How Sildenafil Citrate Works
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Sildenafil Citrate
Viagra (Sildenafil Citrate) is the most popular erection pill known to men.
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Sildenafil acts as an inhibitor of the receptors in the enzyme guanylate cyclase found in the soft sponge like tissue in the penis. It releases nitric oxide, which attaches to the enzyme, which boosts the amount of guanosine monophosphate or [cGMP], the effect is relaxation of the muscle, a widening of the blood vessels leading to increased blood flow and an erection as the end result.
Sildenafil is both a strong and discerning drug, targeting a specific enzyme with a precise role. Because of this exact function within the body, it achieves its targeted objective of chemical reaction that results in an improved erection. This improvement arises in concurrence with sexual stimulus, which triggers the Nitric oxide and cGMP signaling system; in other words no stimulation, no reaction. Sildenafil and its two major competitor’s tadalafil and vardenafil each work the same way.
After metabolizing in the liver, the liver and kidneys expel the sildenafil. This means it is more effective if taken on an empty stomach or if eating is necessary, a light fat free meal as it will be absorbed quicker. When taken using this precaution the sildenafil can be up to one third more effective.
Sildenafil as a Treatment
Erectile Dysfunction
Otherwise known as ED, erectile dysfunction is a malady that affects men for various reasons. Before the sildenafil citrate is prescribed for this particular ailment, the clinician will have the patient undergo a number of tests to determine the exact cause of the ED. It can occur in adult men of any age and a physician will understand the proper functioning erection based on the patients age then determine the cause of the dysfunction. There may be nerve damage caused by an accident, a pre existing medical condition such as diabetes or alcoholism. There could be an undiagnosed circulatory problem or the patient could be clinically depressed.
If the individual is suffering from depression and treated with an anti depressant many of these can cause ED. Sildenafil has become a standard form of treatment. Interestingly enough this same research showed that women taking anti-depressants had an improved sexual experience as well.
Pulmonary Hypertension
Sildenafil citrate is proving to be a versatile drug after all. As well as treating men for erectile dysfunction, it has also been successful treating pulmonary arterial hypertension. Sildenafil relaxes the principal artery wall, which decreases the pressure. The heart ventricle’s workload is diminished and there is an improvement in symptoms of heart failure in the right heart. Because sildenafil is specifically targeted, the vasodilation reaction occurs only in the area of the lungs and penis. Pfizer applied for FDA approval for this specific action and approval was granted in 2005.
To avoid any confusion with the ED medication, the drug for PAH was called Revatio and the pill is round and white at 20 mg.
Altitude Sickness
Relatively new research backs up sildenafil citrate as a treatment for altitude sickness. French researchers ran a study that showed sildenafil relieved altitude sickness quicker when taken at the outset of a climb [in this case a helicopter ride 2.7 miles up] as opposed to a group who took a placebo at the same time at altitude. There was an adjustment period at the outset when symptoms were noticeable. However, there was a marked improvement in the sildenafil group in a day or two with relief of their altitude sickness symptoms when surveyed regularly while on the mountain.
Sildenafil is already becoming the normal remedy for this malady. Previously the standard treatment for altitude sickness was a speedy decline from altitude, calcium-channel blockers or steroids. Sildenafil is a useful alternative to these and when a quick descent is hindered by weather or other impediments. The men who took part in the study were all under 30 years old, healthy and had no previous mountaineering experience.
Sildenafil Citrate When Used in Sports
What about the use of sildenafil as a performance-enhancing drug? Many athletes test positive for Viagra when asked to test but currently there are no rules banning the use of sildenafil or its competitive brands when it comes to use in sports. Its use by athletes is becoming so commonplace that the world anti-doping agency is considering its inclusion on its list of substances banned from its global sports.
When drug seizures are made of banned performance enhancing drugs it is common for these ED drugs to be found amongst the other contraband. Since the activity of sildenafil in the subject means the dilation of the blood vessels, some experts believe this means an increase in oxygen levels in the blood and the delivery of that oxygen plus nutrients to the muscles. This can be quite helpful to athletes when competing at higher altitudes and when oxygen is minimized by pollution or other reasons.
Some seem to think that athletes may also be taking sildenafil to counter act the impotence experienced because of the use of other drugs such as steroids. There is little doubt that if the world anti doping agency can prove that sildenafil gives an unfair advantage to culpable athletes than it will go for a ban. That is, however only if it can be done safely from a legal and scientific perspective.
Non-clinical Use of Sildenafil Citrate
Sildenafil When Exploited Recreationally
Of course it was only a matter of time before sildenafil and its counterparts were abused by those who have no medical need for it. Many young adults are experimenting with sildenafil citrate, and why not since that 1 – 3% of twenty something’s that suffer from ED need something to improve their sex lives! Finally their elders have something they can call their own and it is wasted on the young so they can party even more hardy.
The real danger of this kind of use is when certain dangerous drugs such as ecstasy or methamphetamine are laced with sildenafil to counter the side effects of the host drugs such as erectile dysfunction. These combinations are known by such names as sextasy, trail mix or rockin and rollin to name just a few. This mixing of drugs can be extremely dangerous when amateur pharmacists also mix amylnitrite and sildenafil, the result can be deadly. There is much speculation about the use of sildenafil as an enhancer of sexual performance in older men not diagnosed with ED. They just want to perform like they were twenty years old again. Is this considered drug abuse or an accepted form of life improvement? The jury is still out on this. There is little doubt that sildenafil and other major ED drugs are being abused in some dangerous ways.
The use of sildenafil citrate for non medical reasons seems to be on the increase. There is some debate that sildenafil is being used as a lifestyle drug rather than a medical treatment. Insurance and benefits management companies are certainly looking into prescribing practices of clinicians. A recent survey showed that there was a dramatic increase in sildenafil prescriptions among men aged 18 to 45 – a 312 percent increase. While in men aged 46 to 55, the target age for sildenafil, the increase was a mere 216 percent over the same time frame. That said, men in the over 56 age bracket continued to receive the most prescriptions of sildenafil and its competitive brands.
When younger men or those who don’t really have a medical need take sildenafil, they may be disappointed in the results. The side effects most common such as headaches, facial flushing etc are a small price to pay for the determined. However they may simply notice a shorter period between erections rather than a prolonged stimulated period of erection. That may be enough for some who experiment with sildenafil as a lifestyle or recreational drug. More likely they will find the trade off not worth the effort. This is likely the reason why some prescription claims companies show a decrease in secondary refills on some younger patients.
Not all patients who receive sildenafil are suffering from a physical impairment concerning ED. There are various reason why some men are prescribed sildenafil citrate. For example emotional problems may cause some ED problems. One patient who was divorced needed the sildenafil so he could perform with a new partner. Others may have similar psychological needs for the little blue pill. In another case a young man was given a pill from a friend and anticipating an amorous evening soaked in a hot tub, had a glass of wine got out of the hot tub and promptly fainted! A physical examination showed the combined effect of wine, hot water soak and sildenafil increased the dilation of his blood vessels beyond his ability to handle and his romantic evening was a bust.
Wilting Plant Syndrome and Sildenafil
One wonders how far some people will go to achieve a green thumb. Apparently some very bored scientists in England thought that sildenafil might affect droopy flowers the same way it helps weary erections! When freshly cut flowers were placed in a vase with a diluted solution of sildenafil [all of 2% of the normal male erection cure], they lasted up to 2 weeks compared to 1 week with flowers in water alone. Not only did the sildenafil soaked flowers look fresher with longer lasting color, they appeared more vibrant in their erectness.
All joking aside, humans and plants share a common “ingredient” – nitric oxide, so it stands to reason that this testing would be worth the effort if it worked on a variety of different plants. No one is suggesting that sildenafil be sprayed on all vegetation but by fumigating certain plants and vegetables with nitric oxide they found the results rather astonishing. Clearly the results of this study had shown there was a use for nitric oxide in the food and fresh flower industries.
Sildenafil Citrate For Jet Lag
Researchers in Argentina found that hamsters recovered from jet lag quicker when given a hamster size dose of sildenafil when tested in conditions that simulated transatlantic air travel. The choice of hamsters for the study was because they have an activity pattern that is routine and strictly adhered to. The control group of hamsters took an average of 12 days to recover from the replicated jet lag while the sildenafil injected hamsters averaged 8 days to return to a normal rhythm.
The general consensus concerning jet lag is that each hour of travel time equals one day of jet lag upon arrival. Jet lag is more common in travelers heading east rather than west and prolonged bouts of jet lag can be costly in terms of personal efficiency. More seriously, severe time shifts have been found to have fatal consequences in aged mice so there would seem to be a need for some form of treatment for chronic jet lag. There was no indication that the test rodents had any formal complaints with the study.
Treatment Protocols for Sildenafil Citrate
Sildenafil is available in 25, 50 and 100 mg doses from the manufacturer Pfizer. When prescribed by a physician the general dosage for erectile dysfunction is 25 mg up to 100 mg, no more than once a day. It should be taken from 30 minutes to 4 hours before sexual activity. Most clinicians prefer to start a patient on a lower dose initially preferring to prudently administer the sildenafil and monitor a patients reaction to it.
Adverse Reactions To Sildenafil Citrate
There are predictably some contraindications where sildenafil is concerned.
- When taking sildenafil a patient should not take any nitric oxide, nitrites, nitrates such as nitroglycerine pills, sodium nitroprusside or amyl nitrite [known as poppers].
- Any men who have history of cardiovascular health problems and been advised against having sexual intercourse.
- If a patient has any diagnosed liver disease or impairment.
- If the patients renal system or kidneys are under functioning or impaired in some way.
- If the patient suffers from low blood pressure or hypotension.
- If there is a history of stroke or heart attack
- Should a patient have any history of retinal impairment or disease or a hereditary degenerative eye condition.
Sildenafil Citrate Side Effects
During the clinical trials for sildenafil citrate there were some side effects found in some of the study groups members, the most common included the following:
- Headaches
- Flushing
- Heartburn and indigestion
- Some nasal congestion
- Blurred vision
- Diarrhea
- Dizziness
- Rash
Some of those tested said they saw everything in a blue tint which is known as cyanopsia. Others complained of chronic eye blurring and a loss of their peripheral vision. The FDA announced a finding in 2005 that sildenafil might cause vision to become impaired and certain studies have shown sildenafil consumption connected to some very serious optical neuropathic problems.
After market surveys showed some serious but uncommon side effects such as priapism which is a painful long lasting erection beyond the four hours sildenafil citrate is known to work in the system. Some instances of severe low blood pressure, heart attack, heart arrhythmias, stroke, amplified pressure of fluid in the eye and hearing loss. Due to these after market surveys, the FDA called for more prominent labeling on sildenafil citrate containers regarding potential hearing loss.
Interactions with Sildenafil
A major interaction with sildenafil is with patients being medicated with protease inhibitors for HIV treatment. These protease inhibitors slow down the metabolizing sildenafil and multiply the plasma levels of sildenafil citrate which can escalate the harshness of the drug side effects. Recommended dosage for a patient with HIV taking the protease inhibitors is no more than 25 mg for each 48 hour period. Parallel use of sildenafil along with an alpha-blocker could cause low blood pressure in some but this reaction can be avoided if drugs are taken at least 4 hours apart.
Clinical trials of Sildenafil
Every drug goes through many pre trial tests inside the research lab before they are tested on the public. So to was sildenafil before it went to clinical trials of humans. Clinical trial are planned so that they will give the best possible results where accuracy is concerned. They do this by conducting double blind, placebo testing to measure the effect of the drug versus the effect of the placebo on trial subjects.
When it was ready for human testing for erectile dysfunction, some 3000 men between the ages of 19 and 87 years of age were tested in over 20 different studies with sildenafil. There was a marked improvement shown in those trial subjects who were taking the sildenafil citrate as opposed to the placebo. Sildenafil patients were given the medication and tested an hour or so later for the results of their erection. A questionnaire was also completed as part of the study to better understand the patient’s ability to have intercourse after taking sildenafil.
The placebo group was important to better understand the reaction of these participants simply receiving an identical pill without the active ingredient [the placebo effect] versus those taking the actual ingredient laced medication. The double blind study was also important to evaluate the difference and effectiveness of the sildenafil and placebo pills versus actual ED caused by psychological factors or some latent physical conditions.