Amoxicillin Sandoz

1 coated tablet contains:

active substance:

amoxicillin trihydrate 574 (equivalent to 0.5 amoxicillin, respectively),     

excipients :

magnesium stearate;

polyvidone;

sodium carboxymethyl starch (type A);

MCC 

  
film sheath:

titanium dioxide; talc; hypromellose

 Amoxicillin is an antibacterial bactericidal acid-resistant broad-spectrum agent from the group of semi-synthetic penicillins. It inhibits transpeptidase, disrupts the synthesis of peptidoglycan (supporting protein of the cell wall) during the period of 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 rhysiopathiterium rhysiopathiterium , Bacillus anthracis, Actinomycetes, Streptobacilli, Spirillium minus, Pastereulla multocida, Listeria, Spirochaeta (Leptospira, Treponema, Borrelia) and others, as well as various anaerobic microorganisms (including peptococcus, peptostreptococcus, clostridia and

 Pharmacokinetics

Absorption is fast, high (93%), food intake does not affect absorption, does not break down 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 μg / ml and 3.5-5 μg / 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 secretion (in the purulent bronchial secretion, the distribution is weak), pleural and peritoneal fluid, urine, the contents of skin blisters, lung tissue , intestinal mucosa, female genitals, prostate gland, middle ear fluid, bone, adipose tissue, gall bladder (with normal liver function), fetal tissues.

With an increase in the dose by 2 times, the concentration also increases by 2 times. The concentration in bile exceeds the concentration in plasma by 2-4 times. In amniotic fluid and vessels of the umbilical cord, the concentration of amoxicillin is 25-30% of the plasma level of a pregnant woman. It penetrates poorly through the blood-brain barrier, with 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 elimination half-life is 1-1.5 hours.

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

Amoxicillin is indicated for infectious and inflammatory diseases caused by non-drug-resistant bacteria:

• infectious diseases of the upper and lower respiratory tract and ENT organs (tonsillitis, 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);
• Helicobacter pylori eradication (in combination with proton pump inhibitors, clarithromycin or metronidazole);
• infections of the skin and soft tissues;
• leptospirosis, listeriosis, Lyme disease (borreliosis);
• endocarditis (including prevention of endocarditis during dental procedures).

It is possible to use amoxicillin during pregnancy when the benefit to the mother outweighs the potential risk to the fetus.

Amoxicillin is excreted in breast milk in low concentrations. If necessary, the use of the drug during lactation should decide on the termination of breastfeeding.

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

With caution, the drug should be used 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 the increased risk of an erythematous rash on the skin); in children over the age of three.

The incidence of side effects is described in accordance with the following gradation: very frequent - 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 CCC: frequent - tachycardia, phlebitis; rare - lowering blood pressure; very rare - lengthening of the QT interval.

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

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

From the genitourinary system: rare - interstitial nephritis, an increase in the concentration of creatinine in the blood serum.

From the gastrointestinal tract and liver: dysbiosis, taste change, stomatitis, glossitis; frequent - nausea, diarrhea, an increase in hepatic indices (ALT, AST, alkaline phosphatase, γ-glutamyltransferase), an increase in the concentration of bilirubin in blood serum; rare - vomiting, dyspepsia, epigastric pain, hepatitis, cholestatic jaundice; very rare - acute liver failure, diarrhea with an admixture of blood, pseudomembranous colitis, the appearance of a black color of the tongue.

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

On the part of the skin: frequent - pruritus, 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 - fever.

Other: shortness of breath, vaginal candidiasis; rare - superinfection (especially in patients with chronic diseases or low body resistance), reactions similar to serum sickness; isolated cases - anaphylactic shock.

It is possible to increase the absorption time of digoxin during Amoxicillin Sandoz 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, sulfanilamides, chloramphenicol) should be avoided due to the possibility of antagonism. With the simultaneous use of aminoglycosides and amoxicillin, the development of a synergistic effect is possible.

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 competitive inhibition of tubular renal secretion of methotrexate by amoxicillin.

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

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

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 a skin rash.

Inside, before or after a meal.

Adults and children over 10 years old (with a body weight of more than 40 kg) are prescribed 0.5 g 3 times a day; in severe infections - 0.75-1 g 3 times a day.

In acute uncomplicated gonorrhea, 3 g is prescribed once; in the treatment of women, a repeated dose of this dose is recommended.

In acute infectious diseases of the gastrointestinal tract (paratyphoid fever, typhoid fever) and biliary tract, in case of gynecological infectious diseases for adults - 1.5-2 g 3 times a day or 1-1.5 g 4 times a day.

In severe infections (meningitis, septicemia) adults - up to 6 g per day in 3-4 doses. Children - 250-500 mg 3 times a day. The duration of treatment depends on the indications and clinical presentation and is usually 5-7 days. With otitis media and similar infections in children, a two-time administration of Amoxicillin is sufficient. In cases of chronic diseases, recurrent infections, severe infections, adults are prescribed 750 mg - 1 g 3 times a day, children up to 60 mg / kg per day are divided into 3 doses.

With leptospirosis for adults - 0.5-0.75 g 4 times a day for 6-12 days.

With listeriosis, adults - 0.5 g 3 times a day for 6-12 days.

With salmonella carriage for adults - 1.5-2 g 3 times a day for 2-4 weeks.

For the prevention of endocarditis with minor surgical interventions for adults - 3-4 g 1 hour before the procedure. If necessary, a repeated dose is prescribed after 8-9 hours.

In children, the dose is halved.

In patients with impaired renal function with creatinine clearance of 15-40 ml / min, the interval between doses is increased to 12 hours; with creatinine clearance below 10 ml / min, the dose is reduced by 15-50%; with anuria, the maximum dose is 2 g / day.

Symptoms: nausea, vomiting, diarrhea, impaired water-electrolyte balance (as a result of vomiting and diarrhea).
Treatment: gastric lavage, activated charcoal, saline laxatives, drugs to maintain water-electrolyte balance; hemodialysis.

With a course of treatment, it is necessary to monitor the state of the function of the blood, liver and kidneys. It is possible to develop superinfection due to the growth of microflora insensitive to it, which requires a corresponding change in antibiotic therapy.

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

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

When treating mild diarrhea with a course of treatment, antidiarrheal drugs that reduce intestinal motility should be avoided; kaolin or attapulgite-containing antidiarrheal agents may be used. For severe diarrhea, consult a doctor.

Treatment necessarily continues for another 48-72 hours after the disappearance of the clinical signs of the disease.

With the simultaneous use of estrogen-containing oral contraceptives and amoxicillin, other or additional methods of contraception should be used if possible.

Coated tablets