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Dna Gyrase Inhibitor
Dna Gyrase Inhibitor
Dna Gyrase Inhibitor
INHIBITOR
OVERVIEW - synthetic florinated analogs -1st antibacterial quinolones -1st antibacterial quinolones
of nalidixic acid - not flourinated - not flourinated
- excreted too fast - excreted too fast
RESISTANCE - Enzyme mutation-
DNA gyrase,
topoisomerase IV
- Permeability change
- Cross resistance
occurs
MECH. OF ACTION -Block bacterial DNA synthesis
-It bacterial topoisomerase II
(DNA gyrase)→ prevent
relaxation of positively
supercoiled DNA
-topoisomerase IV : intefere
chromosome separation to
daughter cells
ACT ON - Gram + ve bac
- Gram –ve bac
PHARMACOKINETICS Excretion:
Renal
-ciprofloxacin
-clinafloxacin
-enoxacin
-norfloxacin
-ofloxacin
Nonrenal:
-moxifloxacin
Oral: well-absorbed
Elimination: kidney
Concentration: prostate,
kidney, neutrophils, m0
Others:
Arthropathy
Tendiritis
Hepatitis
Hepatic failure
Photosensitivity
Cardiac arrythmia