Beta-Lactams, Cephalosporins, Carbapenems, and Monobactams

monobactam

structurally similar to beta-lactams but lack one of the typical two rings

beta-lactams

moa: inhibit bacterial cell wall synthesis via inhibiting peptidoglycan transpeptidase

transpeptidation

beta-lactams block cross linking of peptidoglycan which is called

penicillin binding proteins

beta-lactams block cross linking by binding to _____________

bactericidal

beta-lactams: bacteriocidal or bacteriostatic

a, b, c

which of the following are mechanisms of beta-lactam resistance:

a. inactivation by beta-lactamases

b. change in drug target (penicillin binding proteins)

c. decreased concentrations in the cell (due to efflux pumps and outer membrane porin down-regulation)

false

true or false: beta-lactams care about reaching the Cp. max than amount of time over the MIC (Concentration-dependent)

renal toxicity (acute interstitial nephritis), hematological toxicity (hemolytic anemia and neutropenia), and seizures

what are the rare adverse reactions of beta-lactams

allergic reactions and GI (N/V/D)

what are the 2 general adverse reactions of beta-lactams

90%

what percent of reported penicillin allergies are not true?

what is the percent likelyhood of cross reactivity of cephalosporins to beta-lactams

what is the percent likelyhood of cross reactivity of carbapenems to beta-lactams

penicillin VK (PO) and penicillin G (IV)

what are the two natural penicillins

streptococci, enterococcus faecalis, and treponema pallidum (syphilis) (upper respiratory gram (+))

what spectrum do natural penicillins cover?

syphilis, pharngitis, endocarditis

what are the three therapeutic uses of natural penicillins

short

natural penicillins have a _______ half-life

ampicillin (IV, PO) and amoxicillin (PO)

what are the 2 aminopenicillins

streptococci, enterococcus, and H. influenzae

What is the spectrum of Aminopenicillins?

Aminopenicillins (Ampicillin/Amoxicillin)

What is the drug class of choice for enterococcal infections (e.faecalis)?

upper respiratory tract infections (pharyngitis, otitis media), dental prophylaxis for endocarditis, UTI caused by E. faecalis

what is the therapeutic use of aminopenicillins

diarrhea

there is high incidence of _________ when aminopenicillins are given orally (Amoxicillin)

oxacillin (IV), Nafcillin (IV), and dicloxacillin (PO)

what are the three antistaphylococcal penicillins

staphylococcus aureus (active vs. MSSA) and streptococci

what is the spectrum of antistaphylococcal penicillins

infections caused by MSSA

what is the therapeutic use of antistaphylococcal penicillins

endocarditis, bacteremia, skin and soft-tissue infections

what are some infections caused by MSSA

piperacillin (IV)

what is the antipsuedomonal penicillin

piperacillin

which drug has enhanced gram negative coverage compared to other penicillins

pseudomonas, streptococci, enterococci, MSSA, e. coli, Anaerobes

what is the spectrum of antipseudomonal penicillins

in combination with a b-lactamase inhibitor

what is unique about the therapeutic use of antispeudomonal penicillins and how they are used in therapy?

Psuedomonas

what do antipseudomonal penicillins (piperacillin) cover that no other penicillin does?

negative, anaerobic

addition of b-lactamse inhibitor improves gram _________ and __________ coverage because B-lactamases are inactivated

true

true or false: penicillin/B-lactamase inhibitors have great gram positive coverage (MSSA, strepto, entero), many anaerobes, and enteric gram negative robs

zosyn

Which penicillin/B-lactamase inhibitor has pseudomonas coverage (adds gram negative coverage) when no other has this coverage

no

(Yes/No) do penicillin/b-lactamase inhibitors have MRSA coverage?

nosocomial pneumonia, intra-abdominal infections, diabetic foot infections

therapeutic uses of piperacillin/tazobactam

sinusitis, otitis media, animal and human bites

what are the therapeutic uses for amoxicillin/clavulanate

penicillin and ampicillin

which penicillins should be taken 1-2 hours before a meal

piperacillin/tazobactam and nafcillin

which beta-lactams are sometimes given by extended or continuous infusion (to extend the time over MIC)

placenta

penicillins diffuse readily into most body tissues and fluids and do cross the __________

if it is inflamed

what factor makes it easier for penicillins to reach the CNS

Penicillin

The spectrum of Beta-lactamase inhibitors are based on the ___________ component

streptococcus, enterococcus, MSSA, e. coli, other gram -, anaerobes

what is the spectrum of beta-lactamase inhibitors?

antipseudomonal and beta-lactamase inhibitors

which penicillin classes cover anaerobes?

Yes

(Yes/No) do you need to adjust dosing of Beta-lactams based on renal function?

cefazolin and cephalexin

what are the 1st generation cephalosporins

S. aureus (MSSA), streptococci, and PEK (proteus, e. coli, klebsiella)

what is the spectrum of first gen cephalosporins

perioperative prohylaxis and skin and soft tissue infections

what are the therapeutic uses of 1st gen cephalosporins

cefaclor, cefprozil, cefuroxime, cefotetan, cefoxitin

what are the second generation cephalosporins

enhanced streptococci coverage compared to 1st gen, MSSA, and HNPEK (proteus, neisseria, proteus, e. coli, klebsiella)

what is the spectrum of 2nd generation cephalosporins

proteus sp, E. coli, K. pneumoniae

what does PEK stand for

haemophilis, neisseria, proteus sp, E. coli, K. pneumoniae

what does HNPEK stand for

pharyngitis, otitis media, step down therapy for community acquired pneumonia

what are the therapeutic uses of 2nd gen cephalosporins

cephamycins (cefoxitin and cefotetan)

what are the only cephalosporins reliable against anaerobics

cephamycins

what drug class is a good option for perioperative prophylaxis during intraabdominal and hysterectomy surgeries

cefotetan

which cephamycin has a MTT side chain that may cause increased risk of bleeding and have a drug interaction with alcohol

third

ceftriaxone, cefdinir, and cefixime, ceftazidime, cefotaxime, and ceftibutan are ______ generation cephalosporins

cefotaxime

this cephalopsorin is primarily used for neonates

ceftriaxone

this is eliminated both renally and via the biliary tract (cannot use in neonats)

ceftazidime

what is the noted inducer of multi--resistant organisms

ceftazidime and ceftolozane

beta-lactamase inhibitors added to __________ and ___________ to add activity against some ESBL-producing bacteria/other resistant bacteria

streptococcus pneumoniae

cefuroxime, cefdinir, cefpodoxime, cefprozil, and cefditoren are best for ________________

haemophilus influenzae

cefuroxime, cefdinir, cefpodoxime, cefprozil, cefibuten, cefixime, cefditoren are best for _______________

daily

cefixime, cefdinir, and cefibuten are dosed __________

enhanced streptococcus coverage, worse MSSA coverage, HENPECKS, and pseudomonas

what is the spectrum for third gen cephalosporins

ceftazidime

what is the only third gen cephalosporin that covers pseudomonas

haemophilis, enterobacter, neisseria, proteus sp, E. coli, citrobacter, K. pneumoniae, serratia

what does HENPECKS stand for

ceftazidime

what third gen cephalosporin has activity against pseudomonas and acinetobacter

anaerobic

third gen cephalosporins lack any significant __________ bacteria coverage

third gen cephalosporins

community acquired pneumonia, meningitis, UTIs, and gonorrhea are the therapeutics uses of:

gonorrhea

ceftriazone and cefotaxime cover...

h. influenzae

gonorrhea

meningitis

syphilis

cefepime

what is the 4th gen cephalosporin

HENPECKS + pseudomonas + acinetobacter + streptococcus + MSSA

what is spectrum for 4th gen

cefepime

_________ has better coverage against beta-lactamases than ceftriaxone and ceftazidime

HAP/VAP, febrile neutropenia, intra abdominal infections, uti

therapeutic uses of 4th gen cephalosporin

Anerobic

4th Gen cephalosporins lack _________ coverage

ceftaroline

5th gen cephalosporin

MRSA, S. pneumonia, catarrhalis, influenze, pneumonia

spectrum of 5th gen cephalosporin

community acquired pneumonia and skin and soft tissue infections

therapeutic uses of 5th gen cephalosporin

MRSA

What is Ceftaroline (5th Gen) claim to fame in regard to spectrum coverage? All other beta-lactams lack

True

(True/False) There are no significant drug-drug interactions or adverse effects of 5th generation Ceftaroline

cefiderocol

what is the siderophore cephalosporin

cefiderocol

chelate ferric ions and use bacterial iron transport systems

drug resistant gram negative (not good for positive or anaerobes)

what is the spectrum of cefiderococl

complicated UTI, HAP, VAP

therapeutic uses for cefiderocol

cefiderocol

what drug has a warning label for higher all-cause mortality in criticall ill patients with multridrug-resistant gram negatitive bacterial infections

drug resistant bugs

what is the spectrum for cephalosporins + betalactamase inhibitor

imipenem, meropenem, ertapenem

3 basic carbapenems

dehydropeptidsase

imipenem is inactivated by ___________ in the renal tubules (add cilastatin to preserve)

Cilastatin

What is typically added to Carbapenems to help preserve and reduce break down in renal tubules

MDR gram neg

In Carbapenems, the addition of relebactam or vaborbactam is used for ______ _______ _________ bacterial infections

seizures

imipenem/cilastatin/relebactam (Recarbrio) (IV) has higher risk of __________ than other beta-lactams

anaerobes, gram positve including enterococcus, and gram negatives including pseudomonas

spectrum for Imipenem's and Meropenems (Carbapenems)

ertapenem

this carbapenem is different because it does not cover pseudomonas, enterococcus, or acinetobacter

infections caused by bacteria that produce ESBLs

therapeutic use for all carbapenems

GI infections, UTIs, cellulities, pneumonia

therapeutic use for ertapenem

sepsis and other serious infections with MDR organisms

therapeutic use for meropenem and imipenem

drug resistant bugs

what is the therapeutic spectrum of a carbapenem + betalactamase inhibitor

carbapenems

what beta-lactam class is considered the BIG GUN antibiotic because it has lots of broad coverage

aztreonam

example of monobactam

gram neg only including pseudomonas

spectrum of monobactam