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d ‐Propoxyphene kinetics after single oral and intravenous doses in man
Author(s) -
Gram Lars F.,
Schou Jens,
Way Walter L.,
Heltberg Jon,
Bodin Nils O.
Publication year - 1979
Publication title -
clinical pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.941
H-Index - 188
eISSN - 1532-6535
pISSN - 0009-9236
DOI - 10.1002/cpt1979264473
Subject(s) - propoxyphene , medicine , pharmacology , anesthesia , analgesic
d‐Propoxyphene kinetics was studied in 8 healthy male subjects after single oral doses of d‐propoxyphene at 65, 130, and 190 mg and after slow intravenous infusion of 65 mg. Total urinary excretion (7 days) indicated complete oral absorption but systemic availability was reduced corresponding to first‐pass elimination of 30% to 70%. There was linearity between oral dose and the corresponding area under the plasma concentration/time curve of d‐propoxyphene and the metabolite norpropoxyphene. The kinetic measurements showed 2‐ to 3‐fold interindividual variations: oral clearance, 1.3 to 3.6 Mmin; systemic clearance, 0.6 to 1.2 l/min; apparent volume of distribution, 700 to 1,800 l; d‐propoxyphene half‐life (t½), 8 to 24 hr; and norpropoxyphene t½, 18 to 29 hr. There were pronounced intraindividual dose‐independent variations in oral clearance in some subjects. The intravenous concentration curves indicated a 3‐compartment distribution model.