Pharmacological properties : תכונות פרמקולוגיות

Pharmacodynamic Properties

5.1   Pharmacodynamic properties

Pharmacotherapeutic group: ANTIBACTERIALS FOR SYSTEMIC USE
ATC code: J01FA06 (J: anti-infectives)
Roxithromycin is an antibiotic of the macrolide group.
SPECTRUM OF ANTIMICROBIAL ACTIVITY

The MIC breakpoints differentiating susceptible strains from intermediate strains, and intermediate strains from resistant strains, are as follows:
S ≤1 mg/L and R > 4 mg/L.

The prevalence of acquired resistance in certain species can vary geographically and over time. It is therefore useful to have local information on resistance, especially in treating severe infections. These data are only guidelines indicating the probability of susceptibility of a bacterial strain to this antibiotic.
When the variability of the prevalence of resistance of a bacterial species is known in France, it is indicated in the table below:

Prevalence of acquired resistance in
Category
France     (> 10%) (range)
SUSCEPTIBLE SPECIES

Gram-positive aerobes
Bacillus cereus
Corynebacterium diptheriae
Enterococci                              50 - 70 %
Rhodococcus equi
Methicillin-susceptible Staphylococcus
Methicillin-resistant* Staphylococcus    70 - 80 %
Streptococcus B
Unclassified streptococcus               30 - 40 %
Streptococcus pneumoniae                 35 - 70 %
Streptococcus pyogenes                   16 - 31 %
Gram-negative aerobes
Bordetella pertussis
Branhamella catarrhalis
Campylobacter
Legionella
Moraxella

Anaerobes
Actinomyces
Bacteroides                              30 - 60 %
Eubacterium
Mobiluncus
Peptostreptococcus                       30 - 40 %
Porphyromonas
Prevotella
Propionibacterium acnes
Miscellaneous
Borrelia burgdorferi
Chlamydia
Coxiella
Leptospires
Mycoplasma pneumoniae
Treponema pallidum

MODERATELY SUSCEPTIBLE
SPECIES
(intermediate susceptibility in vitro)

Gram-negative aerobes
Haemophilus
Neisseria gonorrhoeae

Anaerobes
Clostridium perfringens
Miscellaneous
Ureaplasma urealyticum


RESISTANT SPECIES
Gram-positive aerobes
Corynebacterium jeikeium
Nocardia asteroides
Gram-negative aerobes
Acinetobacter
Enterobacteria
Pseudomonas
Anaerobes
Fusobacterium
Miscellaneous
Mycoplasma hominis



Roxithromycin has in vitro and in vivo activity on Toxoplasma gondii.
In vitro, roxithromycin shows moderate activity on Mycobacterium avium.

* The incidence of methicillin resistance is approximately 30 to 50% for all staphylococci, and is mainly found in the hospital setting.

Pharmacokinetic Properties