Note: Descriptions are shown in the official language in which they were submitted.
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1
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,
CA 02498639 2005-03-02
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
CA 02498639 2005-03-02
3
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
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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
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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°
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6
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).
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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.
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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.
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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
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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.
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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-
2
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.'°
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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
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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
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14
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
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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
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16
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
CA 02498639 2005-03-02
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
CA 02498639 2005-03-02
18
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
CA 02498639 2005-03-02
19
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
CA 02498639 2005-03-02
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.
