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AU 15 - Pharm Final > Antibacterial Drugs #2 > Flashcards

Antibacterial Drugs #2 Flashcards

(131 cards)

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1
Q

What drugs Inhibit Nucleic Acid Synthesis

A

Sulfonamides
Trimethoprim
Rifamprin

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2
Q

Sulfonamide Mechanism

A

Competitive Inhibitor of Dihydropteroate synthase - which is required for the synthesis of folic acid

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3
Q

Is Sulfonamide Bacteriostatic or bacteriocidal?

A

Static

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4
Q

Sulfonamide Selectivity

A

Bacteria must synthesize their own folate, while humans utilize dietary folate

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5
Q

Sulfonamide Antibacterial spectrum

A

Gram+ and Gram-

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6
Q

Sulfonamide Clinical uses

A

UTIs
Toxoplasmosis
Malaria
Prophylactive for burns and AIDS patients preventing P jirovecii

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7
Q

Sulfonamide Toxicities

A

Dose related - Crytalluria, Hemolytic anemia, Kernicterus

Dose Unrelated - Hypersensitivity

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8
Q

Trimethoprim Mechanism

A

Inhibitor of Dihydrofolate reductase (DHFR)

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9
Q

Is Trimethoprim Bacteriostatic or Bacteriocidal

A

Static

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10
Q

Trimethoprim Selectivity

A

Bacteria must synthesize their own folate, while humans utilize dietary folate

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11
Q

Trimethoprim Antibacterial Selectivity

A

Gram+ and Gram-

Broader spectrum than Sulfonamides

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12
Q

Trimethoprim Clinical Uses

A

Usually used in combination with Sulfamethoxazole (makes it bacteriocidal)
UTIs
GI infections
P. jarovecii prophylaxis in AIDS patients

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13
Q

Trimethoprim Toxicities

A

Slight blood dyscrasia

Anemia in patients that are folate deficient

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14
Q

Rifamprin Mechanism

A

Binds to an inhibits RNA polymerase

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15
Q

Is Rifamprin Bacteriostatic or Bacteriocidal?

A

Cidal

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16
Q

Rifamprin Selectivity

A

Does not bind to human RNA

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17
Q

Rifamprin Spectrum

A

Potent against M. tuberculosis

Some activity against Stphylococci

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18
Q

Rifamprin Clinical Uses

A

First line anti-tuberculosis in compination with other anto-tubercular drugs (RIPE)

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19
Q

Rifamprin Toxicities

A

Liver damage - Jaundice

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20
Q

Rifamprin Resistance Mechanisms

A

Inductance of resistance is rapid - therefor not used as monotherapy

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21
Q

What drugs are DNA damaging?

A

Quinolones
Nitrofurantoin
Metronidazole
Methenamine

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22
Q

Quinolones mechanism

A

Poison DNA Gyrase A - inhibiting the uncoiling funciton of DNA gyrase ahead of the replication fork

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23
Q

Are Quinolones bacteriostatic or bacteriocidal?

A

Cidal

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24
Q

Quinolones Selectivity

A

Mammalian DNA topoisomerase is not inhibited to the same extent as DNA Gyrase II and Topoisomerase IV in bacteria

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25
Quinolones Spectrum
Gram+ and Gram-
26
Quinolones Clinical Uses
UTI RTI Anti-tubercular
27
Quinolones Toxicities
Generally well-tolerated | Avoid using with Ciprofloxin with children - leads to potential tendon ruptures
28
Quinolones Resistance Mechanisms
1) Mutations in Gyrase or Topoisomerase targets 2) Increased efflux pumps 3) Altered porins (gram-)
29
Nitrofurantoin Mechanism
DNA damage caused by formation of oxygen free radicals subsequent to reduction of a nitro group
30
Are Nitrofurantoins Bacteriostatic or bacteriocidal?
Static
31
Nitrofurantoins Selectivity
Bacteria cause reductive activation more extensively than mammalian cells
32
Nitrofurantoins Antibacterial spectrum
Broad spectrum against Gram+ and Gram- | Not effective against P. aeruginosa
33
Nitrofurantoins Clinical Uses
UTI RTI Anti-tubercular
34
Nitrofurantoin Toxicities
Poor renal function leads to toxicity - fever, rashes, urticaria, and eventually pulmonary fibrosis
35
Metronidazole Mechanism
Reductive activation of nitro group specifically in anaerobic bacteria leads to free radical species and reactive intermediates that bind to and effect DNA function
36
Is Metronidazole bacteriostatic or bacteriocidal?
Cidal
37
Metronidazole selectivity
Bacteriocidal agent against most obligate anaerobic gram+ bacteria
38
Metronidazole spectrum
Gram+ anaerobic
39
Methenamine Mechanism
Hydrolyzed at acidic pH to form formaldehyde - which has been shown to damage DNA
40
Is Methenamine bacteriostatic or bactericidal?
Cidal
41
Methenamine antibacterial spectrum
Gram-
42
Methenamine Clinical Uses
Only for prophylaxis of UTIs
43
Which drugs Inhibit Cell Wall synthesis?
``` Beta-Lactams -Penicillins -Cephalosporins -Monobactams -Carbapenems B-lactamase inhibitors Vancomyocin Bacitracin ```
44
Penicillin mechanisms
Mimics D-ala-D-ala structure of pentapeptide on peptidoglycan and ties up transpeptidase
45
Is penicillin bacteriostatic or bactericidal?
Cidal
46
Penicillin selectivity
Inhibits cell wall synthesis - there is no cell wall in eukaryotic cells
47
Penicillin clinical uses
Streptococcus pneumoniae
48
Penicillin resistance mechanisms
1) B-lactmases (Gram+ and gram-) 2) Altere PBPs 3) Altered porins (gram-) 4) Increases efflux (enhanced pump mechanisms)
49
Are penicillins Time dependent or Concentration dependent?
Time dependent
50
Cephalosporins Mechanisms
Mimics D-ala-D-ala structure of pentapeptide on peptidoglycan and ties up transpeptidase
51
Are Cephalosporins bacteriostatic or bacteriocidal?
Cidal
52
Cephalosporin Selectivity
Inhibits cell wall synthesis - there is no cell wall in eukaryotic cells
53
Cephalosproin toxicities
Relatively nontoxic, but direct toxic effect in the kidney have been noted as well as hypersensitivity
54
B-lactamase Mechanism
Inhibits B-lactamase - binds to serine at the active site of lactamase
55
Are B-lactamases bacteriostatic or bactericidal?
Cidal
56
B-lactamases selectivity
Inhibits cell wall synthesis - there is no cell wall in eukaryotic cells
57
B-lactamase clinical use
Used in combination with beta-lactam antibiotics (extends their spectrum)
58
Vancomyocin Mechanism
Binds to the carboxyl terminus of D-ala-D-ala and thereby: 1) Inhibits Peptidoglycan synthase 2) Inhibits transpeptidation reaction (so there's no cross-linking)
59
Is Vancomyocin bacteristatic or bactericidal
Cidal
60
Vancomyocin selectivity
Inhibits cell wall synthesis - there is no cell wall in eukaryotic cells
61
Vancomyocin Antibacterial spectrum
Narrow spectrum - active against Gram+ staph and strep
62
Vancomyocin Toxicities
Hearing loss (dose related) often relate to renal impairment Some renal toxicity has been noted Red neck syndrome
63
Vancomyocin Resistance Mechanism
Resistance is a major issue | Due to altered D-ala-D-ala peptide structures causing Vancomyocin to not bind as avidly
64
Bacitracin Mechanism
Binds to isoprenyl-phosphate lipid carrier, inhibiting dephosphorylation and utilization
65
Is Bacitracin bacteriostatic or bactericidal?
Cidal
66
Bacitracin Selectivity
Inhibits cell wall synthesis - there is no cell wall in eukaryotic cells
67
Bacitracin Antibacterial spectrum
Gram+ cocci | Some Gram- activity
68
Bacitracin Clinical uses
Superficial skin and opthalmic infections
69
What drugs damage the cell membrane?
Polymyxins | Daptomycin
70
Polymixin Mechanism
Acts as a cationic detergent
71
Are polymixins bacteriostatic or bactericidal?
Cidal
72
Polymixins Spectrum
Gram-
73
Polymixins Clinical uses
Particularly useful in hospital settings against pan-resistant (multi-drug resistant) Gram- infections
74
Polymixins toxicities
Dose related nephrotoxicity in patients with renal disease
75
Daptomycin mechanism
Insertion of lipophylic tail into cell membrane, causing membrane depolarization, K efflux, and disruption to DNA and RNA synthesis Works very quickly (~1 hour)
76
Is Daptomycin bacteriostatic or bactericidal?
Cidal
77
Daptomycin Antibacterial spectrum
Gram+ | Because it binds to the LPS layer in gram- bacteria, it can never reach the cell membrane
78
Daptomycin clinical uses
Effective against most Gram+ pathogens (includin MRSA) | Can't use on lung infections because it gets inactivated by pulmonary surfactant
79
What drugs are inhibitors of protein synthesis?
``` Aminoglycosides Tetracyclines Tigecyclines Chlorophenicol Macrolides Ketolide Clindamycin Linezoid Quinupristin/Dalfopristin ```
80
Aminoglycosides Mechanism
Bind to proteins in the interface between 30S and 50S - - interfere with tRNA attachment - block activity of initiation complex - distorting of mRNA triplet codon - leading to mispairing
81
Are Aminoglycosides bacteriostatic or bactericidal?
Cidal
82
Aminoglycosides Selectivity
Don't bind to mammalian ribosomes (80S)
83
Aminoglycosides Antibacterial spectrum
Gram-
84
Aminoglycosides Clinical Uses
Streptomyocin - used in the past for TB | Neomucin - topical use for treatment of burns and wounds
85
Aminoglycosides Toxicities
Ototoxicity - cochlear hair cell death Nephrotoxicity Neuromuscular blockade - leading to muscle weakness and respiratory depression
86
Are aminoglycosides time or concentration dependent?
Concentration | Exhibit a considerable post-antibiotic effect
87
Tetracycline Mechanism
Bind to 30S and bind blocking of tRNA
88
Are tetracyclines bacteriostatic and bactericidal
Static
89
Tetracycline Selectivity
Concentrated to a greater extent in bacterial cells compared to mammalian cells by a specific carrier protein not found in mammalial cells
90
Tetracycline Antibacterial spectrum
Broad spectrum against Gram+ and Gran-
91
Tetracycline toxicities
Photosensitivity | Binds to bone and teeth - can stain teeth and retard bone growth
92
Tetracycline Resistance mechanisms
Decreased influx Increases efflux pump Decreased binding to ribosomes
93
Tigecycline Mechanism
Bind to 30S and block binding of tRNA
94
Is Tigecycline bacteriostatic or bactericidal?
Static
95
Tigecycline Selectivity
Doesn't bind to mammalian ribosomes (80S)
96
Tigecycline Antibacterial Spectrum
Broad spectrum against Gram+ and gram-
97
Tigecycline Clinical uses
Complicated intra-abdominal and skin infections | Not used in bacteriemias because of low serum levels
98
Tigecycline toxicities
Doesn't have the toxicities associated with Tetracyclines
99
Chlorophenicol Mechanism
Binds to 50S - inhibiting peptidyl transferase by preventing the attachment of amino acid end of aminoacyl-tRNA to the "A" site
100
Is Chlorophenicol bacteriostatic or bactericidal?
Static
101
Chlorophenicol Selectivity
Doesn't bind to mammalian ribosomes (80S)
102
Chlorophenicol Clinical uses
Extremely limited clinical use because of potentially Aplastic Anemia
103
Chlorophenicol Antibacterial spectrum
Broad spectrum against Gram+ and Gram-
104
Chlorophenicol toxicities
Aplastic Anemia | Grey baby syndrome
105
Macrolides Mechanism
Binds to 50S - inhibiting translocation and causes the release of oligo-peptidyl tRNA
106
Are macrolides bacteriostatic or bactericidal?
Bacteriostatic against most | Bactericidal against some Gram+
107
Macrolides Selectivity
Doesn't bind to mammalian ribosomes (80S)
108
Macrolides Antibacterial spectrum
Bacteriostatic against most | Bactericidal against some Gram+
109
Macrolides Clinical Uses
``` M. pneumoniae Legionnaire's Chlamydia Pneumonias Middle ear and sinus infections ```
110
Macrolides Toxicities
Fairly safe - some GI issues and hypersensitivity
111
Ketolide Mechanism
Binds to 50S - inhibiting translocation and causes the release of oligo-peptidyl tRNA
112
Is Ketolide bacteriostatic or bactericidal?
Static
113
Ketolide Antibacterial spectrum
Gram+ and Gram-
114
Ketolide Clinical uses
Effective against Macrolide-resistant strains (efflux pumps don't effect them) RTIs
115
Ketolide toxicities
Liver toxicity
116
Clindamycin Mechanism
Binds to 50S
117
Is Clindamycin bacteriostatic or bactericidal?
Static
118
Clindamycin Selectivity
Doesn't bind to mammalian ribosomes (80S)
119
Clindamycin Antibacterial Spectrum
Gram+ and anaerobes
120
Clindamycin Clinical Uses
Against penicillin-resistant anaerobic infections | Topical acne treatment
121
Clindamycin toxicities
Pseudomembranous colitis caused by toxin from C. dificile - which is resistant to Clindamycin
122
Linezolid Mechanism
Binds to 50S - blocks formation of initiation complex
123
Is Linezolid bacteriostatic or bactericidal?
Static
124
Linezolid selectivity
Doesn't bind to mammalian ribosomes (80S)
125
Linezolid Antibacterial Spectrum
Gram+
126
Linezolid Clinical uses
Useful against vancomyocin-resistant Enterococcus faecium and MRSA
127
Quinupristin/Dalfopristin Mechanism
Both bind to 50S Quin = stimulates dissociation of peptidyl-tRNA Dal = prevents binging of aa-tRNA
128
Are Quinupristin/Dalfopristin bacteriostatic or bactericidal?
Static alone | Cidal when used together
129
Quinupristin/Dalfopristin Selectivity
Doesn't bind to mammalian ribosomes (80S)
130
Quinupristin/Dalfopristin Antibacterial Spectrum
Gram+
131
Quinupristin/Dalfopristin Clinical uses
Useful against vancomyocin-resistant Enterococcus faecium and MRSA

AU 15 - Pharm Final (7 decks)

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