2010/12/12

Augmentin

Release form, composition and packing

Film-coated tablets from white to almost white, oval, with a sunken inscription "AUGMENTIN" on one side, on a break - from almost white to yellowish-white color.

1 tab. amoxicillin (in the form of trihydrate) 250 mg clavulanic acid (in the form of potassium salt) 125 mg. Excipients: magnesium stearate, sodium starch glycolate (type A), silica colloidal anhydrous, microcrystalline cellulose. The composition of the shell: titanium dioxide, hydroxypropyl methylcellulose (5 cps), hydroxypropyl methylcellulose (15 cps), polyethylene glycol 4000, polyethylene glycol 6000, dimethicone (silicone oil).

Tablets, film-coated white to almost white, oval, with sunken inscription "AUGMENTIN" on one side.

1 tab. amoxicillin (in the form of trihydrate) 500 mg clavulanic acid (in the form of potassium salt) 125 mg. Excipients: magnesium stearate, sodium carboxymethyl starch, silica colloidal anhydrous, microcrystalline cellulose. The composition of the shell: titanium dioxide, hypromellose (5 cps), hypromellose (15 cps), macrogol 4000, macrogol 6000, dimethicone 500 (silicone oil).

Film-coated tablets from white to almost white, oval, with the letters "A" and "C" on both sides of pills and a line fault on one side, on a break - from almost white to yellowish-white color.

1 tab. amoxicillin (in the form of trihydrate) 875 mg clavulanic acid (in the form of potassium salt) 125 mg. Excipients: magnesium stearate, sodium starch glycolate (type A), silica colloidal anhydrous, microcrystalline cellulose. The composition of the shell: titanium dioxide, hydroxypropyl methylcellulose (5 cps), hydroxypropyl methylcellulose (15 cps), polyethylene glycol 4000, polyethylene glycol 6000, dimethicone (silicone oil).

Powder for oral suspension for white or nearly white, with a characteristic odor; suspension of white or nearly white. 5 ml of finished Valium. amoxicillin (in the form of trihydrate) 125 mg clavulanic acid (in the form of potassium salt) 31.25 mg.

Other ingredients: xanthan gum, aspartame, succinic acid, colloidal silica, hydroxypropyl methylcellulose, silicon dioxide, dry orange flavor 610271E (Tastemaker) and 9 / 027108 (Dragoco), dry raspberry flavor NN07943 (Quest), a dry flavor "golden syrup" 52927 / AP (Firmenich).

Powder for oral suspension for white or nearly white, with a characteristic odor when diluted suspension formed a white or nearly white, while standing a precipitate formed slowly in white or nearly white. 5 ml of finished Valium. amoxicillin (in the form of trihydrate) 200 mg clavulanic acid (in the form of potassium salt) 28.5 mg.

Other ingredients: xanthan gum, aspartame, succinic acid, colloidal silica, hydroxypropyl methylcellulose, silicon dioxide, dry orange flavor 610271E (Tastemaker) and 9 / 027108 (Dragoco), dry raspberry flavor NN07943 (Quest), a dry flavor "golden syrup" 52927 / AP (Firmenich). 7.7 g of powder - glass bottles volume of 70 ml (1) complete with measuring cap - packs cardboard.

Powder for oral suspension for white or nearly white, with a characteristic odor when diluted suspension formed a white or nearly white, while standing a precipitate formed slowly in white or nearly white. 5 ml of finished Valium. amoxicillin (in the form of trihydrate) 400 mg clavulanic acid (in the form of potassium salt) 57 mg.

Other ingredients: xanthan gum, aspartame, succinic acid, colloidal silica, hydroxypropyl methylcellulose, silicon dioxide, dry orange flavor 610271E (Tastemaker) and 9 / 027108 (Dragoco), dry raspberry flavor NN07943 (Quest), a dry flavor "golden syrup" 52927 / AP (Firmenich).

Clinico-pharmacological group: Antibiotic group broad-spectrum penicillin with an inhibitor of beta-lactamases.

Pharmacological action

Combined broad-spectrum antibiotic, resistant to β-lactamase containing amoxicillin and clavulanic acid.

Amoxicillin - a semisynthetic broad-spectrum antibiotic, active against many gram-positive and Gram-negative microorganisms. Amoxicillin was destroyed β-lactamases, therefore, its spectrum of antibacterial activity does not include microorganisms producing β-lactamase. Clavulanic acid - β-lactam compound has the ability to inactivate a wide spectrum β-lactamases, enzymes that normally produce microorganisms that are resistant to penicillins and cephalosporins.

The presence of clavulanic acid in Augmentin protects amoxicillin from the destructive action of β-lactamase, and broadens its spectrum of antibacterial activity with the addition of microorganisms, usually resistant to other penicillins and cephalosporins. Augmentin active against gram-positive aerobic microorganisms: Bacillis anthracis *, Corynebacterium spp., Enterococcus faecalis *, Enterococcus faecium *, Listeria monocytogenes, Nocardia asteroides, Staphylococcus aureus *, coagulase-negative staphylococci (including Staphylococcus epidermidis), Streptococcus spp. (Including Streptococcus agalactiae, Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus viridans); against Gram-positive anaerobes: Clostridium spp., Peptococcus spp., Peptostreptococcus spp.; Against Gram-negative aerobic microorganisms: Bordetella pertussis, Brucella spp., Escherichia coli *, Gardnerella vaginalis, Haemophilus influenzae *, Helicobacter pylori, Klebsiella spp .*, Legionella spp., Moraxella catarrhalis * (Branhamella catarrhalis), Neisseria gonorrhoeae *, Neisseria meningitidis *, Pasteurella multocida, Proteus mirabilis *, Proteus vulgaris *, Salmonella spp .* , Shigella spp .*, Vibrio cholerae, Yersinia enterocolitica *; against Gram-negative anaerobes: Bacteroides spp *. (Including Bacteroides fragilis), Fusobacterium spp .*; against other microorganisms: Borrelia burgdorferi, Chlamydiae, Leptospira icterohaemorrhagiae, Treponema pallidum. *- Some strains of these species of bacteria produce β-lactamase that is resistant to amoxicillin monotherapy.

Augmentin tablets containing 500 mg of amoxicillin and 125 mg clavulanic acid, represent a dosage form with sustained release, which differs from the conventional tablets other pharmacokinetic parameters. This provides sensitivity to the preparation of the strains of Streptococcus pneumoniae, in which resistance to amoxicillin is mediated by penicillin-binding proteins (penicillin-resistant strains of Streptococcus pneumoniae).

Pharmacokinetics

Pharmacokinetic parameters of amoxicillin and clavulanic acid were obtained in separate studies in healthy volunteers after administration of fasting: 1 tablet augmentin (250 mg/125 mg) or 2 tablets of Augmentin (250 mg/125 mg) or 1 Augmentin tablets (500 mg/125 mg ) or amoxicillin (500 mg) or clavulanic acid (125 mg) separately. In applying augmentin amoxicillin concentrations in plasma similar to those with oral single dose of amoxicillin in equivalents.

Suction

Amoxicillin and clavulanic acid is readily soluble in aqueous solutions with physiological pH values and after administration of Augmentin administered quickly and completely absorbed from the gastrointestinal tract. Absorption of active ingredients augmentin optimal in the case of its acceptance at the beginning of the meal.

Distribution

Therapeutic concentrations of both active substances are defined in various organs, tissues and body fluids (including the lungs, abdominal organs, fat, bone and muscle tissue, pleural, synovial and peritoneal fluid, in skin, bile, urine, purulent discharge, sputum, in the interstitial fluid).

Plasma protein binding moderate: 25% for clavulanic acid and 18% for amoxicillin. Amoxicillin (as most penicillins) is excreted in breast milk. Breastmilk also detected trace amounts of clavulanic acid. Except for the risk of sensitization is not known any other negative effects of amoxicillin and clavulanic acid on the health of babies breastfed. In experimental animal studies demonstrated that amoxicillin and clavulanic acid crosses the placental barrier.

However revealed no impaired fertility or adverse effects on the fetus. In animal studies found no cumulation augmentin ingredients in any organ.

Metabolism and Elimination

Amoxicillin is primarily excreted by the kidneys, whereas clavulanic acid through both renal and extrarenal mechanisms. After a single oral administration of one tablet of 250 mg/125 mg or 500 mg/125 mg approximately 60-70% of amoxicillin and clavulanic acid 40-65% during the first 6 h excreted in the urine in unchanged form. Approximately 10-25% of the initial dose of amoxicillin is excreted in the urine as inactive penitsilloevoy acid. Clavulanic acid in the human body is subjected to intensive metabolism with the formation of 2,5-dihydro-4-(2-hydroxyethyl)-5-oxo-1H-pyrrol-3-carboxylic acid and 1-amino-4-hydroxy-butane-2-one and is excreted in urine and feces.

Statement

Infectious-inflammatory diseases caused by microorganisms susceptible to the drug:
infections of the upper respiratory tract and ENT organs (including recurrent tonsillitis, sinusitis, otitis media), usually caused by Streptococcus pneumoniae, Haemophilus influenzae, Moraxella catarrhalis, Streptococcus pyogenes;
infections of the lower respiratory tract: exacerbation of chronic bronchitis, lobar pneumonia and bronchopneumonia, usually caused by Streptococcus pneumoniae, Haemophilus influenzae and Moraxella catarrhalis;
urinary tract infections: cystitis, urethritis, pyelonephritis, infection of female genital organs, usually caused by species of the family Enterobacteriaceae (mostly Escherichia coli), Staphylococcus saprophyticus and species of the genus Enterococcus, as well as gonorrhea caused by Neisseria gonorrhoeae;
infections of skin and soft tissue, usually caused by Staphylococcus aureus, Streptococcus pyogenes and species of the genus Bacteroides;
Infections of bones and joints: osteomyelitis, usually caused by Staphylococcus aureus, with the need for long-term therapy;
other mixed infections, such as septic abortion, obstetric sepsis, intraabdominal infection.

Dosing regimen

The dosage regimen is determined individually depending on age, weight, renal function the patient and the severity of the infection. For optimal absorption and reduce possible side effects of digestive system Augmentin is recommended to take at the beginning of the meal. Treatment should not continue for more than 14 days without a review of clinical situations.

If necessary, may conduct sequential therapy (early in intravenous drug with subsequent transition to oral).

Adults and children over 12 years of age or weighing over 40 kg. 1 tablet (875 mg 125 mg) 2 times daily or 1 tablet (500 mg + 125 mg) 3 times a day.

Children under 12 years

Dose, depending on age and body weight indicate a mg / kg body weight per day or per ml of suspension.

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