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Flunisolide metabolism and dynamics of a metabolite
A metabolic explanation for the clinical observation that flunisolide can be administered intranasally and by inhalation in therapeutically effective doses without causing significant reduction in adrenal function is offered.
Absorption, distribution, metabolism, and excretion of naproxen in various laboratory animals and human subjects.
Naproxen was found to be rapidly absorbed in all species and, once in the blood, was eliminated with half-lives ranging from 2 to 35 hr, while the rat and the monkey showed minor amounts of transformation products.
Clinical pharmacokinetics of ganciclovir in patients with normal and impaired renal function.
Hemodialysis efficiently reduced levels of ganciclovir in plasma by approximately 53.0% +/- 11.5%, a finding that indicates this drug should be administered after dialysis.
Chiral Kinetics and Dynamics of Ketorolac
The data demonstrate that the kinetics and interconversion of the enantiomers of ketorolac is different in animals and humans as well as from most other NSAIDs.
Nonlinear plasma level response to high doses of naproxen
Accelerated renal clearance at high doses because of disproportionate increases in the amount of unbound drug appeared to be the most likely explanation for the plateau effect of naproxen.
Pharmacokinetics of naproxen overdoses
The pharmacokinetics of naproxen when administered in single doses of J, 2, 3, or 4 gm (up to eight times the clinically e.ffective dose in rheumatoid arthritis) to healthy subjects are described and an increase in urinary excretion rate and continuation of the previously documented nonlinear plasma level response were observed.
Inhibition and induction of hepatic drug metabolism in rats and mice by nafimidone and its major metabolite nafimidone alcohol.
Induction of a predominating cytochrome P-448-type of Phase I drug-metabolizing activity by nafimidone alcohol is suggested, which is similar to that of imidazole.
Sex-dependent differences in drug metabolism in the rat. IV. Effect of morphine administration.
The concept that administered morphine depresses the metabolism of type I drugs in mature male rats by impairing an androgen-induced stimulation of the hepatic mono-oxidase system is supported.
Role of phospholipids in the hepatic microsomal drug-metabolizing system.
These studies provide further evidence that the type I and type II binding sites differ and that thetype I binding site is associated with membrane phospholipids, and show that type I binding is not required for the oxidation of type I compounds by microsomal enzymes.
Disposition of flunisolide in the rat, mouse, dog, rhesus monkey, and cynomolgus monkey.
  • N. Chu, B. Amos, +7 authors M. Chaplin
  • Chemistry, Medicine
    Drug metabolism and disposition: the biological…
  • 1 March 1979
Radioactivity was rapidly and efficiently absorbed in all species, but in the rhesus and cynomolgus monkeys most of the plasma radioactivity was due to the 6 beta-OH metabolite and to water-soluble conjugates, suggesting extensive first-pass metabolism of flunisolide.