Aminoglycosides

AMINOGLYCOSIDES ANTIBIOTICS...
EXAMPLES: Gentamicin, tobramycin, amikacin, neomycin, streptomycin.
MECHANISM OF ACTION: Bacteriocidal antibiotic that blocks protein synthesis by binding to the bacterial 30S ribosomal subunit. This prevents the process of tRNA attachment and mRNA translation is disrupted.

  • Septicaemia
  • Biliary tract infection
  • Acute pyelonephritis and prostatitis
  • Endocarditis
  • Adjunct in Listeria meningitis
  • Myasthenia gravis (aminoglycosides can impair neurotransmission within muscles).
  • Caution in renal failure (doses should be reduced).
  • GI disturbance.
  • Nephrotoxicity.
  • Rash and vestibular and auditory damage (ototoxicity).
  • Blood dyscrasias.
  • Aminoglycosides are excreted unchanged in the urine.
  • t½ for gentamicin is 2–3 h.
  • Regular monitoring of U&Es.
  • For single daily dosing, gentamicin level must be taken 6–12 h after the first dose.
  • Levels should be interpreted using the Hartford Nomogram, which will determine dosing frequency.
  • Increased risk of ototoxicity with loop diuretics.
  • Aminoglycosides can enhance the effects of non-depolarising muscle relaxants.
  • Increased risk of nephrotoxicity with ciclosporin.
  • Predominantly Gram-negative Enterobacteria spp. cover (e.g. UTI, abdominal sepsis) and Pseudomonas spp.
  • Poor oral absorption hence given parenterally (except neomycin).
  • Once daily aminoglycoside dosing is preferable and provides adequate serum concentrations. Exceptions include the treatment of bacterial endocarditis.
  • Continuation of gentamicin therapy for more than 7 days carries an increased risk of nephrotoxicity and ototoxicity.