Dna Gyrase Inhibitor

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DNA GYRASE FLOUROQUINOLONES NALIDIXIC ACID CINOXACIN

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

CLINICAL USES  UTI


 Bacterial dirrhea
 Soft tissue infctn
 Bones n joint infctn
 Intraabdominal infctn
 Respiratory tract infctn
 Ciprofloxacin- gonococcal,
chlamydial urethritis,
legionellosis (2nd line),
TB, atypical mycobacteria
ADVERSE EFFECTS  Extremely well tollerated
 Nausea, vomiting, dirrhea
 Headache, dizziness,
insomnia, skin rash
 Contraindicated in
pregnant mother

Others:
 Arthropathy
 Tendiritis
 Hepatitis
 Hepatic failure
 Photosensitivity
 Cardiac arrythmia

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