Quinolones Flashcards
MOA of Quinolones
interfere bacterial DNA synthesis by inhibiting:
topoisomerase II (DNA gyrase) - in gram (-) *prevents relaxation of supercoiled DNA
topoisomerase IV - gram (+)
*interferes w/ the separation if replicated chromosomal DNA during cell division
1st Generation Fluoroquinolones
Nalidixic acid
Cinoxacin
Rosoxacin
Oxolinic acid
2nd Generation Fluoroquinolones
Ciprofloxacin Ofloxacin Norfloxacin Lomefloxacin Enoxacin
3rd Generation Fluoroquinolones
Levofloxacin Gemifloxacin Moxifloxacin Sparfloxacin Grepafloxacin Gatifloxacin Pazufloxacin Tosufloxacin Balofloxacin
4th Generation Fluoroquinolones
Trovafloxacin
Alatrofloxacin
Prulifloxacin
Clinafloxacin
Fluoroquinolone with activity against ANAEROBES
Moxifloxacin
Fluoroquinolone with activity against Pseudomonas aeruginosa
Ciprofloxacin
Levofloxacin
Respiratory Fluoroquinolones
MO - GE - LE
Moxifloxacin
Gemifloxacin
Levofloxacin
Adverse effects of Fluoroquinolones
HYPERGLYCEMIA EXCEPT GATIFLOXACIN - hypoglycemia
ARTHROPATHY
*d.t. chelation of Mg damaging chondrocyte interaction
PROLONGED QT INTERVAL
Resistance to Fluoroquinolones
decreased intracellular accumulation of the drug via the production of efflux pumps
changes in porin structure
changes in the sensitivity of the target enzymes via point mutations in the antibiotic binding regions
Fluoroquinolone that is withdrawn d.t. SEVERE CARDIOTOXICITY
Grepafloxacin
Fluoroquinolone that is withdrawn d.t. DIABETES MELLITUS
Gatifloxacin
Used for CAP caused by Chlamydia, Mycoplasma and Legionella (ATYPICALS)
Levofloxacin
Can cause PROLONG QT
Gemifloxacin
Levofloxacin
Moxifloxacin
