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FLUOROQUINOLONES

FLUOROQUINOLONES. Ciprofloxacin (most common) Norfloxacin Ofloxacin Pefloxacin All these dugs are given oral except ciprofloxacin is given oral & injection CIPROFLOXACIN Mechanism of action Inhibit DNA synthesis by inhibiting DNA gyrase ( topoisomerase II).

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FLUOROQUINOLONES

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  1. FLUOROQUINOLONES Ciprofloxacin(mostcommon)Norfloxacin OfloxacinPefloxacin All these dugs are given oral except ciprofloxacin is given oral & injection CIPROFLOXACIN Mechanism of action Inhibit DNA synthesis by inhibiting DNA gyrase(topoisomerase II). It’s the only injected quinolone

  2. CIPROFLOXACIN ( CONT. ) Antibacterial spectrum Mainly effective against G – bacteria : Enterobacteriacae H. influenzae M. catarrhalis Campylobacter Pseudomonas N. gonorrheae Intracellular pathogens M. Tuberculosis Mycoplasma Chlamydia LegionellaBrucella It doesn’t work against anerobes

  3. Ciprofloxacin ( Cont. ) • Pharmacokinetics • Well absorbed orally ( availablei.v. ) • Di & tri- valentcations interfere with its absorption (milk, Mg, Al, Ca, antacid) • Concentrates in many tissues, esp. kidney, prostate, lung & bones/ joints • Do not cross BBB • Excreted mainly through the kidney (tubular & glomerular) (probencid interferes with tubular secretion) • Accumulate in renal insufficiency • Up to 20% metabolized by liver • t1/2= 3.3 hrs

  4. CIPROFLOXACIN ( CONT. ) Clinical uses 1. Urinary tract infections (P.aeruginosae,E.coli,Klebsiella) 2. Osteomyelitis due to P. aeruginosa 3. Gonorrhea 4. Travellers’ diarrhea- ciprofloxacin commonly used (if there’s a bloody diarrhea) 5. Prostatitis 6. Legionnaires’ disease 7. Brucellosis 8. Diabetic foot infections 9. Anthrax 10. Eradication of menengiococci from carriers For P.aeruginosa infection outside urinary tract or the bones use AGS, penicillin

  5. CIPROFLOXACIN ( CONT. ) Side effects • Nausea , vomiting & diarrhea • CNS effects : confusion, insomnia, headache, dizziness & anxiety.(indirectly by modifying GAPA transmitter in the CNS) • May damage growing cartilage • Tendinitis ( rare but more serious ) (irreversible) (may lead to tendon rupture) • Phototoxicity avoid excessive sunlight Contraindications Children / adolescents (under 18), pregnancy and lactation (secreted in milk) It’s not contraindicated in adolescents it’s not preferred so u have to measure benfits vs. risks Drug interaction Iron or antacids containing Mg, Ca, or Al  reduce oral absorption Elevates serum levels of theophylline, warfarin & glibenclamide

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