9-1 Penicillins Flashcards
[B- Lactams]
A: MOA
B: [Mechanism of Resistance] (3)
C: ___-dependent Killing
C2: Whatโs the exception to this?
D: Half Life
[B- Lactams]
A: MOA =BacteriCIDAL that INHIBITS CELL WALL SYNTHESIS by inhibiting [Penicillin Binding Protein] in the cell membrane
B: [Mechanism of Resistance] = Bacteria can..
1) Alter their [Penicillin Binding Protein]
2) DEC Penetration of Abx thru [outer membrane Porin]
3) Produce [B-Lactamase]
C: TIME-DEPENDENT KILLING (exception = Enterococcus which is ALSO NOT BacteriCIDAL)
D: Half Life = 2 Hours
A: [B-Lactams] are Eliminated ______ by ______
A2: Exception: (4)
B: Any Cross-Allergenicity?
A: Eliminated UNCHANGED by Kidneys
A2: Exceptions: = โthe B Lactam PONT crew are too good for the Kidneysโ
1) cefoPerazone
2) Oxacillin = Liver Elimination
3) Nafcillin = Liver Elimination
4) cefTriaxone
B: [B-lactams ALL have (cross-allergenicity) except aztreonam]
When do [B-Lactams] have the ability to inhibit [PBP]? (i.e. when are (PBP) expressed? )
ONLY DURING BACTERIAL CELL DIVISION
[Penicillin Binding Proteins] are ONLY expressed during cell division!
Transpeptidase
A:What does it do?
B: What activates it?
Transpeptidase
A: Enzyme that allows cross-linking in the [peptidoglycan cell wall]
B: Activated by [PBP], and so when PBP is inhibited by Penicillin โ> NO TRANSPEPTIDASE
Penicillin - Semisynthetic Derivatives:
A: ParEnteral Agents: (3) List Name and [Administration Route]
B: Oral Agent
Penicillin - Semisynthetic Derivatives:
A: Parenteral agents: = BAP
- [Benzathine penicillin G -IM-LONG ACTING[
- [Aqueous penicillin G IV]
- [Procaine penicillin G IM]
B: Oral agent: Penicillin VK
MOST IMPORTANT BACTERIA THAT Natural Penicillins (penicillin G, penicillin VK) treat
A: Gram POSITIVE bacteria (4)
B: Gram negative bacteria (2)
C: AnAerobes:
D: Spirochetes:
MOST IMPORTANT BACTERIA THAT Natural Penicillins (penicillin G, penicillin VK) treat:
A: Gram POSITIVE bacteria:
- [Group streptococci]
- [streptococci viridans]
- Enterococcus
- MssA
B: Gram negative bacteria:
- Neisseria
- [Pasteurella Multocida]
C: AnAerobes:
1. Clostridium species
D: Spirochetes:
1. Treponema Pallidum
Name the 4 [[B-LactamASE] RESISTANT] Penicillin Abx Derivatives
B: How were they altered to resist [B-LactamASE]
- Nafcillin
- Oxacillin
- Methicillin (NO LONGER AVAILABLE)
- Dicloxacillin
B: Contain an Acyl side chain
PBP can be converted into [PBP2A] when the [___ gene] is encodedโ> ______!
[PBP2A] is resistant to binding of all [B-Lactams] EXCEPT ______.
PBP can be converted into [PBP2A] when the [mecA gene] is encodedโ> MRSA!
[PBP2A] is resistant to binding of all [B-Lactams] EXCEPT [CefTaRoline 5ยฐ Cef].
Aminopenicillins
A: Why were they developed?
B: What molecular change was made?
C: Examples include:
- Parenteral agent (1)
- Oral agents (2)
D: Other Clinical Usages (3)
Aminopenicillins
A: Developed to have MORE [gram-negative Aerobe] activity
B: addition of amino group
C: Examples include:
- Parenteral agent: Ampicillin
- Oral agents: Ampicillin and Amoxicillin
D: Also Used Clinically for: R U E
1) [Endocarditis Prophylaxis] in valve Dz pts
2) Respiratory infections
3) UTI
AMINOPENICILLINS (ampicillin / amoxicillin)
Gram-negative bacteria (5)
Gram POSITIVE bacteria (2)
AMINOPENICILLINS (ampicillin / amoxicillin)
Gram-negative bacteria: B-SEPS
- ฮฒL- H. influenzae
- Salmonella some
- E. coli (some)
- Proteus mirabilis
- Shigella
Gram POSITIVE bacteria:
1. Enterococcus
2 Listeria
๏ฟผ
[TICARCILLIN - Carboxypenicillins] were originally designed to _______
B: Whatโs the caveat?
C: What is its target bacteria?
[TICARCILLIN - Carboxypenicillins] were originally designed to INC activity against [gram negative Aerobes].
B: It is NO LONGER AVAILABLE.
C: Itโs target was to treat [Pseudomonas Aeruginosa]
[PIPERACILLIN- UreidoPenicillin]
A: Why were they developed?
B: What molecular change was made?
C: Examples include:
- Parenteral agent
- Oral agents
D: Other Clinical Usages (2)
[PIPERACILLIN- UreidoPenicillin]
A: Developed to have MORE [gram-negative] activity but does have coverage of both
B: Derivative of Aminopenicillin + [acyl side chain adaptation]
C: Examples include:
Parenteral ONLY
D: Other Clinical Usages:
1) [Hospital Acquired Empiric Therapy]
2) Complicated UTI
[PIPERACILLIN- UreidoPenicillin]
A: Gram-negative bacteria (5)
B: Has _____ [Good/Poor] activity with AnAerobes
๏ฟผ
[PIPERACILLIN- UreidoPenicillin]
A: Gram-negative bacteria:
โ[PIPERACILLIN- UP] PEAKS with gram negative bacteriaโ
1) **PSEUDOMONAS AERUGINOSA ***
2) EnteroBacter
3) Aminopenicillin Coverage + the other 4
4) Klebsiella (some)
5) Serratia
B: AnAerobes: GOOD ACTIVITY!
๏ฟผ
A: How do [B-LactamASE] inhibitors molecularly work?
A2: When are they used?
B: Examples (4)
C: Gram negative bacteria (2)
D: Gram POSITIVE bacteria:
E: AnAerobes:
A: Irreversibly binds to catalytic site of the [Bacteria B-LactamASE enzyme] โgags the [B-Lactamase scissors]โ
A2: Used in combo with cephalosporins
B: Ex:
1) Clavulanate
2) Sulbactam
3) Tazobactam
4) Avibactam
C: Gram negative bacteria:
- [Haemophilus Influenzae]
- Moraxella Catarrhalis
D: Gram POSITIVE bacteria:
+: [REGULAR Staph Aureus]
E: AnAerobes:
1) Bacteroides Species
A: There is No [Post Antibiotic Effect] for gram _____ bacteria treated with [____-Dependent Abx] (such as Penicillins)
B: Penicillins have Synergy with aminoglycosides against
which 4 Bacteria?
C: Most penicillins are degraded by _____ _____ ergo [Oral penicillins] are variably absorbed and concentration achieved PO are _____[lower/Higher] than IV
Pen VK absorbed **better** than \_\_\_\_\_ \_\_\_\_\_ # Amoxicillin is absorbed **better** than \_\_\_\_\_
_____ is absorbed the best of the [Penicilinase Resistant Penicillins]
A: There is No PAE for gram negative bacteria treated with [TIME-Dependent Abx] (such as Penicillins)
B: Penicillins have Synergy with [Aminoglycosides TAGS] against S E V N:
- Staph SPECIES
- Enterococcus SPECIES
- Virdans Strep
- Negative-gram bacteria
C: Most penicillins are degraded by **gastric acid,** ergo *[Oral penicillins] are variably absorbed* and concentration achieved PO are _lower_ than IV # Pen VK absorbed better than [oral Pen G] # Amoxicillin absorbed better than ampicillin # **Dicloxacillin is absorbed the best** of the PRPs
