Amoxicillin Sandoz, 1 g 12 pcs

Pharmacological action – broad spectrum antibacterial.
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 breeding stage. 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.

The others are 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 from 75 to 90%. The presence of food has no effect on absorption of the drug. As a result of oral administration of amoxicillin in a single dose of 500 mg, the drug concentration in plasma is 6-11 mg/l. After oral administration, Cmax in plasma is reached after 1-2 hours.

From 15 to 25% of amoxicillin is bound to plasma proteins. The drug rapidly 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. With inflammation of the meninges the drug concentrations in the cerebrospinal fluid may be 20% of its concentration in blood 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 6-8 hours after drug administration. A small amount of the drug is excreted with the bile. T1/2 is 1-1.5 h. In patients with terminal renal failure T1/2 varies from 5 to 20 hours. The drug is excreted with hemodialysis.

Indications

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 (sore throat, acute otitis media, pharyngitis, bronchitis, pneumonia, lung abscess);

Infectious diseases of urogenital 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 inflammatory diseases of the biliary tract (cholangitis, cholecystitis);

eradication of Helicobacter pylori (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).

Endocarditis (including prevention of endocarditis during dental procedures).

Active ingredient

Composition

How to take, the dosage

Intravenously.

The therapy of infections

As a rule, it is recommended to continue therapy for 2-3 days after the disappearance of symptoms. In the case of infections caused by ?-hemolytic streptococcus, complete eradication of the pathogen requires therapy for at least 10 days.

Parenteral therapy is indicated when oral therapy is not possible and in the treatment of severe infections.

Adult dosages (including elderly patients)

The standard dose: The usual dose ranges from 750 mg to 3 g of amoxicillin per day in several doses. In some cases it is recommended to limit the dose to 1500 mg/day in several doses.

Short course of therapy: uncomplicated urinary tract infections – two doses of the drug of 3 g with an interval between doses of 10-12 hours.

Children’s doses (up to 12 years of age)

The daily dose for children is 25-50 mg/kg/day in several doses (maximum 60 mg/kg/day), depending on the indication and the severity of the disease.

Children with body weight over 40 kg should receive an adult dose.

Dosing in renal failure

In patients with severe renal insufficiency, the dose should be reduced. If renal clearance is less than 30 ml/min, increasing the interval between doses or reducing subsequent doses is recommended. Short courses of therapy of 3 g are contraindicated in renal insufficiency.

Adults (including elderly patients):

In hemodialysis: 500 mg should be administered after the end of the procedure.

Kidney function impairment in children with a body weight less than 40 kg:

Interaction

There may be increased 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 agents (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

Before prescribing Amoxicillin Sandoz® it is necessary to make sure that the strains of microorganisms causing the infectious disease are sensitive to the drug.

In severe gastrointestinal infections accompanied by prolonged diarrhea or nausea, oral administration of Amoxicillin Sandoz® is not recommended because of possible low absorption of the drug.

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

In case of severe persistent diarrhea, the development of pseudomembranous colitis (caused by Clostridium difficile) should be excluded. In this case Amoxicillin Sandoz® should be discontinued and appropriate treatment should be prescribed. In this case the drugs which slow down gastrointestinal peristalsis are contraindicated.

In case of course treatment it is necessary to monitor the hematopoietic, hepatic and renal function.

The development of superinfection due to growth of microflora insensitive to it is possible, which requires appropriate change in antibiotic therapy.

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

The treatment must be continued for another 48-72 h after clinical signs of the disease have disappeared.

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

Amoxicillin Sandoz® is not recommended for the treatment of acute respiratory viral infections due to low efficacy.

Particular caution is recommended in patients with allergic diathesis or bronchial asthma, a history of gastrointestinal disorders (in particular, colitis caused by antibiotic treatment).

In case of prolonged use of Amoxicillin Sandoz® Nystatin, levorin or other antifungal drugs should be prescribed simultaneously.

It is not recommended to consume ethanol during treatment.

The use of Amoxicillin Sandoz® has no effect on the results of enzymatic glucosuria test, however, false positive results of urine glucose test are possible.

When taking Amoxicillin Sandoz®, it is recommended to drink plenty of fluids to prevent formation of amoxicillin crystals in the urine.

Impact on the ability to drive vehicles and perform other activities requiring concentration and rapid psychomotor reactions

Because of the possibility of side effects such as drowsiness, headache and confusion, caution should be exercised when engaged in potentially dangerous activities requiring increased concentration and rapid psychomotor reactions.

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 (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; viral infections; acute lymphoblastic leukemia; infectious mononucleosis (due to increased risk of erythematous skin rash); in children over three 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, nephrotoxicity, crystalluria, epileptic seizures.

Treatment: administration of activated charcoal, symptomatic therapy, correction of water-electrolyte balance disorders, hemodialysis may be performed.

Pregnancy use

Animal studies have shown that amoxicillin has no embryotoxic, teratogenic and mutagenic effects on the fetus. However, adequate and controlled studies on the use of amoxicillin in pregnant women have not been conducted, so the use of amoxicillin during pregnancy is possible only if the estimated benefit to the mother exceeds the potential risk to the fetus.

The drug is excreted with the breast milk, therefore during treatment with amoxicillin during lactation it is necessary to decide on the cessation of breastfeeding since diarrhea and/or fungal colonization of the mucosa and sensitization to beta-lactam antibiotics may develop in the nursing infant.

Similarities