Lecture 7: Penicillins Flashcards by Emily Byford

How is the MOA similar among all B-lactams?

ALL inhibit cell wall synthesis & PBPs
Inhibition of PBP = failed cell wall synthesis = lysis & death

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

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

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How are the Pharmacodynamics similar among B-lactams?

T>MIC

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How is the Elimination similar among all B-lactams?

Short half time [>2 hours]
Except Ceftriaxone, Cefotetan, Cefixime, Ertapenem

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How is Renal Elimination similar among all B-lactams?

Unchaged by Glomerular Filration and Tubular Secretion
Except Nafcillin, Oxacillin, Ceftriaxone, Cefoperazone

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

ALL except Aztreonam

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What is the reason that Penicilins are Bactericidal?

Inhibit PBP = Failed Cell Wall Synthesis = Lysis & death
ONLY Bacteriostatic to Entercoccus

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

Gram (+): Only S. Aureus
Gram (-): Aerobes & Anarobes

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What are the Different Classes of Penicillins?

Natural Penicillins
Antistaphyococcal Penicillins
Aminopenicillins
Carboxypenicillins
Urediopenicillins
Combos

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What are the Natural Penicillins?

Penicillin G [IV]
Benzathine Penicllin [IM]
Procaine Penicillin [IM]
Penicillin VK [Oral]

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What is the spectrum of activity for the Natural penicillins?

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

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

Staphylococcsus

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What is Penicillin G still considered Drug of Choice?

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

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What are the Antistaphylococcal Penicillins?

Nafcillin, Methicillin, Dicloxacillin

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

Resistant to all drugs within the class
BUT susecptable to all too is MSSA

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What is the spectrum of activity for Antistaphylococcal Penicillins?

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

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What are the Aminopenicillins that are used?

Ampicillin, Amoxicillin

What is the spectrum of activity for Aminopenicillins?

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

“SHEP”

What is Ampicillin/Amoxicillin the Drug of Choice for?

Entercoccus sp.
Listeria Moncytogenes

What are the Carboxypenicillins used?

Ticarcillin

What is the spectrum of activity toward the Carboxypenicillins?

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

“SHEPMEPP”

What are the Carboxypencillins NOT active against?

Klebsiella sp., Serratia sp.

What are the Ureidopenicillins that are used?

Pipericillin

Has acyl chain = increases in cell wall penetration

What is the spectrum of activity for the Ureidopenicillins?

Gram (+), Gram (-), Anaerobes

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

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

- Irreversibly bind to the catalytics site of the B-lactamase; inhibiting hydrolysis

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

- **Amoxicillin/Clavulanic [Augmentin] PO** - **Ampicillin/Sulbactam [Unasyn] IV** - Ticarcillin/Clavulanic [Timentin] IV - **Pipercillin/Tazobactam [Zosyn] IV**

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

- 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**

What are the important Pharmacodynamic Principles of Penicillins?

- **T>MIC** - **Bactericidal** but are ONLY Bacteriostatic to Enterococcus

What is important to know about the absorption of Pencillins?

- Gedraded by gastric acid = not good for oral use; MUST do parenteral

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

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

What is important to know about the distribution of Penicillins?

- Into body tissues and fliuds [i.e.: pleural, synovial, bone, bile, placenta, pericardial - **NOT into eye or prostate tho**

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

- **CSF**; they are ONLY good when HIGH DOSES are used

What is the way that the Penicillins are eliminated?

- **KIDNEYS** by Glomerular Secretion and Tubular Secretion - **EXCEPT Nafcillin, Oxacillin, Pipericillin** becases they are eliminated by the liver | **SHORT HALF LIFE < 2 HOURS**

Which Penicillins are removed via Hemodialysis?

- **ALL** except Nafcillin and Oxacillin

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

- **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**

What are the Clinical Uses for the Natural Penicillins?

- 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] | - Mild to Mod: **Pharyngitis** -

What are some of the clinical uses for Antistaphylococcal Penicillins/

- **Infection do to MSSA**; skin soft tissue, endocarditis... [**Nafcillin**] - Oral Dicloxacillin for Mild to Mod

What are the clinical uses for the Aminopenicillins?

- Respiratory Tract Pathogens - Parenteral for **Enterococcal & Listeria Monocytogenes** - Endocarditis Prophylaxis - Salmonella [Amox] & Shigella [Ampi]

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

- **Piperacillin is the MOST active against Pseudomonas Aeruginosa** - Used as empiric

What are the Adverse Effects for the Penicillins?

- 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]

Lecture 7: Penicillins Flashcards

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