25 - Antibacterial drugs Flashcards

1
Q

Term: antibacterial that can eradicate an infection in the absence of host defense mechanisms

A

bactericidal

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2
Q

Term: antibacterial that can inhibit microbial growth but requires host defense mechanisms to eradicate the infection

A

bacteriostatic

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3
Q

Enumerate: Bactericidial Antibiotics

A
  • Vancomycin
  • Fluoroquinolones
  • Penicillins
  • Aminoglycosides
  • Metronidazole

Very Finely Proficient At Murder

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4
Q

Enumerate: Bacteriostatic antibiotics

A
  • Erythromycin
  • Sulfamethoxazole
  • Trimethoprim
  • Tetracycline
  • Clindamycin
  • Chloramphenicol

ESTTCC (static!)

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5
Q

Term: lowest concentration of antimicrobial drug capable of inhibiting growth of an organism in a defined growth medium

A

Minimum Inhibitory Concentration

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6
Q

Term: initiation of drug treatment before identification of a specific pathogen

A

Empiric therapy

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7
Q

Term: use of an antimicrobial drug to decrease the risk of infection

A

Antibiotic prophylaxis

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8
Q

DOC for MRSA

A

Vancomycin

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9
Q

DOC for VRSA

A

Linezolid

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10
Q

Enumerate: Drug classes of Beta-Lactam Antibiotics

A
  • Penicillins
  • Cephalosporins
  • Monobactams
  • Carbapenems
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11
Q

MOA of Beta-lactam anitbiotics:

A
  • binds to penicillin-binding proteins

- inhibits the transpeptidation reaction, disrupting cell wall synthesis

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12
Q

DOC for syphillis

A

Penicillin G

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13
Q

Common adverse reactions to Penicillin (give 3)

A
  • Hypersensitivity
  • cross-reactivity with other penicillins
  • gastrointestinal disturbance
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14
Q

Enumerate: (2) long-acting preparations of Penicillin G

A
  • Benzathine Penicillin

- Procaine Penicillin

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15
Q
  • Give example of extended spectrum Penicillin

- Enumerate: bacteria covered by extended spectrum penicillins.

A

-Ampicillin

  • Haemophilus influenza
  • Escherichia coli
  • Listeria monocytogenes
  • Proteus mirabilis
  • Salmonella
  • enterococci

HELPSe

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16
Q

Enumerate: anti-pseudomonal Penicillins

A
  • Ticarcillin
  • Carbenicillin
  • Piperacillin

Takes Care of Pseudomonas

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17
Q

Drug of choice for Acute Rheumatic Fever:

A

Penicillin G

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18
Q

Drug of choice for Streptococcus agalactiae:

A

Penicillin G

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19
Q

Treatment for Group D streptococcus:

A

Penicillin + gentamicin

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20
Q

DOC for Streptococcus pneumoniae

A

Penicillin G

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21
Q

DOC for cutaneous anthrax

A

Ciprofloxacin

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22
Q

DOC for pseudomembranous colitis

A

metronidazole

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23
Q

DOC for pertussis

A

Erythromycin

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24
Q

treatment for cholera:

A

Tetracycline or azithromycin

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25
Q

Drug that is given as prophylaxis before GI surgeries:

A

cefoxitin

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26
Q

DOC for early Lyme disease

A

doxycycline

Lyme = Borrelia burgdorferi = Ixodes = i-XO-des = d-OX-ycycline!!!!!

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27
Q

DOC for all rickettsial infections:

A

doxycycline

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28
Q

Why is cilastatin given together with imipenem?

A

Cilastatin inhibits renal metabolism of imipenem by dihydropeptidase

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29
Q

This class of beta-lactam drugs is reserved for serious, life-threatening infections:

A

Carbapenems

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30
Q

Drug class of Aztreonam

A

Monobactam

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31
Q

This drug has no cross-allergenicity with penicillins, and does not cause hypersensitivity

A

Aztreonam

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32
Q

Enumerate (3): beta-lactams and beta-lactamase inhibitor pairs

A
  • Piperacillin-Tazobactam (Pip-Tazo)
  • Amoxicillin-Clavulanic acid (Co-amoxiclav)
  • Ampicillin-Sulbactam (Ampi-Sul)
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33
Q

Drug class of Vancomycin:

A

glycopeptide

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34
Q

MOA of Vancomycin:

A

Inhibits cell wall synthesis by binding to D-ala-D-ala terminus, inhibiting transglycosylation, inhibiting elongation and cross-linking of the peptidoglycan chain

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35
Q
  • Adverse effect of Vancomycin:

- How to avoid this adverse effect?

A
  • Redman syndrome

- slow down infusion rate

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36
Q

Formulation of Vancomycin that can be used in the treatment of pseudomembranous colitis:

A

oral Vancomycin

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37
Q

Enumerate: drugs of last resort

A
  • Imipenem
  • Amikacin
  • Meropenem
  • Linezolid
  • Streptogramins
  • Vancomycin

I AM your Last Shot at Victory

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38
Q

MOA of Bacitracin

A

Interferes with a late stage in cell wall synthesis in gram-positive organisms

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39
Q

Adverse effect of bacitracin:

A

nephotoxicity (thus only used topically)

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40
Q

MOA of Cycloserine

A

blocks incorporation of D-Ala into the pentapeptide side chain of the peptidoglycan

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41
Q

uses of Cycloserine (1)

A

2nd line drug for drug-resistant tuberculosis

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42
Q

MOA of Daptomycin

A

binds to cell membrane causing depolarization and rapid cell death

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43
Q
  • Adverse effect of Daptomycin

- how to monitor this adverse effect?

A
  • Myopathy

- serial monitoring of creatine phosphokinase

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44
Q
  • MOA of fosfomycin

- uses?

A
  • prevents formation of NAM

- uncomplicated UTI

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45
Q

Enumerate: 30S ribosomal subunit inhibitors:

A
  • Aminoglycosides
  • Tetracyclines

AT CELLS

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46
Q

Enumerate: 50S ribosomal subunit inhibitors:

A
  • Chloramphenicol
  • Erythromycin and other macrolides
  • Lincosamides (Clindamycin)
  • Linezolid
  • Streptogramins

AT CELLS

47
Q
  • Enumerate: protein synthesis inhibitors that are bactericidal
  • Enumerate: protein synthesis inhibitors that are bacteriostatic
A
  • cidal: Aminoglycosides, Streptogramin

- static: all the rest - Tetracycline, Chloramphenicol, Erythromycin, Lincosamide (Clindamycin), Linezolid

48
Q

Prominent adverse effect of chloramphenicol:

A

gray baby syndrome

49
Q

Most potent tetracycline:

A

minocycline

50
Q

tetracycline with the broadest spectrum:

A

tigecycline

51
Q

Adverse effect of tetracyclines:

A

tooth enamel discoloration/dysplasia

52
Q

Enumerate: 3 examples of macrolides:

A
  • Erythromycin
  • Azithromycin
  • Clarithromycin
53
Q

All macrolides inhibit CYP450 except:

A

Azithromycin

54
Q

General indication for use of macrolides:

A

useful as alternative for those allergic to penicillins

55
Q

Enumerate: Adverse effect of macrolides (2)

A
  • GI upset

- QT prolongation

56
Q

Drug class of Clindamycin:

A

Lincosamide

57
Q

Adverse effect of Clindamycin

A

-Pseudomembranous colitis (Clostridium difficile growth)

58
Q

Differentiate Clindamycin vs Metronidazole in terms of usage:

A
  • Clindamycin - used for anaerobic infections above the diaphragm
  • Metronidazole - used for anaerobic infections below the diaphragm
59
Q

Representative drug for Streptogramin:

A

Quinupristin-Dalfopristin

60
Q
  • Enumerate: Two modes of antibacterial action:

- give examples of drugs that exhibit these modes:

A
  1. concentration-dependent killing action - e.g. aminoglycosides
  2. time-dependent killing action - e.g. penicillins, cephalosporins
61
Q
  • What is Post-Antibiotic effect?

- What classes of drugs exhibit this effect?

A
  • killing action continues even when the drug levels in the plasma have declined below measurable levels
  • e.g. aminoglycosides, quinolones
62
Q

Identify: Aminoglycoside with the narrowest spectrum

63
Q
  • What class of drugs have a synergistic effect with aminoglycosides?
  • explain mechanism of this synergism
  • classic drug combination that utilizes this synergism:
A
  • cell wall synthesis inhibitors
  • they enhance the uptake of aminoglycosides into the cell

e.g. Ampicillin+Amikacin

64
Q
  • Enumerate: (6) examples of aminoglycosides

- Enumerate: (3) adverse effects of aminoglycosides

A
  • Gentamicin
  • Neomycin
  • Amikacin
  • Tobramycin
  • Streptomycin
  • Spectinomycin
  • Nephrotoxicity
  • Ototoxicity
  • Teratogen

GNATSS NOT!

65
Q

Enumerate: (2) most ototoxic aminoglycosides:

A

amikacin, kanamycin

66
Q

Identify: Aminoglycoside with the least resistance

67
Q

Treatment for Yersinia pestis:

A

Streptomycin

68
Q

Why is neomycin limited to topical and oral use only? (adverse effect)

A

because it can cause hepatic encephalopathy

69
Q

Use of spectinomycin:

A

Drug-resistant Neisseria gonorrhoeae or for patient allergic to penicillins

70
Q

Treatment of Neisseria gonorrhoeae

A

ceftriaxone + doxycycline

71
Q

Enumerate: (2) most vestibulotoxic aminoglycosides:

A

tobramycin, gentamicin

72
Q

Enumerate: (2) most nephrotoxic aminoglycosides:

A

tobramycin, gentamicin

73
Q

adverse effect of spectinomycin:

A

non-depolarizing NMJ blockade

74
Q
  • MOA of fusidic acid

- uses of fusidic acid

A
  • inhibits translocation during protein synthesis

- topical antimicrobial against common skin pathogens, e.g. Staphylococcus aureus

75
Q

MOA of sulfonamides:

A

-competitive inhibition of dihydropteroate synthase, inhibiting folic acid synthesis (competes with PABA)

76
Q

MOA of trimethoprim:

A

-selective inhibitor of dihydrofolate reductase

77
Q

Explain mechanism of synergism of Trimethoprim-Sulfamethoxazole:

A
  • sequential blockade of folate synthesis

- drug combination is bactericidal

78
Q

Drug class of silver sulfadiazine:

A

Sulfonamide

79
Q

use of silver sulfadiazine

A

burn infections

80
Q

Use of trimethoprim-sulfamethoxazole:

A
  • Pneumocystis jirovecii pneumonia
  • Nocardia
  • UTI
81
Q

Enumerate: adverse effects of sulfonamides:

A
  • SJS/TEN
  • GI distress
  • granulocytopenia, thrombocytopenia
  • crystalluria, hematuria
82
Q

MOA of quinolones: (2)

A
  • inhibit topoisomerase II (DNA gyrase) in gram (-) bacteria
  • inhibit topoisomerase IV in gram (+) bacteria

thus inhibiting DNA synthesis

83
Q
  • What subset of the population should not be treated with quinolones?
  • why?
A
  • patients less than 18 years old

- may damage growing cartilage and cause arthropathy

84
Q

-Quinolones vs Fluoroquinolones?

A
  • Quinolones: 1st gen

- Fluoroquinolones: 2-4th gen

85
Q
  • example of 1st gen quinolone? (4)

- uses?

A

Nalidixic acid, cinoxacin, rosoxacin, oxolinic acid

UTIs

86
Q

-example of 2nd gen fluoroquinolone? (2)

A

Ciprofloxacin, ofloxacin

87
Q

-example of 3rd gen fluoroquinolone?

A

Levofloxacin, moxifloxacin

88
Q

-example of 4th gen fluoroquinolone?

A

Trovafloxacin

89
Q

Fluoroquinolone with activity agains anaerobic bacteria?

A

4th gen fluoroquinolones, e.g. Trovafloxacin

90
Q

MOA of metronidazole?

A

-reactive reduction by ferredoxin forming free radicals that disrupt electron transport chain. Bactericidal.

91
Q

Uses of metronidazole: bacterial (give 4)

A
  • pseudomembranous colitis (Clostridium difficile)
  • botulism (Clostridium botulinum)
  • bacteroides fragilis
  • Gardnerella vaginalis
92
Q

drug class of metronidazole?

A

nitroimidazole

93
Q

drug class of nitrofurantoin?

A

nitrofuran

94
Q

MOA of nitrofurantoin?

A

Forms multiple reactive intermediates when acted upon by bacterial nitrofuran reductase that disrupt protein, RNA, and DNA synthesis

95
Q

Use of nitrofurantoin?

A

uncomplicated cystitis

96
Q

MOA of mupirocin:

A

inhibits Staphylococcal isoleucyl tRNA synthetase

97
Q

Uses of mupirocin:

A

for minor skin infections such as impetigo

98
Q

MOA of isoniazid:

A

inhibits mycolic acid synthesis, interfering with cell wall synthesis

99
Q

Adverse effects of isoniazid: (2)

A

hepatotoxicity and neurotoxicity (peripheral)

100
Q

How to prevent neurotoxicity of isoniazid:

A

co-administer pyridoxine (Vit. B6), 2-4 hours apart

101
Q

MOA of rifampicin

A

inhibits DNA-dependent RNA polymerase, inhibiting RNA synthesis

102
Q

Adverse effect of rifampicin (2)

A

orange-colored body fluids

hepatotoxicity

103
Q

MOA of pyrazinamide:

104
Q

adverse effect of pyrazinamide:

A

hepatotoxicity

105
Q

Enumerate: Hepatotoxic anti-TB drugs: (from least to most hepatotoxic)

A

Isoniazid < Rifampicin < Pyrazinamide

HRZ!

106
Q

MOA of ethambutol:

A

inhibits arabinosyl transferases involved in the synthesis of arabinogalactan in mycobacterial cell wall.

107
Q

Identify: bacteriostatic anti-TB drug:

A

Ethambutol

108
Q

Adverse effect of ethambutol (3):

A

visual disturbance,
red-green color blindness,
hyperuricemia

109
Q

Uses for streptomycin:

A
  • TB

- Yesinia pestis

110
Q

MOA of dapsone:

A

inhibits folic acid synthesis

111
Q

uses of dapsone:

A

Mycobacterium leprae (most active drug)

112
Q
  • drug for dapsone-resistant M. leprae
  • MOA:
  • adverse effect:
A
  • Clofazimine
  • binds to guanine bases in bacterial DNA
  • skin discoloration
113
Q

Repository form of dapsone which has drug action that can last for months:

A

Acedapsone