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Kinetics, dynamics, and bioavailability of bumetanide in healthy subjects and patients with chronic renal failure
Author(s) -
Lau Henry S H,
Hyneck Martha L,
Berardi Rosemary R,
Swartz Richard D,
Smith David E
Publication year - 1986
Publication title -
clinical pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.941
H-Index - 188
eISSN - 1532-6535
pISSN - 0009-9236
DOI - 10.1038/clpt.1986.112
Subject(s) - bumetanide , bioavailability , diuretic , crossover study , renal function , volume of distribution , medicine , pharmacokinetics , excretion , chemistry , free water clearance , endocrinology , creatinine , fractional excretion of sodium , chronic renal failure , pharmacology , sodium , cotransporter , alternative medicine , organic chemistry , pathology , placebo
Six patients with chronic renal failure (CRF group) and four healthy subjects (HS group) were given 5 mg oral and intravenous doses of bumetanide in a random, crossover design. The CRF group had significantly lower plasma and renal clearances, resulting in a five‐ to sixfold reduction in the fractional urinary excretion of the drug. The percent free drug in plasma for the CRF group was more than double that for the HS group, and significant correlations were observed for volume of distribution at steady state vs. percent free (r = 0.661; P < 0.05), nonrenal clearance vs. percent free (r = 0.796; P < 0.01), and renal clearance vs. creatinine clearance (r = 0.995; P < 0.001). Although bioavailability was relatively consistent among the HS (0.664 ± 0.112) and CRF (0.689 ± 0.149) groups, the absorption‐time profiles were more irregular for both groups. Cumulative sodium excretion and overall efficiency of response to bumetanide did not differ significantly between the two routes of administration in either group. Clinical Pharmacology and Therapeutics (1986) 39, 635–645; doi: 10.1038/clpt.1986.112