European Journal of Clinical Pharmacology

, Volume 21, Issue 5, pp 421–425

Pharmacokinetics and biotransformation of the new benzodiazepine, lormetazepam, in man

III. Repeated administration and transfer to neonates via breast milk


  • M. Hümpel
    • Schering AG
  • I. Stoppelli
    • Department of Obstetrics and GynaecologyUniversity of Sassari
  • S. Milia
    • Department of Obstetrics and GynaecologyUniversity of Sassari
  • E. Rainer
    • Schering SPA

DOI: 10.1007/BF00542330

Cite this article as:
Hümpel, M., Stoppelli, I., Milia, S. et al. Eur J Clin Pharmacol (1982) 21: 421. doi:10.1007/BF00542330


The concentrations of lormetazepam and its glucuronide in plasma and milk were determined during administration of 10 daily doses of lormetazepam 2 mg (2 tablets of NOCTAMID® - 1) to five mothers delivered by Caesarian section. Their babies were breast-fed throughout the study, and the plasma levels of lormetazepam and its glucuronide were determined three times in the babies. At 12 and 24h after administration, the plasma level of lormetazepam was about 3.5 ng/ml and 1.8 ng/ml in mothers, and below 0.09 ng/ml in the children. In milk the lormetazepam concentration was below 0.2 ng/ml. The plasma level of glucuronide varied between 24 ng/ml at 12h and 11 ng/ml 24h after administration. Almost no accumulation of unchanged lormetazepam was observed (factor: 1.3). The ratio of the levels of lormetazepam in milk and plasma was estimated to be below 0.06, and for the glucuronide the ratio was 0.04. The quantity of free and conjugated active ingredient transferred to the children via breast milk was calculated to be at most 100 ng/kg, corresponding to 0.35% of the maternal dose, which is regarded as tolerable.

Key words

benzodiazepinelormetazepamlormetazepam glucuronidetransfer to milkpharmacokinetics
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© Springer-Verlag 1982