Pharmaceutical Composition for Alcohol Dependency

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Solution Overview

Problem

Current pharmacological treatments for alcohol dependence primarily focus on managing physical withdrawal symptoms rather than addressing the robust state of psychic dependence, leading to high relapse rates and limited efficacy due to significant side effects.

Innovation Solution

A pharmaceutical composition combining a compound with antagonistic action on 5-HT2 serotoninergic receptors, such as cyproheptadine, with a compound having antagonistic action on alpha1-noradrenergic receptors, like prazosin, alfuzosin, terazosin, or tamsulosin, to treat alcohol dependence, reducing the risk of major side effects while maintaining therapeutic efficacy.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If naltrexone is used to treat alcohol dependence, then the desire to drink and relapse rate are reduced, but gastrointestinal side effects occur

Engineering Contradiction:
Improvetreatment efficacyVSAvoidgastrointestinal side effects
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent divides the treatment approach into two separate components: an opiate antagonist (for craving reduction) and a compound with antagonistic action on 5-HT2 serotoninergic receptors and/or alpha1-noradrenergic receptors (for side effect mitigation). This segmentation allows each component to address specific aspects of alcohol dependence treatment independently, reducing the burden of side effects while maintaining efficacy.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The invention combines two different pharmacological agents with distinct mechanisms of action into a single therapeutic regimen. The opiate antagonist targets the dopaminergic system to reduce craving, while the second compound acts on serotoninergic and/or noradrenergic systems to modulate mood and reduce side effects, creating a composite treatment that addresses multiple pathways involved in alcohol dependence.

Inventive Principle:
Principle #40Composite materials

2Object-affected harmful factors

If substitution products are used to limit physical withdrawal symptoms, then physical dependence symptoms are reduced, but psychic dependence remains unaddressed

Engineering Contradiction:
Improvephysical withdrawal symptomsVSAvoidtreatment of psychic dependence
Core Design Contradiction:
Object-affected harmful factorsVSReliability

Solution Approach 1:

The patent employs a multi-functional treatment approach where the combination of agents addresses both physical and psychic dimensions of alcohol dependence. The opiate antagonist primarily targets psychic dependence through dopaminergic modulation, while the second compound provides additional benefits for both physical symptom management and psychic dependence through its action on serotoninergic and noradrenergic systems, making the treatment universally applicable to multiple aspects of the disorder.

Inventive Principle:
Principle #6Universality (Multi-functionality)

3Object-affected harmful factors

If acamprosate is used to modulate glutamatergic transmission, then withdrawal symptoms are treated, but efficacy against alcohol craving is uncertain

Engineering Contradiction:
Improvewithdrawal symptomsVSAvoidefficacy against craving
Core Design Contradiction:
Object-affected harmful factorsVSReliability

Solution Approach 1:

The patent changes the pharmacological parameters of the treatment by selecting agents with specific receptor profiles. Instead of relying solely on glutamatergic modulation, the invention uses an opiate antagonist combined with a compound targeting 5-HT2 serotoninergic and/or alpha1-noradrenergic receptors, thereby altering the mechanism of action to more directly address both craving and withdrawal symptoms with greater reliability.

Inventive Principle:
Principle #35Parameter changes

Data Source

PatentUS9238014B2Pharmaceutical composition for treating alcohol dependency
Publication Date: 2016.01.19 KINNOV THERAPEUTICS
  • US9238014B2 patent drawing
  • US9238014B2 patent drawing
  • US9238014B2 patent drawing

AI summary

Pharmaceutical composition for treating alcohol dependence in humans comprising two active ingredients:a compound having an antagonistic action on the 5-HT2 serotoninergic receptors selected as being cyproheptadine; anda compound having an antagonistic action on the alpha1-noradrenergic receptors selected from prazosin, alfuzosin, terazosin and tamsulosin.