Beta Lactams Flashcards

0
Q

Penicillin G and Penicillin V Clinical Uses

A
  • Penicillin G: IV form, acid labile
  • Penicillin V: oral form, acid stable
  • Bactericidal and requires actively growing organism
  • Mostly gram + (S. pneumonia, S. pyogenes, Actinomyces) and syphilis.
  • Bactericidal for gram + cocci, gram + rods, gram - cocci, and spirochetes
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1
Q

Penicillin G and Penicillin V source and MOA

A
  • Natural penicillins produced by fungus
  • Beta lactam inhibits synth of crosslinks b/t disaccharide subunits of cell wall by binding transpeptidase
  • Structural analogue of D-alanyl-D-alanine substrate transpeptidase
  • Mechanism:
    1. Bind penicillin binding proteins
    2. Block transpeptidase cross linking of peptidoglycan
    3. Activate autolytic enzymes
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2
Q

Penicillin G and Penicillin V Pharmacokinetics

A
  • Good distribution except CNS
  • Renal elimination
  • Penicillin G is acid labile and only 1/3 oral dose active
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3
Q

Penicillin G and Penicillin V Toxicities and Resistance

A
  • Tox: hypersensitivity and hemolytic anemia

- Resistance: beta lactamase cleaves beta lactam ring

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4
Q

Methacillin

A
  • Penicillinase resistant penicillin
  • Mechanism:
    1. Bind penicillin binding proteins
    2. Block transpeptidase cross linking of peptidoglycan
    3. Activate autolytic enzymes
  • Clinical use: S. aureus except MRSA
  • Resistant b/c altered penicillin binding protein target site
  • Tox: hypersensitivity rxn, intestinal nephritis
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5
Q

Nafcillin

A
  • Penicillinase resistant penicillin
  • Mechanism:
    1. Bind penicillin binding proteins
    2. Block transpeptidase cross linking of peptidoglycan
    3. Activate autolytic enzymes
  • Clinical use: S. aureus except MRSA
  • Resistant b/c altered penicillin binding protein target site
  • Tox: hypersensitivity rxn, intestinal nephritis
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6
Q

Dicloxacillin

A
  • Penicillinase resistant penicillin
  • Mechanism:
    1. Bind penicillin binding proteins
    2. Block transpeptidase cross linking of peptidoglycan
    3. Activate autolytic enzymes
  • Clinical use: S. aureus except MRSA
  • Resistant b/c altered penicillin binding protein target site
  • Tox: hypersensitivity rxn, intestinal nephritis
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7
Q

Oxacillin

A
  • Penicillinase resistant penicillin
  • Mechanism:
    1. Bind penicillin binding proteins
    2. Block transpeptidase cross linking of peptidoglycan
    3. Activate autolytic enzymes
  • Clinical use: S. aureus except MRSA
  • Resistant b/c altered penicillin binding protein target site
  • Tox: hypersensitivity rxn, intestinal nephritis
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8
Q

Ampicillin

A
  • Extended range Aminopenicillins
  • Mechanism:
    1. Bind penicillin binding proteins
    2. Block transpeptidase cross linking of peptidoglycan
    3. Activate autolytic enzymes
  • Use: H. influenzae, E. Coli, Listeria monocytogenes, Proteus mirabilis, Salmonella, Shigella, enterococci. (HELPSS)
  • Tox: Hypersensitivity rxn, ampicillin rash, psuedomembraneous colitis
  • Resistance: betal lactamases cleave beta lactam ring
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9
Q

Amoxicillin

A
  • Extended range Aminopenicillins
  • Mechanism:
    1. Bind penicillin binding proteins
    2. Block transpeptidase cross linking of peptidoglycan
    3. Activate autolytic enzymes
  • Use: H. influenzae, E. Coli, Listeria monocytogenes, Proteus mirabilis, Salmonella, Shigella, enterococci. (HELPSS)
  • Tox: Hypersensitivity rxn, ampicillin rash, psuedomembraneous colitis
  • Resistance: betal lactamases cleave beta lactam ring
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10
Q

Ticarcillin

A
  • Antipseudomonals
  • Mechanism:
    1. Bind penicillin binding proteins
    2. Block transpeptidase cross linking of peptidoglycan
    3. Activate autolytic enzymes
  • Use: Pseudomonas spp and gram - rods; use with clavulanic acid
  • susceptable to penicillinase
  • Tox: Hypersensitivity rxn
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11
Q

Carbenicillin

A
  • Antipseudomonals
  • Mechanism:
    1. Bind penicillin binding proteins
    2. Block transpeptidase cross linking of peptidoglycan
    3. Activate autolytic enzymes
  • Use: Pseudomonas spp and gram - rods; use with clavulanic acid
  • susceptable to penicillinase
  • Tox: Hypersensitivity rxn
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12
Q

Piperacillin

A
  • Antipseudomonals
  • Mechanism:
    1. Bind penicillin binding proteins
    2. Block transpeptidase cross linking of peptidoglycan
    3. Activate autolytic enzymes
  • Use: Pseudomonas spp and gram - rods; use with clavulanic acid
  • susceptable to penicillinase
  • Tox: Hypersensitivity rxn
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13
Q

Beta Lactamase Inhibitors

A
  • Clavulanic acid, sulbactam, Tazobactam

- Added to penicillin antibiotics to protect antibiotic from destruction by beta lactamase

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14
Q

Cefazolin

A
  • 1st generation cefalosporins
  • MOA: beta lactam drug that inhibits cell wall synthesis but less susceptible to beta lactamase
  • Bactericidal
  • Use: Gram + cocci, Proteus mirabilis, E. coli, Klebsiella pneumonia
  • NOT effective against listeria, atypicals, MRSA, or enterococci
  • Tox: Hypersensitivity rxn (cross hyersensitivity w/ penicillins in 5-10%)
    1. vit K deficiency
    2. Increases nephrotoxicity of aminoglycosides
    3. disulfram like rxn with alcohol
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15
Q

Cephalexin

A
  • 1st generation cefalosporins
  • MOA: beta lactam drug that inhibits cell wall synthesis but less susceptible to beta lactamase
  • Bactericidal
  • Use: Gram + cocci, Proteus mirabilis, E. coli, Klebsiella pneumonia
  • NOT effective against listeria, atypicals, MRSA, or enterococci
  • Tox: Hypersensitivity rxn (cross hyersensitivity w/ penicillins in 5-10%)
    1. vit K deficiency
    2. Increases nephrotoxicity of aminoglycosides
    3. disulfram like rxn with alcohol
16
Q

Cefoxitin

A
  • 2nd generation cefalosporins
  • MOA: beta lactam drug that inhibits cell wall synthesis but less susceptible to beta lactamase
  • Bactericidal
  • Use: Gram + cocci, H. influenzae, Enterobacter aerogenes, Neisseria Proteus mirabilis, E. coli, Klebsiella pneumonia, and Serratia marcescens
  • NOT effective against listeria, atypicals, MRSA, or enterococci
  • Tox: Hypersensitivity rxn (cross hyersensitivity w/ penicillins in 5-10%)
    1. vit K deficiency
    2. Increases nephrotoxicity of aminoglycosides
    3. disulfram like rxn with alcohol
17
Q

Cefaclor

A
  • 2nd generation cefalosporins
  • MOA: beta lactam drug that inhibits cell wall synthesis but less susceptible to beta lactamase
  • Bactericidal
  • Use: Gram + cocci, H. influenzae, Enterobacter aerogenes, Neisseria Proteus mirabilis, E. coli, Klebsiella pneumonia, and Serratia marcescens
  • NOT effective against listeria, atypicals, MRSA, or enterococci
  • Tox: Hypersensitivity rxn (cross hyersensitivity w/ penicillins in 5-10%)
    1. vit K deficiency
    2. Increases nephrotoxicity of aminoglycosides
    3. disulfram like rxn with alcohol
18
Q

Cefuroxime

A
  • 2nd generation cefalosporins
  • MOA: beta lactam drug that inhibits cell wall synthesis but less susceptible to beta lactamase
  • Bactericidal
  • Use: Gram + cocci, H. influenzae, Enterobacter aerogenes, Neisseria Proteus mirabilis, E. coli, Klebsiella pneumonia, and Serratia marcescens
  • NOT effective against listeria, atypicals, MRSA, or enterococci
  • Tox: Hypersensitivity rxn (cross hyersensitivity w/ penicillins in 5-10%)
    1. vit K deficiency
    2. Increases nephrotoxicity of aminoglycosides
    3. disulfram like rxn with alcohol
19
Q

Ceftriaxone

A
  • 3rd generation cefalosporins
  • MOA: beta lactam drug that inhibits cell wall synthesis but less susceptible to beta lactamase
  • Bactericidal
  • Use: serious gram - infections resistant to other beta lactams
    1. meningitis
    2. gonorrhea
  • NOT effective against listeria, atypicals, MRSA, or enterococci
  • Tox: Hypersensitivity rxn (cross hyersensitivity w/ penicillins in 5-10%)
    1. vit K deficiency
    2. Increases nephrotoxicity of aminoglycosides
    3. disulfram like rxn with alcohol
20
Q

Cefotaxime

A
  • 3rd generation cefalosporins
  • MOA: beta lactam drug that inhibits cell wall synthesis but less susceptible to beta lactamase
  • Bactericidal
  • Use: Serious gram - infections resistant to other beta lactams
  • NOT effective against listeria, atypicals, MRSA, or enterococci
  • Tox: Hypersensitivity rxn (cross hyersensitivity w/ penicillins in 5-10%)
    1. vit K deficiency
    2. Increases nephrotoxicity of aminoglycosides
    3. disulfram like rxn with alcohol
21
Q

Ceftazidime

A
  • 3rd generation cefalosporins
  • MOA: beta lactam drug that inhibits cell wall synthesis but less susceptible to beta lactamase
  • Bactericidal
  • Use: serious gram - infections resistant to other beta lactams
    1. Pseudomonas
  • NOT effective against listeria, atypicals, MRSA, or enterococci
  • Tox: Hypersensitivity rxn (cross hyersensitivity w/ penicillins in 5-10%)
    1. vit K deficiency
    2. Increases nephrotoxicity of aminoglycosides
    3. disulfram like rxn with alcohol
22
Q

Cefepime

A
  • 4th generation cefalosporins
  • MOA: beta lactam drug that inhibits cell wall synthesis but less susceptible to beta lactamase
  • Bactericidal
  • Use: Increased activity against pseudomonas and gram +
  • NOT effective against listeria, atypicals, MRSA, or enterococci
  • Tox: Hypersensitivity rxn (cross hyersensitivity w/ penicillins in 5-10%)
    1. vit K deficiency
    2. Increases nephrotoxicity of aminoglycosides
    3. disulfram like rxn with alcohol
23
Q

Aztreonam

A
  • monobactam resistant to beta lactamase
  • MOA: Inhibits cell wall synthesis via binding to PBP3
  • Synergistic w/ aminoglycosides
  • No cross-allergenicity w/ penicillins
  • Use: Gram - rods only
    1. No activity against gram + or anaerobes
    2. For penicillin allergic patient
    3. Pt has renal insufficiency & cannot tolerate aminoglycosides
  • Toxicity: GI upset
24
Q

Imipenem

A
  • MOA: broad spectrum beta lactamase resistant carbapenem
  • Always administered w/ cilastatin
    1. Inhibitor of renal dehydropeptidase
    2. decreases drug inactivation in renal tubules
  • Use: gram + cocci, gram - rods,
    1. Side effects limit to use in life threatening or other drugs failed
  • Tox: GI distress, skin rash, CNS (seizures) at high doses
25
Q

Meropenem

A
  • MOA: broad spectrum beta lactamase resistant carbapenem
  • Use: gram + cocci, gram - rods,
    1. Side effects limit to use in life threatening or other drugs failed
    2. Reduced risk of seizure and stable to dihydropeptidase 1
  • Tox: GI distress, skin rash, CNS (seizures) at high doses