CA2498639A1

CA2498639A1 - Niacin used as oral supplementation for the treatment and prevention of sexual dysfunction in human males and females

Info

Publication number: CA2498639A1
Application number: CA002498639A
Authority: CA
Inventors: J.D. Globus
Original assignee: Individual
Current assignee: Individual
Priority date: 2005-03-02
Filing date: 2005-03-02
Publication date: 2006-09-02

Abstract

The present invention addresses a vitamin and a method for treating the major underlying physiological causes of Peyronie's Disease in human males, as well as phallic erectile dysfunction in both genders. A combination of flush niacin, and extended-release nicotinic acid, is employed in suggested dosing regimes. The flush form of vitamin PP provides a rapid increase of blood circulation to the peripheral vessels which supply the erectile tissue of the genitalia. Niacin also provides a systemic antihyperlipidemic effect, which ameliorates vascular and arterial insufficiencies, both genital and coronary, associated with erectile dysfunction.

Description

SPECIFICATION
This invention relates to the combined use of oral flush niacin and slow-release niacin, and a method for the employment of this vitamin in treating sexual dysfunction. The proposed method is intended to address both the prevention and the treatment of Peyronie's Disease in males, as well as phallic erectile dysfunction in both sexes.
BACKGROUND
The current North American era of sexual liberation erroneously places an exorbitant strain on males, to be perpetually virile. Between the sexes, the larger phallus of the male has assumed the lead role, primarily as an instrument of penetration. To the silent detriment of many couples, the strength of the male ego has been bound to the functionality of the penis. The present invention also addresses the treatment of sexual dysfunction in females. From the standpoint of developmental biology, the clitoris is regarded as the precursor of the penis.
Both sexes are considered to have a phallus, regardless of size, capable of erection.' Sexual dysfunction, particularly in males, carries stigma, as it is often misconstrued as a sign of weakness, inadequacy, psychological illness, or disinterest in a partner. Although there are valid emotional factors which interfere with the translation of mental desire into physical arousal, there are often underlying physiological causes of sexual dysfunction. (The term 'sexual dysfunction" is intended to include FSAD (Female Sexual Arousal Disorder. In most instances in the text, FSAD is also implied where ED is mentioned.) Venous and arterial insufficiencies are two major factors that contribute to the complexities of ED and Peyronie's disease (PD)Z In fact, the most common causes of impotence are considered to be vascular problems with the flow of blood in and out of the penis.3 Rudolph Virchoff identified three factors that contribute to atherosclerosis, and thus, to ED. His triad consists of arterial wall disease, blood consistency, Z
and abnormalities of blood flow. 4 With regards to penile vascular health, high cholesterol diets that damage the coronary vessels, will also harm the penis.3b The identification of "polsters" in penile veins, originally thought to be valves, were discovered to be minute plaques, (deposits of fat, calcium and tissue).
Polsters not only alter the consistency of the blood, they also interfere with the filow of blood in the phallus, which heightens chances of developing impotency.3°
It has been documented in several sources that hyperlipidemia, hypertension, anxiety, obesity, and diabetes, all contribute to ED. I=or the purposes of this remedy, a preventative, systemic approach is adopted. The present invention of an oral indication for flush and slow-release niacin, is intended to complement or replace an existing ED therapy, (on the recommendation of, and under the supervision of, a physician).
Niacin is effective as both a peripheral nervous system (PNS) conditioner, as well as a central nervous system (CNS) conditioner. Central nervous system conditioners are defined as treatments which improve the internal "milieu" of the CNS, to enable erection. Peripheral nervous system (PNS) conditioners are defined as treatments which improve functions in phallic nerves and blood vessels, associated with engorgement and subsequent erections The term "arousal," can be misleading, as a degree of muscular relaxation is necessary for the blood to properly accumulate during the erectile phase.
The term "stress" is often used as a "blanket" diagnosis to refer to both external aggravations, (time pressure, distractions), as well as internal stressors, (performance anxiety and insecurities). This latter set of factors is equally as disruptive to sexual function as the former. Only a limited number of informal studies exist, with regards to the effectiveness of the sedative properties of niacin. However, a closely related compound, niacinamide, has been proven to have benzodiazepine-like effects on the CNS 6 Unlike niacin, niacinamide is not a vasodilator, nor is it a cholesterol-lowering agent;' hence the favoured use of niacin in the present invention. An ED/PD patient's condition is often aggravated by physiological complications, such as vitamin deficiencies,3d hypertension, physical anxiety, and over-stimulation of the sympathetic nervous system.
Hypertension has been successfully lowered, over the course of several months of daily use of niacin.
A complex interplay of nerves and blood vessels governs human sexual response. The phallus in both sexes is innervated by erectile nerves, which influence smooth muscle relaxation in the pudendal arteries which supply blood to the erectile tissue.'b In females, as the arteries relax, an influx of blood flows into the vascular mucous membranes of the vagina '°, and triggers mucosal lubrication. In males, nitric oxide (NO), is required for vasodilation to occur in the penis. Endothelial cells, which are required for the release of N0, are damaged by diabetes and high cholesterol5b The implementation of dietary restriction as a monotherapy, may not be an adequate method to lower cholesterol. An antihyperlipidemic agent such as niacin, prevents cholesterol accumulation in the coronary and penile blood vessels, and thus, indirectly protects the endothelium. Specific suggestions for diabetics are supplied in the methodology.
Disadvantages of existing ED therapies The range of existing ED/PD therapies for men include oral medications, penile injections, (ICIs), urethral pellets, (MUSE), vacuum pumps (VCDs), implants and surgery. Prior to sexual activity, the concept of inserting a needle or urethral pellet into the penis, presents an invasive image which usually detracts from a state of arousal. As this paper is intended to highlight the benefits of niacin therapy, only the major disadvantages of existing therapies will be presented.
Oral medications address the symptoms of ED; however, the underlying causes are often neglected. With the use of the PDES inhibitors, (e.g.
sildenafil, tadalafil, vardenafil), NO production is enhanced. However, the ED / FSAD

patient may have latent systemic vascular and arterial insufficiencies that impede erectile processes. Such disorders at the root of ED are not addressed by symptomatic treatments. Studies are still in their infancy, concerning a particular arrhythmia caused by drug-induced Q-T interval prolongation in the heart.g ED/PD patients with heart conditions, or those who experience coital angina after taking a PDES inhibitor, (e.g. tadalafil), are of particular vulnerability.9 The limited body of knowledge regarding drugs of this class carries mixed reports, and undoubtedly requires further investigation by neutral researchers.
In the young male "after-hours" social scene, current trends favour prolonged periods of erectile performance, and often lead to misuse of drugs such as Viagra. Priapisms longer than 24 hours can result in penile fibrosis and irreversible tissue damage.'° "Poppers"(amyl nitrite), are often abused during anal penetration scenarios. Poppers are inhaled as a volatile liquid, in order to relax anal muscles and encourage engorgement of the genital tissues.
Impurities such as acetone, cause "head rushes", headaches, elevated blood pressure and heart rates, even in healthy individuals.
There is also a misconception that physical arousal is enhanced by drugs which stimulate the sympathetic nervous system, such as cocaine and antidepressants. Although one may become mentally and/or partially physically aroused, following the ingestion of stimulants, the actions of the complementary parasympathetic nervous system become impaired. Increased sexual appetite is initially reported by amphetamine users; however, erections are usually sustainable once the substance levels wane in the bloodstream.
The eff'ICacy of apomorphine in producing erections capable of penetration, was tested on ED subjects without a major organic component to their sexual dysfunction. However, the success rate ranged only from approximately 46°!o to 60%, depending on the dosage.s° Since this drug stimulates the dopamine pathways in the brain's arousal centre, there is the potential for abuse.
Aminobenzoate potassium treatments are documented to be effective in softening arterial and venous plaques." However, Potaba is noted to cause nausea and hypoglycemia in diabetics and the elderly.'2 The discovery that the use of colchichine has caused birth defects in other animals, should serve as a warning for humans. "Fertility problems" have also been encountered during the course of preventative anti-inflammatory therapy with this drug.'Zb A
potentially safer alternative of oral vitamin E (400iu/d), does protect against heart attacks, but must be taken for more than two years in order to be 40% effective.'3 Over one-third of men treated with intercavernosal injection treatment, have reported pain from prostaglandin injections2~'4 The injection of nicotinyl alcohol into the penis causes local vasodilation. Since nicotinyl alcohol breaks down into nicotinic acid in the body, (pat#4127118). one could equate the vasodilative effects of the alcohol to those of orally ingested niacin. However, all injections cause scarring, even in resilient areas such as the gluteus maximus. Bearing this in mind, it is the opinion of the experimenter that the practice of repeated injection, of any medication, into the limited area of penile flesh, is counterproductive. Scars may appear as small nodules, which then exacerbate the existing ED by contributing to penile fibroid formation. Although the injectable calcium blocker, Verpamil, is available in oral forms, the lengthy list of adverse effects includes heart attack, water in the lungs, and of most concern, impotence.'S
MUSE therapy, (Medicated Urethral Systems for Erection), utilizes Alprostadil, a prostaglandin-based therapy, to dissolve scars. Insertion of urethral pellets overcomes the issues surrounding injection.SdHowever, insertion of foreign objects into the urethra defies the natural direction through which urine and semen flow, and could present possible discomfort, as well as the conceivable risk of infection.
An individual with an irregularly shaped penis may encounter difficulties, using a vacuum constriction device (VCD). A PD patient may not be able to "crack the plaque" of his fibrosis, due to inadequate force within the pump.2°

Plaques close to the base of the penis can aggravate the surrounding tissue, when using a VCD with a constriction band.Zd Home-made "tie-offs", such as rubber bands or shoelaces, should also be avoided by the PD patient.
Despite the delicate and irreversible nature of this surgery,'6 modern-day surgeons often take a casual, assembly-line approach to penile implantation, A
recent study reported "mechanical failure" in a significant 12.5°l0 of men who received penile implants,2e Benefits of Present Invention It is the intent of the present invention to transcend the discomfort and side-effects of many existing ED remedies. The objective is to connect enhanced erectile response with a positive sexual experience. The surgical and pharmaceutical industries have neglected the needs of ED and PD patients who fall into a low-income bracket. In 2005 Canadian dollar prices, a bottle of 90 (100mg) tablets, sells for under six dollars. It is easily accessible OTC at most health food stores. Flush niacin is an inexpensive, legal alternative to conventional therapies for sexual dysfunction. (The term"sexual dysfunction"
is intended to include FSAD (Female Sexual Arousal Disorder. FSAD is implied where ED is mentioned in the text) Niacin has a low side-effect profile, and can be tolerated in fairly high doses by most individuals. Due to its water-soluble composition, the remedy has a low risk of causing toxicity. A customized regime of slush niacin can accomplish many simultaneous therapeutic objectives. Both flush and slow-release forms of the vitamin have been employed by physicians, as time-tested remedies for hyperlipidemia. (pat#2438551). Flush niacin possesses anti-hypertensive and anxiety-quelling effects, which provide positive psychological reinforcement for repeated use.
The ability of niacin to move quickly cross the blood-brain barrier, is beneficial to the majority of ED patients, who apply their remedy shortly preceeding sexual activity.(pat.#2103399).

Virchoff recognized that various impairments to blood flow, play a major role in the onset and persistence of PVD (peripheral vascular disease). The applicaton of the same principles of blood flow should be extended to the treatment arena of Peyronie's disease and sexual dysfunction. Upon ingestion of the niacin, a "flushing" reaction occurs. Gentle surges of blood flow primarily into the subcutaneous blood vessels of the head and torso. Excess blood lipids are lowered on a systemic level, thus deterring plaque formation and associated erectile interference. Some individuals report blood flow radiating to the palms of the hands and feet. For many, the physical sensation could be described as a warm, tingling, "body buzz". This feature may be of assistance to those with peripheral neuropathies, such as diabetics. Provided the doses of flush niacin are increased gradually, (and the niacin is well tolerated), niacin therapy can be a viable alternative to the pain associated with priapism and needles.
Many men and women of the modern age do not have the time or the desire to monitor their caloric intake. Niacin therapy can drastically reduce this need to be hyper-vigilant about dietary restrictions. The beneficial effects of the vitamin on the circulatory system are residual, even when several days are skipped.
Intercourse is targeted as an aggravating factor for ED and PD patients.
Although men with cardiovascular disease and/or PD are often advised to abstain from sex, individuals driven by a high libido, will likely disregard this advice.
Women with FSAD may feel pressured by an insensitive partner, despite a lack of vaginal lubrication to make the experience sexually pleasurable. Niacin is capable of improving blood flow to the genitalia, thus "bridging the gap" between sexual desire and sexual activity.

METHODOLOGY
An understanding of the physiology and biochemistry of an erection is required in order to comprehend the mechanisms through which a remedy for sexual dysfunction operates. The sympathetic nervous system (SNS) contributes to maintaining the flaccid state of the penis, and similarly, the soft state of the clitorai tissue. The parasympathetic nervous system (PNS) is responsible for the erectile state of arousal.
Directing the blood to the phallus requires a properly functioning nervous system.3e In order for an erection to take place, the SNS must shut off, in order for the PNS
supply to turn on.'d The blood vessels of the external genitalia dilate, in response to signals from the parasympathetic system."
The provocation of mating habits in other species, such as those of male fish, has been associated with prostaglandin production.'g In human sexual response, prostagiandins are also synthesized.se Similarly, the ingestion of flush niacin also triggers a prostaglandin-mediated response in humans. The flush is most prominent in the subcutaneous facial and truncal areas of the body.
Vasodilation in the blood vessels of the chest, stimulate circulation to the erectile tissue of the nipples, which, "in some men (and most women), become firm and erect."3f The experimenter invites men and their partners to overcome the taboo surrounding nipple stimulation. Over time, most individuals will discover a connection between the nerves of the nipples, and the neural network of the phallus/clitoris.
It would be a simplistic approach to merely administer a systemic vasodilative agent, without conscious training of the network of nerves and blood vessels supplying the genitals. Individuals attempting to restore phallic/clitoral sensitivity, may practise a sequence of flexing and relaxing the muscles of the abdominals, buttocks, pelvis, and genitals. These exercises are subtle enough to be done discreetly throughout the day.

Patience is required for first-time experimenters with flush niacin, as it takes the body time to adjust to the flushing, and build up to the higher dosages.
It also takes time for the brain to re-establish a connection with the genital nerves.
In ED/PD patients with underlying conditions such as hypertension and hyperlipidemia, it may take approximately two months to notice a substantial improvement in blood circulation. Sensitivity of the genital nerve endings occurs gradually; one may notice a change as subtle as a heightened awareness of one's own clothing resting against the genital skin.
It is strongly advised that all potential users of niacin commence therapy based on the recommendation and supervision of a qualified physician.
When dietary measures alone are not adequate in reducing blood lipids, niacin can be quite dramatic in achieving this effect. Niacin can be employed by the physician as a complement to a statin-based therapy2' . For example, an ectomorphic diabetic may have elevated LDLs and VLDLs, and suffer from angina and peripheral circulation problems. (It is encouraging to note that the PNS
is quite resilient in its ability to regenerate.'e ) Although the extended-release form of niacin is indicated for diabetics with hyperlipidemia in the Compendium,'b blood sugar levels should be carefully monitored for elevations. It may be necessary to employ an oral hypoglycemic agent or make insulin modifications.22 The proper formulation and duration of vitamin PP treatment has the potential to improve erectile function while simultaneously resulting in some or all of the following:
1) a reduction in blood lipids 2) a reduction in hypertension 3) an amelioration of peripheral neuropathies 4) a reduction of the use/dosage of heart and/or blood pressure medications, such as beta blockers 1~
The present invention proposes a method that physiologically enables the patient to restore the condition of his/her circulatory system and enhance phallic erectile function through the combined supplementation of flush niacin and controlled-release niacin. For the purposes of the present invention, the immediate-release form, or flush form of nicotinic acid is preferred. It is the observation of the experimenter that repeated "flushes", or surges of blood, are part of the mechanism through which the vascular system is restored. The high dosages which are required to achieve cholesterol and triglyceride reduction, can be administered without the severe flushing that would occur with an equivalent dose of flush niacin. A combination of sustained release and flush niacin tablets are used to accomplish a two-fold objective of antihyperlipidemic action, combined with peripheral vasodilative stimulation. The tablets should be ingested on an empty stomach, in order to obtain the most rapid and optimal relief. The following table illustrates the "free nicotinic acid content" in three forms of niacin.2°
flush niacin 520 mg slow-release niacin 502.6 mg non-flush niacin 0 mg Based on the results of the experimenter, the degree of flushing was found to be directly proportionate to the content of nicotinic acid. The flush niacin brought a vigorous prostaglandin-mediated reaction in under five minutes. The sustained-release form produced an almost negligible amount of facial "pins and needles", without flushing. Niacinamide (NAM), was found to be ineffective in providing a vasodilative effect, and hence, discontinued. It is also documented to be four times more potentially toxic than nicotinic acid.'9 However, the present medical indications favour the primary use of sustained release niacin.

On a "per-use" basis, a suggested starting dose ranges from approximately 50-200 mg flush niacin, but can be increased to 500 mg per dose. The types of niacin employed in this experiment were Swiss Brand flush Niacin 100mg tablets and Now Brand 500mg tablets. The 100 mg (Swiss Brand) flush tablets were chosen over the 500 mg flush tablets (of the same brand), as they were discovered to be more potent and rapid, in terms of vasodilative action.
Utilizing flush niacin correctly in a dosing regime, can be surprisingly powerful in quickly subduing physical anxiety, that may be organic in nature, or related to pertormance anxiety. When one is anxious, blood flow to the penis is restricted.. Flush niacin effectively counteracts the anxiety-related vasoconstriction of the peripheral vascular system. Finding the appropriate dosage should be based on a balance between the highest degree of niacin-induced flush reaction that one can tolerate without undesirable side effects.
The subject should be assessed for a "blushing" of the skin, as opposed to a burning or swelling of the skin. It is best to allow at least 2 hour intervals between doses, staggering them equidistant from one another. The body develops a tolerance to the flushing effect after approximately one month , and in order to maintain the intensity of the blood surge, it is necessary to increase the daily dosages conservatively, (in 50-100mg increments), until the original effect is achieved. Tolerance, however, is only one factor in dose modulation.
Dosages require continual adjustments according to pre-existing medical conditions. Patients with schizophrenic disorders can have subdued or even negligible flushing reactions. (pat.#225fi394) For these patients, concurrent treatment with other anti-psychotics, (such as quetiapine fumarate), can intensify the flush. For both flush and controlled-release forms, ranges of 1-grams per dose are given in the Compendium, with a daily maximum of 6 grams.(in exceptional cases up to 9 grams) At the higher doses, liver function should be monitored. The maintenance antihyperlipidemic dosage range for either form is 2-6 grams per day, or 1-2 grams, 2-3 times per day, with meals.'°

The proper dosage range should be determined by the supervising physician. At the higher doses, liver function should be monitored. The use of flush niacin is preferred over sustained-release, as far as is practical and tolerable. It may be helpful to take the flush doses in the privacy of one's home, and reserve the slow-release for settings that require discretion. The following tables illustrate a recommended dosing schedule of two months, to use as a guideline, for an individual without pre-existing health concerns. For the first set of tables (mixed regime), assume flush, unless otherwise indicated.
Example Niacin Regime For a Generally Healthy Individual:
Week One (1 St half) Dose Numb~r Dose Time dosage (mgj 1 9 am 50 2 6 pm 50 2 6pm 100 ~QO mg..daily total Week Two Dose Number Dose Time Dosag~r: (mg) y ..

1 7 am 100 2 9 am 100 3 6 pm 100 4 8 pm 100 e~~0 rng daily~total Week Three (SL = slow release) Dose Number Doss Time Dosage (mg) 1 ? am 100 2 ~2 pm 500 (SL) 3 ~ pm 100 4 9 pm 100 800 rrtg daily total Week Four and Week Five Dose Number Dose Time Dos~~e (mg) 1 ~ am 100 2 12 pm 500 (SL) 3 fi pm 500 (SL) 4 9 pm 100 120 mg daily total Week Six Dose Number Dose Time Dosage (ttngj 1 ~ am 500 (SL) 2 12 pm 500 (SL) 3 7 pm 500 (SL) 1540 mg daily total Week Seven and Eight Individuals who tolerate these basal doses are also encouraged to experiment with flush niacin, between 5 to 15 minutes before a sexual encounter. A
suggested dosage would be 100 mg to 500 mg at a time. Information from a personal chart can be a definitive tool in determining the suitable doses of niacin to be administered. Charting consists of recording the date, time, amount and type of niacin,. prescribed medications, and any other substances consumed, (including cigarettes and alcohol), for the duration of the treatment. It is helpful for the physician to monitor the reduction of both blood pressure, as well as LDLs, VLDLs and trigycerides, that will occur in the course of niacin therapy.
In the event that: the patient has an intolerance to the flush formulation, a strictly slow-release dosing schedule may be suggested by the physician.
Example Slow-Release Only Niacin Regime:
For an ED Patient with Hyperlipidemia Week One (1''t half Dose Numt~er Doss Tirriwe Dosag~,(ra9) 1 9 am 500 2 fi pm 0 5Q0 mg dally total Week One (2nd half Dose Number Doss Time. C~~~a~e-,~t,i) ..
g am 500 ~ pm 500 ~10~0 ~mg d~ily~totai Week Two and Three Week Four and Week Five Dose Nunnber :Doss Time . Dosage (mg) 1 0 am 1000 6 pm 1000 2Q00 ~m~ daily total Week Six Week Seven and Eight Dose Number Dose Tim~ Dcrsag~- (mg) 1 7 am 1000 2 12 pm 1000 3 7 pm 1000 3Q00 mg daily to't~l Current Limitations Niacin has relatively few contraindications; however, patients with diabetes, hypotension, bleeding problems, glaucoma, gout, or liver problems, should only engage in niacin therapy under the strict advice and supervision of a doctor.
Medications used for high blood pressure or high cholesterol, heart conditions (eg.nitrates) and blood thinners will also affect the type and dosage of niacin to be employed.''' Individuals with a niacin allergy or hypersensitivity, should refrain from usage. Dizziness, nausea, or joint pain can occur if the individual doses are too high, and such side effects can become more likely with daily doses in excess of 1 gram. If a dose evokes a response similar to that of a menopausal "hot flash", or vertigo, the individual should assume a supine position, and 'wait for the uncomfortable reaction to pass. It should subside in 10 minutes or less. In order to avoid these types of reactions, it is advisable to increase doses in small increments of 50-100 mg at a time. Although the prostaglandin-induced reaction is generally considered "harmless"(U.S.
pat.#6048881), an excess of prostaglandins have been linked to fever, nausea, vomiting, and inflammatory conditions such as arthritis.'=~h Individuals with allergies/sensitivities to compounds belonging to the "nightshade" plants, (e.g.
tobacco, from which nicotine is derived,~3) should obtain thorough medical advice prior to commencing niacin therapy, especially regarding dosage.
Dosing regimes could pose an inconvenience, especially if obvious flushing became an issue in the workplace. Slow-release niacin alleviates dosing l~
frequency as the tablets are available in higher dosages; however these formulations are intentionally manufactured to minimize peripheral vascular vasodilation. Certain brands of both slow-release and flush tablets, (unknown to the experimenter), have been reported to be hepatoxic.2°b This topic requires further research into whether the toxicity is dosage-dependent, due to poor quality formulations, or otherwise.
The findings of Meyers et al reveal that flush and slow-release tablets have a similar content of nicotinic acid. However, from the experimenter's experience, a quantity of at least 50-200mg must be released into the bloodstream at once, in order to provide any noticeable rise in circulation or relief from anxiety.
Although it is well documented that slow-release tablets of niacin are effective in treating hyperlipidemia, it is yet to be determined whether this type of tablet could be formulated to release an adequate amount of niacin at the correct times of day, to encourage regular blood flow to the erectile tissues of the phallus and/or nipples.
With regards to prior art, the applicant has made all conceivable efforts to avoid patent infringement. During the preliminary research, the patent which utilizes niacin in the treatment of vascular disease (#2123935), was discovered.
The present invention uses niacin in the treatment of sexual dysfunction which occurs as a result of vascular and arterial insufficiencies. Therefore, the claims section omits the following applications for niacin treatment in humans:
1) sexual dysfunction due to vascularlarterial insufficiencies, as a result of:
a) cardiac disorders b) hypertension c) diabetic complications d) peripheral neuropathies This experiment is fairly embryonic, as preventative therapy is a more recent concept in the realm of ED treatments. Due to the fact that niacin is considered a pharmaceutical, issues of patient safety and the experimenter's liability became limiting factors. Bearing this in mind, the majority of the data was obtained by testing done on the experimenter, by the experimenter. It should be noted that the nicotinic acid content of OTC niacin has not been federally regulated in Canada or the United States. These formulations need to standardized, in order to yield reliable and repeatable experimental results. However, despite its modest beginnings, the present invention is being submitted with the hope that its novelty, effectiveness, and therapeutic properties will lead to further clinical testing, product refinement, and advancement in preventative medicine.
FUTURE APPLICATIONS
Combination Therapies The local secretion of vasoactive prostaglandins is dependent on the availability of fatty acid precursors. Linoleic and arachidonic acid provide the building blocks for healthy vessel walls, which in turn, improve vascular resistance.z4 Linoleic acid has also been credited with the ability to protect against prostate cancer.26 EFAs are employed in a multitude of remedies, including ameliorating peripheral neuropathies, and treating impotence.(pat#2218699) A brief investigation was made into the efficacy of EFAs in treating hyperlipidemia. Fish oil, which contains both DHA and EPA, has had mixed reviews in regards to its abilities to improve hyperlipidemias. and neuropathies. A study revealed that fish oil actually raises LDLs, and promotes hyperglycemia in diabetics.24b Anti-hypercholesterolemic therapies, such as treatment with a statin and fish oil, can be enhanced by the addition of niacin.
For example, a prescribed lipid-lowering regime may consist of lovastatin (40mg b.i.d.),a fish oil, (iig/d), with oral niacin (500mg/d).24°
The human metabolism requires adequate levels of vitamin B6. for the synthesis of niacin from tryptophan, as well as for the production of gamma amino butyric acid (GABA).'9b Deficiency in vitamin B6 and/or GABA, can result in peripheral neuropathies'9° Inadequate levels of B6 can cause atherosclerosis of the blood vessels, whereas deficiencies of GAGA can also result in physical anxiety,25 which causes the phallus to remain in a contractile state, in spite of arousal.
Grape seed proanthocyanidins (PCOs), (classified as llavonoids, with anti-oxidant properties), have proven to be beneficial to the cardiovascular and circulatory systems.2' PCOs are effective in treating both peripheral vascular and neural disorders and promoting nerve regeneration (pat.#2470603).
Proanthocyanidins reinforce capillary walls and collagen in blood vessels.
These scavengers of free-radicals reduce vein leakage, by preventing lesions that encourage LDLs to form plaques. Presently, there is a French patent by Jacques Masquelier, for his PCO formulation,2g Beyond Grape Seed", by Flora. T"' A
patent that operates along the same vein as the present invention addresses the treatment of vascular disease with niacin in combination with aspirin and other trace elements. (pat# 2123935). Phospholipid complexes of PCOs are employed in the prevention and treatment of atherosclerosis (pat#2312795). Current measures used in the treatment and prevention of ED/PD may be potentially improved by the addition of an oral formulation which combines PCOs with niacin supplementation.
Extended Hypotheses NADPH is one of the constituents required for the synthesis of nitric oxide.
Since the principal forms of nicotinic acid that exist in animal tissues are documented as NADH and NADPH,29 it is possible that NADPH may be utilized as a resource for the NO required for erection to take place.
Injectable nicotinyl alcohol can be used for the treatment of ED
(pat#4217118). The nicotinyl alcohol is converted to nicotinic acid in the body, which induces a local prostaglandin-mediated "swell" in the penile tissue.
However, a high percentage of males are experiencing post-injection pain.(44%
in one study3°) In order to rectify inherent problems with injection, prostaglandin creams have been invented. The Alprostadil cream used to treat FSAD could potentially cause burning of the sensitive inner labia of the vagina. Methyl nicotinate, also related to nicotinic acid, is presently formulated into a cream for women3'. In order to circumvent the problem of skin irritations, the inventor proposes a future application of niacin, formulated as an ointment. Since prostaglandins are vasoactive locally, the cream could be applied directly to the genitals and/or nipples where enhanced blood flow is required, (avoiding the mucous membranes). In females, yeast infections, (which are a common side effect with the use of topical ointments.), are more easily avoided when the internal environment of the vagina is kept more acidic in pH. Although not overly acidic, nicotinic acid is still on the acidic side of the pH scale. Provided that a niacin ointment formulation was tolerated without skin reactions, it may be a helpful tool in avoiding the invasive use of needles, pellets, and stinging creams.
Since on a biological level, mates secure their bond with an extended coital process,32 it would be prudent to pursue ED/FSAD remedies which make the sexual experience pleasurable for both partners.

Claims

1. A method of treating human sexual dysfunction, consisting of the oral administration of niacin; wherein the sexual dysfunction is:
a) Peyronie's disease in males b) erectile dysfunction in males c) compromised clitoral engorgement in females d) a deficiency of vaginal secretion in females e) associated with lack of sensitivity in the nipples of males and/or females f) caused by the peripheral (distal genital) vasoconstriction associated with physical anxiety

2. The method in accordance with claim 1 , wherein the niacin, (flush and/or sustained release), is orally administered in the forms including, but not limited to, tablet, pill, capsule, powder, solution, liquid, lozenge, or chewing gum.

3. The method in accordance with claim 2, wherein the niacin is administered in a total amount ranging from, but not limited to, approximately 100 mg to approximately 6g per day.

4. The method in accordance with claim 3, wherein the niacin is administered in a regime comprised of, but not limited to, two to four doses per day, of approximately 50 mg to approximately 2g per dose.