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Placental transfer of diphenhydramine in chronically instrumented pregnant sheep.

Authors
  • Yoo, S D
  • Axelson, J E
  • Taylor, S M
  • Rurak, D W
Type
Published Article
Journal
Journal of pharmaceutical sciences
Publication Date
Jul 01, 1986
Volume
75
Issue
7
Pages
685–687
Identifiers
PMID: 3761171
Source
Medline
License
Unknown

Abstract

To study the placental transfer and pharmacokinetics of the H1 receptor blocker, diphenhydramine [2-(diphenylmethoxy)-N,N-dimethylethylamine], 100 mg of the drug was administered to four pregnant sheep (122-129 d gestation) by intravenous injection through catheters chronically implanted in the ewe and fetus. Rapid placental transfer occurred, with peak fetal plasma concentrations occurring within 5 min after injection. The fetal-maternal ratio of the area under the plasma concentration versus time curves averaged 0.85, indicating significant fetal exposure to the drug. The average apparent terminal elimination half-life in the ewe (52 min) was not significantly different from that obtained in the fetus (46 min). The maternal total body clearance was 3.6 L X h-1 X kg-1, and the volume of distribution at steady state was 3.2 L/kg. In summary, this study demonstrates rapid and extensive placental transfer of diphenhydramine after maternal drug administration. Since placental permeability to lipid-soluble compounds does not differ greatly in different species, it is likely that a similar situation exists in humans.

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