Name the category.
Antibacterials
Name the main drug.
Gentamicin
What kind of antibiotic is gentamicin?
Aminoglycosides
What is the route of administration?
IV or IM
Describe the mechanism of action.
Bind to 30S subunit of the bacterial ribosome → irreversible inhibition of initiation complex → inhibition of bacterial protein synthesis → cell death (bactericidal effect)
Misreading of mRNA
Blockage of translocation
Synergistic effect when combined with β-lactam antibiotics: β-lactams inhibit cell wall synthesis → facilitated entry of aminoglycoside drugs into the cytoplasm
How is the CNS penetration of gentamicin?
poor
Name the route of elimination.
renal (via glomerular filtration)
List clinical uses of gentamicin.
Severe gram-negative rod infections
Not effective against anaerobes (aminoglycosides require oxygen to be absorbed by cells)
Neomycin, which is not absorbed systemically, is administered orally to prepare the gut for bowel surgery.
Streptomycin is used as a second-line treatment for Mycobacterium tuberculosis and M. avium-intracellulare
What are adverse effects?
Nephrotoxicity
Ototoxicity and vestibulotoxicity (risk of ototoxicity is higher when used concurrently with loop diuretics) resulting in:
Tinnitus
Ataxia
Vertigo
Neuromuscular blockade
Teratogenicity
List contraindications.
Myasthenia gravis
Botulism
Pregnancy
Cautious use in patients with renal dysfunction
Describe the mechanisms of resistance in gentamicin.
inactivation via acetylation, phosphorylation, and/or adenylation by secreted bacterial transferase enzymes
Last changed2 years ago