Penecillin Flashcards

1
Q

structure of penicillin

A

house with a garage

4-member B-lactam ring next to 5-member sulfa ring

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2
Q

B-lactam MOA

A

bind the cell wall and inhibit cell wall/peptidoglycan synthesis (penicillin binding proteins). inhibits transpeptidase which makes cross links in peptidoglycan.

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3
Q
B-Lactam:
Bacteriocidal or Bacteriostatic?
concentration dependent or time dependent?
Elimination half-life?
Elimination route (primarily)?
A

Bacteriocidal (except against entercoccus species)

Time-dependent

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4
Q

Which B-lactams aren’t eliminated by the kidney?

A

nafcillin, oxacillin,

ceftriaxone, cefoperazone

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5
Q

Most common mechanism of B-lactam resistance?

A

B-lactamase (hydrolyzes B-lactam ring)

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6
Q

B-lactamase activity in gram pos?

A

destroy B-lactams extracellularly

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7
Q

B-lactamase activity in gram neg?

A

destroy B-lactams in the periplasm (between inter and outer membrane) after B-lactams enter through porins

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8
Q

Natural penecillins examples (with attributes)?

A
IV:
Penicillin G (still used)
Benzapine (long-lasting, used 1x/week for latent syphilis)
Procaine (short acting)
Oral:
Penicillin VK (more readily absorbed)
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9
Q

Bacteria treated by Natural Penicllins?

A

Gram+ = Group Strep and viridians strep
gram- cocci = neisseria spp
Anaerobes = clostridium (not C.Diff)
syphilis

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10
Q

Penicllinase-resistant Penicllin examples?

A

IV: Nafcillin, Oxacillin, Methicillin (Ox and Meth not used)
Oral: Dicloxacillin (not absorbed well orally)

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11
Q

Bacteria treated by Penicillinase-resistant Penicillins?

A

Gram+ = MSSA (Methicilline susceptible staph aureus)

made specifically for staph aureus’s penicillinase

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12
Q

What gene causes staph aureus to be resistant to penicillinase-resistant penicillin (MRSA)? And how does it convey resistance? What is only drug that can treat MRSA?

A

mecA gene. changes the binding site.

Ceftaroline.

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13
Q

Aminopenicillins: Why created? examples?

A

Gram neg activity (especially for Ecoli)
IV: Ampicillin
Oral: Amoxicillin (Ampicillin can be given but it isn’t)

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14
Q

Bacteria treated by Aminopenicillins?

A
Gram+ = same as penicillin, but better with enterococci. Only drug that treats Listeria monocytogenes (Gram+)
Gram- = proteus mirabilis, Ecoli (most), salmonella, shigella, H.flu
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15
Q

Carboxypenicillins: why made? examples?

A

Gram neg bacteria

IV: Ticarcillin (only available in combination)

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16
Q

Bacteria treated by Carboxypenicillins?

A
Gram+ = carboxy group diminishes gram+ effects, so none
gram- = pseudomonas aeruginosa (hospital-acquired illness)
17
Q

Ureidopenicillins: why made? examples?

A

gram neg bacteria treatment but still retaining some gram pos treatment ability
IV: Piperacillin (only available in combo with tazobactam)

18
Q

Bacteria targeted by Ureidopenicillins?

A

Gram- = pseudomonas aeruginosa (also enterbacter, klebsiella, and serratia marcescens)
Anaerobes (very often used on anaerobes)

19
Q

B-lactamase inhibitor action?

A

irreversibly bind catalytic site of B-lactamase

20
Q

B-lactamase inhibitor/penicillin combos?

A

IV: ampicillin-sulbactam
ticarcillin-clavulanate (no longer available)
Piperacillin-tazobactam
Oral: amoxicillin-clavulanate

21
Q

bacteria treated with B-lactamase inhibitor combos

A

gram+ = non-MRSA staph aureus
gram- = H.flu, moraxella catarrhalis
Anaerobes: bacteroides spp

22
Q

What needs to happen to get adequate penicillins into CSF?

A

ONLY n the presence of inflamed meninges with high-dose IV administration

23
Q

clinical uses of natural penicillins?

A

anything that is penicillin susceptible like strep
syphilis
endocarditis prophylaxis

24
Q

clinical uses of penicllinase-resistant penicillin?

A

MSSA

25
Q

Aminopenicillins clinical use?

A

Resp tract infections
Entercoccal infections
Listeria monocytogenes
endocarditis prophylaxis

26
Q

Carboxypenecillin and ureidopenecillin clinical uses?

A

gram neg aerobic bacterial infections (pneumonia, bacteremia, UTIs)
empiric therapies
pseudomonas aeruginosa (especially piperacillin)

27
Q

Adverse effects of penicillin?

A

(more with IV) ranges from rash to anaphylaxis and death

ABs made to metabolic by-products

28
Q

Neurologic adverse effects?

A

irritability, jerking, seizures, confusion

29
Q

Hematological adverse effects?

A

leukopenia, neutropenia, thrombocytopenia

usually from prolonged therapy, reversible upon stopping

30
Q

Adverse GI effects?

A

increased LFTs, nausea, vomiting, diarrhea, pseudomembranous colitis (diarrhea from C.Diff)

31
Q

Adverse Renal effects?

A

Interstitial nephritis=damage to renal tubules leading to renal failure