医学ppt课件_《医用基础药理学》.pptVIP

* * * * * * * * * * * * * * * * * * * * Spectrum of activity of Aminoglycosides Aminoglycosides are effective against aerobic gram-negative bacteria, especially in bacteremia, sepsis, or endocarditis. Mechanism of action of Aminoglycosides The mechanism of Aminoglycosides is to inhibit protein synthesis in susceptible microorganisms?. by interfering with the initiation complex of peptide formation. inducing misreading of the code on the mRNA template, which causes incorporation of inappropriate amino acid into peptide. by rupturing the polysomes into monosome, which become nonfunctional. Pharmacokinetics of aminoglycosides The aminoglycosides are poorly absorbed from the gastrointestinal tract. Aminoglycosides must be given intramuscularly or intravemously for systemic infection. Aminoglycosides are excreted almost entirely unchanged by glomerular filtration, which is greatly reduced in renal impairment, causing toxic blood levels. Untoward effects of aminoglycosides Ototoxicity Aminoglycosides are potentially toxic to branches of the eighth cromial nerve. The evidence indicates that the sensory receptor portions of the inner ear ( hair cells of the cochlea) are affected rather than the nerve itself. The cochlear damage and vestibular impairment, cause vertigo and disturbance in maintaining postural equilibrium. Nephrotoxicity Nephrotoxicity may develop during or after use of an aminoglycosides, those elderly, debilitated patients, and patients with preexisting renal dysfunction. Nephrotoxicity is dose dependent and damage to the proximal tubular epithelium usually begins after five to seven days of therapy. The toxicity results from accumulation and retention of aminoglycosides in the proximal tubular cells. The renal injury may lead to acute renal failure.