Beta Lactams Flashcards
What is the mechanism of action of the beta lactams?
They interfere with the synthesis of the bacterial cell wall peptidoglycan by binding to the active site of the trans-peptidase enzyme (PBP), preventing the cross-linking of terminal peptide components of the linear polymer chains.
What type of antibiotics are beta lactams?
Bactericidal
What are the 4 classes of beta lactams?
- Penicillins
- Cephalosporins
- Carbapenems
- Monobactam
What are the 4 classes of penicillins?
- Natural penicillins
- Penicillinase-resistant penicillins
- Aminopenicillins
- Anti-pseudomonal penicillins
What is the coverage for natural penicillins?
- Mostly gram-positive
- Some gram-negative microbes and spirochetes (syphilis)
What are the 2 natural penicillins?
- Penicillin G - IM, IV
- Penicillin V - PO
How are natural penicillins excreted?
Renal clearance
What is the coverage of penicillinase-resistant penicillins?
- Penicillinase-producing Staphylococci & other gram-positives
Ineffective against gram-negative organisms
How is penicillinase-resistant penicillin excreted?
Renal clearance
How is penicillinase-resistant penicillin CSF penetration?
Nil
What is the route of administration of penicillinase-resistant penicillins?
PO, IM, IV
What is the CSF penetration of natural penicillins?
Only IV aqueous penicillin G reaches effective conc.
How are beta-lactamase-resistant penicillins resistant to beta-lactamases?
They possess bulky side groups which limit the beta-lactamase accessibility to the catalytic site of action
What is the coverage for aminopenicillins?
- Broad spectrum for both gram-positives & gram-negatives
- Does not cover pseudomonas or Klebsiella
How are aminopenicillins able to exhibit activity against gram-negatives?
They possess additional hydrophilic groups, allowing their penetration into gram-negative bacteria via the porins
What is the CSF penetration for aminopenicillins?
IV ampicillin & IV amoxicillin can reach adequate CNS conc.
How are aminopenicillins excreted?
Renal clearance
What is the coverage for anti-pseudomonal penicillins?
- Greater activity against gram-negatives; especially Pseudomonas, Proteus & Klebsiella
- Also covers gram-positives
What is the CSF penetration for anti-pseudomonal penicillins?
Fairly high penetration