DNA/RNA Disruptors

Quinolone: Nalidixic acid
  • Most common uses
– Gram-negative bacteria Was particularly useful against urinary tract infections prior to widespread resistance.
  • Mechanism of Action
– Inhibits DNA replication via inhibition of topoisomerase type II (aka, gyrase) in Gram-negative bacteria
  • Adverse effects
– Nausea and vomiting – Visual changes – Headache – Rash
Fluoroquinolones: Ciprofloxacin, Levofloxacin, and Moxifloxacin
  • Most common uses
– Gram-negative infections of the urinary and gastrointestinal tracts. – Moxifloxacin has activity against some Gram-positive bacteria and anaerobes, and is used to treat respiratory infections caused by Haemophilus influenzae and Streptococcus pneumoniae.
  • Mechanism of Action
– Halt DNA replication by inhibiting topoisomerase type II (in Gram-negative bacteria) or topoisomerase type IV (in Gram-positive bacteria)
  • Mechanism of Resistance
– Modification of these enzymes – Increases in efflux pumps
  • Adverse effects
– Gastrointestinal upset – Rash – Headache – QT prolongation – Tendinopathy or rupture can occur – Colitis – They should not be taken with antacids, or during pregnancy. – They should not be administered to children, due to the possibility of cartilage or bone tissue erosion.
Metronidazole
  • Most common uses
– Anaerobes Helicobacter pylori Gardnerella vaginalis Clostridium difficile – Also used to treat some parasitic infections
  • Mechanism of Action
– Produces free radical metabolites that damage bacterial DNA
  • Adverse effects
– Gastrointestinal upset – Metallic taste – Disulfiram-like reaction when combined with alcohol
Rifamycins: Rifampin and Rifabutin
  • Most common uses
– Mycobacteria – Rfabutin is particularly active against [Myocbacterium avium
  • Mechanism of Action
– Inhibit bacterial RNA synthesis
  • Mechanism of Action
– Resistance appears more likely to develop with monotherapy
  • Adverse effects
– Reddish-brown hue to the urine, saliva, tears, and other bodily fluids. – Gastrointestinal upset – Rash – Headache