Evolution of Fluoroquinolone Antimicrobials

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Which of the following best describes the impact of the discovery of quinolone antimicrobials?

It resulted in the expansion of the spectrum of activity, improvement of pharmacokinetics, and stabilization of compounds against common resistance mechanisms. (correct)

It discouraged the use of antimicrobials in human and agricultural medicine.

It had no impact on the development of new antimicrobials.

It led to the creation of numerous compounds without clinical significance.

Which of the following factors contributed to the rapid integration of quinolone antimicrobials into human and agricultural medicine?

Their inability to overcome common mechanisms of resistance.

Their narrow activity spectrum.

Their enhanced pharmacokinetic properties, expanded activity spectrum, and stability against resistance mechanisms. (correct)

Their negative impact on human and animal health.

What key progress was made after the synthesis of nalidixic acid in the early 1960s?

Continued modification of the quinolone nucleus improved pharmacokinetics, expanded the activity spectrum, and stabilized compounds against common resistance mechanisms. (correct)

Pharmacokinetic properties were worsened.

Resistance to quinolone antimicrobials increased.

Activity spectrum of quinolone antimicrobials was narrowed.

How did the development of quinolone antimicrobials affect their resistance to common mechanisms?

It stabilized them against common mechanisms of resistance. (D) Signup and view all the answers

What significant event occurred in the early 1960s concerning quinolone antimicrobials?

The synthesis of nalidixic acid. (C) Signup and view all the answers

Which type of spectrum of activity do first-generation fluoroquinolones have?

Narrow spectrum (C) Signup and view all the answers

What is the primary mechanism of action of fluoroquinolones?

Interference with DNA ligation (C) Signup and view all the answers

What is the mechanism of action of fluoroquinolones?

Inhibition of nucleic acid synthesis (A) Signup and view all the answers

Which enzyme is the primary target of fluoroquinolones in gram-negative bacteria?

DNA gyrase (A) Signup and view all the answers

Which enzyme are fluoroquinolones known to inhibit in bacterial cells?

DNA gyrase (B) Signup and view all the answers

What property of fluoroquinolones helps them to be bactericidal rather than bacteriostatic?

They stabilize the DNA-enzyme complex (D) Signup and view all the answers

Which property of fluoroquinolones contributes to their bactericidal effect?

Interference with DNA replication and repair (B) Signup and view all the answers

Which of the following best describes the antimicrobial spectrum of fluoroquinolones?

They exhibit AUC/MIC-dependent killing (D) Signup and view all the answers

What role does topoisomerase IV play in the action of fluoroquinolones?

It is the target in gram-positive bacteria (A) Signup and view all the answers

What is a significant feature of fluoroquinolones in terms of bacterial spectrum?

They show many variations in activity based on the specific fluoroquinolone (D) Signup and view all the answers

What is one of the common therapeutic applications of fluoroquinolones?

Managing bacterial infections (B) Signup and view all the answers

What is a common mechanism of fluoroquinolone resistance seen in clinical pathogens?

Mutation of DNA gyrase (C) Signup and view all the answers

What is a key trait of fluoroquinolones in terms of their impact on bacteria?

They lead to rapid cell death (C) Signup and view all the answers

Which enzyme do fluoroquinolones primarily target in bacteria?

DNA gyrase (D) Signup and view all the answers

What is a key feature of the antimicrobial spectrum of fluoroquinolones?

Broad spectrum covering a range of bacterial species (D) Signup and view all the answers