Abstract
The pharmacokinetics of isepamicin, a broad-spectrum aminoglycoside antibiotic, were studied in men after intravenous administration. Three groups of six volunteers received isepamicin for 10 consecutive days by 0.5-h intravenous infusions at respective dosages of 7.5 mg/kg of body weight once daily, 7.5 mg/kg twice daily, and 15 mg/kg once daily. Levels of isepamicin in plasma and urine were determined by a specific high-performance liquid chromatography method. For all three groups, steady-state concentrations of the drug in plasma were attained with the first dose. The area under the concentration-time curve for plasma and urinary drug excretion were dose proportional. A half-life ranging from 2.0 to 2.5 h was independent of the dosage regimen. Isepamicin excreted in urine over 24 h accounted for about 100% of the dose. The results show that the pharmacokinetics of isepamicin are linear with these dosage regimens. The drug does not accumulate upon multiple dosing, undergoes no detectable biotransformation, and is cleared solely by urinary excretion.
Full Text
The Full Text of this article is available as a PDF (173.5 KB).
Selected References
These references are in PubMed. This may not be the complete list of references from this article.
- Chung M., Costello R., Symchowicz S. Comparison of netilmicin and gentamicin pharmacokinetics in humans. Antimicrob Agents Chemother. 1980 Feb;17(2):184–187. doi: 10.1128/aac.17.2.184. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Chung M., Schrogie J. J., Symchowicz S. Pharmacokinetic study of sisomicin in humans. J Pharmacokinet Biopharm. 1981 Oct;9(5):535–551. doi: 10.1007/BF01061025. [DOI] [PubMed] [Google Scholar]
- Jacoby G. A., Blaser M. J., Santanam P., Hächler H., Kayser F. H., Hare R. S., Miller G. H. Appearance of amikacin and tobramycin resistance due to 4'-aminoglycoside nucleotidyltransferase [ANT(4')-II] in gram-negative pathogens. Antimicrob Agents Chemother. 1990 Dec;34(12):2381–2386. doi: 10.1128/aac.34.12.2381. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Jahre J. A., Fu K. P., Neu H. C. Kinetics of netilmicin and gentamicin. Clin Pharmacol Ther. 1978 May;23(5):591–597. doi: 10.1002/cpt1978235591. [DOI] [PubMed] [Google Scholar]
- Laskin O. L., Longstreth J. A., Smith C. R., Lietman P. S. Netilmicin and gentamicin multidose kinetics in normal subjects. Clin Pharmacol Ther. 1983 Nov;34(5):644–650. doi: 10.1038/clpt.1983.227. [DOI] [PubMed] [Google Scholar]
- Lin C., Korduba C., Affrime M., Radwanski E., Nomeir A., Batra V., Cutler D., Cayen M. N. Pharmacokinetics and metabolism of 14C-isepamicin in humans following intravenous administration. Antimicrob Agents Chemother. 1995 Oct;39(10):2201–2203. doi: 10.1128/aac.39.10.2201. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Neu H. C., Fu K. P. 1-N HAPA gentamicin B, a new aminoglycoside active against gentamicin resistant isolates--activity compared to other aminoglycosides. J Antibiot (Tokyo) 1978 May;31(5):385–393. doi: 10.7164/antibiotics.31.385. [DOI] [PubMed] [Google Scholar]
- Pechere J. C., Dugal R. Clinical pharmacokinetics of aminoglycoside antibiotics. Clin Pharmacokinet. 1979 May-Jun;4(3):170–199. doi: 10.2165/00003088-197904030-00002. [DOI] [PubMed] [Google Scholar]
- Pechere J. C., Dugal R., Pechere M. M. Kinetics of netilmicin in man. Clin Pharmacol Ther. 1978 Jun;23(6):677–684. doi: 10.1002/cpt1978236677. [DOI] [PubMed] [Google Scholar]
- Regamey C., Gordon R. C., Kirby W. M. Comparative pharmacokinetics of tobramycin and gentamicin. Clin Pharmacol Ther. 1973 May-Jun;14(3):396–403. doi: 10.1002/cpt1973143396. [DOI] [PubMed] [Google Scholar]
- Winslade N. E., Adelman M. H., Evans E. J., Schentag J. J. Single-dose accumulation pharmacokinetics of tobramycin and netilmicin in normal volunteers. Antimicrob Agents Chemother. 1987 Apr;31(4):605–609. doi: 10.1128/aac.31.4.605. [DOI] [PMC free article] [PubMed] [Google Scholar]