| Autor: |
L. P. C. Delbressine, M. E. G. Moonen, G. Voortman, Peter L. Jacobs, J. E. Paanakker, G. N. Wagenaars, Cees J. Timmer, Frans M. Kaspersen, H.J.M. Van Hal |
| Rok vydání: |
1998 |
| Předmět: |
|
| Zdroj: |
Clinical Drug Investigation. 15:45-55 |
| ISSN: |
1173-2563 |
| DOI: |
10.2165/00044011-199815010-00006 |
| Popis: |
This paper investigated the pharmacokinetics and biotransformation of mirtazapine in healthy human volunteers. The results showed that the area under the plasma drug concentration-time curve (AUC) of mirtazapine in human plasma appeared to be three times higher than the AUC of demethylmirtazapine. As mirtazapine is marketed as a racemic mixture and both enantiomers possess pharmacological properties essential for the overall activity of the racemate, the pharmacokinetics of mirtazapine were examined and appeared to be enantioselective. The R(-)-enantiomer showed the longest elimination half-life from plasma. This was ascribed to the preferred formation of a quaternary ammonium glucuronide of the R(-)-enantiomer. This glucuronide may be deconjugated, leading to a further circulation of the parent compound, thus causing a prolongation in the elimination half-life. The S(+)-enantiomer was preferentially metabolised into an 8-hydroxy glucuronide. Other metabolic transformation pathways found for mirtazapine were demethylation and N-oxidation. Mirtazapine was extensively metabolised and almost completely excreted in the urine (over 80%) and faeces within a few days after oral administration. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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