Penicillins Flashcards

1
Q

What are the 3 B-lactamase inhibitors?

A

Clavulonic Acid
Sulbactam
Tazobactam

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2
Q

What is the mehcanism of action for Penicillins?

A

Inhibit bacterial cell wall synthesis by blocking crosslinking of adjacent peptidoglycan strands with subsequent lysis.

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3
Q

What are Penicillin-binding proteins (PBPs)?

What enzymes fall into this classification?

A

Targets of B-lactam antibiotics; Include:
Transpeptidases
Transglycolases
D-alanine carboxykinase
-Peptidoglycan transpeptidase is one PBP that is inhibited.

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4
Q

T/F

Penicillins are bactericidal.

A

TRUE

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5
Q

What bugs exhibit Beta-lactamase Production?

A

Staph

H. flu

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6
Q

What bugs don’t allow antibiotic to penetrate to PBP targets?

A

Gram negative organisms (porin channel penetration)

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7
Q

What bugs exhibit low affinity binding of antibiotic to PBPs?

A

Pneumococcus, MRSA, Enterococcus

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8
Q

What feature allows Ampicillin and Amoxicillin to target some G– ?
What feature allows Piperacillin to target G– all the way through “SPACE bugs”?

A

Amine on side chain

long side chain with amines

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9
Q

When will a patient’s peak levels of penicillin be in reference to taking orally?

What effect does food have on penicillins?

A

1-2 hours after ingestion

Peak levels 2-3 hrs
Decreases absorption (excet Pen V, Amoxicillin, and Carbenicillin)
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10
Q

Why is inflammation needed for PCNs distribution to brain, CSF, and prostate.

A

Insoluble in lipid

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11
Q

T/F

Some PCNs are acid stable; others are acid labile

A

TRUE

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12
Q

Are PCNs well distributed throughout the body?

What is their major route of Excretion and what does that make you take into consideration when prescribing?

A

Yes, but hydrophilic

Renal Excretion primarily; MUST ADJUST FOR RENAL INSUFFICIENCY

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13
Q

T/F
Hypersensitivity may not occur on re-exposure or may occur without previous reaction.

What two types of hypersensitivity are exhibited?

A

TRUE

-Immediate Reaction (anaphylaxis) - IgE mediated. -Delayed Reaction (i.e. rash) - IgM or IgG mediated.
Maculopapular rash is most common.

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14
Q

Why was methicillin removed from shelves?

A

Interstitial Nephritis

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15
Q

Besides Hypersensitivity, what 3 other adverse effects are associated with PCNs?

A
  • Eosinophilia/Thrombocytopenia/Neutropenia
  • Interstitial Nephritis
  • Pseudomembranous colitis
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16
Q

What 2 kinds of salts do Pen G come in?

A

K+

Na+

17
Q

Why is benzathine penicillin used to treat syphillis and phrphylaxis against rheumatic fever?

A

sustained release (21 days)

18
Q

What bugs do PenG/VK cover?

A

Streptococcus
SOME Enterococcus

PS: Strep Pneumo PBP changes on rise causing more resistance

19
Q

Why is Nafcillin great to use in patients with renal dysfunction?

A

hepatic elimination

20
Q

What PCNs belong to the “Penicillinase Resistant Penicillins” (Antistaphylococcal penicillins)?

Which are IV only and which are PO only?

A

Methicillin, Oxacillin, Nafcillin
Cloxacillin, Dicloxacillin

Methicillin, Oxacillin, Nafcillin

Cloxacillin, Dicloxacillin

21
Q

What bugs do Penicillinase Resistant Penicillins cover?

A

Staph

Strep

22
Q

What PCNs belong to the “Aminopenicillins”?

What special ability is conferred by their structure?

A

Ampicillin (QID)/Amoxicillin(TID)

-Amino group allows for penetration into gram negative cell wall.

23
Q

What bugs do Aminopenicillins cover?

A

-Streptococcous
-Enterococcus
-Haemophilus (non-b-lactamase producing)
Salmonella/Shigella (non-b-lactamase)
-Proteus mirabilis (watch sensitivity)
-E.coli (watch sensitivity, esp if GI is the source of E.coli)
-Klebsiella (watch sensitivity)

24
Q

What is the drug of choice for Enterococcus?

A

Ampicillin (Amoxicillin if ampicillin is not available)

25
Q

Besides Hypersensitivity, what adverse effect is associated with Aminopenicillins?

What is advised to do when taking aminopenicillins?

A

Diarrhea (ampicillin worse than amoxicillin because less absorbed)

Take with food (Amoxicillin absorption not impaired)

26
Q

What PCNs belong to the “Carboxypenicillins”?

What special ability is conferred by their structure?

A

Carbenicillin
Ticarcillin

INCREASED permeability to G– cell wall.

27
Q

What bugs do Carboxypenicillins cover?

A
  • Streptococcus
  • Piddly
  • PEK
  • SPACE
  • First group in PCN family discussed that covers Pseudomonas aeruginosa*
28
Q

Which Carboxypenicillin does this describe:

  • Indanyl salt - stable oral form (Geocillin®)
  • High urine concentrations.
  • Body normally cannot tolerate high dosages necessary for concentrations to treat systemic infections.
A

Carbenicillin

29
Q

Which Carboxypenicillin does this describe:

  • more active than other carboxypenicillin against pseudomonas.
  • Na+ load = 5.2 meq/gm
A

Ticarcillin

30
Q

Why would you hesitate to prescribe Ticarcillin for a patient who has CHF or Renal insufficiency?

A

SODIUM LOAD

31
Q

Besides Hypersensitivity, what 2 other adverse effects are associated with Carboxypenicillins?

A
  • platelet dysfunction (due to Carboxy group)

- Na+ overload (use caution in hypernatremia, severe CHF, and renal failure)

32
Q

What PCNs belong to the “Ureidopenicillins”?

What is their sodium load like in comparison with Ticarcillin?

A

Piperacillin
Mezlocillin

Less than half

33
Q

What bugs do Ureidopenicillins cover?

A

Streptococcus, Enterococcus
• PEK Bugs
• SPACE Bugs

34
Q

What 3 location do anaerobes generally colonize the body?

A

Mouth
GI
Colon

35
Q

What are the 4 B-Lactamase Inhibitor/Penicillin Combinations?

A
  • Augmentin®
  • Unasyn®
  • Timentin®
  • Zosyn®
36
Q

What is Augmentin made of?

What is Unasyn made of?

What is Timentin made of?

What is Zosyn made of?

A

Amoxicillin/Clavulanic acid (PO)

Ampicillin/Sulbactam (IV)

Ticarcillin/Clavulanic acid (IV)

Piperacillin/tazobactam (IV)