II. Indications

  1. Activity
    1. Aerobic and facultative Gram Negative Rods
    2. NO anaerobic activity
      1. Aminoglycosides require oxygen for active transport into Bacterial cells
  2. Organisms
    1. Enterobacter
    2. Escherichia coli
    3. Klebsiella Pneumoniae
    4. Proteus species
    5. Serratia
    6. Pseudomonas

III. Mechanism

  1. Bactericidal, Protein Synthesis Inhibitor
    1. Aminoglycosides undergo oxygen dependent active transport into the Bacterial cytoplasm where they concentrate
    2. Binds 70s Bacterial ribosome at the interface between its 30s and 50s subunits
    3. Results in mis-reading of Bacterial mRNA and defective Bacterial Proteins
  2. Antibiotic Resistance mechanisms
    1. Decreased Bacterial cell permeability and decreased active transport of Aminoglycosides into Bacterial cells
    2. Bacterial enzymatic degradation of Aminoglycosides
    3. Binding site mutations

IV. Medications: Active

V. Medications: Other

  1. Kanamycin
    1. Kanamycin is not typically used in U.S., however, Amikacin is derived from Kanamycin A
    2. Kanamycin is an Antibiotic complex extracted from Streptomyces kanamyceticus (found in Japanese soil)
    3. Kanamycin complex has three components (A, B, C) of which only Kanamycin A has significant medical use

VI. Pharmacokinetics

  1. Renal excretion unchanged in urine
  2. Not distributed to the eye or Central Nervous System
  3. Parenteral use, inhaled (Tobramycin in CF) or topical use (otic Antibiotics, Ophthalmic Antibiotics)
    1. Aminoglycosides have no significant oral Bioavailability (other than Kanamycin)

VII. Adverse Effects

  1. Nephrotoxicity
    1. See risk factors below
  2. Ototoxicity
    1. Risk of permanent Deafness
    2. With higher Aminoglycoside peak concentrations
    3. Increased risk in Mitochondrial DNA mutations (e.g. m.1555A>G)
  3. Neuromuscular Blockade
    1. May increase Neuromuscular Blocker effect
    2. May exacerbate Myasthenia Gravis

VIII. Risk Factors: Nephrotoxicity

  1. Advanced age
  2. Prior Renal Insufficiency
  3. Dehydration
  4. Hypokalemia
  5. Hypomagnesemia
  6. Liver disease
  7. Sepsis
  8. Drug Interactions with other nephrotoxic medications
    1. Cephalothin (Keflin) and other Cephalosporins
    2. Cyclosporin A
    3. Cisplatin
    4. NSAIDS
    5. ACE Inhibitors
    6. Methoxyflurane
    7. Loop Diuretics
    8. Amino Acids

IX. References

  1. Olson (2020) Clinical Pharmacology, Medmaster Miami, p. 112-3
  2. Block (2023) Aminoglycosides, StatPearls, Treasure Island, Fl
    1. https://www.ncbi.nlm.nih.gov/books/NBK541105/

Images: Related links to external sites (from Bing)

Related Studies

Ontology: Antibiotics, Aminoglycoside (C0003233)

Definition (NCI) Any antibiotic containing amino-modified sugars originally isolated from various Streptomyces and Micromonospora species. Aminoglycoside antibiotics bind to the 16S RNA of the bacterial 30S ribosomal subunit, inhibiting translation and protein synthesis. Aminoglycoside use is associated with ototoxicity, neurotxicity and nephrotoxicity.
Definition (NCI_NCI-GLOSS) A family of antibiotics that works against many types of bacteria and includes streptomycin, gentamicin, and neomycin. Aminoglycosides are used to treat bacterial infections.
Definition (CSP) any of a group of antibiotics derived from various species of Streptomyces or produced synthetically; they inhibit protein synthesis by binding with the 30S ribosomal subunit.
Concepts Antibiotic (T195) , Carbohydrate (T118)
SnomedCT 14443002
English Antibiotics, Aminoglycoside, aminoglycosides, aminoglycosides (medication), aminoglycoside antibiotics, aminoglycosides antibiotics, AMINOGLYCOSIDE ANTIBACTERIALS, aminoglycoside antibiotic, Aminoglycoside -class of antibiotic- (substance), Aminoglycoside -class of antibiotic-, Aminoglycoside, NOS, Aminoglycosides, Aminoglycoside Agents, Aminoglycoside Antibiotic, Aminoglycoside Drugs
Spanish aminoglucósido (clase de antibiótico) (sustancia), aminoglucósido (clase de antibiótico)

Ontology: Kanamycin (C0022487)

Definition (NCI) An aminoglycoside antibiotic with antimicrobial property. Amikacin irreversibly binds to the bacterial 30S ribosomal subunit, specifically in contact with 16S rRNA and S12 protein within the 30S subunit. This leads to interference with translational initiation complex and, misreading of mRNA, thereby hampering protein synthesis and resulting in bactericidal effect. This agent is usually used for treatment of E. coli, Proteus species (both indole-positive and indole-negative), E. aerogenes, K. pneumoniae, S. marcescens, and Acinetobacter species.
Definition (MSH) Antibiotic complex produced by Streptomyces kanamyceticus from Japanese soil. Comprises 3 components: kanamycin A, the major component, and kanamycins B and C, the minor components.
Definition (CSP) aminoglycoside antibiotic complex effective against aerobic gram-negative bacilli and some gram-positive bacteria including mycobacteria.
Concepts Antibiotic (T195) , Carbohydrate (T118)
MSH D007612
SnomedCT 387396008, 71451001
LNC LP14342-7, MTHU008095
English Kanamycin, kanamycin, D-Streptamine, O-3-amino-3-deoxy-alpha-D-glucopyranosyl-(1-6)-O-(6-amino-6-deoxy-alpha-D-glucopyranosyl-(1-4))-2-deoxy-, Kanamycin [Chemical/Ingredient], Kanamycin Complex, antibacterial kanamycin, kanamycin (medication), KANAMYCIN, Kanamycin product, Kanamycin (product), Kanamycin (substance)
Swedish Kanamycin
Czech kanamycin
Finnish Kanamysiini
Russian KANAMITSIN, КАНАМИЦИН
Japanese カナマイシン
Croatian KANAMICIN
Polish Kanamycyna
Portuguese Kanamicina, Canamicina
Spanish canamicina (sustancia), canamicina, kanamicina (producto), kanamicina (sustancia), kanamicina, Kanamicina
French Kanamycine
German Kanamycin
Italian Kanamicina