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Pharmacology > Cell Wall/Membrane Inhibitors > Flashcards

Cell Wall/Membrane Inhibitors Flashcards

1
Q

1st step in cell wall synthesis

A

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

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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

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3
Q

3rd step in cell wall synthesis

A

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

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4
Q

Spectrum of action of vancomycin

A

Gram-positive
Used for drug resistant gram positive organisms

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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

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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

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7
Q

Elimination of vancomycin

A

Excreted unchanged in urine (80%) or stool

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8
Q

Half life of vancomycin with normal renal function

A

6 hours

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9
Q

Half life of vancomycin with renal dysfunction

A

7-9 days

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10
Q

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

A

Renal dysfunction

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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

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12
Q

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

A

Vancomycin

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13
Q

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

A

Vancomycin

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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”

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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

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16
Q

Spectrum of action of Bacitracin

A

Narrow gram positive cocci

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17
Q

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

A

Bacitracin

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18
Q

2 main adverse effects of Bacitracin

A

Severe hypersensitivity and nephrotoxicity if systemically absorbed

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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

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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

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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

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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

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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

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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

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25
Q

Why is caution needed in using penicillins with meningitis?

A

Penicillins are neurotoxic

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26
Q

Caution is required in this as penicillins are neurotoxic

A

Meningitis

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27
Q

Elimination of penicillins

A

Renal
10% filtration, 90% tubular secretion
Biotransformation or biliary (Nafcillin, Ampicillin, Piperacillin)

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28
Q

Nafcillin, Ampicillin, and Pipercillin are penicillins that are eliminated via these routes

A

Biotransformation or biliary

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29
Q

Natural penicillin that is unstable in acid, intramuscular and IV route of administration

A

Penicillin G

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30
Q

Natural penicillin that is acid stable, oral route of administration

A

Penicillin V

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31
Q

Penicillin G and Penicillin V are this type of penicillin

A

Natural penicillins

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32
Q

Spectrum of action of natural penicillins

A

Narrow gram positive

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33
Q

These are drugs of choice for syphilis and S. pneumoniae

A

Natural penicillins (Penicillin G and V)

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34
Q

Spectrum of action of Semisynthetic/Aminopenicillins

A

Broad (very extended)
“HELPS”
Haemophilus influenzae
E. coli
Listeria monocytogenes
Proteus mirabilis
Salmonella

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35
Q

Penicillins with broad (very extended) spectrum of action
“HELPS”
Haemophilus influenzae
E. coli
Listeria monocytogenes
Proteus mirabilis
Salmonella

A

Semisynthetic/Aminopenicillins

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36
Q

Drugs of choice for preventing endocarditis with surgical or dental procedures

A

Semisynthetic/Aminopenicillins

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37
Q

Ampicillin and Amoxicillin are vulnerable to these

A

Beta lactamases

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38
Q

Semisynthetic/Aminopenicillins are vulnerable to these

A

Beta lactamases

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39
Q

Ampicillin and Amoxicillin are this type of penicillin

A

Semisynthetic/Aminopenicillins

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40
Q

Spectrum of action of Antistaphylococcal penicillins (aka Pellicinase-resistant penicillins)

A

Very narrow gram positive
Staphylococcal infections

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41
Q

Another name for Antistaphylococcal penicillins

A

Penicillinase-resistant penicillins

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42
Q

Antistaphylococcal penicillins are penicillin analogs with bulky side chains that make them resistant to some beta lactamases, but can’t bind this

A

Mutated PBPs

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43
Q

Methicilin, Nafcillin, Oxacillin, and Dicloxacillin are this type of penicillin

A

Antistaphylococcal penicillins (Penicillinase-resistant penicillins)

44
Q

Ticarcillin, Carbenicillin and Piperacillin are this type of penicillin

A

Antipseudomonal penicillins

45
Q

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)

A

Antipseudomonal penicillins

46
Q

These are paired with agents sensitive to beta-lactamases with similar pharmacokinetics to overcome some resistance

A

Suicide inhibitors (irreversible beta-lactamase inhibitors)

47
Q

Clavulanate is this

A

Suicide inhibitor (irreversible beta-lactamase inhibitor)
Paired with agents sensitive to beta-lactamase with similar pharmacokinetics to overcome some resistance

48
Q

Sulbactam is this

A

Suicide inhibitor (irreversible beta-lactamase inhibitor)
Paired with agents sensitive to beta-lactamase with similar pharmacokinetics to overcome some resistance

49
Q

Tazobactam is this

A

Suicide inhibitor (irreversible beta-lactamase inhibitor)
Paired with agents sensitive to beta-lactamase with similar pharmacokinetics to overcome some resistance

50
Q

Clavulanate, Sulbactam and Tazobactam are this

A

Suicide inhibitor (irreversible beta-lactamase inhibitor)
Paired with agents sensitive to beta-lactamase with similar pharmacokinetics to overcome some resistance

51
Q

These should be used when resistance by beta-lactamase is expected

A

Suicide inhibitor (irreversible beta-lactamase inhibitor)
Paired with agents sensitive to beta-lactamase with similar pharmacokinetics to overcome some resistance

52
Q

Allergic responses (~10%), Allergic cross reactions are significant (~6%), Neurotoxicity, and Vitamin K deficiency are adverse effects of this

A

Penicillins

53
Q

Vitamin K deficiency is a characteristic adverse effect of this

A

Penicillins

54
Q

Moving from first to higher generation of cephalosporins, how does the activity against gram negatives change?

A

Is increased

55
Q

Moving from first to higher generation of cephalosporins, how does resistance to beta-lactamases change?

A

Is increased

56
Q

Moving from first to higher generation of cephalosporins, how does distribution change?

A

Increased distribution to body tissues and fluids, especially during inflammation
Third and later generations can cross blood brain barrier

57
Q

Moving from first to higher generation of cephalosporins, how does activity against gram positives change?

A

Is decreased
Fourth and fifth generation agents have more gram positive activity than third generation

58
Q

Cefazolin and Cephalexin are this type of agents

A

1st generation cephalosporins

59
Q

Spectrum of action of 1st generation cephalosporins

A

Extended gram positive

60
Q

Cefotetan, Cefuroxime and Cefoxitin are this type of agents

A

2nd generation cephalosporins

61
Q

Cefotaxime, Ceftazidime, Cefpodoxime proxetil and Ceftriaxone are this type of agents

A

3rd generation cephalosporins

62
Q

Cefazolin is this type of agent

A

1st generation cephalosporins

63
Q

Cephalexin is this type of agent

A

1st generation cephalosporins

64
Q

Cefotetan is this type of agent

A

2nd generation cephalosporins

65
Q

Cefuroxime is this type of agent

A

2nd generation cephalosporins

66
Q

Cefoxitin is this type of agent

A

2nd generation cephalosporins

67
Q

Cefotaxime is this type of agent

A

3rd generation cephalosporins

68
Q

Ceftazidime is this type of agent

A

3rd generation cephalosporins

69
Q

Cefpodoxime proxetil is this type of agent

A

3rd generation cephalosporins

70
Q

Ceftriaxone is this type of agent

A

3rd generation cephalosporins

71
Q

Drug of choice for treatment of gonorrhea

A

Ceftriaxone (3rd generation cephalosporin)

72
Q

Ceftriaxone is the drug of choice for this

A

Gonorrhea

73
Q

These are the drugs of choice for syphilis and S. pneumoniae

A

Natural penicillins

74
Q

Natural penicillins are the drugs of choice for these

A

Syphilis and S. pneumoniae

75
Q

Semisynthetic/Aminopenicillins are drugs of choice for preventing this

A

Endocarditis with surgical or dental procedures

76
Q

Cefepime is this type of agent

A

4th generation cephalosporin

77
Q

Ceftaroline is this type of agent

A

5th generation cephalosporin

78
Q

Cefepime has more or less gram positive activity than a given 3rd generation cephalosporin?

A

More

79
Q

Spectrum of action of Ceftaroline (5th generation cephalosporin)

A

Broad
Active against many resistant gram positive agents (MRSA, VRSA, VISA, hVISA)

80
Q

Disulfiram-like reaction with alcohol is noted for this cephalosporin

A

Cefotetan (2nd generation cephalosporin)

81
Q

Cephalosporins adverse reactions are similar to those of:

A

Penicillins

82
Q

Characteristic adverse effect noted for Cefotetan

A

Disulfiram-like reaction with alcohol

83
Q

Broadest spectrum of beta lactams, highly resistant to most beta-lactamases, reserved for treating bacteria with MDR
Includes Imipenem

A

Carbapenems

84
Q

If penicillin/cephalosporin allergy suspected, patient can be given a ______ skin challenge before receiving a therpaeutic dose of this drug

A

Carbapenem

85
Q

Spectrum of activity of Aztreoname (Monobactam)

A

Gram negative
Resistant to beta lactamases

86
Q

Aztreonam (Monobactam) are resistant to these

A

Beta lactamases

87
Q

Aztreoname is this type of agent

A

Monobactam

88
Q

Aztreoname (monobactam) has low cross reactivity noted in patients sensitive to either of these

A

Penicillins or cephalosporins

89
Q

Is there cross reactivity in Aztreoname (monobactam) with patients sensitive to penicillins or cephalosporins?

A

Low cross reactivity

90
Q

This is the preferred agent for penicillin-sensitive patients

A

Aztreonam (monobactam)

91
Q

Aztreonam (monobactam) is the preferred agent for this

A

Penicillin-sensitive patients

92
Q

Drug that binds to phospholipids in membrane to disrupt membrane integrity

A

Polymyxins

93
Q

MOA of polymyxins

A

Membrane disruption

94
Q

Spectrum of action of polymyxins

A

Aerobic gram negative

95
Q

Colistin is this type of agent

A

Polymyxin

96
Q

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

A

Polymyxins

97
Q

High toxicity of polymyxins limits systemic use to this

A

“must use” only indications

98
Q

High toxicity of this limits systemic use to “must use” only indications

A

Polymyxins

99
Q

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

A

Daptomycin

100
Q

Antibiotic that lethally depolarizes bacteria

A

Daptomycin

101
Q

MOA of Daptomycin

A

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
Q

Spectrum of action of Daptomycin

A

Narrow gram positive

103
Q

Antibiotic that is degraded by pulmonary surfactants so cannot be used in pneumonia

A

Daptomycin

104
Q

Daptomycin is degraded by these, so cannot be used in pneumonia

A

Pulmonary surfactants

105
Q

Daptomycin is degraded by pulmonary surfactants, so cannot be used in this

A

Pneumonia

106
Q

Hypersensitivity, GI distress, superinfections, Myopathy, and peripheral neuropathy are adverse effects of this antibiotic

A

Daptomycin

107
Q

Myopathy and Peripheral neuropathy are characteristic adverse effects of this antibiotic

A

Daptomycin

Pharmacology (14 decks)

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