FLUOROQUINOLONES Ciprofloxacin most common Ofloxacin Norfloxacin Pefloxacin All

FLUOROQUINOLONES Ciprofloxacin (most common) Ofloxacin Norfloxacin 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). • It’s the only injected quinolone

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

Ciprofloxacin ( Cont. ) Pharmacokinetics • Well absorbed orally ( available i. v. ) • Di & tri- valent cations 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 • t 1/2 = 3. 3 hrs

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

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