Download - Quinolones New
Dr.U.P.RathnakarMD.DIH.PGDHM
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Chemotherapy
Quinolones & Fluoroquinolones,
July 2011
Fluoro-[quinolones]Quinolone Fluoroquinolone
FluoroquinoloneFluoroquinolone
FluoroquinoloneFluoroquinolone
QuinolonesNalidixic Acid
I generationClass I
Norfloxacin
Class II
Ofloxacin Ciprofloxacin
Table No. 1
II generation
LevofloxacinSparfloxacin
Gatifloxacin[Banned in indiaWEF 3/11]
Moxifloxacin
III generation
TrovafloxacinGemifloxacin
Quinolones & Fluoroquinolones: Classification
DNA separation +ve supercoiling
DNA gyrase[G-ve]
-ve supercoils
TopoisomeraseIV [G+ve]
Separates daughter strands
-Ve supercoiling by nicking and sealing coiled strands and facilitate copyingSeparates daughter DNA strands after replication
FQInhibit
FQ-MOA
MOAConcn. dependent
• Concentration-dependent killing-PAE
[FQ]
• Time dependent: As long as concn exceeds MIC –No PAE
[Betalactams]
Resistance
• Enzymes with less affinity• Decreased permeation of drug• Increased efflux
FQ-PK[Cipro]
• Orally absorbed• Food delays• High tissue penetrability-Cipro• Excreted in urine-high concentrations
Quinolones:Spectrum[Bactericidal]
Quinolones
[Nalidixic acid]• Narrow G-ve
coverage• Ecoli,
Shigella, Klebsiella
• GIT & UTI
• Class I[Norflox]• Narrow G-ve
coverage• Low tissue concn.• Ecoli, Shigella,
Klebsiella• Not G+ve
• GIT & UTI• Class II [Ciproflox]• Aerobic G-Ve• E.Coli, Enterobacter,
Salmonella, Shigella, Proteus, H.Influenza
• Nisseriae, Vibrio, Yersinia• H.Ducreyi• Pseudomonas, Staph, Myco• Not Strepto and pneumo
• Second+• G+ve-Strepto
and pneumococci• Atypical-
Mycoplasma, Chlamydia• Myco• Atypical Myco• Less to
pseudomonas
• Third+• Improved
G+ve• Anaerobes
IGeneration
IIGeneration
IIIGeneration
Gemiflox
ADE• GIT Discomfort• CNS toxicity- mild headache and dizziness, Rarely,
hallucinations, delirium, and seizures[NSAIDs worsen]• Phototoxicity• Tendonitis• Cartilage damage in young animals[???????]• Enzyme inhibitor [DI-Theo, Warfarin]• Chelation[Antacids, Sucralfate, Iron]• CI in pregnancy• QTc prolongation-Gatiflox
ADE
• Fluoroquinolones are associated with an increased risk of tendonitis and tendon rupture.
Over 60 years of ageTaking steroids (corticosteroids)Kidney, heart, or lung transplant recipient
'Gatifloxacin-ADEs
• 'Gatifloxacin was banned in India on the 18th of March along with Tegaserod. A statement from the health ministry said: 'The use of the following drugs is likely to involve certain risks to human beings, whereas safer alternatives to the said drugs are available.' The move comes after international studies revealed that Gatifloxacin posed 17 times higher risk of developing serious hyperglycemia (high blood sugar) than other antibiotics in elderly patients"
Table No. 1
Quinolones: Uses
Nalidixic acid•Un-complicated UTIs & GIT [G-ve]
•Not for use in systemic infections
I generation
Class I [Norflox] • Uncomplicated urinary tract infection and Inf of GIT• Not for use in systemic infection
Class II [Cipro]• UTI-Complicated & Uncomplicated• PPNG Infections• Chancroid• GE• Typhoid• Respiratory-Mycoplasma• TB• Meningitis
Fluoroquinolones-uses
II generation[Respiratory]•Same as for second generation•Community acquired pneumonia•TB, MAC
III generation• Consider for treatment of intra-abdominal infections [Anaerobic]•Severe infections
FQUses
• Enteric fever:
1. Cipro -500-750mg.oral/10days[4-8 weeks for carriers]
2. Others Ceftriaxone--DOC Chloramphenicol Co-trimoxazole Ampicillin/Amoxicillin
FQUses
• Other Infections• Myco bacteria [MDR TB]- and Atypical Myco
[M.Avium] -Moxi, Cipro, Ofloxacin• Leprosy [Ofloxacin]