Micro Exam 2: Antibiotics (more specific) – Flashcards

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question
What is Gentamicin? 
answer
most commonly prescribed aminoglycoside
question
What is Tobramicin?
answer
an anti-pseudomonal aminoglycoside
question
What is a common first line antibioitic for uncomplicated UTI's?;
answer
TMP/SMX
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Which drugs require therapeutic drug monitoring?
answer
drugs with low therapeutic range; aminoglycosides and vancoymycin
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Combination therapy may prevent the emergence of resistance of what?
answer
  • mycobacterium tuberculosis
  • s aureus (fluroquinolone/rifampin)
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What are transglycosylases?
answer
they are a PBP that is takes nascent peptidoglycan to backbone of cell wall;
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What are carboxypeptidases and transpeptidases?;
answer
  • PBPs with a similar function
  • cleave terminal D-ala from pentapeptide;
  • ratio determines extent of cross linking
  • thought to influence cell shape
question
Beta lactams are contraindicated in what type of patient?
answer
patient with immediate hypersensitivity reaction history!
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if there is a history of skin rash with penicillins, what should you use?
answer
cephalosporins are almost always safe!
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What are types of glycopeptides? What do they act against?;
answer

They are cell wall active agents;;

vancomycin/teicoplanin

act against gram positive!!

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What is the action of glycopeptides?;
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bind to terminal D-ala of nascent cell wall peptides and prevent cross-linking of these peptides to create mature peptidoglycan
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What are the 2 types of cell wall active agents?
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  • beta-lactams
  • glycopeptides
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S. pneumoniae is responsible for what type of B-lactam resistance?
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altered PBPs
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MRSA is responsible for what type of beta-lactam resistance?
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Novel PBPs
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What are the 4 types of B-lactam resistance?
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  • B-lactamase (msot common)
  • altered PBPs
  • Novel PBPs
  • altered permeability
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Glycopeptide resistanct is a primary concern for which microorganisms?
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enterococcus and S. aureus
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Mechanisms of glycopeptide resistance:
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altered target/ substitude D-lac for D-ala and vancomycin can no longer bind
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Beta-lactamase inhibitors do not affect which microorganisms?;
answer
pseudomonas or enterobacter
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List 2 beta-lactamase inhibitors and their relative beta-lactam drugs:
answer
  • clavulanic (amoxicillin and ticarcillin)
  • tazobactam (piperacillin)
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List bacteria which can be inhibited by beta-lactamase inhibitors:;
answer
  • S. aureus
  • H. influenza
  • Niesseria sp.;
  • Bacteriodes fragillis
  • E. Coli
  • Klebsiella
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What does MLS stand for and what type of antibiotic are they?
answer
  • stands for macrolide, licosamides, streptogramins
  • protein synthesis inhibitor
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List protein synthesise inhibiting antibioitics:
answer
  • MLS
  • aminoglycosides
  • tetracyclines
  • linezolid
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Most common macrolide and what to look for to decide whether an antibiotic is a macrolide:
answer
  • Erythromycin
  • look for -mycin
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What subunit of ribosome do macrolides bind to?
answer
50s
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Two mechanisms of action of macrolides include:
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  1. block growth of nascent peptide chain by stimulating dissociation of peptidyl-tRNA from ribosome
  2. inhibits assembly of new large ribosomal subunits (leads to depletion in cell)
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Macrolide resistance is caused by two (three kind of) mechanisms, what are they? What genes code for them? What phenotype?
answer
  1. Efflux pump coded by mef(A); M phenotype
  2. Target Site Modification erm(B); MLSB phenotype
  3. rRNA (MLS)
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Active Efflux resistance is resistance to which antibiotic only?
answer
macrolides
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is ribosomal modifications of macrolides inducive or constitutive?
answer
inducive
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methylate adenine 2058 of 23s rRNA has to do with what antibiotic and what process?
answer
macrolides (also MLSB;phenotype) and process of ribosomal modification resistance (target site modification) erm(B) can be other letters
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What are the 4 first choices of macrolide uses?
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  • community acquired pneumoniae
  • pertussis
  • chlamydia trachomatis
  • mycoplasma
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What are 2 second choice uses of macrolides?
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pyogenic streptococcal infections and C jejuni gastroentitis
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What is different about 2nd generation fluroquinolones? What mechanisms of action and name of drug.;
answer

ciprofloxacin

- anti-pseudomonal and broader spectrum

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What is different about 3rd generation fluroquinolones? What mechanisms of action and name of drug.;

answer

Moxifloxacin

- enhanced gram positive

+/- anaerobic

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what is Qnr resistance?
answer
protection of topoisomerase in fluroquinolone action
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How is acquired resistance to fluroquinolones achieved?
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acquisition of resistance determinants from viridans streptococci
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First aminoglycoside and date? Are they natural?
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  • streptomycin (1944)
  • aminoglycosides are natural and semi-synthetic
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Aminoglycoside activity against gram positive and negative?
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  • excellent activity against gram negatives (including pseudomonas)
  • good gram positive
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When deciding if aminoglycoside or not?;
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  • look for -icin or just;-cin
  • ex. gentamicin, tobramicin, amikacin
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Do aminoglycosides work in absesses? Why or why not?;
answer

NO NO NO, do not work in any anaerobic conditions

they gain entry into inner membrane through energy dependent transport system - depend on the electron transport chain where O2 is needed

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What step of aminoglycoside action is rate limiting and by what?
answer
the active transport through inner membrane is rate limiting and binding; blocked by divalent cations and anaerobiosis
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Is binding of aminoglycosides reversable or irreversable? What ribosomal subunit do they bind to?
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  • irreversable
  • bind to 30s (like tetracyclines)
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What part of protein production does aminoglycosides inhibit?
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proofreading; causes aberrant or truncated proteins
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Can aminoglycosides affect mammalian cells?
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yes, at high concentrations it affects proteins (thats why it has a low therapeutic range with vancomycin!!)
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What are the three mechanisms of aminoglycoside resistance?;
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  1. altered ribosomal binding site (streptomycin only)
  2. reduced uptake or decreased cell permeability
  3. enzymatic modification (most common)
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What is the most common form of aminoglycoside resistance?;
answer

enzymatic modification!

- ;70 enzymes; plasmid mediated, different substrate specificities

question
What drugs inhibit metabolic pathways?
answer

trimethoprim and sulfonamides

(TMP AND SMX)

SMX stands for sulfonamethoxazole

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TMP/SMX action against gram positive and negative
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good gram negative, some gram positive
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sulfonamides act at what part of metabolic inactivation?
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mimic PABA and stop transformation of PABA to dihydrofolic acid by tetrahydropteric acid synthetase
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trimethoprimes act at what part of metabolic inactivation
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inhibit dihydrofolate reductase

stops dihydrofolic acid from being tetrahydrofolic acid

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TMP/SMX is commonly used for uncomplicated what?
answer
UTI infections
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What is TMP/SMX used against
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  • common uncomplicated UTIs
  • gastrointestinal infunction
  • management of PCP pneumonia
  • very active against anti-staphylococcal agents (CA-MRSA)
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Mechanisms of metronidazole action
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short lived toxic intermediates or free radicals that damage DNA and other macromolecules

;

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does metronidazole have a high or low bioavailability orally (PO)
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high (;90%)
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Does metronidazole have a long or short half life?
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LONG - take bidaily
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side effects of metronidazole use
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  • GI intolerance
  • antibuse effect
  • peripheral neuropathy
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metronidazole resistance? price?
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  • resistance slow to develope
  • cheap
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Uses of metronidazole
answer
  • anaerobic infections
  • C. Difficile colitis
  • Giardiasis
  • Trichmonas vaginitis and BV
  • H pylori (in combination)
  • parianal disease in IBD
question
define transglycocylation;
answer
the process where building blocks of peptidoglycan are added to the peptidoglycan backbone
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generations of cephalosporins are divided based on:
answer
spectrum of activity
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second generation cephalosporins are also known as:

3rd generation are:

answer
  • 2nd gen: respiratory cephalosporins
  • 3rd gen: IV drugs, gram neg activity, little gram pos
  • 5th gen: taken off market
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what worries people about VRE and MRSA in hospitals
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VRE is resistant to drug that can be used against MRSA so scared that gene will transfer
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What is the best macrolide drug today?
answer
clarithromycin
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what macrolide drug is bad to take - rips gut and you have to take many doses a day?
answer
erythromycin
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In terms of Target Site Modification and Efflux pumps (in macrolides), which gives you low level resistance and which gives you high level resistance?
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efflux = low level; TSM = high level
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can you get resistance from down regulation of porin channels?
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NO, if you have efflux AND downregulation you can though (these are acquired genes)
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why must mycoplasma be treated with macrolides?
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because mycoplasma doesnt have a cell wall! - it causes lower pneumonia (microlids are used for lower tract infections - upper you use something else)
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Are fluroquinolones natural or synthetic?
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completely and totally SYNTHETIC - not found in nature
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what were fluroquinolones first designed for?
answer
malaria
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What kind of drug is a respiratory fluroquinolone?
answer
Moxifloxacin and other 3rd gen ..?
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What are the best 2 drugs to treat patients with anaerobic infections?
answer
metronidazole and clindamicin;
question
Can you take metronidazole and drink alcohol?
answer
hell no sir. (violently sick)
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