PHARMACOKINETICS OF INTRAVENOUSLY ADMINISTERED NICOMORPHINE AND ITS METABOLITES AND GLUCURONIDE CONJUGATES IN SURGICAL PATIENTS

被引：5

作者：

KOOPMANKIMENAI, PM

VREE, TB

BOOIJ, LHDJ

DIRKSEN, R

机构：

[1] ACAD HOSP NIJMEGEN ST RADBOUD,DEPT CLIN PHARM,6525 GA NIJMEGEN,NETHERLANDS

[2] ACAD HOSP NIJMEGEN ST RADBOUD,INST ANAESTHESIOL,NIJMEGEN,NETHERLANDS

来源：

DRUG INVESTIGATION | 1994年 / 7卷 / 02期

关键词：

D O I：

10.1007/BF03257401

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

After intravenous administration of 3,6-dinicotinoylmorphine (nicomorphine) 30, 20 and 1Omg to patients undergoing surgery, this agent is rapidly metabolised into the metabolites 6-mononicotinoylmorphine (6MNM) and morphine. The elimination half-lives are 1 minute for nicomorphine, 13 minutes for 6MNM and 120 minutes for morphine. Morphine is subsequently metabolised into morphine-3-glucuronide (M3G) and morphine-6-glucuronide (M6G). The half-life of these 2 glucuronide conjugates is similar, about 225 minutes. A glucuronide conjugate of 6MNM was not detected. The area under the serum concentration-time curve of nicomorphine and its metabolites is linearly related to the dose.

引用

收藏

页码：63 / 73

页数：11

相关论文

共 31 条

[1]

BERKOWITZ BA, 1975, CLIN PHARMACOL THER, V17, P629

[2] METABOLISM OF MORPHINE AND HEROIN IN MAN [J].

BOERNER, U ;

ABBOTT, S ;

ROE, RL .

DRUG METABOLISM REVIEWS, 1975, 4 (01) :39-73

[3] MORPHINE 6-GLUCURONIDE AND MORPHINE 3-GLUCURONIDE AS MOLECULAR CHAMELEONS WITH UNEXPECTED LIPOPHILICITY [J].

CARRUPT, PA ;

TESTA, B ;

BECHALANY, A ;

ELTAYAR, N ;

DESCAS, P ;

PERRISSOUD, D .

JOURNAL OF MEDICINAL CHEMISTRY, 1991, 34 (04) :1272-1275

[4] EFFECTS OF RENAL-INSUFFICIENCY ON THE PHARMACOKINETICS AND PHARMACODYNAMICS OF OPIOID ANALGESICS [J].

CHAN, GLC ;

MATZKE, GR .

DRUG INTELLIGENCE & CLINICAL PHARMACY, 1987, 21 (10) :773-783

[5]

DIRKSEN R, 1988, P VILAN R WORKSHOP G, P10

[6] PHARMACOKINETICS OF MORPHINE AND ITS SURROGATES .3. MORPHINE AND MORPHINE 3-MONOGLUCURONIDE PHARMACOKINETICS IN THE DOG AS A FUNCTION OF DOSE [J].

GARRETT, ER ;

JACKSON, AJ .

JOURNAL OF PHARMACEUTICAL SCIENCES, 1979, 68 (06) :753-771

[7] PHARMACOKINETICS OF MORPHINE AND ITS SURROGATES .1. COMPARISONS OF SENSITIVE ASSAYS OF MORPHINE IN BIOLOGICAL-FLUIDS AND APPLICATION TO MORPHINE PHARMACOKINETICS IN DOG [J].

GARRETT, ER ;

GURKAN, T .

JOURNAL OF PHARMACEUTICAL SCIENCES, 1978, 67 (11) :1512-1517

[8] DISPOSITION OF MORPHINE-6-GLUCURONIDE AND MORPHINE IN HEALTHY-VOLUNTEERS [J].

HANNA, MH ;

PEAT, SJ ;

KNIBB, AA ;

FUNG, C .

BRITISH JOURNAL OF ANAESTHESIA, 1991, 66 (01) :103-107

[9] MORPHINE PHARMACOKINETICS AND METABOLISM IN HUMANS - ENTEROHEPATIC CYCLING AND RELATIVE CONTRIBUTION OF METABOLITES TO ACTIVE OPIOID CONCENTRATIONS [J].

HASSELSTROM, J ;

SAWE, J .

CLINICAL PHARMACOKINETICS, 1993, 24 (04) :344-354

[10] ENTEROHEPATIC RECIRCULATION AND RENAL METABOLISM OF MORPHINE IN THE RAT [J].

HORTON, TL ;

POLLACK, GM .

JOURNAL OF PHARMACEUTICAL SCIENCES, 1991, 80 (12) :1147-1152

← 1 2 3 4 →