| Autor: |
Koopman-Kimenai PM; Department of Clinical Pharmacy, Academic Hospital Nijmegen Sint Radboud, The Netherlands., Vree TB, Booij LH, Dirksen R |
| Jazyk: |
angličtina |
| Zdroj: |
Pharmacy world & science : PWS [Pharm World Sci] 1994 Dec 02; Vol. 16 (6), pp. 248-53. |
| DOI: |
10.1007/BF02178565 |
| Abstrakt: |
The pharmacokinetics of 30 mg nicomorphine after rectal administration with a suppository are described in 8 patients under combined general and epidural anaesthesia. No nicomorphine or 6-mononicotinoylmorphine could be detected in the serum. Morphine appeared almost instantaneously with a lag-time of 8 min and had a final elimination half-life of 1.48 +/- 0.48 h. Morphine was metabolized to morphine-3-glucuronide and morphine-6-glucuronide. These glucuronide conjugates appeared after a lag-time of 12 min and the half-life of these two glucuronide conjugates was similar: about 2.8 h (P > 0.8). The glucuronide conjugate of 6-mononicotinoylmorphine was not detected. In the urine only morphine and its glucuronides were found. The renal clearance value for morphine was 162 ml.min-1 and for the glucuronides 81 ml.min-1. This study shows that administration of a suppository with 30 mg nicomorphine gives an excellent absolute bioavailability of morphine and its metabolites of 88%. The lipid-soluble prodrug nicomorphine is quickly absorbed and immediately hydrolysed to morphine. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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