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Protein binding of the analgesics alfentanil and sufentanil in maternal and neonatal plasma

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Summary

Maternal and umbilical venous plasma was obtained at delivery from 8 mothers and their neonates after an i.v. bolus injection of alfentanil, and from 6 mothers and their neonates after epidural administration of sufentanil. Plasma levels of total (free + bound) alfentanil in neonates were about 3.4-times lower than in their mothers. At 33–55 min after 30 µg sufentanil, total drug levels in mothers were around the limit of detection of the radioimmunoassay (0.05 ng/ml); in one mother who had received 250 µg, the plasma level of total sufentanil was 2.6-times higher than in her neonate. Plasma protein binding of alfentanil was 88.2% in mothers and 67.2% in neonates. Plasma protein binding of sufentanil was 90.7% in mothers and 79.3% in neonates. For both drugs, plasma protein binding was significantly related to the α1-acid glycoprotein (α1-AGP) level, which was about 2.5-times lower in the infants. Free alfentanil levels in mothers and neonates were similar. Free levels of sufentanil in mothers and neonates differed less from each other than did the total drug levels.

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Authors and Affiliations

  1. Departments of Drug Metabolism and Pharmacokinetics and of Clinical Research, Janssen Pharmaceutica, Beerse, Belgium

    W. Meuldermans, R. Woestenborghs, H. Noorduin & J. Heykants

  2. Department of Anaesthesiology, Academisch Ziekenhuis, Vrije Universiteit Brussel, Brussels, Belgium

    F. Camu

  3. Department of Anaesthesiology, Hôpital Ste. Anne, Brussels, Belgium

    A. van Steenberge

Authors
  1. W. Meuldermans
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  2. R. Woestenborghs
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  3. H. Noorduin
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  4. F. Camu
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  5. A. van Steenberge
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  6. J. Heykants
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Meuldermans, W., Woestenborghs, R., Noorduin, H. et al. Protein binding of the analgesics alfentanil and sufentanil in maternal and neonatal plasma. Eur J Clin Pharmacol 30, 217–219 (1986). https://doi.org/10.1007/BF00614307

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  • DOI: https://doi.org/10.1007/BF00614307

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