Quinolone Antimicrobial Agents Flashcards
What do first generation quinolones have limited activity against
gram (+) bacteria
What are first generation quinolones only useful for
treatment of lower urinary tract infections
Describe the activity of second generation quinolones
broader spectrum of bactericidal activity and are more potent
Most potent fluoroquinolone
Ciprofloxacin
What do second generation quinolones have activity against
extended activity against gram (+) organisms and mycoplasma
What do 3rd and 4th generation quinolones have improved activity against
gram (+) organisms, particularly Streptococcus pneumoniae
Moxifloxacin is considered?
a drug of last resort because of its severe side effects
What do gyrases and topoisomerases do?
untangle DNA by cutting one or two strands, and then allowing strand passage through the break or allowing the DNA to twist
How do different topoisomerases cleave DNA
so that either the 3’-hydroxyl or the 5’-hydroxyl of the DNA can become enzyme-linked
The topoisomerase-catalyzed reaction is?
reversible and usually equilibrium favors the uncleaved DNA, so cleavage complexes are present in very small amounts
How do bacterial/mammalian gyrases and topoisomerases cleave DNA
cleaves both opposing strands with a four-base stagger
What step is blocked by quinolones
DNA religation
Most common use of quinolones
urinary tract infections
Which quinolones are effective for urinary tract infections
Norfloxacin, ciprofloxacin, ofloxacin, and nalidixic acid
Which quinolones are effective for prostatitis?
Norfloxacin, ciprofloxcin, and ofloxacin