Viagra for pulmonary hypertension: 200 shocking truths

What is Pulmonary Hypertension (PH)

The condition when the blood pressure within the arteries of your lungs increases is called as Pulmonary Hypertension. It is often a serious health issue and can be life-threatening. In this condition, the blood vessels that carry blood from your heart to your lungs become narrowed, thickened or stiff.

The right side of your heart has to work harder to pump the blood through these narrowed arteries. This extra stress can result your heart to lose its ability to pump enough blood through the lungs to meet the requirements of the rest of the body. Over time, your heart becomes weaken and thus, you can develop heart failure.

What are the symptoms of PH?

The symptoms of pulmonary hypertension include the following:

  • Shortness of breath during routine activity, such as climbing flights of stairs. This becomes severe with the increase in the activity.
  • difficulty breathing with exertion
  • Fatigue/ Tiredness
  • lethargy
  • dizziness
  • rapid breathing
  • People may also complain of chest pain and angina.
  • Palpitations (heartbeat rate increased)
  • Pain on the upper right side of the abdomen
  • Poor/ decreased appetite
  • Lightheadedness
  • Chest pain, pounding of the heart and fainting are less common but can occur with the worsening of this disease.
  • With the expansion of this condition and resulting right heart failure, shortness of breath may become worse and retention of fluid in your body may increase (due to failure of the heart to pump blood forward) resulting in swelling in the legs.
  • Hypoxia (low oxygen level in the blood)
  • Rarely, patients will cough up blood or have a change in their voice.

As pulmonary hypertension advances, you may find it hard to do any physical activities.

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Groups of pulmonary hypertension

There are 5 main groups of pulmonary hypertension, as it can be caused by different things.

Group 1: Pulmonary Arterial Hypertension: PAH is characterized by progressive scarring of the tiny blood vessels going to the lungs. A number of diseases and conditions can cause this scarring including: connective tissue disorders like scleroderma and lupus; exposure to certain toxins and drugs, including methamphetamine and cocaine; infections, including HIV and schistosomiasis; cirrhosis of the liver; and congenital heart abnormalities.

Group 2: pulmonary hypertension due to left heart disease

Group 3: pulmonary hypertension due to lung disease and/or chronic hypoxia

Group 4: pulmonary hypertension due to blood clots in the lungs

Group 5: pulmonary hypertension due to blood and other disorders

Phosphodiesterase-5 (PDE-5) inhibitors, such as sildenafil, have been approved for treatment of pulmonary arterial hypertension (PAH), which holds promise in improving quality of life and therefore making this class of medications effective palliative therapy agents.

In this article, we summarize the emergence of sildenafil as a treatment for PAH and its role as palliative therapy.

What Causes Pulmonary Arterial Hypertension?

PAH is characterized by progressive scarring of the tiny blood vessels going to the lungs. A number of diseases and conditions can cause this scarring including: connective tissue disorders like scleroderma and lupus; exposure to certain toxins and drugs, including methamphetamine and cocaine; infections, including HIV and schistosomiasis; cirrhosis of the liver; and congenital heart abnormalities.

When the cause of PAH is unknown, it is called idiopathic pulmonary arterial hypertension.

What Are Risk Factors?

You are more likely to get pulmonary arterial hypertension if you are a young female, since the idiopathic form of the disease occurs more often in women of childbearing age than in men. There is an inherited form of PAH, so a family history of the disease may put you at increased risk for this disease.  

Patients with diseases like lupus, scleroderma, cirrhosis of the liver, and HIV infection can develop it as well. Use of methamphetamine and cocaine increase the risk for developing this disease.

Is there a cure for pulmonary hypertension?

There are two main kinds of PH. One runs in families or appears for no known reason. The other kind is related to another condition, usually heart or lung disease.

Despite advances in various treatments, there is no cure for pulmonary hypertension. Treatments can control symptoms. These new treatments which have emerged for past 2 decades has led to improvement in the functional status and time to clinical worsening of this disease.

These methods involve treating the heart or lung disease, medicines, oxygen, and sometimes lung transplantation.

Viagra is now being used to treat not only erectile dysfunction (ED) but also pulmonary arterial hypertension. Viagra is now marketed under the name Revatio for this uncommon but serious disorder of high pressure in the blood vessels leading to the lungs.

What is sildenafil?

Sildenafil is an oral medication called a phosphodiesterase-5 (PDE5) inhibitor approved for the treatment of pulmonary arterial hypertension (PAH) in World Health Organization (WHO) Group 1 patients.

The goal of this therapy is to improve exercise ability and delay clinical worsening. Sildenafil is marketed as Revatio for PAH. Sildenafil is also marketed as Viagra which is approved for the treatment of erectile dysfunction but not for the treatment of PAH.

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How does sildenafil work in treating PAH?

PDE5 is a substance produced in the lungs and other parts of the body that breaks down another substance called cyclic guanosine monophosphate (GMP). Cyclic GMP causes the blood vessels (arteries) to relax and widen.

Sildenafil is a PDE5 inhibitor which means it decreases the activity of PDE5, so that more cyclic GMP is available for the blood vessels inside the lungs. This leads to relaxation, or widening of those vessels. Relaxing and widening of the blood vessels in the lungs decreases the pulmonary blood pressure to the heart and improves its function.

This reduces blood pressure in the lungs which generally results in the ability to be more active.

How is sildenafil supplied?

Revatio is only available as a round, white 20 mg pill.

Revatio injection is supplied as a single-use vial containing 10 mg (12.5 mL) of sildenafil.

How can you obtain sildenafil from the market?

Sildenafil is a prescription drug; so it must be prescribed by your healthcare professional, and insurance approval must be obtained prior to starting therapy.

What are the frequent side effects of sildenafil?

As per the information available; Sildenafil is generally well tolerated. The most frequent side effects are:

  • Headache
  • Nose bleeds
  • Upset stomach and heartburn
  • Flushing of the skin
  • Difficulty sleeping
  • Worsening shortness of breath
  • Nasal congestion.

Other side effects include:

  • Fluid retention
  • Nausea and diarrhea
  • Pain in the extremity (arm or leg)
  • Temporary muscle aches
  • Fever
  • Numbness

Precautions/ points to remember while taking sildenafil

  • This drug relaxes the blood vessels (arteries) throughout the body; hence it may cause a reduction in blood pressure throughout the body. So, if you have low blood pressure related issues; kindly inform your healthcare professional before the drug is being prescribed.
  • Caution must also be taken if you are having dehydration, left-sided heart diseases and certain abnormalities of the body’s nervous system function.
  • Taking certain medications such as nitrates, nitric oxide donors or alpha blockers along with sildenafil can cause a significant drop in blood pressure. This could result in loss of consciousness or in worst cases; even death. You should make certain that you are not taking these medications before starting sildenafil. Use of sildenafil with medications known as nitrates is strictly not advised.
  • After taking Revatio, if you have an erection that lasts more than 4 hours, consult your healthcare professional immediately. This condition can permanently damage your penis. It is a rare but very serious side effect.
  • Sudden vision loss in one or both eyes can be a sign of a serious eye problem called non-arteritic anterior ischemic optic neuropathy (NAION). Such an event may represent serious dysfunction of the optic nerve and requires immediate medical attention. Stop taking this drug and call your healthcare provider right away if you have any sudden vision loss.

How are side effects of sildenafil monitored?

No regular bloodwork for side effects is required. Your doctor may ask you to monitor your blood pressure on a regular basis particularly during your first few days on treatment or with a dose increase. Blood pressure monitoring is not needed for most patients.

If you experience any of the symptoms mentioned above, consult your healthcare professional immediately.

What are considerations for use of sildenafil in special populations?

The safety and effectiveness of sildenafil in pediatric PAH patients has not been established.

Sildenafil does not exhibit harm to the fetus in animal studies; however it has not been evaluated in pregnant women or women who are breastfeeding. It should be used in pregnant or nursing mothers only if the potential benefit justifies the risk to the fetus or infant.

Safety and efficacy in pediatric patients has not been established, and this drug should not be used in patients under 18 years of age.

Mild-to-moderate liver disease does not require a dose adjustment. Severe liver disease has not been studied.

No dose adjustment is required in patients with kidney disease.

Can you be allergic to sildenafil?

This is possible, but not likely.

What are important drug interactions with sildenafil?

  • Sildenafil should not be used in combination with nitrates or nitric oxide donors as an unsafe drop in systemic blood pressure may occur.
  • Caution should be used if sildenafil is to be used in combination with either alcohol or anti-hypertension or blood-pressure-lowering medications.
  • Sildenafil is broken down predominantly by an enzyme called CYP3A in the liver; therefore, important interactions may occur with medications that affect this enzyme pathway.
  • Simultaneous use of bosentan and sildenafil may result in increased bosentan blood levels and decreased sildenafil blood levels. It is not known if these changes are clinically significant. Although a drug interaction has been demonstrated with sildenafil and bosentan, dose adjustments are presently not recommended for either drug.
  • Patients with human immunodeficiency virus (HIV or AIDS) who are taking medicines called antiretroviral agents should not use a phosphodiesterase inhibitor such as sildenafil since it can dramatically impair the efficacy of the antiretroviral.
  • Use of sildenafil with epoprostenol may reduce the blood level of sildenafil.
  • Use of sildenafil with beta blockers (another type of heart or blood pressure medicine) may increase the levels of sildenafil.

Miscellaneous considerations:

 Is there any risk of blindness when using sildenafil?

There have been rare reports of blindness with use of all the currently available PDE5 inhibitors, including sildenafil. This type of blindness, which may be permanent, is called non-arteritic anterior ischemic optic neuropathy (NAION).

It is not yet clear whether this is related to the use of sildenafil or to the underlying cardiovascular diseases that place the persons at risk for this particular type of blindness, even in the absence of sildenafil use.

There is no research to determine whether use of sildenafil is beneficial or safe in patients with retinitis pigmentosa, and use in these patients is not recommended.

As noted above, patients taking sildenafil should seek immediate medical attention in the event of sudden vision loss.

Can men and women take sildenafil?

Yes, studies have evaluated sildenafil in both men and women with PAH, and no differences in side effects have been reported between genders. Studies have not shown any effect on sexual function in women who have taken sildenafil.

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