Combination Therapy for Premature Ejaculation

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Solution Overview

Problem

Current treatments for premature ejaculation, such as psychotherapy, topical anesthetics, and antidepressant compounds, are either ineffective, cause significant side effects, or require specialized therapists, making them inconvenient and embarrassing to use, and do not address the issue effectively for all patients.

Innovation Solution

A combination of a μ-opiate analgesic like tramadol, an NMDA receptor antagonist like dextromethorphan, and a cyclic-GMP-specific phosphodiesterase type 5 inhibitor like sildenafil, potentially with a cytochrome P450 inhibitor like quinidine, is administered to delay ejaculation and improve sexual performance without the drawbacks of existing methods.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If psychotherapy is used to treat premature ejaculation, then specialized therapeutic intervention is provided, but it requires specialized therapists and is inconvenient and embarrassing for patients

Engineering Contradiction:
Improvetreatment effectivenessVSAvoidconvenience of treatment
Core Design Contradiction:
ReliabilityVSEase of operation

Solution Approach 1:

The patent replaces the mechanical/behavioral intervention system of psychotherapy with a pharmacological system. Instead of requiring specialized therapists to deliver behavioral therapy, the invention uses chemical compounds (antidepressants, topical anesthetics, or their combinations) to achieve the therapeutic effect of delaying ejaculation, thereby eliminating the need for specialized therapeutic intervention and improving patient convenience.

Inventive Principle:
Principle #28Mechanics substitution (Replace mechanical system)

2Duration of action of moving object

If topical anesthetics are used to treat premature ejaculation, then ejaculation is delayed, but significant side effects occur

Engineering Contradiction:
Improveduration of intercourseVSAvoidside effects
Core Design Contradiction:
Duration of action of moving objectVSObject-affected harmful factors

Solution Approach 1:

The patent changes the chemical parameters of the treatment by using different classes of compounds (antidepressants like SSRIs, or topical anesthetics like lidocaine) with varying mechanisms of action and side effect profiles. By selecting compounds with appropriate potency and specificity, the invention aims to achieve the desired duration extension while minimizing harmful side effects through parameter optimization rather than using a single fixed treatment approach.

Inventive Principle:
Principle #35Parameter changes

3Duration of action of moving object

If antidepressant compounds are used to treat premature ejaculation, then ejaculation is delayed, but significant side effects occur

Engineering Contradiction:
Improveduration of intercourseVSAvoidside effects
Core Design Contradiction:
Duration of action of moving objectVSObject-affected harmful factors

Solution Approach 1:

The patent employs parameter changes by using different antidepressant compounds (SSRIs, SNRIs, TCAs) with varying pharmacological properties, dosages, and side effect profiles. The invention optimizes treatment by selecting specific compounds and dosages to achieve the desired delay in ejaculation while minimizing adverse effects through careful parameter adjustment rather than uniform treatment protocols.

Inventive Principle:
Principle #35Parameter changes

4Reliability

If a combination of μ-opiate analgesic, NMDA receptor antagonist, and phosphodiesterase type 5 inhibitor is used, then sexual performance is improved with minimal side effects, but the treatment complexity increases

Engineering Contradiction:
Improvetreatment effectivenessVSAvoidtreatment complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent merges multiple pharmacological agents (μ-opiate analgesics like tramadol, NMDA receptor antagonists like dextromethorphan, and phosphodiesterase type 5 inhibitors like sildenafil) into a single combination therapy. This merging approach addresses different physiological mechanisms simultaneously - pain modulation, excitatory neurotransmission blockade, and vascular function enhancement - thereby improving overall treatment effectiveness while potentially reducing the need for multiple separate treatments.

Inventive Principle:
Principle #5Merging (Combining)

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

This combination effectively prolongs sexual intercourse, allowing both partners to reach orgasm, with minimal side effects and no need for specialized therapy, improving sexual satisfaction and reducing premature ejaculation issues.

Implementation Method 1

a μ-opiate analgesic, which is a μ-opiate receptor agonist, partial agonist or agonist/antagonist

Methodology Applied
Scientific EffectOpiate receptor agonism:

Implementation Method 2

an NMDA receptor antagonist or a pharmaceutically acceptable salt thereof

Methodology Applied
Scientific EffectNMDA receptor antagonism:

Implementation Method 3

a cyclic-GMP-specific phosphodiesterase type 5 inhibitor like sildenafil

Methodology Applied
Scientific EffectPhosphodiesterase inhibition:

Implementation Method 4

a cytochrome P450 inhibitor like quinidine

Methodology Applied
Scientific EffectCytochrome P450 inhibition:

Data Source

PatentUS9272037B2Method to treat premature ejaculation in humans
Publication Date: 2016.03.01 TRINITY LABORATORIES INC
  • US9272037B2 patent drawing
  • US9272037B2 patent drawing
  • US9272037B2 patent drawing

AI summary

The present invention belongs to the fields of pharmacology, medicine and medicinal chemistry, and provides methods and compositions for treating sexual dysfunction; more particularly, the invention relates to treatment of premature ejaculation in humans.