Transcript 06. FLUOROQUINOLONES.pptx

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
Chlamydia
It doesn’t work against anerobes
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
• t1/2 = 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
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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