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THE ABSORPTION, PHARMACODYNAMICS, METABOLISM AND EXCRETION OF 14 C‐SUMATRIPTAN FOLLOWING INTRANASAL ADMINISTRATION TO THE BEAGLE DOG
Author(s) -
BARROW A.,
DIXON C. M.,
SAYNOR D. A.,
PERREN M. J.,
STOWE R.,
SMITH I.
Publication year - 1997
Publication title -
biopharmaceutics and drug disposition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.419
H-Index - 58
eISSN - 1099-081X
pISSN - 0142-2782
DOI - 10.1002/(sici)1099-081x(199707)18:5<443::aid-bdd35>3.0.co;2-d
Subject(s) - sumatriptan , nasal administration , pharmacokinetics , beagle , pharmacology , medicine , bioavailability , excretion , absorption (acoustics) , pharmacodynamics , route of administration , anesthesia , endocrinology , receptor , physics , acoustics , agonist
The pharmacodynamics, pharmacokinetics, metabolism, and excretion of 14 C‐sumatriptan have been studied in the beagle dog following administration by the intranasal and other routes. The pharmacological response which was monitored, an increase in carotid arterial vascular resistance, correlated with the plasma levels of unchanged sumatriptan following intranasal, intravenous, or intraduodenal administration to the anaesthetised dog. The pharmacokinetics and metabolism of sumatriptan were then confirmed in conscious male and female dogs. Intranasal administration of 14 C‐sumatriptan resulted in rapid absorption of part of the dose. The overall bioavailability of sumatriptan was 40–50%. Sumatriptan was eliminated from plasma with a half‐life of 1·5 or 1·9 h after intravenous or intranasal dosage respectively. Radioactivity was largely excreted in urine (up to 75% of the dose) with small amounts in the bile and faeces after intravenous and intranasal dosing, as sumatriptan and a major metabolite. The results from these studies suggest that intranasal administration provides a viable method for delivering sumatriptan to the systemic circulation. © 1997 John Wiley & Sons, Ltd.