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Aminoglycosides

QuestionAnswer
Aminoglycosides Drugs ? * Gentamicin --- Amikacin --- Tobramycin --- Streptomycin --- Neomycin
Basic MOA ? * Protein Synthesis Inhibitors acting at the 30S ribosome
Aminoglycosides (AGs) basics ? * Most commonly used in Gram (-) Aerobes ..... * Always used in combo, usu b-lactams ..... * Use is limited due to severe toxicity
AGs most Cx use ? * empiric therapy of serious infections, when we think it is a severe G (-) bacteria.... * use in hospital bc given IV and once the culture is done, an appropriate drug is used
AGs spectrum of activity to use in ? * Serious infections by aerobic G- bacilli, including Pseudomonas, Proteus, Serratia, and G+ Staph .... * Used in b-lactam combo for Pseudomonas, Invasive enterococcal infections and Serious Stap.
When AGs can be used as a monotherapy ? * Tularemia - Plague - UTIs
Gentamicin basics and use ? * one of the most used AGs ..... *Usually used in combination with a cillin for severe infections: Pseudomonas (a DOC) -- Enterococcal (a DOC)...... * Enterococcal endocarditis and tularemia
Amikacin unique features and uses? * Primarily used for pseudomonas and other serious infections caused by organisms resistant to other AGs..... * broadest spectrum due to its unique metabolism
Streptomycin use ? * Used as single agent to treat tularemia and plague
Neomycin use ? * primarily OTC drugs.... * primarily for gut sterilization before surgery
Aminoglycosides – MOA ? * Irreversibly binds to 30S ribosome --> interferes with initiation complex formation --- causes misreading of mRNA --- restricts polysome formation ..... * Unique bc it is Bactericidal
AG drug resistance is common in ? * Especially a problem for enterococci , due to AME (Aminoglycoside Modifying Enzyme)
AG Pharkokinetics ? * Must know and monitor kidney function (CrCl) bc they are eliminated by glom. filtration in the kidneys....* so adjust dose based on kidney monitoring
AGs Dosing ? * Intermittent Dosing - 3 x a day small doses and Extended Dosing - 1 time a day
Extended Dosing Advantages ? * compariable outsomes to intermittent, seems to be better on the kidneys, don't have to monitor serum levels of the drug as much,
Extended Drug Dosings 2 advantages ? * Post-antibiotic effect (PAE) and Concentration-dependent killing ....* basically, more drug is on board, so it will kill more and since we have PAE (post antibiotic effect), we still get killing after concentrations drop below the MIC
How is it less toxic ? * Bc it is time and concentration dependent.... * get less drug accumulation due to the once a day dosing
When not to use extended AG dosing ? * Pts w/ unstable renal function --- CrCl < 60ml/min --- Endocarditis or meningitis --- Increased Vd (pregnancy, ascites, edema) --- Pts receiving concurrent nephrotoxic or ototoxic drugs
AGs SEs ? * Very low TI .....* Can cause ireeversible Ototoxicity, reversible neuromuscular block (CI in myasthenia gravis), and causes Nephrotoxicity
Why we see the SEs ? * the more you use the drug, the more likely it is to have a SE.... * Ototoxicity is due to it being trapped in the endolymph
TmT for AGs Toxicity ? * IV Calcium Salts
*b-Lactam Drugs* --> Monobactams --> Aztreonam basics ? * Effective against gram negatives only ...... *Same mechanism of action as other b-lactams by only binds to a PBP (penicillin binding protein) present in gram negatives
Aztreonam uses ? * Almost the same use as AGs ...... *serious gram negative aerobes infections --> Pseudomonas (DOC), Enterobacter........ * Good for MDR pseudomonas and for those with a penicillin allergy
Streptogramins --> quinupristin + dalfopristin MOA ? * Protein Synthesis Inhibitors acting at the 50S ribosome
Quinupristin + Dalfopristin use ? * Always used in combo with each other...... * Drug resistant G+ cocci infections like Staph. or Entero Faecium that is Vanc resistant (VREF)
Quinupristin + Dalfopristin SEs ? * myalgias and inhibit p450s
Urinary Antiseptic --> Nitrofurantoin basics ? * a very rapidly excreted drug that is used exclusively in uncomplicated UTIs....* not a first line drug....* also can be used for reoccurring/chronic UTIs
Nitrofurantoin MoA ? * ROS that damages DNA... * true MoA not really known
Nitrofurantoin SEs ? * Hypersensitivity reactions - skin rashes..... * Causes Hemolytic anemia in G6PD deficiency...... * Acute pneumonitis in Elderly..... * Turns the Urine BROWN
Created by: thamrick800
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