2. Structure GlycosidicAminosugar- O
-Aminocyclitol2-deoxystreptamine- O-AminosugarStreptomycin
Streptidine- O -Strepose aminosugar- O -N-methyl-Lglucosamine
aminosugarStreptobiosamine 3. Aminoglycosides Penetrate Bact. Cell
Wall To Periplasmic Space Transport Across Cytoplasmic Membrane
(Oxygen Dependent)Bind To 30s Ribosomal Units Prevent Formation of
Initiation Complex Misreading of Genetic Code on mRNA Incorrect
Amino Acids into Peptide Chain Inhibits Protein Synthesis 4.
Allderived from an actinomycete or are semisynthetic derivatives
Bactericidal Are actionhighly polar compoundsGIT poor absorption so
IV/IM Moreactive in alkaline pH 5. STREPTOMYCIN (1944) KANAMYCIN
(1957 ) GENTAMICIN (1964) AMIKACIN SISOMICIN NEOMYCIN NEITILMICIN
FRAMYCETIN TOBRAMYCIN 1967 6. Suffix-Mycin-Streptomyces
Micin-Micromonospora 7. Halflife 1-3hr. Concentration
Singledepended killingdaily dose result in higher tissue
concentration Interval8-12hr 8. 1. Plasmid Mediated Bacterial
TransferaseEnzymes 2. Deletion of Porin Channels 3. Alteration of
Receptor Protein on 30sRibosomal Unit 9. Very Poor Oral
Bioavailability Poor Distribution Do Not Cross BBB Excreted Through
Kidney Excretion is directly proportion to creatineclearence 10.
AEROBIC G-ve BACILLI ENTEROBACTERIACEAE NOT EFFECTIVE AGAINST :G
+ve BACILLI G ve COCCI ANAEROBES 11. OTOTOXICITY:AG causes
impairment of 8th cranial nerve., accumulate in the endolymph and
perilymph of the inner ear leading to vestibular and cochlear
damage. IrrversibleNEUROMUSCULAR BLOCKADE 12.
NEPHROTOXICITYInhibition of intracellular Phospholipase A2 in renal
brush border Leads to lysosomal distension ,rapture Release acid
hydrolases & AGFree drug binds to other cellular organelles
Leading to degeneration and necrosis 13. Spectrum : Y. Pestis,
Brucella, F.Tularensis, M.Tuberculosis TOXICITY : Vestibular >
Auditory Lowest Nephrotoxicity USES : Tuberculosis SABE Plague
Tularemia & Brucellosis 14. Spectrum : Pseudomonas, Proteus, E.
Coli, Klebsiella, Enterobacteria & Seretia. TOXICITY : More
Nephrotoxic USES : Respiratory Infection in Critically Ill Pt.
Pelvic Infection SABE UTIs Pseudomonal Infections Infected Wounds,
Burns, & Conjunctivitis 15. Clinically & PK similar to
GentamicinSusceptible to Aminoglycoside Inactivating EnzymesUsed
Interchangeably with Gentamicin 16. Semi synthetic Derivative of
SISOMYCINResistant to Inactivating EnzymesLesser OtotoxicityUsed in
Gentamicin Resistant Infections 17. Identical To Gentamicin2-4
times More Active Against Pseudomonas & ProteusOtotoxicity
& Nephrotoxicity < GentamicinReserve Alternative to G 18.
RESISTANT TO BACTERIAL ENZYMESUSED against Gentamicin &
Tobramycin Resistant InfectionsUSES: Multi drug Resistant TB
Hospital Acquired InfectionsHearing loss > Vestibular loss 19.
HIGHLY TOXICUESE Infected Wounds, Ulcers, Burn External Ear &
Eye Infections Preoperative Intestinal Antiseptic Hepatic Coma
