Female sexual dysfunction treatment

Details Female sexual dysfunction treatment Female sexual dysfunction treatment

1999-07-02

2001-02-27

Page, Thurman K. (Department: 1615)

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

Implant or insert

C424S447000

Reexamination Certificate

active

06193992

ABSTRACT:

FIELD OF THE INVENTION
This invention relates to methods for ameliorating female sexual dysfunction.
BACKGROUND OF THE INVENTION
Apomorphine is a dopamine receptor agonist that has been widely utilized as an emetic agent, sedative, antiparkinsonian agent as well as a behavior altering agent. Recent research and clinical studies have demonstrated that in males apomorphine has an erectogenic effect manifested by penile erection.
The effect of apomorphine on female sexual functionality has not been previously investigated. Females also can have sexual dysfunction, however, that increases with age. Female sexual dysfunction usually is associated with the presence of vascular risk factors, genital smooth muscle atrophy, and onset of menopause. Some of the vascular and muscular mechanisms that contribute to penile erection in the male are believed to be similar vasculogenic factors in female genital response. It is known that in women sexual arousal is accompanied by arterial inflow which engorges the vagina and increases vaginal lubrication, and that the muscles in the perineum assist in achieving clitoral erection.
In the female patient, sexual dysfunction can arise from organic and psychogenic causes, or from a combination of the foregoing. Female sexual dysfunction includes a failure to attain or maintain vaginal lubrication-swelling responses of sexual excitement until completion of the sexual activity. Organic female sexual dysfunction is known to be related in part to vasculogenic impairment resulting in inadequate blood flow, vaginal engorgement insufficiency and clitoral erection insufficiency.
Female sexual dysfunction has not been studied as extensively as male sexual dysfunction. This has partly been due to historical belief that female sexual dysfunction was orgasmic-related (delayed or non-orgasmic) or libido, and hence lacked an appropriate animal model.
The use of New Zealand White male rabbits as animal models for impotence has been well established. More recently, studies have reported that New Zealand White female rabbits are also suitable animal model for studying the vascular pathology in female sexual dysfunction. Such studies have shown that vaginal vascular engorgement and clitoral erection depend on blood inflow. See, for example, Park et al, “Vasculogenic female sexual dysfunction: the hemodynamic basis for vaginal engorgement insufficiency and clitoral erectile insufficiency,”
International Journal of Impotence Research,
9, (1), 27-37 (March 1997).
For psychogenic sexual dysfunction management, psychological sex therapy can also be employed to help the patient.
Apomorphine previously was shown to have very poor oral bioavailability. See, for example, Baldessarini et al., in Gessa et al., (eds.),
Apomorphine and Other Dopaminomimetics, Basic Pharmacology,
1, 219-228, Raven Press, N.Y. (1981).
More recently, studies with males show that oral administration of apomorphine can be used to induce an erection in a psychogenic male patient, as long as the apomorphine dose required to achieve a significant erectile response is not accompanied by nausea and vomiting or other serious undesirable side effects such as arterial hypotension, flushing and diaphoresis. See U.S. Pat. No. 5,624,677 to El-Rashidy et al. and Heaton et al.,
Urology,
45, 200-206 (1995). The specific mechanisms by which apomorphine acts to produce an erectile response in a human patient are not yet completely understood but are believed to be centrally acting through dopamine receptor stimulation in the medial preoptic area of the brain.
It has now been found that certain controlled delivery systems for apomorphine can provide a practical therapeutic use in ameliorating sexual dysfunction in human females while reducing the likelihood of undesirable side effects.
SUMMARY OF THE INVENTION
Administration of apomorphine to a human female increases nerve stimulated clitoral intracavernosal blood flow and vaginal wall blood flow, each of which is associated respectively with enhanced clitoral erection and vaginal engorgement in a female.
A sublingual apomorphine dosage form, usually containing about 2 to about 12 milligrams, preferably about 2 to about 8 milligrams, of apomorphine, is preferred for producing sexual readiness in human females without inducing substantial nausea or other undesirable side effects. Other dosage forms can be utilized as well.
Administration of apomorphine in an amount sufficient to produce vaginal engorgement is effected preferably about 15 to about 20 minutes prior to sexual activity. The plasma concentration of apomorphine is maintained at no more than about 5.5 nanograms per milliliter, preferably about 0.3 to about 4 nanograms per milliliter, and more preferably about 1 to about 2 nanograms per milliliter, so as to maintain a circulating serum level and mid-brain tissue level of apomorphine during the period of sexual activity sufficient to maintain vaginal engorgement, its associated lubrication and clitoral erection during coitus, but less than the amount that induces substantial nausea.
While sublingual administration of apomorphine is preferred for present purposes, other routes of administration are also suitable. Illustrative of such alternate routes of administration are buccal patch, transdermal patch, cream, ointment, intranasal spray, tablets, capsules and the like.


REFERENCES:
patent: 5562917 (1996-10-01), Durif et al.
patent: 5945117 (1999-08-01), El-Rashidy et al.

Affiliated with

Also associated with

Rating

Female sexual dysfunction treatment does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Female sexual dysfunction treatment, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Female sexual dysfunction treatment will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFUS-PAI-O-2612165