Cell Wall/Membrane Inhibitors Flashcards

1
Q

1st step in cell wall synthesis

A

Precursor (UDP-acetylmuramyl-pentapeptide) synthesized in the cell

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

2nd step in cell wall synthesis

A

Formation of sugar-pentapeptide in the cell, and its transport out of membrane and subsequent addition and polymerization to linear peptidoglycan strands

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

3rd step in cell wall synthesis

A

Cross-linking of adjacent peptidogycan (murein) strands by a transpeptidase reaction

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Spectrum of action of vancomycin

A

Gram-positive
Used for drug resistant gram positive organisms

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

MOA of vancomycin

A

Inhibits cell wall synthesis at step 2
Binds to D-ala-D-ala terminal of the peptidoglycan pentapeptide side chain and prevents polymerization of the linear peptidoglycan
concentration-independent killing

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Antibiotic with this MOA:
Inhibits cell wall synthesis at step 2
Binds to D-ala-D-ala terminal of the peptidoglycan pentapeptide side chain and prevents polymerization of the linear peptidoglycan

A

Vancomycin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Elimination of vancomycin

A

Excreted unchanged in urine (80%) or stool

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Half life of vancomycin with normal renal function

A

6 hours

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Half life of vancomycin with renal dysfunction

A

7-9 days

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Vancomycin half life is ~6 hours, but increases to 7-9 days in patients with this

A

Renal dysfunction

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Hypersensitivity, Ototoxicity, Fever and chills, flushing or “red man syndrome”, hemolysis in G6PD deficiency, and nephrotoxicity are adverse effects of this antibiotic

A

Vancomycin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Ototoxicity is a characteristic adverse effect of this cell wall/membrane inhibitor

A

Vancomycin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Hemolysis in G6PD deficiency is a characteristic adverse effect of this cell wall/membrane inhibitor

A

Vancomycin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Histamine-induced rash of the head and upper thorax caused by vancomycin direct action on mast cells

A

Flushing or “Red Man Syndrome”

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

“Red man syndrome” is a histamine-induced rash of the head and upper thorax caused by this antibiotic direct action on mast cells

A

Vancomycin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Spectrum of action of Bacitracin

A

Narrow gram positive cocci

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

Severe hypersensitivity and nephrotoxicity if systemically absorbed are adverse effects of this narrow gram positive cocci antibiotic

A

Bacitracin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

2 main adverse effects of Bacitracin

A

Severe hypersensitivity and nephrotoxicity if systemically absorbed

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

Antibiotic that inhibits incorporation of sugar-pentapeptide in to cell wall by interfering with the final dephosphorylated step in the phospholipid carrier cycle
Damages cell membrane and cell wall
Bacteriostatic at normal doses, bactericidal at higher doses

A

Bacitracin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

MOA of bacitracin

A

Inhibits incorporation of sugar-pentapeptide into cell wall by interfering with the final dephosphorylated step in the phospholipid carrier cycle

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

Antibiotic with this MOA:
Binds to penicillin-binding proteins (PBPs) located in membrane
Blocks the transpeptidase crosslinking of cell wall components (step 3 of cell wall synthesis)
Activates autolysis enzymes (releases murein hydrolase0 to promote cell wall dissolution
Results in weakened cell wall, aberrant morphological form, cell lysis and death

A

Beta-lactam antibiotics

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

MOA of beta-lactam antibiotics (3)

A

Binds PBPs in membrane
Blocks transpeptidase crosslinking of cell wall components
Activates autolytic enzymes to promote cell wall dissolution

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

Antibiotic with the following 2 mechanisms of resistance:
Express enzymes that inactivate antibiotic ring
Formation of aberrant PBP that does not allow effective antibiotic binding

A

Beta-lactam antibiotics

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

2 mechanisms of resistance of beta-lactam antibiotics

A

Express beta-lactamases that inactivate (open) beta-lactam ring
Formation of aberrant PBP that does not allow effective beta lactam binding

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Why is caution needed in using penicillins with meningitis?
Penicillins are neurotoxic
26
Caution is required in this as penicillins are neurotoxic
Meningitis
27
Elimination of penicillins
Renal 10% filtration, 90% tubular secretion Biotransformation or biliary (Nafcillin, Ampicillin, Piperacillin)
28
Nafcillin, Ampicillin, and Pipercillin are penicillins that are eliminated via these routes
Biotransformation or biliary
29
Natural penicillin that is unstable in acid, intramuscular and IV route of administration
Penicillin G
30
Natural penicillin that is acid stable, oral route of administration
Penicillin V
31
Penicillin G and Penicillin V are this type of penicillin
Natural penicillins
32
Spectrum of action of natural penicillins
Narrow gram positive
33
These are drugs of choice for syphilis and S. pneumoniae
Natural penicillins (Penicillin G and V)
34
Spectrum of action of Semisynthetic/Aminopenicillins
Broad (very extended) "HELPS" Haemophilus influenzae E. coli Listeria monocytogenes Proteus mirabilis Salmonella
35
Penicillins with broad (very extended) spectrum of action "HELPS" Haemophilus influenzae E. coli Listeria monocytogenes Proteus mirabilis Salmonella
Semisynthetic/Aminopenicillins
36
Drugs of choice for preventing endocarditis with surgical or dental procedures
Semisynthetic/Aminopenicillins
37
Ampicillin and Amoxicillin are vulnerable to these
Beta lactamases
38
Semisynthetic/Aminopenicillins are vulnerable to these
Beta lactamases
39
Ampicillin and Amoxicillin are this type of penicillin
Semisynthetic/Aminopenicillins
40
Spectrum of action of Antistaphylococcal penicillins (aka Pellicinase-resistant penicillins)
Very narrow gram positive Staphylococcal infections
41
Another name for Antistaphylococcal penicillins
Penicillinase-resistant penicillins
42
Antistaphylococcal penicillins are penicillin analogs with bulky side chains that make them resistant to some beta lactamases, but can't bind this
Mutated PBPs
43
Methicilin, Nafcillin, Oxacillin, and Dicloxacillin are this type of penicillin
Antistaphylococcal penicillins (Penicillinase-resistant penicillins)
44
Ticarcillin, Carbenicillin and Piperacillin are this type of penicillin
Antipseudomonal penicillins
45
Penicillin type with broad spectrum of action, resistant to many but not all beta lactamases expressed by gram negative bacteria Side groups allow greater penetration into gram negative bacteria (Pseudomonas, Anaerobes)
Antipseudomonal penicillins
46
These are paired with agents sensitive to beta-lactamases with similar pharmacokinetics to overcome some resistance
Suicide inhibitors (irreversible beta-lactamase inhibitors)
47
Clavulanate is this
Suicide inhibitor (irreversible beta-lactamase inhibitor) Paired with agents sensitive to beta-lactamase with similar pharmacokinetics to overcome some resistance
48
Sulbactam is this
Suicide inhibitor (irreversible beta-lactamase inhibitor) Paired with agents sensitive to beta-lactamase with similar pharmacokinetics to overcome some resistance
49
Tazobactam is this
Suicide inhibitor (irreversible beta-lactamase inhibitor) Paired with agents sensitive to beta-lactamase with similar pharmacokinetics to overcome some resistance
50
Clavulanate, Sulbactam and Tazobactam are this
Suicide inhibitor (irreversible beta-lactamase inhibitor) Paired with agents sensitive to beta-lactamase with similar pharmacokinetics to overcome some resistance
51
These should be used when resistance by beta-lactamase is expected
Suicide inhibitor (irreversible beta-lactamase inhibitor) Paired with agents sensitive to beta-lactamase with similar pharmacokinetics to overcome some resistance
52
Allergic responses (~10%), Allergic cross reactions are significant (~6%), Neurotoxicity, and Vitamin K deficiency are adverse effects of this
Penicillins
53
Vitamin K deficiency is a characteristic adverse effect of this
Penicillins
54
Moving from first to higher generation of cephalosporins, how does the activity against gram negatives change?
Is increased
55
Moving from first to higher generation of cephalosporins, how does resistance to beta-lactamases change?
Is increased
56
Moving from first to higher generation of cephalosporins, how does distribution change?
Increased distribution to body tissues and fluids, especially during inflammation Third and later generations can cross blood brain barrier
57
Moving from first to higher generation of cephalosporins, how does activity against gram positives change?
Is decreased Fourth and fifth generation agents have more gram positive activity than third generation
58
Cefazolin and Cephalexin are this type of agents
1st generation cephalosporins
59
Spectrum of action of 1st generation cephalosporins
Extended gram positive
60
Cefotetan, Cefuroxime and Cefoxitin are this type of agents
2nd generation cephalosporins
61
Cefotaxime, Ceftazidime, Cefpodoxime proxetil and Ceftriaxone are this type of agents
3rd generation cephalosporins
62
Cefazolin is this type of agent
1st generation cephalosporins
63
Cephalexin is this type of agent
1st generation cephalosporins
64
Cefotetan is this type of agent
2nd generation cephalosporins
65
Cefuroxime is this type of agent
2nd generation cephalosporins
66
Cefoxitin is this type of agent
2nd generation cephalosporins
67
Cefotaxime is this type of agent
3rd generation cephalosporins
68
Ceftazidime is this type of agent
3rd generation cephalosporins
69
Cefpodoxime proxetil is this type of agent
3rd generation cephalosporins
70
Ceftriaxone is this type of agent
3rd generation cephalosporins
71
Drug of choice for treatment of gonorrhea
Ceftriaxone (3rd generation cephalosporin)
72
Ceftriaxone is the drug of choice for this
Gonorrhea
73
These are the drugs of choice for syphilis and S. pneumoniae
Natural penicillins
74
Natural penicillins are the drugs of choice for these
Syphilis and S. pneumoniae
75
Semisynthetic/Aminopenicillins are drugs of choice for preventing this
Endocarditis with surgical or dental procedures
76
Cefepime is this type of agent
4th generation cephalosporin
77
Ceftaroline is this type of agent
5th generation cephalosporin
78
Cefepime has more or less gram positive activity than a given 3rd generation cephalosporin?
More
79
Spectrum of action of Ceftaroline (5th generation cephalosporin)
Broad Active against many resistant gram positive agents (MRSA, VRSA, VISA, hVISA)
80
Disulfiram-like reaction with alcohol is noted for this cephalosporin
Cefotetan (2nd generation cephalosporin)
81
Cephalosporins adverse reactions are similar to those of:
Penicillins
82
Characteristic adverse effect noted for Cefotetan
Disulfiram-like reaction with alcohol
83
Broadest spectrum of beta lactams, highly resistant to most beta-lactamases, reserved for treating bacteria with MDR Includes Imipenem
Carbapenems
84
If penicillin/cephalosporin allergy suspected, patient can be given a ______ skin challenge before receiving a therpaeutic dose of this drug
Carbapenem
85
Spectrum of activity of Aztreoname (Monobactam)
Gram negative Resistant to beta lactamases
86
Aztreonam (Monobactam) are resistant to these
Beta lactamases
87
Aztreoname is this type of agent
Monobactam
88
Aztreoname (monobactam) has low cross reactivity noted in patients sensitive to either of these
Penicillins or cephalosporins
89
Is there cross reactivity in Aztreoname (monobactam) with patients sensitive to penicillins or cephalosporins?
Low cross reactivity
90
This is the preferred agent for penicillin-sensitive patients
Aztreonam (monobactam)
91
Aztreonam (monobactam) is the preferred agent for this
Penicillin-sensitive patients
92
Drug that binds to phospholipids in membrane to disrupt membrane integrity
Polymyxins
93
MOA of polymyxins
Membrane disruption
94
Spectrum of action of polymyxins
Aerobic gram negative
95
Colistin is this type of agent
Polymyxin
96
Cell membrane inhibitor with the following adverse effects: Hypersensitivity High toxicity limits systemic use to "must use" only indications Black box: Nephrotoxicity, Neurotoxicity, Not safe in pregnancy
Polymyxins
97
High toxicity of polymyxins limits systemic use to this
"must use" only indications
98
High toxicity of this limits systemic use to "must use" only indications
Polymyxins
99
Antibiotic that at higher concentrations, binds membranes of gram positive bacteria to cause rapid depolarization leading to cell death and inhibition of intracellular synthesis of DNA, RNA and proteins
Daptomycin
100
Antibiotic that lethally depolarizes bacteria
Daptomycin
101
MOA of Daptomycin
Lethally depolarizes bacteria At higher concentrations, binds membranes of gram positive bacteria to cause rapid depolarization leading to cell death and inhibition of intracellular synthesis of DNA, RNA and proteins
102
Spectrum of action of Daptomycin
Narrow gram positive
103
Antibiotic that is degraded by pulmonary surfactants so cannot be used in pneumonia
Daptomycin
104
Daptomycin is degraded by these, so cannot be used in pneumonia
Pulmonary surfactants
105
Daptomycin is degraded by pulmonary surfactants, so cannot be used in this
Pneumonia
106
Hypersensitivity, GI distress, superinfections, Myopathy, and peripheral neuropathy are adverse effects of this antibiotic
Daptomycin
107
Myopathy and Peripheral neuropathy are characteristic adverse effects of this antibiotic
Daptomycin