Source: Υπουργείο Υγείας (CY) Revision Year: 2013 Publisher: Codal-Synto Ltd, 33 Theklas Lysioti Street, 3030 Limassol, Cyprus
Pharmacotherapeutic group: Combinations of penicillins, incl. beta-lactamase inhibitors;
ATC code: J01CR02
Syntoclav is a combination of amoxicillin (as amoxicillin trihydrate) and clavulanic acid (as potassium clavulanate).
Amoxicillin is a semisynthetic penicillin with a broad spectrum of bactericidal activity against many gram-positive and gram-negative microorganisms. It acts by inhibiting the biosynthesis of cell wall mucopeptide. However, Amoxicillin is susceptible to degradation from ß-lactamases, and therefore its spectrum of activity does not include ß-lactamase producing microorganisms.
Clavulanic acid is a ß-lactam antibiotic, structurally related to the penicillins, which posses the ability to inactivate a wide range of ß-lactamase enzymes, commonly found in microorganisms resistant to penicillins and cephalosporins.
The combination of amoxicillin and clavulanic acid results in the protection of amoxicillin from degradation by ß-lactamase enzymes, and effectively extends the antibiotic spectrum of amoxicillin to include many bacteria, normally resistant to amoxicillin and other ß-lactam antibiotics.
Gram positive (aerobic): Bacillus anthracis, Corynebacterium sp., Enterococcus faecalis, Enterococcus faecium, Listeria monocytogenes, Staphylococcus aureus, coagulase negative Staphylococcus sp., Staphylococcus epidermidis, Streptococcus pneumoniae, Staphylococcus saprophyticus, Streptococcus pyogenes, Streptococcus viridans.
Gram positive (anaerobic): Clostridium sp., Peptococcus sp., Peptostreptococcus sp.
Gram negative (aerobic): Bordatella pertussis, Branhamella (Moraxella) catarrhalis, Brucella sp., Enterobacter sp. (although most are resistant in vitro, clinical efficacy in urinary tract infections has been shown) Escherichia coli, Haemophilus influenzae, Klebsiella sp., Legionella sp., Neisseria gonorrhoeae, Neisseria meningitidis, Pasteurella multocida, Proteus mirabilis, Proteus vulgaris, Salmonella sp., Shigella sp.
Gram negative (anaerobic): Bacteroides sp., including Bacteroides fragilis.
For many of the species listed, some strains are beta lactamase producers, which render them insensitive to amoxicillin alone.
The combined administration of amoxicillin and clavulanic acid does not affect the pharmacokinetic properties of each one of the drugs, administered separately.
About 80% of an orally administered dose of amoxicillin trihydrate is absorbed from the gastrointestinal tract. Amoxicillin is stable in the presence of gastric acid and the presence of food in the stomach does not affect its absorption. After the administration of 250 mg of amoxicillin the peak plasma concentration is 5 µg/ml and is achieved within 2 hours. Serum levels are proportional to the dose administered. It diffuses readily into most of body tissues and fluids, with the exception of the brain and spinal fluids, unless there is inflammation of the meninges. It crosses the placenta and is excreted in human milk in small amounts.
After the administration of clavulanic acid orally the maximum concentration of the drug in plasma is reached within one hour.
Neither amoxicillin nor clavulanic acid are highly bound to plasma proteins (amoxicillin about 20%, clavulanic acid about 30%). The half-life of amoxicillin is about 1.3 hours and that of clavulanic acid is about 1 hour.
Approximately 50% to 70% of amoxicillin and 25% to 40% of clavulanic acid are excreted unchanged in urine, during the first 6 hours after administration.
Amoxicillin is partly excreted in the urine as the inactive metabolite penicilloic acid, equivalent to between 10% and 25% of the dose. Clavulanic undergoes extensive metabolism to 2, 5-dihydro-4-(2-hydroxyethyl)-5-oxo-1H-pyrrole-3-carboxylic acid and 1-amino-4-hydroxy-butan-2-one which are eliminated in urine and faeces.
No further data of clinical relevance.
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