Important note: Information in this article was accurate in 1988. The state of the art may have changed since the publication date.
Pentamidine pharmacokinetics in patients with AIDS with impaired renal function.
J Infect Dis. 1987 Dec;156(6):885-90. Unique Identifier : AIDSLINE MED/88060610 Conte JE Jr; Upton RA; Lin ET; School of Medicine, University of California, San Francisco; 94143-0208.
Abstract:
In patients with normal renal function, pentamidine elimination half-life and plasma clearance (mean +/- SD) were 6.22 +/- 1.17 hr and 411 +/- 55 liters/hr, respectively. With creatinine clearances from 35 to 145 ml/min, neither the elimination half-life (P = .47) nor the plasma clearance (P = .40) was correlated with renal function. Plasma concentrations in patients receiving dialysis ranged between 5.9 and 582 ng/ml and appeared not to be significantly affected by dialysis. The number of prior doses and the elimination half-life estimated from the terminal slope were correlated (r = .81, P = .025), and the results suggested that the current assay technology is still not sensitive enough to detect true elimination half-life. Trough plasma concentrations ranged between 4.3 and 67.5 ng/ml (28.4 +/- 26.6 ng/ml) in patients who had received prior doses of pentamidine, a result suggesting that drug accumulation occurs with multiple dosing. The data suggest that dosage adjustments are not necessary with creatinine clearances of greater than 35 ml/min. Because multiple dosing leads to increased trough concentrations and drug accumulation, lower dose regimens may still be efficacious, yet associated with reduced toxicity.
Keywords: Acquired Immunodeficiency Syndrome/COMPLICATIONS/*METABOLISM Adult Amidines/*PHARMACOKINETICS Child Female Half-Life Hemodialysis Human Infant Infusions, Intravenous Injections, Intramuscular Kidney Failure, Chronic/COMPLICATIONS/*METABOLISM Male Middle Age Pentamidine/ADMINISTRATION & DOSAGE/*PHARMACOKINETICS Peritoneal Dialysis Prospective Studies Support, Non-U.S. Gov't Support, U.S. Gov't, P.H.S. JOURNAL ARTICLE
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