Pharmacokinetics
and pharmacodynamics of Dextropropoxyphene (DXP)
DXP is rapidly absorbed after oral administration
and the peak plasma levels are usually attained within one hour of a single
dose. However, since DXP undergoes marked first-pass biotransformation, only a
small proportion of the absorbed dose enters the circulation in unchanged form.
The remainder of the drug is metabolized by intestinal and hepatic enzymes
during absorption, under-going demethylation to norpropoxyphene.
Hence, following repeated administration of
DXP the norpropoxyphene plasma concentration rises, and it is eliminated more
slowly than the parent drug, the plasma concentration of norpropoxyphene
becomes considerable higher than of DXP. (Wolen et al., 1971, Wagner et al.,
1972, McMahon et al., 1974, Verebely and Inturrisi, 1974, Welling et al.,
1976, Musa and Lyons, 1976, Gram et al., 1979, Gibson et al., 1980, Inturrisi et
al., 1982, Young 1983, Lawsson and Northrigde, 1987.)
It has been
found to alcohol reduces the first-pass biotransformation of DXP, so that the
availability of the administered dose may enhanced by 25-50% (Oguma and Levy,
1981, Girre et al., 1991.)
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me
Excerpts from “Studies on Dextropropoxyphene With Special Reference to Dependence Among
Chronic Pain Patients, Classification of the Manner of Death in Fatal
Poisonings, and Characteristics of the Fatal Poisoning Victims” by Birgitta Jonasson. Acta Universitatis
Upsalienses, Uppsala 2000.
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