Lecture 21: Inhibitors of Protein Synthesis I Flashcards
Aminoglycosides are poly cations and their ___is responsible for their pharmacokinetic properties
Polarity
Due to polarity of Aminoglycosides none is absorbed after ___ administration, none penetrates ___ readily
Oral, CSF
___excretes Aminoglycosides
Kidneys
What is the mechanism of action of Aminoglycosides
Inhibit protein synthesis by inhibiting 30s ribosomal subunit
Aminoglycosides treat what infections
- Gram negative enteric bacteria
- Suspicion of sepsis or endocarditis
Aminoglycosides require ___dependent active transport into bacterial cells and therefore would be ineffective against __organisms
Oxygen, anaerobic
Under aerobic conditions, aminoglycosides are bacteriocidal or bacteriostatic?
Bacteriocidal
Aminoglycosides have ___dependent killing
Concentration
Do aminoglycosides have a high or low post antibiotic effect
High, so antibacterial activity continues beyond the time that antibiotic is measurable
___dose of Aminoglycosides is better than ___dose
Single, large dose better than multiple small dose
(Concentration dependent killing)
What is the main mechanism of resistance to aminoglycosides
Plasmid mediated (R-Factor derived) chemical changes of enzymes that adenylate, phosphorylation or acetylate the drugs—>. Bacteria cells metabolize drug
What are Aminoglycosides active against
- Gram negative rods
- P. Aeruginosa
- Synergistic with beta-lactams against gram positive
- Gram negative infections in all species
Aminoglycosides can treat gram positive infections when combined with
Beta-lactams
What are the 4 examples of aminoglycosides
- Neomycin
- Gentamicin
- Amikacin
- Tobramycin
What is neomycin used for
- Labeled for cattle, sheep, goats, and birds orally for treatment of susceptible enteric infections
- Topically for treating skin, eye, ear infections
Is gentamicin a narrow or broad spectrum
Broad spectrum
What does gentamicin have activity against
Pseudomonas, proteus, staphylococcus, Coryne-bacterium, gram negative aerobes
What is gentamicin used for
- Labeled use in pigs
- Labeled for uterine infusion in horses
- Used in all species for treatment of susceptible infections of skin, respiratory tract, ear, eye, urinary tract, septicemia
What is amikacin labeled for
Dogs for susceptible UTI’s
Tobramycin is similar to gentamicin but has more potent ___activity and reduced ___
Anti-pseudomonas, Nephrotoxicity
T or F: tobramycin can be used in food animals
False
A dog was started on an antibiotic for systemic gram negative infection and then kidney function decreases. What antibiotic is likely?
Aminoglycosides