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Anti-infectives Exam 1 > Penicillin > Flashcards

Penicillin Flashcards

1
Q

Natural Penicillins Examples with Routes

A

Penicillin G (IV)

Benzathine Penicillin (IM)

Penicillin V Potassium (PO)

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2
Q

Natural Penicillins MOA

A

Bind to penicillin binding proteins (PBPs)

Inhibit cross-linking of peptidoglycan in the cell wall -> autolysis -> cell death

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3
Q

Natural Penicillins Mechanism of Resistance

A

Beta-lactamase enzymes -> destruction of antibiotic (more common for Gram-negative)

Failure to penetrate outer membrane of bacteria and reach binding site (Gram-negative)

Pumped out of the cell via efflux pump (Gram-negative)

Alteration of binding site (Gram-positive)

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4
Q

Natural Penicillins

Gram-positive Aerobes

Good against: ___
Limited activity against___
Treatment of Choice for ___

A

Good against: Enterococcus faecalis

Limited activity against: Staphylococcus aureus

TOC: for susceptible Streptococcus spp.

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5
Q

Group A streptococcus

A

strep pyogenes

skin flora –> cellulitis

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6
Q

Group B Streptococcus

A

Strep agalactiae

Skin and vaginal flora

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7
Q

Group C, F, G Streptococcus

A

Skin flora –> cellulitis

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8
Q

Streptococcus pneumoniae

A

Respiratory flora –> pneumonia

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9
Q

Viridans Streptococcus

A

oral flora –> dental infections, endocarditis

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10
Q

Natural Penicillins

Gram Negative Aerobes

A

Minimal Activity

Some activity against: Neisseria Meningitidis

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11
Q

Natural Penicillins

Atypical

A

No activity

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12
Q

Natural Penicillins

Anaerobes

Good activity against:
TOC:
Limited activity:

A

Good activity: Gram + anaerobes (oral flora)

    • Actinomyces spp.
  • -Peptostreptococci
  • -Propionibacterium acnes (Cutibacterium acnes)

TOC: Clostridium perfringens

Limited activity: Gram - anaerobes

  • -Bacteroides fragilis
  • -Prevotella spp.
  • -Fusobactierium necrophorum
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13
Q

Natural Penicillins

Other organisms

A

TOC against spirochete, Treponema pallidum, which causes syphilis

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14
Q

Natural Penicillins

Metabolism

A

Substrate of organic transporters (OAT) 1/3

Poor penetration across BBB but with inflamed meningitis, does exceed MIC of susceptible organisms with new breakpoints (Streptococcus)

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15
Q

Natural Penicillins

Elimination: Half life

A

Half-life in normal renal function is only 30-60 minutes -> leading to frequent dosing
–> often seen dosed as 2-3 million units q4hr

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16
Q

Natural Penicillins

Elimination: Excretion

A

Excreted in urine, mostly as unchanged drug -> requires dose adjustment in renal dysfunction

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17
Q

Natural Penicillins

Adverse effects: CNS

A

Seizures at very high doses (40-100 million units/day)

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18
Q

Natural Penicillins

Adverse effects: hematologic

A

Neutropenia

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19
Q

Natural Penicillins

Adverse effects: Hypersensitivity

A

Ranges from rash/hives to anaphylaxis

Serum sickness can occur but is uncommon

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20
Q

Natural Penicillins

Adverse effects: Renal

A

Acute interstitial nephritis

Renal tubular disease

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21
Q

Natural Penicillins

Drug Interactions

A

Drugs that interact with the organic anion transporters 1/3
–Pretomanid, Teriflunomide, Fexinidazole

Probenecid

  • -Increases plasma levels of penicillin by competitively inhibiting renal tubular secretion
  • -Used as alternative dosing strategy to extend half-life and increase drug concentrations
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22
Q

Penicillinase-resistant Penicillins

Examples with Routes

A

Nafcillin (IV)
Oxacillin (IV)
Dicloxacillin (PO)

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23
Q

Penicillinase-resistant Penicillins

MOA

A

Bind to penicillin binding proteins (PBPs)

Inhibit cross-linking of peptidoglycan in the cell wall -> autolysis -> cell death

Acyl side chain prevented disruption of the beta-lactam ring

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24
Q

Penicillinase-resistant Penicillins

Gram + Aerobes

No activity:
Good activity:
TOC:

A

No activity: Enterococcus faecalis or MRSA

Good activity: penicillin-susceptible Streptococcus spp.

TOC: methicillin-susceptible Staphylococcus aureus (MSSA)

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25
Q

Penicillinase-resistant Penicillins

Gram - Aerobes

A

No activity

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26
Q

Penicillinase-resistant Penicillins

Anaerobes

A

No activity

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27
Q

Penicillinase-resistant Penicillins

Atypical

A

No activity

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28
Q

Penicillinase-resistant Penicillins

Metabolism: Nafcillin/Oxacillin

A

Nafcillin is moderate CYP3A4 inducer

Widely distributed with increased CSF penetration with meningeal inflammation

90-95% protein bound

29
Q

Penicillinase-resistant Penicillins

Elimination: Nafcillin/Oxacillin

A

Half-life only 20-60 min -> dosed every 4 hours

Excreted primarily through feces (nafcillin) and bile/urine (oxacillin) -> no renal dose adjustments

30
Q

Penicillinase-resistant Penicillins

Metabolism: Dicloxacillin

A

Moderate CYP2C19, weak CYP2C9, and weak CYP3A4 inducer

Rapid and incomplete absorption that is affected by food

Low CSF penetration

95-99% protein bound

31
Q

Penicillinase-resistant Penicillins

Elimination: Dicloxacillin

A

45 min half-life - > dosed every 6 hours

Excreted in feces and urine as unchanged drug -> no renal dose adjustments

32
Q

Penicillinase-resistant Penicillins

Adverse Effects: GI

A

Dicloxacillin

Abdominal pain, diarrhea, nausea

33
Q

Penicillinase-resistant Penicillins

Adverse Effects: Hepatic

A

nafcillin/oxacillin

Increased serum transaminases
Hepatotoxicity

34
Q

Penicillinase-resistant Penicillins

Adverse Effects: Hematologic

A

nafcillin/oxacillin

Neutropenia

35
Q

Penicillinase-resistant Penicillins

Adverse Effects: Renal

A

nafcillin/oxacillin

Acute interstitial nephritis
Renal tubular disease

36
Q

Penicillinase-resistant Penicillins

Adverse Effects: Local

A

nafcillin/oxacillin

injection site reactions
phlebitis

37
Q

Penicillinase-resistant Penicillins

Drug interactions

A

CYP3A4 substrates will be affected by Nafcillin and should be monitored
Antifungal azoles, anti-epileptics, statins, transplant medications, etc.

Dicloxacillin
Transplant medications (sirolimus, tacrolimus, mycophenolate) CYP3A4
Carbamazepine CYP3A4
Fosphenytoin/Phenytoin CYP2C19
Omeprazole CYP2C19
38
Q

Aminopenicllins

Examples and Routes

A

Ampicillin (IV)

Amoxicillin (PO)

39
Q

Aminopenicllins

MOA

A

Bind to penicillin binding proteins (PBPs)

Inhibit cross-linking of peptidoglycan in the cell wall -> autolysis -> cell death

40
Q

Aminopenicllins

Gram + aerobes

TOC:
Limited activity:
Same as penicillin against:

A

TOC: Enterococcus Faecalis and Listeria Monocytogenes

Limited Activity: Staphylococcus aureus

Same as penicillin against: Streptococcus spp. but broader

41
Q

Aminopenicillins

Gram - Aerobes

Limited activity:

A

Limited activity overall - > expanded activity compared to natural penicillins
Not active if beta-lactamase producing

E. coli and P. mirabilis can be susceptible, especially in younger patients without prior antibiotic exposure

H. influenzae is covered if beta-lactamase negative (otitis media or sinusitis)

42
Q

Aminopenicillins

Atypical

A

no activity

43
Q

Aminopenicillins

Gram + Anaerobes

A

Good activity against Gram-positive anaerobes (oral flora)

Actinomyces spp.
Peptostreptococci
Propionibacterium acnes (Cutibacterium acnes)

44
Q

Aminopenicillins

Gram - Anaerobes

A

Limited activity against Gram-negative anaerobes due to resistance

Bacteroides fragilis is considered resistant

Prevotella spp. and Fusobacterium necrophorum have high likelihood of producing beta-lactamases and being resistant

45
Q

Aminopenicillins

Gram - Anaerobes

A

Limited activity against Gram-negative anaerobes due to resistance

Bacteroides fragilis is considered resistant

Prevotella spp. and Fusobacterium necrophorum have high likelihood of producing beta-lactamases and being resistant

46
Q

Aminopenicllins

Metabolism and Elimination

Ampicillin

A

Distributes well into bile, penetration into CSF with inflamed meninges

10-18% Protein bound

Half-life 1 to 2 hours, extended up to 20 hours in anuric patients

Primarily excreted in urine as unchanged drug (∼90%) -> requires renal dose adjustment

47
Q

Aminopenicllins

Metabolism and Elimination

Amoxicillin

A

Widely distributed

20% Protein bound

Half-life 2 hours

Primarily excreted in urine as unchanged drug (∼60%) -> requires renal dose adjustment

48
Q

Aminopenicllins

Adverse Effects: GI

A

Amoxicillin

Abdominal pain, diarrhea, nausea

49
Q

Aminopenicllins

Adverse Effects: Dermatologic

A

ampicillin

Erythema multiforme
Exfoliative dermatitis
Skin rash
Urticaria

50
Q

Aminopenicllins

Adverse Effects: Hematologic

A

ampicillin

Neutropenia
Leukopenia
Anemia
Eosinophilia

51
Q

Aminopenicllins

Adverse Effects: Renal

A

Ampicillin

Acute interstitial nephritis (rare)

52
Q

Aminopenicllins

Drug Interactions

A

No significant drug interactions

53
Q

Penicillin + Beta-Lactamase Inhibitor

Examples and Routes

A

Ampicillin/sulbactam (IV)

Amoxicillin/clavulanate (PO)

Piperacillin/tazobactam (IV)

54
Q

Penicillin + Beta-Lactamase Inhibitor

MOA

A

Bind to penicillin binding proteins (PBPs)

Inhibit cross-linking of peptidoglycan in the cell wall -> autolysis -> cell death

55
Q

___ was the first beta-lactamase inhibitor

A

Clavulanic acid

56
Q

Penicillin + Beta-Lactamase Inhibitor

Gram + Aerobes

No added activity:
Added activity:
No activity:

A

No added activity: Enterococcus or Streptococcus spp.

Added Activity: S.aureus (methicillin susceptible)

No activity: MRSA

57
Q

Penicillin + Beta-Lactamase Inhibitor

Gram - Aerobes

TOC:

Activity against:

A

TOC: Amox/clav and Amp/sulb are TOC for Haemophilus influenza, Moraxella catarrhalis, Pasteurella multocida & Capnocytophaga species

Activity against: Acinetobacter baumannii, E.coli, Klebsiella, Proteus spp., psedomonas aeruginosa

58
Q

Penicillin + Beta-Lactamase Inhibitor

Gram + anaerobes

A

TOC: anaerobes that cause oral infections
Actinomyces spp.
Peptostreptococci
Propionibacterium acnes (Cutibacterium acnes)

59
Q

Penicillin + Beta-Lactamase Inhibitor

Gram - anaerobes

A

TOC:
Bacteroides fragilis,
Prevotella spp.
Fusobacterium necrophorum

Intra-abdominal infections
Diabetic foot infections

60
Q

Penicillin + Beta-Lactamase Inhibitor

Metabolism and Elimination

Sulbactam

A

Widely distributed

Protein binding: 38%

Half-life elimination: 1 to 1.3 hours

Excretion: Urine (~75% to 85% as unchanged drug) within 8 hours

61
Q

Penicillin + Beta-Lactamase Inhibitor

Metabolism and Elimination

Clavulanic Acid

A

Protein binding: ~25%

Half-life elimination: 1 hour

Excretion: Urine (25% to 40% as unchanged drug)

62
Q

Penicillin + Beta-Lactamase Inhibitor

Metabolism and Elimination

Piperacillin/tazobactam

A

Widely distributed

Protein binding: Piperacillin: ~26% to 33%; Tazobactam: 31% to 32%

6 – 9% of Piperacillin is metabolized to desethyl metabolite (weak activity)

22% of tazobactam is metabolized to an inactive metabolite

Half-life elimination: Piperacillin and tazobactam’s half-lives are 45 minutes to 1.5 hours

Piperacillin and tazobactam are primarily excreted into the urine (68% for piperacillin and 80% for tazoactam as unchanged drug)

63
Q

Penicillin + Beta-Lactamase Inhibitor

Adverse Effects: GI

A

amox/clav

Abdominal pain, diarrhea, nausea

64
Q

Penicillin + Beta-Lactamase Inhibitor

Adverse Effects: Dermatologic

A

Skin Rash

Urticaria

Pruritis

65
Q

Penicillin + Beta-Lactamase Inhibitor

Adverse Effects: Hematologic

A

Pancytopenia

Thrombocytopenia

66
Q

Penicillin + Beta-Lactamase Inhibitor

Adverse Effects: Hepatic

A

Increased LFTs

Hepatitis

67
Q

Penicillin + Beta-Lactamase Inhibitor

Adverse Effects: Renal

A

Interstitial nephritis

68
Q

Penicillin + Beta-Lactamase Inhibitor

Drug Interactions

A

Piperacillin-tazobactam + Vancomycin increases risk of nephrotoxicity

Anti-infectives Exam 1 (11 decks)

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