Abstract
The new tetracyclic antidepressant levoprotiline, ~[(met~ylamino)methyl]-9,10ethanoantracene-9( NH)-ethanol hydrochloride, is the R( -)-isomer of the racemate oxaprotiline. In contrast to the racemate and to the S(+)-isomer, levoprotiline is completely devoid of norepinephrine uptake inhibiting properties [l, 21. However, in clinical studies levoprotiline displayed antidepressant effects comparable to those of the racemic compound [3]. After oral administration to man the drug is almost completely absorbed and extensively metabolized. Direct 0-glucuronidation is the major metabolic pathway [4]. Several sensitive methods for the analysis of unchanged levoprotiline in blood or in plasma have been described recently [S-7]. Based upon the detection of derivatives, the reported procedures are rather time-consuming and therefore not altogether suitable for routine analysis. The specified sensitivity of the only direct HPLC method, using three-fold liquid-liquid extraction of plasma samples followed by UV detection [8] could not be reproduced in the authors’ laboratory.
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