Multidrug Infusion Formulation for Pain Control
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Solution Overview
Problem
Achieving effective, durable, and safe pain relief, especially in aged patients and those with end-stage malignancies, is challenging due to poorly controlled pain with unacceptable side effects from existing multimodal systemic approaches.
Innovation Solution
A formulation comprising an opioid, a Na channel blocker, an alpha2-receptor agonist, an opioid mu or delta receptor competitive antagonist, and an intravenous anesthetic/neurologic acting agent, administered via various routes including intrathecal, epidural, and sub-cutaneous methods, with a kit option for continuous infusion using a catheter and implanted pump.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If multimodal systemic approaches with multiple drugs are used to control pain, then pain relief effectiveness is improved, but systemic side effects increase and become unacceptable
Solution Approach 1:
The patent divides the pain control function into multiple independent drug components (opioid, Na channel blocker, alpha2-receptor agonist, opioid antagonist, intravenous anesthetic) that work through different mechanisms. Each component targets specific pain pathways independently, allowing effective multimodal pain control while using lower doses of each individual drug to minimize systemic side effects
Solution Approach 2:
The formulation enables localized action at the site of administration (intrathecal, epidural, or peripheral nerve) with each drug component acting on specific local receptors and channels. This localized delivery concentrates the therapeutic effect at the pain source while reducing systemic exposure and associated side effects
2Reliability
If higher doses of opioids are used to achieve better pain control, then pain relief is improved, but side effects such as respiratory depression and cognitive impairment increase
Solution Approach 1:
The patent combines multiple analgesic mechanisms into a single formulation: opioid for central pain control, Na channel blocker for neuropathic pain, alpha2-receptor agonist for synergistic analgesia, and opioid antagonist to modulate opioid effects. This combination allows effective pain control at lower opioid doses, reducing opioid-specific side effects while maintaining or improving overall analgesia
Solution Approach 2:
The formulation includes an opioid mu or delta receptor competitive antagonist that acts as a modulator to fine-tune opioid receptor activity. This intermediary component helps achieve effective pain control with reduced opioid doses by optimizing receptor engagement and reducing unwanted opioid side effects such as respiratory depression and cognitive impairment
3Adaptability or versatility
If multiple separate drug administrations are used to achieve comprehensive pain control, then therapeutic coverage is improved, but treatment complexity increases
Solution Approach 1:
The patent merges five different drug components with distinct mechanisms of action into a single integrated formulation that can be administered through one route (intrathecal, epidural, or peripheral nerve injection). This unified approach provides comprehensive multimodal pain control while simplifying the treatment protocol compared to administering multiple separate drugs through different routes and schedules
Data Source
AI summary
The present invention relates to a formulation comprising an opioid, a Na channel blocker, an alpha2-receptor agonist, an opioid mu or delta receptor competitive antagonist and an intravenous anesthetic and/or a neurologic acting agent for use in pain control and/or cognitive function improvement.