Antibiotics Flashcards by emma wilkinson

beta-lactam classes

penicillin
cephalosporin
carbapenem
monobactam

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penicillin subclasses

aminopenicillin (amoxicillin, ampicillin), anti-staphylococcal penicillin (methicillin, oxacillin, nafcillin), anti-pseudomonal penicillin (ticarcillin, piperacillin)

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aminopenicillin examples

amoxicillin, ampicillin

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anti-staphylococcal penicillin examples

methicillin, nafcillin

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anti-pseudomonal penicillin examples

ticarcillin, piperacillin

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beta-lactam mechanism

binds to the penicillin binding proteins (PBPs) in the cell wall –> inhibits cross-linking of peptidoglycan

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beta-lactam resistance mechanisms

beta-lactamases
altered penicillin binding proteins (MRSA)- resistance transferred via MecA operon
decreased permeability (Pseudomonas)

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penicillin mechanism

binds to the penicillin binding proteins (PBPs) in the cell wall –> inhibits cross-linking of peptidoglycan

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penicillin resistance

beta-lactamases
altered penicillin binding proteins (MRSA)- resistance transferred via MecA operon
decreased permeability (Pseudomonas)

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cephalosporin examples

cefazolin (1st gen)
cefoxitin (2nd gen)
ceftriaxone (3rd gen)
gefepime (4th gen)
ceftaroline (MRSA active)

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monobactam examples

aztreonam

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cephalosporin mechanism

binds to the penicillin binding proteins (PBPs) in the cell wall –> inhibits cross-linking of peptidoglycan

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cephalosporin resistance mechanisms

altered penicillin binding proteins

beta lactamases

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monobactam mechanism

binds to the penicillin binding proteins (PBPs) in the cell wall –> inhibits cross-linking of peptidoglycan

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monobactam target

only have activity against gram negative aerobes (but does not include pseudomonas)

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carbapenem examples

imipenem, meropenem, ertapenem

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carbapenem mechanism

binds to the penicillin binding proteins (PBPs) in the cell wall –> inhibits cross-linking of peptidoglycan

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carbapenem resistance mechanism

decreased permeability of GNR outer membrane through loss of porins (i.e. Pseudomonas)
carbapenemases (broad spectrum beta lactamases)
carbapenem resistance enterobacteracae (CRE)

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carbapenem target

everything except MRSA, enterococci and listeria

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vancomycin mechanism

interferes with cell wall synthesis by binding to d-alanine-d-alanine

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MLS group

macrolides, clindamycin (lincosamides), streptogramins (no longer used)

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MLS group mechanism

inhibits protein synthesis by binding to the ribosome

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macrolide examples

erythromycin, clarithromycin, azithromycin

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macrolide mechanism

inhibit protein synthesis by binding to ribosome

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macrolide resistance mechanism

ribosomal methylation | drug efflux

clindamycin mechanism

inhibit protein synthesis by binding to ribosome

clindamycin resistance mechanism

ribosomal methylation

aminoglycoside examples

streptomycin, gentamicin, amikacin, tobramycin

aminoglycoside mechanism

inhibits protein synthesis by binding to ribosome

aminoglycoside resistance mechanism

enzymatic inactivation (i.e. sulfation, acetylation, phosphorylation)

tetracycline mechanism

inhibits protein synthesis by binding to ribosome

tetracycline resistance mechanism

altered ribosome | drug efflux

glycyclcycline example

tigecycline

glycyclcycline mechanism

inhibits protein synthesis by binding to ribosome

glycylcycline resistance mechanism

drug efflux

co-trimoxazole example

trimethoprim/sulfamethoxazole (TMP/SXT)

TMP/SXT mechanism

blocks biosynthesis of nucleic acids (targets folic acid formation)

TMP/SXT resistance mechanism

increased production of dihydrofolate reductase

fluoroquinolone examples

ciprofloxacin, levofloxacin, moxifloxacin

fluoroquinolone mechanism

inhibits DNA gyrase and topoisomerase

fluoroquinolone resistance mechanism

DNA gyrase/topoisomerase mutation | drug efflux

rifampin (rifamycin) mechanism

inhibits DNA dependent RNA polymerase (inhibits protein synthesis at the translation level)

rifampin (rifamycin) resistance mechanisms

mutations in the DNA dependent RNA polymerase

lipopeptide examples

daptomycin

lipopeptide mechanism

Ca2+ dependent increase in membrane permeability to potassium

oxazolidine examples

linezolid, tedizolid

oxazolidine mechanism

inhibits protein synthesis at level of ribosomal translation

polymyxin examples

polymyxin B, colistin

polymyxin mechanism

intercalates with LPS in gram negative membrane

cephalosporin target

gram negative bacteria and MRSA (ceftaroline)

ceftriaxone target

can cross the blood-brain barrier --> **use for meningitis

aminoglycoside target

gram negative only, no activity against anaerobes

fluoroquinolone benefit

very bioavailable

aminoglycoside consequence

**high toxicity to therapeutic ratio

polymyxin consequence

toxic

fidaxomicin target

only used to treat Clostridium difficile | nonabsorbable oral drug

rifampin use

always use in combination with another drug to protect rifampin

rifampin benefit

gets past biofilm layer

beta-lactam pharmacodynamics

time above MIC

aminoglycoside pharmacodynamics

peak MIC

fluoroquinolone pharmacodynamics

AUC/MIC

antibiotics used in synergy

ampicillin and aminoglycosides to treat enterococci

antifungals used in synergy

amphotericin B and flucytosine to treat cryptococcus

drugs that cross the blood-brain barrier

ceftriaxone (antibiotic), fluconazole (anti-fungal)

type 1 allergic reaction to beta-lactams

immediate hypersensitivity- IgE/mast cell mediated

type 2 allergic reaction to beta-lactams

innocent bystandard- adherence of a drug as a hapten to a cell, leads to hemolytic anemia

type 3 allergic reaction to beta-lactams

"Arthus" immune complex- serum sickness; fever, glomerulonephritis, arthritis, adenopathy

type 4 allergic reaction to beta-lactams

delayed hypersensitivity- T cell mediated, usually after 7-10 days of antibiotics; presents with a rash

antibiotics that target the cell wall

beta lactams (penicillin, cephalosporins, carbapenems, monobactam), vancomycin

antibiotics that bind the ribosome (to inhibit protein synthesis)

macrolides, clindamycin, aminoglycosides, tetracyclines, glycylcycline

antibiotics that target DNA gyrase and topoisomerase

fluoroquinolones

antibiotics that target DNA dependent RNA polymerase

rifampin

antibiotics that inhibit protein synthesis at the level of ribosomal translation

oxazolidine

antibiotics that increase membrane permeability

lipopeptides

antibiotics that intercalate with LPS

polymyxins

Antibiotics Flashcards

(75 cards)