Antibiotics Aminoglycosides -Mechanism of action -Classification -Pharmacokinetics -Side Effect Streptomycin Gentamicin Neomycin Kanamycin Market Preparation

2. A Presentation on Aminoglycoside
Antibiotic.
 Presented By:-
 Md. Ashraful Zaman Akash ID-131017
 Asraful Islam Rayhan ID-131039
 Md. Nazmus Sakib ID-131032
 Sanzida Afroze ID-131004
 Shamsunnahar Lipa ID-131021
 Md. Rubel Haque ID-131024
Dept. of PHARMACY
JESSORE UNIVERSITY OF SCIENCE & TECHNOLOGY.

3. Outline:-
 Antibiotics
 Aminoglycosides
-Mechanism of action
-Classification
-Pharmacokinetics
-Side Effect
 Streptomycin
 Gentamicin
 Neomycin
 Kanamycin
 Market Preparation

5. Antibiotics ?

7. What is aminoglycoside ?

8. Aminoglycosides are a group of antibiotics that are
effective against:
Aminoglycoside
(AGL)
Aerobic gram( - )bacteria
e.g.: pseudomonas,
Acinetobacter,
enterobacter
Some mycobacteria
e.g.:
bacteria that cause
tuberculosis
Some gram ( + ) bacteria

9. Characteristics of Aminoglycosides:-
 Formulations are Sulfate or hydrochloric salts
 Formulations are water soluble and stable
 Highly polar basic drugs.
 Ionize during dissolution
 Penetration through BBB is minimal
 Least metabolized by hepatic enzymes
 Excretion is mainly renal

10. Bactericidal in nature
More active in alkaline pH
MOA is by interfering with protein synthesis
Attach with 30S ribosomal subunit (ATT)
Mainly gram negative
Therapeutic index is narrow
Natural and semi-synthetic antibiotics
Characteristics of Aminoglycosides:-

12. Mechanism of action of AGL

14. Resistance against aminoglycosides
 Development and synthesis of plasmid mediated bacterial
transferase enzyme, which inactivates Aminoglycosides.
 Impaired active transport
 Inactivating enzymes in the cell membrane & inactivate
Aminoglycosides
 Aminoglycoside can not bind at target ribosomal subunit
and site.
 Decreased affinity of ribosomal proteins for binding with
Aminoglycosides

17. Aminoglycoside
(AGL)
Stretomyces
Suffix -mycin
Streptomycin Paromomycin
Neomycin Tobramycin
Micromonospora
Suffix -micin
Gentamicin Amikacin
Netilmicin
Common Members of Aminoglycosides

19. Streptomycin

20. Streptomycin
Streptomycin is
discovered by the
American scientist
Harry Waxman in
1944
Harry Waxman

21. Source of Streptomycin :-
Streptomyces griseus

22. Streptomycin
• Narrow spectrum (Gram negative)
• Bacteriocidal (High dose)
• Bacteriostatic (Low dose)
• Resistance develops fast

24. Mechanism of action of Streptomycin
Streptomycin
Binds with 30s
ribosomal sub-unit
Block peptide
formation
Inhibit protein
synthesis

25. Indication of Streptomycin :-
 Pulmonary Tuberculosis
 Plague
 Dysentery
 SABE
 Urinary tract infection
 Respiratory tract infection
 Peritonitis & Meningitis

26. Contraindication of Streptomycin
1.Kidney disease 2.Disturbance of
hearing

27. Adverse effects of Streptomycin
1.Ototoxicity
2.Nephrotoxicity
3.Neurotoxity
4.Hypersensitivity
5.Superinfection

29. Gentamicin

30. Gentamicin
Gentamicin was
discovered by
G.Wagman in 1963.
G. Wagman

31. Source :-
Micromonospora purpurea

32. Gentamicin
 Broad spectrum
 Most commonly used Aminoglycosides
 Synergism with Beta lactams
 Activity decreases in presence of pus
 Use- Usually in combination with Penicillin, Cephalosporin

33. Structure of Gentamicin

34. Pharmacokinetics of Gentamicin

35. Indication of Gentamycin
 Bacteraemia & septicaemia
 Abdominal & pelvic sepsis
 Infected Burn
 Osteomyelitis
 Peritonitis
 Pneumonia

36. •Allergic responses
•Neuromuscular problems
•Rash
•Haemolytic anaemia
•Nerve damage
Adverse effects

37. Neomycin

38. Neomycin
Neomycin is also
discovered by the
American scientist
Harry Waxman in
1949.

39. Source:-
Streptomyces fradiae

40.  Neomycin is an aminoglycoside antibiotic found in
many topical medications such as creams, ointments,
and eyedrops.
 Poorly absorbed in GIT
 Excreted by the GIT.
Neomycin

41. Indication:-
 Topical preparation used in:-
1. Infected wounds
2. Infected burns
3. Infected ulcers
4. Infected dermatosis
 Oral preparation Used in:-
1. Surgery
2. Hepatic coma.

42. Kanamycin
 Highly Ototoxic
 Highly Nephrotoxic
 Narrow spectrum
 Rarely used now
 Second line anti-tubercular drug

44. Amikacin

45. Amikacin
 Semi-synthetic derivative of Kanamycin
 Resistant is less
 Widest spectrum
 Reserve drug as alternate to Gentamicin
 More hearing loss

46. Tobramycin
 More active against Pseudomonas
and Proteus
 Reserve alternative of Gentamicin

47. Sisomicin:-
Obtained from Micromonospora
Same as gentamicin
Greater efficacy against
Pseudomonas

48. Special concern in treatment:-

49. Special concern in treatment:-
 Tobramycin is superior to gentamicin for treatment of
P.aeruginosa .
 Gentamicin is the preferred AGL used in combination treatment of
enterococcal endocarditis.
 Streptomycin has the greatest activity of all the AGL against
M.tuberculosis.
 Capreomycin is an AGL use as alternative drug to treat of
mycobacterial infection
 Streptomycin & gentamicin are drugs of choice to treat tularemia
 Streptomycin is drug of choice to treat plague & brucellosis

50. Patient counseling :
 Do not take AGL if you are pregnant or could become pregnant during
treatment.
 Do not take AGL if you are breast-feeding a baby.
 Take each dose with a full glass of water.
 Take AGL with food.
 Store AGL at room temperature away from moisture, heat, and direct light.

51. Available dosage form
( all aminoglycosides have very poor
absorption from G.I.T )
Dose regimen
(if creatinine clerance > 90ml/min)
Drug
I.V , I.MI.V
25-30 mg/weak ( tuberculosis )Streptomycin
OralOral
500 mgParomomycin
Oral , topical
It is not given intravenously, as it is extremely
nephrotoxic
Oral
For hepatic encephalopathy :
4-12 gm/d
As prophylactic in GI surgery :
1.0 gm po x3 with erythromycin
Neomycin
I.V , I.M , inhalationI.V
5.1 ( if critically ill ) mg/kg q24hTobramycin
I.V , I.M , Topical
I.V
5.1 ( if critically ill ) mg/kg q24hGentamicin
I.V , I.M
I.V
15mg/kg q24hAmikacin
I.V , I.M
The lowest ototoxic AGL
I.V
6.5 mg/kg q24hNetilmicin

53. Market Preparation of aminoglycosidic
Drug
IN
Bangladesh

54. Market Preparation Of Streptomycin
 Brand Name:- Streptopen (Renata Pharma Ltd.)
 Dose:- Streptomycin 1gm/vial
 Dosage Form :- Injection

55. Market Preparation Of Gentamicin

56. Market Preparation Of Neomycin

57. Market Preparation Of Amikacin