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Use of methylnaltrexone and related compounds

a technology of methylnaltrexone and related compounds, which is applied in the direction of heterocyclic compound active ingredients, biocide, drug compositions, etc., can solve the problems of limited efficacy of common treatments of bulking agents and laxatives, and associated with undesirable side effects

Inactive Publication Date: 2005-03-03
PROGENICS PHARMA NEVADA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The present invention is directed at methods for preventing and treating opioid-induced inhibition of gut motility and constipation.
An aspect of the invention is a composition for preventing or treating opioid-induced inhibition of gastrointestinal motility comprising administering enterically coated quaternary derivatives of noroxymorphone as disclosed in U.S. Pat. No. 4,176,186 to Goldberg et al. (herein incorporated by reference) to a patient. In certain embodiments the composition is in the form of pill, tablet, capsule or granule. The preferred quaternary derivatives of noroxymorphone is methylnaltrexone.

Problems solved by technology

However, their use is associated with a number of undesirable side effects.
Opioid-induced changes in gastrointestinal motility are almost universal when these drugs are used to treat pain, and at times may limit their use, leaving the patient in pain.
Common treatments of bulking agents and laxatives have limited efficacy and may be associated with side effects such as electrolyte imbalances.
However, high levels of MNTX in the plasma can lead to undesirable side effects such as orthostatic hypotension.

Method used

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  • Use of methylnaltrexone and related compounds
  • Use of methylnaltrexone and related compounds
  • Use of methylnaltrexone and related compounds

Examples

Experimental program
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Effect test

example 1

Effects Of Enterically Coated MNTX On Oral-Cecal Transit Time and Plasma Levels of MNTX

Oral methylnaltrexone, whether enterically coated or uncoated, was shown to reverse the inhibitory effects of opioid administration on gastrointestinal motility as measured by oral-cecal transit time. As compared to non-enterically coated MNTX, however, treatment with enterically coated MNTX enhanced the efficacy of the drug at a lower dose while producing lower plasma levels of MNTX.

Subjects were divided into five treatment groups A-E. With the exception of subjects in Group A, who were given a placebo in place of morphine, all were given an intravenous dose of morphine at 0.05 mg / kg. Prior to morphine administration, subjects were given either a placebo or MNTX in various doses and formulations (see Table 1). The subjects in Group A and B were given a placebo in place of MNTX. Group C received uncoated MNTX at 6.4 mg / kg, Group D received enterically coated MNTX at 6.4 mg / kg active drug, and ...

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Abstract

A composition for preventing or treating the opioid induced side effect, inhibition of gastrointestinal motility is disclosed. The composition comprises methylnaltrexone or another quaternary derivative of noroxymorphone administered to a patient prior to the administration of an opioid or after the onset of side effects induced by the administration of an opioid, wherein the methylnaltrexone or quaternary derivative is administered orally in an enterically coated form.

Description

FIELD OF THE INVENTION The present invention is directed at the treatment of certain side effects associated with the use of opioids as analgesics. In particular the present invention is directed at treating opioid-induced inhibition of gastrointestinal motility and constipation. BACKGROUND OF THE INVENTION Opioids are effective analgesics. However, their use is associated with a number of undesirable side effects. One such effect is constipation. Opioid-induced changes in gastrointestinal motility are almost universal when these drugs are used to treat pain, and at times may limit their use, leaving the patient in pain. Common treatments of bulking agents and laxatives have limited efficacy and may be associated with side effects such as electrolyte imbalances. One treatment for opioid side effects is the use of opioid antagonists which cross the blood-brain-barrier, or which are administered directly into the central nervous system. Opioid antagonists such as naltrexone and nal...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/485
CPCA61K31/485A61P1/00
Inventor FOSS, JOSEPH F.ROIZEN, MICHAEL F.MOSS, JONATHANYUAN, CHUN-SUDRELL, WILLIAM
Owner PROGENICS PHARMA NEVADA
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