| 1 Discovered Aminoglycosides
2 Aminoglycosides are isolated from | 1 Schatz and associates
(1939- 1944)
2 genus Streptomyces (griseus) |
| Structurally related to Streptomycin | 1 Kanamycin,
2 Neomycin,
3 Paromomycin,
4 Gentamicin,
5 Tobramycin,
6 Netilmicin |
| Semisynthetic derivative of Kanamycin | Amikacin |
| Aminoglycosides Characteristic | Absorbed very poorly (less than 1%) following oral administration
Treatment for systemic infections (Parenteral) |
| Aminoglycosides Side Effects | 1 Neurotoxicity
2 Allergic reactions
3 Nephrotoxicity
4 Ototoxicity
NANO |
| Aminoglycosides are
1 strongly basic compounds that exist as __
2 Their inorganic acid salts are __ in water
3 All are available as __
4 Solutions of the aminoglycoside salts are stable to __ | .
1 polycations at physiological pH.
2 very soluble
3 sulfates.
4 autoclaving. |
| Aminoglycosides
1 __ of the aminoglycosides contributes to their pharmacokinetic properties.
2 Aminoglycosides distribute well into most body fluids but not into the __
3 Aminoglycosides tend to concentrate in __ | .
1 The high water solubility
2 Central Nervous System,
Bone, or Fatty or Connective Tissues.
3 Kidneys |
| Aminoglycosides Spectrum Of Activity | 1 Broad spectrum
2 Treatment of serious systemic infections caused by aerobic gram -ve bacilli
3 Aerobic Gram +ve and -ve cocci is less sensitive
--> Beta lactam rings are preferred |
| Aminoglycosides Mode of Action | 1 act directly on the bacterial ribosome to INHIBIT THE INITIATION OF PROTEIN SYNTHESIS
2 They bind to the 30S RIBOSOMAL SUBUNIT to form a complex that cannot initiate proper amino acid polymerization.
3 Causes MISREADING mutations of the genetic code (mRNA), and hence incorporation of improper amino acids into the peptide chain |
| Aminoglycoside + sulfate = | more soluble |
