U.S. patent application number 12/687207 was filed with the patent office on 2010-05-06 for penis enlargement.
Invention is credited to Kenneth W. Adams.
Application Number | 20100112027 12/687207 |
Document ID | / |
Family ID | 31188417 |
Filed Date | 2010-05-06 |
United States Patent
Application |
20100112027 |
Kind Code |
A1 |
Adams; Kenneth W. |
May 6, 2010 |
Penis Enlargement
Abstract
A method for causing a permanent increase in the length and
girth of a male subject's penis, the method comprising treatment
comprising the step of (a) administering to the male an effective
amount of a vasodilator selected from the group consisting of a
vasodilator per se and compositions thereof comprising a
pharmaceutically-acceptable diluent or carrier, to induce a
cumulative prolonged engorgement of the subject's penis; and (b)
repeating step (a) as necessary to cause the increase during the
treatment. A potentiator which enhances the effect of the
vasodilator may also be used.
Inventors: |
Adams; Kenneth W.; (North
York, CA) |
Correspondence
Address: |
MORGAN LEWIS & BOCKIUS LLP
1111 PENNSYLVANIA AVENUE NW
WASHINGTON
DC
20004
US
|
Family ID: |
31188417 |
Appl. No.: |
12/687207 |
Filed: |
January 14, 2010 |
Related U.S. Patent Documents
|
|
|
|
|
|
Application
Number |
Filing Date |
Patent Number |
|
|
10986027 |
Nov 12, 2004 |
7671091 |
|
|
12687207 |
|
|
|
|
Current U.S.
Class: |
424/422 ;
514/171; 514/226.2; 514/304; 514/307; 514/401; 514/535;
514/573 |
Current CPC
Class: |
A61K 31/485 20130101;
A61K 45/06 20130101; A61K 38/2221 20130101; A61P 15/00 20180101;
A61K 31/5575 20130101; A61K 31/46 20130101 |
Class at
Publication: |
424/422 ;
514/307; 514/226.2; 514/304; 514/401; 514/573; 514/171;
514/535 |
International
Class: |
A61K 9/00 20060101
A61K009/00; A61K 31/472 20060101 A61K031/472; A61K 31/5415 20060101
A61K031/5415; A61K 31/4748 20060101 A61K031/4748; A61K 31/417
20060101 A61K031/417; A61K 31/19 20060101 A61K031/19; A61K 31/568
20060101 A61K031/568; A61P 15/00 20060101 A61P015/00; A61K 31/24
20060101 A61K031/24 |
Foreign Application Data
Date |
Code |
Application Number |
Jul 25, 2003 |
CA |
PCT/CA2003/001139 |
Claims
1. A method for causing, a permanent increase in the length and
girth of a male subject's penis, said method comprising treatment
comprising the step of (a) administering to said male an effective
amount of a vasodilator and a potentiator for said vasodilator to
induce a cumulative prolonged engorgement of the subject's penis;
and (b) repeating step (a) as necessary to cause said permanent
increase during said treatment.
2. A method as defined in claim 1, wherein said vasodilator is in
admixture with a pharmaceutically-acceptable diluent or
carrier,
3. (canceled)
4. A method as defined in claim 1, wherein said prolonged
engorgement is sustained for at least 4 hours.
5. A method as defined in claim 1, wherein said vasodilator is
administered as one dose in said treatment step throughout the
prolonged engorgement.
6. A method as defined in claim 1, wherein said vasodilator is
administered as at least two doses as defined in said treatment
throughout the prolonged engorgement.
7. A method as defined in claim 6, wherein the engorgement
comprises a first erectile response of at least 65%, and a second
dose or subsequent doses are administered after the first erectile
response falls below 65% during said treatment.
8. (canceled)
9. A method as defined in claim 1, wherein said treatment is
applied to said patient at least four times per week for a period
of at least 3 months.
10. A method as defined in claim 1, wherein the length of the fully
erect penis has increased by at least 5% after a treatment period
of 12 to 18 months.
11. A method as defined in claim 10, wherein the length of the
fully erect penis is increased by at least 30% after a treatment
period of 12 to 18 months.
12. A method as defined in claim 1, wherein the girth of the fully
erect penis is increased by at least 5% after a treatment period of
12 to 18 months.
13. A method as defined in claim 12, wherein the girth of the fully
erect penis is increased by at least 30% after a treatment period
of 12 to 18 months.
14. A method as defined in claim 1, wherein said engorgement
comprises a 75-100% erectile response for at least 90% of the time
of the prolonged engorgement.
15. A method as defined in claim 1, wherein said engorgement
comprises a 75-100% erectile response for 50-90% of the time of the
prolonged engorgement.
16. A method as defined in claim 1, wherein said engorgement
comprises a 75-100% erectile response for up to 50% of the time of
the prolonged engorgement.
17. A method as defined in claim 1, wherein said engorgement
comprises a 40-75% erectile response for at least 3 hours.
18. A method as defined in claim 1, wherein said vasodilator is
selected from the group consisting of nitrovasodilators, ACE
inhibitors, angiotensin receptor antagonists, phosphodiesterase
inhibitors, direct vasodilators, adrenergic receptor antagonists,
calcium channel blocking drugs, alpha blockers, beta blockers,
lymphthomimetics, vitamins, organic nitrates, serotonin
receptorblocking agents, angina blocking agents, other hypertensive
agents, cardiac stimulating agents, agents which improve renal,
vascular function, sympathomimetic amine, and salts, derivatives
precursors, pharmaceutically active sequences or regions,
peptidomimetics, mimetics, and mixtures thereof.
19. A method as defined in claim 18, wherein said vasodilator is
selected from the group consisting of papaverine, chlorpromazine,
atropine, phentolamine, and prostaglandin E1, or a mixture
thereof.
20. A method as defined in claim 19, wherein said vasodilator is
prostaglandin E1.
21. A method as defined in claim 1, wherein said vasodilator is
formulated for administration by direct injection to the cavernosal
tissue, by needle, auto-injector, slow sustained injection pump,
high pressure injection device, microinfusion pump, urethral
suppository, or implantable sustained release drug or device.
22. A method as defined in claim 1, wherein said vasodilator is
formulated for systemic administration by oral, sublingual, or
suppository administration, intravenous administration by needle,
auto-injector, slow sustained injection pump, high pressure
injection device, microinfusion pump, or implantable sustained
release drug or device, or topical administration, such as through
the use of creams, lotions or patches.
23. A method as defined in claim 1, wherein said vasodilator is
administered to the dense connective tissue surrounding the
erectile tissue of the penis by a deep injection that goes below
the dermis and subcutaneous tissues.
24. A method as defined in claim 1, wherein said vasodilator is
administered to the dorsal suspensory ligand of the penis.
25. A method as defined in claim 1, wherein said vasodilator is
administered as an intracavemosal injection.
26. A method as defined in claim 21, wherein said vasodilator is
administered as an implantable sustained release drug or
device.
27. A method as defined in claim 20, wherein said prostaglandin El
is administered at a dosage of 0.5 to 100 micrograms/kg body
weight/day by intracavemosal injection.
28. A method as defined in claim 20, wherein the prostaglandin El
is administered systemically at a dosage of 2 to 10,000
microgramslkg body weight/day by an implantable sustained release
drug or device.
29. (canceled)
30. A method as defined in claim 1, wherein the potentiator is
administered by direct injection to the cavernosal tissue, by
needle, auto-injector, slow sustained injection pump, high pressure
injection device, microinfusion pump, urethral suppository, or
implantable sustained release drug or device.
31. A method as defined in claim 1, wherein the potentiator is
systemically administered by oral, sublingual, or suppository
administration, intravenous administration by needle,
auto-injector, slow sustained injection pump, high pressure
injection device, microinfusion pump, or implantable sustained
release drug or device, or topical administration, such as through
the use of creams, lotions or patches.
32. A method as defined in claim 1, wherein the potentiator is
administered to the dense connective tissue surrounding the
erectile tissue of the penis by a deep injection that is well below
the dermis and subcutaneous tissues.
33. A method as defined in claim 1, wherein the potentiator is
administered to the dorsal suspensory ligand of the penis.
34. A method as defined in claim 1, wherein the potentiator is
administered by intracavemosal injection.
35. A method as defined in claim 1, wherein the potentiator is
administered as an implantable sustained release drug or
device.
36. A method as defined in claim 1, wherein the potentiator is
administered separately from the composition.
37. A method as defined in claim 1, wherein the potentiator is
administered concurrently with the composition.
38. A method as defined in claim 1, wherein the potentiator is
administered more than once during said treatment.
39. A method as defined in claim 1 wherein the potentiator is a
hormone.
40. A method as defined in claim 39, wherein the hormone is an
androgen selected 15 from the group consisting of the naturally
occurring androgens and derivatives thereof, or an agent that will
stimulate the androgen receptor directly or indirectly, including
androsterone, androsterone acetate, androsterone propionate,
androsterone benzoate, androstenediol, androstenediol-3-acetate,
androstenediol-17-acetate, androstenediol-3, 17-diacetate,
androstenediol-17-20 benzoate,
androstenediol-3-acetate-17-benzoate, androstenedione,
dehydroepiandrosterone (DHEA; also termed "prasterone"), sodium
dehydroepiandrosterone sulfate, 4-dihydrotestosterone (DHT; also
termed "stanolone"), 17.beta.-hydroxyandrost-4-en-3-one,
5.alpha.-dihydrotestosterone, dromostanolone, dromostanolone
propionate, 25 ethylestrenol, nandrolone phenpropionate, nandrolone
decanoate, nandrolone furylpropionate, nandrolone
cyclohexanepropionate, nandrolone benzoate, nanodrolone
cyclohexanecarboxylate, oxandrolone, stanozolol and testosterone,
pharmaceutically acceptable esters of testosterone and
4-dihydrotestosterone, including esters formed from the hydroxyl
group present at the C-17 position, including, but not limited to,
the enanthate, propionate, cypionate, phenylacetate, acetate,
isobutyrate, buciclate, cyclopentylpropionate, isocarponate,
heptanoate, decanoate, undecanoate, caprate and isocaprate esters,
pharmaceutically acceptable derivatives of testosterone such as
methyl testosterone, testolactone, oxymetholone and
fluoxymesterone; synthetic androgens, and 7-Methyl-Nortestosterone
("MENT''") and its acetate ester, and salts, derivatives,
precursors, pharmaceutically active sequences or regions,
peptidomimetics, mimetics, and mixtures thereof.
41. A method as defined in claim 40, wherein the androgen is
testosterone.
42. A method as defined in claim 40, wherein the androgen is
dihydrotestosterone.
43. A method as defined in claim 1, wherein the potentiator
promotes the elongation of collagen.
44. A method as defined in claim 1, wherein the potentiator
inhibits collagen cross-linkage.
45. A method as defined in claim 1, wherein the potentiator is
selected from a group consisting of insulin like growth factor,
growth hormone, metallo-porteinases or metallo-proteinase agonists
or promoters of collagenase activity, tissue inhibitors of matrix
metalloprotenases (TIMPS) other agents that increase collagen
solubility, prostaglandins, corticosteroids, potassium
aminobenzoate, and dimethyl sulfoxide (DMSO), D-penicillamine, and
salts, derivatives, precursors, pharmaceutically active sequences
or regions, peptidomimetics, mimetics, and mixtures thereof.
46. (canceled)
47. A method as defined in claim 45, wherein the prostaglandin is
selected from prostaglandin F2 alpha and prostaglandin E2.
48. A method as defined in claim 45, wherein the potentiator is
relaxin, prostaglandin F2 alpha, or prostaglandin E2, or the
biochemical mediator that results in the desired changes in
collagen or the connective tissue that produces and remodels
collagen and express the effects of relaxin, prostaglandin F2
alphs, or prostaglandin E2.
49. A method as defined in claim 45, wherein the potentiator is
potassium aminobenzoate.
50. A method as defined in claim 45, wherein the potentiator is
dimetnyl sulfoxide (DMSO).
51. A method as defined in claim 45, wherein relaxin is
administered at a dosage of 0.02 to 1 micrograms/kg body weight/day
by intracaversonal injection.
52. A method as defined in claim 45, wherein relaxin is topically
administered at a dosage of 25 to 400 micrograms/kg body
weight/day.
53. A method as defined in claim 45, wherein relaxin is
administered at a dosage of 0.02 to 1 micrograms/kg body weight/day
by injection into the dense connective tissue of the erectile
tissue surrounding the penis.
54. A method as defined in claim 1, comprising applying a device to
prolong the retention of the composition in the penis.
55. A method as defined in claim 54, comprising fitting said device
in the form of a ring around the base of the penis.
56. A kit comprising a vasodilator per se or a composition thereof
in admixture with a pharmaceutically-acceptable diluent or carrier,
and instructions for administering said vasodilator to a human male
according to a method as defined in claim 1.
57. A kit as defined in claim 56, wherein the instructions are
provided in written form.
58. A kit as defined in claim 56 for use wherein the instructions
are provided orally by a health professional.
59. A kit as defined in claim 56, wherein the instructions are
provided in video compact disc form.
60. A kit as defined in claim 56, further comprising a potentiator
for enhancing the effect of the vasodilator.
61. A kit as defined in claim 57, further comprising a potentiator
for enhancing the effect of the vasodilator.
62. A kit as defined in claim 58, further comprising a potentiator
for enhancing the effect of the vasodilator.
63. A kit as defined in claim 59, further comprising a potentiator
for enhancing the effect of the vasodilator.
64. A method as defined in claim 19 wherein the potentiator is a
hormone.
65. A method as defined in claim 1 wherein the vasodilator is
prostaglandin E1, papavarine, phentolamine, atropine or
chlorpromazine and the potentiator is testosterone,
dihydrotestosterone, prostaglandin F, potassium aminobenzoate or
dimethyl sulfoxide.
Description
RELATED APPLICATIONS
[0001] This application claims priority from U.S. application No.
60/398,562, filed Jul. 26, 2002, and PCT/CA2003/001139, filed Jul.
25, 2003.
FIELD OF INVENTION
[0002] This invention is in the field of penis enlargement.
BACKGROUND OF INVENTION
[0003] There are various circumstances under which a male subject
may desire the permanent enlargement of the length and/or girth of
his penis, in both its flaccid and erect states. Penis enlargement
may be desired for medical reasons, for example, if a patient is
unable to penetrate during coitus due to an unusually small penis
size; for cosmetic reasons; or to improve a person's
self-esteem.
[0004] There have been many attempts to create a safe and effective
means for achieving permanent penis enlargement, including the use
of external weights and suction devices. The use of external
weights is cumbersome and impractical and produces localized
compressive forces that may cause localized ischemia. Furthermore,
use of weights often leads to a thinning of the penis and may even
impair penis function.
[0005] Suction devices are also cumbersome and impractical to wear
on a prolonged basis, have limited effectiveness, and pose a number
of risks. Suction devices produce localized compressive forces that
may cause localized ischemia. Vacuum seals with pressure over 20 mm
Hg can obstruct capillary flow and inhibit tissue perfusion.
Suction devices often come with warnings that the devices should
not be used for periods exceeding 20-30 minutes, which may be
insufficient to achieve the desired result. Use of suction devices
can also result in the thickening of the skin and accumulation of
fluid in the superficial layers of the skin and subdermis. The skin
of the penis is hypermobile, and only very loosely connected to
deeper connective tissues and structures that comprise the erectile
tissues of the penis. The skin of the penis can readily separate
from the fibrous connective tissue capsule which encloses the
erectile tissue of the penis when externally applied suction forces
are applied to the penis.
[0006] Also, any suction forces applied to the penis will have a
proportionately larger effect on the skin, and the forces on the
deeper structures diminish dramatically. The increase in the
surface area of the skin causes the suction forces to be applied
mainly to the skin, not to the erectile tissue and the surrounding
capsule of the cavernosal tissue. As a result, the skin can be
thickened as fluid is extravasated and there is typically no, or
only a limited enlargement, of the underlying erectile tissues of
the penis. Use of suction devices may also cause the separation of
the skin from the subdermis and the formation of seromas or
blisters on the penis. The application of suction devices to the
penis causes the extravasation of red blood cells out of the
vascular spaces and into the extracellular compartments. If vacuum
devices are applied for extended periods of time, this may lead to
a significant pigmentation of the penis. Applying a suction device
repeatedly may cause the deposition of large amounts of iron and
other hemoglobin degradation products in the tissue of the penis
causing hemosiderosis, which ultimately results in fibrosis.
Furthermore, erectile dysfunction may result from prolonged use of
these devices.
SUMMARY OF THE INVENTION
[0007] In a first aspect, this invention provides a pharmaceutical
vasodilator which induces a cumulative prolonged engorgement of a
human penis, optionally as a composition together with a
pharmaceutically-acceptable diluent or carrier, for use in causing
a permanent increase in size of the human penis. As explained in
greater detail below, the permanent increase in size is achieved by
repeated use of the vasodilator or composition thereof, say, once a
day for a few days a week over many weeks, possibly many
months.
[0008] In accordance with another aspect of this invention, there
is provided a method of enhancing penis size by administering said
vasodilator or composition thereof so as to induce a cumulative
prolonged engorgement of the penis. According to the method, such
an administration lasts for a limited time during one day, and is
repeated up to daily or a few days a week over a period of several
weeks.
[0009] Thus, in one aspect the invention provides a method for
causing a permanent increase in the length and girth of a male
subject's penis, said method comprising treatment comprising the
step of a (a) administering to said patient an effective amount of
a vasodilator selected from the group consisting of a vasodilator
per se and compositions thereof comprising a
pharmaceutically-acceptable diluent or carrier, to induce a
cumulative prolonged engorgement of the subject's penis; and (b)
repeating step (a) as necessary to cause said increase during said
treatment.
[0010] Preferably, the composition includes a pharmaceutically
acceptable diluent or carrier, which can aid in the administration
of the vasodilator of the composition for inducing a prolonged
engorgement of a human penis, for use in causing a permanent
enlargement of the penis.
[0011] Although it is known in the prior art that vasodilators can
be administered to a male to induce engorgement of the penis, the
prior art is silent on the period of engorgement. In contrast, the
present invention provides for a prolonged period of engorgement as
defined herein. Further, in accordance with the practise of the
present invention, a permanent increase as defined herein is the
primary object of the invention.
[0012] The prior art is both silent on the hereindefined period of
engorgement and on the resulting permanent increase in penis size.
In contrast to the disclosure and teachings of the prior art, in
the present invention, engorgement of the penis is not the final
desired result, nor in isolation is the required period of
engorgement. The present invention defines the nature of the
compound and its function, i.e. a vasodilator of use in the present
invention, and how it provides the solution of the problem by
administration thereof to provide the essential prolonged
engorgement feature to effect permanent increase in penis size,
through one or more administrative treatments.
[0013] This invention provides the use of pharmacological
vasodilators to cause a permanent increase in the length and girth
of a human penis. As used herein, the term "permanent increase"
refers to a long-term increase and refers to an increase that lasts
for several months or years, or maybe even the life-time of the
person.
[0014] The term "penis length" refers to the maximum length of the
penis, as measured along the dorsal surface of the penis from the
symphysis pubis to the tip or end of the glans penis when the glans
penis is pulled manually and put under tension. Preferably, the
measurement is taken when the penis is fully erect.
[0015] The term "penis girth" refers to the largest measured value
obtained for circumference of the erect penis, as measured in the
midshaft region (middle third). Preferably, the measurement is
taken when the penis is fully erect.
[0016] An engorgement is deemed "cumulative prolonged" when an
erectile response lasts for at least 3 hours over a 24 hours
period. Typically, an engorgement of the invention, one that is
suitable to cause penis enlargement, is repeatedly induced for a
cumulative period of 3 to 6 hours, daily (or at least four days per
week), for weeks or months, but for at least 4 weeks.
[0017] Erectile responses may be categorized according to the
following: a 100% response or engorgement is a maximal erection
which is very hard, firm and unbendable, a 75% response is the
softest response considered hard enough for penetration, a 65-75%
response would be partially engorged but would not be sufficient
for penetration and intercourse, 40-65% is not a usable erection
for sexual intercourse but will have therapeutic effect for
enlargement according to the invention, and a response of less than
40% is a slightly engorged, very soft penis wherein the size of the
penis is close to the non-erect dimension of flaccid penis with no
discernable significant firmness when it is manually palpated by an
experienced health professional, and is probably not useful for
penis enlargement. Therefore, a "cumulative prolonged engorgement"
would be an erectile response that is over 40% for a period of at
least 3 hours in a 24 hours period.
[0018] As used herein, a "full erection", or the term "fully
erect", refers to an erectile response of between 75-100%.
[0019] The engorgement of the invention is typically for a
"cumulative prolonged" period, as described further below. The
engorgement period is thus usually at least 3 hours, but may be
31/2 hours, 4 hours, 41/2 hours, 5 hours, 51/2 hours, even up to 6
hours, but heavy engorgement of a penis, say 40% or more, is
usually avoided for extended periods of time, i.e., of more than 6
hours. The erectile response may, thus, be of the 3-6 hours
engorgement resulting from a single administration per 24 hours or
as a result of a plurality of administrations in this 24 hours
period.
[0020] It is possible, thus, with some patients to obtain the
required engorgement or a suitable length of time by administering
a single dose. Other patients may require doses, one at the
beginning of a daily treatment, and one or more later one during
the same treatment so as to maintain the engorgement, say above 40%
engorgement. Multiple dosing also may simply be a preferred method
of obtaining and maintaining a suitable degree of engorgement
without inducing (or at least inducing for a relatively short
period of time) a heavy engorgement of say 75%, 90% or 100%, which
the subject may simply want to avoid for personal or other
reasons.
[0021] Typically, the initial erectile response is at least 65%.
Later doses can be administered if the engorgement falls below 65%,
or say 40 to 45%.
[0022] Administration may be two times a week for one month, more
likely 3 or 4 or more days per week, and treatments may to on for
several weeks or months, often at least 3 months.
[0023] Sometimes an endpoint is chosen after a degree of
enlargement is obtained, say 5% (length, and/or girth) within 12 to
18 months, for example. More typically, an increase of say 30% is
sought, depending upon the desire of the subject and the
effectiveness of the treatment, which can vary.
[0024] Accordingly, the daily engorgement can include a 75-100%
erectile response for at least 90% of the time of the prolonged
engorgement. In another embodiment, the engorgement includes a
75-100% erectile response for 50-90% of the time of the prolonged
engorgement time. Alternatively, the engorgement can include a
75-100% erectile response for up to 50% of the time of the
prolonged engorgement. Also, engorgement can include a 40-75%
erectile response for at least 3 hours.
[0025] The active ingredient is a compound which causes
vasodilation, e.g., a vasodilator. The vasodilator may be selected
from the group consisting of nitrovasodilators, ACE inhibitors,
angiotensin receptor antagonists, phosphodiesterase inhibitors,
direct vasodilators, adrenergic receptor antagonists, calcium
channel blocking drugs, alpha blockers, beta blockers,
lymphthomimetics, vitamins, organic nitrates, serotonin
receptor-blocking agents, angina blocking agents, other
hypertensive agents, cardiac stimulating agents, agents which
improve renal, vascular function, sympathomimetic amine, and salts,
derivatives, precursors, pharmaceutically active sequences or
regions, peptidomimetics, mimetics, and mixtures thereof.
[0026] Preferably, the vasodilator is selected from the group
consisting of papaverine, chlorpromazine, atropine, phentolamine,
and prostaglandin E1, and mixtures thereof. A preferred vasodilator
is prostaglandin E1.
[0027] Administration can be by direct injection to the cavernosal
tissue, by needle, auto-injector, slow sustained injection pump,
high pressure injection device, micro pump infustion, urethral
suppository, or implantable sustained release drug or device.
[0028] The composition can be formulated for systemic
administration by oral, sublingual, or suppository administration,
intravenous administration by needle, auto-injector, slow sustained
injection pump, micro pump infusion, high pressure injection
device, or implantable sustained release drug or device, or topical
administration, such as through the use of creams, lotions or
patches.
[0029] The composition can be formulated for administration to the
dense connective tissue surrounding the erectile tissue of the
penis by a deep injection that goes below the dermis and
subcutaneous tissues. The composition can be formulated for
administration to the dorsal suspensory ligand of the penis.
[0030] A preferred embodiment includes a composition formulated for
intracavernosal injection, but the composition might also be
formulated for administration by an implantable sustained release
drug or device.
[0031] Prostaglandin E1 could be administered in a dosage range of
from about 0.5 to about 100 micrograms by intracavernosal
injection, or systemically at a dosage of 2 to 10,000 micrograms by
an implantable sustained release drug or device.
In another aspect of the invention, the active agent is combined
with a potentiator, either directly or in vivo.
[0032] The potentiator can thus be formulated for administration by
direct injection to the cavernosal tissue, by needle,
auto-injector, slow sustained injection pump, high pressure
injection device, micro pump infusion, urethral suppository, or
implantable sustained release drug or device, etc.
[0033] The composition can be formulated for systemic
administration by oral, sublingual, or suppository administration,
intravenous administration by needle, auto-injector, slow sustained
injection pump, high pressure injection device, micro pump
infusion, or implantable sustained release drug or device, or
topical administration, such as through the use of creams, lotions
or patches.
[0034] The potentiator can be formulated for administration to the
dense connective tissue surrounding the erectile tissue of the
penis by a deep injection that goes below the dermis and
subcutaneous tissues.
[0035] The potentiator can be formulated for administration to the
dorsal suspensory ligand of the penis, or for intracavernosal
injection, or for administration by an implantable sustained
release drug or device.
[0036] The potentiator can be administered separately from the
composition or concurrently with the composition.
[0037] The pharmaceutical composition can be such that the
potentiator is for administration more than once both separately
from and concurrently with the composition.
[0038] The potentiator can be a hormone. The hormone can be an
androgen selected from the group consisting of, but not limited to,
the naturally occurring androgens and derivatives thereof, or any
agent that will stimulate the androgen receptor directly or
indirectly, including androsterone, androsterone acetate,
androsterone propionate, androsterone benzoate, androstenediol,
androstenediol-3-acetate, androstenediol-17-acetate,
androstenediol-3,17-diacetate, androstenediol-17-benzoate,
androstenediol-3-acetate-17-benzoate, androstenedione,
dehydroepiandrosterone (DHEA; also termed "prasterone"), sodium
dehydroepiandrosterone sulfate, 4-dihydrotestosterone (DHT; also
termed "stanolone"), 17.beta.-hydroxyandrost-4-en-3-one,
5.alpha.-dihydrotestosterone, dromostanolone, dromostanolone
propionate, ethylestrenol, nandrolone phenpropionate, nandrolone
decanoate, nandrolone furylpropionate, nandrolone
cyclohexanepropionate, nandrolone benzoate, nandrolone
cyclohexanecarboxylate, oxandrolone, stanozolol and testosterone,
pharmaceutically acceptable esters of testosterone and
4-dihydrotestosterone, including esters formed from the hydroxyl
group present at the C-17 position, including, but not limited to,
the enanthate, propionate, cypionate, phenylacetate, acetate,
isobutyrate, buciclate, cyclopentylpropionate, isocarponate,
heptanoate, decanoate, undecanoate, caprate and isocaprate esters,
pharmaceutically acceptable derivatives of testosterone such as
methyl testosterone, testolactone, oxymetholone and
fluoxymesterone; synthetic androgens, and 7-Methyl-Nortestosterone
("MENT'") and its acetate ester, and salts, derivatives,
precursors, pharmaceutically active sequences or regions,
peptidomimetics, mimetics, and mixtures thereof.
[0039] A specific potentiator is the androgen testosterone. Another
is 4-dihydrotestosterone.
[0040] The potentiator can be selected to promote the elongation of
collagen, or to inhibit collagen cross-linkage, or to increase
collagen solubility.
[0041] The potentiator can be selected from a group consisting of
relaxin, insulin like growth factors, growth hormone,
metallo-proteinases or metallo-proteinase agonists or promoters of
collagenase activity, tissue inhibitors of matrix metalloprotenases
(TIMPS), other agents that increase collagen solubility,
prostaglandins, corticosteroids, potassium aminobenzoate
(Potaba.TM.), and dimethyl sulfoxide (DMSO), D-penicillamine, and
salts, derivatives, precursors, pharmaceutically active sequences
or regions, peptidomimetics, mimetics, and a mixture thereof.
[0042] A particular potentiator is relaxin.
[0043] A prostaglandin potentiator can be prostaglandin F2 alpha or
prostaglandin E2. The potentiator might be relaxin, prostaglandin
F2 alpha, or prostaglandin E2, or the biochemical mediators that
result in the desired changes in collagen or the connective tissue
that produces and remodels collagen and express the effects of
relaxin, prostaglandin F2 alpha, or prostaglandin E2.
[0044] Another potentiator is aminobenzoate potassium (Potaba.TM.),
or dimethyl sulfoxide (DMSO).
[0045] Relaxin can be administered at a dosage of 0.02 to 10
micrograms/kg body weight/day by intracavernosal injection. Relaxin
might be for topical administration at a dosage of 25 to 400
micrograms/kg body weight/day. The relaxin might be for
administration at a dosage of 0.02 to 1 micrograms/kg body
weight/day by injection into the dense connective tissue
surrounding the erectile tissue of the penis.
[0046] A device can be used to prolong the retention of the
composition in the penis. For example, a ring designed to fit
around the base of the penis might be used.
[0047] Thus, as hereinabove defined, the invention provides a
method for causing enlargement of a male subject's penis,
comprising the steps of (a) administering to the patient an
effective amount of a pharmaceutical vasodilator, optionally in
admixture with a pharmaceutically acceptable agent to induce a
prolonged engorgement of the subject's penis; and (b) repeating
step (a) as necessary to cause said enlargement.
[0048] The invention includes a kit that include a composition of
the invention as disclosed herein, in combination with instructions
for administering the composition to a human male according to a
method disclosed herein for the purposes disclosed herein.
[0049] Typically, such instructions are provided in written form,
but they could be provided orally by a health professional, or in
an electronic form on a medium such as a video compact disc,
laser-readable disk, video tape, audio tape or disk, etc.
DETAILED DESCRIPTION OF THE INVENTION
[0050] In one embodiment of the invention, a pharmaceutical
vasodilator composition is administered to a male patient to cause
a prolonged engorgement of the penis in order to cause expansion of
the erectile tissue. The pharmaceutical composition comprises a
pharmaceutically acceptable vasodilator for causing a prolonged
suitable engorgement of the penis, together with a pharmaceutically
acceptable diluent or carrier. The vasodilator may be a drug
typically used to treat erectile dysfunction, but administered at a
similar or higher dosage or sequentially as two or more lesser
doses to achieve a prolonged period of engorgement followed by an
additional period of lesser engorgement. Optionally, the agent may
be administered at a slow rate with a micro infusion pump,
time-release device or other self-injection technique or device.
During a treatment, the penis should be engorged for a minimum of 3
hours and typically there is one treatment per day, and at least
four treatments per week.
[0051] A very hard firm erection which is usually preferred for
erectile dysfunction will have more veno-occlusive obstruction of
the circulation and the reduced flow of fresh oxygenated blood into
the erectile tissue will limit the maximum duration that the
erection can be safely maintained. A softer less firm response can
be safely and comfortably maintained for a greater length of time
than a full erection.
[0052] The vasodilator drug may be one which either directly or
indirectly causes vasodilation and may be classified, without
limitation, in one of the following categories, namely,
nitrovasodilators, ACE inhibitors, angiotensin receptor
antagonists, phosphodiesterase inhibitors, direct vasodilators,
adrenergic receptor antagonists, calcium channel blocking drugs,
alpha blockers, beta blockers, lymphthomimetics, vitamins, organic
nitrates, serotonin receptor-blocking agents, angina blocking
agents, other hypertensive agents, cardiac stimulating agents,
agents which improve renal, vascular function, sympathomimetic
amine and mixtures thereof. For example, the drug may be any
suitable vasodilator, such as papaverine, chlorpromazine, atropine,
phentolamine, and prostaglandin E1, and salts, derivative,
precursors, pharmaceutically active sequences or regions,
peptidomimetics, mimetics, and mixtures thereof. Other drugs which
may cause vasodilation include, without limitation, any of the
following: niacin, nitroglycerine, nilatrin hydrochloride,
pentoxyphylene, phenoxybenzamine, dichlophenac, hydralazine,
hydrazaline, hydrochlorothiazide, sodium nitroprusside, isoxaprine
hydrochloride, epoprostenol sodium, nylidrin hydrochloride,
tolazoline hydrochloride, nicotinyl alcohol, phentolamine mesylate,
phentolamine hydrochloride, yohimbine, thymoxamine imipramine,
verapamil, isoxsuprine, naftidrofuryl, tolazoline, hydroisosorbide,
dibenamine dinitrate, captopril, enalapril, enalaprilat, quinapril,
lisinopril, ramipril, losartan, amrinone, milrinone, vesnarinone,
nicorandil, prazosin, labetalol, celiprolol, carvedilol,
bucindolol, nifedipine, dobutamine, minoxidil, nylidrin, and salts,
derivatives, precursors, and mixtures thereof. Preferably, the
vasodilator is prostaglandin E1, alone or with other vasodilators,
administered as one or more doses that are typically lower than
what would be used to treat erectile dysfunction. For example, the
prostaglandin E1 may be administered by intracavernosal injection
in a dosage range of 0.2 mcg to 500 mcg, more preferably in a
dosage range of 0.5 mcg to 100 mcg. For example again, the
prostaglandin E1 may be administered by an implantable sustained
release drug or device in a dosage range of 0.5 mcg to 20,000 mcg,
more preferably in a dosage range of 2 to 10,000 mcg (mcg
=microgram).
[0053] Optionally, the patient may be treated with an additional,
second pharmacological agent, to potentiate the effect of the
composition which causes a prolonged, engorgement of the penis.
Here, the second agent is called a "potentiator". The potentiator
may be administered as part of the composition, separately from the
composition, or a combination of both.
[0054] The potentiator may be a pharmacological agent or
combination of agents that promote cellular processes that result
in biological and/or mechanical creep and ultimately induce
remodelling of the connective tissues that help define the size and
shape of the penis. In addition, an agent which increases
solubility of collagen may be used as a potentiator. Agents with
very specific mechanisms of action may be used, or other agents
with pleomorphic mechanisms of action, such as relaxin or growth
hormone which trigger diverse mechanisms to induce growth in the
penis may be used. For example, agents may be administered that
facilitate the elongation of collagen fibres and accelerate the
turnover remodelling rates of collagen through numerous mechanisms.
For example, D-penicillamine and dimethyl sulfoxide (DMSO), which
promote the elongation of collagen by inhibiting or interfering
with inter- and intramolecular collagen cross-linkage may be used.
Other agents include, but are not limited to, relaxin, insulin like
growth factors, growth hormone, metalloproteinases or
metalloproteinases agonists or promoters of collagenase activity,
tissue inhibitors of matrix metalloprotenases (TIMPs) other agents
that increase collagen solubility, prostaglandins, corticosteroids,
or aminobenzoate potassium, a commercial brand being known as
Potaba.TM.. Preferred prostaglandins are prostaglandin F2 alpha and
prostaglandin E2. Also included are pharmaceutically active
sequences, peptidomimetics, or mimetics above the above-listed
molecules.
[0055] Relaxin directly and indirectly triggers a cascade of
complex biochemical and cellular effects that can cause general
morphological changes to genitalia. Prostaglandins such as
prostaglandin F2 alpha and prostaglandin E2 have similar effects.
This invention includes the mediators of these cascades as
potentiators.
[0056] Collagen is a component of the extracellular matrix (ECM),
which is a dynamic entity with many other components (e.g.,
proteoglycans, fibronectin, elastin, laminin, etc.) that functions
as a storage reservoir for cytokines and enzymes and interacts
intimately with surrounding cells to provide a structural scaffold
and an efficient biochemical communication network within tissues.
Enzymes primarily responsible for ECM remodeling are the Matrix
MetalloProteinases (MMPs), which break down ECM components, and the
Tissue Inhibitors of Matrix MetalloProteinases (TIMPs). Maintenance
of a balance of ECM synthesis and MMP/TIMP activity in tissues is
required for normal homeostasis; imbalances will generally lead to
diseases or developmental problems such as scleroderma, periodontal
disease, restenosis, osteoarthritis, liver cirrhosis,
glomerulonephritis, and ulceration.
[0057] Relaxin is a 6 kDa peptide hormone that is structurally
similar to insulin; the prohormone form consists of B-C-A chains
(20 kDa), and the C chain is proteolytically excised in `mature`
relaxin. However, unlike many other pro-hormones, pro-relaxin
retains its biological activity. The profile of conserved amino
acid sequences among various species such as pig, human, whale,
porpoise, and shark suggests that relaxin is an ancient hormone
with a unique molecular evolutionary history. The most recognized
effect of relaxin on target cells is induction of MMP expression
and inhibition of collagen synthesis.
[0058] Historically, relaxin has been classified as a "pregnancy
hormone" that acts on reproductive tissues only during pregnancy,
preparing the female for parturition by "relaxing" the pelvic
ligaments and tendons. However, recent evidence suggests that
relaxin may be classified as a "master hormone" that also induces
biochemical changes in a number of non-reproductive tissues. In
addition to up-regulating MMP expression in reproductive tissues
such as the cervix and placenta relaxin up-regulates expression of
MMP-1 and MMP-3 in lung fibroblasts, skin fibroblasts, and
fibrocartilaginous cells. Relaxin receptors are found in the brain
heart, skin, nipples, small intestine, mammary gland, blood
vessels, and testes. The bioactivity of relaxin is unique when
compared with other cytokines that affect ECM remodeling.
[0059] The potentiator or potentiators may be administered as part
of the composition, separately from the primary composition, or a
combination of both. For example, the potentiator Potaba.TM. may be
administered orally and the composition administered
intracavernosally. Optionally, the potentiater may be administered
locally into the cavernosal tissue, externally but adjacent the
cavernosal tissue by injection into the surrounding connective
tissue or the dorsal suspensory ligament of the penis, or a
combination. The potentiator may be an agent which activates the
androgen receptor, which is involved with male sexual development
and function. For example, the potentiator may be an androgen
hormone such as, but not limited to, the naturally occurring
androgens and derivatives thereof, including androsterone,
androsterone acetate, androsterone propionate, androsterone
benzoate, androstenediol, androstenediol-3-acetate,
androstenediol-17-acetate, androstenediol-3,17-diacetate,
androstenediol-17-benzoate, androstenediol-3-acetate-17-benzoate,
androstenedione, dehydroepiandrosterone (DHEA; also termed
"prasterone"), sodium dehydroepiandrosterone sulfate,
4-dihydrotestosterone (DHT; also termed "stanolone"),
17.beta.-hydroxyandrost-4-en-3-one, 5.alpha.-dihydrotestosterone,
dromostanolone, dromostanolone propionate, ethylestrenol,
nandrolone phenpropionate, nandrolone decanoate, nandrolone
furylpropionate, nandrolone cyclohexanepropionate, nandrolone
benzoate, nandrolone cyclohexanecarboxylate, oxandrolone,
stanozolol and testosterone; pharmaceutically acceptable esters of
testosterone and 4-dihydrotestosterone, typically esters formed
from the hydroxyl group present at the C-17 position, including,
but not limited to, the enanthate, propionate, cypionate,
phenylacetate, acetate, isobutyrate, buciclate, heptanoate,
decanoate, undecanoate, caprate and isocaprate esters; and
pharmaceutically acceptable derivatives of testosterone such as
methyl testosterone, testolactone, oxymetholone and
fluoxymesterone. Testosterone and testosterone esters, such as
testosterone enanthate, testosterone propionate and testosterone
cypionate, may be used. The aforementioned testosterone esters are
commercially available or may be readily prepared using techniques
known to those skilled in the art or described in the pertinent
literature.
[0060] The aforementioned androgenic agents are selected from the
group consisting of naturally occurring androgens, synthetic
androgens, and derivatives thereof, and any agent that will
stimulate the androgen receptor directly or indirectly. The active
agents may be incorporated into the present dosage units and thus
administered in the form of a pharmaceutically acceptable
derivative, analog, ester, salt, or amide, or the agents may be
modified by appending one or more appropriate functionalities to
enhance selected biological properties such as penetration through
mucosal tissue. Preparation of esters, as noted in the preceding
section, involves functionalization of hydroxyl and/or carboxyl
groups that may be present, as will be appreciated by those skilled
in the arts of pharmaceutical chemistry and drug delivery. For
example, to prepare testosterone esters, the 17-hydroxyl group of
the testosterone molecule is generally caused to react with a
suitable organic acid under esterifying conditions, such conditions
typically involving the use of a strong acid such as sulfuric acid,
hydrochloric acid, or the like, and a temperature sufficient to
allow the reaction to proceed at reflux. Esters can be reconverted
to the free acids, if desired, by using conventional hydrogenolysis
or hydrolysis procedures.
[0061] Testosterone is the principal steroid secreted by the testes
and is the primary circulating androgen found in the plasma of
males. Testosterone is converted to 4-dihydrotestosterone(DHT) by
the enzyme 5 alpha-reductase in many peripheral tissues. DHT is
thus thought to serve as the intracellular mediator for most
androgen actions (Zhou, et al., Molec. Endocrinol. 9:208-18
(1995)). Other steroidal androgens include esters of testosterone,
such as the cypionate, propionate, phenylpropionate,
cyclopentylpropionate, isocarporate, enanthate, and decanoate
esters, and other synthetic androgens such as
7-Methyl-Nortestosterone ("MENT'") and its acetate ester.
[0062] Optionally, a mechanical device such as a ring may be used
at the base of the penis to prolong retention of the composition
within the penis. The mechanical device may also be used to prolong
retention of any pharmacological agent used to potentiate the
effect of the composition, i.e., the potentiator.
[0063] The pharmaceutical composition is administered to the
patient in a pharmaceutically acceptable dosage and schedule of
administration to achieve engorgement which lasts for several
hours. The treatment regimen typically begins with the physician
determining a first dosage amount to try on a patient to determine
that subject's erectile responsiveness to the composition. The
amount of the first dosage given will be determined, among other
things, by the route of intended administration, the age of the
man, the recent history of erectile function of the man, and
pre-existing health conditions of the man.
[0064] To achieve an erectile response, one or more doses may be
administered which are typically of similar or a higher amount than
that used to treat erectile dysfunction. This should produce a full
erection. Alternatively, two or more lesser doses may be
administered to achieve a prolonged engorgement of about 40-75%
response. Optionally, a combination of similar, higher, and lesser
doses may be administered.
[0065] It is the duration of a full erection and the subsequent
period of engorgement that determines the starting dose. The penis
may be visually inspected and palpated to determine the extent of
the response to the composition.
[0066] A desirable first erectile response for the purposes of this
invention is considered to be at least a 45-100% response for a
period of at least two hours, but preferably 3-6 hours duration.
For intracavernosal injections, first dosage amounts may range from
about 0.5 mcg to about 30 mcg of prostaglandin E 1, and more
preferably from 1 mcg to 6 mcg. If a 70-100% erection is not
achieved within 20 minutes of the first test dosage amount
administered by intracavernosal injection, a second injection of
less, the same or more of the composition as the initial test
injection, depending on if there was any response with the first
test dosage. For example, if there was a 55-70% response, a
"booster" shot of a lesser amount than the first dosage amount may
be administered. If there was no response, the same or more than
the amount of the first dosage amount may be administered. Other
administrative routes may take a longer or shorter time to achieve
the initial response. The dosage is gradually increased by an
amount that is usually within 50% to 200% the previously
administered dosage until a satisfactory response is achieved.
Using these general guidelines a maximum of two injections are
administered per visit.
[0067] If an erection is not achieved with the first or second
injection, one or more additional appointment/visits on another day
may be required to establish the dose.
[0068] Once the correct response is achieved, it will be followed
by one or more confirmatory doses on subsequent visits. Once a
starting dosage amount of a single or a sequence of two or more
injections is established that provides a response of suitable
duration, the dosage may be titrated, for example, to provide the
subject with an initial 70%-100% engorgement followed by a further
period of reduced engorgement of at least 40% for at least 3-6
hours. The firmness of the penis generally decreases over this
period, but will be at least 40% engorged for at least 3 and
preferably up to 6 hours and less than 75% engorged for the
majority of the time.
[0069] Depending on the subject's response to the treatment, higher
dosages may be used as determined by the physician. However, it
should be noted that higher dosages may increase the risk of a very
firm erection that may cause ischemia. If the veno-occlusive
mechanism closes to an extent that it reduces the inflow of fresh
oxygenated blood for a sufficient period to cause pain and tissue
damage it can cause a medical condition called a priapism. The risk
of priapism can be reduced by using smaller multiple doses. The
subject's condition should be monitored and the dosage adjusted to
ensure that the patient experiences a prolonged period of
engorgement, rather than a prolonged full erection, which may lead
to priapism and associated health complications.
[0070] Subjects should have careful instruction in the signs and
symptoms of priapism, and have access to 24 hour emergency medical
treatment to allow prompt treatment and eliminate any risks of
ischemia to the penis.
[0071] A physician should closely monitor the subject's response to
medication, to determine signs of edema, tenderness, and other
early signs that the dose is excessive and needs adjusting.
[0072] If lumps or unexpected thickening of the penis occurs during
treatment, the patient may have to stop or suspend treatment for a
period of time. Once the appropriate dosage for a given patient has
been determined, the treatment may be self-administered under the
close supervision of a properly trained physician or health
professional.
[0073] The treatment is repeated over a period of time sufficient
to cause a permanent increase in the length and girth of the
patient's penis. The treatment may comprise administration with the
composition alone, or in conjunction with potentiator. For example,
the treatment may be repeated daily or at least two times a week
over a period of several weeks or at least one month. More
preferably, the treatment may be repeated at least 3-4 times a week
for a period of at least 3 months. For treatment periods of between
12 and 18 months, an increase of at least 5% may be achieved in the
length and girth of an erect penis, and increases of at least 30%
or even at least 50% in the length and girth of an erect penis may
be achieved. Active treatment for more extended periods, e.g. 24
months, may yield greater results.
[0074] The subject may continue with normal sexual activities
during the course of treatment. In fact, due to the prolonged
elevation in penile blood flow, patients using this treatment will
experience a very significant increase in erectile function. During
treatment, patients will have dramatic improvements in the
frequency, strength and duration of their own naturally stimulated
erections. Men using this treatment will require much lower levels
of sexual arousal and stimulation to produce and maintain their own
naturally induced erections.
[0075] The pharmaceutical composition and/or potentiator may be
administered using a variety of different methods known to those of
skill in the art, including administration by direct manual
injection to the cavernosal tissue by needle, auto-injector, slow
sustained injection pumps, high pressure injection devices,
urethral suppository, implantable sustained release drug or device,
microinfusion pump or systemically by oral administration,
parenteral administration such as subcutaneously or intra
muscularly, intravenous administration by needle, auto-injector,
slow sustained injection pump, high pressure injection device or
implantable sustained release drug device, or topical
administration, such as through the use of creams, lotions or
patches with suitable additives for transdermal delivery. Most
conveniently, the treatment with the vasodilators is administered
by intracavernosal injection. Optionally, the pharmaceutical
composition and/or potentiator may be administered by a deep
injection that is well below the dermis and subcutaneous tissues
which is administered into the dense connective tissue that
surround the erectile tissue of the penis. This may be in the form
of a depot oil. The pharmaceutical composition and/or potentiator
may also be administered to the dorsal suspensory ligand of the
penis.
[0076] For example, relaxin may be administered by intracavernosal
injection at a dosage ranging from 0.01 to 50 mcg/kg body
weight/day, more preferably at a dosage ranging from 0.02 to 10
mcg/kg body weight/day, or topically at a dosage ranging from 5 to
1000 mcg/kg body weight/day, more preferably at a dosage ranging of
25 to 400 mcg/kg body weight/day, or by injection into the dense
connective tissue surrounding the erectile tissue of the penis at a
dose ranging from 0.01 to 50 mcg/kg body weight/day, more
preferably at a dosage ranging from 0.02 to 10 mcg/kg body
weight/day, and more preferably still, at a dosage ranging from
0.02 to 1 mcg/kg body weight/day.
[0077] Kits of the composition are part of this invention. The kit
may include a pharmaceutical composition of the invention and
written instructions as to how and when to administer the
composition in order to achieve an enlarged penis by repeated
treatments, over a period of weeks or months. Optionally, the kit
may include a pharmaceutical composition of the invention with
written and possibly videotaped/cd rom (compact disc) video
instructional information and/or be accompanied by oral
instructions from a health professional as to how and when to
administer the composition in order to achieve an enlarged penis.
Preferably, the patient does not self-administer the composition
without the supervision of a health professional. Optionally, the
kit may also include an agent which will potentiate the effects of
the pharmaceutical compositions of this invention. In this case,
written, video format instructions or oral instructions will be
included as to how to use the agent to potentiate the effect of the
composition.
[0078] Without binding itself to any particular theory, applicant
believes that this invention works by inducing biological creep
(induction of cellular processes for tissue remodelling and
cellular growth) and, to a lesser degree, biomechanical creep
(mechanical microscopic tearing and viscoelastic stretching of the
connective tissue). The pharmaceutical composition of the present
invention induces prolonged penile engorgement, which results in a
significant increase in the arterial blood flow through the penis.
This increase in blood flow can safely activate the veno-occlusive
mechanism that then expands and pressurizes the erectile tissue for
several hours, while providing a constant flow of fresh oxygenated
blood flow into the penis. This avoids the complications and health
risks caused by priapism and ischemia and safely applies prolonged,
continuous stimulation of the cellular processes necessary to
induce maximal rates of biological and mechanical creep to enlarge
the penis with minimal distortions in the shape or architecture of
the penis. The potentiators may be co-comittently administered to
accelerate the rate of the cellular processes that remodel the
tissues of the penis in the growth/enlargement process.
[0079] In order that the invention may be better understood,
preferred embodiments will now be described in the following
examples.
EXAMPLE 1
[0080] A male patient, age 41, was treated with intracavernosal
injections of a vasodilator, prostaglandin E1, on a regular basis
(approximately four to five times per week) over an 18 month
treatment period. A sufficient quantity was administered to
maintain a prolonged engorgement of an erectile response between
40-75% over a period of several hours, generally 3 to 6 hours. The
quantity of medication was adjusted from time to time in accordance
with the patient's response, which was monitored at least
weekly.
[0081] The size of the patient's fully erect penis increased from
5.8 inches to 8.6 inches in length (about an 48% increase) and 3.7
inches to 5.8 inches in girth (about an 56% increase) over the
18-month treatment period. Following the discontinuation of this
treatment, the erect penis length remained stable for two years at
over 81/2 inches. Treatment was re-institued combining
intracavernosal injections 3-4 times per week of a mixture of
testosterone (0.5 mg) and vasodilators with low dose oral Potaba
(500-1000 mg) 3-4 times per day. After a short treatment period of
21/2 months, the patient's erect penis was over 9 inches in length,
which means he has gained an additional 0.4-0.5 inches in length
(about an 6% increase). The total increase in length was therefore
about 3.2 inches (about an 55% increase) in length.
EXAMPLE 2
[0082] A male patient, age 30, was treated with intracavernosal
injections of the vasodilator on a regular basis (approximately
four to five times per week) over a 6-month treatment period. A
sufficient quantity was administered to maintain a prolonged
engorgement over a period of about 3 to 6 hours. The quantity of
medication was adjusted in accordance with the patient's response,
The potentiator potaba (aminobenzoate) (1000 mg/4 times per day)
was administered orally to the patient for the last 60 days of
treatment.
[0083] The patient's erect penis increased from 5.6 inches to 7.7
inches (about an 38% increase) in length and 3.2 inches to 5.3
inches (about an 65% increase) in girth over the 6-month treatment
period.
EXAMPLE 3
[0084] A male patient, age 52, was treated with separate
intracavernosal injections of vasodilators, Papavarine,
phentolamine and prostaglandin E1, on a regular basis, selected
from treatments of 0 to 4 times per week, over a 7 month treatment
period along with daily subcutaneous injections of a prostaglandin
F analogue. A sufficient quantity of vasodilator was administered
to maintain a prolonged engorgement of an erectile response greater
than 70% for 3.5-5 hours duration. The quantity of medication was
adjusted from time to time in accordance with the patient's
response, which was monitored initially weekly then monthly once
the patient had mastered the IC technique and the responses were
consistently of the same duration.
[0085] The size of the patient's fully erect penis increased from
5.0 inches to 6.3 inches in length, i.e. about a 26% increase, over
the 7-month treatment period. Following the discontinuation of this
treatment, the erect penis length remained stable.
EXAMPLE 4
[0086] A male patient, age 34, was treated with intracavernosal
injections of a triple mix of the vasodilators Atropine,
Chlorpromazine and Papavarine on a regular basis (approximately two
to five times per week) over a 4-month treatment period. A
sufficient quantity was administered to maintain a prolonged
engorgement of 60-90% over a period of about 3 to 4.5 hours. The
quantity of medication was adjusted in accordance with the
patient's response. The potentiator, Potaba.TM.--potassium
aminobenzoate (1000 mg/3-4 times per day) was administered orally
starting 1 month before starting the IC injections of the
vasodilators Atropine, Chlorpromazine and Papavarine.
[0087] After 5 months of treatment the patient's erect penis
increased from 6.0 inches to 7.1 inches (about an 18% increase) in
length.
EXAMPLE 5
[0088] A male patient, age 44, was treated with intracavernosal
injections of a quadruple mix of the vasodilators prostaglandin E1,
Atropine, Chlorpromazine and Papavarine on a regular basis
(approximately two to four times per week) over a 4-month treatment
period. A sufficient quantity was administered to maintain a
prolonged engorgement over a period of about 3 to 5 hours. The
quantity of medication was adjusted in accordance with the
patient's response. The potentiator dihydrotestosterone 5% ointment
was administered orally starting two weeks before starting the IC
injections of the vasodilators Atropine, Chlorpromazine and
Papavarine and prostaglandin.
[0089] After 4 months of treatment the patient's erect penis
increased from 5.2 inches to 6.5 inches (about a 25% increase) in
length.
EXAMPLE 6
[0090] A male patient, age 44, was treated with intracavernosal
injections of the vasodilator phentolamine on a regular basis
(approximately two to four times per week) over a 4-month treatment
period. Phentolamine was frequently combined with indirect
vasodilating effects of oral Viagra to produce and maintain a
prolonged engorgement of 60-90% over a period of about 3 to 5
hours. The quantity of medication was adjusted in accordance with
the patient's response. The potentiator dihydrotestosterone gel was
administered orally starting two weeks before starting the IC
injections of the vasodilators Atropine, Chlorpromazine and
Papavarine and prostaglandin.
[0091] After 4 months of treatment the patient's erect penis
increased from 5.2 inches to 6.5 inches (about a 25% increase) in
length.
EXAMPLE 7
[0092] A male patient, age 72, was treated with intracavernosal
injections of the quadruple mix of the vasodilators prostaglandin
E1, Atropine, Chlorpromazine and Papavarine on a regular basis
(approximately two to four times per week) over a 3-month
treatment. The indirect vasodilating effects of oral Cialis and
Levitra were sometimes added to the quadruple mix of the
vasodilators prostaglandin E1, Atropine, Chlorpromazine and
Papavarine to produce and maintain a prolonged engorgement of
60-85% over a period of about 2.5 to 3 hours. The quantity of
medication was adjusted in accordance with the patient's response.
The potentiators Potaba 1000 mg 4.times./day orally and
prostaglandin F topically were also used with the vasodilators.
After 3 months of treatment the patient's erect penis increased
from 6.5 inches to 7.1 inches (about a 9% increase) in length.
EXAMPLE 8
[0093] A male patient, age 47, was treated with intracavernosal
injections of a triple mix of the vasodilators Atropine,
Chlorpromazine and Papavarine on a regular basis (approximately
three to four times per week) over a 6-month treatment period. A
sufficient quantity was administered to maintain a prolonged
engorgement of an erectile response between 60-95% over a period of
several hours, generally 3 to 4.5 hours. The quantity of medication
was adjusted from time to time in accordance with the patient's
response, which was monitored initially weekly. After 2 months of
treatment subcutaneous injections of testosterone 14-20 mg into the
penis were added as an accelerator.
[0094] The size of the patient's fully erect penis increased from
5.2 inches to 6.0 inches in length (about a 15% increase) over the
6 month treatment period.
EXAMPLE 9
[0095] A male patient, age 52, was treated with intracavernosal
injections of the quadruple mix of the vasodilators prostaglandin
E1, Atropine, Phentolamine and Papavarine on a regular basis (using
IC medications approximately two to four days per week) over a
3-month treatment. Since the maximum duration of the engorgement of
the erection from a single dose was only 45 to 80 minutes, the
patient used two to three separate IC injects spaced through out
the treatment days to achieve a total i.e. cumulative daily
duration of 3 to 4 hours. The indirect vasodilating effects of oral
Cialis and Levitra were sometimes added to the quadruple mix of the
vasodilators prostaglandin E1, Atropine, Chlorpromazine and
phentolamine to produce and maintain a prolonged engorgement of
60-85% over a period of about 3 to 4 hours.
[0096] The quantity of medication was adjusted in accordance with
the patient's response. The potentiator Potaba 1000mg 4.times./day
orally was used with the vasodilator. After 4 months of treatment
the patient's erect penis increased from 5.4 inches to 6.1 inches
(about a 13% increase) in length and 4.4 to 5.1 inches in
circumference (about a 16% increase in circumference).
EXAMPLE 10
[0097] A male patient, age 27, was treated with intracavernosal
injections of a prostaglandin E1 on a regular basis (approximately
two to five times per week) over a 3-month treatment period. Due to
a sensitivity to Prostraglandin E1 causing aching and pain at
higher doses, the maximum tolerated dose which produced a
comfortable erection was only lasting 90 to 120 minutes. The
patient used two separate IC injects spaced throughout the
treatment days to achieve a total daily cumulative engorgement
duration of 3 to 4 hours. The quantity of medication was adjusted
in accordance with the patient's response. The 15 mg of the
potentiator Dihydrotestosterone was injected subcutaenously into
the penis daily throughout the treatment period. After 3 months of
treatment the patient's erect penis increased from 6.3 inches to
7.1 inches (about an 13% increase) in length.
[0098] Although various examples of combined elements of the
invention have been described, it will also be understood that
these are not intended to be exhaustive and features of one
embodiment may be combined with those of another, and such other
combinations are contemplated to be within the scope of the
invention disclosed herein.
[0099] All publications and other documents mentioned herein are
hereby incorporated by reference into this specification.
[0100] While preferred embodiments of the invention have been
illustrated and described, it will be appreciated that various
changes and modifications can be made therein without departing
from the spirit and scope of the invention as defined by the
following claims.
* * * * *