| Autor: |
Yoo, S.D., Axelson, J.E., Taylor, S.M., Rurak, D.W. |
| Zdroj: |
Journal of Pharmaceutical Sciences; July 1986, Vol. 75 Issue: 7 p685-687, 3p |
| Abstrakt: |
To study the placental transfer and pharmacokinetics of the H1receptor blocker, diphenhydramine [2-(diphenylmethoxy)-N,N-dimethylethylamine], 100mg 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 5min 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.h−1.kg−1, and the volume of distribution at steady state was 3.2L/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. |
| Databáze: |
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