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Pharm Test 3 > Penicillins > Flashcards

Penicillins Flashcards

1
Q

B- Lactams- Mech of Action

A

inhibitors of cell wall synthesis

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2
Q

B- Lactams- Mechs of Resistance

A

destruction by B-lactamase enzymes; alteration in penicillin binding proteins (PBPs); decreased permeability of outer cell membrane in Gram (-) bacteria

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3
Q

B-Lactams- Pharmacodynamic Properties

A

time-dependent bactericidal activity, EXCEPT AGAINST ENTEROCOCCUS SPP.

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4
Q

B-Lactams- Half-Life

A

Short elimination half-life; repeated, frequent dosing is needed for most agent to maintain concentrations above MIC (EXCEPT CEFTRIAXONE, CEFOPERAZONE, CEFOTETAN, CEFIXIME, ERTAPENEM)

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5
Q

B- Lactams- Elimination

A

Renal elimination; primarily eliminated unchanged by glomerular filtration and tubular secretion (EXCEPT NAFCILLIN, OXACILLIN, CEFTRIAXONE, CEFOPERAZONE)

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6
Q

B- Lactams- Cross-Allergenicity

A

ALL EXCEPT AZTREONAM

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7
Q

B- Lactams- Bactericidal or Bacteriostatic?

A

Bactericdal, except against Enterococcus spp. where they are bacteriostatic

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8
Q

Mechanism of Resistance to Penicillin Abx

A
  1. Production of B-lactamase enzymes
  2. Alteration in the structure of Penicillin binding proteins (PBPs= enzymes that deal w/ synthesis of cell wall); MRSA, PRSP
  3. Inability of the antibiotic to reach the PBP target due to poor penetration through the outer membrane of the bacteria (Gram (-))
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9
Q

Production of B-lactamase Enzymes

A

Most important and most common mechanism of bacterial resistance. Bacteria produces B-lactamase enzyme that hydrolyzes the B-lactam ring, inactivating the antibiotic.

  • For Gram (+), enzyme is secreted outside the cell
  • For Gram (-), enzyme is in periplasmic space
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10
Q

Natural Penicillins

A 
The first penicillins to be used clinically.
Examples:
AQUEOUS PENICILLIN G
BANZATHINE PENICILLIN G
PROCAINE PENICILLIN G
PENICILLIN VK
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11
Q

Natural Penicillin Spectrum of Activity (Penicillin G, Penicillin VK)

A

Gram (+): Group Streptococci, Viridans Strep, Bacillus anthracis, Corynebacterium spp.; very little activity against Staph spp. due to penicillinase production
Gram (-): Neisseria spp.
Anaerobes: Clostridium
Other: TREPONEMA PALLIDUM (SYPHILIS)

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12
Q

Penicillinase-Resistant Penicillins

A

Developed to resist penicillinase-producing Staph.
Examples-
Parenteral: NAFCILLIN
Oral: DICLOXACILLIN

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13
Q

Penicillinase-Resistant Penicillins Spectrum of Activity (Nafcilin, oxacillin, methicillin)

A

Gram (+): MSSA, Viridans and Group Streptococci (less activity than Pen G), No activity against Enterococcus spp., S pneumo, or MRSA
Gram (-): no activity
Anaerobes: limited

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14
Q

Aminopenicillins

A

Developed in response to the need for agents w/ Gram (-) activity. Include addition of amino group.
Examples:
Ampicillin
Amoxicillin

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15
Q

Aminopenicillins Spectrum of Activity (Ampicillin, Amoxicillin)

A

Gram (+): Enterococcus spp. (has better activity than natural penicillin), Listeria monocytogenes
Gram (-): Proteus mirabilis, some E. coli, Salmonella, Shigella, BL-H. Influenzae

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16
Q

Amino penicillins (Ampicillin, Amoxicillin) are drug of choice for…

A

Listeria monocytogenes, Enterococcus

17
Q

Carboxypenicillins

A

Developed in response to more Gram (-) resistant bacteria and increasing P. aeruginosa. Include addition of carboxyl group.
Examples: Ticarcillin (parenteral)

18
Q

Carboxypenicillins Spectrum of Activity (Carbenicillin, Ticarcillin)

A

Gram (+): marginal
Gram (-): PSEUDOMONAS AERUGINOSA, Enterobacter spp.
NOT ACTIVE AGAINST KLEBSIELLA OR SERRATIA

19
Q

Ureidopenicillins

A

Developed in response to need for even more activity against Gram (-) bacteria. Includes acyl side chain.
Examples: Piperacillin

20
Q

Ureidopenicillins Spectrum of Activity (Piperacillin, azlocillin)

A

Gram (+): viridans strep, Group strep, some Enterococcus
Gram (-): PSEUDOMONAS AERUGINOSA, SERRATIA MARCESCENS, SOME KLEBSIELLA SPP, Enterobacter sp.,
Aerobes: fairly good activity

21
Q

B-Lactamase Inhibitor Combinations

A

Contain a penicillin and a B-lactamase inhibitor. Have enhanced activity against B-lactamase producing bacteria.
Examples:
Amoxicillin/Clavulanic Acid (Augmentin), PO
Ampicillin/ Sulbactam (Unasyn), IV
Piperacillin/Tazobactam (Zosyn), IV

22
Q

B-Lactamase Inhibitor Combos (Unasyn, Augmentin, Timentin, Zosyn)

A

Gram (+): Staph. aureus (not MRSA)
Gram (-): SPICE bacteria- Serratia marcescens, P. aeruginosa, Indole-positive Proteus spp., Citrobacter spp., and Enterobacter spp.
ANAEROBES: enhanced activity against B-lactamase producing strains of B. FRAGILIS and B. FRAGILIS GROUP (DOT) organisms

23
Q

Penicillins Pharmacodynamics

A
  • Display TIME-DEPENDENT bactericidal activity
  • clinical efficacy correlates w/ TIME ABOVE MIC
  • PAE from Gram (+), not from Gram (-)
  • are BACTERICIDAL except for Enterococcus
  • BACTERICIDAL ACTIVITY (synergy) can be reached against Enterococcus by ADDING AN AMINOGLYCOSIDE
24
Q

Penicillins Distribution

A

Widely distributed in tissues & fluids.

Adequate [ ]s in CSF ONLY REACHED W/ INFLAMED MENINGES WHEN HIGH DOSES ARE USED

25
Q

Penicillins Elimination

A
  • Most are eliminated unchanged by the kidney.
  • NAFCILLIN and OXACILLIN are ELIMINATED BY THE LIVER, THUS DON’T REQUIRE ADJUSTMENT IN RENAL INSUFFICIENCY
  • ALL PENICILLINS HAVE SHORT HALF-LIVES
26
Q

Penicillins Sodium Load

A

Many parenteral penicillins contain sodium, which MUST BE CONSIDERED IN PATIENTS W/ CARDIAC OR RENAL DYSFUNCTION.
Example.
TICARCILLIN- 5.2 mEq per gram

27
Q

Natural Penicillins are drug of choice for…

A 
S. pneumoniae
Other Streptococci, including S. pyogenes
Neisseria meningitidis
Treponema pallidum
Clostridium perfringens or tetani
Actinomyces
28
Q

Penicillinase-Resistant Penicillins drug of choice for…

A

MSSA

29
Q

Carboxypenicillins and Ureidopenicillins drugs of choice for…

A

Hospital-acquired infections
Infections due to Pseudomonas aeruginosa (except Piperacillin)
Serious infections due to Gram (-) bacteria

30
Q

B-Lactamase Inhibitor Cominations drug of choice for…

A 
Polymicrobial infections (Zosyn, Unasyn, Timentin)
Empiric therapy for febrile neutropenia or hospital-acquired infections (Zosyn)
31
Q

Penicillins Adverse Effects

A
  • Neurologic- SEIZURES
  • INTERSTITIAL NEPHRITIS- (METHICILLIN, NAFCILLIN); initial manifestations may be fever, eosinophilia, pyuria, EOSINOPHILURIA, AND ABRUPT INCREASE IN SERUM CREATININE
  • PHLEBITIS (nafcillin)
  • HYPOKALEMIA (carbenicillin & ticarcillin)
  • SODIUM OVERLOAD & FLUID RETENTION (ticarcillin, piperacillin)

Pharm Test 3 (10 decks)

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