Anti-Microbial Drugs I Flashcards

1
Q

All aminoglycosides concentrate in:

A

Renal cortex

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2
Q

Spectrum of the aminoglycosides:

A
More Gram (-) rods
Some Gram (+) cocci
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3
Q

Aminoglycosides are DOC for:

A
Enterobacter
E. coli
K. pneumonia
Proteus
Serratia
P. aeruginosa
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4
Q

“mycin” drugs are derived from:

A

Streptomyces

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5
Q

“micin” drugs are derived from:

A

Micromonospora

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6
Q

Once a day dosing is effective if the drug has:

A

Significant post-antibiotic effect

Concentration dependent killing

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7
Q

Most stable aminoglycoside against R-plasmid enzymes?

A

Amikacin

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8
Q

Most vesitbulotoxic aminoglycosides:

A

Streptomycin

Gentamycin

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9
Q

Most hearing toxic aminoglycosides:

A

Neomycin
Kanamycin
Amikacin

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10
Q

Most nephrotoxic aminoglycosides:

A

Neomycin
Tobramycin
Gentamycin

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11
Q

Aminoglycosides must not be used with __ due to its __ effects

A

Neuromuscular blockers; neurotoxic

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12
Q

Penicillins bind to PBPs at the ___ terminal and inhibit the ___ enzyme.

A

d-ala-d-ala; transpeptidase

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13
Q

Exceptions to renal clearance of PCNs:

A

Naficillin (biliary)

Oxacillin, Cloxacillin, Dicloxacillin (biliary and renal)

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14
Q

This drug inhibits secretion of PCN:

A

Probenecid

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15
Q

Nafcillin is not as nephrotoxic as other PCN but may cause:

A

neutropenia

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16
Q

Most active PCN against pneumococci:

A

Aminopenicillins

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17
Q

Extended spectrum penicillins are combined with ___ to achieve synergistic effect:

A

aminoglycoside

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18
Q

Cephalosporins are NOT active against:

A

L-monocytogenes
Atypicals
MRSA
Enterococci

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19
Q

Cephalosporins excreted through bile:

A

Cefamandole
Cefoperazone
Ceftriaxone

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20
Q

Cephalosporins with disulfiram-like effectsL

A

Cefamandole
Cefoperazone
Moxalactam

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21
Q

Only first generation Cephalosporin still in use:

A

Cefazolin

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22
Q

2nd Gen Ceph used against community acquired pneumonia:

A

Cefuroxime

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23
Q

More effective than Cefuroxime in crossing the BBB:

A

3rd Gen:

Ceftriaxone
Ceftaxime

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24
Q

2nd Gen Ceph active against Bacteriodes:

A

Cefoxitin

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25
Q

2nd Gen Ceph more susceptible to beta-lactamase:

A

Cefaclor

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26
Q

2nd Gen Ceph active against H. influenzae:

A

Cefmandole
Cefuroxime
Cefaclor

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27
Q

Only 3rd Gen Ceph that cannot cross the BBB:

A

Cefoperazone

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28
Q

Only 3rd Gen Ceph with activity against Gram (+):

A

Cefotaxime

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29
Q

Ceftriaxone is effective against:

A

Resistant salmonella typhi

Gonorrhea

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30
Q

3rd Gen Ceph more active against pseudomonas:

A

Ceftazidime (+ cefoperazone)

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31
Q

3rd Gen Ceph with more activity against anaerobes:

A

Ceftizoxime (+ moxolactam)

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32
Q

Ceftriaxone and Cefotaxime are effective against:

A

Meningitis due to pneumococci, meningococci, h. influenza

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33
Q

For neutropenic, febrile, immunocompromised patient:

A

Ceftazidime+ antibiotic

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34
Q

4th Gen Cephalosporin:

A

Cefepime

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35
Q

Aztreonam is only active against:

A

Gram (-) rods (including pseudomonas)

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36
Q

Absorption of aztreonam:

A

IV only, not absorbed orally

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37
Q

Advantages of Aztreonam:

A

Not nephrotoxic
“cidal” under anaerobic conditions
No PCN cross allergenicity

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38
Q

Carbapenem only active against intracellular bacteria:

A

Imipenem

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39
Q

This carbapenem is more often used and is more active against:

A

Meropenem; Enterobacteria and p. aeruginosa

40
Q

Carbapenems bind to these PBPs preferentially, leading to rapid lysis:

A

PBP-1 “steady”

PBP-2 “moving”

41
Q

Imipenem is combined with this drug to increase it’s half-life:

A

Cilastatin (inhibitor of renal dihydropeptidase)

42
Q

Beta-lactamase inhibitors:

A

Clavulanic Acid
Sulbactam
Tazobactam

43
Q

Lack of ____ in neonates leads to this adverse reaction:

A

hepatic glucoronosyltransferase (glucoronic acid); Gray baby syndrome

44
Q

Dose dependent adverse reaction to chloramphenicol:

A

Aplastic anemia

45
Q

Chloramphenicols are an alternate drug for ____ and ineffective against ____.

A

Pneumonia; chlamydia

46
Q

Chloramphenicols have an antagonistic effect with:

A

Aminoglycosides and Penicillins (-cidal drugs)

47
Q

Lincosamides inhibit protein synthesis by binding to:

A

23s portion of 50s subunit

48
Q

Lincosamides are active against ___, except for:

A

Gram (+) cocci, anaerobes;

Not active against: Staph, strep, enterococcus

49
Q

Drug associated with pseudomembranous colitis:

A

Clindamycin

50
Q

Excretion of lincosamides:

A

Biliary and renal

51
Q

Lincosamides have good penetration in ___, but not in:

A

Bone, fibrous CT, alveolar macrophages;

no penetration in CNS

52
Q

Clinical uses for Lincosamides:

A
Acne
Osteomylitis
Pneumocystis carinii
Toxoplasmosis gondii
Prophylaxis for valvular diseases
53
Q

DOC against clostridium dificile:

A

Metronidazole (also amoeba organisms)

54
Q

Spectrum of Macrolides:

A

Gram (+) aerobes
Some gram (-) aerobes (DOC for legionella)
Atypicals

55
Q

Macrolide excreted in bile and feces:

A

Erythromycin (renal failure no problem)

56
Q

Macrolide excreted in liver and kidneys:

A

Clarithromycin

57
Q

Macrolide excreted slowly in urine, unchanged:

A

Azithromycin

58
Q

Macrolide with high distribution in tissues and phagocytes vs. plasma:

A

Azithromycin

59
Q

This drug is used in treatment of gastroparesis by binding to:

A

Erythromycin; motilin receptors

60
Q

This macrolide is CI in pregnant women due to risk of ___.

A

Erythromycin estolate; acute cholestatic hepatitis

61
Q

Absorption of erythromycin is mainly in the:

A

Duodenum (impeded by food)

62
Q

Best absorbed erythromycin:

A

estolate salt

63
Q

Erythromycin and CYP3A inhibitors increase the risk of:

A

Cardiac arrhythmia

64
Q

Co-administration of these drugs with erythromycin should be avoided by those with heart abnormalities:

A

Diltiazem or verapamil

65
Q

Reasons for telithromycin (ketolide) effectiveness against resistant strains:

A

Poor substrate for efflux pump

Higher affinity for ribosomes

66
Q

MOA of polymixin:

A

Disrupt bacterial cell membranes

Bind and activate endotoxin

67
Q

Adverse effects of polymixin:

A

Substantial nephrotoxicity
Substantial neurotoxicity
(no longer used systematically)

68
Q

First oral anti-pseudomonal drug:

A

Quinolones

69
Q

MOA of Quinolones?

A

Inhibit DNA gyrase (topo II and topo IV)

70
Q

Quinolones more active against p.aeruginosa:

A

Ciproflaxin

71
Q

Quinolones active against staphylococci:

A

Fluoroquinolones

72
Q

Quinolones active against streptococci:

A

Levofloxacin and Moxifloxacin

73
Q

Inhibitors of folic acid synthesis:

A

Sulfonamides (dihydropteroate synthetase)

Diaminopyrimidines (dihydrofolate reductase)

74
Q

Tetracyclines have excellent activity against:

A

Mycoplasma pneumonia

Chlamydia trachomatis

75
Q

Tetracyclines have good activity against:

A

Gram (+), e. coli, klebsiella

76
Q

Tetracyclines have minimal activity against:

A

anaerobes

77
Q

Primary indications of tetracycline:

A
Mycoplasma
Chlamydia
Rickettsia
Vibrios
Borrelia
78
Q

Secondary indications of tetracyclines:

A

Syphilis
Respiratory infection
Leptospirosis
acne

79
Q

Most tetracyclines are excreted ___, except for:

A

Renally; Doxycycline (liver)

80
Q

Tetracylcine affinity for ____ is responsible for it’s effect of:

A

Chelators (calcium, iron, aluminum); enamel dysplasia (mottling of teeth)

81
Q

Adverse reactions of tetracycline:

A

Hepatotoxicity
Nephrotoxicity (Fanconi like syndrome)
Photosensitivity
Vestibular toxicity

82
Q

Vancomycin is a ___ and so does not cross the BBB:

A

Glycopeptide

83
Q

Red man syndrome is associated with:

A

Type I hypersensitivity caused by Vancomycin

84
Q

2 streptogamins in a ____ ratio that interact ___:

A

Dalfopristin (Streptogamin A) and Quinipristin (Streptogamin B); 70:30 ratio; synergystically

85
Q

Excretion of vancomycin is completely:

A

Renal (problem in renal patients)

86
Q

Resistance to streptogamins is due to modification of the ___ site:

A

quinipristin

87
Q

Spectrum of streptogamins:

A

Gram (+) cocci (including drug resistant)

88
Q

Oxazolidinones have a unique __ binding site:

A

23s

89
Q

Oxazolidinones are primarily static, but bactericidal for:

A

Streptococci

90
Q

Most common adverse reaction to oxazolidinones:

A

Thrombocytopenia

91
Q

Inhibits very early stage of bacterial wall synthesis:

A

Fosfomycin

92
Q

These drugs act only in the urinary bladder, not systemically:

A
Nitrofurantoin (except p. aeruginosa & proteus)
Methenamine hippurate (except proteus)
Phenazopyridine (analgesic only)
93
Q

MOA of daptomycin:

A

Disruption of cytoplasmic membrane

94
Q

Daptomycin is effective against ___ but not against ___.

A

Staphylococcus; respiratory infections

95
Q

Bacteriostatic activity against MRSA:

A

Tigecycline