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Penicillins
Penicillins
33
Pharmacology
Graduate
02/08/2012

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Term
What are the intracellular parasites?
Definition
Chlamydia and Rickettsia (Bartonella, Ehrlichia, Coxiella)
Shigella and Salmonella (Not obligate. Use AP + BLI)
Term
Which bugs lack accessibility of peptidoglycan?
Definition
Mycoplasma (No cell wall)
Mycobacteria (Waxy Cell Wall)
Encapsulated Bugs ( Strep. Pneumonia, H. Influenzae, N. Meningitis, Kleb. Pneumonia)
Gram Negative: OM can impede B-Lactams.
Viruses, Fungi, Protozoa (No peptidoglycan)
Term
Which Gram - Rods are destroyed in vitro, but not in vivo?
Definition
Brucella (zoonotic)
Bordatella Pertussis (whooping cough)
Term
What are "Essential" Binding Proteins?
Definition
Builders (10%)
Glycosylase Links Sugars
Peptidases links Amino Acids
Term
What are "Non-essential" binding proteins?
Definition
Digesters (90%)
90% of a Penicillin dose will be taken up by "non-essential" PBPs. We need a high enough dose so that we can still bind up the "Essential" PBPs.
Term
Reactivity of a Beta-Lactam
Definition
Ring Strain and Non-coplanar
Rxns occur by: Acid/base catalyzed, Nu, Enzyme catalyzed
Term
Toxicity of a Beta-Lactam
Definition
A free floating Beta-Lactam that the ring has opened is toxic.
Term
What are the Natural Penicillins (NP)?
Definition
Pen G and Pen V
Term
What are the Anti-staphylococcal Penicillins (ASPs)?
Definition
Methicillin, Nafcillin
Isoxazoles (Dicloxacillin, Oxacillin)
Term
What are the Amino Penicillins (APs)?
Definition
Amoxicillin
Ampicillin
Term
What are the ESPs?
Definition
Ureidos (Piperacillin, Mezlocillin, Azlocillin)
Carboxypenicillins (Ticarcillin, Carbenicillin)
Term
What do all penicillins require?
Definition
Bicyclic Ring (5 membered with sulfur next to Beta Lactam)
Amide group off of the 6th
What is different is what is connected off the carbonyl of the amide
Term
Pen G
Definition
-Original Penicillin- Benzyl Penicillin
-Limited spectrum
Term
Pen V
Definition
-Added an oxygen next to the amide
-Stabilized to gastric acid
-Limited Spectrum
Term
NP Profile
Definition
-Won't bind as well to Pseudomonas and Gram -
-Bind well to Enterococci and Listeria
-Often used in combo with an aminoglycoside
-An AP may be preferred though..
Term
Methicillin
Definition
ASP- target staphylococcal
-Kidney Toxicity
-Acid--> orally non-stable ---> IV only
Term
Nafcillin
Definition
ASP- target staphylococcal
-changed methicillin structure to be less toxic
-Acid--> orally non-stable ---> IV only
ONLY penicillin NOT primarily eliminated renally. BILIARY.
Term
Isoxazoles(Oxacillin, Cloxacillin, Dicloxacillin, Flucloxacillin)
Definition
Inductive/ Resonance withdraw added
So Acid/Orally stable, Lipophilic (distribution), and still effective against MSSA
Term
ASP Profile
Definition
All of these are effective against Staph/Strep because:
-the extra bulk prevents BLase binding affinity so it's effective against staph/strep that has BLases
-the bulk also prevents PBP binding outside of Staph and Strep
-Will also affect G+ Anaerobes
-Effective against all Strep except PBP strains of S. Pneum (PRSP)
-Not effective against Enterococci, MRSA, MRSE
-Can't get into G- rods in the first place
-You would never combine an ASP with a BLI (doesn't do anything)
Term
Ampicillin
Definition
Amino Penicillins
Increased spectrum
Low gut solubility
Acid Stable!- stays in gut and kills microflora (CDAD)
Potentially effective against Enterobacteria, but not Pseudomonas
Term
Amoxicillin
Definition
Amino Penicillins
Increased spectrum
Added a -OH to increase gut solubility
Potentially effective against Enterobacteria, though not Pseudomonas.
Term
Amino Penicillin Profile
Definition
Will need a BLI against a BLase
Staph/ Strep
Potentially effective against Enterobacteria (like E. Coli, though not Pseudomonas)
Do bind better to enterococci and Listeria
Often used in combo with aminoglycosides
Term
Carbenicillin
Definition
ESPs: Carboxy Penicillins
Di-anion. Acid added instead of base.
Renal elimination.
Takes Na with and leaves K in body
Term
Ticercillin
Definition
ESPs Carboxy Penicillins
Di-anion. Acid added instead of base.
Renal elimination.
The Di-NA salt form can be dangerous for CHF pts.
May result in hypokalemia at the ion exchange pumps in the kidney
Term
Piperacillin
Definition
ESPs: Ureido Penicillins
Gets 90% of Ureido use in USA. Others are mezlocillin and azlocillin.
IV ONLY!
Term
ESP Profile
Definition
Can be effective against many Gram - bugs
Can even target pseudomonas (though not Burholderia or Stenotrophomonas)
Pseudomonas has a modified OM that blocks entry that only ESPs can get in. Even then, a BLI is probably necessary.
**Piperacillin/Tazobactam is the preferred penicillin treatment in emergency for Pseudomonas and Enterobacteria.
Term
What are the Beta Lactamase Inhibitors?
Definition
Sulbactam- IV
Tazobactam- IV; Blocks AmpC
Clavulanic Acid- Oral
**None target C'ase**
Term
BLI Profile
Definition
Works by inhibiting BLases so that the BLactam can work.
Will work if:
-the penicillin would normally kill the bug if the bug didn't have the BLase
-if the BLI can target the BLase
-IV only will not work as an oral combination
Term
BLI Targets: NSBL's
Definition
Chew up only the Penicillins
All BLIs work
Term
BLI Targets: BSBL's
Definition
Chew up Penicillins and some Cephs.
All BLIs work
-assume enterobacteriaceae are BSBL's
Term
BLI Targets: ESBL's
Definition
Chew up all Penicillins and almost all Cephs
BLI's "sometimes" work
Term
BLI Targets: Amp C
Definition
Chew up all but Carbapenems
Only Tazo works.
Term
BLI Targets: Carbapenamases
Definition
Chew up everything.
No BLI's work
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