NMDA and Opioid Receptor Modulator Combination for Abuse Reduction
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
NMDA receptor modulators, used for treating mood disorders, have high abuse potential and are often misused as recreational drugs, necessitating a need for compositions and methods that minimize or eliminate abuse liability while maintaining pharmacological effectiveness.
Innovation Solution
A pharmaceutical composition comprising a N-methyl-D-aspartate receptor modulator and a μ-opioid receptor modulator, where the μ-opioid receptor modulator occupies at least 10% of μ-opioid receptors in vivo, as measured by positron emission tomography, to reduce abuse liability while administering the NMDA receptor modulator for treating various diseases or disorders.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If NMDA receptor modulators are administered to treat mood disorders, then therapeutic effectiveness is improved, but abuse potential increases
Solution Approach 1:
The patent introduces a μ-opioid receptor modulator as an intermediary substance that blocks the abuse-related effects of NMDA receptor modulators. This intermediary agent allows the therapeutic benefits of NMDA modulation to persist while preventing the harmful euphoric effects that lead to abuse, effectively mediating between therapeutic effectiveness and abuse potential
Solution Approach 2:
The patent converts the harmful abuse potential of NMDA receptor modulators into a beneficial therapeutic strategy by utilizing the μ-opioid receptor modulator's ability to block abuse effects. The previously problematic opioid system is repurposed as a protective mechanism that eliminates abuse liability while preserving therapeutic efficacy
2Object-affected harmful factors
If μ-opioid receptor modulator is added to block abuse effects, then abuse liability is reduced, but composition complexity increases
Solution Approach 1:
The patent merges two pharmacological agents with different mechanisms of action into a single co-formulated composition. The NMDA receptor modulator and μ-opioid receptor modulator are combined in specific ratios and administered together, creating an integrated therapeutic system that achieves both therapeutic effectiveness and abuse prevention in one formulation
3Object-affected harmful factors
If μ-opioid receptor modulator occupies at least 10% of μ-opioid receptors, then abuse potential is minimized, but dosage precision requirements increase
Solution Approach 1:
The patent establishes specific occupancy thresholds (at least 10% of μ-opioid receptors) as a critical parameter for preventing abuse. By defining this quantitative benchmark, the patent transforms the complex pharmacological interaction into a measurable and controllable parameter that can be monitored and maintained through standardized dosing regimens
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
The combination of NMDA and μ-opioid receptor modulators effectively treats diseases like major depressive disorder while minimizing the abuse potential of NMDA receptor modulators, providing a therapeutic benefit with reduced risk of misuse.
Implementation Method 1
the μ-opioid receptor modulator is present in an amount that, when administered to a subject, occupies at least 10% of the subject's μ-opioid receptors in vivo
Implementation Method 2
occupies at least 10% of the subject's μ-opioid receptors in vivo as measured by positron emission tomography with a [11C]-carfentanil ligand
Data Source
AI summary
The present application provides pharmaceutical compositions and methods for treating diseases or disorders. The pharmaceutical composition comprises N-methyl-D-aspartate receptor modulator and μ-opioid receptor modulator. The present application also discloses formulations, dosing and administration routes for the pharmaceutical composition. Diseases can be treated by the pharmaceutical composition are also described.