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10 Cards in this Set

  • Front
  • Back
General Spectrum and Clinical Status
-effective for
-limited by
-highly effective vs. aerobic gram-neg. bacilli
-used for hospital acquired-infections due to aerobic gram-neg. bacilli
-especially useful in immunosuppressed patients when unable to use less toxic drugs
-limited by some serious toxicities
Chemistry and Mechanism
-highly polar basic cations
-limited distribution to primarily extracellular space
-bactericidal inhibitor of
-bacterial protein synthesis that causes misreading of mRNA so abnormal proteins inserted in bacterial membrane
bind at 30S ribosome
-misread proteins inserted into bacterial membrane causes channels that allow influx of antibiotic
Therapeutic Uses
-serious aerobic gram-neg. infections in hospitalized neutropenic patients
-life-threatening infections may require combination therapy with aminoglycosides
such as pneumonias, endocarditis, septicemia, osteomyelitis
-Aerobic gram-neg. bacilli
E. coli, Klebsiella, Proteus, Enterobacter, Pseudomonas aeruginosa
-Staphylococcus aureus
(need combination therapy to avoid resistance)
-Ineffective vs anaerobic bacteria
-Inactivation by bacterial enzymes
acetylases, phosphorylases, adenylases
-Alteration of active transport system
energy and oxygen dependent
-Mutation of ribosomal protein binding site
poor oral absorption
systemic use requires intravenous admin.
limited to extracellular space
poor distribution into CSF
dependent upon renal glomerular filtration
Adverse Effects
Vestibular toxicity (vertigo, ataxia)
Auditory effects (irreversible damage to hair cells in cochlea of Organ of Corti)
proximal tuberular necrosis due to release of lysosomal enzymes into cytoplasm
-Neuromuscular blockade
reversible by calcium or neostigmine
Drug Interactions
-Combination Therapy
broaden spectrum or enhance activity
antipseudomonal penicillins or cephalosporins synergistic vs Pseud. aerug. and some gram-neg. bacilli
-Penicillins inactivated by mixing with aminoglycosides in high concentraion
-Other nephrotoxic drugs
potent diuretics, cyclosporine, cisplatin, amphotericin B, vancomycin
Clinical Problems
-Monitor renal function
-Monitor plasma concentration to determine drug intervals if reduced renal function
-Single daily dosing may be utilized if good renal function
post-antibiotic effect is concentration-dependent
Drug Prototypes
-Gentamicin (Garamycin)
lowest cost
-Amikacin (Amikin)
expensive, but less resistance
topical or orally prior to abdominal surgery