Antibiotics - Classes Flashcards
1
Q
What class?
What is the mechanism?
Useful for what types of bacteria?
“TETRACYCLINE”
A
1) Class: TETRACYCINE
2) Mechanism: binds 30S; prevents tRNA binding
3) Bacteria: BROAD SPECTRUM
Note: Not used widely due to common resistance (by EFFLUX PUMPs and some ribosomal 30S modification)
2
Q
What class?
What is the mechanism?
Useful for what types of bacteria?
“TETRACYCLINE”
A
1) Class: TETRACYCINE
2) Mechanism: binds 30S; prevents tRNA binding
3) Bacteria: broad spectrum
Note: Not used widely due to common resistance (by EFFLUX PUMPs and some ribosomal 30S modification)
3
Q
What class?
What is the mechanism?
Useful for what types of bacteria?
“DOXYCYCLINE”
A
1) Class: TETRACYCINE
2) Mechanism: binds 30S; prevents tRNA binding
3) Bacteria: broad spectrum
Note: Not used widely due to common resistance (by EFFLUX PUMPs and some ribosomal 30S modification)
4
Q
What class?
What is the mechanism?
Useful for what types of bacteria?
“MINOCYCLINE”
A
1) Class: TETRACYCINE
2) Mechanism: binds 30S; prevents tRNA binding
3) Bacteria: broad spectrum
Note: Not used widely due to common resistance (by EFFLUX PUMPs and some ribosomal 30S modification)
5
Q
What class?
What is the mechanism?
Useful for what types of bacteria?
“TIGECYCLINE”
A
1) Class: TETRACYCINE
2) Mechanism: binds 30S; prevents tRNA binding
3) Bacteria: broad spectrum
Note: Not used widely due to common resistance (by EFFLUX PUMPs and some ribosomal 30S modification)
6
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7
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10
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11
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12
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13
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14
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15
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16
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17
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18
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19
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20
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21
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22
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23
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34
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35
What class?
What is the mechanism?
Useful for what types of bacteria?
1) Class:
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3) Bacteria:
36
What are the antibiotics of the Tetracyclines?
1) Tigecycline
2) Tetracycline
3) Minocycline
4) Doxycline
"TTMD" = Tetracycline
37
What is the mechanism of action of the Tetracyclines?
protein inhibitor = 30S
binds to 30S of bacterial ribosome and prevents aminoacyl-tRNA binding (i.e. prevents initiation)
38
What are the antibiotics of the Aminoglycosides?
1) TOBRAmycin
2) AMIKACIN
3) GENTAmycin
4) STREPTOmycin
"TAGS" = aminoglycosides
39
What makes the aminoglycosides special?
They are the only bacteriCIDAL (kill bacteria) of the ribosomal inhibitors.
40
What is the mechanism of action of the Aminoglycosides?
protein inhibitor = 30S
binds to 30S (IRREVERSIBLY) and creates premature mRNA release, mis-reading, and arresting of initiation
41
What is the common mechanism of resistance of Tetracylcines?
efflux pumps
| minor: changes to bacterial ribosome
42
What is the common mechanism of resistance of the aminoglycosides?
enzymatic modification of the antibiotic
| modification of the drug prevents its ability to bind to the ribosome, and preform bactericidal actions
43
What class?
What is the mechanism?
Useful for what types of bacteria?
"DOXYCYCLINE"
1) Class: TETRACYCINE
2) Mechanism: binds 30S; prevents tRNA binding
3) Bacteria: BROAD SPECTRUM
Note: Not used widely due to common resistance (by EFFLUX PUMPs and some ribosomal 30S modification)
44
What class?
What is the mechanism?
Useful for what types of bacteria?
"MINOCYCLINE"
1) Class: TETRACYCINE
2) Mechanism: binds 30S; prevents tRNA binding
3) Bacteria: BROAD SPECTRUM
Note: Not used widely due to common resistance (by EFFLUX PUMPs and some ribosomal 30S modification)
45
What class?
What is the mechanism?
Useful for what types of bacteria?
"TIGECYCLINE"
1) Class: TETRACYCINE
2) Mechanism: binds 30S; prevents tRNA binding
3) Bacteria: BROAD SPECTRUM
NOTE: Not used widely due to common resistance (by EFFLUX PUMPs and some ribosomal 30S modification)
46
What class?
What is the mechanism?
Useful for what types of bacteria?
TOBRAMYCIN
1) Class: AMINOGLYCOSIDES
2) Mechanism: BIND TO 30S (IRREVERSIBLY); mis-reading and premature mRNA release
3) Bacteria: G- (NEGATIVE)* [e.g. Pseudomonas]
* Does NOT penetrate G+ well
* Weak against anerobes
NOTE: Enzymatic modification of TOBRAMYCIN is common form of anti-bacterial resistance.
Adverse: OTO- and NEPHRO- toxicity
47
What class?
What is the mechanism?
Useful for what types of bacteria?
"AMIKACIN"
1) Class: AMINOGLYCOSIDES
2) Mechanism: BIND TO 30S (IRREVERSIBLY); mis-reading and premature mRNA release
3) Bacteria: G- (NEGATIVE)* [e.g. Pseudomonas]
* Does NOT penetrate G+ well
* Weak against anerobes
NOTE: Enzymatic modification of AMIKACIN is common form of anti-bacterial resistance.
Adverse: OTO- and NEPHRO- toxicity
48
What class?
What is the mechanism?
Useful for what types of bacteria?
"GENTAMYCIN"
1) Class: AMINOGLYCOSIDES
2) Mechanism: BIND TO 30S (IRREVERSIBLY); mis-reading and premature mRNA release
3) Bacteria: G- (NEGATIVE)* [e.g. Pseudomonas]
* Does NOT penetrate G+ well
* Weak against anerobes
NOTE: Enzymatic modification of GENTAMYCIN is common form of anti-bacterial resistance.
Adverse: OTO- and NEPHRO- toxicity
49
What class?
What is the mechanism?
Useful for what types of bacteria?
"STREPTOMYCIN"
1) Class: AMINOGLYCOSIDES
2) Mechanism: BIND TO 30S (IRREVERSIBLY); mis-reading and premature mRNA release
3) Bacteria: G- (NEGATIVE)* [e.g. Pseudomonas]
* Does NOT penetrate G+ well
* Weak against anerobes
NOTE: Enzymatic modification of STREPTOMYCIN is common form of anti-bacterial resistance.
Adverse: OTO- and NEPHRO- toxicity
50
What class?
What is the mechanism?
Useful for what types of bacteria?
PENICILLIN G
1) Class: Beta-Lactams (Penicillins / Panems)
2) Mechanism: binds to PBPs; prevents peptidoglycan crosslinking
3) Bacteria: G+ (POSITIVE)*
Note: Penicillin G and V are NOT USEFUL against Gram negatives (especially enterics because it hydrolyzed by gastric acid)
51
What class?
What is the mechanism?
Useful for what types of bacteria?
PENICILLIN V
1) Class: Beta-Lactams (Penicillins / Panems)
2) Mechanism: binds to PBPs; prevents peptidoglycan crosslinking
3) Bacteria: G+ (POSITIVE)*
Note: Penicillin G and V are NOT USEFUL against Gram negatives
52
What class?
What is the mechanism?
Useful for what types of bacteria?
AMOXICILLIN
1) Class: Beta-Lactams (Penicillins / Panems)
2) Mechanism: binds to PBPs; prevents peptidoglycan crosslinking
3) Bacteria:
G+ (POSITIVE) COCCI
G- (NEGATIVE) ENTERICS
53
What class?
What is the mechanism?
Useful for what types of bacteria?
PIPERACILLIN
1) Class: Beta-Lactams (Penicillins / Panems)
2) Mechanism: binds to PBPs; prevents peptidoglycan crosslinking
3) Bacteria:
G- (NEGATIVE) BACILLI
(e.g. pseudomonas)
54
What class?
What is the mechanism?
Useful for what types of bacteria?
TRICARCILLIN
1) Class: Beta-Lactams (Penicillins / Panems)
2) Mechanism: binds to PBPs; prevents peptidoglycan crosslinking
3) Bacteria:
G- (NEGATIVE) BACILLI
(e.g. pseudomonas)
55
What is the common mechanism of resistance of the aminoglycosides?
enzymatic modification of the antibiotic
| modification of the drug prevents its ability to bind to the ribosome, and preform bactericidal actions
56
What is the mechanism of panems?
bind to PBPs and prevent cross-linking of peptidoglycan
57
What are the panems?
1) PENICILLIN G
2) PENICILLIN V
3) AMOXICILLIN
4) PIPERACLIIN
5) TRICARCILLIN
58
What is the common mechanism of resistance against the b-lactams?
Beta-lactamase
59
How do you deal with Beta-lactamase? (specific)
Add a Beta-lactamase inhibitor (which binds to it) along with the antibiotic
examples:
clauvanic acid
sulbactam
tazobactam
60
What class?
What is the mechanism?
Useful for what types of bacteria?
CEFAZOLIN
1) Class: CEPAHLOSPORIN --- GEN 1
2) Mechanism: bind to PBPs (irrversibly) and prevent cross-linking of peptidoglycan (same as other Beta-lactams)
3) Bacteria:
> 1ST GEN, so mostly G+ (POSITIVE)
>Klebsiella
>E.Coli
NOTE: Cefazolin does NOT fight against Enterococcus, anaerobic bacteria or atypical bacteria among others.
NOTE:
Cefazolin is useful for (MSSA) (strep)
But...does NOT work for (MRSA) (staph)
NOTE: Cepahlosporins are less susceptible to beta lactamases!
61
What class?
What is the mechanism?
Useful for what types of bacteria?
CEPHALEXIN
1) Class: CEPAHLOSPORIN --- GEN 1
2) Mechanism: bind to PBPs (irrversibly) and prevent cross-linking of peptidoglycan (same as other Beta-lactams)
3) Bacteria:
> 1ST GEN, so mostly G+ (POSITIVE)
>Klebsiella
>E.Coli
Note: Cepahlosporins are less susceptible to beta lactamases!
62
What class?
What is the mechanism?
Useful for what types of bacteria?
CEFAZOLIN
1) Class: 1st GEN CEPAHLOSPORIN --- GEN 1 (--in)
2) Mechanism: bind to PBPs (irrversibly) and prevent cross-linking of peptidoglycan (same as other Beta-lactams)
3) Bacteria:
> 1ST GEN, so mostly G+ (POSITIVE)
>Klebsiella
>E.Coli
NOTE: Cefazolin does NOT fight against Enterococcus, anaerobic bacteria or atypical bacteria among others.
NOTE:
Cefazolin is useful for (MSSA) (strep)
But...does NOT work for (MRSA) (staph)
NOTE: Cepahlosporins are less susceptible to beta lactamases!
63
What class?
What is the mechanism?
Useful for what types of bacteria?
CEPHALEXIN / CEFALEXIN
1) Class: 1st GEN CEPAHLOSPORIN --- GEN 1 (--in)
2) Mechanism: bind to PBPs (irrversibly) and prevent cross-linking of peptidoglycan (same as other Beta-lactams)
3) Bacteria:
> 1ST GEN, so mostly G+ (POSITIVE)
>Klebsiella
>E.Coli
Note: Cepahlosporins are less susceptible to beta lactamases!
64
What class?
What is the mechanism?
Useful for what types of bacteria?
CEFUROXIME
1) Class: 2ND GEN CEPAHLOSPORIN --- GEN 2
2) Mechanism: bind to PBPs (irrversibly) and prevent cross-linking of peptidoglycan (same as other Beta-lactams)
3) Bacteria:
> 2nd GEN, so less G+ (POSITIVE)
> NISSERIA
> HAEMOPHILUS
Note: Cepahlosporins are less susceptible to beta lactamases!
65
What class?
What is the mechanism?
Useful for what types of bacteria?
CEFOXITIN
1) Class: 2ND GEN CEPAHLOSPORIN --- GEN 2
2) Mechanism: bind to PBPs (irrversibly) and prevent cross-linking of peptidoglycan (same as other Beta-lactams)
3) Bacteria:
> 2nd GEN, so less G+ (POSITIVE)
NOTE: IT IS A STRONG BETA-LACTAMASE INDUCER!
Note: Cepahlosporins are less susceptible to beta lactamases!
66
What class?
What is the mechanism?
Useful for what types of bacteria?
CEFTRIAXONE
1) Class: 3RD GEN CEPAHLOSPORIN --- GEN 3
2) Mechanism: bind to PBPs (irrversibly) and prevent cross-linking of peptidoglycan (same as other Beta-lactams)
3) Bacteria:
> 3RD GEN, so less G+ (POSITIVE)
> Drug of choice for non-listeria MENINGITIS
NOTE: not useful against pseudomonas
Note: Cepahlosporins are less susceptible to beta lactamases!
67
What class?
What is the mechanism?
Useful for what types of bacteria?
CEFTAZIDIME
1) Class: 3RD GEN CEPAHLOSPORIN --- GEN 3
2) Mechanism: bind to PBPs (irrversibly) and prevent cross-linking of peptidoglycan (same as other Beta-lactams)
3) Bacteria:
> 3RD GEN, so less G+ (POSITIVE)
> MOSTLY G- (NEGATIVES)
```
Gram-negative aerobes...
> Enterobacter
> E. coli
> H. influenzae
> Klebsiella
> Proteus
> Pseudomonas
> N. meningitidis
```
```
Gram-positive aerobes
> Staphylococcus aureus
> group B streptococci (GBS)
> Streptococcus pneumoniae,
> Streptococcus pyogenes (GAS)
```
Anaerobes
> Bacteroides
Note: Cepahlosporins are less susceptible to beta lactamases!
68
What class?
What is the mechanism?
Useful for what types of bacteria?
CYCLOSERINE
1) Class: n/a (cell wall inhibitor)
2) Mechanism: (intracellular/cytoplasmic)
>competitively inhibits the addition of D-Alanine to MurNAc (needed for peptidoglycan)
3) Bacteria:
> M. Tuberculosis
69
What class?
What is the mechanism?
Useful for what types of bacteria?
BACITRACIN
1) Class: n/a (cell wall inhibitor)
2) Mechanism: (intracellular/cytoplasmic)
> prevents phosphate removal (and thus recycling) of the lipid carrier needed for transferring peptidoglycan substrates across the lipid bilayer
3) Bacteria: G+ (POSITIVE)
> especially against GAS (S. pyogenes)
NOTE: only useful for external surfaces
(cannot be taken within the body due to toxicity)
70
What class?
What is the mechanism?
Useful for what types of bacteria?
FOSFOMYCIN
1) Class: n/a (cell wall inhibitor)
2) Mechanism: (intracellular/cytoplasmic)
> prevents MurNAc (NAM) systehsis inside the bacterial cell
3) Bacteria:
> G+ AND G-
71
What class?
What is the mechanism?
Useful for what types of bacteria?
VANCOMYCIN
1) Class: GLYCOPEPTIDE (cell wall inhibitor)
2) Mechanism: binds to "D-Ala-D-Ala" end reside, therby preventing PBP from binding and causing cross-linking of the peptidoglycan
3) Bacteria: G+ (POSITIVE) ONLY*
* this is because the molecule is very large
NOTE: Resistance is usually conferred by the bacteria changing the peptidoglycan by substituting D-Lac for the last D-Ala. This prevents Vancomycin binding but still allows for PBP specificity and cross-linking because the 5th reside (in this case D-Lac, but what is normally D-Ala) is removed during the cross-linking process
72
What class?
What is the mechanism?
Useful for what types of bacteria?
DAPTOMYCIN
1) Class: LIPOPEPTIDE (cell membrane inhibitor)
2) Mechanism:
> depolarizes the cytosolic membrane; membrane disruption
3) Bacteria: G+ (POSITIVE)
Note: DAPTOMYCIN mediated cytosolic membrane depolarization is novel mechanism; thus is is more useful against antibiotic resistant strains
73
What class?
What is the mechanism?
Useful for what types of bacteria?
POLYMIXIN B
1) Class: LIPOPEPTIDE (cell membrane inhibitor)
2) Mechanism:
> binds to LPS and disrupts both outer and cytosolic membranes
3) Bacteria: G- (NEGATIVE)
> e.g. pseudomonas
Note: POLYMIXIN B mediated membrane destruction is novel mechanism; thus is is more useful against antibiotic resistant strains
74
What class?
What is the mechanism?
Useful for what types of bacteria?
COLISTIN
1) Class: LIPOPEPTIDE (cell membrane inhibitor)
2) Mechanism:
> binds to LPS and disrupts both outer and cytosolic membranes
3) Bacteria: G- (NEGATIVE)
> e.g. pseudomonas
Note: COLISTIN mediated membrane destruction is novel mechanism; thus is is more useful against antibiotic resistant strains
75
What is the mechanism of panems?
bind to PBPs and prevent cross-linking of peptidoglycan
76
What is the common mechanism of resistance against the b-lactams?
Beta-lactamase
77
How do you deal with Beta-lactamase? (specific)
Add a Beta-lactamase inhibitor (which binds to it) along with the antibiotic
examples:
>CLAVULANIC ACID
>SULBACTAM
>TAZOBACTAM
78
What is the mechanism of cephalosporins?
bind to PBPs and prevent cross-linking of peptidoglycan
79
What is the common mechanism of cephalosporin resistance?
Beta-lactamase
80
What are the common cephalosporins?
1ST GEN
1) CEPHAZOLIN (cef-azolin) (cefa---in)
2) CEPHALEXIN (cef-alexin) (cefa---in)
2ND GEN
3) CEFUROXIME (-oxi-)
4) CEFOXITIN (-oxi-)
3RD GEN
5) CEFTRIAXONE
6) CEFTAZIDIME
4TH GEN
7) CEFEPIME
81
What are the common cephalosporins?
1ST GEN
1) CEPHAZOLIN (cef-azolin) (cefa---in)
2) CEPHALEXIN (cef-alexin) (cefa---in)
2ND GEN
3) CEFUROXIME (-oxi-)
4) CEFOXITIN (-oxi-)
3RD GEN
5) CEFTRIAXONE
6) CEFTAZIDIME
4TH GEN
7) CEFEPIME
82
Which antibiotics are membrane disruptors?
Disrupts cytosolic membrane === G+ use
> DAPTOMYCIN
Disrupts both membranes ==== G- use
> POLYMYXIN B
> COLISTIN
83
What class?
What is the mechanism?
Useful for what types of bacteria?
DAPTOMYCIN
1) Class: LIPOPEPTIDE (cell membrane inhibitor)
2) Mechanism:
> depolarizes the cytosolic membrane; membrane disruption
3) Bacteria: G+ (POSITIVE)
Note: DAPTOMYCIN mediated cytosolic membrane depolarization is novel mechanism; thus is is more useful against antibiotic resistant strains
84
What class?
What is the mechanism?
Useful for what types of bacteria?
ERYTHROMYCIN
1) Class: MACROLIDE
2) Mechanism: (50S; prevents elongation )
3) Bacteria: G+ (POSITIVE)
85
What class?
What is the mechanism?
Useful for what types of bacteria?
AZITHROMYCIN
1) Class: MACROLIDE
2) Mechanism: (50S; prevents elongation )
3) Bacteria: G+ (POSITIVE)
Note: more broad specificity than erythromycin
86
What class?
What is the mechanism?
Useful for what types of bacteria?
CLARITHROMYCIN
1) Class: MACROLIDE
2) Mechanism: (50S; prevents elongation )
3) Bacteria: G+ (POSITIVE)
87
What is the mechanism of action of the Tetracyclines?
protein inhibitor = 30S
binds to 30S of bacterial ribosome and prevents aminoacyl-tRNA binding (i.e. prevents initiation)
BacteriSTATIC
88
What is the mechanism of action of the Aminoglycosides?
protein inhibitor = 30S
binds to 30S (IRREVERSIBLY) and creates premature mRNA release, mis-reading, and arresting of initiation
BactericCIDAL (only ribosome inhibitors to do so)
89
What is the mechanism of panems?
bind to PBPs and prevent cross-linking of peptidoglycan
BactericCIDAL
90
What is the mechanism of cephalosporins?
bind to PBPs and prevent cross-linking of peptidoglycan
BactericCIDAL
91
Which antibiotics are membrane disruptors?
Disrupts cytosolic membrane === G+ use
> DAPTOMYCIN
Disrupts both membranes ==== G- use
> POLYMYXIN B
> COLISTIN
BactericCIDAL
92
What are the macrolides?
Nomeclature: (----thromycin)
1) Erythromycin
2) Azithromycin
3) Clarithromycin
93
What is the mechanism of the macrolides?
Ribosome Inhibitor: (50S; prevents elongation )
BacteriSTATIC
94
What is the mechanism of the macrolides?
Ribosome Inhibitor: (50S; prevents elongation )
BacteriSTATIC
95
What class of bacteria are used for the macrolides?
Gram-POSITIVE
G+
96
What are the common forms of bacterial resistance for macrolides (2) ?
1)
2)
