gastric ulcer and 12 duodenal ulcer in the acute phase (in combination with metronidazole).
Dosage and administration: A suspension is prepared from amoxicillin powder. To do this, first shake the powder in a bottle, then add boiled and then cooled to room temperature drinking water to the mark “100 ml” and shake vigorously. After the foam has settled, add an additional volume of the suspension to 100 ml with water and shake well. The suspension is ready to use.
Before each use, the vial is shaken vigorously and left to stand until the resulting foam settles.
The dosage regimen is set individually, depending on the sensitivity of microorganisms and the localization of the infectious process.
Inside. Adults are prescribed on average 1.5-2 g / day. If necessary, the dose can be increased to 3 g / day. Multiplicity of admission is 3 times / day.
Adults with acute infectious diseases of the gastrointestinal tract (paratyphoid fever, typhoid fever) and biliary tract, as well as with gynecological infectious diseases, the drug is prescribed 1.5-2 g 3 times / day or 1-1.5 g 4 times / day.
With leptospirosis, adults are prescribed 500-750 mg 4 times / day for 6-12 days.
With salmonella carriage for adults – 1.5-2 g 3 times / day for 2-4 weeks.
For the prevention of endocarditis with minor surgical interventions, adults are administered 3-4 g 1 hour before the procedure. If necessary, a repeated dose is prescribed after 8-9 hours.
In acute uncomplicated gonorrhea in men, 3 g of the drug is prescribed in 1 dose in combination with 1 g of probenecid. In the treatment of gonorrhea in women, the indicated dose is recommended to be repeated.
In the treatment of infections associated with Helicobacter pylori – chronic gastritis in the acute phase, peptic ulcer and 12 duodenal ulcer in the acute phase: 500 mg 3 times / day for 10 days in conjunction with metronidazole.
In children, the dose should be halved.
Treatment should be continued for 2-5 days after the symptoms disappear. To prevent complications of streptococcal infections, at least 10 days should be treated.
In patients with impaired renal function with (CC) below 30 ml / min, the dose is reduced and / or the interval between doses is increased. With a CC of 15-40 ml / min, the interval between doses of the drug should be at least 12 hours. In patients with anuria, the dose of the drug should not exceed 2 g / day.
In infectious diseases of the genitourinary tract, dose adjustment is not required.
For children, the drug is prescribed in doses of 30-60 mg / kg / day. Multiplicity of admission – 2 times / day.
|till 1 year||250 мg|
|1-6 years||500 мg|
|6-10 years||750 мg|
|10-14 years||1 g|
|14-18 years||1,5 g|
In severe cases of an infectious disease, the dose for children can be increased to 100 mg / kg / day. In premature and newborns, the dose of the drug is reduced and / or the interval between doses is increased.
Side effects: From the digestive tract: rarely – a change in taste, nausea, vomiting, diarrhea; in some cases, a moderate increase in the activity of “liver” transaminases, and extremely rarely, pseudomembranous and hemorrhagic colitis.
From the urinary system: extremely rarely – the development of interstitial nephritis.
From the hemopoietic system: agranulocytosis, neutropenia, thrombocytopenia, hemolytic anemia are possible, but they are also extremely rare.
Side effects from the nervous system when using amoxicillin are not registered.
Allergic reactions: skin reactions, mainly in the form of a specific maculopapular rash; rarely – erythema multiforme exudative (Stevens-Johnson syndrome); in some cases – anaphylactic shock, angioedema.
Contraindications: Polyvalent hypersensitivity to xenobiotics, including both the drug and other beta-lactam antibiotics, cephalosporins, infectious mononucleosis, lymphocytic leukemia, bronchial asthma, hay fever, allergic diathesis, gastrointestinal diseases in the anamnesis (especially colitis associated with the use of antibiotics, pregnancy) lactation period.
When used with metronidazole – diseases of the nervous system, hypersensitivity to nitroimidazole derivatives.
Drug interactions: Probenecid, phenylbutazone, oxyphenbutazone, to a lesser extent acetylsalicylic acid and sulfinpyrazone inhibit tubular secretion of penicillins, which leads to an increase in the half-life and an increase in the concentration of amoxicillin in blood plasma. Bactericidal antibiotics (including aminoglycosides, cephalosporins, vancomycin, rifampicin), while taking a synergistic effect; antagonism is possible when taken with certain bacteriostatic drugs (for example, chloramphenicol, sulfonamides). Concomitant use with estrogen-containing oral contraceptives can lead to a decrease in their effectiveness and an increase in the risk of “breakthrough” bleeding. Simultaneous administration with allopurinol does not increase the frequency of skin reactions, unlike the combination of allopurinol with ampicillin.
Special instructions: A presence of erythroderma is not a contraindication for the administration of amoxicillin. Cross-resistance or hypersensitivity to penicillin preparations and cephalosporins is possible. As with other penicillin drugs, superinfection is possible.
The appearance of severe diarrhea, characteristic of pseudomembranous colitis, is an indication for drug withdrawal. Prescribe the drug to patients with infectious mononucleosis and lymphocytic leukemia with caution, because the occurrence of exanthema of non-allergic genesis is high.
Pregnancy and lactation: It is possible to prescribe the drug during pregnancy and lactation if the expected positive result from the use of the drug exceeds the risk of side effects. In small amounts, amoxicillin is excreted in breast milk, which can lead to the development of sensitization phenomena in the baby.
The drug should be stored out of the reach of children and not used after the expiration date.
Overdose: Symptoms: violation of the gastrointestinal tract – nausea, vomiting, diarrhea; the result of vomiting and diarrhea may be a violation of the water-electrolyte balance.
Treatment: prescribe gastric lavage, activated charcoal, saline laxatives; apply measures to restore the water-electrolyte balance, hemodialysis.
Release form: Powder for suspension 125 mg / 5 ml or 250 mg / 5 ml. 24 g in plastic bottles with dispensing spoons.
Storage conditions: In a dry, dark place, at a temperature of no higher than 25ºС.
Shelf life: 2 years. The prepared suspension is 7 days when stored in the refrigerator at a temperature of 10°C.
Pharmacy sales terms: On prescription.