Cystine Esters Reverse Opioid Ventilatory Depression
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Current medications for treating impaired ventilatory drive associated with conditions like COPD, OSA, and opioid-induced respiratory depression are either ineffective or come with significant side effects, and there is a lack of a safe and effective respiratory stimulant in pulmonary and critical care medicine.
Innovation Solution
The use of thiol-based compounds, specifically cystine esters and their adducts, which are administered to attenuate and treat opioid-induced ventilatory and respiratory depression by stimulating respiratory drive while maintaining or augmenting opioid-induced analgesia.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If methylxanthines are administered to treat apnea of prematurity, then ventilatory drive is improved, but effectiveness is lost in older patients
Solution Approach 1:
The patent changes the chemical parameters of respiratory stimulants by developing new compounds with different molecular structures (e.g., doxapram, ethyl doxapram, carbonyl derivatives) that have improved pharmacokinetic and pharmacodynamic properties, making them effective across broader age groups while maintaining safety profiles
Solution Approach 2:
The patent combines multiple therapeutic agents or uses composite chemical structures that integrate beneficial properties of different compounds, creating respiratory stimulants with enhanced efficacy and reduced age-related limitations
2Reliability
If almitrine is administered to improve ventilatory drive in COPD patients, then respiratory stimulation is achieved, but pulmonary arterial hypertension and peripheral neuropathy develop
Solution Approach 1:
The patent extracts and isolates the beneficial respiratory stimulant properties from almitrine while eliminating or reducing the harmful cardiovascular and neurological effects through structural modification and selective receptor targeting
Solution Approach 2:
The patent introduces new chemical compounds as intermediaries that mediate respiratory stimulation through alternative pathways, avoiding the toxic mechanisms that cause pulmonary arterial hypertension and peripheral neuropathy while maintaining ventilatory drive improvement
3Ease of operation
If narcotics are administered to control pain in critical care patients, then pain management is achieved, but respiratory depression occurs
Solution Approach 1:
The patent converts the harmful respiratory depressant effects of narcotics into beneficial outcomes by using the same or related compounds in controlled formulations that provide analgesia while incorporating respiratory stimulants or monitoring systems that prevent respiratory depression
Solution Approach 2:
The patent applies preliminary respiratory stimulation or protective measures before administering narcotics to prevent respiratory depression, or uses antagonists and monitoring systems that counteract harmful effects before they manifest
4Reliability
If no effective respiratory stimulant is available, then unmet medical need persists, but development of new compounds requires extensive testing and validation
Solution Approach 1:
The patent performs preliminary computational modeling, in silico screening, and preclinical studies to validate new respiratory stimulant compounds before full clinical development, reducing the complexity and time of the overall drug development process while ensuring efficacy and safety
Data Source
AI summary
A method of attenuating opioid induced ventilatory and/or respiratory depression and/or augmenting opioid induced analgesia in a subject in need thereof includes administering to the subject a therapeutically effective amount of a composition comprising a cystine ester or an adduct, a pharmaceutically acceptable salt, a tautomer, or a solvate thereof.