Amoxicillin, tablets 500 mg 20 pcs

Amoxicillin is an antibacterial bactericidal acid-resistant broad-spectrum agent of the group of semisynthetic penicillins.

Inhibits transpeptidase, disrupts the synthesis of peptidoglycan (supporting protein of the cell wall) during division and growth, causes lysis of bacteria.

The drug is active against both Gram-positive and Gram-negative microorganisms due to its wide spectrum of action. Clinically relevant gram-negative microorganisms sensitive to amoxicillin include Escherichia coli, Proteus mirabilis, Salmonella, Shigella, Campilobacter, Haemophilus influenzae, Bordetella pertussis, Leptospira, Chlamydia.

In addition, amoxicillin is active against all microorganisms sensitive to penicillin G, such as Streptococcus group A,B,C,G,H,I,M, Streptococcus pneumoniae, Staphylococcus and Neisseria spp, not producing penicillinase, Erysipelothrix rhysiopathiae, Corynebacterium, Bacillus anthracis, Actinomycetes, Streptobacilli, Spirillium minus, Pastereulla multocida, Listeria, Spirochaeta (Leptospira, Treponema, Borrelia) and others, as well as various anaerobic microorganisms (including peptococci, peptostreptococci, clostridia and fusobacteria).

Pharmacokinetics

Absorption – fast, high (93%), food intake has no effect on absorption, is not destroyed in the acidic environment of the stomach. When taken orally in doses of 125 and 250 mg, the maximum concentration is 1.5-3 mcg/ml and 3.5-5 mcg/ml, respectively. The action develops 15-30 minutes after administration and lasts for 8 hours.

The time to reach maximum concentration after oral administration is 1-2 hours. It has a large volume of distribution – high concentrations are found in plasma, sputum, bronchial secretion (poor distribution in purulent bronchial secretion), pleural and peritoneal fluid, urine, contents of skin blisters, lung tissue, mucosa, female genitalia, prostate gland, middle ear fluid, bone, fatty tissue, gall bladder (with normal liver function), fetal tissues.

If the dose is increased by a factor of 2, the concentration also increases by a factor of 2. The concentration in bile exceeds the concentration in plasma by 2-4 times. In amniotic fluid and umbilical cord vessels, the concentration of amoxicillin is 25-30% of the level in plasma of a pregnant woman. It penetrates poorly through the blood-brain barrier; during inflammation of the meninges (meningitis) the concentration in the cerebrospinal fluid is about 20%. Binding with plasma proteins is 17%.

Partially metabolized to form inactive metabolites. Elimination half-life is 1-1.5 hours.

It is eliminated 50-70% unchanged by kidneys through tubular (80%) and glomerular filtration (20%), liver – 10-20%. A small amount is excreted with breast milk. In patients with impaired renal function (creatinine clearance less than or equal to 15 ml/min), half-life is increased up to 8.5 hours. Amoxicillin is eliminated by hemodialysis.

Indications

Amoxicillin is indicated for infectious and inflammatory diseases caused by bacteria that are not resistant to the drug:

infectious diseases of the upper and lower respiratory tract and ENT organs (angina, acute otitis media, pharyngitis, bronchitis, pneumonia, lung abscess);
infectious diseases of the genitourinary system (urethritis, pyelonephritis, pyelitis, chronic bacterial prostatitis, epididymitis; cystitis, adnexitis, septic abortion, endometritis, etc.);
gastrointestinal infections: bacterial enteritis. Combination therapy may be required for infections caused by anaerobic microorganisms;
infectious and inflammatory diseases of the biliary tract (cholangitis, cholecystitis);
eradication of Helicobacter pylori (in combination with proton pump inhibitors, clarithromycin or metronidazole);
skin and soft tissue infections;
leptospirosis, listeriosis, Lyme disease (borreliosis);
endocarditis (including prevention of endocarditis during dental procedures).

Pharmacological effect

Amoxicillin is a broad-spectrum antibacterial, acid-resistant, bactericidal agent from the group of semisynthetic penicillins.

Inhibits transpeptidase, disrupts the synthesis of peptidoglycan (supporting protein of the cell wall) during division and growth, and causes lysis of bacteria.

Due to the breadth of the spectrum of action, the drug is active against both gram-positive and gram-negative microorganisms. Clinically significant gram-negative microorganisms sensitive to amoxicillin include Escherichia coli, Proteus mirabilis, Salmonella, Shigella, Campilobacter, Haemophilus influenzae, Bordetella pertussis, Leptospira, Chlamydia.

In addition, amoxicillin is active against all microorganisms sensitive to penicillin G, for example, group A, B, C, G, H, I, M streptococci, Streptococcus pneumoniae, staphylococci and Neisseria spp., which do not produce penicillinase, Erysipelothrix rhysiopathiae, Corynebacterium, Bacillus anthracis, Actinomycetes, Streptobacilli, Spirillium minus, Pastereulla multocida, Listeria, Spirochaeta (Leptospira, Treponema, Borrelia) and others, as well as various anaerobic microorganisms (including peptococci, peptostreptococci, clostridia and fusobacteria).

Pharmacokinetics

Absorption – fast, high (93%), food intake does not affect absorption, is not destroyed in the acidic environment of the stomach. When taken orally at a dose of 125 and 250 mg, the maximum concentration is 1.5-3 mcg/ml and 3.5-5 mcg/ml, respectively. The action develops 15-30 minutes after application and lasts 8 hours.

The time to reach maximum concentration after oral administration is 1-2 hours. It has a large volume of distribution – high concentrations are found in plasma, sputum, bronchial secretions (in purulent bronchial secretions the distribution is weak), pleural and peritoneal fluid, urine, the contents of skin blisters, lung tissue, intestinal mucosa, female genital organs, prostate gland, middle ear fluid, bone, adipose tissue, bile bladder (with normal liver function), fetal tissues.

When the dose is doubled, the concentration also doubles. The concentration in bile exceeds the concentration in plasma by 2-4 times. In the amniotic fluid and umbilical cord vessels, the concentration of amoxicillin is 25-30% of the level in the plasma of a pregnant woman. It penetrates the blood-brain barrier poorly; in case of inflammation of the meninges (meningitis), the concentration in the cerebrospinal fluid is about 20%. Communication with plasma proteins – 17%.

Partially metabolized to form inactive metabolites. The half-life is 1-1.5 hours.

It is excreted 50-70% unchanged by the kidneys by tubular excretion (80%) and glomerular filtration (20%), by the liver – 10-20%. A small amount is excreted in breast milk. If renal function is impaired (creatinine clearance less than or equal to 15 ml/min), the half-life increases to 8.5 hours. Amoxicillin is removed by hemodialysis.

Special instructions

During a course of treatment, it is necessary to monitor the state of the function of the hematopoietic organs, liver and kidneys. It is possible that superinfection may develop due to the growth of microflora that is insensitive to it, which requires a corresponding change in antibacterial therapy.

When prescribed to patients with bacteremia, the development of a bacteriolysis reaction (Jarisch-Herxheimer reaction) is possible.

In patients who are hypersensitive to penicillins, cross-allergic reactions with cephalosporin antibiotics are possible.

When treating mild diarrhea during a course of treatment, antidiarrheal drugs that reduce intestinal motility should be avoided; You can use kaolin- or attapulgite-containing antidiarrheal agents. If diarrhea is severe, consult a doctor.

Treatment must continue for another 48-72 hours after the disappearance of clinical signs of the disease.

When using estrogen-containing oral contraceptives and amoxicillin simultaneously, other or additional methods of contraception should be used if possible.

Active ingredient

Amoxicillin

Composition

1 tablet contains:

active ingredient:

amoxicillin trihydrate (in terms of amoxicillin) – 500 mg.

Contraindications

hypersensitivity to penicillin and other components of the drug;
hypersensitivity to other beta-lactam antibiotics, such as cephalosporins, carbopenems (possibility of cross-reaction);
children under 3 years of age (for this dosage form).

The drug should be used with caution in patients with impaired renal function; severe digestive disorders accompanied by constant vomiting and diarrhea; allergic diathesis; asthma; hay fever; with viral infections; with acute lymphoblastic leukemia; infectious mononucleosis (due to an increased risk of erythematous skin rash); in children over three years of age.

Side Effects

The frequency of side effects is presented in accordance with the following gradation: very common – more than 10%; frequent – from 1 to 10%; infrequent – from 0.1 to 1%; rare – from 0.01 to 0.1%; very rare – less than 0.01%.

From the cardiovascular system: frequent – tachycardia, phlebitis; rare – decreased blood pressure; very rare – prolongation of the QT interval.

From the blood and lymphatic system: frequent – eosinophilia, leukopenia; rare – neutropenia, thrombocytopenia, agranulocytosis; very rare – anemia (including hemolytic), thrombocytopenic purpura, pancytopenia.

From the nervous system: frequent – drowsiness, headache, dizziness; rare – nervousness, agitation, anxiety, ataxia, behavior changes, peripheral neuropathy, anxiety, sleep disturbance, depression, paresthesia, tremor, confusion, convulsions; very rare – hyperesthesia, impaired vision, smell and tactile sensitivity, hallucinations.

From the genitourinary system: rare – interstitial nephritis, increased concentration of creatinine in the blood serum.

From the gastrointestinal tract and liver: dysbacteriosis, changes in taste, stomatitis, glossitis; frequent – nausea, diarrhea, increased liver parameters (ALT, AST, alkaline phosphatase, γ-glutamyltransferase), increased concentration of bilirubin in the blood serum; rare – vomiting, dyspepsia, epigastric pain, hepatitis, cholestatic jaundice; very rare – acute liver failure, diarrhea mixed with blood, pseudomembranous colitis, the appearance of a black color of the tongue.

From the musculoskeletal system: rare – arthralgia, myalgia, tendon diseases including tendonitis; very rare – tendon rupture (possible bilaterally and 48 hours after the start of treatment), muscle weakness, rhabdomyolysis.

Skin disorders: frequent – pruritis, rash; rare – urticaria; very rare – photosensitivity, swelling of the skin and mucous membranes, malignant exudative erythema (Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell’s syndrome).

From the endocrine system: rare – anorexia; very rare – hypoglycemia, especially in patients with diabetes.

From the respiratory system: rare – bronchospasm, dyspnea; very rare – allergic pneumonitis.

General: rare – general weakness; very rare – increased body temperature.

Other: difficulty breathing, vaginal candidiasis; rare – superinfection (especially in patients with chronic diseases or reduced body resistance), reactions similar to serum sickness; isolated cases – anaphylactic shock.

Interaction

It is possible that the absorption time of digoxin may increase during Amoxicillin therapy.

Probenecid reduces the excretion of amoxicillin by the kidneys and increases the concentration of amoxicillin in bile and blood.

The simultaneous use of amoxicillin and other bacteriostatic drugs (macrolides, tetracyclines, sulfonamides, chloramphenicols) should be avoided due to the possibility of developing antagonism. With the simultaneous use of aminoglycosides and amoxicillin, a synergistic effect may develop.

The simultaneous use of amoxicillin and disulfiram is not recommended.

With the simultaneous use of methotrexate and amoxicillin, an increase in the toxicity of the former is possible, probably due to the competitive inhibition of renal tubular secretion of methotrexate by amoxicillin.

Antacids, glucosamine, laxatives, food, aminoglycosides slow down and reduce absorption, while ascorbic acid increases the absorption of amoxicillin.

Increases the effectiveness of indirect anticoagulants (suppressing intestinal microflora, reduces the synthesis of vitamin K and the prothrombin index); reduces the effectiveness of estrogen-containing oral contraceptives; medications, during the metabolism of which para-aminobenzoic acid (PABA) is formed, ethinyl estradiol preparations – the risk of developing “breakthrough” bleeding.

Diuretics, allopurinol, oxyphenbutazone, phenylbutazone, non-steroidal anti-inflammatory drugs and other drugs that block tubular secretion increase the concentration of amoxicillin in the blood.

Allopurinol increases the risk of developing skin rashes.

Overdose

Symptoms: nausea, vomiting, diarrhea, water and electrolyte imbalance (as a result of vomiting and diarrhea).

Treatment: gastric lavage, activated carbon, saline laxatives, medications to maintain water and electrolyte balance; hemodialysis.

Storage conditions

In a dry place, protected from light, at a temperature not exceeding 25 ° C. Keep out of the reach of children.

Shelf life

2 years.

Manufacturer

Barnaul plant, Russia