Pharmacokinetics and tolerability of intravenous infusion of adenosine (SUNY4001) in healthy volunteers.

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Uematsu T, Kozawa O, Matsuno H, Niwa M, Yoshikoshi H, Oh-uchi M, Kohno K, Nagashima S, Kanamaru M

Pharmacokinetics and tolerability of intravenous infusion of adenosine (SUNY4001) in healthy volunteers.

Br J Clin Pharmacol. 2000 Aug;50(2):177-81. doi: 10.1046/j.1365-2125.2000.00214.x.

PubMed ID
10930971 [ View in PubMed
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Abstract

AIMS: To examine the tolerability and disposition of i.v. adenosine (SUNY4001) in healthy male Japanese volunteers. METHODS: SUNY4001 was infused i.v. for 6 min at 0 (placebo), 60, 100, 120 and 140 microg kg-1 min-1 in a dose-escalating manner in 30 healthy subjects. Adenosine and its metabolites were determined in the plasma and urine. RESULTS: Only plasma hypoxanthine was increased from 3 min during until 5-10 min after SUNY4001 infusion at the higher rates without any significant dose-related changes in plasma adenosine, inosine, xanthine or uric acid, or in urinary adenosine and all metabolites compared with the placebo. There was a dose-related increase in the incidence of subjective symptoms such as heat sensation, flushed face, dyspnoea, chest discomfort, etc. Transient and self-subsiding episodes of second-degree atrioventricular block were found in two subjects each at the higher doses. CONCLUSIONS: Adenosine infusion at < or = 140 microg kg-1 min-1 was concluded to be generally well tolerated.

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