B-lactam wall inhibitors Flashcards
(219 cards)
Groups of drugs that inhibit the cell wall (6)
Penicillins and aminopenicillins
B-lactamase inhibitors
Cephalosporins
Carbapenems
Monobactams
Non-B-lactam cell wall inhibitors
Natural penicillins
Benzylpenicillin (penicillin G)
Benzathine penicillin G
Procaine penicillin G
Penicillin V
Long acting natural penicillins
Benzathine penicillin G
Procaine penicillin G
Mechanism of action of natural penicillins
Inhibition of peptidoglycan synthesis by blocking the transpeptidation reaction of D-alanyl-D-alanine –> acetilation of transpeptidases by binding PBPs (bactericidal)
Benzylpenicillin Penicillin G spectrum - Gram positive bacteria
- Streptococci: Rheumatic fever, endocarditis (S. viridans, S. bovis), Group B strep prophylaxis (S. agalactiae)
- Clostridium perfringens (gas gangrene)
- S. pyogenes, S. pneumoniae (w/ vancomycin + 3rd-gen cephalosporin)
- Actinomyces israelii (agent of choice)
Benzylpenicillin Penicillin G spectrum - Gram negative bacteria
- Actinomyces israelii
- Pasteurella multocida (dog/cat bites)
- Listeria monocytogenes (agent of choice, combined with gentamicin)
- n. Meningitis
Benzylpenicillin Penicillin G spectrum - Spirochetes
- Leptospira spp. (leptospirosis)
- Treponema pallidum (syphilis)
- Borrelia burgdorferi (Lyme disease)
Adverse effects of penicillin G
- IgE-mediated hypersensitivity reactions
- Direct Coombs+ hemolytic anemia
- Drug-induced interstitial nephritis
- Impaired hemostasis
Contraindications & cautions of benzylpenicilline (Penicillin G)
- Never IV with benzathine formulation → toxicity
- Uremia or Probenecid use → toxic CNS levels → seizures
- Better CSF penetration if meninges are inflamed
Resistance mechanisms of Penicillin G (benzylpenicilline)
- Ineffective against most S. aureus & S. epidermidis
- β-lactamases (penicillinases) cleave β-lactam ring
- Mutations in PBPs → decreased binding affinity
Long acting form of penicillin G
Benzathine Penicillin G = slow absorption
Difference in uses between penicillins G
- Benzylpenicillin G = severe infections (endocarditis, meningitis, syphilis)
- Benzathine penicillin G = long term therapy or prohylaxis
- Procaine penicillin G = less frequent dosing
Main contraindication of procaine penicillin
IM ONLY NEVER IV (toxicity risk)
Procaine penicillin Spectrum – Gram-Positive Bacteria
- Rheumatic fever prophylaxis
- Left-sided endocarditis (S. viridans, S. bovis) + gentamicin
- Group B strep (S. agalactiae) intrapartum prophylaxis
- Clostridium perfringens (gas gangrene)
- Streptococcus pyogenes
- Streptococcus pneumoniae (with vancomycin + 3rd-gen cephalosporin)
- Actinomyces israelii (agent of choice)
Procaine penicillin Spectrum – Gram-Negative Bacteria
- Actinomyces israelii
- Streptobacillus moniliformis
- Pasteurella multocida (dog/cat bites)
- Listeria monocytogenes (agent of choice, with gentamicin)
Procaine penicillin Spectrum – Spirochetes
- Leptospira spp. (Leptospirosis)
- Treponema pallidum (Syphilis)
- Borrelia burgdorferi (Lyme disease)
Procaine penicillin G adverse effects
- IgE-mediated hypersensitivity reactions
- Direct Coombs+ hemolytic anemia
- Drug-induced interstitial nephritis
- Impaired hemostasis
Procaine penicillin G contraindications & cautions
- NEVER IV → Risk of Hoigné syndrome (CNS toxicity: hallucinations, seizures, anxiety, dizziness)
- Risk of CNS toxicity (seizures) in uremic patients or when combined with Probenecid
- Penetrates CSF better if meninges are inflamed
Procaine penicillin G resistance mechanisms and which are resistant microorganisms
- Ineffective against most S. aureus & S. epidermidis
- β-lactamases (penicillinases) cleave β-lactam ring
- Mutations in PBPs → decreased binding affinity
Forms of administration of penicillin G
- Benzylpenicillin G = IM, IV
- Benzathine penicillin G = IM ONLY
- Procaine penicillin G = IM ONLY
Aminopenicillins
Ampicillin
Amoxicillin
Ampicillin administration
PO and IM
Mechanism of action of ampicillin
Inhibit peptidoglycan synthesis by blocking the transpeptidation reaction of D-alanyl-D-alanine
Acylates transpeptidases by binding PBPs
Without with clavulanic acid for β-lactamase protection, ampicillin is…
Penicillinase-sensitive