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Host Defense - Antibiotics
NA
116
Medical
Graduate
10/31/2013

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Term
Name 2 alternative antibiotics to oxacillin and vancomycin
Definition
– Linezolid
– Quinupristin/dalfopristin
Term
Name 2 older antibiotics that may still work on CA-MRSA
Definition
– Tetracycline
– Clindamycin
Term
Name four beta lactam antibiotics
Definition
Penicillium
Cephalosporium
Monobactam
Carbapenem
Term
The core of penicillin is ________. For PCN it's called the _______ ring. For cephalosporin it's called __________ ring .
Definition
6-aminopenicillianic acid
Beta lactam ring
thiazolidine ring
Term
Semisynthetic penicillins contain ____________ which differentiate them from natural PCNs
Definition
side chain radicals
Term
Penicillin G is __________, _______, and has (narrow/wide) spectrum. Penicillin V is ___________, ______, and has (narrow/wide) spectrum.
Definition
acid labile, high potency, narrow spectrum
acid stable, low potency, narrow spectrum
Term
Penicillin G/V works against what?
Definition
Gram + bacilli and cocci
Gram - cocci
spirochetes (syphilis)
Term
Semisynthetic PCNs are used because they have increased stability to __________, increased __________, and resistance to _________.
Definition
stomach acid
increased spectrum of activity
resistance to B-lactamase
Term
How does Penicillin work?
Overall effect is _______________
Definition
Interferes with peptidoglycan synthesis and activates autolytic enzymes
bactericidal
Term
What are two side effects of penicillin and why?
Definition
Hypersensitivity due to allergic rxn by host
GI issues due to disruption of normal flora
Term
What enzymes can the bacteria produce to become penicillin resistance?
Definition
B-lactamase
Term
What is extended-spectrum B-lactamases (ESBLs)
Definition
B-lactamase that can break down all B-lactam rings
Term
PCN resistance can come from altered __________ and ___________ which will slow the influx of PCN into cells
Definition
altered cell wall formation
efflux pumps
Term
PCN resistance can come from mutation of _______
Definition
Penicillin binding proteins
Term
PCN resistance can come from tolerance. Explain tolerance.
Definition
Low MIC, High MBC (easily stopped from replicating, hard to kill bacteria)
Term
The nucleus of cephalosporins are __________ composed of a ________ ring
Definition
7-aminocephalosporanic acid
dihydrothiazine ring
Term
Cephalosporins will work against what bacteria?
Definition
Gram + and Gram - (broad spectrum)
Term
___% of patients allergic to PCN are also sensitive to cephalosporins
Also, GI stress occurs because _______
Definition
10%
disruption of normal flora
Term
What enzyme can bacteria produce to become resistant to cephalosporins
Definition
cephalosporinase - breaks down dihydrothiazine ring
Term
Name 3 B-lactamase inhibitors
Definition
Clavulanic acid
Sulbactam
Tazobactam
Term
Clavulanic acid + amoxicillin = _____________
Sulbactam + Ampicillin = _____________
Tazobactam + Piperacillin = ___________
Definition
Augmentin
Unasym
Zosyn
Term
2 other Beta lactam antibiotics __________ which is (narrow/broad) and __________ which is (narrow/broad)
Definition
Carbapenems (broad)
Monobactam (narrow)
Term
Give the carbapenems (DIEM)
Definition
doripenem
imipenem
ertapenem
meropenem
Term
Give the monobactam
Definition
aztreonam
Term
What is the mechanism of action of vancomycin
Definition
Inhibits linking of polypeptide and is bactericidal
Term
Vancomycin works against ________ and is (narrow/broad)-spectrum because ______.
Definition
gram + bacteria
narrow
Vancomycin is too large to cross outer cell membrane of gram-neg
Term
Bacitracin mechanism of action?
Definition
Inhibits transfer of peptidoglycan precursors and is bactericidal
Term
Bacitracin is (narrow/broad)
It is applied by ______ application and _____ admin
side effect?
Definition
narrow
topical and oral
nephrotoxic
Term
Mycobacterial infections are treated with what? These are always used ________ to prevent ___________.
Definition
isoniazid, ethionamid, ethambutol, cyclserine
combo
microbial resistance
Term
Mammalian cells have ______ ( _____ + ______) ribosomes. Bacterial cells have _______ (_______+________) ribosomes
Definition
80S = 60S + 40S
70S = 50S + 30S
Term
30S ribosomal subunit contains ____________
50S ribosomal subunit contains _________________
Definition
amino-acyl transfer RNA
linking of amino acids
Term
What is the mechanism of action of aminoglycosides?
Definition
irreversible binding to 30S ribosome subunit and bactericidal
Term
Aminoglycosides are not active under _______ conditions bc ________________.
Definition
anaerobic conditions
uptake of aminoglycosides is O2 dependent
Term
Aminoglycosides leads to what 3 things
Definition
Failure to initiate protein synthesis
failure to elongate proteins
deformed proteins
Term
Aminoglycosides are ______ absorbed and must be given ________.
Definition
poorly absorbed
intravenously
Term
Aminoglycosides are (narrow/broad) spectrum and function against ...?
Definition
narrow
Gram-neg bacteria but no anaerobic
Term
Two side effects of aminoglycosides
Definition
ototoxicity (CNVIII)
nephrotoxicity
Term
Resistance of aminoglycosides can occur through enzyme modification of ...?
Definition
Acetyltransferase
phosphotransferase
nucleotidyltransferase
Term
Resistance to aminoglycosides can occur by decreased __________, increased ____________ or mutation of _________
Definition
uptake
expulsion
binding site
Term
What is the mechanism of action for tetracyclines
Definition
reversible binding to 30S ribosomal subunit and bacteriostatic
Term
Tetracyclines are (narrow/broad)-spectrum and can kill ....
Definition
VERY broad
Gram + or neg., aerobes and anaerobes
Term
What are the side effects of tetracycline
Should NOT be used in ___________ or ___________
Definition
Discoloration and abnormal growth of teeth and bone
GI discomfort
not to be used in pregnant women or children
Term
What are 4 mechanisms of resistance to tetracycline
Definition
Less permeable
active efflux of tetracycline
alteration of ribosomal binding site
enzymatic modification
Term
What is the MOA of Chloramphenicol
Definition
Reversible binding of 50S ribosomal subunit and bacteriostatic
Term
Side effects of chloramphenicol
Which is dose-related
Definition
Reversible bone marrow depression (anemia, leukopenia, thrombocytopenia) - dose related
Aplastic anemia --> fatal
Term
What is the mechanism of resistance for chloramphenicol
Definition
Acetyltransferase
mutations to alter outer membrane porins
Term
Name the two types of macrolides
Definition
erythromycin derivatives
ketolide derivatives
Term
Name erythromycin derivatives of macrolides
Definition
Clarithromycin, Azithromycin, & Roxithromycin
Term
Name ketolide derivatives of macrolides
Definition
Telithromycin
Term
What is the MOA of macrolides
Definition
binds to 50S ribosomal subunit and bacteriostatic
Term
Most ______ bacteria are resistant to _____________
Definition
gram-neg
erythromycin
Term
Erythromycin is (narrow/broad)
Definition
broad
Term
Side effect to erythromycin is...
Definition
GI distress
Term
Name two mechanisms of resistance to erythromycin
Definition
Alteration of 50S subunit
Esterase
Term
Name a lincosamide
Definition
Clindamycin
Term
MOA of lincosamides.
They kill _________ bacteria
Definition
Binding 50S ribosomal subunit and bacteriostatic
anaerobic
Term
Lincosamides are notorious for what side effect?
Definition
GI disruptions
Term
Mechanism of resistance for lincosamides?
Definition
Altering the 50S subunit
Term
_________ is a streptogramin antibiotic that combines ______ and _____
Definition
Synercid = Quinupristin + Dalfopristin
Term
Streptogramins MOA
Definition
Inhibits protein synthesis
Dalfopristin - inhibits 50S subunit
Quinupristin - premature release of peptide
Term
Streptogramins work on __________ bacteria. What is the recommended use?
Definition
Gram+
Use on Vancomycin-resistance Enterococcus faecium (VREF)
Term
Side effect of Streptogramins
Definition
Hepatotoxicity
Term
Oxazolidinones are also called _____________
Definition
Linezolid
Term
MOA of Oxazolidinones
Definition
Inhibits protein synthesis at 30S ribosome and bacteriostatic
Term
What do you use Oxazolidinones for (2)?
Definition
Vancomycin resistant Enterococcus faecium (VREF) Methicillin resistant Staphylococcus aureus (MRSA)
Term
Oxazolidinones have an interaction with ____________
Definition
pseudoephedrine
Term
Name the MOA of sulfonamides
Definition
inhibits folic acid synthesis (aka DNA synthesis) by inhibiting PABA --> Dihydrofolic acid enzyme = tetrahydropteric acid synthetase
Term
Sulfonamides are (narrow/broad) spectrum and (bacteriostatic/bacteriocidal)
Definition
broad
bacteriostatic
Term
Sulfonamides are used ________ for _______ infections
Definition
topically
urinary tract infections and GI tract infections
Term
Name 3 side effects of sulfonamides
Definition
hypersensitivity (skin rash)
anemia
thrombocytopenia
Term
Name 4 mechanisms of resistance for sulfonamides
Definition
decreased permeability (drug cant get into cell)
bacteria get folate from the environment
alteration of tetrahydropteric acid synthetase
overproduce PABA
Term
Dapsone and Para-Aminosalicylic Acid have a structure similar to ____________ with a MOA similar to
Definition
sulfonamides
sulfonamides
Term
Dapsone and Para-Aminosalicylic Acid are (narrow/broad) spectrum and are used for what?
Definition
narrow
mycobacterium (M. leprae)
Term
What is the structure of trimethoprim?
Definition
2,4-diaminopyrimidine
Term
MOA of trimethoprim
Definition
inhibits dihydrofolate reductase and bacteriostatic
(inhibits dihydrofolic acid --> tetrahydrofolic acid)
Term
trimethoprim are (narrow/broad) spectrum and (bacteriocidal/bacteriostatic)
Definition
broad
bacteriostatic
Term
Name two uses of trimethoprim
Definition
UTIs
traveler's diarrhea
Term
Coltrimoxazole is ________ and ________ together (_____ dilution). Coltrimoxazole is (bacteriocidal/bacteriostatic)
Definition
trimethoprim and sulfamethoxazole
(1:5)
bacteriocidal
Term
Name 2 side effects to trimethoprim
Definition
hypersensitivity
blood abnormalities
Term
4 mechanisms of resistance for trimethoprim
Definition
• Overproduction of Dihydrofolic acid
• Alteration of Dihydrofolic Reductase
• Development of Folic Acid Dependency
• Decreased Permeability
Term
Metronidazole MOA
Definition
produces short-lived intermediates that break down bacterial DNA
Term
Metronidazole is (broad/narrow) spectrum and (bactericidal/bacteriostatic)
Definition
narrow
bactericidal
Term
Metronidazole has an interaction with what?
Definition
alcohol
Term
Rifampin is made from _________
Definition
streptomyces
Term
Rifabutin is active against ________________
Definition
mycobacterium avium
Term
What is the MOA of Rifampin
Definition
Inhibits DNA-dependent RNA polymerase
Term
Rifampin is (broad/narrow)
Definition
Term
Rifampin works against _____________
Definition
Mycobacterium tuberculosis
Term
Side effects of rifampin are ?
Definition
skin rashes
thrombocytopenia
Term
What is a mechanism of resistance for rifampin
Definition
alteration of RNA polymerase
Term
Nalidixic acid MOA?
Definition
inhibits bacterial DNA gyrases and topoisomerases
Term
Nalidixic acid is (narrow/broad) and kills _______ bacteria. it's primarily used for __________
Definition
narrow
gram-neg
UTI
Term
Quinolones are derivatives of _______________
Definition
nalidixic acid
Term
Give 3 names of quinolones
Definition
•Gatifloxacin, Levofloxacin, & Ciprofloxacin
Term
Quinolones MOA?
Definition
Inhibits bacterial DNA dependent gyrase and topoisomerases
Term
Quinolones are (broad/narrow) and kill __________ bacteria. They are administered ________.
Definition
broad
gram + and gram-neg bacteria
orally
Term
What are the side effects of quinolones
Definition
Gi disturbances
Term
Mechanisms of resistance to quinolones can occur by altering __________ enzymes, altering ________, or increasing __________.
Definition
Bacterial DNA gyrase/topoisomerases
OMPs
export of antimicrobial agent through efflux pumps
Term
What is the structure of polymixin
Definition
basic polypeptide
Term
What are 2 names of polymixin
Definition
polymixin B and E (colistin)
Term
MOA of polymixin
Definition
cationic detergent disrupts cell membrane
bactericidal
Term
Polymixin is (narrow/broad) and kills ___________.
Definition
narrow
gram-neg
Term
Topical polymixins are ___________ and _______
Definition
bacitracin and neomycin
Term
Polymixins are not __________ by the _________ which means they are used in _________________.
Definition
absorbed
GI tract
guy "sterilization"
Term
Polymixins are used as a last resort to treat systemic infections of ___________ and __________.
Definition
Acetinobacter and pseudomonas
Term
2 side effects of polymixins
Definition
neurotoxic
nephrotoxic
Term
Mechanism of resistance for polymixins
Definition
alteration of lipopolysaccharide (cell membrane)
Term
Daptomycin MOA
Definition
membrane depolarization and disruption of ionic gradients
Term
Daptomycin is (narrow/broad) spectrum and kills ______ bacteria
Definition
narrow
gram+
Term
Clofazimine MOA
Definition
lipophilic antibiotic that binds to DNA
Term
Clofazimine is used to treat
Definition
Mycobacterium leprae
Term
Pyrazinamide (PZA) is used to treat what?
Definition
Mycobacterium tuberculosis
Term
Agar dilution is a ________ procedure that determines _____ value. What is done?
Definition
quanitative procedure
MIC
Plating several different bacterial colonies and several antimicrobial concentrations
Term
Tube broth dilutions uses the same principle as __________ except in broth culture tubes
Definition
agar dilution
Term
In Tube broth dilution the first culture exhibiting no growth is the ....
How do you find MBC?
Definition
MIC - lowest concentration of antimicrobial that will inhibit growth.
3 cultures can then be plated onto agar with no antibiotic. The cultures that don't grow can be tracked back to antibiotic concentration that kills bacteria
Term
In a beta lactamase test, if the bacteria turns ________ it is producing beta lactamase
Definition
pink
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