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Protein synthesis inhibitors, image - Coggle Diagram
Protein synthesis inhibitors
Aminoglycosides
MOA
Resistance
Decreased efficiency of the aminoglycoside
transporting mechanism
Mutation decreasing the affinity
Inactivating enzymes by conjugation and transfer of plasmids.
polybasic amino groups linked
glycosidically to two or more aminosugar
Streptomycin was the first member in 1944 by Waksman
pk
injection site in muscles is rapid: peak
plasma levels are attained in 30–60 minutes
distributed only extracellularly
Low concentrations -serous fluids
Not metabolized, Excreted unchanged in urine- GF
Entry in steps in G- Difffusion through porins and crossing cytoplasmic membrane by carrier mediated energy dependent processes
Action
streptomycin
binds to 30S ribosomes
cell wall synthesis inhibitors exhibit synergism
Penetration is favoured by high pH
~20 times more active in alkaline than in acidic medium.
Dosing
Streptomycin/kanamycin/amikacin 7.5–15 mg/kg/day
Gentamicin/tobramycin/sisomicin/netilmicin 3–5 mg/kg/day
conc dependent killing and PAE
subthreshold for
ototoxicity and nephrotoxicity
Toxicity
ototoxicity irreversible
vestibular S(most),T
cochlear A(most), K, Neo, T
Netil- least
nephrotoxicity
Neo(most) so topical
G(most), Tobra
S(least)
NM blockade
inhi of presynaptic Ach release and postsynaptic sensitivity decrease
Resp. depression treat-iv calcium
Risk factrs- hypocalcemia, periotoneal administration, CI- MG
Neo,S(most), T(least)
Uses
Neo& framycetin topical neo gut sterilisation in HE
Netil- serious infections
S- Tb, plague,tularemia
Synergistic with B lactams
G,T,A against G- except salmonella
A- 2nd line tb
Spectinomycin- PPNG & P allergic gonorrhea
