Amoxicillin, 500 mg capsules 16 pcs

Pharmacotherapeutic group

Antibiotic, semi-synthetic penicillin

ATX code: J01CA04

Pharmacodynamics:

The semisynthetic aminopenicillin bactericidal acid-resistant broad-spectrum agent belongs to the group of beta-lactam antibiotics. It inhibits transpeptidase disrupts synthesis of peptidoglycan (support protein of cell wall) during division and growth causing lysis of bacteria.

Active against aerobic gram-positive bacteria: Bacillus anthracisCorynebacterium spp. EnterococcusfaecalisListeriamonocytogenesStaphylococcus spp. (except penicillinase-producing strains) Streptococcus spp.; including Streptococcuspneumoniae

Aerobic Gram-negative bacteria: BordetellapertussisBrucella spp. EscherichiacoliHaemophilusinfluenzaeKlebsiellaspp. NeisseriagonorrhoeaNeisseriameningitidesShigella spp. Salmonella spp. Pasteurellaseptica; Proteusmirabilis Vibriocholerae;

other microorganisms: Clostridium spp. Leptospira spp. and HelicobacterpyloriBorreliaburgdorferi.

Amoxicillin is degraded by beta-lactamases so its spectrum of antibacterial activity does not include microorganisms producing beta-lactamases (penicillinase, etc.).

Pharmacokinetics:

Absorption is fast high (about 93%) food intake has no effect on absorption; amoxicillin is not destroyed in the acidic environment of the stomach. Maximal concentration in plasma (Сmax) is reached after 1-2 hours (ТСmax) and is 35-5 µg/ml when administered orally in dose of 250 mg. The elimination half-life (T1/2) is 1-15 hours.

The binding to plasma proteins is about 17%. Intensively distributed in organs and tissues it is found in biological fluids and pathological secretions; it crosses histohematic barriers except for unchanged blood-brain barrier. In high concentrations found in blood plasma pulmonary bone and fat tissues intestinal mucosa female genital organs prostate gall bladder (with normal liver function) fetal tissues pleural and peritoneal fluid content of skin blisters sputum bronchial secretion (to a lesser extent in purulent discharges) in the exudate from middle ear inflammation.

The concentration in bile exceeds the concentration in blood plasma by 2-4 times. In amniotic fluid and umbilical cord vessels amoxicillin concentration is 25-30% of the value in the plasma of a pregnant woman. During inflammation of the brain membranes amoxicillin crosses the blood-brain barrier and its concentration in the cerebrospinal fluid reaches 20% of that in plasma. A small amount penetrates into breast milk. With increasing dose amoxicillin concentration in organs and tissues increases proportionally.

Partially metabolized to inactive penicillic acid. It is excreted mainly by the kidneys – 50-70% unchanged by tubular secretion (80%) and glomerular filtration (20%) through the intestine – 10 – 20%.

In case of impaired renal function (creatinine clearance less than or equal to 15 ml/min) the half-life is increased up to 85 hours.

Indications

Infectious and inflammatory diseases caused by microorganisms sensitive to amoxicillin:

upper respiratory tract infections (tonsillopharyngitis, sinusitis, acute otitis media);
lower respiratory tract infections (acute bacterial bronchitis, exacerbation of chronic bronchitis, community-acquired pneumonia);
infections of the genitourinary system (pyelonephritis, pyelitis, cystitis, urethritis, endometritis, cervicitis, gonorrhea);
abdominal infections (cholangitis, cholecystitis);
eradication of Helicobacter pylori in patients with gastric and duodenal ulcers (always in combination with other drugs);
infections of the skin and soft tissues (erysipelas, impetigo, secondary infected dermatoses);
leptospirosis, listeriosis;
Lyme disease;
infections of the gastrointestinal tract (enterocolitis, typhoid fever, dysentery, salmonellosis caused by Salmonella typhi, sensitive to ampicillin, salmonella carriage;
prevention of bacterial endocarditis during surgical procedures in the oral cavity and upper respiratory tract.

Pharmacological effect

Pharmacotherapeutic group

Antibiotic, semi-synthetic penicillin

ATX code: J01CA04

Pharmacodynamics:

Semi-synthetic aminopenicillin is a bactericidal, acid-resistant, broad-spectrum agent that belongs to the group of beta-lactam antibiotics. Inhibits transpeptidase, disrupts the synthesis of peptidoglycan (supporting protein of the cell wall) during the period of division and growth, causing lysis of bacteria.

Active against aerobic gram-positive bacteria: BacillusanthracisCorynebacterium spp. EnterococcusfaecalisListeriamonocytogenesStaphylococcus spp. (except for strains producing penicillinase) Streptococcus spp.; incl. Streptococcus pneumoniae

aerobic gram-negative bacteria: BordetellapertussisBrucella spp. EscherichiacoliHaemophilusinfluenzaeKlebsiellaspp. NeisseriagonorrhoeaNeisseriameningitidesShigella spp. Salmonella spp. Pasteurellaseptica; Proteusmirabilis Vibriocholerae;

other microorganisms: Clostridium spp. Leptospira spp. as well as Helicobacter pylori Borrelia burgdorferi.

Amoxicillin is destroyed by beta-lactamases; therefore, the spectrum of its antibacterial activity does not include microorganisms that produce beta-lactamases (penicillinase, etc.).

Pharmacokinetics:

Absorption is fast, high (about 93%), food intake does not affect absorption; amoxicillin is not destroyed in the acidic environment of the stomach. When taken orally at a dose of 250 mg, the maximum concentration in the blood plasma (Cmax) is reached after 1-2 hours (TCmax) and is 35-5 mcg/ml. Half-life (T1/2) -1-15 hours.

Plasma protein binding is about 17%. Intensely distributed throughout organs and tissues, found in biological fluids and pathological discharge; overcomes histohematic barriers except the unchanged blood-brain barrier. It is found in high concentrations in the blood plasma of the lungs, bone and fatty tissues, the intestinal mucosa, the female genital organs, the prostate gland, the gallbladder (with normal liver function), the tissues of the fetus, the pleural and peritoneal fluid, the contents of skin blisters, sputum, bronchial secretions (to a lesser extent in purulent discharge) in the exudate of inflammation of the middle ear.

The concentration in bile exceeds the concentration in blood plasma by 2-4 times. In the amniotic fluid and umbilical cord vessels, the concentration of amoxicillin is 25-30% of the value in the plasma of a pregnant woman. When there is inflammation of the meninges, amoxicillin overcomes the blood-brain barrier; its concentration in the cerebrospinal fluid reaches 20% of that in the blood plasma. Passes into breast milk in small quantities. As the dose increases, the concentration of amoxicillin in organs and tissues increases proportionally.

Partially metabolized to inactive penicillic acid. It is excreted primarily by the kidneys – 50-70% unchanged through tubular secretion (80%) and glomerular filtration (20%) through the intestine – 10 – 20%.

If renal function is impaired (creatinine clearance less than or equal to 15 ml/min), the half-life increases to 85 hours.

Special instructions

In patients with hypersensitivity to cephalosporins and carbapenems, the possibility of cross-allergy should be taken into account.

For severe gastrointestinal infections accompanied by persistent diarrhea or vomiting, amoxicillin should not be administered orally due to the possibility of poor absorption.

The use of antibiotics is ineffective in the treatment of acute respiratory viral infections.

Particular caution should be observed in patients with allergic diathesis or bronchial asthma and hay fever (hay fever), a history of gastrointestinal diseases (especially colitis associated with the use of antibiotics).

When taking Amoxicillin for a long time, nystatin, levorin or other antifungal drugs should be prescribed simultaneously.

With long-term use of high doses of the drug in patients, liver and kidney function indicators should be monitored and general urine tests should be performed. It is advisable to monitor the peripheral blood picture.

Active ingredient

Amoxicillin

Composition

1 capsule 500 mg contains:

active ingredient:

amoxicillin 500.00 mg (in the form of amoxicillin trihydrate 573.9 mg);

excipients – magnesium stearate 9.20 mg, microcrystalline cellulose PH 102 – 26.90 mg; capsule No. 0: gelatin up to 96 mg; capsule cap: titanium dioxide [E 171] – 0.49920 mg, sunset yellow dye [E PO] – 0.13774 mg, azorubine dye [E 122] – 0.13336 mg; capsule body: titanium dioxide [E 171] -0.57600 mg, iron dye yellow oxide [E 172] -0.26899 mg.

Pregnancy

There is currently no data on the possible embryotoxic, teratogenic or mutagenic effects of the drug when taken during pregnancy.

Amoxicillin is found in breast milk, which should be taken into account when prescribing Amoxicillin during lactation.

Contraindications

Hypersensitivity to amoxicillin, other beta-lactam antibiotics (other penicillins, cephalosporins, monobactams, carbapenems) or any components of the drug;
infectious mononucleosis, lymphocytic leukemia;
children up to 3 years of age (for this dosage form).
With caution:

Allergic reactions (including bronchial asthma, hay fever, hypersensitivity to acetylsalicylic acid) in the anamnesis, diseases of the gastrointestinal tract in the anamnesis (especially colitis associated with the use of antibiotics), renal failure, pregnancy and breastfeeding.

Side Effects

Allergic reactions:

urticaria, skin rash, erythema, exanthema, Quincke’s edema, rhinitis, conjunctivitis, photosensitivity; rarely – fever, joint pain, eosinophilia; in isolated cases – anaphylactic shock.

Others:

Superinfection may develop with the appearance of loose stools and nausea.

Interaction

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

Ethanol reduces the rate of absorption of amoxicillin.

Amoxicillin increases the absorption of digoxin.

Probenecid, competing for the elimination route, slows down the elimination of amoxicillin, which leads to an increase in the concentration of amoxicillin in the blood plasma. Similarly, amoxicillin interacts with diuretics and non-steroidal anti-inflammatory drugs (oxyphenbutazone, phenylbutazone, acetylsalicylic acid, indomethacin).

Amoxicillin helps reduce the clearance of methotrexate, which can lead to the development of toxic effects of the latter.

When taking allopurinol simultaneously, the risk of developing allergic skin reactions increases.

Amoxicillin, by suppressing intestinal microflora, helps reduce the synthesis of vitamin K and the prothrombin index, which increases the effectiveness of indirect anticoagulants and drugs, during the metabolism of which para-aminobenzoic acid is formed, which ultimately increases the risk of breakthrough bleeding.

Amoxicillin reduces the effectiveness of oral contraceptives, since under conditions of altered intestinal biocenosis, estrogen reabsorption decreases.

When amoxicillin is used together with bactericidal antibiotics (aminoglycosides, cephalosporins, cycloserine, vancomycin, rifampicin), a synergistic antibacterial effect is observed. Bacteriostatic drugs (macrolides, chloramphenicol, lincosamides, tetracyclines, sulfonamides), on the contrary, weaken the bactericidal effect of amoxicillin.

Metronidazole increases the antibacterial activity of amoxicillin.

Storage conditions

Store in a dry place, protected from light, at room temperature.

Shelf life

2 years.

Manufacturer

Hemofarm A.D., Serbia