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