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Eur J Clin Pharmacol ; 55(10): 755-9, 2000 Jan.
Article in English | MEDLINE | ID: mdl-10663455

ABSTRACT

OBJECTIVE: We investigated whether sulfoconjugation contributes to the inactivation of intravenously infused dopamine (DA) in low concentrations with a predominant action on the kidney. METHODS: Plasma DA and dopamine sulfate (DA-S) concentrations were determined during 4 h of intravenous infusion of DA (2 microg/kg/min) and up to 18 h after cessation of infusion. Twenty-seven healthy young subjects participated in the placebo controlled, randomised and double-blind study. RESULTS: Intravenously administered DA was sulfoconjugated rapidly and to a great extent. After starting the infusion, DA levels rose within minutes and reached a steady state after 30-60 min. The steady-state levels averaged 151.3 +/- 8.2 nmol/l. DA-S levels also increased markedly with infusion from 16.7 +/- 9.9 nmol/l at the start of infusion up to 261.2 +/- 24.2 nmol/l at 30 min after cessation of infusion. Plasma DA concentrations after cessation of the infusion decreased rapidly with an initial half-life of elimination of 4.8 min. Concentrations of plasma DA-S declined with a half-life of 4.5 h. Persistent elevations of free and conjugated DA compared with pre-treatment levels were observed even 18 h after cessation. Heart rate and blood pressure remained unchanged both during DA and saline infusion. CONCLUSION: Findings indicate that the sulfoconjugation pathway contributes markedly to the inactivation of intravenously infused DA and seems not to be saturable by DA infusion in low doses.


Subject(s)
Dopamine/blood , Sulfuric Acid Esters/blood , Adult , Blood Pressure/drug effects , Dopamine/administration & dosage , Dopamine/pharmacokinetics , Heart Rate/drug effects , Humans , Infusions, Intravenous , Male , Time Factors
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