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February 22 2003
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New Anti-Impotence Drugs Released

 

Two new anti-impotence drugs were released in areas of Europe such as Britain and Germany, as well as in Australia, to compete against Pfizer’s Viagra.

U.S. firms Eli Lilly and Icos Corp. released the drug Cialis, while Bayer came out with Levitra, also known as vardenafil.

Viagra was introduced five years ago to treat impotence and has had much commercial success--in 2002 alone, global sales reached $1.74 billion.

All three drugs work by blocking the PDE-5 enzyme, which affects blood flow to the penis. However, the new drugs claim to provide a more effective treatment, including being longer lasting, than has been offered in the past. And, rivals see room for growth in the market, as only 10 percent to 15 percent of the 30 million men with impotence in Europe receive treatment, according to Eli Lilly.

Anti-impotence drugs have created a major market on the Internet as well, though concern has been voiced about patients not having to consult a doctor to receive the medication. Certain Web sites have begun to offer Cialis already--for a price of up to $113 for four pills, a cost that is more than three times the price through the government-funded National Health Service.

According to an Eli Lilly representative, Cialis should be prescribed only by doctors and should not be taken by men who have had a recent stroke or heart attack or who have unstable angina.

The U.S. Food and Drug Administration has not yet cleared Cialis and Levitra, but both drugs are expected to be available in the United States in the second half of 2003.

Reuters February 4, 2003

Reuters February 5, 2003



Dr. Mercola Dr. Mercola's Comments:

These drugs have not yet been released in the United States, but Cialis just hit Europe earlier this month. Will they work? No doubt about it.

However, are they treating the problem and will they have any side effects? If you have been reading this newsletter for a while you can confidently answer both of those questions--no, they are not treating the problem, and yes, they will have side effects.

There are practical alternatives to these drugs, as I mentioned last month:

In addition to Viagra causing blue-green color blindness, headaches and flushing it has now been indicated as a major risk factor for heart disease and stroke.

Fortunately there are natural alternatives that frequently solve the problem.

In November 1998 I posted the following information that includes background information about impotence and Viagra as well as natural alternatives to the drug:

On March 27, 1998 the FDA approved Viagra. I have warned readers of this newsletter on three previous occasions of the dangers of this drug, and I would like to offer some practical alternatives.

Viagra was initially investigated as a potential anti-angina medication based on its ability to release nitric oxide and increase blood flow to the heart. Viagra failed as a heart medication, but London researchers became excited when many of the men in their clinical trials reported the frequent occurrence of unaccustomed erections and improved sexual performance.

Five years after this serendipitous finding, Viagra was granted approval as a treatment for men suffering from difficulty in achieving erection. In the two months following its release, over 1 million prescriptions were issued, making it one of the most successful drugs ever introduced. Viagra may even provide similar benefits, enhancing sexual sensation and orgasmic enjoyment, for women and the drug is now in clinical trials for that purpose.

Vascular smooth muscle cells surround arteries and arterioles, contracting and relaxing the arteries to regulate blood pressure. The given state of smooth muscle cells and their effect on blood pressure understandably have a profound effect on the male sexual organ.

Normally, in the presence of sexual stimulation, blood flow is directed into pockets known as the corpus cavernosum, contained within the shaft of the penis. The resulting inflow of blood leads to the enlargement and stiffening of the penis. This engorgement is triggered by a short-lived neurotransmitter. Nitric oxide, synthesized from the oxidation of the amino acid arginine, activates an enzyme that manufactures cyclic guanosine monophosphate (cGMP), which is a biochemical signaling enzyme. Under normal circumstances, cGMP directs the smooth muscle cells to relax, leading to the dilation of the penile arteries.

However, immediately following release of nitric oxide and production of cGMP another enzyme, cGMP phosphodiesterase type 5 (PDE-5), is activated. PDE-5's main activity is to destroy cGMP almost as fast as it is formed. The result of this breakdown of cGMP by PDE-5 is a rapid decrease in smooth muscle relaxation and a loss of blood flow to the penis. Subsequently, the penis returns to a flaccid state.

Unfortunately, as we age cellular concentrations of cGMP decrease. Viagra works to achieve and maintain erections by enhancing the effect of nitric oxide and maintaining higher levels of cGMP.

The way Viagra does this is to selectively inhibit the cGMP destroying actions of PDE-5. By blocking the actions of this enzyme system, cGMP is no longer broken down. This leads to elevated cGMP levels in the corpus cavernosum. This, in turn, prevents relaxation of the smooth muscle in the corpus cavernosum, increases blood flow to the genitals, and leads to stronger erections and intensified sensations.

Natural Alternatives to Viagra

Aside from the risk of dying and increasing the risk of retinal dysfunction, the biggest drawback to Viagra is the high cost, which can range upwards of $10 per pill. Fortunately, there is a safer, less expensive and more natural way to achieve many of the actions to Viagra. The key is L-arginine, the direct precursor to nitric oxide.

In the 1990s, scientists discovered that L-arginine, a non-essential amino acid commonly found in the diet, is an oxidative precursor of nitric oxide. Under conditions in which nitric oxide is produced for a specified physiologic purpose, the concentration of L-arginine from which nitric oxide is formed can be a limiting factor.

Researchers at New York University School of Medicine gave L-arginine to a group of 15 men and found that six received benefit. Doses were around 1,000 to 3,000 mg per day.

Sexual arousal occurs not just in the genitals, but in the whole body and especially in the brain. For men, it actually begins when the brain sends impulses down the spinal cord and out to the nerves that serve the penis. These impulses trigger the production of nitric oxide.

The neurotransmitter that causes the sexual message is acetlycholine (ACH). ACH also seems to control sexual behavior through its activity in the brain. For women, ACH is also a very important part of sexual function. With too little ACH, sexual activity goes down. ACH is involved in the buildup toward orgasm and the urethral and vaginal contractions that occur during orgasm.

One way to safely and effectively enhance ACH levels in the body is to take supplements of choline (1,000 to 3,000 mg) and vitamin B5 (500 to 1,500 mg) so that the body will produce more ACH.

Vitamin B5, also known as pantothenic acid, actually seems to enhance endurance by two routes. The first is by increasing ACH and the second is its role in the energy producing Krebs cycle. The choline and vitamin B5 are ideally taken about 20 to 30 minutes before sex in order to get the full effect.

Yohimbine is from a native tree in West Africa. For centuries a tea distilled from the inner bark of this tree has been used to amplify male virility and sexual prowess.

Yohimbine’s primary path of action duplicates a key biochemical role in male erection. It acts upon a specific network of nerve cells called the alpha-2-adrengeric system and shuts down this system, which increases the flow of blood through arteries into the penis while at the same time decreasing the blood flow from the penis through veins. It also results in higher levels of ACH. Several controlled trials have been done with yohimbine, and the response rate is about 40 percent.

Related Articles:

Impotence Drug May Promote Heart Attacks

Study Urges Use of Drugs to Treat Antidepressant-Related Impotence

Say No to Viagra

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