Antimicrobials 3-4 Flashcards
Old Cephalosporins
Cephalosporium acremonium
Nucleus of cephalosporin:
7-aminocephalosporanic acid (7-ACA)
- excellent agents for skin and soft tissue infections due to S. aureus and S. pyogenes
1st generation
• more resistant to B-lactamases and better acid stability
Cephalosporin
- DOC for many G(-) bacteria
- parenterally
3rd generation
used for UTI in pregnant women
Cefalexin
new DOC for typhoid fever
Ceftriaxone
for the treatment of community -acquired pneumonia (CAP)
Cefotaxime, Ceftriaxone
- used for the treatment of nosocomial infections
4th generation
- broad spectrum for multidrug-resistant bacteria, including P. aeruginosa
Carbapenems
B-lactamase-resistant but is deactivated by renal dehydropeptidase-I (DHP)
Imipenem
inhibits impenem degradation by dehydropeptidase
Addtion of Cilastatin
active against MRSA and Pseudomonas
5th Generation
greateractivityagainstG(+)cocci, Enterobacter, and Pseudomonas
4th generation
What are the antipseudomonal cephalosporins (useful for pseudomonads):
Cefoperazone, Cefotaxime, Ceftazidime, Ceftriaxone, Moxalactam
be used to treat respiratory tract infections in IV form
Cefuroxime
can be used to treat respiratory tract infections in PO form
Cefuroxime axetil
- from Streptomyces cattleya
Thienamycin
contributes to high protein binding and prolongs
the half-life of the drug in ertapenem
benzoic acid
+ Cilastatin: inhibits impenem degradation by dehydropeptidase. Under what brand name
Tienam®
inactive against G(+ and with moderate activity against a narrow group of G(-) bacteria, including P. aeruginosa
Monobactam
therapeutically equivalent to impenem
Meropenem
isolated from Chromobacterium violaceum
Aztreonam
Also know as “Suicide Drugs”
B-Lactamase Inhibitors
with very little to no antibacterial activity
B-Lactamase Inhibitors
+piperacillin
Tazobactam
Piperacillin + Tazobactam brand names
Tazocin®, Piptaz®, Zosyn®
- from Streptomyces clavuligerus
Clavulanic acid
Sulbactam + ampicillin brand name
Unasyn ®
Clavulanic acid + amoxicillin =
Co-amoxiclav
Co-amoxiclav brand name
Augmentin®
- irreversibly bind to and inactivate B-lactamase or penicillinase
B-Lactamase Inhibitors
Clavulanic acid + ticarcillin brand name
Timentin®
What are the suicide drugs
Clavulanic acid
Sulbactam
Tazobactam
Carbapenems drugs
Thienamycin
Meropenem
Imipenem
Ertapenem
the first cephalosporin
Cephalosporin C