Antimicrobials Flashcards

1
Q

What had biggest effect on human life expectancy?
A. Public health measures, sanitation, and immunization
B. Antimicrobials

A

A. Public health measures

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2
Q

% of death worldwide due to infectious disease?

A

10%

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3
Q

How are antibacterials classified?

A

By MOA

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4
Q

MIC definition?

A

Lowest concentration of drug that inhibits visible growth

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5
Q

MBC definition?

A

Lowest concentration of drug that kills bacteria

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6
Q

Define bacteriostatic in terms of MBC and MIC

A

MBC&raquo_space; MIC

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7
Q

Define bactericidal in terms of MBC and MIC

A

MBC roughly equals MIC

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8
Q

The lower the MBC/MIC of an organism/drug combo, the ____ the organism.

A

more susceptible

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9
Q

Methods for determining microbial susceptibility/resistance?

A

Culture based (disk diffusion and E-test) or molecular detection of resistance mutations (i.e. PCR)

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10
Q

What is a hospital antibiogram?

A

Summary of antibiotic susceptibilities in your own site to track resistance trends

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11
Q

Pharmacodynamics is…

A

the biological effects of the drug on the body (i.e. time course and intensity of therapeutic and adverse effects)

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12
Q

Pharmacokinetics is…

A

the body’s effect on the drug (i.e. time course of absorption, distribution, metabolism, and excretion)

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13
Q

Cmax is?

A

Peak concentration of drug in body

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14
Q

AUC is?

A

Area under the curve

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15
Q

Time dependent killing goal?

A

Maximize time above the MIC; you want serum [drug] above MIC for at least 50% of dosing interval

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16
Q

Beta lactam MOA?

A

bind PBP and inhibit peptidoglycan synthesis

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17
Q

Name the 5 beta lactam subclasses

A

penicillins, carbapenems, monobactams, clavulanic acid, cephalosporins

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18
Q

Glycopeptides MOA?

A

inhibit transglycosylase activity in peptidoglycan synthesis

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19
Q

Function of PBPs?

A

make peptidoglycan

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20
Q

PBPs must have ____ function, and may also have ____ function.

A

peptidyltransferase; transglycosylase

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21
Q

Penicillin resembles…

A

D-Ala D-Ala moiety

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22
Q

Concentration-dependent killing goal?

A

Maximize Cmax and therefore AUC

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23
Q

Drugs with TDK MOA?

A

Penicillins, Cephalosporins, Macrolides, Clindamycin

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24
Q

Drugs with CDK MOA?

A

Fluoroquinolones, Aminoglycosides

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25
Q

Post antibiotic effect is…

A

time it takes bacteria to return to log phase growth after removal of abx

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26
Q

Bacteria with longer PAEs require need ___ frequencies of dosing.

A

lower

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27
Q

Which generally needs longer PAE? CDK or TDK?

A

CDK

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28
Q

Which generally needs longer PAE? Gram + or -?

A

Gram +

29
Q

What are the three main antibiotic resistance mechanisms?

A

Enzymatically inactivate drug, alter drug target, alter drug exposure

30
Q

What does beta-lactamase do?

A

Enzymatically inactivate beta-lactams

31
Q

What does clavulanic acid do?

A

Inhibits beta-lactamase, overcome abx resistance

32
Q

2 beta-lactamases to know?

A

ESBL (extended spectrum beta lactamases) and Metal-dependent/New Delhi

33
Q

What is the “nuclear option” for beta-lactam resistance?

A

PBP mutation that alters affinity for beta-lactams, but still retain transpeptidase activity

34
Q

Prioritize choosing abx with ____ fitness cost for resistance

A

higher

35
Q

Gram ___ bacteria alter their membrane permeability to pump out abx

A

negative

36
Q

2 ways to alter drug exposure?

A

decrease membrane permeability; increase efflux of drug to shoot out of cell

37
Q

Main abx resistance mechanism for vancomycin?

A

Alter D-Ala D-Ala slightly with lac so that vancomycin cannot bind precursor.

38
Q

Lipopeptides MOA?

A

disrupt cell membrane of G+ by binding phosphatidyl-glycerol forming pores

39
Q

Why are lipopeptides specific?

A

Phosphatidyl-glycerol is abundant in bac cells but not human cells

40
Q

What part of body should lipopeptides not be used to treat?

A

Lungs (surfactant)

41
Q

Main lipopeptide to know?

A

Daptomycin

42
Q

Main class of folate synthesis inhibitors?

A

Sulfonamides

43
Q

Main sulfonamide to know?

A

Sulfamethoxazole

44
Q

Are sulfonamides bacteriostatic or bactericidal?

A

Bacteriostatic, combine with trimethoprim to make bactericidal

45
Q

Are fluoroquinolones bacteriostatic or bactericidal?

A

Bactericidal

46
Q

Fluoroquinolone resistance is usually via ____ and/or ___

A

altering the drug target (mutations in topoisomerase genes); altering the drug exposure by decreasing uptake

47
Q

Rifamycins MOA?

A

inhibit mRNA synthesis by binding DNA dep RNA Pol

48
Q

Rifamycins bacteriostatic or bactericidal?

A

Either! Depends on concentration

49
Q

Rifamycin to know?

A

Rifampin

50
Q

Rifamycin is rarely used alone because it quickly develops abx resistance by ____

A

mutations in RNA polymerase gene (altered drug target)

51
Q

2 main classes of drugs that damage DNA?

A

fluoroquinolones and nitroimidazoles

52
Q

Main nitroimidazole to know?

A

metronidazole

53
Q

Nitroimidazole MOA?

A

forms free radicals that damage DNA

54
Q

Which class of abx is a prodrug? What does this mean?

A

nitroimidazoles - must be activated by microbial enzymes

55
Q

Most likely cause of abx resistance in nitroimidazoles?

A

mutations in microbial enzymes that convert prodrug to active compound

56
Q

Name all the classes of 30S ribosome antibiotics.

A

tetracyclines, aminoglycosides

57
Q

Name the 2 important tetracyclines to know.

A

Tetracycline, doxycycline

58
Q

Name the 2 important aminoglycosides to know.

A

gentamycin, streptomycin

59
Q

Name the 2 classes of abx used for anaerobic microbes exclusively. Which one is bacteriostatic and which one is bactericidal?

A

Lincosamides, nitroimidazoles; lincosamides = static, nitroimidazoles = cidal

60
Q

Aminoglycosides should not be used in what part of the body and why?

A

the GI tract; will be ineffective because anaerobes are intrinsically resistant

61
Q

Tetracycline is bacteriostatic or bactericidal?

A

Bacteriostatic

62
Q

Bacteriostatic drugs + bactericidal drugs = ?

A

Antagonistic effect

63
Q

5 classes of abx that bind 50S subunit?

A

oxazolidenones, streptomycins, lincosamides, macrolides, chloramphenicol

64
Q

Clindamycin falls under what class of antibiotic?

A

Lincosamide

65
Q

2 main types of macrolides to know?

A

erythromycin, azithromycin

66
Q

MLSb resistance is associated with which abx? Why does it happen?

A

macrolides, lincosamides, and streptogramins; similar MOA

67
Q

What does the D test detect?

A

inducible clindamycin resistance

68
Q

Main oxazolidinone to know?

A

linezolid