MXPA00000067A - Medicine containing yohimbine and arginine for treating erectile dysfunction - Google Patents
Medicine containing yohimbine and arginine for treating erectile dysfunctionInfo
- Publication number
- MXPA00000067A MXPA00000067A MXPA/A/2000/000067A MXPA00000067A MXPA00000067A MX PA00000067 A MXPA00000067 A MX PA00000067A MX PA00000067 A MXPA00000067 A MX PA00000067A MX PA00000067 A MXPA00000067 A MX PA00000067A
- Authority
- MX
- Mexico
- Prior art keywords
- arginine
- yohimbine
- dose
- drug
- administration
- Prior art date
Links
- BLGXFZZNTVWLAY-CCZXDCJGSA-N Yohimbine Natural products C1=CC=C2C(CCN3C[C@@H]4CC[C@@H](O)[C@H]([C@H]4C[C@H]33)C(=O)OC)=C3NC2=C1 BLGXFZZNTVWLAY-CCZXDCJGSA-N 0.000 title claims abstract description 25
- BLGXFZZNTVWLAY-UHFFFAOYSA-N beta-Yohimbin Natural products C1=CC=C2C(CCN3CC4CCC(O)C(C4CC33)C(=O)OC)=C3NC2=C1 BLGXFZZNTVWLAY-UHFFFAOYSA-N 0.000 title claims abstract description 25
- BLGXFZZNTVWLAY-SCYLSFHTSA-N yohimbine Chemical compound C1=CC=C2C(CCN3C[C@@H]4CC[C@H](O)[C@@H]([C@H]4C[C@H]33)C(=O)OC)=C3NC2=C1 BLGXFZZNTVWLAY-SCYLSFHTSA-N 0.000 title claims abstract description 25
- 229960000317 yohimbine Drugs 0.000 title claims abstract description 25
- AADVZSXPNRLYLV-UHFFFAOYSA-N yohimbine carboxylic acid Natural products C1=CC=C2C(CCN3CC4CCC(C(C4CC33)C(O)=O)O)=C3NC2=C1 AADVZSXPNRLYLV-UHFFFAOYSA-N 0.000 title claims abstract description 25
- 239000004475 Arginine Substances 0.000 title claims abstract description 23
- ODKSFYDXXFIFQN-UHFFFAOYSA-N arginine Natural products OC(=O)C(N)CCCNC(N)=N ODKSFYDXXFIFQN-UHFFFAOYSA-N 0.000 title claims abstract description 23
- 239000003814 drug Substances 0.000 title claims abstract description 20
- 201000001881 impotence Diseases 0.000 title claims abstract description 13
- 208000010228 Erectile Dysfunction Diseases 0.000 title claims abstract description 11
- ODKSFYDXXFIFQN-BYPYZUCNSA-P L-argininium(2+) Chemical compound NC(=[NH2+])NCCC[C@H]([NH3+])C(O)=O ODKSFYDXXFIFQN-BYPYZUCNSA-P 0.000 title claims abstract description 10
- 229940079593 drug Drugs 0.000 title claims description 19
- 239000004480 active ingredient Substances 0.000 claims abstract description 9
- 238000011282 treatment Methods 0.000 claims description 12
- 239000012458 free base Substances 0.000 claims description 10
- 150000003839 salts Chemical class 0.000 claims description 6
- 239000002775 capsule Substances 0.000 claims description 5
- 239000000243 solution Substances 0.000 claims description 4
- 239000008187 granular material Substances 0.000 claims description 2
- 239000002674 ointment Substances 0.000 claims description 2
- 239000007921 spray Substances 0.000 claims description 2
- 239000000829 suppository Substances 0.000 claims description 2
- 239000003826 tablet Substances 0.000 claims description 2
- -1 patches Substances 0.000 claims 1
- 230000002195 synergetic effect Effects 0.000 abstract description 2
- 235000009697 arginine Nutrition 0.000 description 14
- 239000008280 blood Substances 0.000 description 6
- 210000004369 blood Anatomy 0.000 description 6
- 239000000902 placebo Substances 0.000 description 6
- 229940068196 placebo Drugs 0.000 description 6
- UCTWMZQNUQWSLP-UHFFFAOYSA-N adrenaline Chemical compound CNCC(O)C1=CC=C(O)C(O)=C1 UCTWMZQNUQWSLP-UHFFFAOYSA-N 0.000 description 4
- 210000005226 corpus cavernosum Anatomy 0.000 description 4
- 210000003899 penis Anatomy 0.000 description 4
- 206010052004 Organic erectile dysfunction Diseases 0.000 description 3
- 230000000694 effects Effects 0.000 description 3
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 2
- ODKSFYDXXFIFQN-BYPYZUCNSA-N L-arginine Chemical compound OC(=O)[C@@H](N)CCCN=C(N)N ODKSFYDXXFIFQN-BYPYZUCNSA-N 0.000 description 2
- 229930064664 L-arginine Natural products 0.000 description 2
- 235000014852 L-arginine Nutrition 0.000 description 2
- 230000001800 adrenalinergic effect Effects 0.000 description 2
- 210000001367 artery Anatomy 0.000 description 2
- 230000017531 blood circulation Effects 0.000 description 2
- 230000001856 erectile effect Effects 0.000 description 2
- 238000000034 method Methods 0.000 description 2
- 230000001107 psychogenic effect Effects 0.000 description 2
- 239000000126 substance Substances 0.000 description 2
- 210000003462 vein Anatomy 0.000 description 2
- 208000019901 Anxiety disease Diseases 0.000 description 1
- 240000002900 Arthrospira platensis Species 0.000 description 1
- 235000016425 Arthrospira platensis Nutrition 0.000 description 1
- 240000007436 Cananga odorata Species 0.000 description 1
- 235000007571 Cananga odorata Nutrition 0.000 description 1
- 244000223760 Cinnamomum zeylanicum Species 0.000 description 1
- KRKNYBCHXYNGOX-UHFFFAOYSA-K Citrate Chemical compound [O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O KRKNYBCHXYNGOX-UHFFFAOYSA-K 0.000 description 1
- 244000228088 Cola acuminata Species 0.000 description 1
- 235000010205 Cola acuminata Nutrition 0.000 description 1
- 241000682653 Corynanthe Species 0.000 description 1
- 241000196324 Embryophyta Species 0.000 description 1
- CKLJMWTZIZZHCS-REOHCLBHSA-N L-aspartic acid Chemical compound OC(=O)[C@@H](N)CC(O)=O CKLJMWTZIZZHCS-REOHCLBHSA-N 0.000 description 1
- WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 description 1
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 1
- 208000019695 Migraine disease Diseases 0.000 description 1
- 206010029216 Nervousness Diseases 0.000 description 1
- 244000131316 Panax pseudoginseng Species 0.000 description 1
- 235000005035 Panax pseudoginseng ssp. pseudoginseng Nutrition 0.000 description 1
- 235000003140 Panax quinquefolius Nutrition 0.000 description 1
- 235000008690 Pausinystalia yohimbe Nutrition 0.000 description 1
- 208000013738 Sleep Initiation and Maintenance disease Diseases 0.000 description 1
- 244000273928 Zingiber officinale Species 0.000 description 1
- 235000006886 Zingiber officinale Nutrition 0.000 description 1
- 102000030484 alpha-2 Adrenergic Receptor Human genes 0.000 description 1
- 108020004101 alpha-2 Adrenergic Receptor Proteins 0.000 description 1
- 230000003042 antagnostic effect Effects 0.000 description 1
- 230000036506 anxiety Effects 0.000 description 1
- 229940009098 aspartate Drugs 0.000 description 1
- 230000036772 blood pressure Effects 0.000 description 1
- 230000001684 chronic effect Effects 0.000 description 1
- 235000017803 cinnamon Nutrition 0.000 description 1
- 150000001875 compounds Chemical class 0.000 description 1
- 230000007423 decrease Effects 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 208000035475 disorder Diseases 0.000 description 1
- 208000002173 dizziness Diseases 0.000 description 1
- 230000004064 dysfunction Effects 0.000 description 1
- 230000001667 episodic effect Effects 0.000 description 1
- 230000009986 erectile function Effects 0.000 description 1
- 210000005225 erectile tissue Anatomy 0.000 description 1
- 238000011156 evaluation Methods 0.000 description 1
- 239000007903 gelatin capsule Substances 0.000 description 1
- 235000008397 ginger Nutrition 0.000 description 1
- 235000008434 ginseng Nutrition 0.000 description 1
- 229930195712 glutamate Natural products 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 206010022437 insomnia Diseases 0.000 description 1
- 239000008101 lactose Substances 0.000 description 1
- 210000003205 muscle Anatomy 0.000 description 1
- 210000005036 nerve Anatomy 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 230000008092 positive effect Effects 0.000 description 1
- 230000003518 presynaptic effect Effects 0.000 description 1
- 210000000664 rectum Anatomy 0.000 description 1
- 230000002040 relaxant effect Effects 0.000 description 1
- 230000000284 resting effect Effects 0.000 description 1
- 229940082787 spirulina Drugs 0.000 description 1
- 210000001519 tissue Anatomy 0.000 description 1
- 230000002227 vasoactive effect Effects 0.000 description 1
Abstract
The invention concerns the use in combination of yohimbine and arginine as active ingredients for preparing a medicine for treating erectile dysfunction. The combination has a marked synergistic effect.
Description
DRUG FOR THE TREATMENT OF ERECTILE DYSFUNCTIONS
DESCRIPTION OF THE INVENTION The invention relates to the use of yohimbine and arginine, in combination, in the preparation of a drug that is intended for the treatment of erectile dysfunction. The erection process is known as outlined schematically below. The erectile tissue of the penis, known as the corpus cavernosum, is a spongy tissue capable of being filled with blood. When at rest, the arteries of the penis are subject to adrenergic tone, which keeps them contracted, so that there is no blood flow to fill the corpus cavernosum. With a stimulus, the erectile nerves inhibit the adrenergic tone, the arteries of the penis dilate, and the corpus cavernosum is filled with blood, it grows, and the increased internal pressure causes it to become rigid. As it grows, it compresses the veins of the penis to prevent drainage of the blood it contains, which ensures that stiffness is maintained. After ejaculation, adrenaline is released locally again, and the blood flow of blood is immediately reduced, the pressure inside the cavernous body decreases, and the accumulated blood can be drained through the veins that are not already compressed, which it results in the loss of rigidity and returns to the resting state. It is known that a very significant proportion of men suffer from permanent or temporary erectile dysfunctions. These disorders may have an organic origin, in which case specific treatments adapted to each cause are required. However, a majority of non-organic erectile dysfunctions are observed, often of psychogenic origin. For these latter cases, several treatments are available. The cavernous intrabody injection of vasoactive substances is apt to give good results, but is not easily accepted by a significant proportion of patients. Oral treatments are generally better accepted. For this purpose, different products have been proposed which are often derived from plants: ginseng, ginger, yohimbine, cola nut, spirulina, ilang-ilang, chirivia, cinnamon, etc. Yohimbine is a substance extracted from the bark of Corynan the yohimbe. It has antagonistic properties with respect to the presynaptic alpha-2-adrenergic receptors. In other words, they inhibit the effects of adrenaline, and thus promote the supply of the corpus cavernosum with arterial blood. It has been proposed as a treatment for impotence of psychogenic origin. Certain studies published on this subject cite improvements in approximately 35 to 45% of cases treated with yohimbine, but these results have been disputed. In addition, several side effects have been observed, such as dizziness, anxiety, nervousness, migraines, insomnia, and elevated blood pressure, although for relatively high doses; see, for example, The Medical Letter, French Edition, Vol. 17, No. 2, 5-6 (ML USA No. 938), 1995. It is also proposed to administer L-arginine. The administration of arginine would have the effect of relaxing the arterial muscles of the cavernous body, relaxation which is necessary to obtain an erection. The administration of 2800 mg per day of L-arginine would have a positive effect on erectile dysfunction in approximately 40% of cases; see A. W. Zorgniotti and E. F. Lizza, Int. J. Impotence Res., 6, 33-36 (1994). It has now been discovered that in this domain, the combination of yohimbine and arginine has interesting properties. Indeed, tests have shown that the combination of arginine and yohimbine, due to a synergistic effect, provides positive results in the treatment of non-organic erectile dysfunctions, mainly using weaker doses of yohimbine than those previously used. The combination of yohimbine and arginine also allows a reduction in the dose of arginine used. In many cases, this combination seems to act quickly, and in this way, it can be used for the treatment of temporary erectile dysfunctions. Thus, the object of the invention is to use yohimbine and arginine in combination as the active ingredients in the preparation of a drug that is intended for the treatment of non-organic erectile dysfunctions. Yohimbine and arginine can be used in the form of a free base or in the form of pharmacologically acceptable salts. The active ingredients in the drug according to the invention can be presented separately, each in an appropriate pharmaceutical form, or combined in the same package. To facilitate the simultaneous administration of the active ingredients, however, it is generally preferred to prepare the drug according to the invention in a pharmaceutical form comprising both yohimbine and arginine.
The drug according to the invention can be prepared in a pharmaceutical form that allows the administration of a sufficient dose of yohimbine, notably a dose of 2 to 8 mg, particularly 2 to 6 mg per day, administered in one or two doses. This dose is calculated by the weight of yohimbine in free base form. The drug according to the invention is prepared in a pharmaceutical form that allows the administration of a sufficient dose of arginine, for example, a dose of 1 to 4 g per day, particularly 1 to 2 g per day, administered one or two times, so the dose is calculated by the weight of arginine as a free base. The drug according to the invention can be administered orally, sublingually, nasally, rectally, or cutaneously. For this purpose, it can be presented in any form that allows administration by mouth (particularly in the form of capsules, drinkable solutions, granules or tablets), by the nose (solutions to be administered in the form of drops or sprays), or by the rectum (suppositories) or through the skin (ointments or patches). These pharmaceutical forms are prepared in the customary manner and can comprise suitable excipients and conventional vehicles.
Yohimbine can be used in the form of a free base or in the form of a salt such as a hydrochloride. Arginine can be used in the form of a free base or in the form of an acceptable salt in pharmacology, such as a hydrochloride, glutamate, aspartate or citrate. The duration of treatment may vary, for example, from 2 to 4 weeks or more. It can also be considered episodic use. The following examples illustrate the invention.
EXAMPLE 1 A capsule was prepared consisting of a gelatin capsule comprising: - Arginine: 0.5 g. Yohimbine: 1 mg.
EXAMPLE 2 Double blind randomized trials were conducted with 42 adults, married men, aged 28 to 64, suffering from erectile dysfunction with no detectable organic cause. The treatment consisted of administering any of (21 cases) 4 capsules as described in Example 1 above (2 in the morning and 2 at night), or analogously (21 cases) a placebo (4 capsules of identical appearance but containing only 0.5 g of lactose). The people participating in the trial as well as the people who supplied the test compounds did not know which of them received or supplied the combination of yohimbine + arginine or placebo. 2 weeks later, participants in the trial were questioned to see if they had noticed an improvement in erectile function. An evaluation of the results allows to draw the following conclusions: -between the subjects suffering from temporary erectile dysfunction (22 cases), 12 received the placebo, 7 cases reported improvements with the combination being tested and 4 cases with the placebo; -between subjects suffering from chronic erectile dysfunction (20 cases), 9 received placebo, 4 cases reported improvements with the combination being tested and 1 case with placebo.
It is noted that in relation to this date, the best method known to the applicant to carry out the aforementioned invention, is that which is clear from the present description of the invention.
Claims (11)
1. The use, in combination, of yohimbine and arginine as active ingredients in the preparation of a drug that is intended for the treatment of erectile dysfunction.
2. The use according to claim 1, wherein yohimbine and / or arginine are used in the form of a free base or in the form of a salt.
3. The use according to claim 1, wherein the drug is prepared in a pharmaceutical form that allows simultaneous administration of the active ingredients.
4. The use according to any of the preceding claims characterized in that the drug is prepared in a pharmaceutical form that allows the administration of a dose of 2 to 8 mg of yohimbine, administered in one or two doses, so the dose is calculated by the weight of yohimbine in free base form.
5. The use according to any of the preceding claims characterized in that the Me. The drug is prepared in a pharmaceutical form that allows the administration of a dose of 1 to 4 g, particularly 1 to 2 g, of arginine, administered in one or two doses, whereby the dose is calculated by the weight of the arginine. in the form of a free base.
6. The drug is intended to treat erectile dysfunctions, characterized in that it contains arginine in free form or salt and yohimbine in free or salt form as active ingredients.
7. The drug according to the preceding claim, characterized in that it contains the active ingredients separately, in one and the same package.
8. The drug according to claim 6, characterized in that it is presented in a single pharmaceutical form containing the two active ingredients.
The drug according to any of claims 6 to 8, characterized in that it is presented in a pharmaceutical form that allows the administration of a dose of 2 to 8 mg, particularly 2 to 6 mg of yohimbine administered in one or two doses , so the dose is calculated by the weight of yohimbine in free base form.
10. The drug according to any of claims 6 to 9, characterized in that it is presented in a pharmaceutical form that allows the administration of a dose of 1 to 4 g, particularly 1 to 2 g, of arginine, administered in one or two doses , so the dose is calculated by the weight of arginine in free base form.
11. The drug according to any of claims 6 to 10, characterized in that it is presented in the form of capsules, drinkable solutions, granules, tablets, ointments, patches, suppositories or nasal solutions to be administered in the form of drops or sprays.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| FR97/08504 | 1997-07-04 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| MXPA00000067A true MXPA00000067A (en) | 2001-11-21 |
Family
ID=
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AU710111B2 (en) | Methods and formulations for modulating the human sexual response | |
| Waldhauser et al. | Efficiency and side effects of prostaglandin El in the treatment of erectile dysfunction | |
| Parkes et al. | Bromocriptine in Parkinsonism: long-term treatment, dose response, and comparison with levodopa. | |
| AU743825B2 (en) | Medicine containing yohimbine and arginine for treating erectile dysfunction | |
| EP1210076A2 (en) | Drug therapy of the restless leg syndrome | |
| JPH04501707A (en) | Composition for the treatment of erectile dysfunction | |
| Segraws | Antidepressant-induced orgasm disorder | |
| Sorbera et al. | IC-351 | |
| McMahon et al. | Pharmacological treatment of premature ejaculation | |
| Aung et al. | Alternative therapies for male and female sexual dysfunction | |
| JP2003534286A (en) | Use of proanthocyanidin as an active ingredient of a stimulant and L-arginine or a salt thereof as a source of nitric oxide for improving erectile dysfunction symptoms | |
| AU2002363874B2 (en) | Use of desoxypeganine for treating clinical depression | |
| RU2006139819A (en) | APPLICATION OF SYMETICON FOR PATIENTS POSITIONED FOR CONSTIPATION | |
| MXPA00000067A (en) | Medicine containing yohimbine and arginine for treating erectile dysfunction | |
| US20010003120A1 (en) | Method for treating erectile dysfunction | |
| Sommer et al. | A conservative treatment option of curing venous leakage in impotent men | |
| WO2000023056A2 (en) | The use of dopaminergic agents in the management of sexual dysfunction | |
| US20030125390A1 (en) | Method of treatment and prophylaxis | |
| JP2002531408A (en) | Production and use of a combination of a purine and a nitric oxide donor for the prevention or treatment of sexual dysfunction | |
| Aung et al. | Alternative therapies for sexual dysfunction | |
| KR20040034328A (en) | The Product for Improving the Impotence with Mixtures of Red Ginseng and Natural Substances, and Including Food Theirof | |
| HK1029924A (en) | Medicine containing yohimbine and arginine for treating erectile dysfunction | |
| FR3012039A1 (en) | MEDICINE OR DIETETIC PRODUCT AND USE THEREOF FOR PREVENTING OR TREATING SEXUAL DYSFUNCTIONS IN MAN AND WOMEN | |
| CN120813353A (en) | Compounds for the treatment of erectile dysfunction | |
| IT201600119871A1 (en) | USE OF THE ASSOCIATION OF INHIBITORS OF PHOSPHODIESTERASE 5 WITH PROSTAGLANDIN E1 FOR THE TREATMENT OF THE ERECTILE DYSFUNCTION |