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Pharmacokinetics and tolerability of intravenous infusion of adenosine (SUNY4001) in healthy volunteers
Author(s) -
Uematsu Toshihiko,
Kozawa Osamu,
Matsuno Hiroyuki,
Niwa Masayuki,
Yoshikoshi Hirofumi,
Ohuchi Mikio,
Kohno Kenichi,
Nagashima Satoru,
Kanamaru Mitsutaka
Publication year - 2000
Publication title -
british journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.216
H-Index - 146
eISSN - 1365-2125
pISSN - 0306-5251
DOI - 10.1046/j.1365-2125.2000.00214.x
Subject(s) - tolerability , adenosine , hypoxanthine , medicine , pharmacokinetics , placebo , xanthine , inosine , anesthesia , pharmacology , uric acid , urine , crossover study , adverse effect , chemistry , biochemistry , alternative medicine , pathology , enzyme
AimsTo examine the tolerability and disposition of i.v. adenosine (SUNY4001) in healthy male Japanese volunteers.MethodsSUNY4001 was infused i.v. for 6 min at 0 (placebo), 60, 100, 120 and 140 µg kg −1 min −1 in a dose‐escalating manner in 30 healthy subjects. Adenosine and its metabolites were determined in the plasma and urine.ResultsOnly 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.ConclusionsAdenosine infusion at ≤ 140 µg kg −1 min −1 was concluded to be generally well tolerated.