Aminoglycosides Flashcards
Drugs from Streptomyces bacteria
Streptomycin
Tobramycin
Neomycin
Kanamycin
-mycin
Drugs from Micromonospora
Gentamicin
Amikacin
Netilmicin
-micin
Half-life of aminoglycosides
2-3 hours
Used for this kind of bacteria
Gram-negative enteric bacteria
Reversible or irreversible inhibitors of protein synthesis
Irreversible
Reversible: Tetracyclines
Inhibits the 30S portion (both aminoglycosides and tetracyclines)
Mechanism of action is enhanced by
Penicillin or Vancomycin
Due to the synergistic effect
Mechanism of action is inhibited by
Low extracellular pH and anaerobic conditions
Primary mode of resistance
Production of transferase enzyme that inactivate aminoglycosides by adenylation, acetylation, or phosphorylation (PAA)
Other modes of resistance: Deletion and alteration of a porin protein and deletion or alteration of the receptor protein
Route of administration for the treatment of gram-negative bacterial infections, gram-positive endocarditis, and tuberculosis
Intravenous
Administered as a 30-60 minute infusion
Route of administration that is well-absorbed
Intramuscular
Peak blood concentration: 30-90 minutes
Route of administration where the entire dose is excreted in the feces
Oral
Poor absorption in an intact GIT
Absorption may be increased in an ulcerated tract (like ulcerated colitis)
Bactericidal or bacteriostatic
Bactericidal
Higher concentration = higher antimicrobial activity
Route of elimination
Renal
Higher creatinine clearance = lower dosage needed
Do not penetrate cells readily due to its polarity
Dose adjustments for those with renal impairment
Most ototoxic
Neomycin, Amikacin, Kanamycin
NAK
Most vestibulotoxic
Streptomycin
Gentamicin
SG (Singapore)