Vardenafil for ED and PAH Therapy: Applications, Side Effects, Dosages

Vardenafil has made its name as one of the main competitors of Viagra. Arguably, this is a more efficient drug when it comes to treat a complex of sexual dysfunctions including erectile dysfunction and premature ejaculation. Vardenafil has been a very successful under several brands most notably Levitra, Staxyn, and Vivanza. Developed independently by several huge international pharmaceutical corporations, the compound has made impact across the globe. In order to evaluate its efficiency and compare it to its direct competitors like tadalafil or sildenafil, we must understand how it works and why it is so popular as an erectile dysfunction drug.

First synthesized in 1994, the compound has been immediately identified as a very strong PDE5 inhibitor which was similar to sildenafil which had been going through clinical trial at that time. There were three main companies that were involved in the development of the drug. All three of them received major rights to distribute the drug under the brand of Levitra later on. After a series of clinical trials, the drug was approved by FDA in 2003 and started its quite successful movement through the North American market in 2004.

Vardenafil is a safe compound that works just like sildenafil, but has a slightly different molecular structure and may behave slightly differently in some individuals. The reaction is mostly metabolic resulting in a longer or shorter period of activity of the drug in the body. Even molecular structure differences are minor, but the piperazine ring is from an ethyl group. This does not change vardenafil’s mechanism of action.

Due to its similarity to other PDE5 inhibitors namely tadalafil and sildenafil, vardenafil has the same indications and adverse effects as other drugs from the PDE5 inhibitors group.

The Mechanism of Action

Vardenafil works similarly to other PDE5 inhibitors. Its physiological effect is based on the enhanced rate of production of NO or nitric oxide. This compound is an important participant of certain biological processes in the body namely the regulation of vasculature of the tissues called corpus cavernosum. These sponge-like tissues inside the penis are responsible for erection by filling up with blood. Nitric oxide is necessary for the increase of guanylate cyclase enzyme which is a catalyst that encourages the organism to rapidly produce more cGMP which is an abbreviation for cyclic guanosine monophosphate, a special microelement that relaxes blood vessels and their muscles.

Due to the relaxation, blood vessels transport more liquid and allow penile tissues to soak in blood faster. This leads to a stronger maintainable erection that occurs due to sexual stimulation and happens naturally. Note that without sexual stimulation there can be no erection.

Just like any other PDE5 inhibitor, vardenafil helps in overcoming physiological reasons of impotence, but not psychological ones. When the cause of sexual disorders has a psychological nature, combining together certain antidepressants and vardenafil can be efficient.

Another important part of the mechanism of action is that vardenafil is a vasodilator. It lowers the blood pressure and this is something that you need to be aware of when talking any type of PDE5 inhibitors. Using it together with other nitrites, nitrates, and/or alcohol can be quite dangerous for your organism. Unlike other PDE5 inhibitors like tadalafil, vardenafil is not distributed as a drug against arterial hypertension or essential hypertonia.

Medical applications

While other PDE5 inhibitors are often used to treat issues that are not related to erectile dysfunction, vardenafil is generally recommended as a drug against certain sexual disorders like premature ejaculation and erectile dysfunction. Tadalafil is often branded as ADCIRCA and prescribed for high-blood pressure and arterial hypertension. At the same time, some doctors prescribe it in cases when erectile dysfunction is paired with BPH (benign prostate hyperplasia).

Vardenafil is prescribed mostly as an effective drug against erectile dysfunction that can help to get rid of impotence. It is not a recreational drug and should be used mostly as a when-needed medication and a temporary mean of treatment. Many erectile dysfunction treatment drugs are used as a temporary solution with tadalafil being a recreational drug. However, one of the most attractive traits of vardenafil is that it is more effective compared to some other PDE5 inhibitors and dissolves in the body quickly enough to ensure that there is no intoxication.

Is certain scenarios, the drug can be prescribed as an effective way of treating premature ejaculation. While in the vast majority of cases premature ejaculation is a psychological problem and rarely can be named a genuine problem, some men have problems with Premature Ejaculation. In such cases, dopamine production enhancers are usually prescribed, but vardenafil can be efficient as well. Various clinical tests have shown that vardenafil has a strong effect and notably prolongs the average length of a sexual intercourse. Unlike other PDE5 inhibitors it can make sexual experience richer due to its potential to significantly prolong the time you can maintain erection.

A specific study conducted by Italian medics who partnered with Vivanza manufacturers managed to conduct a thorough study involving over 600 patients who enrolled into a 16-week long experiment that tried to find empirical evidence that vardenafil is indeed effective in cases of PE. Both placebo and non-placebo groups shown improvements, but those patients who used the drug showed statistically significant improvements to their sexual experience and reported that they could better control their sexual intercourses. The average length of the intercourse increased by roughly 2 minutes for those who used vardenafil.

Drug interactions

Vardenafil works similarly to many other PDE5 inhibitors which means that it interacts negatively with the same drugs as sildenafil. Consider avoiding vardenafil when you use any of the following:

  • Nitrites (poppers) that are usually distributed as aphrodisiacs. The work as strong vasodilators and often lower the blood pressure. The same goes for nitrates. Do not mix together NO based drugs and vardenafil.
  • Other erectile dysfunction treatment drugs. The vast majority of effective erectile dysfunction drugs are based on either tadalafil or sildenafil which are also vasodilators and strong PDE5 inhibitors.
  • Avoid mixing vardenafil with certain antibiotics and anti-angina drugs that can be prescribed to you.
  • Vardenafil should be carefully used with alpha-blockers that usually prescribed for benign prostate hyperplasia. Alpha blockers also lower the blood pressure. Consult with your doctor before mixing them with any PDE5 inhibitor.
  • Carefully with drugs like amiodarone which are prescribed to alter your QT interval which is notably affected by vardenafil.

That it is highly dangerous to mix any prescribed medication with alcohol and drugs, but vardenafil combined with alcohol is a sure way to a life-threateningly low level of blood pressure. While drinking a small amount of wine is fine, do not try to wash down your vardenafil with a shot of vodka. This may end terribly.

Other contradictions

There are certain medical conditions that prevent you from taking vardenafil. Again, as any other pDE5 inhibitor, vardenafil has certain limitations and should not be used when you have any of the following medical conditions:

  • A history of strokes or heart attacks;
  • Recovering from a stroke or a heart attack;
  • Heart, liver, and/or kidney related diseases;
  • Problems with blood (anemia, hemophilia, bleeding);
  • Physical deformity of the penis;
  • Stomach ulcer;
  • Specific allergies like an allergy for sildenafil.

Side effects

Vardenafil may cause a variety of adverse effects which you should be aware of before starting using it. Note that the vast majority of the effects are temporary and do not threaten your health. However, there are dangerous side effects.

However, there are dangerous side effects. Amongst the most common mild side effects:

  • Redness of the skin;
  • Flushing;
  • Stuffy nose or runny nose;
  • Dizziness;
  • Back pains and muscle pains;
  • Lowered blood pressure;
  • Headaches, pains in the back of the head;
  • Changes in vision (color changes) and in extremely rare cases temporary loss of vision;
  • Changes in hearing and in extremely rare cases a sudden loss of hearing.

That for vardenafil the occurrence rate of muscle and back pains is much lower compared to sildenafil. These side effects are common and wear off within several hours after the intake and do not threaten your health. However, there are side effects like priapism. This is an extremely rare condition when the erection does not go away after the intercourse. When the erection remains after 3 hours, start seeking for medical attention to prevent further damage!

Dosing and Administration of Vardenafil

There are various types of dosing that can be used. Note that vardenafil is a when-needed drug and the dose for each individual should be adjusted depending on how well the organism reacts to the drug. While 5mg before an intercourse is usually a sufficient dose in the vast majority of cases, in more severe cases of erectile dysfunction stronger dosage may be more effective. Changing the dose to 2.5mg is recommended when used together with alpha-blockers. Changing to a larger dose may be recommended when the drug seemingly does not work.

The only way of administration is oral. There are no empiric evidences that other form factors rather than tablets are effective. The drug works perfectly fine in a pill form.

Additional notes and information

Note that vardenafil is a drug that is administered orally and thus should be taken on an empty stomach for the best result. Taking it with food does not negate the effect, but it may occur slower. Usually, vardenafil takes 20-30 minutes to activate in the body. Eating before taking a pill may slow down the effect and it may take up to one hour for the drug to start working.

Vardenafil is a strong vasodilator and increasing the dosage without talking to your doctor can be dangerous. Do not increase the dose since it won’t improve the effect of the drug and won’t intensify it. This means that PE or ED treatment will not be better with an increased dosage. An organism either responds to the treatment or does not respond.

In specific cases, using vardenafil may be inefficient. Certain individuals simply do not respond to the treatment. In such scenarios, using PDE5 inhibitors in general may be inefficient. Roughly 2% of men do not respond to the drug. The success rate of the medication is very high and hovers near the 80% mark.

Vardenafil compared with sildenafil

For a long time, there were hardly any effective drug treatments for persistent erectile dysfunction. In 1998, this was changed when the drug sildenafil (Viagra) was the first PDE5 inhibitor to enter the market. Today, several different medications are available for the treatment of erectile dysfunction, and all of these help at the cellular level the patient to achieve and maintain an erection.

Two of the active substances that have this effect are vardenafil (Levitra) and sildenafil (Viagra). Both PDE5 inhibitors have their own specific properties, but essentially they have identical effect. All PDE5 inhibitors are taken orally in tablet form.

Erectile dysfunction (impotence) is defined as a condition when at least 70 percent of all planned sexual activities are not realized because the penis is not rigid or the erection does not last long enough.

Approximately 1 million US men are estimated to be affected and the risk of erectile dysfunction increases with age. While only a few percent in the age group 30 to 39 years are affected, the number has increased markedly when men are in the age group 50 to 59 years. In about 70 percent of cases, the causes of erectile dysfunction are of a physiological nature. These include, for example, circulatory disorders, metabolic diseases or a generally unhealthy lifestyle that causes these erectile dysfunction. Psychic triggers of sexual function problems include stress and relationship conflicts. For the affected men and their partners, impotence can be very difficult.

For men who wish to treat sexual function problems, PDE5 inhibitors are a very effective treatment method. They widen the blood vessels in the penis and affect at the cellular level the mechanism responsible for creating erections. A condition that PDE5 inhibitory drugs should have an effect is the incidence of sexual stimulation and individual response to this.

Both vardenafil and sildenafil increase blood flow to the penis and allow its swelling bodies to be filled with blood, which causes an erection. Cyclic guanosine monophosphate (cGMP) lowers the potassium levels in the muscle cells, so the smooth muscle of the penis becomes relaxed and allows the blood to flow freely. The erection lasts as long as the cGMP level is high enough to prevent the constriction of the arteries in the penis. This happens as soon as the body’s enzyme phosphodiesterase type 5 (PDE5) begins to lower the levels of cGMP in the body. In erectile dysfunction, the interaction between these two subjects is out of balance, which gives the PDE5 the upper hand.

PDE5 inhibitors like sildenafil and vardenafil restore the balance between cGMP and PDE5. As a result, they increase the power and durability of the erection. During the duration of the drug, multiple erections are possible without taking more tablets. Degradation of PDE5 inhibitors is done by means of liver enzymes. Residues are secreted by the liver’s metabolism and kidneys.

The American pharmaceutical company introduced 1998 sildenafil (Viagra) on the market. At the time, the new drug was celebrated as a revolution. Nowadays, there are also generic versions of sildenafil with sildenafil. These differ only from the original by a lower price, another tablet form and another color.

Viagra with the active substance sildenafil is available in doses of 25, 50 and 100 milligrams. The standard dose is 50 mg and this dose helps over 60 percent of users overcome their erection problems. The tablets should be taken between 30 and 60 minutes before a planned intercourse. If the tablet is taken after a meal, the effect of the drug can be delayed and weakened slightly. The highest concentration of sildenafil in the blood plasma is reached after approximately one hour. The effect of sildenafil lasts for about four to five hours. During this time no additional tablet should be taken.

The following side effects are possible when using sildenafil:

Very common: headache, body aches, strong redness in the face or on the upper body, diarrhea and indigestion

Common: dizziness, bloodshot eyes, influenza, bronchitis, cough, changed blood test results, insomnia, visual impairment (e.g. impaired color vision, blurred vision, sensitivity to light or decrease of vision and double vision), eye irritation and pain in the eyes, runny nose, nasal congestion, sinusitis, anemia, bleeding, water retention, anxiety and nervous tension, migraine, weight gain, dangers, numbness, inflammation of the stomach or intestine, bloating, heartburn, pain in the muscles, alopecia (hair loss in men), fever.

Rare: hypersensitivity, disease, too high (hypertension) or low blood pressure (arterial hypotension), arrhythmias, myocardial infarction, sudden cardiac death, angina, impotence, nosebleeds, loose and / or painful erection.

Sildenafil should not be used by people under the age of 18, patients with cardiovascular disease, people who have recently had a heart attack or stroke, people with low blood pressure, people who have liver problems or eye diseases, as well as people who are allergic to sildenafil or any of the excipients in sildenafil.

Vardenafil with the active substance vardenafil has been developed by a German pharmaceutical company and was released on the market in 2003. Vardenafil is available in doses of 5, 10 and 15 milligrams. If you have eaten very fat food, the effect of the medicine may be slightly reduced.

The tablets are taken approximately 15 to 30 minutes before scheduled sexual intercourse. The highest concentration of vardenafil in the blood plasma is reached after approximately one hour. Vardenafil effect lasts for about four to five hours. During this time no additional tablet should be taken.

The following side effects are possible with vardenafil:

Usual: headache, dizziness, changed blood pressure, indigestion, clogged or runny nose, facial flushing;

Less common: back pain, body aches, muscle stiffness, increased muscle enzyme in the blood, reflux of stomach acid, stomach pain, nausea and vomiting, diarrhea, swelling in the mouth and throat, swelling on the face and on the lips, insomnia, palpitation, difficulty breathing, eye pain and sensitivity to light, ringing in the ears, long-lasting erections;

Vardenafil should not be used in case of allergy to vardenafil or any of the excipients in the medicine. It should also not be used by people taking medicines containing nitrates, indinavir or ritonavir, have serious cardiovascular or liver problems, dialysis, or stroke or heart attack in the past year.

Note: As a disclaimer, we should mention that this article was created with the intention of providing educational materials. It cannot be viewed or used as a substitute for professional medical advice. We are not responsible for any health concerns.