What is Sildenafil Citrate? A Comprehensive Guide To The Active Component

What Is Sildenafil Citrate

  • Sildenafil Citrate is an active component that belongs to a class of PDE5 inhibitors.
  • Sildenafil citrate is used mostly in the treatment of erectile dysfunction in men.  It is branded under the name of Viagra.
  • Studies have shown recently that sildenafil citrate can be also successfully used for pulmonary hypertension, thanks to the dilation it causes in pulmonary vascular pathways.
  • Pulmonary vascular is a common term for diseases that happen in the blood vessels on the route between the heart and the lungs.

What the multiple types of research have found, is that sildenafil citrate significantly improves pulmonary human dynamics when at rest and, during exercise, in patients with chronic obstructive pulmonary disease-associated pulmonary hypertension.

Do we need sexual stimulation for sildenafil to work?

Yes, sexual stimulation is pretty much a prerequisite to ensure sildenafil citrate would work at all. A common misunderstanding of sildenafil citrate is that it is sort of a magic pill that causes an erection no matter what, under any circumstances.

It is not the case. Sildenafil simply an enhancer of naturally occurring biochemical and physiological processes in the human organism that affect erectile functions.  Sildenafil is effective when with the presence of psychogenic stimulation and reflexive stimulation an erection cannot occur for some reasons. It is time to discuss the possible reasons for this erection failure.

How is an erection obtained from the physiological point of view?

How is an erection obtained from the physiological point of view1

There are two major types of stimulation that can cause an erection: Psychogenic and reflexive stimulation (learn more). Psychogenic are the messages being delivered from the higher brain regions. And the sensory stimulation refers to the stimulation of the sensory fibers, particularly from the glands in the genital area.

During an erection, the human parasympathetic nervous system takes over the sympathetic nervous system, while during the course of ejaculation, or orgasm, your sympathetic nervous system is taken over.

A man has the release of neurotransmitters from the parasympathetic nerves, which stimulates the release of nitric dioxide within the endothelial cells that are aligned at penile vessels (running across the penis).

Then nitric dioxide diffuses into smooth muscles. Once nitric dioxide gets into the smooth muscles, it activates an enzyme called guanylate cyclase. Then it converts in creatine phosphate, which, in its turn, converts to cyclic glycine monophosphate. The latter activates the enzyme that causes the relaxation of muscle fibers. The dilation occurs as a result, and the massive blood flow comes into the spongy corpus cavernosa. At a certain point, there is no inflow or outflow to or from the penis, which allows it to maintain an erection.

PDE5, or phosphodiesterase type 5, is an enzyme responsible for accepting and consequently quickly breaking down cGMP that keeps a penis from being erect permanently. Otherwise, if the parasympathetic system is stimulated, then cGMP causes the relaxation and penile erection occurs.

What can cause erectile dysfunction in men?

The most common causes of erectile dysfunction include:


Diabetes could cause erectile dysfunction because of the damage to the blood vessels leading to the nerves that possibly enervate the penis.

Cornea arterial disease and hypertension

Cornea arterial disease and hypertension are associated with vascular problems that may over the significant period of time cause hardening, or sclerosis, of the cardiovascular system that, in its turn, can hinder the system from working toward and an achievement of an erection.

Endocrinopathies (complications with hormones)

We have all sorts of hormones secreted from the human brain, from the pituitary gland in particular. The hormones when secreted regulate our bodies.

Postponing, stopping, or anyhow imbalance of this hormone regulation may lead to serious consequences, one of these can be erectile dysfunction.

Benign Prostatic Hyperplasia

In the case of Benign Prostatic Hyperplasia (BPH), there is no direct correlation with erectile dysfunction. However, the treatment of Benign Prostatic Hyperplasia has been known to have caused erectile dysfunction.

Benign prostatic hyperplasia is a very serious disease, that is why Smart Canadian Pharmacy experts recommend that you learn more about it:

Also, you can read this information about Cialis (PDE5 Inhibitor) and BPH: smartcanadianpharmacy.com/cialis-for-benign-prostate-hyperplasia.html

Anxiety and Depression-associated disorders

The brain has a lot to do with anxiety and depression associated disorders. These can be all sorts of disorders from social phobia to severe depression disorder. As we noted before elsewhere, the stimulation of our minds has a lot to do with the achievement of an erection.

Sildenafil citrate properties

The rate of absorption

Sildenafil citrate is a very rapidly absorbed drug. When you are administering Sildenafil citrate orally, your peak plasma concentration is about 30 to 90 minutes (when a drug is taken on an empty stomach), with the peak time averaging in about 60 minutes.

Metabolization of Sildenafil citrate

Sildenafil citrate is largely metabolized by the liver. There are the pharmacological effects that show when the drug is taken in combination with other drugs, and can occur because of the Sildenafil metabolization in the liver.

Excretion of Sildenafil citrate

Sildenafil citrate is excreted primarily in the stool with the extremely small portion excreted in the urine.

Pharmacodynamics of Sildenafil citrate

Sildenafil citrate is PDE5 inhibitor (phosphodiasterese inhibitor). If we block PDE5, the metabolization in cGMP allows causing vasodilation which in its turn is used in the achievement of an erection.

If you have too much of PDE5 inhibitor, it would inhibit cGMP from allowing the release of an enzyme, that causes the release of vasodilation and then helps to achieve an erection. That is to say, too much of PDE5 with no matter how much parasympathetic stimulation one gets, and an erection cannot possibly be achieved or maintained for a sufficiently long time.

 What can possibly go wrong with Sildenafil citrate?

What can possibly go wrong with Sildenafil citrate?

You cannot have virtually any active component taken without side effects.

Common side effects of taking Sildenafil citrate

  • Face flushing. Caused by systemic vasodilation.
  • A mild headache. Caused by systemic vasodilation.
  • Nasal congestion. Caused by systemic vasodilation.
  • Heartburn.

Less common side effects

  • Diarrhea;
  • urinary tract infection;
  • blue-tinged vision;
  • increased light sensitivity;
  • priapism.

Very rare side effects

  • Non-arthritic anterior ischemic optic neuropathy.

In extremely rare case it can cause permanent blindness. It must be noted that in most cases this unfortunate adverse effect occurred, it was in concurrence with underlying anatomic or vascular factors. (Such as a patient may be greater than 50 years old, can suffer from diabetes, hypertension, hyperlipidemia, smoking, and others).

 Sildenafil citrate interactions

Sildenafil citrate is largely metabolized by the liver, so naturally, interactions can occur with all the drugs that are also metabolized by the liver. Primarily these are metabolized by the system called CYP3A4, and to a lesser degree by the system called CYP2C9. Some of the drugs are antifungals that are metabolized in that way. What happens with these drugs, they are antifungal agents inhibiting the metabolism of Sildenafil citrate and causing elevated plasma level which can potentially increase the risk of adverse effects.

Interactions with macrolides

Macrolides are inhibiting the growth of various bacteria and are often prescribed for the treatment of common bacterial infections. These can inhibit the metabolism of Sildenafil citrate. Again, they cause elevated plasma levels, leading to a possible risk of increased side effects.

Protease inhibitors

Protease inhibitors comprise a class of antiviral medications that are commonly used to treat HIV/AIDS and also hepatitis C (see full overview). Again, these inhibit the metabolism of Sildenafil citrate. They cause elevated plasma levels, leading to a possible risk of increased side effects. For example, the risk of hypotension is definitely increased and everything that goes along with that.

Absolute contraindication with Sildenafil citrate

Nitrate must not be used in combination with Sildenafil citrate. Because what happens is that Sildenafil citrate potentiates vasodilating effect of Nitric Oxide from the nitrates, which results in significant decrease in the blood pressure. The decrease may be great enough to cause death.

You may also like: Complete Your Viagra Therapy With Nitric Oxide Stimulator

What can a doctor teach the patients on Sildenafil citrate?

What can a doctor teach the patients on Sildenafil citrate

A brief guidance is necessary to ensure a patient understands the basics of Sildenafil citrate functioning:

  • Sildenafil citrate is not effective without accompanied sexual stimulation and arousal. You have to have your natural body mechanisms and your biological factors working to achieve an erection. That is to say, Sildenafil citrate only helps with an erection; it does not cause an erection.
  • Sildenafil citrate is to be taken around 1 hour prior to the preplanned sexual activity. One hour will allow Sildenafil citrate to be absorbed in the system of a patient and to show its full potential.
  • Do not ever, under any circumstances take Sildenafil citrate with Nitrates.
  • Avoid high-fat meals when taking Sildenafil citrate. This is because high-fat meals decrease the absorption and cause delay the peak in extra sixty minutes. This is a long time and may cause frustration in patients.
  • In an unfortunate case, if a vision loss occurs, a patient is to notify his health care provider immediately. A vision loss is considered to be a serious side effect which may potentially lead to blindness.
  • Priapism. Priapism is an erection that is lasting for a period of more than 4 hours. An erection lasting for that long a time is very uncomfortable and detrimental; besides, it may lead to the damage to the penis. In the case priapism happens, a patient is to call an emergency immediately. Information about Priapism from Wiki: en.wikipedia.org/wiki/Priapism.

Sildenafil taken without Erectile Dysfunction

Medications capable of treating erectile deficiencies are becoming a fashion and are often used for non-therapeutic purposes. When it came to the market, sildenafil made history. There was no talk of everything else: full pages in the newspapers, extensive services within the news. It was felt that the drug could have become a specific therapy as well as a costume phenomenon, good or bad – all because it is easy to handle and without any particular contraindications.

Within a few years sildenafil was complemented with tadalafil and vardenafil (marketed under the trademarks of Cialis and Levitra respectively). The problem today is that the three pills have become a leisure drug, a fun substance. Sure, drugs are still useful to those who really need it. On the other hand, there are many people who use it for gambling and this is not good.

Viagra made a $300 million market that could rise to 6 billion in six years. According to our medical professionals, if a drug like this comes out of the medical check-ups the risks of abuse and speculation are high. Unfortunately, the discriminant between an impotent person and another who wants to improve sexual performance is slim, difficult to find. This aspect became more acute when two other pharmaceutical industries joined the first manufacturing company: the competition was the real turning point.

The result is that today it is used improperly and the emphasis on which some not-scientific papers talk about erectile deficits, the real meaning of which is all to be discussed, certainly does not help framing the problem in its right boundaries. Unfortunately, the message – often distorted – comes straight to the consumer who wants the blue pill without talking to the doctor, considering limits and contraindications. And if today’s audience is composed of middle-aged people, tomorrow may be the youngest one.

What is the solution then? The role of a family physician is of utmost importance, the one who knows the patient, is able to advise him in the best way to avoid clamorous mistakes that could affect his health.

As soon as it came into commerce it immediately discussed. Professionals from different spheres started talking about sildenafil, a drug considered by many revolutionary experts because it can restore sexual vigor to even older people. For this reason, the famous blue pill quickly crossed the boundaries of medical-scientific communication to become a topic of costume on which editorialists, psychologists and sociologists confronted each other. Then, with the same clamor, doctors spoke of dangerous side effects: strange blue tinge in vision, sudden infarction just in the face of overwhelming passion.

Sildenafil was passed sometimes wrong and hasty judgments on, especially by non-practitioners. After almost twenty years we can say that sildenafil has definitely passed the exam. Is it a drug like another and if it is to improve the quality of life of many men, why not take it?

There is a great resistance from physicians to prescribing this drug and patients a kind of shyness in expressing their need to family physicians. The substance definitely offers a better quality of life to those who have erectile dysfunction problems. This disorder can also be determined by the environmental situation in which you live. Even the stress of everyday life greatly affects the performance of a satisfying sexual life. Many people fail to have a normal sexual life and then when they are on vacation they are a perfect partner.

Many men take sildenafil as a means to improve sexual temperament, but the substance does not work in such a way. Sildenafil provides a controllable and lasting effect over time but is not ‘automatic’ as an intracavernous injection. This means that to have an erection, man should still be subjected to an erogenous stimulus, otherwise nothing happens. In addition, as a result of blood flow to the penis, man may have a second erection after ejaculation and many patients report to achieve better performance even the day after taking sildenafil. That means the drug helps those who have problems but does not replace mental stimulation.

The problem with recreational abuse of sildenafil pills is that patients take the drug without talking to a healthcare specialist first. This practice is fraught with hidden dangers of overlooking possible contradictory conditions that would make the use of sildenafil detrimental.

Sildenafil has a lot to do with side effects. Actually, patients at risk are well identified. These are those who suffer from severe heart failure, for whom intense sexual activity is also not recommended or are being treated with coronary-dilatatory drugs. Vascular and cardiac side effects may only affect predisposed persons, and in particular cardiopaths and diabetics. It is a small part of the male population. There is also the so-called over-boosting effect, which is not risky for the health, which tells healthy subjects who take sildenafil to have better sexual performance.

Additionally, it is not always easy to see if erectile disorder is psychological or organic. But is it really necessary to make this difference? Why, in the absence of well-founded suspicions of a major organic disease, the cause must be subject to formal, often long, expensive and rarely useful study, when a tablet can help resolve the inconvenience? After all, regardless of origin, both organic and psychological, the result is the same: a serious problem for the man who suffers from this disorder.

So how to make sure that you qualify for sildenafil use? Talk to your doctor, who will proceed from your objective physiological condition and will take several tests to confirm the diagnosis. But if you genuinely cannot achieve a stable erection, if you have a sexual desire that you cannot realize it because of a problem that is solvable, sildenafil has excellent chances of helping you. There have been improvements in the quality of life of many men, not just the elderly.

Surely those who are ahead with age have a greater desire to regain lost power, but there are also many mature men who just want to regain the vigor of 20 years. In addition, in younger subjects, sildenafil has also had good results in controlling premature ejaculation. This is not found in the directions or in the package leaflet instructions, but it is commonly prescribed by healthcare specialists to patients with Premature Ejaculation. In particular, at Smart Canadian Pharmacy you can find a combined drug Viagra Super Force containing sildenafil and dapoxetine, jointly targeting the problem of PE.

Smart Canadian Pharmacy www.smartcanadianpharmacy.com emphasizes the importance of receiving a proper medical consultation. It often happens that the general practitioner requires a proper andrological visit for the patient before prescribing the product. It is above all the family doctor who knows the person well and the situation as a whole, to assess whether it is the case or not to prescribe the medication. Why can the doctor prescribe morphine if the patient has the pain, sleep medication if he has sleep disorders, antidepressant if needed, and not the drug that will help him in case of erectile deficiency? The family physician must be given the moral and professional responsibility of a decision that has not only a clinical but also a psychological edge.

Sildenafil alternatives

Before sildenafil invention in 1997, the only possible way to help the patient with erectile dysfunction had been the injection into the penile of a vasodilator drug. The injected medicinal substance causes an erection within a few minutes irrespective of the circumstances. Sildenafil’s ‘revolution’ lies in the fact that it facilitates a process that must be mediated by an erogenous stimulus.

Since that time, surgery made some progress. Today the results of the surgery are not comparable to those of 20 years ago: more than 50% of young people, after a radical surgery for prostate cancer, resumes normal sexual activity over 12 and 18 months.