aminoglycosides Flashcards
natural
shatan ka gegu
streptomycin tobramycin neomycin kanamycin gentamycin
semisynthetic
apna selfish
amikacin paromomycin netilmicin sisomicin framycetin
route
IV + IM
absorption
poor GI
1% absorbed
neomycin given orally for local use
highly polar low lipid solubility
freely circulate in blood
low plasma protein binding
distribution
poor
poor blood conc.
high conc - middle ear + kidney
plasma half life
2-3hrs
effect persists for 24hrs - post antibiotic effect
give once daily
excretiom
kidney + freely filtered
metabolism
not in body
MOA
passive diffusion through outer porin channels
reach periplasmic space
cross cell mem. by active transport ( energy+oxygen dependent rx EDP-1)
BIND TO 30S SUBUNIT
block initiation + terminate + add incorrect AA
inhibit protein syn
bacteriocidal effect
transport inhibited by
low pH
anaerobic cond.
Ca++
transport promoted by
B-lactam drugs
KEEP STaPled CaSh in PurSe
klebsiella enterobacter e. coli pseudomonas +proteus s. agalactaei TB + talaremia plague catarrhalis shigella influenza providentia serratia
resistance
dec. permeation
inactivation of drug
deletion of 30S receptor
gentamycin
micromonospora purperae IV + IM combination with b lactam drug g+ /G- active anaerobes - no activity
(G) aerobic g+
UTI
meningitis
pneumonia
septicemia
peritonitis
peritonial dialysis
inf.
p. aeruginosa
MRSA
g- bacilli
burn
endocarditis
enterococcal
with penicillin