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Overview of Antimicrobial Agents Flashcards

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1
Q

Natural Penicillins

A

Penicillin G(IV, IM)

Penicillin V (PO)

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2
Q

Anti-staphylococcal Penicillins

A

Oxacillin(IV, IM)
Dicloxacillin(PO)
Nafcillin (IV, IM)

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3
Q

Aminopenicillins*

A

Ampicillin(PO, IV, IM)

Amoxicillin(PO)

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4
Q

Anti-pseudomonalPenicillins

A

Piperacillin (IV)

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5
Q

First Generation Cephalosporins

A

Cefazolin(IV, IM)

Cephalexin [Keflex] (PO)

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6
Q

Second Generation Cephalosporins

A

Cefoxitin(IV)

Cefuroxime (PO, IV, IM)

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7
Q

Third Generation Cephalosporins*

A

Ceftriaxone[Rocephin] (IV, IM)

Ceftazidime(IV, IM)

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8
Q

Fourth Generation Cephalosporins*

A

Cefepime(IV, IM)

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9
Q

Carbapenems

A

Imipenem/cilastatin (IV)
Meropenem(IV)*
Ertapenem(IV, IM)*

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10
Q

Monobactams

A

Aztreonam (IV, IM, INH)

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11
Q

B-lactamase Inhibitors*

A

Ampicillin-sulbactam(IV)
Amoxicillin-clavulanic acid [Augmentin] (PO)
Piperacillin-tazobactam(IV)

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12
Q

Glycopeptides*

A

Vancomycin(PO, IV)

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13
Q

Lipopeptides

A

Daptomycin(IV)

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14
Q

Fluoroquinolones

A

Ciprofloxacin [Cipro] (PO, IV, topical)
Levofloxacin(PO, IV, topical)*
Moxifloxacin (PO, IV, topical)

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15
Q

Aminoglycosides

A

Tobramycin (IV, IM, INH, topical)

Gentamicin(IV, IM, topical)*

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16
Q

Tetracyclines/Glycylcyclines

A

Minocycline (PO, IV)

Doxycycline(PO, IV)*

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17
Q

Macrolides/Ketolides

A

Clarithromycin (PO)

Azithromycin[Zithromax, Z-pak] (PO, IV, topical)*

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18
Q

Lincosamides*

A

Clindamycin[Cleocin] (PO, IV, IM, topical)

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19
Q

Metronidazole

A

Flagyl

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20
Q

Sulfonamides/Trimethoprim

A

Sulfamethoxazole/trimethoprim (PO, IV)

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21
Q

Most common categories

A

penicillins and macrolides

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22
Q

Top 5 drugs:

A 
Azithromycin
Amoxicillin
Amoxicillin-clavulanate
Ciprofloxacin
Cephalexin
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23
Q

Ask yourself whether an antimicrobial agent is warranted:

A

Is an antimicrobial indicated based on clinical findings?
Have appropriate cultures been obtained?
What is the most likely causative organism?
What must be done to prevent secondary exposure?
Is there clinical evidence or established guidelinesthat have determined antimicrobial therapy provides a clinical benefit?

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24
Q

prophylaxis

A

no infection

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25
pre-emptive
infection
26
empiric
symptoms
27
definitive
pathogen isolated
28
suppression
resolution
29
A 37 yofemale with a history of end-stage renal disease, on dialysis, is admitted to the hospital with healthcare-associated pneumonia. Antibiotics are initiated to cover the most likely pathogen(s).
empiric
30
A 68 yomale presents for a total hip replacement. Prior to surgery, he is given one dose of cefazolin to prevent development of a surgical wound infection
prophylaxis
31
A 37 yofemale with a history of end-stage renal disease, on dialysis, is admitted to the hospital with healthcare-associated pneumonia. Cultures result with sensitive Pseudomonas, vancomycin is discontinued
definitive
32
An 8 yomale presents to the ED with a perforated appendix. Antibiotics are initiated pre-operatively to reduce risk of intra-abdominal abscess & wound infection
pre-emptive
33
A 75 yomale presents to his PCP for follow-up of prosthetic hip joint infection. He receives continued low dose antimicrobial therapy. Hip prosthesis was unable to be removed and replaced during hospitalization.
suppressive
34
Gram Positive cocci anaerobic
peptococcus | peptostreptococcus
35
Gram Positive cocci aerobic clusters coagulase positie
staph aureas
36
Gram Positive coccie aerobic clusters coagulase negative
``` staph epi staph saprophyticus staph hominis staph hemolyticus staph warneri ```
37
Gram Positive cocci aerobic diplococci
streptococcus pneumonia entrococcus
38
Gram Positive cocci aerobic chains b hemolytic
strep pyogenes group a strep agalectiae group b strep groups cfg
39
Gram Positive cocci aerobic chains a hemolytic
viridans strep | strep pneumonia
40
Gram Positive bacilli anaerobic
``` c diff clostridium perfringens actinomyces lactobacillus ```
41
Gram Positive bacilli aerobic
bacillus anthracis nocardia listeria acynebacterium jelkelium
42
Gram Negative bacilli anaerobic
prevotella fusobacterium bacteroides
43
Gram Negative bacilli aerobic lactose fermenting oxidase positive
aeromonas pasteurella vibrio
44
Gram Negative bacilli aerobic lactose fermenting oxidase negative
ecoli klebsiella enterobacter citrobacter
45
Gram Negative bacilli aerobic non lactose fermenting oxidase postiive
``` pseudomonas flavobacterium aitaligenes achromobacter moraxella ```
46
Gram Negative bacilli aerobic non lactose fermenting oxidase negative
``` proteus proficendia serrates morganella slamonella shigella strenotrophomonas acinetobacter ```
47
Gram Negative bacilli aerobic misc
``` brucella bordetella campylobacter pasteurella vibrio ```
48
Gram Negative cocci
Neisseria meningitides neisseriia gonohorrhoaea vellionella
49
Gram Negative coccbacilli
h influenza | Moraxella catarrhalis
50
Susceptible:
Likely to inhibit pathogenic microorganism
51
Intermediate:
May be effective at higher dosage, more frequent administration, or in specific body site
52
Resistant:
Not effective at inhibiting growth of microorganism
53
Minimum inhibitory concentration (MIC):
lowest concentration of drug required to inhibit growth | Breakpoints established by Clinical and Laboratory Standards Institute (CLSI)
54
Clinical and Laboratory Standards Institute (CLSI) Breakpoints MIC (μg/mL
Susceptible ≤ 4 Intermediate 8-16 Resistant ≥ 32
55
Clinical and Laboratory Standards Institute (CLSI) Breakpoints Zone Diameter (mm)
Susceptible ≥ 20 Intermediate 15-19 Resistant ≤ 14
56
Zone Diameter (mm)
Act on a single or a limited group of microorganisms
57
Extended-spectrum
Active against gram-positive bacteria but also against significant number of gram-negative bacteria
58
Broad-spectrum
Act on a wide variety of bacterial species, including both gram-positive and gram-negative
59
Bacteriostatic:
arrests growth and replication of bacteria (limits spread of infection)
60
Bactericidal:
kills bacterial  Concentration-dependent killing: rate and extent of killing increase with increasing drug concentrations Time-dependent killing: activity continues as long as serum concentration above minimum bactericidal concentration
61
Bacteriostatic vs. Bactericidal | This concept is relative
Certain drugs are –cidalagainst specific bacteria while –static against others
62
Drug-drug enhancement or synergism
Gentamicin –ineffective against enterococci in the absence of a cell-wall inhibitor Combining penicillin with gentamicin leads to bactericidal activity
63
Antimicrobials classified based on
Class and spectrum of microorganisms it kills Biochemical pathway it interferes with Chemical structure
64
Site of Antibacterial Action cell wall synthesis
``` cycloserine vancomycin bacitracin fosfomycin penicillins cephalosporins monbactams carbapenems ```
65
Site of Antibacterial Action folic aid metabolism
Bactrim both paba
66
Site of Antibacterial Action cell membrane
polymyxins
67
Site of Antibacterial Action dna replication (dna gyrase)
nalidixic acid | quinolones
68
Site of Antibacterial Action dna dependent rna polymerase
rifampin
69
Site of Antibacterial Action protein synthesis (50 S)
erythromycin chloramphenicol clindamycin
70
Site of Antibacterial Action protein synthesis (30S)
``` tetracyclin spectinomycin streptomycin gentamicin tobramycin amikacin ```
71
Site of Antibacterial Action
``` Cell wall synthesis Cell membrane synthesis Protein synthesis Nucleic acid metabolism Function of topoisomerases Folate synthesis ```
72
cell wall inihbitors blactams
penicillins cephalosporins 1-4th gnereations carbapenems monobactams
73
cell wall inihbitors other antibiotics
bacitracin vancomycin daptomycin
74
cell wall inihbitors blactamase inhibitors
clavulanic acid sulbactam tazobactam
75
β-Lactam Mechanism of Action
Time-dependent; structural analogs of D-Ala-D-Ala; covalently bind penicillin-binding proteins (PBPs), inhibit the last transpeptidation step in cell wall synthesis
76
β-Lactamase Inhibitors
Amoxicillin + clavulanic acid, ticarcillin + clavulanic acid, ampicillin + sulbactam, piperacillin + tazobactam  MOA: prevent destruction of B-lactam antibiotics
77
Fluoroquinolone Mechanism of Action
Concentration-dependent, targets bacterial DNA gyrase& topoisomerase IV. Prevents relaxation of positive supercoils
78
Inhibitors of Protein Synthesis
Formation of initiation complex Amino-acid incorporation Formation of peptide bond Translocation
79
Aminoglycosides moa
blocks initiation of protein synthesis blocks further translation and elicits premature termination incorporation of incorrect amino acid
80
Tetracyclines moa
binds 30 s and block the a site
81
Macrolides moa
bind 50s they inhibit translocation
82
Sulfonamides and Trimethoprim moa
Inhibit folic acid synthesis; block sequential steps in pathway. pcp pneumonia block sequential steps in folic acid production
83
Β-Lactams | MOA
structural analogs of D-Ala-D-Ala; covalently bind penicillin-binding proteins (PBPs), inhibit transpeptidation
84
Β-Lactams | resistance
Structural difference in PBPs Decreased PBP affinity Inability for drug to reach site of action (i.e. gram-negative organisms) Active efflux pumps Drug destruction/inactivation by B-lactamases
85
Natural Penicillins drugs
Penicillin G (IV, IM), penicillin V (PO)
86
Natural Penicillins spectrum
highly effective against gram-positive cocci (GPC) but easily hydrolyzed by penicillinase
87
Natural Penicillins therapeutic use
narrow-spectrum, Streptococcus pneumoniaepneumonia and meningitis. Penicillin V for Streptococcus pyogenespharyngitis, toxic shock, viridians streptococci endocarditis if susceptible, syphilis
88
Anti-Staphylococcal Penicillins drugs
Oxacillin (IV, IM), dicloxacillin (PO), nafcillin (IV, IM)
89
Anti-Staphylococcal Penicillins spectrum
penicillinase resistant; agents of first choice for Staphylococcus aureus(MSSA) and Staphylococcus epidermidis(MSSE) that are not methicillin resistant
90
Anti-Staphylococcal Penicillins therapeutic use
estricted to infections with known Staphylococcussensitivity
91
Aminopenicillins drugs*
Ampicillin(PO, IV, IM), amoxicillin(PO)
92
Aminopenicillins spectrum*
extended-spectrum; extends beyond gram-positive to gram-negative (Haemophilus influenzae, Escherichia coli, Proteus mirabilis), Listeria monocytogenes, susceptible meningococci, enterococci
93
Aminopenicillins therapeutic use*
upper respiratory tract infections (S. pyogenes, S. pneumoniae, H. influenzae), sinusitis, otitis media, enterococcalinfections
94
Anti-PseudomonalPenicillins drugs
Ticarcillin(IV), piperacillin(IV)*
95
Anti-PseudomonalPenicillins spectrum*
Spectrum: extends spectrum to Pseudomonas aeruginosa, Enterobacter, and Proteusspp.
96
Anti-PseudomonalPenicillins therapeutic use*
serious gram-negative infections, hospital acquired pneumonia (HAP), immunocompromised patients, bacteremia, burn infections, UTI
97
Penicillins | Adverse effects:
Allergic reactions (0.7-10%) Anaphylaxis (0.004-0.04%) Nausea, vomiting, mild to severe diarrhea Pseudomembranous colitis
98
1st-Generation Cephalosporins drugs
Cefazolin(IV, IM), cephalexin (PO)
99
1st-Generation Cephalosporins spectum
good gram-positive coverage, modest gram-negative (covers Moraxella, E. coli, Klebsiellapneumoniae, P. mirabilis), orally active anaerobes
100
1st-Generation Cephalosporins therapeutic use
skin and soft tissue infections (SSTIs), surgical prophylaxis
101
2nd-Generation Cephalosporins drugs
Cefoxitin (IV), cefuroxime (PO, IV, IM)
102
2nd-Generation Cephalosporins spectrum
somewhat increased activity against gram-negative, but less active than 3rd-generation. Subset active against Bacteroidesfragilis
103
2nd-Generation Cephalosporins therapeutic use
used in gram-negative mixed anaerobic (intra-abdominal infections, pelvic inflammatory disease, diabetic foot infections)
104
3rd-Generation Cephalosporins drugs*
Ceftriaxone(IV, IM), ceftazidime(IV, IM)
105
3rd-Generation Cephalosporins spectrum*
less active against gram-positive, more active against Enterobacteriaceae(although resistance increasing due to B-lactamase producing strains)
106
3rd-Generation Cephalosporins therapeutic use*
serious gram-negative infections (Klebsiella, Proteus, Providencia, Serratia, Haemophilus), ceftriaxone DOC for all forms of gonorrhea & severe Lyme’s disease; meningitis. Ceftazidimecovers Pseudomonas
107
4th-Generation Cephalosporin drugs*
Cefepime(IV, IM)
108
4th-Generation Cephalosporin spectrum*
extends beyond 3rd-generation, useful in serious infections in hospitalized patients. Effective against Pseudomonas
109
4th-Generation Cephalosporin therapeutic use*
empirical treatment of nosocomial infections
110
Cephalosporins | Adverse effects:
1% risk of cross-reactivity to penicillins | Diarrhea
111
Carbapenems drugs*
Imipenem/cilastatin (IV), meropenem(IV), ertapenem(IV, IM)
112
Carbapenems spectrum*
aerobes & anaerobes; gram-positive, Enterobacteriaceae, Pseudomonas, Acinetobacter.Stenotrophomonasmaltophiliais resistant.
113
Carbapenems therapeutic use
UTI, lower respiratory tract infection (LRTI), intra-abdominal, gynecological, SSTI, bone and joint infections
114
Carbapenems adverse effects*
Nausea/vomiting (1-20%), seizures (1.5%), hypersensitivity
115
Monobactam drugs
Aztreonam (IV, IM, INH)
116
Monobactam spectrum
activity against gram-negative (Enterobacteriaceae, Pseudomonas, H. influenzae, gonococci), no activity against GPC or anaerobes
117
Monobactam therapeutic use
patients who are allergic to B-lactams appear not to react to aztreonam > effective for gram-negative infections which would usually be treated with B-lactam
118
Glycopeptides drugs
Vancomycin (PO, IV)
119
Glycopeptides moa
inhibits cell wall synthesis binding with high affinity to D-Ala-D-Ala terminal of cell wall precursor units.
120
Glycopeptides resistance
alteration of D-Ala-D-Ala target to D-alanyl-D-lactate or D-alanyl-D-serine which binds glycopeptides poorly. Intermediate resistance may also occur
121
Glycopeptides spectrum
broad gram-positive coverage –S. aureus(including MRSA), S. epidermidis(including MRSE), Streptococci, Bacillus, Corynebacterium spp., Actinomyces, Clostridium
122
Glycopeptides therapeutic use
osteomyelitis, endocarditis, MRSA, Streptococcus, enterococci, CNS infections, bacteremia, orallyfor C. difficile
123
Glycopeptides adverse effects
Macular skin rash, chills, fever, rash Red-man syndrome (histamine release): extreme flushing, tachycardia, hypotension Ototoxicity, nephrotoxicity (33% with initial trough > 20 mcg/mL)
124
Fluoroquinolones moa
concentration-dependent; targets bacterial DNA gyrase & topoisomerase IV.
125
Fluoroquinolones spectrum
E. coli, Salmonella, Shigella, Enterobacter, Campylobacter, Neisseria, Pseudomonas aeruginosa, S. aureus(not MRSA), limited coverage of Streptococcusspp.  *Levofloxacin, moxifloxacin, “respiratory fluoroquinolones” cover Streptococcusspp.
126
Fluoroquinolones therapeutic use
UTI, prostatitis, STI (chlamydia, Neisseria gonorrhoeae), traveler’s diarrhea, shigellosis, bone, joint, SSTI infections, diabetic foot infections
127
Fluoroquinolones | Adverse effects:
GI 3-17% (mild nausea, vomiting, abdominal discomfort) CNS 0.9-11% (mild headache, dizziness, delirium, rare hallucinations) Rash, photosensitivity, Achilles tendon rupture (CI in children)
128
Aminoglycosides drugs*
Tobramycin (IV, IM, INH, topical), gentamicin(IV, IM, topical)*
129
Aminoglycosides moa*
concentration-dependent; binds 30S ribosomal subunit, disrupts normal cycle of ribosomal function
130
Aminoglycosides spectrum*
aerobic gram-negative bacteria, limited action against gram-positive, synergistic bactericidal effects in gram-positive with cell wall active agent
131
Aminoglycosides therapeutic use*
UTI (not uncomplicated), used if resistance to other agents, seriously ill patients, pneumonia (infective against S. pneumoniaeand anaerobes), HAP, peritonitis, synergy in bacterial endocarditis, tobramycin inhalation in CF
132
Aminoglycosides adverse effects*
Ototoxicity (may be as high as 25%) Nephrotoxicity (8-26%) Neuromuscular block and apnea
133
Tetracyclines/Glycylcyclines drugs*
Minocycline (PO, IV), doxycycline(PO, IV)*, tigecycline(IV)
134
Tetracyclines/Glycylcyclines moa*
bacteriostatic; binds 30S bacterial ribosome. Prevents access of aminoacyl tRNAto acceptor (A) site on mRNA ribosome complex
135
Tetracyclines/Glycylcyclines spectrum*
wide range of aerobic/anaerobic gram-positive and -negative activity; effective for: Rickettsia, Coxiellaburnetii, Mycoplasma pneumoniae, Chlamydiaspp, Legionella, atypical mycobacterium, Plasmodium, Borreliaburgdorferi(Lyme’s disease), Treponema pallidum(syphilis)
136
Tetracyclines/Glycylcyclines therapeutic use*
CAP, atypical CAP coverage, community acquired SSTIs, community acquired MRSA, acne, Rickettsialinfections (Rocky Mountain Spotted Fever), Q fever, anthrax
137
Tetracyclines/Glycylcyclines adverse effects*
``` GI (epigastric burning, nausea, vomiting, diarrhea) Superinfections of C. difficile Photosensitivity Teeth discoloration Thrombophlebitis ```
138
Macrolides/Ketolides drugs*
Clarithromycin (PO), azithromycin(PO, IV, topical)*
139
Macrolides/Ketolides moa*
bacteriostatic; binds reversibly to 50S ribosomal subunit, inhibits translocation
140
Macrolides/Ketolides therapeutic use*
respiratory tract infections (spectrum S. pneumoniae, H. influenzae, and atypicals: Mycoplasma, Chalmydophilia, Legionella), alternative for otitis media, sinusitis, bronchitis, and SSTIs. Pertussis, gastroenteritis, H. pylori, Mycobacterial infections
141
Macrolides/Ketolides adverse effects*
GI (epigastric distress) Hepatotoxicity Arrhythmia QT prolongation
142
Macrolides/Ketolides drug interaction*
CYP3A4 inhibition –prolongs effects of digoxin, warfarin….
143
Lincosamides drugs*
Clindamycin(PO, IV, IM, topical)
144
Lincosamides moa*
binds 50S subunit of bacterial ribosome, suppresses protein synthesis
145
Lincosamides spectrum*
pneumococci, S. pyogenes, viridansStreptococci, MSSA, anaerobes (B. fragilis)
146
Lincosamides therapeutic use*
SSTIs, necrotizing SSTIs, lung abscesses, anaerobic lung and pleural space infections, topically for acne vulgaris
147
Lincosamides adverse effects*
``` GI diarrhea (2-20%) Pseudomembranous colitis (0.01-10%)  Due to C. difficile Skin rashes (10%) Reversible increase in aminotransferase activity May potentiate neuromuscular blockade ```
148
Oxazolidinones drug*
Linezolid(PO, IV)
149
Oxazolidinones moa*
inhibits protein synthesis binding P site of 50S ribosomal subunit, prevents formation of initiation complexes
150
Oxazolidinones spectum
gram-positive Staphylococcus(MSSA, MRSA, VRSA), Streptococcus(penicillin resistant S. pneumoniae), enterococci (VRE), gram-positive anaerobic cocci, gram-positive rods (Corynebacterium, L. monocytogenes)
151
Oxazolidinones therapeutic use*
VRE faecium(SSTI, UTI, bacteremia), nosocomial pneumonia caused by MSSA and MRSA, CAP, complicated/uncomplicated SSTI infections
152
Oxazolidinones adverse effects*
Myelosuppression [thrombocytopenia (2.4%),anemia, leukopenia] Headache Rash
153
Oxazolidinones drug interactions*
weak, nonspecific inhibitor of monoamine oxidase
154
no novel antimocrobial moa since
1987
155
azithromycin used mostly for
cap
156
amoxicillin used mostly for
upper resp tract otitis media
157
teichoic acid
stabilized peptidoglycin
158
lps
it is hydrophobic and is toxic called endotoxin when released can cause shock
159
concentration dependant killing drugs
aminoglycosides and fluoroquinolones
160
time dependent killing drugs
b lactams and vancomycins cell wall inhibitors
161
bacteriostatic are usually
protein synthesis inhibitors
162
cd dependant dosing
qd
163
time dependant dosing
require frequent dosing to make sure we have enough over a certain amount of time
164
enterococci are
gram pos
165
fq extra
normal gyrase prevents this so they inhibit this and it is not allowed to reform the dna strands that have been cleaved already and it is released and damaged
166
Aminoglycosides
bacterialcidial bind 30s
167
Tetracyclines
binds 30 s and block the a site
168
Macrolides
bind 50s they inhibit translocation
169
bind 50s they inhibit translocation extra
pcp pneumonia block sequential steps in folic acid production
170
2nd-Generation Cephalosporins used for
aspiration related mbc of mixed anaerobic
171
Ceftriaxone has no
pseudomonal coverage
172
ceftazidimehas good
psuedomonal coverage
173
Carbapenems save for
save for last line more serious infections if there is another drug that would work serious resistant infecction
174
carbapenams must be stopped with
renal problems
175
use linezolid if resistant to
vancomycin
176
Red-man syndrome (histamine release): extreme flushing, tachycardia, hypotension
direct toxic effect on mass cells, not an allergy
177
fq spectrum
broad gram neg
178
Fluoroquinolones ci
chondorocyte damage pregnancy breast feeding and children it is ci
179
ag don't target
anaerobes bc they require o2 to get into the cell
180
tetracyclines cover
atypicals
181
lincosamide coverage
good gram positive and anaerobes aspiration pneumonia
182
Oxazolidinones di
serotonin syndrome cant give with ssri

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