Antimicrobials Flashcards

1
Q

Sub-classes of Beta-lactam antibiotics

A

Penicillins
Cephalosporins
Monobactams
Carbapenems

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2
Q

Beta-lactamase inhibitors

A

Clavulanic acid
Sulbactam
Tazobactam
NXL104

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3
Q

Penicillin mechanism of action

A

binds to penicillin binding proteins in bacterial cell wall - blacks transpeptidase crosslinking

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4
Q

Penicillin activity spectrum

A

Gram positives and syphillis

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5
Q

Penicillin toxicity

A

hypersensitivity rxns, hemolytic anemia

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6
Q

Penicillinase resistant penicillins

A

methicillin
nafcillin
dicloxacillin

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7
Q

Penicillinase resistant penicillin treats which orgs?

A

S. aureus

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8
Q

Penicillinase resistant penicillin toxicity

A

hypersensitivity,

methicillin: interstitial nephritis

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9
Q

Aminopenicillins

A

Ampicillin

Amoxacillin

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10
Q

Aminopenicillins mechanism of action

A

binds penicillin binding proteins (block transpeptidase activity), wider spectrum

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11
Q

Aminopenicillin use

A
select gram positive and negative bacteria, including:
H. influenzae
Listeria
Proteus
Salmonella
Enterococci
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12
Q

Aminopenicillin toxicity

A

hypersensitivity
ampicillin rash
pseudomembranous colitis

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13
Q

Antipseudomonal drugs

A

Ticarcillin
Piperacillin
Cerbenicillin

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14
Q

Antipseudomonal mechanism of action

A

binds penicillin binding proteins (block transpeptidase activity), wider spectrum

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15
Q

Antipseudomonal use

A

Pseudomonas and gram neg rods

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16
Q

Antipseudomonal toxicitiy

A

hypersensitivity rxn

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17
Q

Bacteriostatic antibiotics

A
Erythromycin
Clindamycin
Sulfamethoxazole
Trimethoprim
Tetracycline
Chloramphenicol
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18
Q

Bactericidal antibiotics

A
Vancomycin
Fluoroquinolones
Penicllin
Amnioglycosides
Cephalosporins
Metronidazole
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19
Q

1st generation cephalosporins

narrow spectrum

A

Cefazolin
Cephalexin

Cefadroxil
Cephaloridine
Cephalothin
Cephapirin
Cephradine
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20
Q

1st generation cephalosporin coverage

A

Gram positive cocci
Proteus
E. coli
Klebsiella

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21
Q

Cephalosporin mechanism of action

A

beta lactams
inhibit cell wall synthesis
less susceptible to penicillinases

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22
Q

2nd generation cephalosporins

expanded spectrum

A

Cefoxitin
Cefaclor
Cefuroxime

Cefamandole
Cefmetazole
Cefonicid
Cefotetan
Cefprozil
Loracarbef
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23
Q

2nd generation cephalosporin coverage

A
same as 1st gen. PLUS:
H. influenzae
Enterobacter
Neisseria
Serratia
(inc. gram neg coverage)
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24
Q

3rd generation cephalosporins

borad spectrum

A
Ceftriaxone
Ceftazidime
Cefotaxime
Cefdinir
Cefditoren
Cefpodoxime

Cefixime
Cefoperazone
Ceftibuten
Ceftizoxime

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25
Q

3rd generation cephalosporin coverage

A

serious gram neg. infections
Ceftriaxone: Neisseria
Ceftazidime: Pseudomonas

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26
Q

4th generation cephalosporins

A

Cefepime
Cefteroline

Cefpirome*
Ceftobiprole*
*not licensed for use in the US

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27
Q

cephalosporin toxicity

A
Hypersensitivity
Vitamin K deficiency
Cross-hypersensitivity w/ penicillins
Nephrotoxicity of aminoglycosides
rxn with alcohol
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28
Q

Monobactam

A

Aztreonam

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29
Q

Aztreonam mechanism

A

beta lactamase resistant monbactam

binds PBPs

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30
Q

Aztreonam use

A

Gram neg rods only

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31
Q

Aztreonam toxicity

A

occasional GI upset

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32
Q

Imipenem/Cilastatin mechanism

A

Beta lactamase resistant cerbapenem

Cilastatin is a renal dihydropeptidase 1 (to decrease renal inactivation)

33
Q

Imipenem coverage

A

Broad spectrum
Gram positive cocci
Gram neg rods
Anerobes

34
Q

Imipenem toxicity

A

GI distress
skin rash
CNS toxicity (seizures) at high levels

35
Q

Vancomycin mechanism of action

A

Binds to terminal D-Ala D-Ala of peptide side chain of peptidoglycan to inhibit cell wall synthesis

36
Q

Vancomycin coverage

A
Gram positives only
reserved for resistant infections
- S. aureus
- Enterococci
- C. diff
37
Q

Vancomycin toxicity

A

(well tolerated in general)
Nephrotoxicity
Ototoxicity
Red man syndrome (hypersensitivity)

38
Q

Mechanism of resistance to vancomycin

A

Bacteria changes terminal D-Ala D-Ala to D-Ala D-Lactate

39
Q

30s ribosomal inhibitors

A

Tetracyclins

Aminoglycosides

40
Q

50s ribosomal inhibitors

A
Clindamycin
Chloramphenicol
Erythromycin
Linezolid
Lincomycin
41
Q

Aminoglycosides

A
Gentamicin
Neomycin
Amikacin
Tobramycin
Streptomycin
42
Q

Mechanism of action of aminoglycosides

A

Bing to 30s ribosomal subunit to prevent protein synthesis

Requires O2 for uptakes

43
Q

Aminoglycoside use

A

No anaerobe coverage
Severe gram neg. rod infections
Synergistic with Beta-lactams
Neomycin for bowel suregery

44
Q

Aminoglycoside toxicity

A

Nephrotoxicity (esp. w/ cephalosporins)
Ototoxicity (esp. w/ loop diuretics (for hypertension))
Teratogen

45
Q

Mechanisms of aminoglycoside resistnace

A

Inactivating enzymes - phosphorylation, adenylation, acetylation
Methylation of 16s ribosomal RNA - high resistance to all aminoglycs
Efflux pumps

46
Q

Tetracyclin mechanism of action

A

Binds to 30s ribosomal RNA to block tRNA and inhibit protein synthesis

47
Q

Tetracyclins (drugs)

A

Tetracyclin
Doxycyclin
Tigecyclin (similar struct)

48
Q

Tetracyclin coverage

A

Most GPs and GNs, esp:

  • Brucella
  • B. bergdorferi
  • Chlamydia (intracel. accumulation)
  • H. pylori
  • Rikettsia
49
Q

Tetracyclin toxicicty

A

GI ditress
Teeth discoloration
Inhibited bone growth in children
Photosensitivity

50
Q

Tetracyclin administration considerations

A

Absorption inhibited by milk/antacids/iron preps

Can be used in pts w/ kidney failure (b/c poor urine conc)

51
Q

Mechanisms of resistance to tetracyclins

A

Ribosomal protection proteins
Efflux pumps
Reduced uptake

52
Q

Macrolide drugs

A

Erythromycin
Azithromycin
Clarithromycin

53
Q

Macrolide mechanism of action

A

Binds to 50s subunit of ribosome to inhibit translocation and protein synthesis

54
Q

Macrolide uses

A

Atypical pneumonias from mycoplasma, chlamydia, legionella
URIs
STDs
Gram pos cocci (in pts allergice to penicillin)
Neisseria

55
Q

Macrolide toxicity

A
(Generally very safe!)
Prolonged QT
GI discomfort
Hypersensitivity
Transient hearing loss
Acute cholestatic hepatitis
56
Q

Mechanism of resistance to macrolides

A

Methylation of the 50s ribosomal subunit (23s binding site) by the erm gene (for erythromycin)
Efflux pump encoded by the mef gene (low level resistance)

57
Q

Chloramphenicol mechanism of action

A

Binds to 50s ribosomal subunit, blicks tRNA

58
Q

Chloramphenicol use/coverage

A
Broad
Crosses BBB well - Meningitis (esp low income countries):
- H. flu
- Neisseria
- S. pneumo
59
Q

Chloramphenicol toxocity

A

Dose-related bone marrow suppression (resolves)

Rare but irreversible aplastic anemia (why not available in US)

60
Q

Clindamycin mechanism of action

A

Binds to 50s ribosomal subunit, inhibits RNA dependent protein synthesis (bacteriostatic)

61
Q

Clindamycin coverage

A

Excellent for anerobes esp aspiration pneumonia and lung abcesses
Reduces toxin production (S. pyogenes and S. aureus)

62
Q

Clindamycin toxicity

A

Pseudomembeanous colitis
Fever
Diarrhea

63
Q

Sulfonamide mechanism of action

A

Competitively inhibits PABA incorporation into folic acid (used in purine synthesis)

64
Q

Sulfonamide coverage

A

Broad spectrum Gram pos and Gram negs

Also opportunistic infection prophylaxis (in HIV pts)

65
Q

Sulfonamide toxicity

A
Hypersensitivity, Serum sickness
GI intolerance
Hemolysis in pts w/ G6PD
Nephrotoxicity
Photosensitivity
66
Q

Mechanism of resistance to sulfonamide

A

Decreased permeability
Decreased target enzyme affinity
Increased PBPA synthesis

67
Q

Trimethoprim mechanism of action

A

Inhibits dihydrofolate reductase, potentiating sulfonamide activity

68
Q

Trimethoprim coverage/use

A

used in combo with sulfamethoxazole for recurrent UTIs, Shigella, Salmonella, pneumocystis

69
Q

Trimethoprim toxicity

A

Bone marrow suppression (leucopenia, agranulocytosis, thrombocytopenia)

70
Q

Fluoroquinolone mechanism of action

A

Inhibits bacterial DNA gyrase (exhibits post-antibiotic effect, inc w/ longer exposure or higher dosage)

71
Q

Sulfonamide drugs

A

Sulfamethoxazole
Sulfisoxazole
Sulfadiazine

72
Q

1st generation fluoroquinolones

A

Naladixic acid

73
Q

2nd generation fluoroquinolones

A

Norfloxacin
Ciprofloxacin
Ofloxacin

74
Q

3rd generation fluoroquinolones

A

Levofloxacin

Moxifloxacin

75
Q

4th generation fluoroquinolones

A

Trovafloxacin (withdrawn)

76
Q

1st generation fluoroquinolone coverage

A

(Naladixic acid)
Good for gram negs. (not pseudomonas)
Indicated for uncomplicated UTIs

77
Q

2nd generation fluoroquinolone coverage

A
Gram negs (inc Pseudomonas), some gram pos (not pneumo)
Indicated for UTIS, STDs, skin/soft tissue infections
78
Q

3rd generation fluoroquinolone coverage

A

Like 2nd generation, but expanded gram pos coverage (inc pneumo)
Indicated for COPD, comm. acq. pneumonia, sinusitis
(not for GC b/c of high resistance)

79
Q

Fluoroquinolone toxicity

A

GI upset