1. Antibiotics - Cell Envelope Flashcards

1
Q

Penicillin - Available Drugs

A

Penicillin G - IV form
Penicillin V - PO
Prototype B-Lactam antibiotic

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2
Q

Penicillin - MOA

A

Bactericidal

  1. Bind penicillin binding proteins
  2. Block transpeptidase cross-linking of peptidoglycan
  3. Activate autolytic enzymes
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3
Q

Penicillin - Clinical Use

A

GRAM + = Strep. pneumonia, Strep. pyogenes, Actinomyces

  • SYPHILIS
  • Benzathine Penicillin G for prophylaxis for syphilis
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4
Q

Penicillin - Toxicities

A

Hypersensitivity rxn, hemolytic anemia.

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5
Q

Penicillin - Resistance

A

B-Lactamase cleaves the B-Lactam ring

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6
Q

Penicillinase Resistant Penicillins - Available Drugs

A

Methicillin
Nafcillin
Dicloxacillin

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7
Q

Penicillinase Resistant Penicillins (Methcillin, Nafcillin, Dicloxacillin) - MOA

A

Bactericidal

  1. Bind penicillin binding proteins
  2. Block transpeptidase cross-linking of peptidoglycan
  3. Activate autolytic enzymes

Penicillinase resistant due to bulkier R group

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8
Q

Penicillinase Resistant Penicillins (Methcillin, Nafcillin, Dicloxacillin) - Clinical Use

A

STAPH. aureus (not MRSA)

“use NAF for STAPH”

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9
Q

Penicillinase Resistant Penicillins (Methcillin, Nafcillin, Dicloxacillin) - Toxicities

A

Hypersensitivity rxn, methicillin-interstitial nephritis

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10
Q

Penicillinase Resistant Penicillins (Methcillin, Nafcillin, Dicloxacillin) - Resistance

A

MRSA resistant due to altered PBP target site.

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11
Q

Aminopenicillins - Available Drugs

A

Ampicillin

Amoxicillin

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12
Q

Aminopenicillins (Ampicillin, Amoxicillin) - MOA

A

Bactericidal

  1. Bind penicillin binding proteins
  2. Block transpeptidase cross-linking of peptidoglycan
  3. Activate autolytic enzymes

“AmOxicillin has better Oral bioavailability”

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13
Q

Aminopenicillins (Ampicillin, Amoxicillin) - Clinical Use

A
Haemophilus influenza
E. coli
Listeria monocytogenes
Proteus mirabilis
Salmonella
Shigella
Enterococci

“Aminopenicillins HELPSS kill ENTEROCOCCI”

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14
Q

Aminopenicillins (Ampicillin, Amoxicillin) - Toxicities

A

Hypersensitivity rxn, ampicillin rash, pseudomembranous collitis

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15
Q

Aminopenicillins (Ampicillin, Amoxicillin) - Resistance

A

B-Lactamase cleaves the B-Lactam ring

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16
Q

Antipseudomonal Penicillins - Available Drugs

A

Ticarcillin
Carbenicillin
Piperacillin

“TCP - Takes Care of Pseudomonas”

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17
Q

Antipseudomonal Penicillins (Ticarcillin, Carbenicillin, Piperacillin) - MOA

A

Bactericidal

  1. Bind penicillin binding proteins
  2. Block transpeptidase cross-linking of peptidoglycan
  3. Activate autolytic enzymes
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18
Q

Antipseudomonal Penicillins (Ticarcillin, Carbenicillin, Piperacillin) - Clinical Use

A

PSEUDOMONAS spp.

Gram (-) rods

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19
Q

Antipseudomonal Penicillins (Ticarcillin, Carbenicillin, Piperacillin) - Toxicities

A

Hypersensitivity rxn

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20
Q

B-Lactamase Inhibitors - Available Drugs

A

Clavulonic Acid
Sulbactam
Tazobactam

“CAST”

21
Q

B-Lactamase Inhibitors (Clavulonic Acid, Sulbactam, Tazobactam) - MOA

A

Block activity of B-Lactamase / Penicillinase

22
Q

B-Lactamase Inhibitors (Clavulonic Acid, Sulbactam, Tazobactam) - Clinical Use

A

Added to penicillin antibiotics to protect the drug from destruction by B-lactamase / Penicillinase

23
Q

Cephalosporins - MOA

A

Bactericidal

  1. Bind penicillin binding proteins
  2. Block transpeptidase cross-linking of peptidoglycan
  3. Activate autolytic enzymes
24
Q

1st Gen. Cephalosporins - Available Drugs

A

Cefazolin

Cephalexin

25
Q

1st Gen. Cephalosporins (Cefazolin, Cephalexin) - Clinical Use

A

Gram (+) cocci
Proteus mirabilis
E. coli
Klebsiella pneumoniae

“PEcK”

26
Q

2nd Gen. Cephalosporins - Available Drugs

A

Cefoxitin
Cefaclor
Cefuroxime

27
Q

2nd Gen. Cephalosporins (Cefoxitin, Cefaclor, Cefuroxime) - Clinical Use

A
Gram (+) cocci
Haemophilus influenzae
Enterobacter aerogenes
Neisseria spp.
Proteus mirabilis
E. coli
Klebsiella pneumoniae
Serratia marcescens

“HEN PEcKS”

28
Q

3rd Gen. Cephalosporins - Available Drugs

A

Ceftriaxone
Cefotaxime
Ceftazidime

29
Q

3rd Gen. Cephalosporins (Ceftriaxone, Cefotaxime, Ceftazidime) - Clinical Use

A

Serious Gram (-) infections resistant to other B-lactams.

  • CEFTRIAXONE - MENINGITIS, GONORRHEA (treatment and prophylaxis)

CEFTAZIDIME - PSEUDOMONAS

30
Q

4th Gen. Cephalosporins - Available Drugs

A

Cefepime

31
Q

4th Gen. Cephalosporins (Cefepime) - Clinical Use

A

Increased activity against PSEUDOMONAS and Gram (+)’s

32
Q

Cephalosporins - Toxicities

A

Hypersensitivity rxn (Cross sensitivity with penicillins in 5-10% of patients)
Vitamin K deficiency
Increases nephrotoxicity of aminoglycosides
Disulfiram-like rxn with EtOH

33
Q

Cephalosporins - Resistance

A

Less susceptible to penicillinases than the penicillins.

Organisms not covered by Cephalosporins are LAME - 
Listeria
Atypicals
MRSA
Enterococci
34
Q

Aztreonam - MOA

A

Monobactam

Bind PBP3 –> Prevent cell wall synthesis

35
Q

Aztreonam - Clinical Use

A

GRAM (-) RODS ONLY

For penicillin allergic or those with renal insufficiency who cannot tolerate aminoglycosides.

36
Q

Aztreonam - Toxicities

A

Usually non-toxic
No cross sensitivity with penicillins or cephalosporins
Some GI upset

37
Q

Aztreonam - Resistance

A

Resistant to B-lactamases

38
Q

Carbapenams - Available Drugs

A

Imipenem(/Cilistatin) - Always given in combo

Meropenem

39
Q

Carbapenams (Imipenam, Meropenam) - MOA

A

Bactericidal

  1. Bind penicillin binding proteins
  2. Block transpeptidase cross-linking of peptidoglycan
  3. Activate autolytic enzymes
40
Q

Carbapenams (Imipenam, Meropenam) - Clinical Use

A

Gram (+) cocci
Gram (-) Rods
Anaerobes

Extremely wide spectrum but use limited by side effects.

41
Q

Carbapenams (Imipenam, Meropenam) - Toxicities

A

GI distress
Skin rash
CNS toxicity - seizures - at high plasma levels - (Imipenam&raquo_space; Meropenam)

42
Q

Vancomycin - MOA

A

Bactericidal

“pay 2 Dalas (dollars) for VANdalizing”

Inhibit cell wall mucopeptide formation by binding D-ala D-ala portion of cell wall precursors.

43
Q

Vancomycin - Clinical Use

A
GRAM (+) ONLY
Serious multi-drug resistant organisms
- S. aureus - MRSA
- Enterococci (not VRE)
- C. diff.
44
Q

Vancomycin - Toxicities

A
"does NOT have many problems"
Nephrotoxicity
Ototoxicity
Thrombophlebitis
diffuse flushing - red man syndrome - prevent with pre-treatment with antihistamines and slower infusion rate
45
Q

Vancomycin - Resistance

A

Change of D-ala D-ala to D-ala D-lac.

46
Q

Cell Envelope Antibiotics - Available Drugs

A
Beta Lactams
- Penicillins
- Cephalosporins
- Carbapenams
- Monobactams (Aztreonam)
- Beta Lactamase Inhibitors
Vancomycin
47
Q

Cilistatin - MOA

A

Inhibit renal dehydropeptidase I

48
Q

Cilistatin - Clinical Use

A

Administered in combination with Imipenam to prevent degradation of Imipenam in renal tubules.