QUINOLONES

· Bacteriocidal
· post antibiotic effect
CLASSIFICATION
FIRST GENERATION
· Norfloxacin
· Derived from nalidixic acid
· Effective against UTI
SECOND GENERATION
· Ciprofloxacin, ofloxacin
· gram +/_ ,gonococcus, mycobacteria, atypical
pneumonia
THIRD GENERATION
· Levofloxacin, gemifloxacin, moxifloxacin
· slightly less active than cipro & ofloxacin against
gram negative
· but more active against gram positive cocci
(MRSA)
· commonly referred to as respiratory
fluoroquinolones
MECHANISM OF ACTION
· interfere with bacterial DNA synthesis
· inhibit topoismomerase II (DNA gyrase)
· inhibit topoismerase IV in gram positive
· block relaxation of super coiled DNA that is
catalyzed by DNA gyrase
· inhibit separation of replicated chromosomal
DNA during cell division
MECHANISM OF RESISTANCE
· Decreased intracellular accumulation of drug via
production of efflux pumps or changes in porin
structure
· changes in sensitivity of the target enzymes via
 point mutations in antibiotic binding regions
CLINICAL USES
· urogenital and GIT infections caused by gram
negative.
· respiratory tract, skin, soft tissue infections
· meningococcal infection, TB, prophylactic
management of Neutropenic patients
· Ofloxacin against chlamydia trachomatis
TOXICITY
· skin rashes, headache, dizziness, abnormal LFTs,
phototoxicity, neurotoxicity, tendinitis, tendon
rupture.
· not recommended for children and pregnant pt.
bcz it may damage growing cartilage, cause
arthropathy.
· prolong QTc interval