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PHRM 865: Theraputics V > Lecture 7: Penicillins > Flashcards

Lecture 7: Penicillins Flashcards

Erdman's Section

1
Q

How is the MOA similar among all B-lactams?

A
  • ALL inhibit cell wall synthesis & PBPs
  • Inhibition of PBP = failed cell wall synthesis = lysis & death
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2
Q

How is the Mechanism or Resistance similar among all B-lactams?

A
  • Destoryed by B-lactamases
  • Alteration of PBP [MRSA & PRSP]
  • Decreased permeability of Gram (-) [Altered Porins]
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3
Q

How are the Pharmacodynamics similar among B-lactams?

A
  • T>MIC
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4
Q

How is the Elimination similar among all B-lactams?

A
  • Short half time [>2 hours]
  • Except Ceftriaxone, Cefotetan, Cefixime, Ertapenem
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5
Q

How is Renal Elimination similar among all B-lactams?

A
  • Unchaged by Glomerular Filration and Tubular Secretion
  • Except Nafcillin, Oxacillin, Ceftriaxone, Cefoperazone
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6
Q

How is Cross-Allergenicity similar among all B-lactams?

A
  • ALL except Aztreonam
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7
Q

What is the reason that Penicilins are Bactericidal?

A
  • Inhibit PBP = Failed Cell Wall Synthesis = Lysis & death
  • ONLY Bacteriostatic to Entercoccus
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8
Q

What are some of the “Bugs” that produce the b-lactamase?

A
  • Gram (+): Only S. Aureus
  • Gram (-): Aerobes & Anarobes
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9
Q

What are the Different Classes of Penicillins?

A
  • Natural Penicillins
  • Antistaphyococcal Penicillins
  • Aminopenicillins
  • Carboxypenicillins
  • Urediopenicillins
  • Combos
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10
Q

What are the Natural Penicillins?

A
  • Penicillin G [IV]
  • Benzathine Penicllin [IM]
  • Procaine Penicillin [IM]
  • Penicillin VK [Oral]
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11
Q

What is the spectrum of activity for the Natural penicillins?

A
  • Gram (+): Group/Virdian Strep, Most Enterococci
  • Gram (-): COCCI; Neisseria sp
  • Anaerobes: ATD & BTD
  • Trepnema Pallidum [DOC of Syphilis]
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12
Q

What is one “Bug” that Natural Penicillins do NOT cover?

A
  • Staphylococcsus
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13
Q

What is Penicillin G still considered Drug of Choice?

A
  • Group/Virdian Strep
  • Niesseria Meningitidis
  • Corynebacterium Diphtheriae
  • Bacillus Anthracis [Anthrax]
  • Clostridium Prefringens/Tetani
  • Treponema Pallidum [Syphilis]
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14
Q

What are the Antistaphylococcal Penicillins?

A
  • Nafcillin, Methicillin, Dicloxacillin
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15
Q

When a patient has “MRSA”, what does that mean for the rest of the class?

A
  • Resistant to all drugs within the class
  • BUT susecptable to all too is MSSA
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16
Q

What is the spectrum of activity for Antistaphylococcal Penicillins?

A
  • Gram (+): Group/Virdian Strep, MSSA [NOT MRSA]
  • Gram (-): Nothing
  • Anaerobes: Nothing
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17
Q

What are the Aminopenicillins that are used?

A
  • Ampicillin, Amoxicillin
18
Q

What is the spectrum of activity for Aminopenicillins?

A
  • Gram (+): Group/Viridan Strep, Entercoccus Sp., Listeria Monocytogenes
  • Gram (-): Salmonells/Shigella, H. Influenzae, E. Coli, P. Mirabilis

“SHEP”

19
Q

What is Ampicillin/Amoxicillin the Drug of Choice for?

A
  • Entercoccus sp.
  • Listeria Moncytogenes
20
Q

What are the Carboxypenicillins used?

A
  • Ticarcillin
21
Q

What is the spectrum of activity toward the Carboxypenicillins?

A
  • Gram (+): WEAK activity to Strep
  • Gram (-): Salmonella/Shigella, H. Influenzae, E. Coli, P. Mirabilis, Morgenlla Sp., Enterbacter Sp., Providenca Sp., Pseudomonas Aeruginosa

“SHEPMEPP”

22
Q

What are the Carboxypencillins NOT active against?

A
  • Klebsiella sp., Serratia sp.
23
Q

What are the Ureidopenicillins that are used?

A
  • Pipericillin

Has acyl chain = increases in cell wall penetration

24
Q

What is the spectrum of activity for the Ureidopenicillins?

Gram (+), Gram (-), Anaerobes

A
  • Gram (+): Group/Viridan Strep
  • Gram (-): Mostly Enterbacterales, S. Marcescens, Klebsiella sp., Pseduomonas Aeruginosa
  • Anaerobes: Bacteroides Fragilis
25
Q

What is important to know about how the B-lactamase inhibitors work?

A
  • Irreversibly bind to the catalytics site of the B-lactamase; inhibiting hydrolysis
26
Q

What are the B-lactamase Inhibitor Combinations that are used?

A
  • Amoxicillin/Clavulanic [Augmentin] PO
  • Ampicillin/Sulbactam [Unasyn] IV
  • Ticarcillin/Clavulanic [Timentin] IV
  • Pipercillin/Tazobactam [Zosyn] IV
27
Q

What is the spectrum of activity for B-lactamase Inhibitor combinations?

A
  • Gram (+): MSSA; not primary antistaph
  • Gram (-): Those with B-lactamase [E. Coli, Proteus sp., Klebsiella sp., H. Influenzae, M. Catarhalis, N. Gonorrhoeae]
  • Anaerobes: Baceroides Fragilis
28
Q

What are the important Pharmacodynamic Principles of Penicillins?

A
  • T>MIC
  • Bactericidal but are ONLY Bacteriostatic to Enterococcus
29
Q

What is important to know about the absorption of Pencillins?

A
  • Gedraded by gastric acid = not good for oral use; MUST do parenteral
30
Q

What are some of the speacial considerations for Absorption in Penicillins?

A
  • Natural: Pen G bad orally = Use Pen VK; Benz/Proc IM [depo]
  • Amino: Amox more bioavailable than Ampi
  • Antistaph: Dicloxcillin best bioavailability
31
Q

What is important to know about the distribution of Penicillins?

A
  • Into body tissues and fliuds [i.e.: pleural, synovial, bone, bile, placenta, pericardial
  • NOT into eye or prostate tho
32
Q

Where is one place that the concentrations of Penicillins are not good at?

A
  • CSF; they are ONLY good when HIGH DOSES are used
33
Q

What is the way that the Penicillins are eliminated?

A
  • KIDNEYS by Glomerular Secretion and Tubular Secretion
  • EXCEPT Nafcillin, Oxacillin, Pipericillin becases they are eliminated by the liver

SHORT HALF LIFE < 2 HOURS

34
Q

Which Penicillins are removed via Hemodialysis?

A
  • ALL except Nafcillin and Oxacillin
35
Q

What are some other important Pharmacologic considerations to know about the Pencillins?

A
  • SODIUM LOAD; will affect patients that have Heart Failure or Renal Dysfunction
  • Pen G = 2.0 mEq
  • Nafcillin = 2.9 mEq
  • Ticarcillin = 5.2 mEq
  • Piperacillin = 1.85 mEq
36
Q

What are the Clinical Uses for the Natural Penicillins?

A
  • Serious Infections = Pen G
  • Mild to Mod Infections = Pen VK
  • Strep Pneumoniae
  • Group/Viridan Strep [IM Benz/ PO or IM]
  • Endocarditis [IV with AG]
  • Treponema Pallidum [THE DOC]
37
Q

What are some of the clinical uses for Antistaphylococcal Penicillins/

A
  • Infection do to MSSA; skin soft tissue, endocarditis… [Nafcillin]
  • Oral Dicloxacillin for Mild to Mod
38
Q

What are the clinical uses for the Aminopenicillins?

A
  • Respiratory Tract Pathogens
  • Parenteral for Enterococcal & Listeria Monocytogenes
  • Endocarditis Prophylaxis
  • Salmonella [Amox] & Shigella [Ampi]
39
Q

What are some of the Clinical Uses for Carboxypenicillins and Ureidopenicillins?

A
  • Piperacillin is the MOST active against Pseudomonas Aeruginosa
  • Used as empiric
40
Q

What are the Adverse Effects for the Penicillins?

A
  • Hypersensitivity [Rash, Itching, Hives, Hypotension, Shock, Anaphylaxis]
  • Neurologic: for those that get a HIGH DOES without renal adjustment
  • GI [N, V, D; C.Diff]
  • Interstitial Nephritis: acts as Hapten then damages kidneys [most common with Methicillin]

PHRM 865: Theraputics V (42 decks)

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