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Pharmacology > Beta-Lactam Antibiotics and other Cell Wall Synthesis Inhibitors > Flashcards

Beta-Lactam Antibiotics and other Cell Wall Synthesis Inhibitors Flashcards

1
Q

Penicillins: Limitid spectrum drugs

A
  • Penicillin G

- Penicillin V

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2
Q

Penicillins: Beta-lactamase-resistant drugs

A
  • Methicillin
  • Nafcillin
  • Oxacillin
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3
Q

Penicillins: Wider spectrum drugs

A
  • Ampicillin
  • Amoxicillin
  • Piperacillin
  • Ticarcillin
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4
Q

Penicillins: Mechanism of Action

A
  • Inhibit bacterial cell wall synthesis
  • Beta-lactam antibiotic
  • Bactericidal drugs
    1) Bind to penicillin-binding proteins (PBPs) located on the bacterial cytoplasmic membrane
    2) Inhibit transpeptidase enzymes (form part of the cell wall)
    3) Activate autolytic enzymes –> cause lesions in the bacterial cell wall
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5
Q

Penicillin G

A
  • Prototype of narrow-spectrum penicillins
  • Beta-lactamase sensitive
  • Therapy against: Common streptococci, meningococci, gram-positive bacilli, and spirochetes
  • Drug of choice for syphilis!
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6
Q

Penicillin V

A
  • Narrow-spectrum penicillin
  • Beta-lactamase sensitive
  • Used in oropharyngeal infections
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7
Q

Methicillin, Nafcillin, Oxacillin

A
  • Very-narrow spectrum penicillins
  • Beta-lactamase resistant
  • Mainly used in staphylococcal infections
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8
Q

Ampicillin, Amoxicillin

A
  • Wide-spectrum penicillins
  • Beta-lactamase sensitive
  • Used against similar pathogens as Penicillin G: Streptococci, meningococci, gram-positive bacilli, spirochetes
  • Also used against: Enterococci, Listeria monocytogenes, E. coli, Proteus mirabilis, H. influenzae, and Moraxella catarrhalis.
  • Synergistic with aminoglycosides when used against enterococci and listeria
  • Ampicillin; drug of choice against L. monocytogenes
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9
Q

Piperacillin, Ticarcillin

A
  • Wide-spectrum penicillins
  • Beta-lactamase sensitive
  • Used against several gram-negative rods: Pseudomonas, Enterobacter, and in some cases Klebsiella species
  • Synergistic action when used with aminoglycosides
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10
Q

Jarisch-Herxheimer reaction

A
  • Side effect when treatment of Syphilis with Penicillin

- Immune-reaction to bacterial components when cell wall are destroyed

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11
Q

Cephalosporins: First generation

A
  • Cefazolin

- Cephradine

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12
Q

Cephalosporins: Second generation

A
  • Cefamandole
  • Cefaclor
  • Cefotetan
  • Cefoxitin
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13
Q

Cephalosporins: Third generation

A
  • Cefoperazone
  • Cefotaxime
  • Ceftazidime
  • Ceftriaxone
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14
Q

Cephalosporins: Fourth generation

A
  • Cefepime
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15
Q

Cephalosporins: Mechanism of Action

A
  • Inhibit bacterial cell wall synthesis
  • Bactericidal drugs
  • Bind to penicillin binding proteins (PBPs) on bacterial cell membranes
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16
Q

Cefazolin, Cephalexin

A
  • First-generation cephalosporins
  • Used against gram-positive cocci (Staphylococci and common Streptococci), and drug of choice in E. coli, and K. pneumonia
  • Also used in surgical prophylaxis
17
Q

Cefotetan, Cefoxitin

A
  • Second-generation cephalosporins
  • Activity against gram-negative organisms
  • Drug of choice in E.coli, Proteus and Klebsiella
  • Used against Bacteroides fragilis
18
Q

Cefamandole, Cefaclor

A
  • Second-generation cephalosporins
  • Activity against gram-negative organisms
  • Used against H. influenza and M. catarrhalis
19
Q

Ceftazidime, Cefoperazone, Cefotaxime

A
  • Third-generation cephalosporins
  • Activity against gram-negative organisms resistant to other beta-lactam drugs
  • Ability to penetrate the blood-brain barrier (except Cefoperazone)
  • Usually reserved for treatment of serious infections (e.g. bacterial meningitis)
20
Q

Ceftriaxone

A
  • Third-generation cephalosporins
  • Increased activity against gram-negative organisms resistant to other beta-lactam drugs
  • Crosses blood-brain barrier
  • Drug of choice in gonorrhea (also Cefixime (oral))
21
Q

Cefepime

A
  • Fourth-generation cephalosporin
  • More resistant to beta-lactamases produced by gram-negative organisms - Enterobacter, Haemophilus, Neisseria, and some penicillin-resistant pneumococci
  • Activity against gram-positive and negative organisms
22
Q

Aztreonam

A
  • Monobactam
  • Inhibitor of bacterial cell-wall synthesis - bind to PBP3
  • Synergistic with Aminoglycosides
  • Resistant to beta-lactamases produced by certain gram-negative rods; Klebsiella, Pseudomonas, and Serratia
23
Q

Imipenem, Meropenem, Ertapenem

A
  • Carbapenems
  • Inhibitor of bacterial cell-wall synthesis
  • Wide activity against gram-positive cocci, gram-negative rods, and anaerobes.
  • Especially useful for infections caused by organisms resistant to other antibiotics
  • Drugs of choice for infections cause by Enterobacter
  • Imipenem is administered with cilastatin (inhibitor of renal dehydropeptidase I) which increases its plasma half-life
24
Q

Beta-lactamase inhibitors

A
  • Clavulanic acid
  • Sulbactam
  • Tazobactam
  • Most active against plasmid-encoded beta-lactamases such as those produced by gonococci, streptococci, E. coli, H. influenza
25
Q

Vancomycin

A
  • Bactericidal
  • Inhibitor of bacterial cell-wall synthesis
  • Bind to D-Ala-D-Ala terminal of the nascent peptidoglycan pentapeptide side chain and inhibits transglycosylation - prevents elongation of peptidoglycan chain
  • Resistant bacteria have replaced the terminal D-Ala by D-lactate
  • Used for serious infections cause by drug-resistant gram-positive organisms; MRSA, penicillin-resistant pneumococci, and C. difficile
  • Rapid IV infusion may cause diffuse flushing (“red man syndrome”)
26
Q

Fosfomycin

A
  • Inhibitor of bacterial cell-wall synthesis
  • Antimetabolite inhibitor of cytosolic enolpyruvate transferase –> prevents the formation of N-acetylmuramic acid (precursor for peptidoglycan chain formation)
  • Resistance occurs via decreased intracellular accumulation of the drug
27
Q

Bacitracin

A
  • Inhibitor of bacterial cell-wall synthesis - interferes with a late stage in the synthesis
  • Active against gram-positive organisms
  • Limited to topical use

Pharmacology (16 decks)

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