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Fluoroquinolones - A Review I

J E
(Compiled by T R Ramanujam)
Prof Head, Department of pharmacology

INTRODUCTION

NEWER FLUOROQUINOLONES

Pharmacological ASPECTS of NEWER QUINOLONES

MAJOR CLINICAL APPLICATIONS

MAJOR CLINICAL APPLICATIONS

Antibacterial efficacy of quinolones depends on;

1. Activity against the target enzyme DNA Gyrase

2. Uptake by the bacterial cell

Physicochemical properties like – Hydrophobicity

- Acid base properties and

- Affinity for divalent cations.

primary target is DNA Gyrase(Topoisomerase II ) in many of the gram-ve organisms whereas in the case of gram+ve organisms Topoisomerase IV appears to be the primary target as is the case of Ciprofloxacin, Norfloxacin, and Sparfloxacin.

For Sparfloxacin in the case of Strerptococci pneumoniae ,DNA gyrase appears to be the primary target.

Peculiarly in case of Sitafloxacin both DNA Gyrase -Topoisomerase II & Topoisomerase IV appears to be the targets and hence it is expected that there is little or no chance for development of resistance.

Next issue of epharma updates

Fluoroquinolones - A Review II

Adverse effects

FUTURE DEVELOPMENTS of Quinolones

Pharmacological outline of Sparfloxacin
S
Fluoroquinolones Page 3