J Pharm Pharmacol. 1989 Jun;41(6):384-7. doi: 10.1111/j.2042-7158.1989.tb06482.x.

Pharmacokinetic profile of idazoxan in the beagle dog.

The Journal of pharmacy and pharmacology

J Vallès, J Pruñonosa, A Menargues, M Nomen, R Obach

PMID: 2570833 DOI: 10.1111/j.2042-7158.1989.tb06482.x

Abstract

The alpha 2-antagonist idazoxan (2- (2- (1,4-benzodioxanyl))-2-imidazoline) has been given intravenously and orally to five beagle dogs at 1, 3 and 10 mg kg-1 doses. Idazoxan plasma levels were determined by a HPLC method. After intravenous administration, a linear kinetic behaviour was obtained. Half-life and mean residence time values ranged 105.2-117.1 and 138.1-154.0 min, respectively. Total plasma clearance values and volume of distribution at steady state values ranged from 25.6-32.1 (mL kg-1) min-1 and 3.60-4.36 L kg-1, respectively. After oral administration, time to peak values averaged around 1 h. Dose normalized peak concentration values ranged 161-182 ng mL-1. Bioavailability values ranged 60-88%. Low idazoxan bioavailability has been described in other animal species and attributed to a first-pass effect.

Substances

• Adrenergic alpha-Antagonists
• Dioxanes
• Dioxins
• Indicators and Reagents
• Idazoxan

MeSH terms

• Administration, Oral
• Adrenergic alpha-Antagonists / pharmacokinetics
• Animals
• Dioxanes / pharmacokinetics
• Dioxins / pharmacokinetics
• Dogs
• Half-Life
• Idazoxan
• Indicators and Reagents
• Injections, Intravenous
• Male

Publication Types

• Journal Article

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