PMID: 12416031Nov 6, 2002Paper

Murine pharmacokinetics and metabolism of oleandrin, a cytotoxic component of Nerium oleander

Journal of Experimental Therapeutics & Oncology
Dan NiR A Newman

Abstract

Pharmacokinetic studies of [3H]oleandrin, a cardiac glycoside component of Anvirzel, were conducted in mice after either an i.v. dose (40 micrograms/kg) or a p.o. dose (80 micrograms/kg). Oleandrin was rapidly absorbed after oral dosing (Cmax at 20 min) although the elimination half-life was longer (2.3 +/- 0.5 h) than that after i.v. dosing (0.4 +/- 0.1 h). The AUC0-infinity values obtained after i.v. and p.o. dosing were 24.6 +/- 11.1 and 14.4 +/- 4.3 (ng.h/ml), respectively, resulting in an oral bioavailability of approximately 30%. After i.v. administration, oleandrin concentration in liver was approximately twice that measured in heart or kidney tissue. Oleandrigenin, the aglycone of oleandrin, was also found in these tissues. At 5 min, > 60% of the total radioactivity in liver was due to oleandrin while 28% of the given dose was present as oleandrigenin. Twenty-four hours following injection, 8% of total radioactivity was excreted in urine and contained both oleandrigenin (4.4% of the injected dose) and oleandrin (1.9%). Sixty-six percent of injected radioactivity was found in feces and consisted of oleandrin and oleandrigenin in equal amounts. Uptake of oleandrin in brain after i.p. injection of oleandrin (3 mg/kg) or ol...Continue Reading

Citations

Jan 25, 2007·Tropical Animal Health and Production·B Soto-BlancoJ E Nóbrega
Nov 23, 2007·Research in Veterinary Science·R R BarbosaB Soto-Blanco
Sep 8, 2007·Journal of Veterinary Diagnostic Investigation : Official Publication of the American Association of Veterinary Laboratory Diagnosticians, Inc·Leslie W WoodsBirgit Puschner
Feb 1, 2018·Clinical Toxicology : the Official Journal of the American Academy of Clinical Toxicology and European Association of Poisons Centres and Clinical Toxicologists·Anselm Wong, Shaun L Greene
Jan 5, 2020·Neurological Research·Sule Terzioglu-UsakMustafa Aziz Hatiboglu
Jul 9, 2020·Food and Chemical Toxicology : an International Journal Published for the British Industrial Biological Research Association·Nazia KanwalZeliha Selamoglu
Dec 12, 2018·Toxicon : Official Journal of the International Society on Toxinology·Ana Flávia M BotelhoMarília Martins Melo

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