Which antimicrobials interfere with protein synthesis?

Aminoglycosides and tetracyclines

What do protein synthesis inhibitors target?
The bacterial ribosome
Which antimicrobials bind to the 30S sub-unit of ribosomes?
Tetracyclines and aminoglycosides
Which antimicrobials attach to the 50S sub-unit of ribosomes?
Macrolides, Lincomycins, and Chloramphenicol
What are aminoglycosides effective against?
Aerobic gram negative infections
What kind of action do aminoglycosides have?
bactericidal
What are the six common aminoglycosides?
Streptomycin Neomycin, Kanamycin, Gentamicin, Tobramycin, and Amikacin
What is the mechanism of action for aminoglycosides?
Biphasic
What are the two phases for aminoglycosides mechanism of action?
PAssive diffusion and Active transport
What is active transport dependent on?
Oxygen
Which bacteria will active transport for aminoglycosides not be active against?
Anaerobes
What to and how do aminoglycosides bind?
They bind irreversibly to 30s subunit
What do aminoglycosides interfere with?
mRNA translation
What effect do protein synthesis inhibitors normally have?
Bacteriostatic

What is the one exception to bacteriostatic protein synthesis inhibitors?

Aminoglycosides
Do aminoglycosides have a post-antibiotic effect?
yes
What is special about the dosing of aminoglycosides?
One single dose is equally efficient as several doses over 24 hours
What is the broadest spectrum of all aminoglycosides?
Amikacin
How does pH affect the antibacterial activity of aminoglycosides?
Alkaline pH increases antimicrobial activity
What has the best absorption for aminoglycosides?
Parenteral
Do aminoglycosides have a short or long withdrawal period?
Long
Where do aminglycosides accumulate?
In the tissues
How are aminoglycosides excreted?
The kidney
What can happen due to the kidney being the major site of drug sequestration?
Nephrotoxicity
What are the three adverse reactions for aminoglycosides?
Nephrotoxicity, Ototoxicity, and Neuromuscular blockade
Which adverse reaction is irreversible for aminoglycosides?
Ototoxicity
What are the three ways that bacterial resistance against aminoglycosides can be acheived?
Enzymatic inactivation, Ribosomal alterations, and Reduced permeability of antibiotic
What is the efficacy predictor of Aminoglycosides?
Type I (concentration -dependent)

What effect does tetracyclines have on bacteria?

Bacteriostatic
What are the two types of common tetracyclines?
Natural and Semisynthetic
What are the three natural common tetracyclines?
Chlortetracycline, Tetracycline, and oxytetracycline
What are the two semisynthetic tetracyclines?
Minocycline and doxycycline
How do tetracyclines penetrate bacterial cells?
Passive diffusion and active transport
How does doxycycline enter cells?
Passive diffusion
What is the microbial susceptibility to tetracyclines?
Gram + aerobic bacteria, Gram - bacteria, Anaerobes, Protozoa, Intracellular organisms, and Rickettsia
What can Oxytetracycline treat?
Equine monocytic Ehrlichiosis
How well are tetracyclines absorbed orally?
Well
What do tetracyclines form?
Chelatin complexes with divalent and trivalent cations
What is bad about using tetracyclines in horses and ruminants?
They may impair GIT microflora
What is the distribution of tetracyclines?
Binds to plasma proteins
Which two tetracyclines penetrate the brain, spinal fluid, and prostate?
Minocycline and doxycycline
What is the rate of metabolism for tetracyclines?
Very low
Which two tetracyclines are oxidized in the liver?
Minocycline and doxycycline
How are tetracyclines excreted?
Urine and feces
Which tetracycline is excreted by bile?
Doxycycline
Which tetracycline would you use in renal function impaired patients?
Doxycycline
What happens if you inject tetracyclines IV?
The Ca availability is reduced and causes collapse
What are the three ways that bacterial resistances can develop for tetracyclines?
Impaired permeation of drug, tetracycline efflux, and ribosomal alteration
What is the efficacy predictor for tetracyclines?
Type III antimicrobial