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Disease and Defense > Antibacterial Agents > Flashcards

Antibacterial Agents Flashcards

1
Q

Penicillins mechanism of action

A

Cell wall synthesis inhibitor (bactericidal)

  • inhibit cross-linking of peptidoglycan polymers at cell wall
  • Covalently binds penicillin binding proteins (PBPs)
  • Promotes lysis of bacteria
  • Effect persists due to covalent binding to bacterial proteins
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2
Q

Resistance to penicillins?

What resistance does MRSA vs. MSSA have?

A

1) B-lactamase: enzyme that hydrolyze B-lactams (penicillins, cephalosporins)
- MSSA → not broken down by B-lactamase
2) Alteration in PBPs (MRSA)

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3
Q

Penicillins have ______ excretion

A

renal

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4
Q

Types of Penicillins

A 
Penicillin G
Penicillin V
Penicillinase-resistant
Extended spectrum
Antipseudomonal
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5
Q

Penicillin V is administered _____ for ________

A

orally for mild-to-moderate infections

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6
Q

Dicloaxillin is a ….

A

penicillinase resistant penicillin

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7
Q

Amoxicillin and ampicillin are…

A

extended spectrum penicillins

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8
Q

Piperacillin is a _______ and typically administered _______ with _________

A

antipseudomonal penicillin

administered IV witha B-lactamase inhibitor

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9
Q

B-lactamase inhibitors

A

Clavulanate or tazobactam

used with amoxicillin/ampicillin and piperacillin

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10
Q

Adverse reactions associated with Penicillins (2)

A

1) Anaphylaxis, type I, RARE

2) rashes (common)

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11
Q

Ampicillin/Amoxicillin side effects and explain why

A

1) Extended spectrum but not effective against C.diff and others –> superinfections possible
2) diarrhea

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12
Q

Penicillin spectrum/uses (2)

A

1) Gram + cocci (staph, strep, entero - NOT MRSA or MSSA)

2) anaerobes (NOT c. dif or b. fragilis)

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13
Q

Dicloxacillin spectrum/uses (1)

A

Penicillinase resistant

1) Gram + cocci (MSSA, NOT MRSA)

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14
Q

Amoxicillin/Ampicillin spectrum/uses (3)

Amox/Clav spectrum / uses

A

Extended spectrum

1) Gram + cocci (NOT MRSA or MSSA)
2) Gram - rods (E.coli)
3) some anaerobes (NOT c.diff or bacteriodes)
- ——————————————
* *add B-lactamase inhibitor (clav)**

1) Gram + cocci including MSSA** (NOT MRSA)
2) Gram - rods (E.coli)
3) some anaerobes including B. fragilis** (NOT c.diff)

-more hydrophobic –> can penetrate gram-

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15
Q

Pipercillin + Tazo spectrum/uses

A

Antipseudomonal + B-lactamase inhibitor

1) Gram - rods (E.coli) AND Pseudomonas**
2) Gram + cocci (MSSA, NOT MRSA)
3) Anaerobes including B. Fragilis

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16
Q

Vancomycin mechanism of action

A

cell wall synthesis inhibitor

inhibits linear polymerization of subunits at cell membrane

-Binds directly to D-ala-D-ala

stage 2 inhibitor - other CW synthesis inhibitors are stage 3

–> NOT inactivated by B-lactamase****

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17
Q

Administration of Vancomycin

A

IV usually

poor oral absorption - only use oral for C.diff GI infection

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18
Q

Excretion of vancomycin

A

renal excretion

Possible renal toxicity

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19
Q

Adverse reactions of Vancomycin (3)

A

1) ototoxicity
2) renal toxicity - MONITOR CP LEVELS!
3) infusion related side effects (chills, fever, rash)

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20
Q

Spectrum/Uses of Vancomycin (2)

A

Narrow spectrum

1) Anaerobes - CDIFF
2) Gram + cocci - MRSA**

NOT EFFECTIVE AGAINST GRAM -

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21
Q

Cephalosporins mechanism of action

A

cell wall synthesis inhibition (bactericidal)

B-lactam antibiotic

  • stage 3 - inhibit cross-linking of peptidoglycan polymers at cell wall
  • NOT susceptible to penicillinase
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22
Q

If your patient has an immediate sensitivity to penicillin you definitely should NOT…

A

give them a cephalosporin

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23
Q

Cephalexin is a…

A

1st Generation Cephalosporin

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24
Q

Ceftriaxone is a ….

A

3rd Generation Cephalosporin

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25
Q

Cephalosporins vs. Penicillins (3 differences)

A

1) Broader spectrum of action vs. gram-neg bacteria
2) Less susceptible to penicillinase (cephalosporinases are emerging)
3) Less cross-reactivity in penicillin sensitive patients

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26
Q

3rd generation cephalosporins (ceftriaxone) can penetrate…

A

THE CNS

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27
Q

Adverse reactions associated with 3rd gen cephalosporin (ceftriaxone)

A

superinfection possible

-not effective against C.diff

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28
Q

Spectrum/uses for Cephalexin (3)

A

1) Gram + cocci (MSSA, not MRSA)
2) Gram - rods (E.coli)
3) some anaerobes (not c.diff or b. fragilis)

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29
Q

Spectrum/uses for Ceftriaxone (5)

A

1) Gram + cocci (MSSA, not MRSA)
2) Gram - rods (E.coli)
3) Gram - cocci (N. Gonorrhoeae)
4) moderate anti-pseusomonal
5) some anaerobes (not c.diff or b. fragilis)

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30
Q

Carbapenems mechanism of action

A

cell wall synthesis inhibition (bactericidal)

  • B-lactamase resistant
  • interact with PBPs responsible for cell wall elongation
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31
Q

Carbapenems are administered…

A

IV/IM only

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32
Q

Carbapenems are excreted…

A

renally

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33
Q

Spectrum of carbapenems

A

WIDE spectrum

-reserve for multidrug resistant organisms

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34
Q

Strep. pneumoniae, strep viridans, N. gonorrhoeae all carry __________ that cause resistance to penicillins

A

Altered penicillin binding proteins (PBPs)

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35
Q

Oral formulations of Vancomycin will work for _______ because IV formulations _________

A

C. diff

will not get into the gut

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36
Q

Macrolides mechanism of action

A

protein synthesis inhibition
50S
bacteriostatic

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37
Q

Macrolides include ______, _________, and ________

A

Erythromycin
Azithromycin
Clarithromycin

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38
Q

Macrolides are all excreted…

A

NON-RENALLY

Erythromycin –> liver metabolism

Azithromycin –> Biliary

Clarithromycin –> metabolized to active metabolite

39
Q

Resistance to macrolides can occur via…

A

methylation of 50S subunit

altered target –> resistance

40
Q

Macrolides are administered…

A

orally (also IV)

41
Q

Adverse reactions associated with Macrolides (2)

A

1) GI disturbances (N/V/D)

2) Inhibits CYP450** –> drug-drug interactions

42
Q

Spectrum/Uses of Macrolides (Erythromycin, Azithromycin, Clarithromycin) (3)

A

Extended spectrum

1) Gram + cocci (MSSA, NOT MRSA)
2) Gram - diplococci (N. Gonorrhoeae)
3) Atypical (Chlamydia, Mycoplasma)

NOT gram - rods or anaerobes (NO ecoli, pseudomonas, c diff)

43
Q

Mechanism of action of tetracyclines

A

protein synthesis inhibitor
30S
Bacteriostatic

44
Q

Tetracyclines include ________ and ________

A

Doxycycline and Minocycline

45
Q

Resistance can occur to tetracyclines via…

A

changes in drug transport out of the cell

46
Q

Doxycycline is excreted _________ and tetracycline is excreted _________

A

non-renally (biliary)

renally

47
Q

Administration of doxy and tetracycline

A

oral

48
Q

Adverse effects of tetracycline and doxy (4)

A
  1. Abnormal bone/tooth development
  2. Fungal superinfection
  3. Drug-Drug interaction with metal cations (antacids, iron supplements, milk)
  4. GI
49
Q

Spectrum/uses for tetracyclines (5)

A

BROAD spectrum (lots of resistance now though)

1) Gram + cocci - MRSA!
2) Gram - diplococci (N. Gonorrhoeae)
3) Gram - rods (E. coli)
4) Atypical - Chlamydia, Mycoplasma
5) Anaerobes - B. Fragilis (NOT c.diff)

NOT pseudomonas, NOT c diff

50
Q

Clindamycin mechanism of action

A

protein synthesis inhibition
50S
bacteriostatic

51
Q

Clindamycin is administered…

A

orally

52
Q

Clindamycin is excreted…

A

non-renally

Hepatobiliary elimination

53
Q

Clindamycin can penetrate…

A

BONE

54
Q

Adverse reactions to Clindamycin

A

1) severe diarrhea

2) Pseudomembranous colitis (C.diff)

55
Q

Spectrum/Uses of Clindamycin (2)

A

NARROW spectrum

1) Gram + cocci (MRSA!)
2) Anaerobes - B. Fragilis (NOT c.diff)

NOT gram- rods, Gonorrhea, c.diff, chlamydia, or mycoplasma

56
Q

Aminoglycoside mechanism of action

A

Protein synthesis inhibition
30S

BACTERICIDAL** - binds irreversible

57
Q

Administration of aminoglycoside

A

Dose once a day

IV/IM - poor oral absorption

58
Q

Aminoglycosides includes _______, ________, ________, and ________

A

Tobramycin
Gentamicin
Neomycin
Streptomycin

59
Q

Aminoglycosides are excreted…

A

renally

60
Q

Aminoglycosides preferentially accumulate where?

A

kidney and inner ear –> ototoxicity, and renal toxicity

61
Q

Adverse reactions associated with aminoglycosides

A

1) vestibular and auditory toxicity

2) Nephrotoxicity - MONITOR CP LEVELS

62
Q

for _______ and _______ you must routinely monitor CP levels due to possible renal toxicity

A

Aminoglycosides (neomycin, streptomycin)

Vancomycin

63
Q

Spectrum of aminoglycosides (1)

A

Narrow Spectrum

1) Gram - aerobes (e.coli, pseudomonas)

NO super infections b/c narrow spectrum

64
Q

What can be used to treat MRSA (3)

A

1) Vancomycin
2) Tetracyclines
3) Clindamycin

65
Q

What can be used to treat N. Gonnorrhoeae? (3)

A

1) Ceftriaxone
2) Macrolides
3) Tetracyclines

66
Q

What can be used to treat c. diff? (2)

A

1) Vancomycin

2) Metronidazole

67
Q

What can be used to treat chlamydia? (2)

A

1) Macrolides

2) Tetracyclines

68
Q

Aminoglycosides will sometimes be used synergystically with _______ or ______ in treatment of _________

A

penicillin or ampicillin

Enterococcal

By themselves aminoglycosides do NOT have activity against enterococcal isolates

69
Q

Erythromycin is given ______ x a day

Azithromycin is given ______ x a day

Clarithromycin is given ______ x a day

A

4x a day

1x a day

2x a day

70
Q

Fluoroquinolones include ________, _________ and __________

A

Ciprofloxacin, Levofloxacin, Moxifloxacin

71
Q

Mechanism of action of fluoroquinolones

A

inhibit DNA gyrase

BACTERICIDAL

72
Q

Resistance to Fluoroquinolones due to…

A

due to point mutations in binding site on DNA gyrase or changes in drug permeability into organism

73
Q

Administration of fluoroquinolones

A

oral (or IV)

74
Q

Adverse reactions associated with fluoroquinolones? (6)

A

1) N/V/D
2) Superinfections with CDIFF possible

3) Drug-Drug interactions
- CYP450 inhibitor***

4) NOT first choice in children less than 12 yrs (arthralgias possible)
5) QT prolongation
6) rashes

75
Q

What Drug-Drug interactions occur with fluoroquinolones?

A

Drug-Drug interactions with theophylline and antacid

Antacids reduce oral absorption of cipro

76
Q

Spectrum of ciprofloxacin

A

1) Gram - rods (psuedomonas)
2) Atypical (chlamydia, mycoplasma)

Uncomplicated-complicated UTIs**

Traveler’s diarrhea

77
Q

Spectrum of Levofloxacin

A

1) gram - rods (including pseudomonas)
2) atypical (chlamydia, and mycoplasma)
3) AND gram + cocci (streps only)

Good for UTI and respiratory

78
Q

Spectrum of Moxifloxacin

A

1) atypical (chlamydia, and mycoplasma)
2) gram + cocci (streps only)
3) some anaerobes

Good for respiratory

79
Q

Nitrofurantoin mechanism of action

A

reduced in cell to intermediates that damage bacterial DNA → BACTERICIDAL

-CANNOT be used for treatment of systemic infections - only UTI

80
Q

Administration and excretion of Nitrofurantoin

A

Oral admin with RAPID renal excretion –> urinary antiseptic

81
Q

Adverse reactions of Nitrofurantoin (1)

A

1) GI side effects

82
Q

Spectrum of Nitrofurantoin (1)

A

1st line agent in uncomplicated UTIs

1) ONLY gram- rods (can’t treat atypical)

83
Q

Metronidazole mechanism of action

A
  • Reduced intracellularly to active form → interfere with DNA function
  • Radical formation → target DNA
  • Only good against anaerobes
  • BACTERICIDAL
84
Q

Administration and excretion of Metronidazole

A

Oral therapy

Hepatic metabolism

85
Q

Spectrum of Metronidazole (2)

A

1) Anaerobes (C. Diff, B. Fragilis)

2) Protozoa

86
Q

Adverse drug reactions of Metronidazole

A

1) Nausea, headache
2) Antabuse-like reaction (drug to tx alcoholism)
3) occasional candidal superinfections

87
Q

Why does Metronidazole have antabuse-like reactions?

A

Inhibits aldehyde dehydrogenase → antabuse-like effect if alcohol is consumed within 3 days of metronidazole

Antabuse → GI upset, vomiting, headache - used in alcohol tx

88
Q

Sulfonamides mechanism of action

A

Inhibits folate metabolism (dihydropteroate synthetase - only in bacteria) → interfere with DNA synthesis

BACTERIOSTATIC alone and BACTERICIDAL in combo (SMX/TMP)

89
Q

SMX/TMP

A

inhibit two sequential enzymatic processes involved in tetrahydrofolic acid biosynthesis

  • Trimethoprim - NOT a sulfonamide
  • Sulfamethoxazole
90
Q

Administration and Excretion of Sulfonamides

A

oral therapy

renal excretion AND hepatic excretion

91
Q

Adverse reactions of sulfonamides

A

1) Hypersensitivity skin reactions
2) Kernicterus in neonates**
3) Renal crystalluria (rare) via decrease in water solubility of metabolites

92
Q

You should NEVER give sulfonamides to who?

A

neonates!

–> Kernicterus due to bili build up

93
Q

Spectrum of TMP/SMX (3)

A

1) Gram + cocci (including MRSA)
2) gram - rods (e. coli)
3) atypical (chlamydia)

Disease and Defense (11 decks)

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