Name: Abbas sheikh Ali jimale No: 090 second year student 15/3/2011

Assignment pharmacology semester 2 circulation system

Aminoglycosides:They are used mostly widely against gram negative bacteria especially in
bacteriemia, sepsis and also with the combination of vancomysin with others used endocarditis
and the treatment tuberculosis. Common types of aminoglycosides
• Streptomycin sulphate injection Kanamycin sulphate injection,Neomycin sulphate cap,
Gentamicin sulphate injection,Tobramycin injection, Amikacin injection
Netilmicin injection,Paromomycin cap, Framycetin ointment, cream or solution.
Physical and chemical properties
Have hexose ring to which various sugars are attached glycosidic linkages so they are water
soluble, stable in solution and more active an alkaline than acidic ph.
Mechanism of resistance: Three principle mechanism of resistance
1. Production of transferaze enzyme by phosphorylation
2. Impaired entry aminoglycosides into the cell
3. Receptor protein 30s ribosomal subunit alternation
Antimicrobial activity
• Narrow spectrum antibiotics
• Gram –ve bacilli, Enterobacteriaceae – E.coli, Proteus, Klebsiella, Shigella, Pseudomonas
aeruginosa, Yersinia pestis,Pasturella tularensis, Haemophilus and Neisseria Mycobacterium
tuberculosis, MIC – 0.25 to 130 μg/ml. Mode of Action
Inhibition of protein synthesis at least three ways made by aminoglycosides and is the following:
1.Interference with the initiation complex peptide formation
2. Misreading and premature termination of MRNA at ribosome
3. Breakup polisomes into non functional monosomes other of mode of action are below:-
• Rapidly bactericidal,Inhibit protein synthesis, Bacterial killing conc. dependent
• Residual bactericidal activity, Act inside the cell, Primary site of action is 30s ribosome subunit
• Resulting abnormal proteins are fatal to microbes. Pharmokinetics properties
• Very poor GIT absorption, Rapid IM absorption, Peak plasma conc. 30 to 90 minutes,Poor
penetration in Eye, CNS, High conc. in renal cortex & inner ear, Excretion in glomerular
filtration, Aminoglycosides toxicity depend on both time and concentration. Adverse effects
All aminoglycosides can produce nephrotoxicity
& ototoxicity Neuromuscular blockade, Optic nerve dysfunction, Peripheral neuritis, Perioral
paraesthessia and fever skin rashes ,allergic and dysfunctions of vestibular
Clinical uses
Are used against gram negative enteric bacteria
• Mycobacterium infection 0.5-1g/d
• Non tuberculosis infection
• Gram –ve bacillary infection – septicemia, pelvic &
Abdominal sepsis, Bacterial endocarditis – enterococcal, streptococcal or,Staphylococcal
injection of heart valves, Pneumonias, Tuberculosis, Tularemia, Plague, Brucellosis and
immunosuppressive therapy, before surgery & inHepatic coma, U.T.I, Pneumonia, Meningitis
Endocarditis, Peritonitis, Intraabdominal and pelvic infection and septic states caused by
sensitive ,bacteria, pseudomonas, entrobacter, klebsiella, Skin, eye and ear infection. Reference:
1. basic and clinical pharmacology 10th addition page number 755-759, ISBN: 978-007-110441
author: BERTRAM G.KATZUNG
2. Introductory clinical pharmacology auther; Roachy, sally s. ISBN-13:978-0-7817-7595-3