antimicrobial beta lactams Flashcards
what essential for the function of beta-lactams
the beta-lactam ring
what does the side chain of the beta-lactam determine?
the antibacterial spectrum and pharmacological properties
what do beta-lactams bind
penicillin binding proteins
what do penicillin binding proteins do?
catalyze the polymerization of the glycan strand (transglycosylation) and the cross-linking between the glycan chains (transpeptidation).
what explains the differences in microbial spectrum?
the affinity of the PBP for the beta-lactam.
are beta-lactamases PBP? what are they?
yes. they are the enzymes responsible for the enzymatic destruction of beta-lactams.
how do the beta-lactam actually cause bacterial death?
they cause a build up of peptidoglycan precursors within the bacteria and this initiates autolysins.
where does gram + produce beta-lactamase
outside the cell. preemptively stopping the activity of the beta-lactam
where do gram - express beta-lactamase
located in the periplasmic space. they allow the beta-lactam into the space and then disable it.
is beta-lactamase a major cause of resistance in gram negative bacteria?
yes.
what are two other ways of gram negative beta-lactam resistance
alteration of the porins on the surface dont allow the passage of the antibiotic and alterations of PBPs (MRSA and strep. pneumoniae)
what are the natural penicillins
G and V
what are the three penicillin-resistant penicillins
oxacillin, nafcillin, dicloxacillin
what is another name for the penicillin-resistant penicillins
antistaphylococcal penicillins
what are the two aminopenicillins
ampicillin and amoxicillin
what are the two carboxy penicillins
carbenicillin and tricarcillin
name the ureidopenicillin
piperacillin
name the types of the beta-lactam
natural, antistaphylococcal, aminopenicillin, carboxypenicillin, ureidopenicillin, cephalosporins, carbapenems, monobactems.
is there a different mechanism for the different types of beta-lactam
no. the same. preventing the transpeptidation (cross-linking) of peptidoglycan layers in the cell wall by binding to PBP.
what are the half lives of the beta-lactam
short. 20 minutes. this is why they are given so frequently
how are most of the beta-lactams eliminated
through the renal route, must take into account renal insufficiency
what are the most common SE of the beta-lactam
GI and HSR. acute interstitial nephritis and drug fever. hives and rash.
what is the downfall for the beta-lactam
they lack activity against organisms without a cell wall, such as mycoplasma and chlamydia pneumonia.
do the beta-lactam have MRSA activity?
no. except for ceftaroline.
what is the antimicrobial spectrum for the natural penicillins
non-beta-lactamase producing gram +. streptococci. anaerobes (actinomyces, clostridium, prevotella, peptostreptococcus), select-gram (-) (neisseria), and syphilis.
what are the clinical uses for natural penicillins
streptococcal infections such as pharyngitis, cellulitis, endocarditis (viridans), and syphilis.
what are the adverse effects of the natural penicillins
HSR, seizures at high dose.
what is the pharmacodynamics of the natural penicillins
ADE -penicillin V is a more stable acid the G. there is wide distribution, and there is renal elimination.
antistreptococcal agents
oxacillin, nafcillin, dicloxacillin
what is the antimicrobial spectrum for the antistreptococcal
MSSA and strep
clinical uses of antistreptococcal
primarily for MSSA. it is actually superior to vancomycin for MSSA.
what to watch out for on antistreptococcal
penicillin HSR!
what is the adverse effects for oxacillin
hepatotoxicity and neutropenia
what are the adverse effects for nafcillin
hepatotoxic and neutropenic and thrombocytopenic.
do you take dicloxacillin with food?
no it decreases its availability
how are the antistreptococcal eliminated
hepatically
how does the antistreptococcal evade the bacterial resistance
they have a bulky side chain that sterically shields the beta-lactam ring. However it also prevents entry into the gram negatives so they are useless there.
what are the two aminopenicillins
amoxicillin and ampicillin
what is special about the aminopenicillins
the aminogroup aids in the hydrophobicity so that it penetrates the gram (-) cell wall. used against oral anaerobes as well.
what is the spectrum for the aminopenicillins
gram (+) (enterococcus, streptococci, and listeria). gram (-) hemophilus and E. coli.
are the aminopenicillins good at killing gram negatives
not particularly because of resistance.