Aminoglycosides - 10 Qs Flashcards
What are Aminoglycosides?
Water soluble PSEUDOGLYCOSIDES
What Aminoglycosides are from streptamine moiety?
Kanamycin
Tobramycin
Gentamycin
Neomycin
What Aminoglycosides are from 2-Deoxystreptamine moiety?
Paromomycin
Are Aminoglycosides stable?
Yes.
They are stable in a wide range of PH (2-11)
What’s the MOA of Aminoglycosides?
BacteriCIDAL
Which Aminoglycosides is the exception to the all bactericidal rule
Spectinomycin (which is bacterioSTATIC)
Name target for Aminoglycosides
Ribosomal DNA in the 30S ribosomal subparticle
Effect of Aminoglycosides used in low doses on target?
Cause mistranslation and nonsense protein formation => inh protein synthesis
This is unique for cidal AB, usually static are the ones that inh protein synthesis
Why are B-lactam usually combined with Aminoglycosides?
To take further advantage of the damaged cell wall (buz the nonsense protein become part of the membrane and let in lots of drugs)
When are Aminoglycosides given orally?
To act in the gut - local action
Otherwise, given IV/ IM
What’s the spray tobramycin solution used for?
Sprayed into the lungs for d successful tx of P. aeruginosa inf in cystic fibrosis pts
What are Aminoglycosides usually reserved for?
For serious inf cuzed by gram (-) org becuz of serious toxicity which is often delayed at onset
Though, they have activity against gram (+), there are better agents for these
What m.o. are Aminoglycosides ineffective against
Anaerobes
How does resistance occur primarily?
A. Reduced permeability to Aminoglycosides
B. deactivating enzymes (R-factor controlled) via
N-acetylation, O-phosphorylation, O-adenylation
List AEs of Aminoglycosides.
Ototoxicity
Nephrotoxicity
Curare-type neuromuscular blockade
What’s Kanamycin sulfate
A fermentation pdt that’s a mixture of 3 comps, but Kanamycin A is predominant.
Main use of Kanamycin sulfate
Part of anti-TB cocktail
What’s kanamycin active against?
Mycobacterium kansasii
M. Marinum
M. intracellulare
What m.o. are usually resistant to Aminoglycosides?
Anaerobes
P. Aeruginosa
Name drugs in the Aminoglycosides class that are part of anti-TB cocktail.
Kanamycin sulfate
Amikacin sulfate
What’s Amikacin sulfate?
Semi-synthetic pdt of Kanamycin
What does Amikacin contain that inh enzymes?
Hydroxyaminobuteryl amide (HABA)
Use of Tobramycin sulfate
For difficult inf including gentamicin resistant P. Aeruginosa
Which Aminoglycosides has a diff source of origin from d others?
Gentamicin
What’s Gentamicin from?
Micromonospora purpurea
Why’s Gentamicin useful as a broad spectrum for difficult pathogens?
Some targets for enzyme inactivation are missing.
T/4 resistance may not dev so rapidly
Are Aminoglycosides clinically stable with B-lactams?
No.
Admin separately I.e. not in the same vial, but they can be admin same time
Which Aminoglycosides is never used systemically?
Neomycin sulfate.
Only used topically
Which Aminoglycosides can be used to lower cholesterol?
Neomycin sulfate
Main use of Parmomycin sulfate
Used PO for suppression of gut flora and amoebic dysentery (Entamoeba Histolytica)
What’s unique about Spectinomycin hydrochloride?
Unusual tricyclic ring
Only bacterioSTATIC Aminoglycosides
What’s the primary use of Spectinomycin hydrochloride?
Used as a single bolus IM injection against PPNG (Penicillase Producing N. Gonorrhoeae)
Any significant SE for Spectinomycin?
No significant Ototoxicity or nephrotoxicity when used as a single bolus IM inj
Which Aminoglycosides is given as a single IM bolus injection for the treatment for PPNG?
Spectinomycin
