FLUOROQUINOLONES Ciprofloxacin Norfloxacin Ofloxacin Pefloxacin CIPROFLOXACIN Mechanism of action Inhibit DNA synthesis by inhibiting DNA gyrase.
CIPROFLOXACIN ( CONT. ) Antibacterial spectrum Mainly effective against G – bacteria : Enterobacteriacae H. influenzae M. catarrhalis Campylobacter Pseudomonas N. gonorrheae Intracellular pathogens M. Tuberculosis Mycoplasma Chlamydia Legionella Brucella ** Not effective against G+ and anaerobes
Ciprofloxacin ( Cont. ) Pharmacokinetics Well absorbed orally ( available i.v ) Di & tri- valent cations interfere with its absorption Concentrates in many tissues, esp. kidney, prostate, lung & bones/ joints Do not cross BBB Excreted mainly through the kidney (tubular- blocked by probenecid- and glomerular ) Accumulate in renal insufficiency Upto 20% metabolized by liver T ½ = 3.3 hrs
CIPROFLOXACIN ( CONT. ) Clinical uses 1. Urinary tract infections (G- bacteria) 2. Osteomyelitis due to P. aeruginosa 3. Gonorrhea 4. Travellers’ diarrhea- ciprofloxacin commonly used 5. Tuberculosis 6. Prostatitis 7. Community- acquired pneumoniae 8. Diabetic foot infections ( P. aeruginosa ) 9. Anthrax
CIPROFLOXACIN ( CONT. ) Side effects Nausea, vomiting & diarrhoea CNS effects – confusion, insomnia, headache, dizziness & anxiety. May damage growing cartilage Tendenitis ( rare but more serious ) Hepatotoxicity – rare Phototoxicity – avoid excessive sunlight Contraindications Children / adolescents, pregnancy and lactation Drug interaction Iron or antacids containing Mg, Ca,or AL reduce oral absorption Elevates serum levels of theophylline, warfarin & glibenclamide