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

Intestinal infections, Fever, Angina, Pharyngitis, Otitis media, Respiratory tract infections, Urinary tract infections, Biliary tract infections, Skin infections, Bronchitis

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

• infectious diseases of the upper and lower respiratory tract and ENT (angina, acute otitis media, pharyngitis, bronchitis, pneumonia, lung abscess);
• Gastrointestinal infections: bacterial enteritis. It may require combined therapy in case of infections caused by anaerobic microorganisms;
• infectious and inflammatory diseases of biliary tract (cholangitis, cholecystitis);
• Skin and soft tissue infections;
• leptospirosis, listeriosis, Lyme disease (borreliosis);
• endocarditis (incl.

Active ingredient

Amoxicillin

Composition

1 tablet of 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.

How to take, the dosage

Overly, before or after meals.

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

In acute uncomplicated gonorrhea 3 g is prescribed once; when treating women the repeated use of the indicated dose is recommended.

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

In case of severe infections (meningitis, septicemia) in adults – up to 6 g a day in 3-4 doses. For children – 250-500 mg 3 times a day. Treatment duration depends on indications and clinical picture and makes usually 5-7 days. In otitis media and similar infections in children two-times use of Amoxicillin is sufficient. In cases of chronic diseases, recurrent infections, infections of severe course, adults are prescribed 750 mg – 1 g 3 times a day, children up to 60 mg/kg per day divided into 3 doses.

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

In listeriosis in adults – 0.5 g 3 times a day for 6-12 days.

In case of salmonella carriage in adults – 1.5-2 g 3 times a day for 2-4 weeks.

In prophylaxis of endocarditis during minor surgical interventions in adults – 3-4 g 1 hour before the procedure. If necessary a second dose is administered after 8-9 hours.

In children the dose is reduced by half.

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

Interaction

There may be an increase in the absorption time of digoxin during therapy with Amoxicillin Sandoz.

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

The concomitant use of amoxicillin and other bacteriostatic drugs (macrolides, tetracyclines, sulfonamides, chloramphenicols) should be avoided because of the possibility of antagonism. When concomitant use of aminoglycosides and amoxicillin a synergistic effect may develop.

The concomitant use of amoxicillin and disulfiram is not recommended.

The concomitant use of methotrexate and amoxicillin may increase the toxicity of the former, probably due to competitive inhibition of renal tubular secretion of methotrexate by amoxicillin.

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

Increases the effectiveness of indirect anticoagulants (by suppressing intestinal microflora, reduces the synthesis of vitamin K and prothrombin index); reduces the effectiveness of estrogen-containing oral contraceptives; drugs that metabolize paraaminobenzoic acid (PABA), ethinylestradiol preparations – risk of bleeding “breakthrough”.

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

Allopurinol increases the risk of developing a skin rash.

Special Instructions

In case of course treatment it is necessary to monitor the hematopoietic, hepatic and renal function. Superinfection due to growth of microflora insensitive to it is possible, which requires appropriate changes in antibiotic therapy.

When administered to patients with bacteremia a bacteriolysis reaction may develop (Jarisch-Herxheimer reaction).

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

In the treatment of mild diarrhea, anti-diarrheal drugs that reduce intestinal peristalsis should be avoided; kaolin- or attapulgit-containing anti-diarrheal agents may be used. If the diarrhea is severe, a physician should be consulted.

The treatment must be continued for an additional 48-72 hours after clinical signs of illness have disappeared.

In case of concomitant use of estrogen-containing oral contraceptives and amoxicillin, other or additional contraceptive methods should be used, if possible.

Contraindications

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

The drug should be used with caution in patients with impaired renal function; severe digestive disorders accompanied by persistent vomiting and diarrhea; allergic diathesis asthma; pollinosis; with viral infections; with acute lymphoblastic leukemia; with infectious mononucleosis (due to increased risk of erythematous skin rash); in children over 3 years old.

Side effects

The frequency of side effects is stated according to 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%.

Systemic diseases: frequent – tachycardia, phlebitis; rare – decrease of BP; very rare – prolongation of QT interval.

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

Nervous system disorders: frequent – somnolence, headache, dizziness; rare – nervousness, agitation, anxiety, ataxia, change of behavior, peripheral neuropathy, anxiety, sleep disturbance, depression, paresthesia, tremor, confusion, convulsions; very rare – hypersthesia, visual, olfactory and tactile sensitivity disorders, hallucinations.

Urogenital system disorders: rare – interstitial nephritis, increased serum creatinine concentration.

Gastrointestinal and liver disorders: dysbacteriosis, change in taste, stomatitis, glossitis; frequent – nausea, diarrhea, increased liver parameters (ALT, AST, alkaline phosphotase, γ-glutamyltransferase), increased serum bilirubin concentration; rare – vomiting, dyspepsia, pain in epigastrium, hepatitis, cholestatic jaundice; very rare – acute liver failure, diarrhea with blood admixture, pseudomembranous colitis, appearance of black coloring of tongue.

Muscular system disorders: rare – arthralgia, myalgia, tendon diseases including tendinitis; very rare – tendon rupture (possible bilateral and 48 hours after treatment start), muscle weakness, rhabdomyolysis.

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

Endocrine system disorders: rare – anorexia; very rare – hypoglycemia, especially in patients with diabetes.

Respiratory system: rare – bronchospasm, dyspnea; very rare – allergic pneumonitis.

General: rare – general weakness; very rare – increase in body temperature.

Others: difficulty breathing, vaginal candidiasis; rare – superinfection (especially in patients with chronic disease or reduced body resistance), serum-like reactions; single cases – anaphylactic shock.

Overdose

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

Treatment: gastric lavage, activated charcoal, saline laxatives, drugs to maintain water-electrolyte balance; hemodialysis.

Pregnancy use

The use of amoxicillin in pregnancy is possible when the benefit to the mother exceeds the potential risk to the fetus.

Amoxicillin is excreted with breast milk in low concentrations. If it is necessary to use the drug during lactation, discontinuation of breastfeeding should be considered.

Similarities

Amoxicillin, Amosin, Amoxicillin VET