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Pharmacological properties

mechanism of action. the bactericidal effect of ciprofloxacin as a fluoroquinolone antibacterial is due to the ability to suppress type II topoisomerase (dna gyrase and iv topoisomerase), which are necessary in many dna life cycle processes, such as replication, transcription, repair, and recombination.

Pharmacokinetic / pharmacodynamic relationships. Efficiency mainly depends on the relationship between Cmax in blood plasma and MIC of ciprofloxacin for a bacterial pathogen and on the values ​​of AUC and MIC.

Resistance mechanism. In vitro ciprofloxacin resistance is usually associated with mutations in the target site, which typically occur in topoisomerase IV and DNA gyrase through multistage mutations. Single mutations, as a rule, do not lead to clinical resistance, however, multiple mutations usually cause clinical resistance to several or all representatives of the fluoroquinolone class.

Such resistance mechanisms as impermeability and / or the efflux pump can have a different effect on the sensitivity to fluoroquinolones, which depends on the physicochemical properties of various representatives of this class and the affinity of the transport systems for each active substance. All in vitro resistance mechanisms are generally observed in clinical isolates. Resistance mechanisms that inactivate other antibacterial agents, such as the permeability barrier (characteristic of Pseudomonas aeruginosa) and efflux mechanisms, can affect ciprofloxacin sensitivity.

The development of plasmid-mediated resistance encoded by the QNR gene has been reported.

The spectrum of antibacterial activity. Control points separate sensitive strains from strains with medium sensitivity, and the latter from resistant strains.

EUCAST Recommendations

Microorganisms Sensitive mg / ml Resistant, mg / ml
Enterobacteria ≤0,5 1
Pseudomonas spp. ≤0,5 1
Acinetobacter spp. ≤1 1
Staphylococcus spp.1 ≤1 1
Haemophilus influenzae and Moraxella catarrhalis ≤0,5 0,5
Neisseria gonorrhoeae ≤0,3 0,06
Neisseria meningitidis ≤0,3 0,06
Non-viewpoint milestones* ≤0,5 1

1Staphylococcus spp. - milestones for ciprofloxacin are related to high dose therapy.

*Non-species-specific control points were determined mainly on the basis of data on the ratio of pharmacokinetic and pharmacodynamic parameters and are independent of the MIC for individual species. They are used only for species that do not have their own points, and not for those in which a sensitivity test is not recommended.

The prevalence of acquired resistance of selected species may vary depending on the area and time, therefore, local information on resistance is important, especially in the treatment of severe infections. If necessary, consult a specialist if the local prevalence of resistance has become so high that the benefits of using the drug, at least for certain types of infections, are doubtful.

The genera and types of bacteria are generally sensitive to ciprofloxacin:

Sensitive (usually) species of microorganisms
Gram positive

aerobic microorganisms:

Bacillus anthracis1

Gram-negative aerobic microorganisms:

Aeromonas spp.

Brucella spp.

Citrobacter koseri

Francisella tularensis

Haemophilus ducreyi

Haemophilus influenzae*

Legionella spp.

Moraxella catarrhalis*

Neisseria meningitidis

Pasteurella spp.

Salmonella spp.*

Shigella spp.*

Vibrio spp.

Yersinia pestis

Anaerobic microorganisms:

Mobiluncus

Other microorganisms:

Chlamydia trachomatis$

Chlamydia pneumoniae$

Mycoplasma hominis$

Mycoplasma pneumoniae$

Species for which the development of acquired resistance is possible
Aerobic gram-positive microorganisms:

Enterococcus faecalis$

Staphylococcus spp.*,2

Aerobic gram-negative microorganisms:

Acinetobacter baumannii+

Burkholderia cepacia*,+

Campylobacter spp.*,+

Citrobacter freundii*

Enterobacter aerogenes

Enterobacter cloacae*

Escherichia coli*

Klebsiella oxytoca

Klebsiella pneumoniae*

Morganella morganii*

Neisseria gonorrhoeae*

Proteus mirabilis*

Proteus vulgaris*

Providencia spp.

Pseudomonas aeruginosa*

Pseudomonas fluorescens

Serratia marcescens*

Anaerobic microorganisms:

Peptostreptococcus spp.

Propionibacterium acnes

 
Microorganisms initially resistant to ciprofloxacin
Aerobic gram-positive microorganisms:

Actinomyces

Enteroccus faecium

Listeria monocytogenes

Aerobic gram-negative microorganisms:

Stenotrophomonas maltophilia

Anaerobic microorganisms.

Except as noted above

Other microorganisms:

Mycoplasma genitalium

Ureaplasma urealitycum

1Clinical efficacy has been demonstrated for sensitive isolates in accordance with approved clinical indications.

+Resistance Index ≥50% in one or more pages

Tags: Ciprofloxacin