Fluoroquinolones Antibiotics Overview

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What is the key difference between the older and newer groups of fluoroquinolones?

Different spectrum of activity

Why are trovafloxacin and gatifloxacin no longer on the market?

Due to liver toxicity and hypoglycemia/hyperglycemia, respectively

Why are the newer fluoroquinolones referred to as respiratory fluoroquinolones?

Due to their activity against S.pneumoniae

What is the primary way in which fluoroquinolones exert their bactericidal effects?

Interference with enzymes required for bacterial DNA synthesis and repair

Why is sparfloxacin no longer available in the United States?

Due to withdrawal from the market

What distinguishes fluoroquinolones from the older quinolone nalidixic acid in terms of antimicrobial efficacy?

$2$ chemical moieties added to the structure

What is responsible for the antipseudomonal activity of fluoroquinolones?

Piperazine moiety

Which enzyme do fluoroquinolones inhibit to prevent the relaxation of positively supercoiled DNA?

DNA gyrase

What is the best predictor for clinical efficacy of fluoroquinolones?

Ratio of exposure to the drug (AUC) to minimum inhibitory concentration (MIC)

Which fluoroquinolone has significant activity against anaerobic organisms?

Moxifloxacin

What has eroded the utility of fluoroquinolones according to the text?

Overuse

Which enzyme is mutated in organisms that develop resistance to fluoroquinolones?

DNA gyrase

Why does the CDC no longer recommend fluoroquinolones for gonorrhea treatment?

Resistance development

What is the main factor associated with clinical failures and resistance development in bacteria?

$AUC:MIC$ less than 125 for gram-negative bacteria and less than 30 for gram-positive bacteria

Which population group is at high risk of developing tendon rupture when taking fluoroquinolones?

Older adults

What is the primary reason why lactating women should use fluoroquinolones sparingly?

To decrease the risk of tendon rupture

Which fluoroquinolone is detected in breast milk but ingested in small doses by infants?

Ciprofloxacin

What is the recommended use of fluoroquinolones in patients younger than 18 years according to the FDA?

For complicated UTIs and pyelonephritis

Which adverse drug reaction has been reported with nearly all antibacterial agents, including fluoroquinolones?

Clostridioides difficile infection (CDI)

What common GI adverse reactions are associated with fluoroquinolones?

Abdominal pain and altered taste

What symptomatology characterizes fluoroquinolone tendinitis?

Painful and swollen tendons leading to rupture

What is the main recommendation by the AAP regarding the systemic use of fluoroquinolones in children?

Use as a last resort against MDR bacteria

What health issue has been associated with prolonged or repeated therapy of fluoroquinolones?

Bacterial or fungal overgrowth of nonsusceptible organisms

Which fluoroquinolones are known to penetrate the placenta?

Ciprofloxacin and ofloxacin

Which fluoroquinolone is known to have minimal metabolism and predominant renal excretion?

Levofloxacin

What side effect is specifically mentioned as a concern for patients with myasthenia gravis taking fluoroquinolones?

Tendon rupture

Why are dosage adjustments necessary for most fluoroquinolones in patients with CrCl of 50 mL/min or less?

Due to renal impairment

Which warning was published by the FDA regarding fluoroquinolone antibiotic use in 2018?

Aortic dissection or aneurysm occurrence

What is the predominant route of elimination for nalidixic acid and moxifloxacin?

Metabolism

What precautions should patients on fluoroquinolones take to prevent adverse reactions related to photosensitivity?

Avoid direct sunlight, sun lamps, and tanning beds during therapy and several days after completion.

What action should patients take if they experience tenderness or inflammation in any tendon while on a fluoroquinolone?

Discontinue the fluoroquinolone, notify the prescriber, rest, and refrain from exercising the affected joint.

What is the recommended daily fluid intake to prevent crystalluria while on fluoroquinolones?

$1,500$ mL per day

When should diabetic patients report any signs or symptoms of hypoglycemia while on fluoroquinolones?

Immediately

What should patients do at any sign of an allergic reaction (hives, itching, dyspnea) while on a fluoroquinolone?

Discontinue the drug immediately.

What is the recommended action for patients experiencing dizziness or lightheadedness while on fluoroquinolones?

Avoid driving and hazardous activities until the patient's reaction is known.

What is a significant implication to consider when selecting fluoroquinolones?

Cost

Which fluoroquinolone may be a cost-effective choice due to being on multiple $4 or reduced cost generic lists?

Ciprofloxacin

What is a reason to use fluoroquinolones judiciously?

To prevent resistance

Which fluoroquinolone is unique as an oral agent effective for P. aeruginosa?

Ciprofloxacin

Which fluoroquinolone achieves a much higher AUC:MIC ratio than levofloxacin and ciprofloxacin?

Gemifloxacin

What should be monitored for patients on prolonged therapy with fluoroquinolones?

Organ function, including renal, hepatic, and hematopoietic function

What effect can dehydration lead to in patients taking fluoroquinolones?

Crystalluria

Why should fluoroquinolones not be taken within 2 to 6 hours of certain drugs?

To prevent absorption issues due to chelation

Which group should avoid using fluoroquinolones unless there are compelling reasons?

Children and pregnant women

What should patients understand about taking antimicrobial drugs like fluoroquinolones?

All doses must be taken and the full course must be completed.

What is a black box warning associated with the use of fluoroquinolones?

Risk of tendonitis and tendon rupture

Which enzyme is inhibited by ciprofloxacin, leading to increased drug levels of caffeine, zolpidem, and other drugs?

CYP1A2

Why should dairy products not be consumed concurrently with ciprofloxacin?

They decrease the drug's absorption

Which fluoroquinolone is specifically mentioned as increasing cyclosporine's nephrotoxic effects?

Norfloxacin

Why are fluoroquinolones no longer recommended as first-line treatment for simple UTIs?

Due to antibiotic resistance issues

In which condition are fluoroquinolones considered first-line therapy for treatment?

Community-acquired pneumonia

What is the recommended self-treatment for traveler’s diarrhea involving fluoroquinolones?

$500 mg of oral ciprofloxacin combined with loperamide

Why does the FDA recommend against using fluoroquinolones for acute bacterial sinusitis?

Owing to a high incidence of serious adverse reactions

'Ciprofloxacin should not be used as chemoprophylaxis in pregnant women or children younger than age 18 years' - Why?

'safer options of ceftriaxone or azithromycin available'

'Ciprofloxacin may be used off-label as a single 500 mg dose as chemoprophylaxis for high-risk adult contacts' - What should be considered before using ciprofloxacin for this purpose?

'confirmed susceptibility on culture and sensitivity'

Learn about the synthetic, broad-spectrum fluoroquinolones antibiotics, their introduction in the 1980s, and their classification into older and newer groups. Understand their chemical relation to nalidixic acid and usage in treating UTIs.

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