Outline

• Overview
• Introduction
• Testosterone Effect on Aging Men
• DHT and Sex Drive
• TestoCreme® and Viagra®
• References

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I. Overview

In comparing Viagra® and TestoCreme® , it is important to note they make a perfect team. Testosterone (T) has been used topically for the treatment of low testosterone levels for decades. However, it is important to distinguish that the timulation of libido by testosterone is essential for drug such as Sildenafil® or Viagra® to exert its erection enhancement effect. There are many cases in which both compounds used simultaneously will provide a synergistic effect. What follows is a quick review of the literature to support the hypothesis that both Viagra® and TestoCreme® used together have a positive action in improving the quality of function and enjoyment for men during intercourse

II. Introduction

Erectile Dysfunction (ED) affects about 30 million men in the United States. The available treatments for ED have undergone a steady evolution in the past 25 years toward less invasive modalities. These treatments have developed in parallel with the understanding of the pathophysiologic mechanisms at work in ED. The recent introduction of the oral agent Viagra® (V) or Sildenafil®, a type-5 phosphodiesterase inhibitor, perhaps represents the culmination of this metamorphosis. The ease of administration of this agent is appealing to a broad sector of men with ED. Oral Sildenafil® therapy provides results comparable to those of other available ED treatment modalities. (Ref. 1)

It is likely that the availability of Sildenafil® has greatly increased the number of men who receive treatment for ED. Other available options that predate Sildenafil include vacuum erection devices (VEDs), intracavernosal injection therapy (ICIT), and intraurethral prostaglandin suppository (IPS). Many men already using these therapeutic regimens may wish to try Sildenafil® as an alternative therapy; however, the relative efficacy of Sildenafil® compared to these treatments remains to be defined. However the combination of Viagra® and testosterone is extremely effective.

III. Testosterone Effect on Aging Men

Use of Viagra® can augment the action of lower testosterone levels. Aging men develop a significant loss of muscle strength that occurs in conjunction with a decline in serum testosterone concentrations. Increasing testosterone concentrations in elderly men increases skeletal muscle protein synthesis and strength. This increase may be mediated by stimulation of the intramuscular IGF-I system. (Ref. 2)

There is considerable interest in the relationship between testosterone and sexual behavior in men, but the few available data bearing on this issue are inconclusive. Testosterone concentration did not correlate with the sexual activity and interest variables. These results provide evidence that differences among men in circulating testosterone concentration within the normal range do not account for differences in sexual activity and interest. It is also unlikely that variations in sexual activity account for differences in testosterone concentration. (Ref. 3) It appears that a factor more sensitive than total testosterone levels can be used as a marker for ED.

IV. DHT and Sex Drive

Dihydrotestosterone is capable of maintaining sex functions in hypogonadal men. There is no evidence that androgen administration in excess of the individually determined critical levels further enhances sex functions. In view of the rapidly declining blood levels of androgens with the available parenteral testosterone ester preparations, the results suggest that hypogonadal patients may benefit from a more frequent administration of these preparations. (Ref. 4) However, if it is the conversion of testosterone to DHT which stimulates libido, then any increase in activity of the enzyme which converts testosterone to higher levels of DHT will stimulate sexual desire.

Androgens are essential for the expression of normal libido in the male, but their role in the maintenance of the erectile response in humans is controversial. In the rat castration induces:

1. loss of penile reflexes
2. considerable reduction in the erectile response to electric field stimulation (EFS) of the cavernosal nerve.

Both affects can both be reversed by testosterone replacement. Castration reduced the EFS-induced erectile response by 50% in comparison with intact rats and testosterone restored this decrease to normal. When finasteride was given to these testosterone-treated castrate rats, erectile response was not restored. DHT was as effective as testosterone in restoring response to EFS in castrates and this effect was not decreased by finasteride. Nitric oxide synthase activity in the penile body was measured by the arginine-citrulline conversion and was found to correlate with the EFS determinations. These results show that DHT is the active androgen in the prevention of erectile failure seen in castrated rats, and suggest that this effect may be mediated, at leastpartially, by changes in nitric oxide synthase levels in the penis. (Ref. 5)

The effects of supraphysiological levels of testosterone, used for male contraception, on sexual behavior and mood were studied The testosterone administration increased trough plasma testosterone levels by 80%, compatible with peak testosterone levels 400-500% above baseline. Various aspects of sexuality were assessed using sexuality experience scales (SES) questionnaires at the end of each 4-week period while sexual activity and mood states were recorded by daily dairies and self-rating scales. In both groups there was a significant increase in scores in the Psychosexual Stimulation Scale of the SES (SES 2) following testosterone administration, but not with placebo. The SES 2 results suggest that sexual awareness and arousability can be increased by supraphysiological levels of testosterone. However, these changes are not reflected in modifications of overt sexual behavior, which in eugonadal men may be more determined by sexual relationship factors. This contrasts with hypogonadal men, in whom testosterone replacement clearly stimulates sexual behavior. There was no evidence to suggest an alteration in any of the mood states studied, in particular those associated with increased aggression. We conclude that supraphysiological levels of testosterone maintained for up to 2 months can promote some aspects of sexual arousability without stimulating sexual activity in eugonadal men within stable heterosexual relationships. Raising testosterone does not increase self-reported ratings of aggressive feelings. (Ref. 6)

The search for a more natural T form has resulted in the development of s Testosterone cream, TestoJel® based on soy proteins. TestoJel is a transdermal system for delivering natural testosterone ( identical to that secreted by the testicles) directly into the blood stream without pills or shots. Therapeutic levels of T hormone (5mg/day) are achieved with only 1-2 tsp. per day.

This dose containing approximately 40-80mg of testosterone is delivered to a testosterone deficient male patient, who can apply it to their scrotum twice a day. By monitoring blood levels of free and total testosterone, absorption is determined and the dose can be adjusted to each individuals needs. Any level over 450 ng/dl is associated with normal sexual function (normal 270-1270 ng/dl). Men claim that their ability to ejaculate frequently improves and their frequency of erections in the morning increase as well. Men with levels in the normal range, report that they also have an increased sense of "well-being" and find it easier to build muscle tissue.

V. TestoCreme® and Viagra®

Prior to the development of TestoCreme® and TestoJel® , the controlled delivery of testosterone to hypogonadal men was provided by TestoDerm®, a self-adherent scrotal testosterone system to provide programmed testosterone delivery through the uniquely permeable scrotal skin. Androderm® was developed as a generic drug containing 5 grams of testosterone for use anywhere on the body .

The responses of men to supplementary testosterone and its metabolites by trans scrotal testosterone systems of varying testosterone content were compared with the response to 200 mg of testosterone enanthate. Daily transscrotal testosterone system administration resulted in a rapid increase of testosterone and bioavailable T or free T. The free testosterone levels are non-sex hormone binding globulin-bound testosterone are biologically active. Testosterone levels peak at two hours, followed by a slow decline over 23 hours, resembling the diurnal variation of endogenous testosterone. One year of daily transscrotal testosterone system therapy demonstrated continued reliable absorption of testosterone and suppression to normal of the luteinizing hormone (LH) in two of three patients.

There was a greatly disproportionate increase of serum dihydrotestosterone ( DHT) over testosterone, suggesting 5-alpha reduction at the scrotal site. The subjects reported marked subjective improvement. Thus, the transscrotal testosterone system is a novel, effective, and well-tolerated method of delivering testosterone to hypogonadal patients. (Ref. 7)

However, patch testosterone preparations fall off easily, they are large and bulky and crinkle with movement. Although they are expected to deliver adquate testosterone with one patch, most of the research supporst two or three patch use for younger men. The cost is prohibitive and the release of AndroGel® creates a similar problem. TestoCreme® requires only 1/2 to 1 gram of cream application for delivery of a comparable amount of testosterone.

In summary, transdermal testosterone has been found to be both safe and efficacious for hormone replacement or supplementation for men who are deficient. The use of TestoCreme® transdermal testosterone-based cream offers a simple alternative method of treating hypogonadism TestoCreme® has been shown to be both effective in raising free and total T and is more convenient for patients than other methods of testosterone delivery. (Ref. 8)

VI. References

1. Anthony Gauthier, MD, et al. Relative Efficacy of Sildenafil Compared to Other Treatment Options for Erectile Dysfunction [South Med J 93(10):962-965, 2000. © 2000 Southern Medical Association]

2. Urban RJ, Bodenburg YH, Gilkison C, Foxworth J, Coggan A.R.Wolfe RR, Ferrando A. Testosterone administration to elderly men increases skeletal muscle strength and protein synthesis. Am J Physiol 1995 Nov; 269(5 Pt 1): E820-6

3. Brown WA, Monti PM, Corriveau DP . Serum testosterone and sexual activity and interest in men. Arch Sex Behav 1978 Mar; 7(2): 97-103

4. Gooren LJ. Androgen levels and sex functions in testosterone-treated hypogonadal men. Arch Sex Behav 1987 Dec;16(6):463-73

5. Lugg JA, Rajfer J, Gonzalez-Cadavid NF. Dihydrotestosterone is the active androgen in the maintenance of nitric oxide-mediated penile erection in the rat. Endocrinology 1995 Apr;136(4):1495-501

6. Anderson RA, Bancroft J, Wu FC. The effects of exogenous testosterone on sexuality and mood of normal men. J Clin Endocrinol Metab 1992 Dec;75(6):1503-7

7. Korenman SG, Viosca S, Garza D, Guralnik M, Place V, Campbell P, Davis SS . Androgen therapy of hypogonadal men with transscrotal testosterone systems. American Journal of Medicine 1987 Sep;83(3):471-8

8. Kryger, AH. The Effect of Administration of a Testosterone Cream in Hypogonadal men. (unpublished). Study available on www.TestoCreme.com .

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