Beta Lactam Antibiotics Flashcards
What is the MOA of beta lactam antibiotics?
interferes with bacterial cell wall synthesis, time dependent killing (high concentration of drug not needed)
What are the main uses of Natural Penicillins?
overall activity: gram (+)»_space;> gram (-)
-streptococci infections (groups a, b, c, f, g)
-mouth anaerobes (dental procedures)
-DRUG OF CHOICE for syphilis (treponema pallidum)
-streptococcus pneumoniae (not the best empiric choice, but could be used in targeted therapy if found susceptible)
Describe the Distribution of Natural Penicillins:
widely distributed throughout the body
What are the adverse effects of Natural Penicillins?
-rash
-anaphylaxis
-FEVER
-seizures
-GI upset (N/V)
What drugs are Natural Penicillins?
penicillin G (IV), penicillin VK (oral), penicillin benzathine/procaine (IM)
What drugs are Aminopenicillins?
ampicillin (IV/PO), amoxicillin (PO)
What are the main uses of Aminopenicillins?
-similar to natural penicillins= strep activity, mouth anaerobes
- ADDS enterococcus (not used for empiric therapy, but is first line for directed therapy)
-streptococcus pneumoniae
-ADDS gram (-): H. influenzae, E. coli, Proteus, Salmonella, Shingella
-drug of choice for listeria (ampicillin)
How are aminopenicillins eliminated?
renally eliminated, dose adjustments may need warranted
What drugs are aminopenicillin + beta lactamase inhibitor combinations?
ampicillin + sulbactam (IV), amoxicillin + clavulanate (PO)
What are the main uses of aminopenicillin + beta lactamase inhibitor?
-gram positive: adds MSSA
-gram negative: more reliable PEK (proteus, E. coli, klebsiella spp. not klebsiella aerogenes), sulbactam has activity against Acinetobacter spp.
-gut anaerobes (due to beta lactamase inhibitors
-often used to treat infection caused by animal bites
What are the adverse drug effects of aminopenicillins?
-rash/allergic reactions
-fever
-seizures (secondary to drug accumulation due to renal insufficiency)
What are the adverse drug reactions of aminopenicillins + beta lactamase inhibitors?
same SE as aminopenicillins (rash/allergic reaction, fever, seizures)
the addition of the beta lactamase inhibitor adds extended spectrum leading to increased GI side effects
What drugs are anti-pseudomonal penicillins?
piperacillin + tazobactam (IV)
What are the main uses of anti-pseudomonal penicillins?
-gram positive: streptococcus, enterococcus
-gram negative: more stable against “SPACE” bugs (serratia spp, pseudomonas spp, acinetobacter spp, citrobacter spp, enterobacter spp. including klebsiella aerogenes)
-gut anaerobes
-often used as empiric therapy for hospital/health system associated infections where multi-drug resistant gram negative organisms (especially pseudomonas spp) are suspected: febrile neutropenia, SIRS/sepsis, pneumonia, urinary tract infection/kidney infection, intra-abdominal infection
What are the adverse drug reactions of anti-pseudomonal penicillins?
-rash (steven-johnson syndrome)/allergic reaction
-C. diff
-fluid adjustment due to large amount of sodium
-fever
-interstitial nephritis (AKI)
What drugs are anti-staphylococcal penicillins?
nafcillin (IV, IM), oxacillin (IV), dicloxacillin (oral), pivmecillinam (PO)
What are the main uses of anti-staphylococcal penicillins?
-MSSA
-group A streptococcus
-dicloxacillin= skin infection
-nafcillin/oxacillin= systemic infections (bacteremia/endocarditis/osteomyelitis), nafcillin may be specifically used for CNS infections
What are the adverse drug reactions of anti-staphylococcal penicillin?
-rash/allergic reaction
-fever
-interstitial nephritis (nafcillin, oxacillin, dicloxacillin)
What is the main use of Pivmecillinam?
only approved for the use of uncomplicated UTI caused by susceptible isolates of E.coli, Proteus, Staph saprophyticus
has activity against ESBL producing organisms
What are the 5 general rules of cephalosporin generations?
-streptococcus activity increases with generation
-staph (MSSA) activity decreases with generation
-staph (MRSA) activity only exists in 5th generation
-cephalosporins have NO ACTIVITY against enterococcus
-gram negative activity increases with generation
What is the drug of choice for syphilis (Treponema pallidum)?
natural penicillin (penicillin benzathine)
What is the drug of choice for Listeria?
aminopenicillins (ampicillin/amoxicillin)
What is that main uses of 1st generation cephalosporins?
-streptococcus spp (unreliable for strep pneumoniae)
- MSSA
-PEK (proteus, e.coli, klebsiella)
What drug is used prior to GI surgeries to prevent infection?
cefazolin (1st generation cephalosporin)
What drugs are 1st generation cephalosporins?
cephalexin (oral), cefazolin (IV), cefadroxil (oral)
What is the main uses of 2nd generation cephalosporins?
-streptococcus, including strep pneumoniae
-gram negative: H. influenzae, Moraxella catarrhalis, Neisseria + PEK (HNPEKM)
What drug can cause decreased Vitamin K dependent clotting factor?
cefoxitin, use caution in combination with warfarin
What drugs are 2nd generation cephalosporins?
cefaclor (oral), cefuroxime (IV, oral), cefprozil (oral), cefoxitin (IV)
What 3rd generation cephalosporin has pseudomonas activity?
ceftazidime
What drugs are 3rd generation cephaosporins?
ceftriaxone, cefotaxime, ceftazidime (IV)
What are the main uses of 3rd generation cephalosporins?
-streptococcus spp, including strep pneumoniae
-HNPEKM
-increased gram negative to add Serratia, Shingella, Salmonella, Morganella, Providencia
-ceftazidime adds pseudomonas activity
What 3rd generation cephalosporin is excreted via biliary excretion?
ceftriaxone, avoid use in neonate patients
Why should Ceftriaxone not be infused at the same time as IV calcium?
precipitation
Describe the distribution of 3rd generation cephalosporins?
widely distributed
What beta lactamase drugs can treat Extended Spectrum Beta Lactamase bugs?
-cephalosporins + beta lactam inhibitors
-carbapenems
What drugs are 4th generation cephalosporin?
cefepime
What are the main uses of 4th generation cephalosporins?
-streptococcus spp, including strep pneumoniae
-MSSA
-HNPEKM
-gram negative: Serratia, Acinetobacter, Citrobacter, Enterobacter (also klebsiella aerogenes), Shingella, Salmonella, Morganella, Providencia
-Pseudomonas
What are the significant adverse drug effects of 4th generation cephalosporin, cefepime?
neurotoxicity, possible seizures
What drugs are 5th generation cephalosporins?
ceftaroline, ceftobiprole
What are the main uses of 5th generation cephalosporins?
-streptococcus spp, including strep pneumoniae
-MSSA +MRSA
-HNPEKM
-loses some gram negative activity from previous generation, but retains: enterobacter, morganella
What is the use of Cefiderocol?
-PEK
-acinetobacter baumannii and pseudomonas aeruginosa
-carbapenemase producing organisms
What drug should not be taken with valproic acid or its derivatives?
carbapenems
What Carbapenems have activity against Pseudomonas?
-imipenem + cilastatin
-meropenem
NOT ertapenem
What is the main uses of Carbapenems?
-streptococcus spp, including strep pneumoniae
-MSSA
-mouth anaerobes
-excellent gram negative: HNPEKM, Serratia, Citrobacter, Enterobacter, imipenem & meropenem have pseudomonas activity
-gut anaerobes
