Aminoglycoside antibiotics drugs

PJL Daniels. Aminoglycoside Antibiotics, Drug Action and Drug Resistance in Bacteria, vol. 2. Baltimore University Park Press, 1975, pp 77-111. 

Figure4.10 Nomogram fortobramycin, an aminoglycoside antibiotic. Drug Facts and Comparisons, 56 ed. (2002), p. 1408, Lippincott, St Louis. Reprinted with permission.

Smith CA, Baker EN (2002) Aminoglycoside antibiotic resistance by enzymatic deactivation. Curr Drug Targets Infect Disord 2 143-160... 

Aminoglycoside antibiotics Reduced ability of cells to take up drugs... 

Development of resistance to rifaximin is primarily due to a chromosomal one-step alteration in the drug target, DNA-dependent RNA polymerase. This differs from the plasmid-mediated resistance commonly acquired by bacteria to aminoglycoside antibiotics such as neomycin... 

A new aminoglycoside antibiotic (5 mg/kg) was infused intravenously over 30 min to a 70-kg volunteer. The plasma concentrations of the drug were measured at various times after the end of the infusion, as recorded in the table and shown in the figure below. 

Renal cell lines have been utilized to a limited extent for evaluation nephrotoxins. A rabbit kidney cell line (LLC-RKi) has been utilized for evaluating nephrotoxic antibiotics (Viano et al., 1983 Hottendorf et al., 1987 Williams et al., 1988). LLC-PKi cells have by far been the most widely employed cell line for studying drug-induced nephrotoxicity, specifically in the evaluation of aminoglycoside antibiotics (Hori et al., 1984 Schwertz et al., 1986 Williams et al., 1986b Holohan et al.,... 

Aminoglycoside Antibiotics From Chemical Biology to Drug Discovery, Second Edition, by Dev P. Arya Cop5Tight 2007 John Wiley Sons, Inc. 

This difference in half-lives in serum and tissues was misinterpreted in the early literature as an accumulation of aminoglycosides in the inner ear and held responsible for their organ-specificity. Such an interpretation is, however, not tenable. Aminoglycoside antibiotics are present in the fluids (perilymph and endolymph) and the tissues of the inner ear at relatively low levels, typically at one-tenth of peak serum levels. The reason for the differential sensitivity of inner ear sensory cells may then be based on the extreme persistence of the drugs or on an intrinsic susceptibility to their actions, notably to the generation of reactive oxygen species as described later. ... 

In principle, various targets for therapeutic intervention exist. A successful drug can interact with viral receptors, virally encoded enzymes, viral structural components, viral genes or transcripts, or cellular factors required for viral replication. In recent years, attention has been given to small molecules that can target viral-specific RNA sites and prevent the formation of key RNA-protein and RNA-RNA complexes. Aminoglycoside antibiotics have provided the impetus for this approach as discussed below. 

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