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Pharm Block 3 > Antibacterials > Flashcards

Antibacterials Flashcards

(50 cards)

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1
Q

What are the types of cell wall agents?

A

beta-lactams, Vancomycin, Telavancin, Fosfomycin, Bacitracin*

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2
Q

What are the types of cell membrane agents?

A

Polymyxins, Cyclic Lipopetides

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3
Q

What are the types of nucleic acid agents?

A

Quinolones, Nitrofurans, Rifampin, Fidaxomicin, Metronidazole*

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4
Q

What are the types of proteins synthesis agents?

A

Aminoglycosides, Spectinomycin, Tetracyclines, Tigecycline, Chloamphenicol, Macolides, Clindamycin, Linezolid

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5
Q

What are the types of anti-folates?

A

Sulfonamides, Trimethoprim*

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6
Q

General properties of beta-lactams

A

usually bactericidal
effective against gram pos and neg
most effective against actively growing bacteria

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7
Q

Mechanism of action of beta-lactams

A

Inhibit transpeptidases by binding to PBP, which catalyze cell wall cross links
competitive, irreversible

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8
Q

What are the methods of bacterial resistance to beta-lactams

A
  • beta-lactamases
  • altered PBP
  • beta-lactam agent can’t reach PBP
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9
Q

What types of killers are beta-lactams

A

time-dependent

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10
Q

Examples of beta-lacatamase inhibitors

A

clavulanic acid, tazobactam

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11
Q

What is an example of a beta-lactam and some of its derivatives(?)

A
  • Penicillin
    • amoxicillin, ampicillin, Penicillin V, Penicillin G, piperacillin, ticarcillin, oxacillin*
  • Cephaolosporin
    • 1st gen: cefazolin, cephalexin
    • 2nd gen: cefuroxime, cefoxitin
    • 3rd gen: ceftriaxone, ceftazidime
    • 4th gen: cefepime*
  • Imipenem*
  • Azteronam*
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12
Q

What is special about oxacillin*

A

It is resistant to Staphylcoccal beta-lacatamase

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13
Q

Excretion/metabolism of penicillins

A 
~30% hepatic metabolism
mostly renal (20% glomerular filtration/80% tubular anionic excretion)
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14
Q

Adverse reactions of penicillins

A
  • allergic
    • anaphylaxis
    • rash
  • diarrhea, enterocolitis
  • elevated liver enzymes
  • hemolytic anemia
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15
Q

What is the mechanism of action of Vancomycin*

A
  • bactericidal
  • inhibits cell wall synthesis by binding to free carboxyl end (D-ala-D-ala) of the pentapeptide to interfere with transpeptidation and transglycosylation
  • could also disrupt cell membranes and inhibit RNA synthesis
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16
Q

When and how are vancomycin* used

A
  • IV for systemic infections
  • oral for C. diff enterocolitis
  • bactericidal
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17
Q

Excretion/metabolism for vancomycin*

A

active form excreted via glomerular filtration

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18
Q

Adverse reactions to vancomycin*

A
  • “red neck” syndrome
  • nephrotoxicity
  • phlebitis
  • ototoxicity
  • hypersensitivity, skin rashes, neutropenia
  • “pain and spasm” syndrome
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19
Q

Mechanism of action of Fosfomycin*

A

inhibits synthesis of peptidoglycan building blocks by inactivating enolpyuvyl transerase, an early-stage cell wall synthesis enzyme

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20
Q

What are Fosfomycin* used for

A

uncomplicated UTI caused by E. Coli enterococcus

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21
Q

Fosfomycin* toxicity

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A

headache, diarrhea, nausea, vaginitis

22
Q

Bacitracin* mechanism of action

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A

interferes w/ cell wall synthesis by interfering with lipid carrier that exports early cell wall components through the cell membrane

23
Q

How are bacitracin* used

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A

topical only, because very nephrotoxic against gram-positive cocci and bacilli

24
Q

Toxicity of bacitracin*

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A

allergic dermatitis

25
Polymyxins mechanism of action
act as cationic detergents that bind LPS in the outer membrane of gram-negatives
26
An example of a polymyxin and how it's used
- Polymyxin B* - topically, esp for Pseudomonas and other gram-negative infections - systemic use has potential for serious nephro and neuro toxicity
27
An example of a cyclic lipopeptides and its mechanism of action
- Daptomycin* | - binds to bacterial cytoplasmic membrane, causing rapid membrane depolarization
28
Side effects of Daptomycin*
nausea, diarrhea, GI flora alteration, muscle pain and weakness
29
Mechanism of action of Quinolones
Inhibit DNA gyrase (usually alpha subunit) to interfere with control of bacterial DNA winding
30
Type of killing by Quinolones
- Bactericidal | - dependent on AUC24hr/MIC
31
How is resistance to Quinolones achieved
- altered DNA gyrase | - combination of decreased permeability
32
What are the two kinds of quinolones
fluorinated and nonfluorinated
33
What are non fluorinated quinolones effective against
Enterobacteriaceae in urinary tract
34
What are examples of fluorinated quinolones
norfloxacin*, ciprofloxacin*, moxifloxacin*
35
Which quinolines are used for urinary tract infection?
norfloxacin*, ciprofloxacin*
36
What are some adverse reactions of quinolones
nausea, vomiting, abd pain, enterocolitis, peripheral neuropathy
37
How is the distribution of quinolines?
well-distributed, including the CSF
38
MAO of nitrofurans
nitroreductase converts them to reactive compounds which can damage DNA
39
Which nitrofuran is used for UTI
nitrofurantoin*
40
What are the uses for nitrofurans?
UTI and intestinal infections
41
Adverse reactions of nitrofurans
nausea, vomiting, diarrhea
42
MAO of rifampin*
inhibits bacterial RNA synthesis by binding RNA polymerase beta
43
What is rifampin* used for
- primarily for pulmonary tuberculosis | - also used for prophylaxis for meningococcal meningitis and Haemophilus influenza type b meningitis
44
Adverse reactions to rifampin*
- serious hepatotoxicity (<1%) - induces hepatic enzymes (many CYPs) that inactivate other drugs - orange color (urine, saliva, tears, sweat)
45
MAO of Fidaxomicin*
nonceompetitive inhibitor of RNA polymerase, which inhibits RNA synthesis
46
What is Fidaxomicin* used for
C. difficile infection (third line to metronidazole, vancomycin)
47
Excretion/metabolism of Fidaxomicin*
fecal elimination, some metabolism by intestinal cells
48
Adverse reaction of Fidaxomicin*
GI upset (4-10%), GI bleeding (4%), neutropenia (2%)
49
MAO of Metronidazole*
Multiple steps: 1. anaerobes reduce the nitro group of metronidazole* 2. resulting product disrupts DNA and inhibits nucleic acid synthesis
50
How does resistance to Metronidazole* occur
anaerobes lose ability to reduce nitro group of metronidazole*

Pharm Block 3 (10 decks)

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