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30 Cards in this Set
- Front
- Back
Aminoglycosides used mostly against
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Gram negative enteric bacteria
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2 conditions that inhibit transport of aminoglycosides by reducing the gradent
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Low extracellular pH and anaerobic conditions
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Synergism of these antibiotics may enhance transport of aminoglycosides into bacteria
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cell wall-active drugs (ie. penicillin or vancomycin)
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Mechanism of action of aminoglycosides
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Protein synthesis inhibition by:
1. Interference of initiation complex of petide formation 2. Misreading of mRNA which cause incorporation of incorrect AAs 3. Breakup of polysomes into nonfunctional monsomes |
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Mechanisms of aminoglycosides resistance
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1) Direct aminoglycoside modification by a transferase enzyme
2) Impaired entry of the drug into the cell (mutation of porin proteins involved in transport) 3) Mutation of the receptor on the 30S ribsomal subunit |
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Aminoglycosides have a concentration-______ killing
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Dependent
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Aminoglycosides have both ____- and _________-dependent toxicity
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time; concentration
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Properties of aminoglycosides that requires once-daily dose rather than multiple smaller doses
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Concentration-dependent killing and postantibiotic effect
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Reason for intrathecal or intraventricular injection to achieve higher levels of aminoglycocides in CSF (Properties of the molecule)
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Highly polar compounds that do not enter cells readily
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Half life of aminoglycosides
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2-3 hrs
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Toxic effects of aminoglycosides (all)
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Ototoxic and Nephrotoxic; Ototoxicity can manifest as auditory damage (tinnitus and high-frequency hearing loss and vestibular damage); Nephrotoxicity can result in rising serum creatinine levels or decreased clearance of creatinine
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Drug combos to treat enterococcal endocarditis, viridans streptococcal and staphylococcal endocarditis
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penicillin-aminoglycoside; Penicillin-streptomycin
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Why can't treat with streptomycin alone?
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Resistance has emerged in most species
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Which drug has largely replaced streptomycin?
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Gentamicin
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Resistance to gentamicin is definitely also resistant to what 3 other drugs but still susceptible to this drug?
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Netilmicin, Tobramycin and Amikacin; supseptible to streptomycin
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Streptomycin is mainly used as a second-line agent for treatment of
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TB
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Drug combo for plague, tularemia and sometimes brucellosis
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Streptomycin (intramuscular) in combo with oral tetracycline
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Adverse rxns of Streptomycin
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1) Hypersensitivity in prolonged usage
2) Irreversible vestibular damage (vertigo, loss of balance) = contraindication during pregnancy |
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Gentamicin effective agains both
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Gram-positive and gram-negative organisms; (staphylococci and coliforms)
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Gentamicin has synergy with these antibiotics against psudomonas, proteus, enterobacter, klebsiella, serratia, stenotrophomas and other gram-negative rods that may be resistant to multiple other antibiotics
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beta-Lactams
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Adverse reactions of Gentimicin
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Reversible Nephrotoxicity and irreversible ototoxicity
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In practicality, genticicin is interchangeable with this aminoglycocide
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Tobramycin
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More active against pseudomonas (Gentamicin vs Tobramycin)
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Tobramycin
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Patient has Lower Respiratory Infection with Pseudomonas aeruginosa complicated with cystic fibrosis, treat with this antibiotics
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Inhale solution of Tobramycin
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Treat infection that is resistant to gentamicin and tobramycin with this aminoglycocides
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Amikacin and netilmicin
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Treat multidrug-resistant Mycobacterium tuberculosis (including streptomycin-resistance) with this aminoglycocide
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Amikacin
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Clinical uses of Neomycin and Kanamycin
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Topical and oral use for elective bowel surgery; too toxic for parenteral use
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Neomycin for hepatic coma has been replaced by
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Lactulose
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Spectinomycin is used solely as an alternative treatment for drug-resistant _____
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Gonorrhea or gonorrhea in penicillin-allergic patients
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Adverse affects of spectinomycin
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Pain at the injection site and occasionally fever and nausea
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