Pharmacokinetics and biotransformation of the new benzodiazepine, lormetazepam, in man. III. Repeated administration and transfer to neonates via breast milk.

Abstract:

: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 24 h 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 12 h and 11 ng/ml 24 h 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/mg, corresponding to 0.35% of the maternal dose, which is regarded as tolerable.

journal_name

Eur J Clin Pharmacol

authors

Hümpel M,Stoppelli I,Milia S,Rainer E

doi

10.1007/BF00542330

subject

Has Abstract

pub_date

1982-01-01 00:00:00

pages

421-5

issue

5

eissn

0031-6970

issn

1432-1041

journal_volume

21

pub_type

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