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Lack of Analgesic Activity of Morphine-6-glucuronide after Short-term Intravenous Administration in Healthy Volunteers
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Zeitschriftentitel: | Anesthesiology |
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Personen und Körperschaften: | , , , , |
In: | Anesthesiology, 87, 1997, 6, S. 1348-1358 |
Format: | E-Article |
Sprache: | Englisch |
veröffentlicht: |
Ovid Technologies (Wolters Kluwer Health)
|
Schlagwörter: |
author_facet |
Lotsch, Jorn Kobal, Gerd Stockmann, Anne Brune, Kay Geisslinger, Gerd Lotsch, Jorn Kobal, Gerd Stockmann, Anne Brune, Kay Geisslinger, Gerd |
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author |
Lotsch, Jorn Kobal, Gerd Stockmann, Anne Brune, Kay Geisslinger, Gerd |
spellingShingle |
Lotsch, Jorn Kobal, Gerd Stockmann, Anne Brune, Kay Geisslinger, Gerd Anesthesiology Lack of Analgesic Activity of Morphine-6-glucuronide after Short-term Intravenous Administration in Healthy Volunteers Anesthesiology and Pain Medicine |
author_sort |
lotsch, jorn |
spelling |
Lotsch, Jorn Kobal, Gerd Stockmann, Anne Brune, Kay Geisslinger, Gerd 0003-3022 Ovid Technologies (Wolters Kluwer Health) Anesthesiology and Pain Medicine http://dx.doi.org/10.1097/00000542-199712000-00014 <jats:sec> <jats:title>Background</jats:title> <jats:p>The analgesic activity of morphine-6-glucuronide (M-6-G) is well recognized for its contribution to the effects of morphine and its possible use as an opioid analgesic with a wider therapeutic range than morphine. The present study attempted to quantify the relative contribution of M-6-G to analgesia observed after systemic administration of morphine.</jats:p> </jats:sec> <jats:sec> <jats:title>Methods</jats:title> <jats:p>In a placebo-controlled, sixfold crossover study in 20 healthy men, the effects of M-6-G were assessed at steady-state plasma concentrations of M-6-G identical to and two and three times higher than those measured after administration of morphine. Morphine and M-6-G were administered as an intravenous bolus followed by infusion over 4 h. Dosage A was M-6-G-bolus of 0.015 mg/kg plus infusion of 0.0072 mg x kg(-1) x h(-1). Dosage B was M-6-G-bolus of 0.029 mg/kg plus infusion of 0.014 mg x kg(-1) x h(-1). Dosage C was M-6-G-bolus of 0.044 mg/kg plus infusion of 0.022 mg x kg(-1) x h(-1). Dosage D was a morphine bolus of 0.14 mg/kg plus infusion of 0.05 mg x kg(-1) x h(-1) for 4 h. Dosage E was M-6-G combined with morphine (doses A + D). Dosage F was a placebo. The analgesic effects of M-6-G and morphine were measured before administration of the bolus and after 3.5 h using an experimental pain model based on pain-related cortical potentials and pain ratings after specific stimulation of the nasal nociceptor with short pulses of gaseous carbon dioxide.</jats:p> </jats:sec> <jats:sec> <jats:title>Results</jats:title> <jats:p>Morphine significantly reduced subjective and objective pain correlates compared with placebo. In contrast, M-6-G produced no statistically significant effects. The addition of M-6-G to morphine did not increase the effects of morphine. Morphine produced significantly more side effects than M-6-G.</jats:p> </jats:sec> <jats:sec> <jats:title>Conclusion</jats:title> <jats:p>After short-term intravenous administration at doses that produce plasma concentrations of M-6-G similar to those seen after administration of morphine, M-6-G had no analgesic effects in the present placebo-controlled study in healthy volunteers.</jats:p> </jats:sec> Lack of Analgesic Activity of Morphine-6-glucuronide after Short-term Intravenous Administration in Healthy Volunteers Anesthesiology |
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10.1097/00000542-199712000-00014 |
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Medizin |
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Ovid Technologies (Wolters Kluwer Health), 1997 |
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1997 |
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Ovid Technologies (Wolters Kluwer Health) |
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ai |
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Anesthesiology |
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49 |
title |
Lack of Analgesic Activity of Morphine-6-glucuronide after Short-term Intravenous Administration in Healthy Volunteers |
title_unstemmed |
Lack of Analgesic Activity of Morphine-6-glucuronide after Short-term Intravenous Administration in Healthy Volunteers |
title_full |
Lack of Analgesic Activity of Morphine-6-glucuronide after Short-term Intravenous Administration in Healthy Volunteers |
title_fullStr |
Lack of Analgesic Activity of Morphine-6-glucuronide after Short-term Intravenous Administration in Healthy Volunteers |
title_full_unstemmed |
Lack of Analgesic Activity of Morphine-6-glucuronide after Short-term Intravenous Administration in Healthy Volunteers |
title_short |
Lack of Analgesic Activity of Morphine-6-glucuronide after Short-term Intravenous Administration in Healthy Volunteers |
title_sort |
lack of analgesic activity of morphine-6-glucuronide after short-term intravenous administration in healthy volunteers |
topic |
Anesthesiology and Pain Medicine |
url |
http://dx.doi.org/10.1097/00000542-199712000-00014 |
publishDate |
1997 |
physical |
1348-1358 |
description |
<jats:sec>
<jats:title>Background</jats:title>
<jats:p>The analgesic activity of morphine-6-glucuronide (M-6-G) is well recognized for its contribution to the effects of morphine and its possible use as an opioid analgesic with a wider therapeutic range than morphine. The present study attempted to quantify the relative contribution of M-6-G to analgesia observed after systemic administration of morphine.</jats:p>
</jats:sec>
<jats:sec>
<jats:title>Methods</jats:title>
<jats:p>In a placebo-controlled, sixfold crossover study in 20 healthy men, the effects of M-6-G were assessed at steady-state plasma concentrations of M-6-G identical to and two and three times higher than those measured after administration of morphine. Morphine and M-6-G were administered as an intravenous bolus followed by infusion over 4 h. Dosage A was M-6-G-bolus of 0.015 mg/kg plus infusion of 0.0072 mg x kg(-1) x h(-1). Dosage B was M-6-G-bolus of 0.029 mg/kg plus infusion of 0.014 mg x kg(-1) x h(-1). Dosage C was M-6-G-bolus of 0.044 mg/kg plus infusion of 0.022 mg x kg(-1) x h(-1). Dosage D was a morphine bolus of 0.14 mg/kg plus infusion of 0.05 mg x kg(-1) x h(-1) for 4 h. Dosage E was M-6-G combined with morphine (doses A + D). Dosage F was a placebo. The analgesic effects of M-6-G and morphine were measured before administration of the bolus and after 3.5 h using an experimental pain model based on pain-related cortical potentials and pain ratings after specific stimulation of the nasal nociceptor with short pulses of gaseous carbon dioxide.</jats:p>
</jats:sec>
<jats:sec>
<jats:title>Results</jats:title>
<jats:p>Morphine significantly reduced subjective and objective pain correlates compared with placebo. In contrast, M-6-G produced no statistically significant effects. The addition of M-6-G to morphine did not increase the effects of morphine. Morphine produced significantly more side effects than M-6-G.</jats:p>
</jats:sec>
<jats:sec>
<jats:title>Conclusion</jats:title>
<jats:p>After short-term intravenous administration at doses that produce plasma concentrations of M-6-G similar to those seen after administration of morphine, M-6-G had no analgesic effects in the present placebo-controlled study in healthy volunteers.</jats:p>
</jats:sec> |
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author | Lotsch, Jorn, Kobal, Gerd, Stockmann, Anne, Brune, Kay, Geisslinger, Gerd |
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description | <jats:sec> <jats:title>Background</jats:title> <jats:p>The analgesic activity of morphine-6-glucuronide (M-6-G) is well recognized for its contribution to the effects of morphine and its possible use as an opioid analgesic with a wider therapeutic range than morphine. The present study attempted to quantify the relative contribution of M-6-G to analgesia observed after systemic administration of morphine.</jats:p> </jats:sec> <jats:sec> <jats:title>Methods</jats:title> <jats:p>In a placebo-controlled, sixfold crossover study in 20 healthy men, the effects of M-6-G were assessed at steady-state plasma concentrations of M-6-G identical to and two and three times higher than those measured after administration of morphine. Morphine and M-6-G were administered as an intravenous bolus followed by infusion over 4 h. Dosage A was M-6-G-bolus of 0.015 mg/kg plus infusion of 0.0072 mg x kg(-1) x h(-1). Dosage B was M-6-G-bolus of 0.029 mg/kg plus infusion of 0.014 mg x kg(-1) x h(-1). Dosage C was M-6-G-bolus of 0.044 mg/kg plus infusion of 0.022 mg x kg(-1) x h(-1). Dosage D was a morphine bolus of 0.14 mg/kg plus infusion of 0.05 mg x kg(-1) x h(-1) for 4 h. Dosage E was M-6-G combined with morphine (doses A + D). Dosage F was a placebo. The analgesic effects of M-6-G and morphine were measured before administration of the bolus and after 3.5 h using an experimental pain model based on pain-related cortical potentials and pain ratings after specific stimulation of the nasal nociceptor with short pulses of gaseous carbon dioxide.</jats:p> </jats:sec> <jats:sec> <jats:title>Results</jats:title> <jats:p>Morphine significantly reduced subjective and objective pain correlates compared with placebo. In contrast, M-6-G produced no statistically significant effects. The addition of M-6-G to morphine did not increase the effects of morphine. Morphine produced significantly more side effects than M-6-G.</jats:p> </jats:sec> <jats:sec> <jats:title>Conclusion</jats:title> <jats:p>After short-term intravenous administration at doses that produce plasma concentrations of M-6-G similar to those seen after administration of morphine, M-6-G had no analgesic effects in the present placebo-controlled study in healthy volunteers.</jats:p> </jats:sec> |
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spelling | Lotsch, Jorn Kobal, Gerd Stockmann, Anne Brune, Kay Geisslinger, Gerd 0003-3022 Ovid Technologies (Wolters Kluwer Health) Anesthesiology and Pain Medicine http://dx.doi.org/10.1097/00000542-199712000-00014 <jats:sec> <jats:title>Background</jats:title> <jats:p>The analgesic activity of morphine-6-glucuronide (M-6-G) is well recognized for its contribution to the effects of morphine and its possible use as an opioid analgesic with a wider therapeutic range than morphine. The present study attempted to quantify the relative contribution of M-6-G to analgesia observed after systemic administration of morphine.</jats:p> </jats:sec> <jats:sec> <jats:title>Methods</jats:title> <jats:p>In a placebo-controlled, sixfold crossover study in 20 healthy men, the effects of M-6-G were assessed at steady-state plasma concentrations of M-6-G identical to and two and three times higher than those measured after administration of morphine. Morphine and M-6-G were administered as an intravenous bolus followed by infusion over 4 h. Dosage A was M-6-G-bolus of 0.015 mg/kg plus infusion of 0.0072 mg x kg(-1) x h(-1). Dosage B was M-6-G-bolus of 0.029 mg/kg plus infusion of 0.014 mg x kg(-1) x h(-1). Dosage C was M-6-G-bolus of 0.044 mg/kg plus infusion of 0.022 mg x kg(-1) x h(-1). Dosage D was a morphine bolus of 0.14 mg/kg plus infusion of 0.05 mg x kg(-1) x h(-1) for 4 h. Dosage E was M-6-G combined with morphine (doses A + D). Dosage F was a placebo. The analgesic effects of M-6-G and morphine were measured before administration of the bolus and after 3.5 h using an experimental pain model based on pain-related cortical potentials and pain ratings after specific stimulation of the nasal nociceptor with short pulses of gaseous carbon dioxide.</jats:p> </jats:sec> <jats:sec> <jats:title>Results</jats:title> <jats:p>Morphine significantly reduced subjective and objective pain correlates compared with placebo. In contrast, M-6-G produced no statistically significant effects. The addition of M-6-G to morphine did not increase the effects of morphine. Morphine produced significantly more side effects than M-6-G.</jats:p> </jats:sec> <jats:sec> <jats:title>Conclusion</jats:title> <jats:p>After short-term intravenous administration at doses that produce plasma concentrations of M-6-G similar to those seen after administration of morphine, M-6-G had no analgesic effects in the present placebo-controlled study in healthy volunteers.</jats:p> </jats:sec> Lack of Analgesic Activity of Morphine-6-glucuronide after Short-term Intravenous Administration in Healthy Volunteers Anesthesiology |
spellingShingle | Lotsch, Jorn, Kobal, Gerd, Stockmann, Anne, Brune, Kay, Geisslinger, Gerd, Anesthesiology, Lack of Analgesic Activity of Morphine-6-glucuronide after Short-term Intravenous Administration in Healthy Volunteers, Anesthesiology and Pain Medicine |
title | Lack of Analgesic Activity of Morphine-6-glucuronide after Short-term Intravenous Administration in Healthy Volunteers |
title_full | Lack of Analgesic Activity of Morphine-6-glucuronide after Short-term Intravenous Administration in Healthy Volunteers |
title_fullStr | Lack of Analgesic Activity of Morphine-6-glucuronide after Short-term Intravenous Administration in Healthy Volunteers |
title_full_unstemmed | Lack of Analgesic Activity of Morphine-6-glucuronide after Short-term Intravenous Administration in Healthy Volunteers |
title_short | Lack of Analgesic Activity of Morphine-6-glucuronide after Short-term Intravenous Administration in Healthy Volunteers |
title_sort | lack of analgesic activity of morphine-6-glucuronide after short-term intravenous administration in healthy volunteers |
title_unstemmed | Lack of Analgesic Activity of Morphine-6-glucuronide after Short-term Intravenous Administration in Healthy Volunteers |
topic | Anesthesiology and Pain Medicine |
url | http://dx.doi.org/10.1097/00000542-199712000-00014 |