Dr. Cluck Anti-Infective Penems and Aztreonam Flashcards
What are the Carbapenems?
Imipenem-Cilastin (Cilastatin prevents breakdown of Imipenem): has the best gram-positive coverage
Meropenem: CNS infections
Ertapenem
-> IV, IM
Spectrum of Activity - Carbapenems
Broad:
-Gram-positive: PRSP (PNC-res-strep pneumo.), MSSA, VSE
-Gram-negative: most gram-negatives (Acinetobacter, Pseudomonas)
Where do Carbapenems lack activity against microbials?
-Ertapenem (Monkey-cillin): Pseudomonas, Acinetobacter, Enterococcus spp (KNOW THIS!)
A-P-E
-All: Stenotrophomonas, Legionella, MRSA, VRE
How does Stenotrophomonas (gram-negative) neutralize Carbapenems?
They produce Metallo-ß-lactamase which hydrolyzes Carbapenems
How can Legionella be treated?
Carbapenem-resistant
Fluoroquinolone, macrolides
Which drug to use for MRSA?
The only ß-lactam that covers MRSA: Ceftaroline
What about VNC?
Which drugs cover Vancomyin-resistant microbes?
Linezolid, Daptomycin
What drug formulation is used for Carbapenems?
IV only
Pharmacokinetics of Carbapenems
-Absorption: Well absorbed
-Distribution: Well throughout the body + CSF
-Metabolism/Excretion: predominantly in the urine/no metabolism
Contraindications of Carbapenems
Hypersensitivity (not common)
Adverse effects of Carbapenems
-Seizures (almost exclusive to imipenem) - have to renal adjust !!
-C. diff infection - due to broad-spectrum activity
Drug Interactions of Carbapenems
-Probenecid - results in increased level of Carbapenems
-Valproic acid (seizures and mood stabilization): using Carbapenems simultaneously results in low levels of Valproic acid (50-80% after 24h of giving Carbapenem) - This cannot be overcome by simply increasing Valproic acid bc Carbapenem is so effective at lowering VPA - EXAM
What is the only Monobactam?
Azactam (aztreonam)
-ONLY cover anaerobic gram-negatives including Pseudomonas (but other drugs are better for Pseudomonas)
-used in PNC-allergic patients - often patients are not actually allergic and even if they can use Cephalosporin or Carbapenem
-eliminated renally
-stable to Metallo-ß-lactamases (hydrolyzes carbapenem)
EXPENSIVE
Which Mechanisms of Resistance do microbes use against Carbapenems?
-ß-lactamases
-PBP modification (binding site of drug)
-can not penetrate the outer membrane through porins anymore (porins down-regulated)
-Clearance of the drug via efflux pumps
What would be the first line to treat an infection empirically?
ß-lactams - unless a specific case is stated