Buprenorphine for Opioid-Induced Bowel Dysfunction
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Solution Overview
Problem
Current treatments for opioid-induced adverse pharmacodynamic responses, such as bowel dysfunction and other side effects, are inadequate as they often come with significant risks and complications, including severe side effects like dehydration and extrapyramidal reactions.
Innovation Solution
Administering buprenorphine in effective amounts to patients to prevent or treat opioid-induced adverse pharmacodynamic responses without substantially affecting the analgesic effectiveness of opioids, even in chronic or high-dose opioid therapy scenarios.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If laxatives are administered to treat opioid-induced bowel dysfunction, then bowel motility is improved, but severe side effects such as dehydration and bowel obstruction occur
Solution Approach 1:
The patent uses opioid antagonists as intermediaries that selectively block opioid receptors in the gastrointestinal tract. These antagonists mediate between the harmful opioid-induced constipation and the desired bowel motility, preventing the binding of exogenous opioids to mu-receptors in the GI tract while allowing endogenous opioids to maintain analgesia. This intermediary approach resolves the contradiction by achieving bowel motility improvement without the severe side effects of traditional laxatives.
Solution Approach 2:
The patent changes the pharmacological parameter by introducing substances with opposite pharmacodynamic properties (opioid antagonists) to counterbalance the opioid-induced effects. By administering agents that bind to opioid receptors with high affinity but do not activate them, the patent alters the receptor occupancy parameters in the GI tract, thereby reversing constipation without causing laxative-induced dehydration or obstruction.
2Ease of operation
If opioid antagonists are administered to suppress receptors causing bowel dysfunction, then bowel motility is improved, but the desired analgesic effect of the opioid is reversed
Solution Approach 1:
The patent applies local quality by using peripherally restricted opioid antagonists that selectively act on opioid receptors in the gastrointestinal tract while having minimal to no effect on central nervous system opioid receptors. This spatial differentiation allows the patent to improve bowel motility locally in the GI tract without reversing the central analgesic effects of opioids, thereby resolving the contradiction between bowel function improvement and analgesic maintenance.
Solution Approach 2:
The patent employs peripherally restricted opioid antagonists as intermediaries that specifically target gastrointestinal opioid receptors. These intermediaries selectively block opioid signaling in the periphery (GI tract) while leaving central opioid signaling intact, thus achieving bowel motility improvement without compromising analgesia. This selective intermediary action resolves the contradiction by differentiating between peripheral and central opioid receptor effects.
3Ease of operation
If prokinetic agents are administered to improve gastrointestinal motility, then bowel function is improved, but extrapyramidal effects such as acute dystonic reactions occur
Solution Approach 1:
The patent uses peripherally restricted opioid antagonists as intermediaries to achieve bowel motility improvement through a different mechanism than prokinetic agents. Instead of directly stimulating gastrointestinal motility (which causes extrapyramidal effects), the antagonists block opioid-induced receptor activation in the GI tract, thereby improving motility through receptor blockade. This intermediary approach resolves the contradiction by achieving the same therapeutic goal without the harmful extrapyramidal side effects of prokinetic agents.
Data Source
AI summary
Disclosed in certain embodiments is a method of treating or preventing an opioid induced adverse pharmacodynamic response comprising administering to a patient in need thereof an effective amount of buprenorphine.