PDE5 Inhibitors Help Treat Erectile Dysfunction

Viagra is a hard act to follow, but in this issue of Elite Fitness News, you'll learn about three new potency drugs that may soon give Viagra some stiff competition.

Table of Contents:

1. IC351 and Vardenafil
2. Losartan
3. Tribulus terrestris for peak performance.

IC351 and Vardenafil

IC351 and Vardenafil are PDE5 inhibitors being developed by Eli Lilly and Bayer respectively specifically to treat erectile dysfunction. Losartan is an antihypertensive medication, sold in Germany as Lorzaar, in India as Losacar, and in Israel as Ocsaar and has demonstrated as a side effect dramatic improvements in treating impotency.

IC351 will soon be sold in the States under the brand name Cailis. Initial research indicates that Cailis may be effective at promoting erections for up to 24 hours. That\'s 20 hours longer than Viagra. The benefits to men with erectile dysfunction are obvious, a drug like this would allow men to engage in much more spontaneous sex than would be possible with Viagra.

Where Viagra begins working after 30 minutes and is in full effect after an hour, Cailis begins working in only 16 minutes. In a double-blind study of 61 men with mild to severe erectile dysfunction, the men taking Cailis were more successful at achieving erections even up to 24 hours later. The men were divided into the treatment group who received Cailis and the control group who received a placebo. Neither doctors nor patients knew who received the drug or the placebo. The men were tested at different intervals for a 24 hour period. They were shown sexual images, and erectile response was measured with a device called a Rigiscan. The treated group was much more likely to be able to achieve potent erections than the non-treated group.

A second study was conducted on 223 men, each of whom took either the drug or a placebo, in the privacy of their own home. The men were instructed to take the drug before engaging in sexual activity and to use a stopwatch to record the time it took to achieve an erection. Men were able to get an erection as early as 16 minutes after taking the drug and could have a second sexual encounter up to 24 hours later. The only side effect reported was the occasional headache.

Cailis will soon be tested head-to-head against Viagra in upcoming studies.

Another exciting potency drug from Bayer has just completed its first large-scale patient trials. The drug vardenafil not only improved erections in up to 80 percent of men studied, but also increased their ability to complete sexual intercourse with ejaculation.

"Vardenafil improved erectile function in these men, regardless of their age, cause, or severity of their problem. This improvement occurred even at the lowest dose of 5 mg," said Dr. Irwin Goldstein of the Boston University School of Medicine. "There was another important finding as well," continued Goldstein. "In the overall study, vardenafil not only helped most men achieve erections, they also were able to sustain their erections and successfully complete intercourse."

The study involved 580 patients of ages 21-70. All had experienced difficulty achieving erections for an average of 2.8 years. The men were divided into four groups and received vardenafil in 5 mg, 10 mg, or 20 mg doses, or placebo on demand, but not more than once a day. Prior to treatment, the men were surveyed based on their ability to penetrate and on their ability to maintain an erection during intercourse. The scoring was based on a five-point scale, with one being the most difficulty penetrating and maintaining erections and five being the least difficulty.

The men who scored themselves at 1.0, having very little ability to penetrate, increased their score to a mean of 1.8 with placebo and to 3.0, 3.1, and 3.7 with 5 mg, 10 mg, and 20 mg of vardenafil, respectively. In other words, the increase in the ability to penetrate was much greater in the men treated than in the untreated men, although a higher dosage did not significantly improve the ability to penetrate over a lower dosage.

Men who scored themselves at 4.0 on their ability to penetrate prior to treatment, deteriorated to a mean score of 3.4 with placebo, but increased to a mean of 4.4, 4.7, or 4.4 for the same increasing doses of vardenafil.

The results for completion of intercourse were similar - the treated subjects improved regardless of severity. Those with a score of 1.0 (i.e., with very little ability to maintain an erection and complete intercourse) increased their score to a mean of 2.0 with placebo and to scores of 3.3, 3.1, and 3.5 with increasing doses of vardenafil. Those with a relatively mild degree of severity starting with a score of 4.0 had a decreased mean of 3.6 on placebo, but reached a score of 4.0, 4.3, or 4.7 with increasing doses of vardenafil.

There were very few side effects. The most frequent adverse events, whether related to the drug or not, were headache (7-15 percent), flushing (10-11 percent), rhinitis (3-7 percent), and dyspepsia (1-7 percent). The events were generally mild in intensity and related to dosage.

Vardenafil is now being evaluated in Phase III trials to better understand if these characteristics will translate into clinical benefits for patients. Results are expected for publication later this year, with completion of the Food and Drug Administration (FDA) review in the second half of 2002.

Losartan

According to a study in this month\'s American Journal of the Medical Sciences, the drug losartan may be a hypertension drug also effective at treating sexual dysfunction.

After 12 weeks of treatment with the drug losartan, 88 percent of hypertensive males with sexual dysfunction reported improvement in at least one area of sexuality, said Carlos Ferrario, M.D., of Wake Forest University Baptist Medical Center (WFUBMC). The percentage of men reporting impotence dropped from 75.3 to 11.8.
"These results suggest a possible solution for people who\'ve stopped taking blood pressure medicines because they interfere with sexual function," said Ferrario. "In addition to controlling blood pressure as well or better than other medications, losartan seems to have a positive effect on sexuality."

The study used a self-administered questionnaire to screen 323 men and women with hypertension for sexual dysfunction, which includes decreased libido, impotence, and poor sexual satisfaction. Sexual dysfunction was diagnosed in 82 men, a prevalence of 42 percent. These 82 men were compared to an equal number of hypertensive men without sexual dysfunction. Both groups took 50 to 100 milligrams of losartan (sold under the brand name of Cozaar) daily for 12 weeks. They completed the questionnaire at both the beginning and end of the treatment period.

The increases in sexual function were dramatic.

In the men with sexual dysfunction, 88 percent reported improvement in at least one area of sexual function after treatment with losartan. The number reporting overall sexual satisfaction increased from 7.3 percent to 58.5 percent. The number reporting a high frequency (at least once a week) of sexual activity improved from 40.5 percent to 62.3 percent. An improved quality of life was reported by 73.7 percent of the men with sexual dysfunction.

Similar results were reported in a small group of women treated with losartan. The sample size, however, was too small for the results to be statistically validated.

In the group of men without sexual dysfunction, the drug treatment produced no changes in sexual function or satisfaction. This would indicate that unlike Viagra, IC351, and vardenafil, losartan would be of little benefit to those wishing to enhance already healthy sexual function, but could be a great alternative to some existing hypertension medications.

Tribulus terrestris for peak performance.

Wouldn\'t is be great to raise testosterone levels, build muscle mass, improve cycle recovery, and even enhance the potency of your erections? Like Clomid and HCG, there is a large body of research that conclusively shows that Tribulus terrestris can do all this and more. You see, Tribulus has a profound effect on LH (luteinizing hormone) production in males, which stimulates the production of testosterone by the testis. LH exerts its effect by stimulating the leydig cells of the testis. In fact, LH stimulation is how both Clomid and HCG exert their effects.

Athletes use Tribulus to increase the body\'s own natural production of testosterone for athletic performance enhancement or to normalize testosterone levels often depressed by steroid use or the prolonged use of steroid precursors. If endogenous testosterone levels are not brought to normal, a dramatic loss in size and strength may occur. Tribulus can play a crucial role in preventing this crash in athletic performance.

When steroids are used in high dosages, they can cause a false signal to go to the hypothalamus that results in a depressed signal to the testicles. In other words, with all the excess testosterone in the body, the testicles get lazy and stop production. Over a period of weeks, this depressed signal causes the testicles to atrophy. To avoid this, athletes can use Tribulus to keep an artificial signal going to the testis. Tribulus therapy has been found to be very effective in the prevention of testicular atrophy as well as to use the body\'s own biochemical stimulating mechanisms to increase plasma testosterone levels during training.

It is interesting to note that both Clomid and HCG exert their testosterone restorative effect in the same way that Tribulus does. Both increase production of LH causing an increase in testosterone production. Also like HCG and clomid, Tribulus has numerous secondary effects that are worth mentioning. Tribulus increases erectile potency and frequency, it increases ejaculatory fluid volume, it increases energy, and it raises libido.

But there is a catch. Unprocessed Tribulus is not a particularly effective supplement. When purchasing Tribulus, the important thing to remember is the concentration of steroidal saponins. What you want is 100% Bulgarian Tribulus terrestris with a minimum of 42% concentration the steroid saponins of the furostanol type with predominating quantity of protodioscine. A concentration of 42% is about the highest that is available. Next time you are in the GNC, take a look at the other brands of Tribulus being sold. If they mention their standardization at all, most often, it is less than 20%.

And now the research:

The medical researchers at the Chemical Pharmaceutical Research Institute in Sofia, Bulgaria decided to investigate the medical benefits of Tribulus. Over the course of the last 20 years, they conducted extensive laboratory and clinical trials (both animal and human) that confirmed the benefits of Tribulus so conclusively that standardized pharmaceutical preparations of the herb were developed and incorporated into mainstream medical treatment.

Tribulus increases erectile potency and frequency.

Isn\'t it funny how an embarrassment of youth eventually becomes a virtue. Erections. One thing that everyone likes is the "lift" that Tribulus gives you in the bedroom.

When scientists first started researching Tribulus terrestris, it was for the sole purpose of discovering a safe, natural treatment for sexual deficiencies.

Studies were conducted on 212 males, between 14 and 60 years old. The men studied suffered from partial or complete impotence. The studies methodology was a simple blind experiment, using a placebo. Tribulus of 42% concentration was individually administered to all patients who had not received hormonal agents for at least one month prior to the treatment.

Almost all the patients, reported a prolongation of erection duration, spontaneous nocturnal erections, and more frequent erections after treatment.

Some of the patients were favorably affected by 3 doses of 750mg daily while another group received twice this much. In the group receiving 3 daily doses of 750mg a two-fold increase in sperm count was observed. In those receiving twice this dosage, the increase in sperm count was observed along with a two-fold increase in ejaculate volume.

Patients experienced a sense of heaviness and distention in the testes between the 40th and 60th day after the start of the treatment with a daily dose of 1500mgs. In fact, a feeling of fullness in the testicles is frequently reported in athletes using Tribulus. Improvement both in the ejaculate volume and the concentration of the spermatozoa was observed towards the end of the treatment. And the testosterone serum level was elevated from 1.75 mg/ml to 3.75 mg/ml.

Tribulus increases libido

Out of 14 patients with reduced libido but no apparent problems with the male genital organs themselves, 12 experienced obvious improvement of the libido and one patient - a slight improvement (after a 60-day treatment cycle) and no effect was observed in one.

Out of a total of 36 patients with chronic prostatitis and reduced libido, 15 were very favorably affected by the end of the treatment cycle, 12 - favorably, and in 9 of the cases with duration of the inflammatory process over 5 years, no effect occurred.

Tribulus significantly raises natural testosterone production.

The effect of Tribulus has been studied on the serum concentration of the hormones: ACTH, STH, LH, FSH, adrenal hormone, aldosterone, and cortisol and on the sex hormones - testosterone and estradiol. The experiments were carried out on 8 males and 8 females, 28 - 45 years of age. Tribulus was administered in a single dose of 250 mg, three times daily for 5 days. Serum samples were drawn at 8 a.m. and 12 a.m., both before and after treatment.

It was established that Tribulus did not change the concentrations of adrenal hormones and of ACTH. However, the hypophyseal-gonadal axis was significantly changed. In females, there was a prominent increase in the concentration of FSH and estradiol. In the males there was a prominent increase in LH and testosterone. The mechanism of that action was presumed to be both by direct effect on the gonads and by the increase in certain hormones.

How much should be taken

While there is no definitive guide on how much Tribulus terrestris should be taken, there are different guidelines suggested by experts in the medical field. Most suggest 250-750mg per day taken evenly throughout the day with meals. A more ambitious dosage would be 675mg to 2,025mg per day for a more pronounced benefit.

Other benefits: Tribulus has several additional benefits that are beyond the scope of this article.

Tribulus has been shown to reduce high blood pressure, as well as sodium and fluid retention and to exert an analgesic effect on the body. Other documented effects include:

Antibacterial, anti- fungal and anti-inflammatory properties. Prevention of kidney stones. Increase in red and white blood cells. Stimulation of the immune system. Increased energy.

Author: George Spellwin