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Use of norepinephrine reuptake modulators for preventing and treating vasomotor symptoms

a norepinephrine reuptake and modulator technology, applied in the direction of biocide, cardiovascular disorder, drug composition, etc., can solve the problems of profuse sweating, disruptive and disabling, and not suitable for all women

Inactive Publication Date: 2008-09-18
WYETH LLC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Hormonal treatments are very effective at alleviating VMS, but they are not appropriate for all women.
It is well recognized that VMS are caused by fluctuations of sex steroid levels and can be disruptive and disabling in both males and females.
It is usually accompanied by outbreaks of profuse sweating.
Hot flushes and outbreaks of sweats occurring during the night can cause sleep deprivation.
As many as one-third of these patients will experience persistent and frequent symptoms severe enough to cause significant discomfort and inconvenience.
In addition, hormone replacement therapy is usually not recommended for women or men with or at risk for hormonally sensitive cancers (e.g. breast or prostate cancer).
However, using such treatment is associated with a number of undesired side effects caused by high doses necessary to abate hot flash described herein and known in the related arts.

Method used

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  • Use of norepinephrine reuptake modulators for preventing and treating vasomotor symptoms
  • Use of norepinephrine reuptake modulators for preventing and treating vasomotor symptoms
  • Use of norepinephrine reuptake modulators for preventing and treating vasomotor symptoms

Examples

Experimental program
Comparison scheme
Effect test

example 1

Effect of NRIS in Alleviating Vasomotor Instability in Pre-Clinical Models of Vasomotor Instability

[0111]Method used as described in the general method section under morphine-dependent rat model with the following exceptions: Rats were injected subcutaneously with vehicle (sterile H2O) or desipramine that may be prepared as described in U.S. Patent Publication No. 2002 / 0107249, dissolved in sterile H2O and administered at 0.1, 1.0, 10 and 30 mg / kg 1 hour prior to naloxone (FIG. 3A). At maximal flush (15 minutes post-naloxone; Δ° C., Mean +SEM) desipramine dose-dependently abates the naloxone-induced flush. [0134] Rats were injected subcutaneously with vehicle (sterile H2O) or desipramine dissolved in sterile H2O and administered at 10 mg / kg) (FIG. 3B). Changes in TST (Δ° C., Mean +SEM) overtime in the telemetry model of OVX-induced thermodysregulation demonstrate that desipramine significantly decreases TST over the entire length of the active phase (FIG. 3B). An analysis of results...

example 2

Effect of a Combination of NRI and SRI on Alleviation of Vasomotor Instability

[0115]Method are described in the general method section under morphine-dependent rat model with the following exceptions: Rats were injected subcutaneously with vehicle sterile H2O), desipramine, (which was prepared as described in U.S. Pat. No. 3,454,554, dissolved in sterile H2O and administered at 0.1, 1.0, 10 mg / kg) or fluoxetine (Sigma, dissolved in sterile H2O at 10, 30, 60 mg / kg) or combination of fluoxetine administered at 10 mg / kg and increasing doses of desipramine listed above 1 hour prior to naloxone.

[0116]At maximal hot flush (15 minutes post-naloxone; Δ° C., Mean +SEM) desipramine dose-dependently abates the naloxone-induced flush in the MD model but results in a shallow slope of the estimated line (solid line, FIG. 4). The shallow slope of the estimated line is typical of compounds that have multiple site interactions. Therefore, a dose of fluoxetine that did not abate the naloxone-induced ...

example 3

Effect of Compounds with Dual NRI / SRI Activity on Alleviating Vasomotor Instability

[0117]Method as described in the general method section under morphine-dependent rat model with the following exceptions: Rats were injected subcutaneously with vehicle (sterile H2O), venlafaxine (dissolved in sterile H2O and administered at 1.0, 10, 20, 40 mg / kg) or), DVS-233 (dissolved in sterile H2O and administered at 1.0, 10, 30, 60 mg / kg) 1 hour prior to naloxone. Venlafaxine and DVS-233 were synthesized as described in U.S. Pat. No. 4,535,186. At maximal flush (15 minutes post-naloxone; Δ° C., Mean +SEM) venlafaxine dose-dependently (ED50 value=15+7 mg / kg) abates the naloxone-induced flush (FIG. 5A). At maximal flush (15 minutes post-naloxone; Δ° C., Mean +SEM) DVS-233 dose-dependently ED50 value=30+3 mg / kg) abates the naloxone-induced flush (FIG. 5B).

[0118]Method of FIGS. 5C and 5D were as described in the general method section under telemetry model. Rats were injected subcutaneously with veh...

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Abstract

The present invention relates to the use of compounds and composition of compounds that modulate norepinephrine levels for the prevention and treatment of vasomotor symptoms, such as hot flush, caused by, inter alia, thermoregulatory dysfunctions.

Description

CROSS-REFERENCE TO RELATED APPLICATIONS[0001]This application is a divisional of U.S. patent application Ser. No. 10 / 684,777, which was filed on Oct. 14, 2003, and which claims benefit of priority to U.S. Application Ser. No. 60 / 418,591, filed Oct. 15, 2002, the disclosure of which is incorporated herein by reference in its entirety.FIELD OF THE INVENTION[0002]The present invention relates to the use of compounds and composition of compounds that modulate norepinephrine levels for the prevention and treatment of, inter alia, vasomotor symptoms (VMS).BACKGROUND OF THE INVENTION[0003]Vasomotor symptoms (VMS), referred to as hot flushes and night sweats, are the most common symptoms associated with menopause, occurring in 60% to 80% of all women following natural or surgically-induced menopause. VMS are likely to be an adaptive response of the central nervous system (CNS) to declining sex steroids. To date, the most effective therapies for VMS are hormone-based treatments, including es...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/381A61K31/137A61P43/00A61K31/13A61K31/138A61K31/155A61K31/167A61K31/4174A61K31/496A61K31/497A61K31/5377A61K31/55A61P5/00A61P9/00
CPCA61K31/13A61K31/137A61K31/55A61K31/5377A61K31/497A61K31/138A61K31/155A61K31/167A61K31/381A61K31/4174A61K31/496A61K2300/00A61P15/12A61P25/00A61P25/20A61P43/00A61P5/00A61P9/00
Inventor DEECHER, DARLENE COLEMANMERCHENTHALER, ISTVAN JOZSEFLEVENTHAL, LIZASIPE, KIMBERLY JEANO'CONNOR, LAWRENCE THOMAS
Owner WYETH LLC
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