Diazepam and N-desmethyldiazepam redistribution after heparin

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Abstract
The effects of heparin [HR], 1000 U i.v., on the blood, plasma and free concentrations of diazepam [DZ] and its metabolite, N-desmethyldiazepam [N-DD], were investigated 3 h after oral administration of 10 mg DZ to 5 normal human subjects. The percent free DZ and N-DD increased 15 min after HR from 1.66 .+-. 0.35 to 3.99 .+-. 1.88 in the case of DZ and from 2.50 .+-. 0.65 to 5.00 .+-. 1.96 in the case of its metabolite. The actual free concentration of DZ rose from 3.6 .+-. 1.04 to 6.9 .+-. 1.33 ng/ml 15 min after HR while total blood concentration was unchanged (144 .+-. 54 vs. 130 .+-. 57 ng/ml). Free concentrations of N-DD rose from 0.62 .+-. 0.17 to 1.01 .+-. 0.34 but the effect, though consistent, was not statistically significant. Blood concentrations did not change (15 .+-. 3.2 vs. 14 .+-. 3.9 ng/ml). That free drug level rose without a change in blood or total plasma levels suggests that factors other than simple plasma binding displacement are involved in this drug interaction.

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