Amoxiclav, pills 875mg+125mg 14pcs

Composition

Active ingredients:

amoxicillin (as a trihydrate) 875 mg;

clavulanic acid (as a potassium salt) 125 mg;

Auxiliary substances:

colloidal silicon dioxide-12 mg;

crospovidone-61 mg;

croscarmellose sodium-47 mg;

magnesium stearate-17.22 mg;

MCC up to 1435 mg

Pharmacological action

The drug Amoxiclav is a combination of amoxicillin and clavulanic acid.

Amoxicillin is a semi-synthetic penicillin (beta-lactam antibiotic) that inhibits one or more enzymes (often referred to as penicillin-binding proteins, PSBs) in the biosynthetic pathway of peptidoglycan, which is an integral structural component of the bacterial cell wall.

Inhibition of peptidoglycan synthesis leads to a loss of cell wall strength, which usually leads to lysis and death of microbial cells.

Amoxicillin is destroyed by the action of beta-lactamases produced by resistant bacteria, so the spectrum of activity of amoxicillin does not include microorganisms that produce these enzymes.

Clavulanic acid is a beta-lactam structurally related to penicillins. It inhibits some beta-lactamases, thereby preventing inactivation of amoxicillin and expanding the spectrum of its activity, including bacteria that are usually resistant to amoxicillin, as well as to other penicillins and cephalosporins. Clavulanic acid itself does not have a clinically significant antibacterial effect.

The drug Amoxiclav® it has a bactericidal effect in vivo on the following microorganisms:

– gram-positive aerobes — Staphylococcus aureus*, Streptococcus pneumoniae, Streptococcus pyogenes;

– gram-negative aerobes-Enterobacter spp. **, Escherichia coli*, Haemophilus influenzae*, species of the genusKlebsiella*, Moraxella catarrhalis* (Branhamella catarrhalis).

The drug Amoxiclav® it has a bactericidal effect in vitro on the following microorganisms (however, the clinical significance is still unknown):

– gram-positive aerobes-Bacillis anthracis*, Corynebacterium species, Enterococcus faecalis*, Enterococcus faecium*, Listeria monocytogenes, Nocardia asteroides, coagulase-negative staphylococci* (including Staphylococcus epidermidis), Streptococcus agalactiae, and other species of the genus Streptococcus, Streptococcus viridans;

– gram-positive anaerobes — species of the genus Clostridium, a species of the genus Peptococcus, species of the genus Peptostreptococcus;

– gram-negative aerobes — Bordetella pertussis, the species of the genus Brucella, Gardnerella vaginalis, Helicobacter pylori, species of the genus Legionella, Neisseria gonorrhoeae*, Neisseria meningitidis*, Pasteurella multocida, Proteus mirabilis*, Proteus vulgaris*, species of the genus Salmonella*, species of the genus Shigella*, Vibrio cholerae, Yersinia enterocolitica*;

– gram-negative anaerobes — species of the genus Bacteroides* (including Bacteroides fragilis), Fusobacterium species*;

– others-Borrelia burgdorferi, Chlamydia spp., Leptospira icterohaemorrhagiae, Treponema pallidum.

* Some strains of these bacterial species produce beta-lactamases, which contributes to their insensitivity to amoxicillin monotherapy.

* * Most strains of these bacteria are resistant to the amoxicillin/clavulanic acid combination in vitro, but the clinical efficacy of this combination has been demonstrated in the treatment of urinary tract infections caused by these strains.

Pharmacokinetics

The main pharmacokinetic parameters of amoxicillin and clavulanic acid are similar. Amoxicillin and clavulanic acid are well soluble in aqueous solutions with a physiological pH value and after taking Amoxiclav® inside, they are quickly and completely absorbed from the gastrointestinal tract. The absorption of active substances-amoxicillin and clavulanic acid-is optimal if the drug is taken at the beginning of a meal.

The bioavailability of amoxicillin and clavulanic acid after oral use is about 70%.

Peak plasma concentrations are reached approximately 1 hour after use. The CMAX values are 3-12 mcg / ml for amoxicillin (depending on the dose), and about 2 mcg/ml for clavulanic acid.

Cmax in blood plasma after a bolus injection at a dose of 1.2 g (1000+200 mg) of the drug is 105.4 mg / l for amoxicillin and 28.5 mg/l for clavulanic acid.

Plasma concentrations of amoxicillin/clavulanic acid are similar to those of the corresponding oral doses of amoxicillin or clavulanic acid separately in equivalent doses.

Both components are characterized by sufficient Vd in various organs, tissues, and body fluids (including lungs, abdominal organs, fat, bone, and muscle tissues, pleural, synovial, and peritoneal fluids, skin, bile, urine, purulent discharge, sputum, and interstitial fluid).

Binding to plasma proteins is moderate — 25% for clavulanic acid and 18% for amoxicillin.

Vd is about 0.3–0.4 l / kg for amoxicillin and about 0.2 l / kg for clavulanic acid.

Amoxicillin and clavulanic acid do not cross the blood-brain barrier in non-inflamed meninges.

Amoxicillin (like most penicillins) is excreted in breast milk. Trace amounts of clavulanic acid were also found in breast milk. Amoxicillin and clavulanic acid cross the placental barrier.

Amoxicillin is mainly excreted by the kidneys, whereas clavulanic acid is excreted by both renal and extrarenal mechanisms. After a single oral dose of one 250+125 mg or 500+125 mg tablet, approximately 60-70% of amoxicillin and 40-65% of clavulanic acid are excreted unchanged in the urine during the first 6 hours. About 10-25% of the initial dose of amoxicillin is excreted in the urine as inactive penicillic acid. Clavulanic acid in the human body undergoes intensive metabolism with the formation of 2,5-dihydro-4 – (2-hydroxyethyl) – 5-oxo-1 N-pyrrole-3-carboxylic acid and 1-amino-4-hydroxy-butane-2-one and is excreted in the urine and feces.

The average T1 / 2 of amoxicillin/clavulanic acid is approximately 1 h, and the average total clearance is approximately 25 l / h in healthy patients. In the course of various studies, it was found that the excretion of amoxicillin in the urine for 24 hours is approximately 50-85%, clavulanic acid — 27-60%. The greatest amount of clavulanic acid is excreted within the first 2 hours after ingestion.

Indications

Infections caused by sensitive strains of microorganisms:

• the upper respiratory tract and organs including acute and chronic sinusitis, acute and chronic otitis media, retropharyngeal abscess, tonsillitis, pharyngitis);
• lower respiratory tract including acute bronchitis with bacterial superinfection, chronic bronchitis, pneumonia);
• urinary tract (e. g. cystitis, urethritis, pyelonephritis);
• gynecology;
• skin and soft tissues, including the biting of humans and animals;
• the bone and connective tissue;
• biliary tract (cholecystitis, cholangitis);
• odontogenic.

Use during pregnancy and lactation

Amoxicillin and clavulanic acid pass in small amounts into breast milk. Amoxiclav can be used during pregnancy in cases where the expected benefit to the mother exceeds the potential risk to the fetus.

Contraindications

• hypersensitivity to the components of the drug;
• hypersensitivity to penicillins, cephalosporins and other beta-lactam antibiotics in the anamnesis;
• cholestatic jaundice and/or other liver disorders caused by taking amoxicillin/clavulanic acid, in the anamnesis;
• infectious mononucleosis and lymphocytic leukemia

Side effects

From the digestive system: possible loss of appetite, nausea, vomiting, diarrhea; rarely-transient increase in the activity of liver enzymes (ALT, AST), liver function disorders; in isolated cases – cholestatic jaundice, hepatitis, pseudomembranous colitis.

Allergic reactions: erythematous rash, pruritus, urticaria; rarely-erythema multiforme, angioedema, anaphylactic shock; in rare cases-exfoliative dermatitis, Stevens-Johnson syndrome.

Other services: rarely-development of superinfection, candidiasis.

Interaction

With the simultaneous use of Amoxiclav and indirect anticoagulants, an increase in prothrombin time is noted. Therefore, this combination is prescribed with caution.

Concomitant use of Amoxiclav with allopurinol increases the risk of side effects such as exanthema.

When used concomitantly, Amoxiclav increases the toxicity of methotrexate.

The combination of Amoxicillin with rifampicin is antagonistic (there is a mutual weakening of the antibacterial effect).

Amoxiclav should not be used simultaneously with bacteriostatic antibiotics (macrolides, tetracyclines), sulfonamides due to the possible decrease in the effectiveness of Amoxiclav.

When used concomitantly, Amoxiclav reduces the effectiveness of oral contraceptives.

How to take it, course of use and dosage

Adults and children over 12 years of age (or weighing more than 40 kg) in case of mild or moderate infection,1 tab. 375 mg is prescribed every 8 hours, in case of severe infection and respiratory tract infections – 1 tab. 625 mg every 8 hours or 1 tab. 1000 mg every 12 hours. The drug in the form of coated tablets is not prescribed for children under 12 years of age (with a body weight of less than 40 kg).

The maximum daily dose of clavulanic acid is 600 mg for adults and 10 mg/kg for children. The maximum daily dose of amoxicillin is 6 g for adults and 45 mg/kg for children. The course of treatment is 5-14 days. The duration of treatment is determined by the attending physician. Treatment should not be continued for more than 14 days without a second medical examination.

For odontogenic infections,1 tablet of 375 mg is prescribed every 8 hours for 5 days.

Overdose

There are no reports of fatal or life-threatening side effects due to overdose of the drug.

Symptoms: in most cases — disorders of the gastrointestinal tract (abdominal pain, diarrhea, vomiting), possibly also anxiety, insomnia, dizziness, in some cases-convulsive seizures.

Treatment: in case of overdose, the patient should be under the supervision of a doctor, treatment is symptomatic.

In the case of recent use (less than 4 hours) of the drug, gastric lavage should be performed and activated charcoal should be prescribed to reduce absorption. Amoxicillin / potassium clavulanate is removed by hemodialysis.

Special instructions

During the course of treatment, the function of hematopoiesis, liver and kidneys should be monitored.

In patients with severe renal impairment, adequate adjustment of the dosage regimen or an increase in the intervals between dosing is required.

In order to reduce the risk of adverse reactions from the gastrointestinal tract, the drug should be taken with meals.

When using Amoxiclav, a false positive reaction is possible when determining the level of glucose in the urine when using Benedict’s reagent or Felling’s solution (it is recommended to use enzymatic reactions with glucose oxidase).

Concomitant use with disulfiram should be avoided.

Form of production

Tablets

Storage conditions

In a dry place, at a temperature not exceeding 25 °C

Shelf life

2 years

Active ingredient

Amoxicillin, Clavulanic Acid

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For pregnant women as prescribed by a doctor, For adults as prescribed by a doctor, For children as prescribed by a doctor, for nursing mothers as prescribed by a doctor, For children over 12 years of age

Indications

Pneumonia, Sinusitis, Osteomyelitis, Tonsillitis, Sore Throat, Urinary Tract Infections, Bronchitis, Periodontitis, Otitis, Pharyngitis