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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
1
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pubmed:dateCreated |
1997-1-29
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pubmed:abstractText |
Morphine, morphine-6-glucuronide and normorphine were administered to male Sprague-Dawley-rats. Analgesic effect was estimated with the hot plate and spinal nociceptive reflex depression. After intraperitoneal administration the molar potency ratio of morphine-6-glucuronide/morphine was 1.7 estimated by the paw lick latency on the hot plate utilizing a linked pharmacokinetic-pharmacodynamic model. The potency ratio of morphine-6-glucuronide/morphine utilizing the spinal nociceptive reflex depression after intravenous administration was estimated to be within the earlier reported range of 1-4 after systemic administration of the drugs. In contrast to what is seen in man virtually no morphine-6-glucuronide was formed in Sprague-Dawley rats after administration of morphine, much lower levels of morphine-3-glucuronide were also seen. The molar AUC ratio of morphine-3-glucuronide/morphine was 1.8 +/- 0.5 and the corresponding ratio for normorphine/morphine was 0.2 +/- 0.06. After intraperitoneal administration of morphine, morphine-6-glucuronide and normorphine mean systemic clearance values of 413 +/- 95, 50 +/- 11 and 187 +/- 54 ml.min.kg-1 respectively were observed. Varea was 9.0 +/- 2.1, 0.8 +/- 0.2 and 4.9 +/- 1.4 L.kg-1 respectively. The slow absorption of morphine-6-glucuronide was illustrated by the mean Tmax-value of the 16 min. as compared with 9 min. for morphine and 10 min. for normorphine. It was possible to fit pharmacokinetic and pharmacodynamic data of behavioural analgesic effect of both morphine and morphine-6-glucuronide to a parametric model linking the sigmoid Emax model to standard pharmacokinetic equations.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Analgesics, Opioid,
http://linkedlifedata.com/resource/pubmed/chemical/Morphine,
http://linkedlifedata.com/resource/pubmed/chemical/Morphine Derivatives,
http://linkedlifedata.com/resource/pubmed/chemical/morphine-6-glucuronide,
http://linkedlifedata.com/resource/pubmed/chemical/normorphine
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pubmed:status |
MEDLINE
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pubmed:month |
Jul
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pubmed:issn |
0901-9928
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
79
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
40-6
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:8841095-Analgesics, Opioid,
pubmed-meshheading:8841095-Animals,
pubmed-meshheading:8841095-Behavior, Animal,
pubmed-meshheading:8841095-Decerebrate State,
pubmed-meshheading:8841095-Dose-Response Relationship, Drug,
pubmed-meshheading:8841095-Electrophysiology,
pubmed-meshheading:8841095-Half-Life,
pubmed-meshheading:8841095-Injections, Intraperitoneal,
pubmed-meshheading:8841095-Male,
pubmed-meshheading:8841095-Morphine,
pubmed-meshheading:8841095-Morphine Derivatives,
pubmed-meshheading:8841095-Pain Threshold,
pubmed-meshheading:8841095-Rats,
pubmed-meshheading:8841095-Rats, Sprague-Dawley,
pubmed-meshheading:8841095-Software
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pubmed:year |
1996
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pubmed:articleTitle |
Disposition and analgesic effects of systemic morphine, morphine-6-glucuronide and normorphine in rat.
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pubmed:affiliation |
Department of Neurosciences, Huddinge University Hospital, Karolinska Institute, Sweden.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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