Effects of 4-Ethoxy-2-methy1-5-morpholino-3 (2H) -pyridazinone (M 73101) on Healthy Man. II. Blood Concentration and Urinary Excretion

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Blood levels and urinary excretion of 4-ethoxy-2-methyl-5-morpholino-3 (2H) -pyridazinone (M 73101) and its metabolites in man were studied. Eighteen healthy male volunteers were administered with oral single dose of M 73101 as follows: 3 volunteers with 1.0mg/kg, 5 with 2.5mg/kg, 3 with 5.0mg/kg, 5 with 10.0mg/kg and 2 with 15.0mg/kg. Two volunteers were medicated with oral repeated dose, three times of 5.0mg/kg at intervals of 4 hours.<BR>The maximal level of unchanged M 73101 was observed at 1/2-1 hour after the single administration, which indicates rapid absorption into the blood from the gastrointestine. The administration of M 73101 did not show a significant ac-cumulation. Metabolites were also detected in the blood but their amount was even less than unchanged M 73101. Increase of blood levels of unchanged M 73101 and its metabolites depended on administered dose. Changes of these blood levels, furthermore, paralleled to the potency of analgesic effect.<BR>The urinary excretion during 0-4 hours was about 50% to the administereddose, and about 70-80% during 0-24 hours. The major urinary metabolite was 5- [carboxymethyl- (2-hydroxyethyl) -amino] -4-ethoxy-2-methyl-3 (2H) -pyrida-zinone (M-6), about 60% to the administered dose, whereas unchanged M 73101 was hardly excreted.
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