Pharmacokinetics and effects of aminorex in horses
- 1 May 2008
- journal article
- Published by American Veterinary Medical Association (AVMA) in American Journal of Veterinary Research
- Vol. 69 (5), 675-681
- https://doi.org/10.2460/ajvr.69.5.675
Abstract
Objective—To investigate the pharmacokinetics and behavioral effects of aminorex administered IV and PO in horses. Animals—7 Thoroughbreds. Procedures—In a cross-over design, aminorex (0.03 mg/kg) was administered IV or PO. Plasma and urinary aminorex concentrations were determined via liquid chromatography– mass spectrometry. Results—Decrease of aminorex from plasma following IV administration was described by a 3-compartment pharmacokinetic model. Median (range) values of α, β, and γ half-lives were 0.04 (0.01 to 0.28), 2.30 (1.23 to 3.09), and 18.82 (8.13 to 46.64) hours, respectively. Total body and renal clearance, the area under the plasma time curve, and initial volume of distribution were 37.26 (28.61 to 56.24) mL·min/kg, 1.25 (0.85 to 2.05) mL·min/kg, 13.39 (8.82 to 17.37) ng·h/mL, and 1.44 (0.10 to 3.64) L/kg, respectively. Oral administration was described by a 2-compartment model with first-order absorption, elimination from the central compartment, and distribution into peripheral compartments. The absorption half-life was 0.29 (0.12 to 1.07) hours, whereas the β and γ elimination phases were 1.93 (1.01 to 3.17) and 23.57 (15.16 to 47.45) hours, respectively. The area under the curve for PO administration was 10.38 (4.85 to 13.40) ng·h/mL and the fractional absorption was 81.8% (33.8% to 86.9%). Conclusions and Clinical Relevance—Aminorex administered IV had a large volume of distribution, initial rapid decrease, and an extended terminal elimination. Following PO administration, there was rapid absorption, rapid initial decrease, and an extended terminal elimination. At a dose of 0.03 mg/kg, the only effects detected were transient and central in origin and were observed only following IV administration.Keywords
This publication has 23 references indexed in Scilit:
- Anorectic Drugs and Pulmonary Hypertension from the Bedside to the BenchThe American Journal of the Medical Sciences, 2001
- Aminorex, Fenfluramine, and Chlorphentermine Are Serotonin Transporter SubstratesCirculation, 1999
- Aminorex to Fen/PhenCirculation, 1999
- Valvular Heart Disease Associated with Fenfluramine–PhentermineNew England Journal of Medicine, 1997
- Anorexic Agents Aminorex, Fenfluramine, and Dexfenfluramine Inhibit Potassium Current in Rat Pulmonary Vascular Smooth Muscle and Cause Pulmonary VasoconstrictionCirculation, 1996
- Stimulus properties of some analogues of 4-methylaminorexPharmacology Biochemistry and Behavior, 1995
- Evaluation of the abuse liability of aminorexDrug and Alcohol Dependence, 1994
- Aminorex produces stimulus effects similar to amphetamine and unlike those of fenfluraminePharmacology Biochemistry and Behavior, 1992
- Appearance of Aminorex as a Designer Analog of MethylaminorexJournal of Forensic Sciences, 1991
- 2-amino-5-Aryl-2-oxazolines. Potent New Anorectic AgentsJournal of Medicinal Chemistry, 1963