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Antibacterial Agents Flashcards

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1
Q

Penicillins mechanism of action

A

Cell wall synthesis inhibitor (bactericidal)

  • inhibit cross-linking of peptidoglycan polymers at cell wall
  • Covalently binds penicillin binding proteins (PBPs)
  • Promotes lysis of bacteria
  • Effect persists due to covalent binding to bacterial proteins
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2
Q

Resistance to penicillins?

What resistance does MRSA vs. MSSA have?

A

1) B-lactamase: enzyme that hydrolyze B-lactams (penicillins, cephalosporins)
- MSSA → not broken down by B-lactamase
2) Alteration in PBPs (MRSA)

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3
Q

Penicillins have ______ excretion

A

renal

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4
Q

Types of Penicillins

A 
Penicillin G
Penicillin V
Penicillinase-resistant
Extended spectrum
Antipseudomonal
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5
Q

Penicillin V is administered _____ for ________

A

orally for mild-to-moderate infections

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6
Q

Dicloaxillin is a ….

A

penicillinase resistant penicillin

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7
Q

Amoxicillin and ampicillin are…

A

extended spectrum penicillins

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8
Q

Piperacillin is a _______ and typically administered _______ with _________

A

antipseudomonal penicillin

administered IV witha B-lactamase inhibitor

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9
Q

B-lactamase inhibitors

A

Clavulanate or tazobactam

used with amoxicillin/ampicillin and piperacillin

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10
Q

Adverse reactions associated with Penicillins (2)

A

1) Anaphylaxis, type I, RARE

2) rashes (common)

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11
Q

Ampicillin/Amoxicillin side effects and explain why

A

1) Extended spectrum but not effective against C.diff and others –> superinfections possible
2) diarrhea

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12
Q

Penicillin spectrum/uses (2)

A

1) Gram + cocci (staph, strep, entero - NOT MRSA or MSSA)

2) anaerobes (NOT c. dif or b. fragilis)

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13
Q

Dicloxacillin spectrum/uses (1)

A

Penicillinase resistant

1) Gram + cocci (MSSA, NOT MRSA)

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14
Q

Amoxicillin/Ampicillin spectrum/uses (3)

Amox/Clav spectrum / uses

A

Extended spectrum

1) Gram + cocci (NOT MRSA or MSSA)
2) Gram - rods (E.coli)
3) some anaerobes (NOT c.diff or bacteriodes)
- ——————————————
* *add B-lactamase inhibitor (clav)**

1) Gram + cocci including MSSA** (NOT MRSA)
2) Gram - rods (E.coli)
3) some anaerobes including B. fragilis** (NOT c.diff)

-more hydrophobic –> can penetrate gram-

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15
Q

Pipercillin + Tazo spectrum/uses

A

Antipseudomonal + B-lactamase inhibitor

1) Gram - rods (E.coli) AND Pseudomonas**
2) Gram + cocci (MSSA, NOT MRSA)
3) Anaerobes including B. Fragilis

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16
Q

Vancomycin mechanism of action

A

cell wall synthesis inhibitor

inhibits linear polymerization of subunits at cell membrane

-Binds directly to D-ala-D-ala

stage 2 inhibitor - other CW synthesis inhibitors are stage 3

–> NOT inactivated by B-lactamase****

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17
Q

Administration of Vancomycin

A

IV usually

poor oral absorption - only use oral for C.diff GI infection

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18
Q

Excretion of vancomycin

A

renal excretion

Possible renal toxicity

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19
Q

Adverse reactions of Vancomycin (3)

A

1) ototoxicity
2) renal toxicity - MONITOR CP LEVELS!
3) infusion related side effects (chills, fever, rash)

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20
Q

Spectrum/Uses of Vancomycin (2)

A

Narrow spectrum

1) Anaerobes - CDIFF
2) Gram + cocci - MRSA**

NOT EFFECTIVE AGAINST GRAM -

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21
Q

Cephalosporins mechanism of action

A

cell wall synthesis inhibition (bactericidal)

B-lactam antibiotic

  • stage 3 - inhibit cross-linking of peptidoglycan polymers at cell wall
  • NOT susceptible to penicillinase
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22
Q

If your patient has an immediate sensitivity to penicillin you definitely should NOT…

A

give them a cephalosporin

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23
Q

Cephalexin is a…

A

1st Generation Cephalosporin

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24
Q

Ceftriaxone is a ….

A

3rd Generation Cephalosporin

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25
Cephalosporins vs. Penicillins (3 differences)
1) Broader spectrum of action vs. gram-neg bacteria 2) Less susceptible to penicillinase (cephalosporinases are emerging) 3) Less cross-reactivity in penicillin sensitive patients
26
3rd generation cephalosporins (ceftriaxone) can penetrate...
THE CNS
27
Adverse reactions associated with 3rd gen cephalosporin (ceftriaxone)
superinfection possible -not effective against C.diff
28
Spectrum/uses for Cephalexin (3)
1) Gram + cocci (MSSA, not MRSA) 2) Gram - rods (E.coli) 3) some anaerobes (not c.diff or b. fragilis)
29
Spectrum/uses for Ceftriaxone (5)
1) Gram + cocci (MSSA, not MRSA) 2) Gram - rods (E.coli) 3) Gram - cocci (N. Gonorrhoeae) 4) moderate anti-pseusomonal 5) some anaerobes (not c.diff or b. fragilis)
30
Carbapenems mechanism of action
cell wall synthesis inhibition (bactericidal) - B-lactamase resistant - interact with PBPs responsible for cell wall elongation
31
Carbapenems are administered...
IV/IM only
32
Carbapenems are excreted...
renally
33
Spectrum of carbapenems
WIDE spectrum -reserve for multidrug resistant organisms
34
Strep. pneumoniae, strep viridans, N. gonorrhoeae all carry __________ that cause resistance to penicillins
Altered penicillin binding proteins (PBPs)
35
Oral formulations of Vancomycin will work for _______ because IV formulations _________
C. diff will not get into the gut
36
Macrolides mechanism of action
protein synthesis inhibition 50S bacteriostatic
37
Macrolides include ______, _________, and ________
Erythromycin Azithromycin Clarithromycin
38
Macrolides are all excreted...
NON-RENALLY Erythromycin --> liver metabolism Azithromycin --> Biliary Clarithromycin --> metabolized to active metabolite
39
Resistance to macrolides can occur via...
methylation of 50S subunit | altered target --> resistance
40
Macrolides are administered...
orally (also IV)
41
Adverse reactions associated with Macrolides (2)
1) GI disturbances (N/V/D) | 2) Inhibits CYP450** --> drug-drug interactions
42
Spectrum/Uses of Macrolides (Erythromycin, Azithromycin, Clarithromycin) (3)
Extended spectrum 1) Gram + cocci (MSSA, NOT MRSA) 2) Gram - diplococci (N. Gonorrhoeae) 3) Atypical (Chlamydia, Mycoplasma) NOT gram - rods or anaerobes (NO ecoli, pseudomonas, c diff)
43
Mechanism of action of tetracyclines
protein synthesis inhibitor 30S Bacteriostatic
44
Tetracyclines include ________ and ________
Doxycycline and Minocycline
45
Resistance can occur to tetracyclines via...
changes in drug transport out of the cell
46
Doxycycline is excreted _________ and tetracycline is excreted _________
non-renally (biliary) renally
47
Administration of doxy and tetracycline
oral
48
Adverse effects of tetracycline and doxy (4)
1. Abnormal bone/tooth development 2. Fungal superinfection 3. Drug-Drug interaction with metal cations (antacids, iron supplements, milk) 4. GI
49
Spectrum/uses for tetracyclines (5)
BROAD spectrum (lots of resistance now though) 1) Gram + cocci - MRSA! 2) Gram - diplococci (N. Gonorrhoeae) 3) Gram - rods (E. coli) 4) Atypical - Chlamydia, Mycoplasma 5) Anaerobes - B. Fragilis (NOT c.diff) NOT pseudomonas, NOT c diff
50
Clindamycin mechanism of action
protein synthesis inhibition 50S bacteriostatic
51
Clindamycin is administered...
orally
52
Clindamycin is excreted...
non-renally Hepatobiliary elimination
53
Clindamycin can penetrate...
BONE
54
Adverse reactions to Clindamycin
1) severe diarrhea | 2) Pseudomembranous colitis (C.diff)
55
Spectrum/Uses of Clindamycin (2)
NARROW spectrum 1) Gram + cocci (MRSA!) 2) Anaerobes - B. Fragilis (NOT c.diff) NOT gram- rods, Gonorrhea, c.diff, chlamydia, or mycoplasma
56
Aminoglycoside mechanism of action
Protein synthesis inhibition 30S BACTERICIDAL** - binds irreversible
57
Administration of aminoglycoside
Dose once a day IV/IM - poor oral absorption
58
Aminoglycosides includes _______, ________, ________, and ________
Tobramycin Gentamicin Neomycin Streptomycin
59
Aminoglycosides are excreted...
renally
60
Aminoglycosides preferentially accumulate where?
kidney and inner ear --> ototoxicity, and renal toxicity
61
Adverse reactions associated with aminoglycosides
1) vestibular and auditory toxicity | 2) Nephrotoxicity - MONITOR CP LEVELS
62
for _______ and _______ you must routinely monitor CP levels due to possible renal toxicity
Aminoglycosides (neomycin, streptomycin) Vancomycin
63
Spectrum of aminoglycosides (1)
Narrow Spectrum 1) Gram - aerobes (e.coli, pseudomonas) NO super infections b/c narrow spectrum
64
What can be used to treat MRSA (3)
1) Vancomycin 2) Tetracyclines 3) Clindamycin
65
What can be used to treat N. Gonnorrhoeae? (3)
1) Ceftriaxone 2) Macrolides 3) Tetracyclines
66
What can be used to treat c. diff? (2)
1) Vancomycin | 2) Metronidazole
67
What can be used to treat chlamydia? (2)
1) Macrolides | 2) Tetracyclines
68
Aminoglycosides will sometimes be used synergystically with _______ or ______ in treatment of _________
penicillin or ampicillin Enterococcal By themselves aminoglycosides do NOT have activity against enterococcal isolates
69
Erythromycin is given ______ x a day Azithromycin is given ______ x a day Clarithromycin is given ______ x a day
4x a day 1x a day 2x a day
70
Fluoroquinolones include ________, _________ and __________
Ciprofloxacin, Levofloxacin, Moxifloxacin
71
Mechanism of action of fluoroquinolones
inhibit DNA gyrase | BACTERICIDAL
72
Resistance to Fluoroquinolones due to...
due to point mutations in binding site on DNA gyrase or changes in drug permeability into organism
73
Administration of fluoroquinolones
oral (or IV)
74
Adverse reactions associated with fluoroquinolones? (6)
1) N/V/D 2) Superinfections with CDIFF possible 3) Drug-Drug interactions - CYP450 inhibitor*** 4) NOT first choice in children less than 12 yrs (arthralgias possible) 5) QT prolongation 6) rashes
75
What Drug-Drug interactions occur with fluoroquinolones?
Drug-Drug interactions with theophylline and antacid Antacids reduce oral absorption of cipro
76
Spectrum of ciprofloxacin
1) Gram - rods (psuedomonas) 2) Atypical (chlamydia, mycoplasma) Uncomplicated-complicated UTIs** Traveler’s diarrhea
77
Spectrum of Levofloxacin
1) gram - rods (including pseudomonas) 2) atypical (chlamydia, and mycoplasma) 3) AND gram + cocci (streps only) Good for UTI and respiratory
78
Spectrum of Moxifloxacin
1) atypical (chlamydia, and mycoplasma) 2) gram + cocci (streps only) 3) some anaerobes Good for respiratory
79
Nitrofurantoin mechanism of action
reduced in cell to intermediates that damage bacterial DNA → BACTERICIDAL -CANNOT be used for treatment of systemic infections - only UTI
80
Administration and excretion of Nitrofurantoin
Oral admin with RAPID renal excretion --> urinary antiseptic
81
Adverse reactions of Nitrofurantoin (1)
1) GI side effects
82
Spectrum of Nitrofurantoin (1)
1st line agent in uncomplicated UTIs 1) ONLY gram- rods (can’t treat atypical)
83
Metronidazole mechanism of action
- Reduced intracellularly to active form → interfere with DNA function - Radical formation → target DNA - Only good against anaerobes - BACTERICIDAL
84
Administration and excretion of Metronidazole
Oral therapy Hepatic metabolism
85
Spectrum of Metronidazole (2)
1) Anaerobes (C. Diff, B. Fragilis) | 2) Protozoa
86
Adverse drug reactions of Metronidazole
1) Nausea, headache 2) Antabuse-like reaction (drug to tx alcoholism) 3) occasional candidal superinfections
87
Why does Metronidazole have antabuse-like reactions?
Inhibits aldehyde dehydrogenase → antabuse-like effect if alcohol is consumed within 3 days of metronidazole Antabuse → GI upset, vomiting, headache - used in alcohol tx
88
Sulfonamides mechanism of action
Inhibits folate metabolism (dihydropteroate synthetase - only in bacteria) → interfere with DNA synthesis BACTERIOSTATIC alone and BACTERICIDAL in combo (SMX/TMP)
89
SMX/TMP
inhibit two sequential enzymatic processes involved in tetrahydrofolic acid biosynthesis - Trimethoprim - NOT a sulfonamide - Sulfamethoxazole
90
Administration and Excretion of Sulfonamides
oral therapy renal excretion AND hepatic excretion
91
Adverse reactions of sulfonamides
1) Hypersensitivity skin reactions 2) Kernicterus in neonates** 3) Renal crystalluria (rare) via decrease in water solubility of metabolites
92
You should NEVER give sulfonamides to who?
neonates! --> Kernicterus due to bili build up
93
Spectrum of TMP/SMX (3)
1) Gram + cocci (including MRSA) 2) gram - rods (e. coli) 3) atypical (chlamydia)

Disease and Defense (11 decks)

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