Fluoroquinolones/UTI drugs Flashcards

1
Q

Fluoroquinolone drugs

A
Ciprofloxacin
Ofloxacin
Levofloxacin
Moxifloxacin
Gatifloxacin
Gemifloxacin
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2
Q

MOA of fluoroquinolones

A

inhibit DNA gyrase, which prevents relaxation of positively supercoiled DNA that is required for normal transcription and replication (Topo IV); bactericidal

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3
Q

Fluroquinolone spectrum

A

aerobic G- rods, good G+ (Exception: moxi and gemi effective against anaerobes)

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4
Q

Cirpofloxacin use

A

UTI, anthrax prophylaxis, P. aeruginosa

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5
Q

Ofloxacin

A

PROSTATITIS, TB

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6
Q

Levofloxacin

A

CAP

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7
Q

Moxifloxacin

A

anaerobes; active against PCN resistant S. pneumoniae

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8
Q

Gatifloxacin

A

ocular application only

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9
Q

Gemifloxacin

A

active against penicillin resistant S. pneumoniae, anaerobes, CAP

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10
Q

Fluroquinolone kinetics

A

oral
wide distribution, excellent tissue penetration (prostatitis- oflox)
poor CNS
excreted by kidney (probenecid delays elimination)

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11
Q

Decrease absorption of fluoroquinolones

A

Mg, Al, Ca

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12
Q

Fluoroquinolones adverse effects

A
increase QT interval
cartilage erosion (don't use in children)
tendon rupture
photosensitivity
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13
Q

Photosensitivity

A

fluoroquinolones, tetracyclines

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14
Q

Fluoroquinolones contraindicated in

A

pregnant
nursing
children (cartilage damage) <18 YO

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15
Q

Don’t use <18 YO

A

Fluorquinolones

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16
Q

Resistance to fluoroquinolones

A
  1. targe-site gene mutations
  2. Reduced membrane permeability
  3. plasmid-mediated resistance
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17
Q

Metronidazole MOA

A

prodrug: non-enzymatically reduced by reacting with ferrodoxin (only found in anaerobes); metabolites are taken up into bacterial DNA and form unstable molecules (bacteriocidal)

18
Q

Reacts with ferrodoxin

A

Metronidazole

19
Q

Metronidazole spectrum

A

anaerobes (G-/+)

20
Q

Use of metronidazole

A

BV, RTI, pseudomembranous colitis (alternative to vanco), endocarditis, H.pylori

21
Q

Metronidazole kinetics

A

oral, IV, topical
liver metabolism
eliminated in urine

22
Q

Adverse effects of metronidazole

A

Dilsulfiram-like reaction
Disgeusia (metal taste)
CNS and PNS toxicity (convulsive seizures, neuropathy), GI disturbance

23
Q

Disulfiram-like reaction

A

cephalosporins and metronidazole

24
Q

Exclusive UTI drugs

A

Nitrofurantoin

Methenamine

25
Q

UTI pathogens

A

E.coli (80%), Staph saprophyticus (G+), Catheter associated UTI’s (proteus, klebsiella, seratia, pseudomonas)

26
Q

Exclusive UTI drug properties

A

renal excretion
achieve high urinary concentration (do no achieve therapeutic concentrations anywhere else in body)
Bactericidal activity in the urine

27
Q

Nitrofurantoin

A

damages bacterial DNA; prodrug: reduced in bacterial cells to intermediate that can attack ribosomal proteins, DNA, metabolism, macromolecules

28
Q

Nitrofurantoin spectrum

A

wide spectrum; static and cidal (e. coli, S. pyogenes, Citrobacter, Klebsiella, enterobacter, shigella, serratia, and indole positive proteus)

29
Q

Resistant organisms to nitrofurantoin

A

Proteus and pseudomonas

30
Q

Use of nitrofurantoin

A

tx of uncomplicated UTI (alternative for tx of E. coli resistant to TMZ-SMX and fluroquinolones)

31
Q

Nitrofurantoin kinetics

A

rapid and complete absorption after oral use
acidic urine increases therapeutic action
drug activity is decreased when glomerular filtration is impaired
should not be used if creatinine clearance is less than 50 mL/min (renal failure)
colors urine brown

32
Q

Nitrofurantoin toxicity

A

GI upset
Allergic rxn: Hemolytic anemia (G6PD deficiency)
Pulmonary fibrosis (chronic use and elderly)
neuro disorders

33
Q

Contraindications of nitrofurantoin

A

pregnancy (38-42 weeks gestation), less than 1 month old, impaired renal function, allergy

34
Q

Methenamine

A

oral; prodrug: decomposes to formaldehyde and ammonia in acid medium of urinary tract

35
Q

Prodrugs

A

metronidazole (ferrodoxin), nitrofurantoin (damage bacterial DNA), Methenamine (formaldehyde and ammonia)

36
Q

No bacterial resistance

A

Formaldehyde (methenamine)

37
Q

Spectrum of methenamine

A

nearly all bacteria; proteus inhibit release of formaldehyde (combine with weak organic acid: hippuric acid)

38
Q

Increases pH of urine

A

Proteus

39
Q

Toxicity of methenamine

A

non-toxic: doesn’t decompose until acidic urine

some GI distress

40
Q

Contraindications of methenamine

A
hepatic insufficiency (conversion to formaldehyde releases ammonia, thus contraindicated in hepatic deficiency)
renal insufficiency (crystalluria)