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Chemical Compound Review

SMP1_000015     4-amino-N-[(1R,2S,3S,5S)-5- amino-2-[(2R,3R...

Synonyms: AC1L9V75, Liposomal Amikacin
 
 
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Disease relevance of AIDS-008709

 

High impact information on AIDS-008709

  • The free amikacin concentration in plasma never exceeded 17.4 +/- 1 micrograms/ml and fell rapidly (half-life, 1.47 to 1.85 h) after the administration of each dose of liposomal amikacin [5].
  • In view of the considerable activity of liposomal amikacin in experimental murine tuberculosis, this finding indicates that liberation of amikacin from the long-life liposomes occurs only in macrophages that are not usually present in the vicinity of the large extracellular clumps of bacilli in the cavity caseum [1].
  • We compared the systemic bioavailability (F) of low-clearance liposomal amikacin in rats following intravenous (i.v.), intraperitoneal (i.p.), intramuscular (i.m.) and subcutaneous (s.c.) injection (20 mg/kg) and intratracheal (i.t.) instillation (10 mg/kg) [6].
  • The plasma AUCs of liposomal amikacin exceeded the AUC of conventional i.v. amikacin by at least 25-fold for all routes [6].
  • Amikacin AUCs in regional lymph nodes exceeded plasma AUCs by 4-fold after s.c. and i.m. injection of liposomal amikacin [6].
 

Chemical compound and disease context of AIDS-008709

 

Anatomical context of AIDS-008709

  • The patient's sputum remained smear- and culture-positive during the treatment period with liposomal amikacin and for 9 months afterward [3].
  • Although complete eradication of M. avium was never achieved following intravenous infection, mycobacterial CFUs decreased by 3 to 4 logs in the spleens and livers of mice treated for three weeks with twice-weekly intravenous injections of liposomal amikacin and continued to stay low in the liver, even in the absence of specific immunity [8].

References

  1. The early bactericidal activity of a low-clearance liposomal amikacin in pulmonary tuberculosis. Donald, P.R., Sirgel, F.A., Venter, A., Smit, E., Parkin, D.P., Van de Wal, B.W., Mitchison, D.A. J. Antimicrob. Chemother. (2001) [Pubmed]
  2. Liposomal amikacin: improved treatment of Mycobacterium avium complex infection in the beige mouse model. Petersen, E.A., Grayson, J.B., Hersh, E.M., Dorr, R.T., Chiang, S.M., Oka, M., Proffitt, R.T. J. Antimicrob. Chemother. (1996) [Pubmed]
  3. Kinetics and toxicity of liposomal and conventional amikacin in a patient with multidrug-resistant tuberculosis. Whitehead, T.C., Lovering, A.M., Cropley, I.M., Wade, P., Davidson, R.N. Eur. J. Clin. Microbiol. Infect. Dis. (1998) [Pubmed]
  4. Antibacterial activity of liposomal amikacin against Pseudomonas aeruginosa in vitro. Antos, M., Trafny, E.A., Grzybowski, J. Pharmacol. Res. (1995) [Pubmed]
  5. Pharmacokinetics and urinary excretion of amikacin in low-clearance unilamellar liposomes after a single or repeated intravenous administration in the rhesus monkey. Fielding, R.M., Moon-McDermott, L., Lewis, R.O., Horner, M.J. Antimicrob. Agents Chemother. (1999) [Pubmed]
  6. Bioavailability of a small unilamellar low-clearance liposomal amikacin formulation after extravascular administration. Fielding, R.M., Moon-McDermott, L., Lewis, R.O. Journal of drug targeting. (1999) [Pubmed]
  7. The activity of low-clearance liposomal amikacin in experimental murine tuberculosis. Dhillon, J., Fielding, R., Adler-Moore, J., Goodall, R.L., Mitchison, D. J. Antimicrob. Chemother. (2001) [Pubmed]
  8. Liposomal amikacin for treatment of M. avium infections in clinically relevant experimental settings. Ehlers, S., Bucke, W., Leitzke, S., Fortmann, L., Smith, D., Hänsch, H., Hahn, H., Bancroff, G., Müller, R. Zentralbl. Bakteriol. (1996) [Pubmed]
 
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