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
topical
ocular inf
inf. burn wounds
intrathecal
meningitis
g-
not recommended
g+
toxicities
nephrotoxicity - 5-35% - reversible - 3-5 days
ototoxicity - irreversible - vesitubular dysfunc.
hypersensitivity
neuromuscular blockade
mycobact. inf.
streptomycin
IM + IV
TB
other TB drugs
intensive phase
non-tuberculous inf.
strep
IM
tularemia + plague + brucellosis - zoonotic
combination therapy
strep + penicillin
enterococcal
endocarditis
streptococcal inf.
topical neomycin
inf. of skin- burns+wounds+ulcers+dermatosis
ointments- inf. skin lesions - staphylococcal inf
oral neomycin
preperation of bowel for surgery
hepatic coma neomycin
prevent encephlopathy
kenamycin
toxic- parental
peritonial cavity after op.
parmomycin
parental route
luminal amoebiasis’
visceral leishmaniosis
framycetin
inf. burns
not parental route
too toxic
neomycin
parmomycin
framycetin
amikacin
derivative of kanamycin
resistant- enzyme -degenerate tobramycin + gentamycin
nosocomial + serious + g- + bacilli inf - in hospitals
atypical mycobacteria in AIDS
multidrug resistant strains _ TB
tobramycin
similar to gentamycin
more active - pseudomonas
natilmicin
resistant - enzyme - degeneration of gentamycin + tobramycin
used against resistant strains
nephrotoxicity
time+ conc. dependent
peak b/w 20-40
trough b/w 4-8
ototoxicity
high conc. in perilymph + endolymph - inner ear
destroy hair cells
maybe permanent
hearing loss - tinitis - dizziness - ataxia
toxicity aggrevated by
- furosemide / ethacrynic acid
- elderly patients
- more than 5 days
- high conc.
- renal insufficiency
most ototoxic
kanamycin, neomycin, amikacin
most vesitubulotoxic
Streptomycin & gentamycin
most nephrotoxic
Neomycin
Tobramycin
Gentamicin
reversible nephrotoxicity
high conc. renal medlulla malfunc. dec. GFR protein hyaline granular castes - urine aggrevate - vancomycin + cyclosporin +amphotericin b
neuromuscular blockade
antidote; Ca++ gluconate or Neostigmine
hypersensitivity
streptomycin
cns
rare
optic nerve damage
neuritis
local irritation
IM
contradictions
pregnancy
renal failure
with neuromuscular blockades
known hypersensitivity
