Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
2001-11-14
2003-03-04
Spivack, Phyllis G. (Department: 1614)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
Reexamination Certificate
active
06528521
ABSTRACT:
FIELD OF THE INVENTION
The present invention is directed to a method for treating sexual dysfunction in a patient taking anti-depressant medication in need of such treatment comprising administering a therapeutically effective amount of apomorphine or a pharmaceutically acceptable salt thereof to said patient. The method may be utilized for patients taking anti-depressants such as tricyclic anti-depressants, monamine oxidase inhibitors or serotonin selective reuptake inhibitors.
BACKGROUND OF THE INVENTION
Depression is a chronic illness that affects people of all ages. Tricyclic antidepressants, monamine oxidase inhibitors, and selective serotonin reuptake inhibitors are classes of drugs which are prescribed for the treatment of depression. Tricyclic anti-depressants include imipramine hydrochloride, imipramine pamoate, amitriptyline hydrochloride, desipramine hydrochloride and protriptyline hydrochloride. Monamine oxidase inhibitors include isocarboxazid, phenelzine sulfate and tranylcypromine sulfate. Of the various classes of anti-depressants currently available, the selective serotonin reuptake inhibitors (SSRI's) are among the most successful.
SSRI's include fluoxetine, fluvoxamine, citalopram, cericlamine, femoxetine, ifoxetine, cyanodothiepin, seritraline, paroxetine and litoxetine. Anti-depressants have many undesirable side effects, such as disturbance of sexual function. Since sexual dysfunction is common in depression as part of the underlying disease, the use of a drug to treat depression which may further cause sexual dysfunction is particularly objectionable.
A variety of strategies have been reported in the management of SSRI-induced sexual dysfunction, including waiting for tolerance to develop, dosage reduction, drug holidays, substitution of another anti-depressant drug, and various augmentation strategies (addition of another drug) with 5-HT
2
, 5-HT
3
and &agr;
2
adrenergic receptor antagonists, 5-HT
1A
and dopamine receptor agonists and phosphodiesterase enzyme inhibitors, as disclosed by Rosen et al. in
J. Clin. Psychopharmacol.
Vol. 19, No 1, pp.67-84.
Augmentation strategies may include co-treatment with cyproheptadine, bethanecol, yohimbine, amantadine, alprazolam, chlordiazepoxide, clonazepam, diazepam or lorazepam according to Forman et al., “Drug-induced infertility and Sexual Dysfunction” in
Textbook of Erectile Dysfunction
, Oxford: Isis Medical Media Ltd, 1999, pp. 40-43; co-treatment with Ginkgo Biloba as disclosed in U.S. Pat. No. 5,897,864; or co-treatment with sidenafil, according to Fava et al., “An Open Trial of Oral Sildenafil in Antidepressant-Induced Sexual Dysfunction”,
Psychother. Psychosom.,
1998, 328-331.
Nevertheless, there is still a need for effective medications which can be used to treat sexual dysfunction in patients taking anti-depressants.
It is therefore an object of the present invention to provide a method for the treatment of sexual dysfunction in patients taking anti-depressants, to treat the condition potentially caused by the depression and exacerbated by the anti-depressant.
SUMMARY OF THE INVENTION
The present invention is directed to a method of treating sexual dysfunction in a patient taking anti-depressant medication in need of such treatment comprising administering a therapeutically effective amount of apomorphine or a pharmaceutically acceptable salt thereof to said patient. The anti-depressant medication may be a tricyclic anti-depressant, a monamine oxidase inhibitor or a serotonin-selective reuptake inhibitor. Preferably, the therapeutically effective amount of apomorphine is an amount wherein a concentration of apomorphine is attained within said patient's plasma of up to 10 nanograms per milliliter.
If the patient is male, the therapeutically effective amount may be an amount sufficient to induce an erection adequate for vaginal penetration. Alternatively, if the patient is female the therapeutically effective amount may be an amount sufficient to induce clitoral erectogenesis and vaginal engorgement. Preferably, the therapeutically effective amount is insufficient to produce emesis. However, if larger (potentially emesis-inducing) doses are required, the apomorphine may be co-administered with an emesis-inhibiting amount of an anti-emetic agent.
The anti-emetic agent may be nicotine, lobeline sulfate, metoclopramide, chlorpromazine, prochlorperazine, pipamazine, thiethylperazine, oxypendyl hydrochloride, domperidone, ondansetron, buclizine hydrochloride, cyclizine hydrochloride, dimenhydrinate, scopolamine, metopimazine, trimethobenzamide, benzauinamine hydrochloride or diphenidol hydrochloride.
In the method, apomorphine may administered intranasally, orally ingested, sublingually or administered by inhalation to the lungs. Moreover, the apomorphine may be administered as a pharmaceutically acceptable salt, preferably the hydrochloride salt.
DETAILED DESCRIPTION OF THE INVENTION
In males, the form of sexual dysfunction is erectile dysfunction. A normal erection occurs as a result of a coordinated vascular event in the penis. This is usually triggered neurally and consists of vasodilation and smooth muscle relaxation in the penis and its supplying arterial vessels. Arterial inflow causes enlargement of the substance of the corpora cavemosa. Venous outflow is trapped by this enlargement, permitting sustained high blood pressures in the penis sufficient to cause rigidity. Muscles in the perineum also assist in creating and maintaining penile rigidity. Erection may be induced centrally in the nervous system by sexual thoughts or fantasy, and is usually reinforced locally by reflex mechanisms. Erectile mechanics are substantially similar in the female for the clitoris.
Impotence or male erectile dysfunction is defined as the inability to achieve and sustain an erection sufficient for intercourse. Impotence in any given case can result from psychological disturbances (psychogenic), from physiological abnormalities in general (organic), from neurological disturbances (neurogenic), hormonal deficiencies (endocrine) or from a combination of the foregoing. Impotence may be hormonal, congenital, vascular or partial ability, among others.
These descriptions are not exact, however. There is currently no standardized method of diagnosis or treatment. As used herein, psychogenic impotence is defined as functional impotence with no apparent overwhelming organic basis. It may be characterized by an inability to have an erection in response to some stimuli (e.g., masturbation, spontaneous nocturnal, spontaneous early morning, video erotica, etc.) but not others (e.g., partner or spousal attention).
Females also can have sexual dysfunction that increases with age and is associated with the presence of vascular risk factors 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, 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.
Apomorphine ((R)-5,6,6a,7-tetrahydro-6-methyl-4H-dibenzo-[de,g]quinoline-10,11-diol) can be represented by the formula
and exists in a free base form or as an acid addition salt. For the purposes of the present invention, apomorphine hydrochloride is preferred, however other pharmacologically acceptable salts thereof can be utilized as well.
Apomorphine can be used in the form of pharmaceuticall
Perdok Renee J.
Ruff Dustin D.
Spivack Phyllis G.
Tap Pharmaceutical Products, Inc.
Wood Phillips Katz Clark & Mortimer
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