Other Antibiotics Flashcards

1
Q

List of Quinolones

4 listed

A
  • Ciprofloxacin
  • Levofloxacin
  • Moxifloxacin
  • Norfloxacin
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2
Q

Quinolones MOA

A

Inhibit bacterial topoisomerase enzymes for bacterial DNA synthesis

  • DNA gyrase
    • induces double-stranded break
    • Repairs break
  • Topoisomerase IV
    • separated daughter chromosomes
    • “Decantenation”

Inhibition of these -> DNA damage -> Cell death

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3
Q

Quinolones AKA

A

Fluoroquinolones if they have a Fluorine attached

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4
Q

Mechanisms of resistance to Quinolones

3 listed

A
  • Alterations of DNA gyrase and/or Topoisomerase IV
  • Alterations in cell permeability
  • Efflux of drug
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5
Q

Coverage of Quinolones

A
  • Many
    • Gpos
    • Gneg
    • Atypicals
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6
Q

Clinical uses of Quinolones

A

Adults only

  • UTIs (E. coli, other enteric gram negatives)
  • Pneumonia (S. pneumo, H. flu, atypicals)
  • Abdominal infections (enteric gram negatives)
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7
Q

What is Nalidixic acid and Norfloxacin?

A
  • Not a fluoroquinolones but just a Quinolones because they didn’t have fluorine
  • Had mostly Gneg coverage and limited/no Gpos coverage
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8
Q

Ciprofloxacin coverage

A
  • some Gpos coverage
    • rarely used for Gpos (resistance)
  • very good Gneg coverage
  • Most reliable Pseudomonas coverage
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9
Q

Ciprofloxacin Clinical uses

A

Used in

  • UTIs
  • GI infections
  • Ciprofloxacin ear drops for otitis externa (swimmer’s ear caused by Pseudomonas)
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10
Q

Otitis externa

A

Swimmer’s ear caused by Pseudomonas

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11
Q

Swimmer’s ear

A

Otitis externa caused by Pseudomonas

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12
Q

Levofloxacin coverage

A

More than ciprofloxacin

  • Gpos
  • Atypicals
    • better strep penumo
    • covers most Methicillin-susceptible Staph aureus
  • Less effective against Pseudomonas than ciprofloxacin
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13
Q

Levofloxacin Clinical uses

A

Commonly used in Pneumonia (Strep, Atypicals)

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14
Q

Modern quinolones

3 listed

A
  • Gatifloxacin
  • Sparfloxacin
  • Moxifloxacin
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15
Q

Modern Quinolones coverage

A
  • Better Gpos/Atypical coverage than Levofloxacin
  • Less effective for Pseudomonas than Levofloxacin
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16
Q

Modern Quinolones clinical uses

A

Also used in Pneumonia

17
Q

Quinolones adverse effects

A
  • GI upset
    • Anorexia, NV and abdominal discomfort
    • 17% of patients
  • Neurologic side effects
    • Headache, dizziness
    • 2 to 6% of patients
  • Very rare but feared: QT prolongation of EKG
    • caused by blockade of K+ channels
    • can lead to Torsade de pointes
  • Tendon rupture/tendonitis
    • most commonly achilles
    • More common older patients (>60), people on steroids
    • Mechanism not well understood
  • Cannot use in pregnancy or children
    • toxic to developing cartilage in animal studies
18
Q

Antacids and Quinolones

A
  • Disrupt the absorption of many drugs
  • Aluminum and Magnesium hydroxide
  • Sucralfate (contains aluminum)
  • key drugs
    • Tetracycline
    • Fluoroquinolones
    • Isoniazid
    • Iron supplements
19
Q

Vancomycin MOA

A

Inhibits peptidoglycan formation (cell wall)

binds D-alanyl-D-alanine peptides and prevents cross linking causing cell wall breakdown > formation -> cell death

Basically same effect as beta-lactams but via a different mechanism

Beta-lactams inhibit transpeptidases (PBPs)

Vancomycin blocks transpeptidase binding

20
Q

Vancomycin bacterial effect

A

Bacteriocidal

21
Q

Mechanisms of resistance to Vancomycin

A
  • Terminal amino acids change
  • D-alanyl-D-alanine changed to D-alanyl-D-lactate
  • VRSA emerges
22
Q

VRSA resistance mechanism

A
  • Terminal amino acids change on peptidoglycan D-alanyl-D-alanine changed to D-alanyl-D-lactate
  • VRSA emerges
23
Q

Vancomycin coverage

A

Gpos only because it is an enormous molecule so it is too large to pass Gneg outer membranes

24
Q

Vancomycin clinical uses

A

generally 2 common uses

  • Methicillin Resistant Staph Aureus (MRSA)
  • Oral therapy for C. diff Pseudomembraneous colitis

Also, often given empirically when MRSA is a concern

  • Endocarditis
  • Severe pneumonia/sepsis
25
Q

Vancomycin adverse effects

A

Generally well tolerated but

  • nephrotoxicity
    • less common with modern preparations
    • increased risk if concomitant aminoglycoside therapy
  • Ototoxicity
    • Tinnitus
    • vertigo
    • hearing loss (rare)
  • Red man syndrome
    • flushing, erythema, itching
    • usually affects the upper body, neck, face more than the lower body
    • 10-20 minutes post-infusion
  • Direct activation of Mast cells -> histamine release (Pseudoallergic drug reaction)
    • may develop with first administration
    • often infusion related -> slow infusion = no symptoms
26
Q

Metronidazole MOA

A
  • Prodrug: must be reduced to activate it
  • reduced metronidazole results in increased drug uptake by the cells
  • the activated form (reduced) generated free radicals causing DNA damage leading to cell death
27
Q

Metronidazole coverage

A
  • Only anaerobic bacteria are capable of reducing metronidazole
  • Good coverage of anaerobes below the diaphragm
    • B. fragilis
    • C. diff
28
Q

Metronidazole clinical uses

A
  • anaerobes below the diaphragm
    • B. fragilis
    • C. difficile
  • Peritonitis
  • Abdominal abscesses
  • Diverticulitis
  • often given with quinolone for anaerobic/GI Gneg
  • Ciprofloxacin/metronidazole often used for diverticulitis as well
  • H. pylori and Gardnerella vaginalis
    • Facultative anaerobic bacteria that are susceptible to Metronidazole
    • part of the triple therapy for H. pylori
    • Treatment of bacterial vaginitis
  • Anaerobic Protozoa (lack mitochondria)
    • Trichomonas vaginalis
    • Entamoeba histolytica
    • Giardia lamblia
29
Q

Metronidazole AKA

A

Flagyl

30
Q

Metronidazole adverse effects

A
  • Unpleasant metallic taste
  • GI: abdominal discomfort, nausea
  • Neuro: Neuropathy, headache
  • Disulfiram-like reaction (when drinking alcohol)
31
Q

Metronidazole bacterial effect

A

Bactericidal

32
Q

Nitrofurantoin MOA

A

Exact mechanism is incompletely understood

33
Q

Nitrofurantoin bacterial effect

A

Bactericidal

34
Q

Nitrofurantoin coverage

A

Rarely used

Only used in UTIs because the drug concentrates in the urine

35
Q

Nitrofurantoin clinical uses

A
  • Only used in UTIs because the drug concentrates in the urine
  • especially for pregnancy because (TMP-SMX and Quinolones are contraindicated)
  • Can trigger hemolysis in G6PD patients
36
Q

Nitrofurantoin adverse effects

A

can trigger hemolysis in G6PD patients