Moxiclav Mechanism of Action

MOXICLAV is a combination of amoxicillin, broad spectrum penicillin and potassium clavulanate, a progressive and irreversible inhibitor of beta-lactamase enzymes. The presence of potassium clavulanate protects Amoxicillin from destruction and subsequent loss of bacterial activity by the beta-lactamase enzymes produced by many Gram-negative and Gram-positive bacteria.
MOXICLAV will not only eliminate primary pathogens but also will not be inactive by non pathogenic beta-lactamase producing organisms at the site of infection.
Pharmacology: Pharmacodynamics: Moxiclav is a combination of amoxicillin (as amoxicillin trihydrate) and clavulanic acid (as potassium clavulanate). Amoxicillin is 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 β-lactamases, and therefore its spectrum of activity does not include β-lactamase producing microorganisms.
Clavulanic acid is a β-lactam antibiotic, structurally related to the penicillins, which posses the ability to inactivate a wide range of β-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 β-lactamase enzymes, and effectively extends the antibiotic spectrum; of amoxicillin; to include many bacteria, normally resistant to amoxicillin and other β-lactam antibiotics.
Resistance to many antibiotics is caused by bacterial enzymes which destroy the antibiotic before it can act on the pathogen. The clavulanate in MOXICLAV anticipates this defense& mechanism by blocking the β-lactamase enzymes, thus rendering the organisms sensitive to amoxicillin's rapid bactericidal effect at concentrations readily attainable in the body.
Clavulanate by itself has little antibacterial activity; however, in association with amoxicillin as MOXICLAV, it produces an antibiotic agent of broad spectrum with wide application in hospital and general practice.
MOXICLAV is bactericidal to a wide range of organisms including: Gram-positive: Aerobes: Enterococcus faecalis*, Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus viridans, Staphylococcus aureus*, Coagulase negative staphylococci* (including Staphylococcus epidermidis*), Corynebacterium species, Bacillus anthracis*, Listeria monocytogenes.
Anaerobes: Clostridium species, Peptococcus species, Peptostreptococcus.
Gram-negative: Aerobes: Haemophilus influenzae*, Moraxella catarrhalis*, Escherichia coli*, Proteus mirabilis*, Proteus vulgaris*, Klebsiella species*, Salmonella species* Shigella species*, Bordetella pertussis, Brucella species, Neisseria gonorrhoeae*, Neisseria meningitidis*, Vibrio cholerae, Pasteurella multocida.
Anaerobes: Bacteroides species* including B. fragilis.
*including Beta-lactamase producing strains resistant to ampicillin and amoxicillin.
Pharmacokinetics: The pharmacokinetics of the two components of MOXICLAV is closely matched. Peak serum levels of both occur about one hour after oral administration. Absorption of MOXICLAV is optimized at the start of a meal. Both clavulanate and amoxicillin have low levels of serum binding; about 70% remains free in the serum.
Doubling the dosage of MOXICLAV approximately doubles the serum levels achieved.
Toxicology: Preclinical safety data: No further information of relevance.
Microbiology: Bacteriology: MOXICLAV is bactericidal to a wide range of Gram-negative and Gram-positive bacteria including many clinically important beta-lactamase producing resistant organisms including: GRAM-POSITIVE: Aerobes: Staphylococcus aureus, Streptococcus pneumoniae, Staphylococcus epidermidis, Streptococcus viridans, Streptococcus pyogenes, Streptococcus faecalis, Bacillus anthracis, Listeria monocytogenes and Corynebacterium species.
Anaerobes: Clostridium species, Peptostreptococcus species, Peptococcus species.
GRAM-NEGATIVE: Aerobes: Escherichia coli, Proteus mirabilis, Proteus vulgaris, Klebsiella species, Salmonella species, Shigella species, Bordetella pertussis, Yersinia enterocolitica, Gardnerella Vaginalis, Brucella species, Neisseria gonorrhoeae, Neisseria meningitidis, Haemophilus influenzae, Pasteurella multocida and Vibrio cholerae.
Anaerobes: Bacteroides species, including Bacteroides fragilis.
Including beta-lactamase producing strains resistant to ampicillin and amoxicillin.