Aminoglycosides are important oligosaccharides which are formed by some species of bacteria. Aminoglycosides are used in medicines.

1. Aminoglycosides and their uses
Abhishek Giri
MSC PART2 (SEM 4)
R.K.TALREJA COLLEGE
ZOOLOGY DEPARTMENT

2. lAminoglycosides
lExamples of aminoglycosides
lOrganisms used for production
lMechanism and action
lPharmacokinetics
lSide effects
lUses
CONTENTS

3. Aminoglycosides
lOligosaccharides antibiotics
lAmino sugar bound through
glycosidic bond
lVery potent antibiotics
lAct against gram+ ve &
gram-ve bacteria
lStreptomycin-1st aminglycosides
lMycobacterium tuberculosis
lExhibits ototoxicity &
nepherotoxicity

4. Nomenclature
lAminoglycosides derived from streptomyces
genus-mycin
lAminoglycosides derived from
micromonospora
- micin
* All derived from actinomyces sps.

5. Organisms used for aminoglycosides
production
Aminoglycosides
lStreptomycin
lNeomycin B & C
lKanamycin A,B & C
lGentamicin
lSisomycin
Organism
lStreptomyces griseus
lS. fradiae
lS. kanamyceticus
lMicromonospora
purpurea
l M. inyoensis

6. Examples of aminoglycosides
lStreptomycin
lGentamicin
lTobramycin
lNeomycin
lNetilmicin
lKanamycin

7. 1.Streptomycin-1943
llaboratory of Selman Abraham Waksman at
Rutgers University
l first aminoglycoside antibiotic
ltreatment of tuberculosis.
lderived from Streptomyces griseus.
lbinds to the16S rRNA of the bacterial ribosome,
lrapidly bactericidal
lOtotoxic & nephrotoxic

8. 2.Neomycin- 1949
lSelman Waksman lab
lProduced by Streptomyces fradiae.
lactivity against gram-negative bacteria
lbetter activity than streptomycin against
aerobic gram-negative bacilli
l Oral neomycin used for bowel decontamination
prior to abdominal surgery.
loto- and nephrotoxicity

9. 3.Gentamicin-
lDerived from Micromonospora in 1963
l bactericidal , more potent than streptomycin
luse : gram - ve bacterial infections
l3 types : C1,C2, C1a .
lC2 have the highest anti bacterial activity
lototoxic and nephrotoxic
lIneffective against M.
tuberculosis

10. 1. Interferes with bacterial protein synthesis
& active transport system
2. Rapidly bactericidal
3. Concentration-dependent bactericidal
Activity
4. Post-antibiotic effect
Mechanism of action &
pharmacological properties

11. Mechanism of action

12. PHARMACOKINETICS
1. Absorption
Poor oral absorption.
Intramuscular absorption is good. ( 0.5 - 1.5 hrs )
2. Distribution.
Urine, kidney, endolymph, and perilymph of the
inner ear. Reasonable concentrations are
achieved in bone,synovial fluid, and peritoneal
fluid.

13. PHARMACOKINETICS
3. Elimination.
lGlomerular filtration by the kidneys accounts
for almost all (99%) of the elimination.
lSmall amts - by bile

14. DOSE
1. Conventional.
The goal is to achieve peak drug levels between
4-10mcg/ml and trough concentrations less than
2.0mcg/ml.
Dose: (gentamicin, tobramycin, netilmicin)1-
2mg/kg (lean body weight) in patients with
normal renal function.

15. DOSE
lAmikacin : 5-7 mg/ kg ( LBW )
2. Once daily dosing.
lA single daily dose(4-7mg/kg of gentamicin,
tobramycin) is administered once daily.

16. SIDE EFFECTS
1. Nephrotoxicity
Toxicity is due to accumulation of aminoglycosides
in proximal tubular cells of the kidney
lMost nephrotoxic-neomycin,
gentamicin,tobramycin
lResponsible for 10 - 15 %
of all renal failure cases

17. SIDE EFFECTS
2. Ototoxicity
l vestibular & auditory
l Accumulat in endolymph
l & perilymph
l Hearing loss
l Loss of hair cells in
organ of corti
Most Ototoxic - neomycin
Kanamycin

18. SIDE EFFECTS
3. Neuromuscular blockage
lRear but potentially serious
lOccurs at high conc.of aminoglycosides
lrespiratory arrest ,neuromuscular paralysis
and death can occur
lNeomycin & streptomycin .

19. OTHER EFFECTS
lLess allergic reactions
lPeripheral neuritis & optic nerve damage
lIntestinal malabsorption syndrome
lDiarrhea
lFlattening of intestinal villi etc.
lNot recommended in pregnants.

20. Uses
l Gram negative infections
l Complicated urinary tract
infections.
l Complicated , skin and
soft tissue infections
l For Endocarditis.
l Intraabdominal infections.
l Severe pelvic iinflammatory
disease
l Effective against tuberculosis

21. References
lBasic Biotechnology - Colin Ratledge & Bjorn
kristiansen
lBiotechnology - U.Satyanarayana
lBiotechnology - B.D.Singh
lhttp://en.m.wikipedia.org/wiki/Aminoglycoside
lhttp://www.uic.edu/pharmacy/courses/pmpr342
/itokazu/aminoglycosides.html

22. THANK YOU