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Therapeutics V > Erdman - Penicillins > Flashcards

Erdman - Penicillins Flashcards

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1
Q

Beta-lactam general characteristics

A

-Inhibit cell wall synthesis
-Bacteria resistances include beta-lactamase degradation, PBP alteration, decreased penetration
-Bactericidal in a time-dependent manner, except against enteroccocus
-Short elimination half-life
-Primarily excreted unchanged by the kidneys
-Cross-allergenicity in class

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2
Q

Beta-lactams that are not eliminated by the kidneys

A

-Nafcillin
-Oxacillin
-Ceftriaxone
-Cefoperazone

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3
Q

Beta-lactam that does not have cross-allergenicity

A

Aztreonam

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4
Q

Which gram-positive bacteria produce beta-lactamase enzymes?

A

Penicillin-resistant Staphylococcus aureus

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5
Q

Which gram-negative bacteria produce beta-lactamase enzymes?

A

-Haemophilus influenza
-Moraxella catarrhalis
-Neisseria gonorrhoeae
-E. Coli
-Klebsiella pneumoniae
-Enterobacter spp.
-etc.

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6
Q

Which gram-negative anaerobes produce beta-lactamase enzymes?

A

Bacterioides fragilis

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7
Q

Which bacteria alter the structure of PBPs leading to decreased binding affinity?

A

-Methicillin-resistant Staphylococcus aureus (MRSA)
-Penicillin-resistant Streptococcus pneumoniae (PRSP)

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8
Q

Three mechanisms of bacterial resistance against antibiotics

A

-Production of beta-lactamase enzymes
-Alterations in the structure of PBPs leading to decreased binding affinity
-Alterations of outer membrane porin proteins leading to decreased penetration

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9
Q

What are the natural penicillins used clinically?

A

-Aqueous penicillin G
-Benzathine penicillin G
-Procaine penicillin G
-Phenoxymethyl penicillin (penicillin VK)

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10
Q

Penicillin spectrum of activity against gram-positives

A

-Group streptococci
-Viridans streptococci
-Enterococcus spp.
-Pen-susceptible S. pneumoniae
-Pen-susceptible S. aureus
-Bacillus spp.

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11
Q

Penicillin spectrum of activity against gram-negatives

A

-Primarily used against some cocci
-Neisseria spp.
-Pasteurella multocida

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12
Q

Penicillin spectrum of activity against anaerobes

A

-Above the diaphragm
-Clostridium spp. but not C. diff.

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13
Q

Most important bacteria that penicillin covers

A

Treponema pallidum (syphilis)

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14
Q

Why were penicillinase-resistant penicillins developed?

A

In response to the emergence of penicillinase-producing Staph aureus

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15
Q

Examples of penicillinase-resistant penicillins

A

-Nafcillin
-Methicillin (no longer used)
-Dicloxacillin

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16
Q

Which penicillinase-resistant penicillin is oral?

A

Dicloxacillin

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17
Q

Penicillinase-resistant penicillin spectrum of activity against gram-positives

A

-Group streptococci
-Viridans streptococci
-Methicillin-susceptible S. aureus (MSSA)* (DOC)

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18
Q

Penicillinase-resistant penicillin spectrum of activity against gram-negatives

A

No activity against gram-negatives

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19
Q

Penicillinase-resistant penicillin spectrum of activity against anaerobes

A

No activity

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20
Q

What are the aminopenicillins?

A

-Ampicillin
-Amoxicillin

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21
Q

Which aminopenicillins are oral?

A

-Ampicillin
-Amoxicillin

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22
Q

Which aminopenicillins are parenteral?

A

Ampicillin

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23
Q

Aminopenicillin spectrum of activity against gram-positives

A

-Group streptococci
-Viridans streptococci
-Pen-susc S. pneumoniae
-Enterococcus spp. (DOC)*
-Pen-susc S. aureus

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24
Q

Aminopenicillin spectrum of activity against gram-negatives

A

(SHEP)
-Salmonella, shigella
-H. influenzae (beta-lactamase negative)
-E. coli (some)
-Proteus mirabilis

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25
What are the carboxypenicillins?
Ticarcillin (parenteral)
26
Carboxypenicillin spectrum of activity against gram-positives
None
27
Carboxypenicillin spectrum of activity against gram-negatives
(SHEPEP) -Salmonella, shigella -H. influenzae (beta-lactamase positive) -E. coli (some) -Proteus mirabilis -Enterobacter spp. -Pseudomonas aeruginosa*
28
What are the ureidopenicillins?
Piperacillin
29
Is piperacillin parenteral or oral?
Parenteral
30
Ureidopenicillin spectrum of activity against gram-positives
-Group strep -Viridans strep -Some enterococcus (Amp is still doc)
31
Ureidopenicillin spectrum of activity against gram-negatives
(SHEPEP + KS) -Salmonella, shigella -H. influenzae (beta-lactamase positive) -E. coli (some) -Proteus mirabilis -Enterobacter spp. -Pseudomonas aeruginosa* (DOC) -Some klebsiella spp. -Serratia marcescens
32
What are the beta-lactamase inhibitor combo products?
-Ampicillin-sulbactam (Unasyn) -Piperacillin-tazobactam (Zosyn) -Amoxicillin-clavulanate (Augmentin)
33
What is Unasyn?
Ampicillin-sulbactam
34
What is Zosyn?
Piperacillin-tazobactam
35
What is Augmentin?
Amoxicillin-clavulanate
36
Ureidopenicillin spectrum of activity against anaerobes
-Fairly good activity -BDA -Mostly used in combo with beta-lactamase inhibitors
37
Beta-lactamase inhibitor combo spectrum of activity against gram-positives
MSSA (not a lot of clinical studies done)
38
Beta-lactamase inhibitor combo spectrum of activity against gram-negatives
-H. influenzae -E. Coli -Proteus spp. -Klebsiella spp. -Neisseria gonorrhoeae -Moraxella catarrhalis
39
Beta-lactamase inhibitor combo spectrum of activity against anaerobes
Bacterioides spp. (great activity against BDA)*
40
What are penicillins dependent on to kill bacteria?
-Time-dependent bacterial killing -Time above MIC (Time>MIC)
41
What is the goal of dosing in penicillins?
Administer agents to maintain serum concentrations > MIC of infecting bacteria for 50% of dosing interval
42
What synergy is used clinically to treat Viridans strep?
Penicillin or ampicillin plus gentamicin
43
What synergy is used clinically to treat enterococcus spp.?
Ampicillin plus gentamicin or streptomycin
44
What synergy is used clinically to treat staphylococcus spp.)
Nafcillin plus gentamicin
45
What synergy is used clinically to treat gram negative bacteria?
Ticarcillin or piperacillin plus gentamicin, tobramycin or amikacin
46
When should you use oral vs IV penicillins?
Oral penicillins should be used for mild to moderate disease and IV should be used for moderate to severe disease
47
Do penicillins penetrate into the CNS?
Adequate concentrations of penicillins (but NOT beta-lactamase inhibitors) are achieved ONLY in the presence of inflamed meninges with high-dose parenteral administration
48
What is the elimination half life of penicillins?
Short
49
How are penicillins eliminated?
Most are eliminated through the liver
50
Which penicillins do not need their doses to be adjusted due to renal insufficiency?
-Nafcillin -Oxacillin
51
Which penicillins contain sodium in their preparations?
-Sodium penicillin G -Nafcillin -Ticarcillin -Piperacillin
52
Sodium content of sodium penicillin G
2 mEq per 1 million units
53
Sodium content of sodium nafcillin
2.9 mEq per gram
54
Sodium content of sodium ticarcillin
5.2 mEq per gram
55
Sodium content of sodium piperacillin
1.85 mEq per gram
56
Clinical use of natural penicillins
Syphilis
57
Clinical use of penicillinase-resistant penicillins
MSSA
58
Clinical use of aminopenicillins
-Enterococcal infections -Listeria monocytogenes
59
Clinical use of carboxypenicillins and ureidopenicillins
-Gram-negative aerobic bacteria -Hospital-acquired infections -Infections due to pseudomonas aeruginosa (piperacillin)
60
Clinical use of Augmentin
-Sinusitis -Otitis media
61
Clinical use of Unasyn, Zosyn
-Polymicrobial infections -Empiric therapy for febrile neutropenia -Hospital-acquired infections (Zosyn)
62
Adverse effects of penicillins
-Hypersensitivity -Neurologic effects: seizures -Hematologic: Neutropenia, thrombocytopenia -GI effects -Interstitial nephritis: abrupt increase in serum creatinine -Phlebitis -Hypokalemia -Na overload
63
Is there cross-reactivity among penicillins?
Yes and some other beta-lactams
64
What can cause neurologic adverse effects in patients taking penicillins?
Patients receiving high IV doses in the presence of renal insufficiency
65
How can you reverse hematologic adverse effects in patients taking penicillins?
Discontinue the medication
66
Which medications are most likely to cause interstitial nephritis?
Methicillin or nafcillin

Therapeutics V (52 decks)

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