Amoxicillin Sandoz, 0.5 g 12 pcs

Pharmacotherapeutic group

An antibiotic of the group of semisynthetic penicillins.

ATC code: J01CA04

Pharmacodynamic action

Pharmacodynamics

Amoxicillin is a semi-synthetic penicillin with bactericidal action.

The mechanism of bactericidal action of amoxicillin is associated with damage to the cell membrane of bacteria that are in the stage of reproduction. Amoxicillin specifically inhibits bacterial cell membrane enzymes (peptidoglycans), resulting in their lysis and death.

Active against:

Gram-positive aerobic bacteria

• Bacillus anthracis
• Corynebacterium spp. (except Corynebacterium jeikeium)
• Enterococcus faecalis
• Listeria monocytogenes
• Streptococcus spp. (including Streptococcus pneumoniae)
• Staphylococcus spp. (except penicillinase-producing strains).

Gram-negative aerobic bacteria

• Borrelia sp.
• Escherichia coli
• Haemophilus spp.
• Helicobacter pylori
• Leptospira spp.
• Neisseria spp.
• Proteus mirabilis
• Salmonella spp.
• Shigella spp.
• Treponema spp.
• Campylobacter

Others

• Chlamydia spp.

Anaerobic bacteria

• Bacteroides melaninogenicus
• Clostridium spp.
• Fusobacterium spp.
• Peptostreptococcus spp.

Inactive against:

Gram-positive aerobic bacteria

• Staphylococcus (β-lactamase-producing strains)<

Gram-negative aerobic bacteria

• Acinetobacter spp.
• Citrobacter spp.
• Enterobacter spp.
• Klebsiella spp.
• Moraxella catarrhalis
• Proteus spp.
• Providencia spp.
• Pseudomonas spp.
• Serratia spp.

Anaerobic bacteria

• Bacteroides spp.

Others

• Mycoplasma spp.
• Rickettsia spp.

Pharmacokinetics

The absolute bioavailability of amoxicillin depends on the dose and is 75 to 90%. The presence of food has no effect on absorption of the drug. After oral administration of amoxicillin in a single dose of 500 mg, the drug concentration in plasma is 6 – 11 mg/l. After oral administration the maximum concentration in plasma is reached after 1-2 hours.

From 15% to 25% of amoxicillin is bound to plasma proteins.

The drug quickly penetrates into lung tissue, bronchial secretion, middle ear fluid, bile and urine. In the absence of inflammation of the meninges amoxicillin penetrates into the cerebrospinal fluid in small amounts.

In inflammation of the meninges the drug concentrations in the cerebrospinal fluid may be 20% of its concentration in plasma. Amoxicillin penetrates through the placenta and is detected in small amounts in breast milk.

Up to 25% of the administered dose is metabolized to form inactive penicillic acid.

About 60-80% of amoxicillin is excreted unchanged by the kidneys within 6 to 8 hours after taking the drug.

A small amount of the drug is excreted in the bile.

The elimination half-life is 1-1.5 hours. In patients with terminal renal failure the half-life varies from 5 to 20 hours. The drug is excreted with 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

Pharmacotherapeutic group

Antibiotic of the group of semisynthetic penicillins.

ATX code: J01CA04

Pharmacodynamic action

Pharmacodynamics

Amoxicillin is a semi-synthetic penicillin that has a bactericidal effect.

The mechanism of the bactericidal action of amoxicillin is associated with damage to the cell membrane of bacteria that are in the reproduction stage. Amoxicillin specifically inhibits the enzymes of bacterial cell membranes (peptidoglycans), resulting in their lysis and death.

Active regarding:

Gram-positive aerobic bacteria

Bacillus anthracis
Corynebacterium spp. (except Corynebacterium jeikeium)
Enterococcus faecalis
Listeria monocytogenes
Streptococcus spp. (including Streptococcus pneumoniae)
Staphylococcus spp. (except for penicillinase-producing strains).
Gram-negative aerobic bacteria
Borrelia sp.
Escherichia coli
Haemophilus spp.
Helicobacter pylori
Leptospira spp.
Neisseria spp.
Proteus mirabilis
Salmonella spp.
Shigella spp.
Treponema spp.
Campylobacter
Others
Chlamydia spp.
Anaerobic bacteria
Bacteroides melaninogenicus
Clostridium spp.
Fusobacterium spp.
Peptostreptococcus spp.
Inactive regarding:

Gram-positive aerobic bacteria

Staphylococcus (β-lactamase-producing strains)
Gram-negative aerobic bacteria
Acinetobacter spp.
Citrobacter spp.
Enterobacter spp.
Klebsiella spp.
Moraxella catarrhalis
Proteus spp.
Providencia spp.
Pseudomonas spp.
Serratia spp.
Anaerobic bacteria
Bacteroides spp.
Others
Mycoplasma spp.
Rickettsia spp.
Pharmacokinetics

The absolute bioavailability of amoxicillin depends on the dose and ranges from 75 to 90%. The presence of food does not affect the absorption of the drug. As a result of oral administration of amoxicillin in a single dose of 500 mg, the concentration of the drug in plasma is 6–11 mg/l. After oral administration, maximum plasma concentration is achieved within 1-2 hours.

From 15% to 25% of amoxicillin is bound to plasma proteins.

The drug quickly penetrates into lung tissue, bronchial secretions, middle ear fluid, bile and urine. In the absence of inflammation of the meninges, amoxicillin penetrates into the cerebrospinal fluid in small quantities.

In case of inflammation of the meninges, the concentration of the drug in the cerebrospinal fluid may be 20% of its concentration in the blood plasma. Amoxicillin crosses the placenta and is found in small quantities in breast milk.

Up to 25% of the administered dose is metabolized to form inactive penicillic acid.

About 60-80% of amoxicillin is excreted unchanged by the kidneys within 6 to 8 hours after taking the drug.

A small amount of the drug is excreted in the bile.

The half-life is 1-1.5 hours. In patients with end-stage renal failure, the half-life varies from 5 to 20 hours. The drug is eliminated 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 0.5 g contains:

Core

Active ingredient: amoxicillin (in the form of amoxicillin trihydrate) 500.0 mg (574.0 mg).

Excipients: magnesium stearate 5.0 mg, povidone 12.5 mg, sodium carboxymethyl starch (type A) 20.0 mg, microcrystalline cellulose 60.5 mg.

Film coating: titanium dioxide 0.340 mg, talc 0.535 mg, hypromellose 2.125 mg.

Pregnancy

Amoxicillin can be used during pregnancy if the benefit to the mother outweighs the potential risk to the fetus.

Amoxicillin is excreted in breast milk in low concentrations. If it is necessary to use the drug during lactation, the issue of stopping breastfeeding should be decided.

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

The absorption time of digoxin may increase during therapy with Amoxicillin Sandoz.

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

4 years.

Manufacturer

Sandoz GmbH, Austria