Cell wall/membrane inhibitors Flashcards

1
Q

Spectrum of action of vancomycin

A

Gram-positive
Used for drug resistant gram positive organisms

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2
Q

MOA of vancomycin

A

Inhibits cell wall synthesis
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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3
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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4
Q

Elimination of vancomycin

A

Excreted unchanged in urine (80%) or stool

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5
Q

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

A

Renal dysfunction

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6
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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7
Q

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

A

Vancomycin

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8
Q

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

A

Vancomycin

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9
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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10
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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11
Q

Spectrum of action of Bacitracin

A

Narrow gram positive cocci

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12
Q

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

A

Bacitracin

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13
Q

2 main adverse effects of Bacitracin

A

Severe hypersensitivity and nephrotoxicity if systemically absorbed

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14
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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15
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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16
Q

Antibiotic class with this MOA:
Binds to penicillin-binding proteins (PBPs) located in membrane
Blocks the transpeptidase crosslinking of cell wall components
Activates autolysis enzymes (releases murein hydrolase) 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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17
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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18
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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19
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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20
Q

Why is caution needed in using penicillins with meningitis?

A

Penicillins are neurotoxic

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21
Q

Caution is required in this as penicillins are neurotoxic

A

Meningitis

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22
Q

Elimination of penicillins

A

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

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23
Q

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

A

Biotransformation or biliary

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24
Q

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

A

Penicillin G

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25
Q

Natural penicillin that is acid stable, oral route of administration

A

Penicillin V

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26
Q

Penicillin G and Penicillin V are this type of penicillin

A

Natural penicillins

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27
Q

Spectrum of action of natural penicillins

A

Narrow gram positive

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28
Q

These are drugs of choice for syphilis and S. pneumoniae

A

Natural penicillins (Penicillin G and V)

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29
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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30
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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31
Q

Drugs of choice for preventing endocarditis with surgical or dental procedures

A

Semisynthetic/Aminopenicillins

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32
Q

Ampicillin and Amoxicillin are vulnerable to these

A

Beta lactamases

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33
Q

Semisynthetic/Aminopenicillins are vulnerable to these

A

Beta lactamases

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34
Q

Ampicillin and Amoxicillin are this type of penicillin

A

Semisynthetic/Aminopenicillins

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35
Q

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

A

Very narrow gram positive
Staphylococcal infections

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36
Q

Another name for Antistaphylococcal penicillins

A

Penicillinase-resistant penicillins

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37
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

38
Q

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

A

Antistaphylococcal penicillins (Penicillinase-resistant penicillins)

39
Q

Ticarcillin, Carbenicillin and Piperacillin are this type of penicillin

A

Antipseudomonal penicillins

40
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

41
Q

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

A

Suicide inhibitors (irreversible beta-lactamase inhibitors)

42
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

43
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

44
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

45
Q

Clavulanate, Sulbactam and Tazobactam are this

A

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

46
Q

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

A

Suicide inhibitors (irreversible beta-lactamase inhibitors)
Ex: Sulbactam, Tazobactam, Clavulanata

47
Q

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

A

Penicillins

48
Q

Vitamin K deficiency is a characteristic adverse effect of this drug

A

Penicillins

49
Q

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

A

Is increased

50
Q

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

A

Is increased

51
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

52
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

53
Q

Cefazolin and Cephalexin are this type of agents

A

1st generation cephalosporins

54
Q

Spectrum of action of 1st generation cephalosporins

A

Extended gram positive

55
Q

Cefotetan, Cefuroxime and Cefoxitin are this type of agents

A

2nd generation cephalosporins

56
Q

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

A

3rd generation cephalosporins

57
Q

Drug of choice for treatment of gonorrhea

A

Ceftriaxone (3rd generation cephalosporin)

58
Q

Ceftriaxone is the drug of choice for this

A

Gonorrhea

59
Q

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

A

Natural penicillins

60
Q

Natural penicillins are the drugs of choice for these

A

Syphilis and S. pneumoniae

61
Q

Semisynthetic/Aminopenicillins are drugs of choice for preventing this

A

Endocarditis with surgical or dental procedures

62
Q

Cefepime is this type of agent

A

4th generation cephalosporin

63
Q

Ceftaroline is this type of agent

A

5th generation cephalosporin

64
Q

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

A

More

65
Q

Spectrum of action of Ceftaroline (5th generation cephalosporin)

A

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

66
Q

Disulfiram-like reaction with alcohol is noted for this cephalosporin

A

Cefotetan (2nd generation cephalosporin)

67
Q

Cephalosporins adverse reactions are similar to those of this drug

A

Penicillins

68
Q

Characteristic adverse effect noted for Cefotetan (2nd gen cephalosporin)

A

Disulfiram-like reaction with alcohol

69
Q

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

A

Carbapenems

70
Q

Imipenem is this type of drug

A

Carbapenem (beta lactam)

71
Q

Spectrum of activity of Aztreoname (Monobactam)

A

Gram negative
Resistant to beta lactamases

72
Q

Aztreonam (Monobactam) are resistant to these

A

Beta lactamases

73
Q

Aztreoname is this type of agent

A

Monobactam

74
Q

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

A

Penicillins or cephalosporins

75
Q

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

A

Low cross reactivity

76
Q

This is the preferred agent for penicillin-sensitive patients

A

Aztreonam (monobactam)

77
Q

Drug that binds to phospholipids in membrane to disrupt membrane integrity

A

Polymyxins

78
Q

MOA of polymyxins

A

Membrane disruption

79
Q

Spectrum of action of polymyxins

A

Aerobic gram negative

80
Q

Colistin is this type of agent

A

Polymyxin

81
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

82
Q

High toxicity of polymyxins limits systemic use to this

A

“must use” only indications

83
Q

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

A

Polymyxins

84
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

85
Q

Antibiotic that lethally depolarizes bacteria

A

Daptomycin

86
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

87
Q

Spectrum of action of Daptomycin

A

Narrow gram positive

88
Q

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

A

Daptomycin

89
Q

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

A

Pulmonary surfactants

90
Q

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

A

Pneumonia

91
Q

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

A

Daptomycin

92
Q

Myopathy and Peripheral neuropathy are characteristic adverse effects of this antibiotic

A

Daptomycin