Beta-Lactams Part 2 of 2 - Characteristics of Beta-Lactam Subclasses & Adverse Events Flashcards
Aminopenicillins
amoxicillin and ampicillin
Antipseudomonal penicillins
ticarcillin and piperacilin
Oldest penicillins developed in the 1940s
Penicillin A-Sensitive
No activity against bacteria producing penicillinase enzymes
Penicillin A-Sensitive
Active against gram-positive pathogens, but limited use due to resistance
Penicillin A-Sensitive
Used rarely, e.g., for susceptible group A. streptococci, pneumococci, Treponema pallidum, Actinomyces spp.
Penicillin A-Sensitive
Active against penicillinase-producing bacteria, especially Staphylococci
Penicillinase-Resistant Penicillins
Drugs of choice for infections due to proven methicillin-susceptible Staphylococcus aureus (MSSA).
Penicillinase-Resistant Penicillins
Penicillin A-Sensitive (treatment) example
Treatment of “strep throat” (caused by Streptococcis pyogenes)
Treatment of syphilis
Treatment of pneumonia caused by penicillin-sensitive Streptococcus pneumoniae
Penicillinase-Resistant Penicillins drug example
Methicillin, oxacillin, dicloxacillin, nafcillin
methicillin susceptibility is tested in vitro using _________
oxacillin
(Penicillinase-Resistant Penicillins) used as oral choice
Dicloxacillin
IV choice for methicillin-susceptible S. aureus (MSSA)
Nafcillin
Penicillinase-Resistant Penicillins is active against
gram-positive cocci, including penicillinase
Do not use if suspect methicillin-resistant S. aureus (MRSA)
Penicillinase-Resistant Penicillins is active against
Extended Spectrum Penicillins (± BLI combos) drugs
Amoxicillin ± clavulanate
Ampicillin ± sulbactam
Ticarcillin ± clavulanate
Piperacillin ± tazobactam
Common BLI used in clinical practice: _________________
clavulanic acid, tazobactam, and sulbactam
Addition of ________________ to Extended Spectrum Penicillins (± BLI combos) extends activity to cover beta-lactamase-producing gram-negative bacilli
beta-lactamase inhibitors (e.g., clavulanate, tazobactam, sulbactam)
Extended Spectrum Penicillins (± BLI combos)
has broader activity against _______________ rods and anaerobes
gram-negative
Used for a wide range of infections
Extended Spectrum Penicillins (± BLI combos)
Extended Spectrum Penicillins (± BLI combos)
that have variable anti-pseudomonal activity
Ticarcillin and piperacillin
very commonly used in empiric treatment of severe, polymicrobial infections
Beta-lactam + BLI combos
Clinical Uses of Penicillins
Limited use for __________ Penicillins due to resistance.
Penicillinase-Resistant Penicillins for proven ________ infections.
Extended Spectrum Penicillins for _____ infections.
- A sensitive;
- MSSA
-broader
Monobactams example
Aztreonam
Narrow-spectrum activity against gram-negatives only, including some P. aeruginosa
Aztreonams
Only active against gram-negative bacilli
Aztreonams
Aztreonams are often needs to be used in combination with _____________ in the context of empiric broad-spectrum _________ coverage for severe of polymicrobial infections
anti-gram positive agents; IV
Safe for use in penicillin/cephalosporin-allergic patients
Aztreonams
has MRSA activity, and it’s spectrum of activity is otherwise more similar to the 3rd generation
5th generation
First Generation Cephalosporins
Cefazolin, cephalexin
Narrow spectrum, mostly gram-positive coverage
First Generation Cephalosporins (Cefazolin, cephalexin)
Limited gram-negative activity
First Generation Cephalosporins (Cefazolin, cephalexin)
Used for mild skin infections and surgical prophylaxis
First Generation Cephalosporins (Cefazolin, cephalexin)
Primarily for skin/soft tissue infection caused by suscpetible organisms (e.g., MSSA)
First Generation Cephalosporins (Cefazolin, cephalexin)
Second Generation Cephalosporins
Cefaclor
Cefuroxime
Cefoxitin
Cefotetan
Slightly more gram-negative activity with variable anaerobic activity
Cefaclor, Cefuroxime, Cefoxitin, Cefotetan (Second Generation Cephalosporins)
2nd Gen Cephalosporins are active against some beta-lactamase-producing organisms such as __________ and ___________, but not _______
Klebsiella & H. influenzae; AmpC beta-lactamase)
Used for mild community-acquired pneumonia (CAP)/sinusitis (e.g., cefuroxime) and other mild community-acquired infections
Cefaclor, Cefuroxime, Cefoxitin, Cefotetan (Second Generation Cephalosporins)
Third Generation Cephalosporins
Ceftriaxone
Ceftazidime
Expanded gram-negative coverage
Third Generation Cephalosporins (Ceftriaxone, Ceftazidime)
Used for serious infections requiring IV therapy
Third Generation Cephalosporins (Ceftriaxone, Ceftazidime)
Used for hospitalized community-acquired pneumonia (CAP), meningitis, neutropenic fever
Third Generation Cephalosporins (Ceftriaxone, Ceftazidime)
the only 4th generation drug used clinically
Cefepime
4th gen cephalosporins have better activity against _________________ and ______________ family
Pseudomonas aeruginosa; Enterobacteriaceae
5th gen cephalosporins
Ceftaroline
Very active against MRSA
Ceftaroline
Ceftaroline is not active against
P. aeruginosa
Restored activity against beta-lactamase-producing gram-negative pathogens
Cephalosporin + BLI Combinations
a novel BLI that has activity against many beta-lactamases including many AmpC-producing pathogens
Avibactam
Carbapenem drugs
-Imipenem-cilastatin
-Ertapenem
-Meropenem
-Doripenem
deactivated by renal dehydropeptidases, thus is manufactured with a dehydropeptidase inhibitor called cilastain
Imipenem
Carbapenem that is not active against P. aeruginosa or Acinetobacter spp.
Ertapenem
Often reserved for severe infections thought to be polymicrobial or involving multidrug-resistant pathogens
Carbapenems
Used for complicated intra-abdominal infections, nosocomial pneumonia, etc
Carbapenems
last line of defence
carbapenem
Beta-Lactams: Adverse Effects
-Hypersensitivity
-Gastrointestinal Events
-Renal Abnormalities (rare)
-Hematological Abnormalities (rare)
-Seizures (Rare)
Hypersensitivity reaction of Beta lactams on 1-5% patients
rash
Hypersensitivity reaction of Beta lactams on <0.05% patients
serious reactions (anaphylaxis)
This ADE is less common between penicillins and cephalosporins
Hypersensitivity
There is no cross-reaction with__________
aztreonam
Beta lactams impose Possible risk of ___________-associated disease
C. difficile