Penicillins

Front 1

Bacteriostatic vs Bacteriocidals

Back 1

-static: Prevents further prolif, lets the hosts immune system kill off organism

-cidal: Kills the organism, good for ImC

Front 2

MIC

MBC

CDKR

PAE

Back 2

MIC= Min Inhib [ ]: Lowest [ ] that stops prolif

MBC= Min Bacteriocidal [ ]; Lowest [ ] that kills 99.9%
overnight

Conc. Dependent Killing Rate: incr dose = incr killing

Post-ABx Effect: Residual Effects after Removal of ABx;
most Bacteriocidals prevent further replication by remaining bacteria for several hours

Front 3

Penicillins

Structure? Type of ABx?

Back 3

Bacteriocidal- Cell Wall Synthesis Inhibitor;

Contain 4 membered Amide N ring (B-Lactam) with joining 5 membered sulfur containg ring; alter R groups

B-Lactamase/Penicillinase cleaves the amide bond opening the ring and inactivationg it

Front 4

Penicillin MoA? Most effective?

Back 4

Bacteria constantly remodel their Cell walls .
Penicillins irreversibly Bind PBP (penicillin binding protein), inhibiting DD-Transpeptidases that are needed for the crosslinking and synthesis of the peptidoglycan cell wall and rapid cell death via autolysis. Most effective when cells are dividing/multiplying.

Front 5

Penicillin Resistance Mech(4)

Back 5

g- are naturally resistant with little peptidoglycan in CW

PBP Mutations (PBP2A-MRSA)

Change in Porin Structure: Decr Permeability

Efflux, g- pump it out of cell

Front 6

Penicillin 4 classes

Back 6

CLASSES BASED ON SPECTRUM
1. Strandard/Natural
2. Antistaphylococcal
3. Aminopenicillins
4. Antipseudomonal penicillins

Front 7

Standard/Natural Penicillins

Spectrum? (g+/g-/good for?)

Back 7

Narrow Spectrum: best against g+, aerobes, some g- cocci (strept/pneu/mening/nisseria); no g- rod coverage; susceptible to B-Lactamase

Good For Treponema Pallidum (syph)

Front 8

Benzylpenicillin

Preparation/Admin/Units? Distribution? Secretion/inhibition secretion? t1/2?

Back 8

Pen-G; (Standard Pen) Stable as a powder needs freshly prepared, 1 IU = .6ug; Acid labile, no oral, IV/IM;
no BBB unless inflammed, t1/2 = 30m
Renal Secretion via ATS: can be prolonged with Probenecid

Front 9

Probenecid

Back 9

Competes with renal tubules for Active Tubular Secretion; increased [ ] and time in blood for penicillins

Front 10

Phenoxymethyl penicillin

Admin?

Back 10

Pen-V (Standard)

Acid Stabile; can be given oral

Front 11

Benzathine/Prociane Penicillins

Effect?

Back 11

(Standard) Delayed Release/Absorption 1-4w effective

Used for Latent Syphyllis/Prophylax B-Heme Strept(RHD)

Front 12

Standard Penicillin Pk

Prego? TI? Ae? Uses? Specially good Tx?

Back 12

Prego Safe; High TI; Rash to Anaphylax

Non B-Lactamase g+, g- cocci, no g- rods, aerobes (Clostridium, Diptheria, Meningococcal)

Tx: SYPHYLLIS

Front 13

Antistaphylococcals/Penicillinase Resistant Penicillins

Spectrum (2)? 6 Drugs?

Back 13

B-Lactamase Resistent

Used against B-Lactamase producing Staph/Streptococcus only

Methicillin/Nafcillin,

Front 14

Cloxacillin

Back 14

Antistaphylococcals/Penicillinase Resistant Penicillins

Front 15

Oxacillin

Back 15

Antistaphylococcals/Penicillinase Resistant Penicillins

Front 16

Dicloxacillin

Back 16

Antistaphylococcals/Penicillinase Resistant Penicillins

Front 17

Floxacillin

Back 17

Antistaphylococcals/Penicillinase Resistant Penicillins

Front 18

Methicillin

Back 18

(Penicillinase Resistant)

Nephrotoxic, no longer used

Front 19

Nafcillin

BBB? Excretion? Tx? Resistance Development and new Tx?

Back 19

(Penicillinase Resistant)

+BBB crossing, Bile/GI Excreted,

B-Lactamase producing Staph/Streptococcus
MRSA can developed with PBP mutation to PMP2A (use Vanco)

Front 20

Aminopenicillins

B-Lactamase effect/solution? Spectrum?

Back 20

Extended Spectrums (better at penetrating g- wall)

B-Lactamase Susceptible- use inhibitors

g+, g- (E. Coli/Hemoph/Listeria/H. Pylori/Burreli/enterococci

Front 21

Ampicillin

Admin/absorbed? Secretion? Ae(2)? Tx (3)?

Back 21

Aminopenicillin; B-Lactam Sensitive; Use Sulbactam
Oral on empty stomach (food interferes)

Ae: only 50% absorbed (Possible C. Diff/DR)

Secreted via Bile/GI, some enterohepatic circulation;

Tx; Listeria Monocytogenes (meningitis), Salmonella, Shigella

Front 22

Amoxicillin

Admin/Absorbed? Secretion? Tx(3)?

Back 22

Aminopenicillin; B-Lactam Sensitive; Use Clavulonic

Oral-complete absorb (no food interf, no DR/ C. diff)
Renal Excretion;

Tx: UTI/URI/Dental Prophylax

Front 23

Clavulonic Acid
Sulbactam
Tazobactam

Who are they paired with (4)? Why?

Back 23

B-Lactamase Inhibitors; Pairing based on similar kinetics
Amoxicillin + Clavulonic = (Augmentin) (ORAL)
Ticarcillin + Clavulonic
Ampicillin + Sulbactam
Piperacillin + Tazobactam

Front 24

Antipseudomonal Penicillins

Back 24

Extended Spectrum; B-Lactamase Sensitive

Carboxys: Ticarcillin, Carbenicillin
Ureidopenicillins: Piperacillin/Azlocillin/Mezlocillin

Front 25

Ticarcillin/Carbenicillin

Tx? Ae (1)?

Back 25

Antipseudomonal Pens; B-Lact Sens, use Clavulonic

Good For Nosocomial Pseudomonas(CF/Burn Victims)

Ae: High Doses can cause platelet interference and Bleeding

Front 26

Pipercillin/Mezlocillin/Azlocillin

Paired with (2)? Tx: (1)?

Back 26

Antipsuedomonals; B-Lact Sens; Use Tazobactam

Pseudomonas/E. Coli

Often used with Aminoglycosides/Fluoroquinelones for extra-urinary tract infections of Pseudomonas/E. Coli

Front 27

ALL Penicillin Allergies

Major Antigenic Determinant>?

Food Effect on Penicillins?

Back 27

Hypersensitivies: Rash to Anaphylaxis (.01%)

Antigenic Determinant: Penicillinoic acid

Food Interferes with absorption of all (except Amoxicillin)

Front 28

Jarische-Herxheimer Rxn


Who? Why? Progression?

Back 28

Allergic reaction seen after injecting penicillins into a sencondary syphillus PT:

HypoTN, FV, Malaise, Joint Pain

CONDITION is benign Tx does not have to be stopped