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41 Cards in this Set
- Front
- Back
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what are the binding sites for tRNA that we can target to prevent bacterial protein synthesis
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P and A site
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what are the 2 classes of 30S inhibitors?
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Aminoglycosides
Tetracyclines |
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Streptomycin
Gentamicin Tobramycin Amikacin Neomycin are what kind of drugs? bind where? |
Aminoglycosides
bind at 30S |
|
Erythromycin
Clarithromycin Azithromycin are what kind of drugs |
Macrolides
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Gentamicin
Acts where? |
30S ribosome
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Amikacin
Acts where? |
30S ribosome
|
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Streptomycin
Acts where? |
30S ribosome
|
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Tobramycin
Acts where? |
30S ribosome
|
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Neomycin
Acts where? |
30S ribosome
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what are aminoglycosides used to treat?
*** |
serious G- aerobic infections
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Combination DOC for pseudomonas?
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Aminoglycosides
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Yersinia pestis, Francisella tularensis DOC?
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Aminoglycosides
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MOA for aminoglycosides?
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Irreversibly binds to 30S ribosome:
1. interferes with initiation complex formation 2. causes misreading of mRNA 3. restricts polysome formation --Blocks ribosomes ability to move along mRNA and synthesize new peptide chain |
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what drug class has a long post antibiotic effect?
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Aminoglycosides
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Aminoglycosides... bactericidal or static? Time or Conc dependent?
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Bactericidal
Concentration-dependent killing |
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what two conditions will prevent AG uptake in G- bacteria?
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anaerobic environment
low extracellular pH (eg lung and bronchial secretions) note: Crossing the inner membrane depends on active transport (O2-dependent) Membrane potential drives transport (coupled to a proton pump) |
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most common mech of resistance to Aminoglycosides
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aminoglycoside modifying enzymes (AME)
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how do you administer aminoglycosides?
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parenteraly
very poorly absorbed orally |
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T/F
AGs Do not cross membranes very well |
TRUE
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what eliminates the aminoglycosides?
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glomerulo filtration
can cause kidney toxicity |
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aminoglycosides can cause what important problem?
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kidney toxicity
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in pts with renal complications what should do you do for pts on aminoglycosides
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adjust the dose / dosing frequency
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what is the dosing for aminoglycosides
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Single daily dosing (consolidated therapy)
7 mg/kg every 24 hrs |
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Total daily dose as single injection of aminoglycosides Is less toxic … but how?
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it is due to the amount of time over the toxicity threshold. Giving one big dose keeps you over the tox threshold for less time than giving a bunch of single doses (the tox threshold is super low)
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What are some of the situations you don't want to use consolidation therapy of aminoglycosides
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Pregnant patients
Osteomyelitis Infective endocarditis Patients receiving concurrent ototoxins (such as furosemide) Patients undergoing solid organ transplantation receiving cyclosporine or other nephrotoxic immunosuppressive drugs |
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if a pt is on a kidney transplant drug or antifungals, what drug is contraindicated
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aminoglycosides
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what is the therapeutic index for aminoglycosides?
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Narrow therapeutic index
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primary toxicities of aminoglycosides?
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Nephrotoxicity [usually reversible]
Ototoxicity [often irreversible] Neuromuscular blockade [reversible] |
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with use of aminoglycosides, what is the important relationship btw plasma creatinine conc and drug half life
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Linear relationship between … plasma creatinine conc. & drug half-life
Tox incidence related to drug concentration |
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most important side effect of aminoglycosides
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Nephrotoxicity
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Antfungals should not be used with what? cause what?
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Aminoglycosides
nephrotox |
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besides neuromuscular and nephro, what other tox can be seen with aminoglycosides? reversible?
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ototoxicity
often irreversible |
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pt comes in and they have Tinnitus & high frequency hearing loss (initial). looking at their drug list, what would you not be surprised to find?
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aminoglycosides
|
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Mysthenia gravis is an absolute contraindication for?
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aminoglycosides
can cause neuromuscular blockade |
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what 2 things can you use to reverse the neuromuscular blockade effect of aminoglycosides
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Ca gluconate
Neostigmine |
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Used alone to treat tularemia and plague
(a DOC) |
Streptomycin
|
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Can use in combination to treat
tuberculosis brucellosis (a DOC with doxycycline) endocarditis (with a cillin) |
Streptomycin
|
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Usually in combination with a cillin for severe infections:
Pseudomonas (a DOC) Enterococcal (a DOC) |
Gentamicin
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Primarily used for pseudomonas and other serious infections caused by organisms resistant to other AGs
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Amikan
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Has the broadest spectrum of the aminoglycosides... and is quite resistant to inactivating enzymes of bacteria
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Amikan
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what drug is used orally to sterilize the gut
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Neomycin
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