Method for treating drug or alcohol dependency

A dependence and drug technology, applied in the direction of drug combination, pharmaceutical formulation, organic active ingredients, etc., can solve problems that have not considered the molecular characteristics of neutral opioid antagonists

Pending Publication Date: 2021-10-29
イーサーセラピューティクスインコーポレイテッド
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] These results lead to the conclusion that 6BN, as the primary metabolite of naltrexone, does not substantially contribute to its primary effect on opioid receptors; however, molecules that are neutral opioid antagonists of this type have not been considered in this conclusion characteristic

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0070] Blockade of peripheral opioid receptors. Step 1.

[0071] This step applies to opioid use disorder. Oral administration of slowly increasing doses of 6β-naltrexol in amounts sufficient to gradually overcome the effects of peripheral opioids in addicted / dependent subjects caused mild withdrawal characterized by restoration of bowel motility without excessive cramps or diarrhea , without central withdrawal symptoms. The recommended initial dose is 2 mg naltrexol orally (assuming approximately 30% oral bioavailability; estimated dose range 0.5 to 10 mg) once or twice daily for 2 to 4 days, followed by 6 mg once or twice daily for 2 to 4 days 4 to 8 days (estimated dose range 2-20 mg twice daily). Step 1 is designed to suppress the peripheral effects of the opioid drug and at least partially reverse opioid dependence with minimal peripheral withdrawal symptoms.

Embodiment 2

[0073] Stabilization of peripheral opioid receptor signaling. Step 2.

[0074] Step 1 was followed by 6-beta-naltrexol administration, 10 mg, once or twice daily (estimated dose range 4-50 mg twice daily) for 1-4 weeks. This dose can be maintained to prevent peripheral side effects and to reverse hyperalgesia and the dependent opioid state of peripheral opioid receptors. Because opioid-induced hyperalgesia is expected to be at least partially reversed during Step 2, the dose of the opioid agonist should be reduced and maintained at the lower dose if withdrawal symptoms do not occur. The goal is to reduce the burden of opioid exposure during Step 2.

[0075] Patients requiring continued pain therapy after completion of Step 2 may be administered a maintenance dose consisting of a 6-beta-naltrexol / opioid analgesic combination formulation containing enough to block peripheral effects without interfering with opioid pain perception Doses of 6-beta-naltrexol that are missing, wit...

Embodiment 3

[0077] Blockade of CNS opioid receptors and complete withdrawal. Step 3.

[0078] Blockade of peripheral opioid receptors followed by administration of increasing doses of 6-β-naltrexol to subjects gradually suppressed the CNS effects of opioid analgesics. The recommended dose is 20 mg (range 10 to 80 mg) once or twice daily for 4 to 8 days, followed by 40 mg (range 20 to 120 mg) once or twice daily for 1 to 4 weeks, and further if necessary Increase to 100 mg (40 to 300 mg range) once or twice daily for maintenance. A single dose of 20 mg intravenous naltrexol in opioid naïve subjects ( subject) could not block the analgesia induced by 10 mg intravenous morphine; the IC50 of blocking morphine that induced slowing of intestinal motility was about 3 mg intravenous naltrexol; the peripheral / central potency ratio of naltrexol in mice was About 10, but can be higher in humans. In addition to increasing the dose of 6-beta-naltrexol, subjects will achieve a gradual and complete ...

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PUM

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Abstract

Provided herein is a method for weaning a subject suffering from a drug addiction or addictive behaviors involving opioid signaling by sequentially blocking peripheral and CNS opioid receptors and modulating opioid dependence.

Description

[0001] field of invention [0002] The present invention is directed to a drug addiction withdrawal program, such as an opioid withdrawal program and an alcohol withdrawal program, or withdrawal of addictive behaviors involving opioid signaling (Opioid Signaling). [0003] All publications, patents, patent applications, and other references cited in this application are hereby incorporated by reference in their entirety for all purposes to the same extent as if each were specifically and individually indicated to be incorporated by reference. Each individual publication, patent, patent application, or other reference is hereby incorporated by reference in its entirety for all purposes. Citation of a reference herein shall not be construed as an admission that said reference is prior art to the present invention. [0004] Cross References to Related Applications [0005] This application claims priority to U.S. Provisional Application Serial No. 62 / 788,167, filed January 4, 20...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/485A61P25/36C07D403/02
CPCA61P25/36A61K31/485C07D491/107
Inventor 沃尔夫冈·萨迪
Owner イーサーセラピューティクスインコーポレイテッド
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