penicillins Flashcards
(36 cards)
Natural Penicillins
Aqueous Penicillin G
Benzathine Penicillin
Procaine Penicillin G
Penicillin VK
Penicillinase-Resistant Penicillins
Nafcillin
Oxacillin
Methicillin
Dicloxacillin
Aminopenicillins
Ampicillin
Amoxicillin
Carboxypenicillins
Ticarcillin
Ureidopenicillins
Piperacillin
B-Lactamase Inhibitor Combinations
Ampicillin-Sulbactam (Unasyn)
Amoxicillin-Clavulanate (Augmentin)
Ticarcillin-Clavulanate (Timentin)
Piperacillin-Tazobactam (Zosyn)
Mechanism of action of B-Lactam Antibiotics
Inhibitors of cell wall synthesis
Mechanisms of Resistance of B-Lactam Antibiotics
Destruction of B-lactamase enzymes
Alteration in PBPs
Decreased permeability of outer cell membrane in Gram(-) bacteria
Pharmacodynamic Properties fo B-Lactams
Display time-dependent (T>MIC) bactericidal activity
Bacterial Exception to Pharmacodynamic Properties of B-Lactams
Enterococcus spp.
Elimination half-life of B-Lactams
<2 hours
Repeated, frequent dosing is needed for most B-Lactams to maintain serum concentrations above the MIC of the infecting bacteria for an adequate amount of time
Exceptions to the short elimination half-life in B-Lactams
Ceftriaxone
Cefotetan
Cefixime
Ertapenem
B-Lactam elimination route
Renal elimination
Primarily eliminated unchanged by glomerular filtration and tubular secretion
Exemptions to renal elimination of B-Lactams
Nafcillin
Oxacillin
Ceftriaxone
Cefoperazone
Cross-allergenicity of B-Lactam
All have risk of cross allergenicity
Exception to cross-allergenicity in B-Lactams
All except aztreonam
Classes of B-Lactams
Penicillins
Cephalosporins
Carbapenems
Monobactams
Penicillins shared chemical structure
5-membered thiazolidine ring connected to a B-lactam ring
What is different among the groups of penicillins and what does that do?
The side chains differ among the groups of penicillins
What it does:
Different antibacterial spectrums
Different pharmacokinetic properties
Greater B-lactamase stability
MOA of Penicillins
Interfere with bacterial cell wall synthesis by binding and inhibiting enzymes (PBPs), which are located in the cell wall of bacteria and are primarily expressed during cell division
PBPs that regulate the synthesis, assembly, and maintenance of peptidoglycan (cross-linking of the cell wall)
Transpeptidases
(cross-linking of the cell wall)
Carboxypeptidases
(breaks down proteins and peptides into smaller peptides)
Endopeptidases
(Break peptide bonds)
Penicillins are bactericidal or bacteriostatic?
Bactericidal
Except against Enterococcus spp., where they are bacteriostatic
Most common B-Lactamse resistance:
Production of B-lactamase enzymes
Production of b-lactamase enzymes occurs in what Gram(+) aerobe?
Staphylococcus aureus