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Aminoglycosides Antibiotic
- 2. A Presentation onAminoglycoside 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 -Mechanismof action -Classification -Pharmacokinetics -Side Effect Streptomycin Gentamicin Neomycin Kanamycin Market Preparation
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- 8. Aminoglycosides are agroup 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 Moreactive 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 actionof 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 NeomycinTobramycin Micromonospora Suffix -micin Gentamicin Amikacin Netilmicin Common Members of Aminoglycosides
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- 20. Streptomycin Streptomycin is discovered bythe 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 actionof 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.Kidneydisease 2.Disturbance of hearing
- 27. Adverse effects ofStreptomycin 1.Ototoxicity 2.Nephrotoxicity 3.Neurotoxity 4.Hypersensitivity 5.Superinfection
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- 30. Gentamicin Gentamicin was discovered by G.Wagmanin 1963. G. Wagman
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- 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
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- 35. Indication of Gentamycin Bacteraemia & septicaemia Abdominal & pelvic sepsis Infected Burn Osteomyelitis Peritonitis Pneumonia
- 36. •Allergic responses •Neuromuscular problems •Rash •Haemolyticanaemia •Nerve damage Adverse effects
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- 38. Neomycin Neomycin is also discoveredby the American scientist Harry Waxman in 1949.
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- 40. Neomycin isan 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 preparationused 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
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- 45. Amikacin Semi-synthetic derivativeof Kanamycin Resistant is less Widest spectrum Reserve drug as alternate to Gentamicin More hearing loss
- 46. Tobramycin More activeagainst Pseudomonas and Proteus Reserve alternative of Gentamicin
- 47. Sisomicin:- Obtained from Micromonospora Sameas gentamicin Greater efficacy against Pseudomonas
- 48. Special concern intreatment:-
- 49. Special concern intreatment:- 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 ofaminoglycosidic Drug IN Bangladesh
- 54. Market Preparation OfStreptomycin Brand Name:- Streptopen (Renata Pharma Ltd.) Dose:- Streptomycin 1gm/vial Dosage Form :- Injection
- 55. Market Preparation OfGentamicin
- 56. Market Preparation OfNeomycin
- 57. Market Preparation OfAmikacin