Pharmacokinetics of Quinolones in Domestic Animals Quiz
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Questions and Answers

Which generation of quinolones does ciprofloxacin belong to?

  • Fourth generation
  • Second generation (correct)
  • Third generation
  • First generation
  • What common feature do quinolone carboxylic acids derived drugs share?

  • Sulfur group
  • Chlorine group
  • Fluorine group (correct)
  • Hydrogen group
  • Which quinolone carboxylic acid derivative is considered a first-generation drug?

  • Pradofloxacin
  • Nalidixic acid (correct)
  • Oxolinic acid
  • Flumequine
  • In which species is pradofloxacin approved for use in the US?

    <p>Cats</p> Signup and view all the answers

    What is the oral bioavailability of ciprofloxacin in cats and horses?

    <p>0%–20%</p> Signup and view all the answers

    Which organ typically has particularly high concentrations of quinolones?

    <p>Kidneys</p> Signup and view all the answers

    What is the major route of elimination for most quinolones?

    <p>Renal excretion</p> Signup and view all the answers

    Which form of administration significantly impacts the bioavailability of fluoroquinolones?

    <p>Oral</p> Signup and view all the answers

    What is the impact of antacids containing divalent cations on fluoroquinolone bioavailability?

    <p>Decreases bioavailability</p> Signup and view all the answers

    Which quinolone is metabolized to form ciprofloxacin?

    <p>Enrofloxacin</p> Signup and view all the answers

    What is the apparent volume of distribution of most quinolones?

    <p>Large</p> Signup and view all the answers

    Which animal species exhibits exceedingly poor oral bioavailability of ciprofloxacin?

    <p>Ruminating cattle</p> Signup and view all the answers

    What is the plasma-protein binding of nalidixic acid in horses?

    <p>~30%</p> Signup and view all the answers

    Which animal exhibits better bioavailability of enrofloxacin that is not affected by feeding?

    <p>Horses</p> Signup and view all the answers

    What happens when fluoroquinolones accumulate in phagocytic WBCs?

    <p>WBCs become more active</p> Signup and view all the answers

    What happens to urine concentrations after fluoroquinolone administration?

    <p>They often are high for 24 hours</p> Signup and view all the answers

    What does the optimal AUC:MIC ratio need to be for efficacy?

    <p>Greater than 125</p> Signup and view all the answers

    For which organisms is the MIC for E coli very high?

    <p>Pseudomonas</p> Signup and view all the answers

    What is more commonly targeted by resistance mechanisms in gram-negative bacteria?

    <p>DNA gyrase</p> Signup and view all the answers

    Which fluoroquinolone has the greatest activity against Pseudomonas spp?

    <p>Ciprofloxacin</p> Signup and view all the answers

    What is one of the mechanisms of resistance to fluoroquinolones?

    <p>Decreased porins</p> Signup and view all the answers

    What tends to be resistant to most quinolones?

    <p>Obligate anaerobes</p> Signup and view all the answers

    Which organisms are the fluoroquinolones active against?

    <p>Klebsiella, P aeruginosa, and Enterococcus faecalis</p> Signup and view all the answers

    What is the mechanism for cartilage damage caused by high prolonged dosages of quinolones?

    <p>Chelation of magnesium in cartilage</p> Signup and view all the answers

    What adverse effect of pradofloxacin led to it not being approved for dogs in the US?

    <p>Bone marrow suppression</p> Signup and view all the answers

    Which toxicity associated with fluoroquinolones may lead to adverse events ranging from neurologic to musculoskeletal to cardiovascular?

    <p>Mitotoxicity</p> Signup and view all the answers

    What type of drug interaction occurs when antacids or other drugs containing multivalent cations and sucralfate are used concurrently with quinolones?

    <p>Gastrointestinal interference</p> Signup and view all the answers

    Which drug impairs the efficacy of quinolones if used concurrently for urinary tract infections?

    <p>Nitrofurantoin</p> Signup and view all the answers

    Which substance's biotransformation do quinolones inhibit, leading to increased serum concentrations that can result in CNS and cardiac toxicity?

    <p>Methylxanthines</p> Signup and view all the answers

    What may be increased via concurrent administration of cyclosporine with fluoroquinolones, potentially leading to prolonged and toxic plasma concentrations?

    <p>Cyclosporine levels</p> Signup and view all the answers

    Which laboratory test results may be altered due to quinolone use?

    <p>Urine glucose test results</p> Signup and view all the answers

    Why are withdrawal times not available for most quinolones in food-producing animals?

    <p>Because they are not approved for use in food-producing animals in most countries.</p> Signup and view all the answers

    What is prohibited for extralabel drug use in food-producing animal species in the US?

    <p>Deviations from the approved dose, treatment duration, frequency, indication, or administration route on the product label.</p> Signup and view all the answers

    What do morphological and ultrastructural changes in bacterial cells indicate as per Cushnie et al. (2016)?

    <p>Antibacterial mechanism of action</p> Signup and view all the answers

    Which agency added a black-box warning for seven fluoroquinolones due to an increased risk of tendinitis and tendon rupture?

    <p>US Food and Drug Administration (FDA)</p> Signup and view all the answers

    How do modifications to the side chain attached to the nitrogen at position 1 affect potency?

    <p>They enhance gram-negative and gram-positive spectra.</p> Signup and view all the answers

    What effect does the addition of a fluorine atom at position 6 have?

    <p>It enhances the gram-positive spectrum.</p> Signup and view all the answers

    How do substitutions on the piperazyl ring at position 7 affect bacterial penetration and potency?

    <p>They enhance bacterial penetration and potency.</p> Signup and view all the answers

    What is the impact of quinolones in acidic urine pH?

    <p>They are much less effective.</p> Signup and view all the answers

    What role do topoisomerase II and topoisomerase IV play in bacterial DNA replication?

    <p>Both support DNA supercoiling and uncoiling.</p> Signup and view all the answers

    How do fluoroquinolones affect cell lysis in the absence of RNA and protein synthesis?

    <p>They induce cell lysis less than non-fluoroquinolones.</p> Signup and view all the answers

    What are bacterial ghosts?

    <p>Bacteria recognizable only as empty cell envelopes.</p> Signup and view all the answers

    Which bacteria are primarily associated with a postantimicrobial effect from quinolones?

    <p>Gram-negative bacteria</p> Signup and view all the answers

    "The drugs are concentration dependent" implies that:

    <p>&quot;The drugs' effectiveness depends on their concentration.&quot;</p> Signup and view all the answers

    How do lower concentrations of fluoroquinolones affect DNA-DNA gyrase complex binding sites?

    <p>They occupy single binding sites resulting in single-strand nicking of DNA.</p> Signup and view all the answers

    What role do mammalian topoisomerase enzymes play in relation to quinolone inhibition?

    <p>Mammalian topoisomerase enzymes are fundamentally different from bacterial gyrase and are not susceptible to quinolone inhibition.</p> Signup and view all the answers

    What is the postantimicrobial effect associated with quinolones?

    <p>A prolonged antimicrobial effect after administration of quinolones.</p> Signup and view all the answers

    What is the recommended plasma drug concentration in relation to the minimum inhibitory concentration (MIC) of the infecting microbe for quinolones?

    <p>10 times the MIC</p> Signup and view all the answers

    Why should quinolones be considered for use in infections located in tough-to-penetrate tissues?

    <p>Because of their lipid solubility and ability to accumulate in phagocytic WBCs</p> Signup and view all the answers

    Why are fluoroquinolones prohibited for extralabel use in food-producing animals in the US?

    <p>Because they have a high risk of causing retinal degeneration in food-producing animals</p> Signup and view all the answers

    What is the risk associated with enrofloxacin at doses of 5 mg/kg or higher in cats?

    <p>Greater chance of developing retinal degeneration</p> Signup and view all the answers

    What is the consequence of changes in the ABCG2 transporter due to exposure to photoreactive fluoroquinolones?

    <p>Generation of reactive oxygen species</p> Signup and view all the answers

    What is the likely consequence of rapid IV administration of high doses of enrofloxacin in horses?

    <p>Transient neurologic clinical signs including excitability and seizure-like activity</p> Signup and view all the answers

    Why should the dose rate and frequency of quinolones be adjusted for the individual animal and the MIC of the infecting organisms?

    <p>To achieve targeted Cmax:MIC ratios for susceptible organisms</p> Signup and view all the answers

    What is the primary cause of retinal damage and degeneration in cats exposed to fluoroquinolones?

    <p>Accumulation of photoreactive fluoroquinolones due to changes in ABCG2 transporter</p> Signup and view all the answers

    What is the effect of pharmacological inhibition of ABCG2 in other species when fluoroquinolones are concurrently administered?

    <p>Resulting retinal degeneration when fluoroquinolones are concurrently administered</p> Signup and view all the answers

    What is the main reason why extralabel use of fluoroquinolones is prohibited in food-producing animals in the US?

    <p>Due to concerns about retinal damage and degeneration in food-producing animals</p> Signup and view all the answers

    What is a notable adverse effect associated with both ciprofloxacin and moxifloxacin?

    <p>Antimicrobial-induced colitis</p> Signup and view all the answers

    What is a common outcome observed with enrofloxacin doses >5 mg/kg/day in cats?

    <p>Retinal degeneration</p> Signup and view all the answers

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