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Aminoglycosides - Coggle Diagram
Aminoglycosides
Activity/Use
Activity enhanced by inhibitors of cell wall synthesis
Aerobic gram - bacteria
Some gram + bacteria
Streptococcus
Use with Penicillin
Listeria monocytogenes
Enterococcus
Use with Amoxicillin
Sepsis
Reserved for very sick patients
Bacteremia
UTI
Infective endocarditis
In combination with other drugs
Intra-abdominal infection
Examples
Gentamicin
Most commonly used
Amikacin
Widest spectrum
Used against Gentamicin & Tobramycin-resistant strains
Tobramycin
Preferred for
Pseudomonas
infections
Neomycin
Netilmicin
Streptomycin
Mechanism of Action
Structure
3 hexagonal rings
Bactericidal
Binds to 30s subunit of bacteria ribosomes
Blocks initiation complex
Alteration of codon:anticodon recognition
Misreading of mRNA
Abnormal bacterial proteins
Penetration through membranes depends on oxygen-dependent active trasport
Minimal action against anaerobes
ADME
Administration
Concentration-dependent action
Give high dose one a day
Peak:MIC ration ≥ 10:1
IV and IM (rare)
Not absorbed in GIT
Distribution
Most body fluids
Crosses placenta
Joints
Pleura
Can't cross
BBB
Cells
Eyes
Secretions
Excretion/Metabolism
Renal excretion: glomerular filtration
Dose reduction required in renal impairment
T1/2 in normal renal function ~2-3 hrs
Removed by hemodialysis and peritoneal dialysis
Side Effects
Nephrotoxicity
Can be reverse with discontinuation
Beware if...
Dehydrated
Other nephrotoxins
Pre-existing renal failure
Ototoxicity
Irreversible damage to sensory cells in ear
Vertigo
Ataxia
Loss of balance
Streptomycin
Gentamicin
Deafness
Neomycin
Amikacin
Paralysis
Due to neuromuscular blockade
Inhibition of Ca2+ uptake necessary for release of ACh
Contraindicated with Myasthenia Gravis