Carbapenems Flashcards
Carbapenems intro
structural changes result in extended spectrum of activity and greater B lactamase stability
MOA
Bactericidal
Inhibit cell wall synthesis by binding to and inhibiting PBPs
Penetrate very well into bacterial cell wall
Mechanisms of resistance
- B-lactamase production
- Decreased permeability
- Alteration in PBPs
Carbapenem Drugs
Imipenem, Meropenem, Doripenem, Ertapenem, Meropenem-vaborbactam, imipenem-relebactam
Carabapenems gram positive aerobes coverage
Imipenem and doripenem are the best
Group streptococci
Viridans streptococci
Pen-susc-S.-Pseumoniae
Enerococcus faecalis (bacterostatic, imipenem)
Meth-susc-S. aureus
Carabapenems gram negative aerobes coverage
Doripenem and meropenem are the best
Gram negative HENPEK-CSSS
H. Influenza
Enterobacter spp.
Niessira
Pseudomonas mirabilis
E. Coli
Klebsiella
Citrobacter
Shigella
Salmonella
Serratia
Psuedomonas Aeruginosa (NOT ERTAPENEM)
Carbapenems Gram positive Anaerobes
Peptostreptococcus spp. Peptococcus spp.
Clostridium perfringens and tetani
Carbapenems Gram Negative Anaerobes
Bacteroides Spp.
True/False: Carbapenems are highly stable against many β-lactamase enzymes and are considered the drugs of choice for serious infections due to ESBL- and AmpC-producing bacteria.
True….Carbapenems are highly stable against many β-lactamase enzymes and are considered the drugs of choice for serious infections due to ESBL- and AmpC-producing bacteria
True/False: Meropenem-vaborbactam and imipenem-relebactam were developed to provide activity against KPC-producing Enterobacterales.
True….Vaborbactam and relebactam help provide activity against KPC-producing Enterobacterales including E coli, K pneumoniae and Enterobacter spp.
Pharmacology
Time dependent
Time above MIC (T>MIC)
Distribution
widely distributed into body tissues and fluids
CSF penetration - Meropenem is the best
Elimination
Primarily eliminated by kidney
Imipenem undergoes hydrolysis by DHP in the renal border to a nephrotoxic metabolite and can stop this with concurrent sure with Cilastatin
Short elimination half lives EXCEPT FOR ERTAPENEM which has half life of 4 hours
Clinical use
- empiric therapy for hospital acquired infections
- Polymicrobial infections
3, Infections due to B-lactamase producing organisms (SPICE, SPACE, ESBLs) - complicated UTI due to KPC producing enterobacterales - Mero/vabro, Imip/rele
- If psuedomonas is known or suspected can be used (NOT ERTAPENEM)
ADVERSE EFFECTS
Hypersensitivtiy reaction - If patient has reaction to penicillin that requires ICU avoid Carbapenems if patient has other reaction and does not require ICU can use carbapenems with caution
Gastrointestinal - C. Diff
Central nervous system - confusion, dizziness, hallucinations, seizures
Risk factors for seizures include preexcisting CNS disorder, high doses, renal insufficiency