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Avanafil (active ingredient)

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What is Avanafil?


Avanafil is the active ingredient in Stendra. Avanafil is a prescribed drug that is used to treat erectile dysfunction (ED), also known as impotence, which is the inability to get or maintain an erection satisfactory for intercourse.

Avanafil (Stendra) was approved by the U.S. Food and Drug Administration (FDA) in 2012 for the treatment of ED and is available in three dosages: 50 milligrams (mg), 100 mg, and 200 mg.

Avanafil is a new, second-generation ED medication. Compared to first-generation ED treatments, such as Sildenafil (Viagra), Avanafil has a higher selectivity (specificity) and affinity for the PDE-5 enzyme. This results in higher peak levels in patients in less time, promoting an erection in a shorter amount of time, typically within 15-30 minutes after oral ingestion. Avanafil also has a reduced side effect profile compared to first-generation ED medications.




How does an erection occur?


The process of achieving an erection is complex. The first step is for a man to experience sexual arousal or an erotic stimulus. This arousal signals a cascade of events that relaxes cavernosal artery smooth muscles in the phallus. Parasympathetic nerves in the phallus release nitric oxide (N.O.), which increases cyclic GMP (cGMP), decreases intracellular calcium levels, and enhances smooth muscle relaxation. The relaxation of smooth muscle in the phallus allows for an influx of arterial blood, increased intracavernosal pressure, and erectile expansion and rigidity. Increased venous outflow, a passive process, maintains the phallus in an erect state.

When arousal has subsided, sympathetic nerves release norepinephrine, which stimulates alpha-adrenergic receptors. The resulting smooth muscle contraction causes the erection to reduce in size in rigidity.




How is phosphodiesterase (PDE) important for erectile function?


Nitric oxide and cGMP are essential components for smooth muscle relaxation in the phallus and vascular dilation. Without enough nitric oxide or cGMP, not enough blood can flow to the phallus for an erection.

Phosphodiesterase (PDE) enhances the breakdown of nitric oxide (N.O.) and reduces the presence of cGMP. There are several types of PDE enzymes, but PDE-5 is the primary PDE enzyme in the male phallus. By preventing or inhibiting PDE-5, cGMP can maintain blood flow by increasing N.O. to the phallus, promoting an erection.

All oral ED medications, including Avanafil (Stendra), are PDE-5 inhibitors. Avanafil is unique and has a higher selectivity for the PDE-5 enzyme compared to other ED medications, as well as a reduced affinity for other PDEs found throughout the body, including PDE-1, PDE-3, PDE-6 and PDE-11. This unique selectivity provides a lower side effect profile of the medication and faster onset of action.




What causes erectile dysfunction?


Erectile dysfunction is the inability to obtain or maintain an erection that is strong enough for sexual activity, including sexual intercourse. Approximately 52% of men older than 40 years old and 26% of men less than 40 years old have some degree of erectile dysfunction.

Many situations can interfere with a normal erectile function, including stress, depression, anxiety, low testosterone, smoking, physical inactivity, and the use of alcohol and/or drugs.

Other causes for ED can include an underlying cardiovascular condition or atherosclerosis. For example, obstructed or narrowed blood vessels can make it difficult for an erection to occur.




How does Avanafil work?


The purpose of Avanafil is to relax restricted or narrowed blood vessels and relax smooth muscles in the phallus in order for an erection to be achieved. Avanafil specifically aims to address blood vessel-related erectile dysfunction by enhancing blood flow, relaxing cavernosal smooth muscle and increasing intracavernosal pressure resulting in a firm, rigid, and natural erection.

The results of several clinical trials show Avanafil to be a more effective and quicker on-demand treatment for ED compared to other ED medications. In one study, approximately 70% of men reported the ability to get an erection in a little as 15 minutes after taking Avanafil. The medication was also shown to be effective for up to six (6) hours when needed. Other studied found that patients taking 200 mg of Avanafil (the approved maximum dosage) had higher rates of orgasmic function, sexual desire, and intercourse satisfaction.




What is the difference between Avanafil and Stendra?


Avanafil is the active ingredient in Stendra. (There are several inactive ingredients, too.) Stendra is a brand name of the drug, whereas Avanafil is the generic ingredient that can often be obtained in compound or at a more affordable price. Stendra is specifically marketed for the on-demand treatment of ED.




What is the best way to use Avanafil for ED?


The best way to take Avanafil is 30 minutes prior to sexual activity, with or without food, starting at a low dose. If taking Avanafil 15 minutes before sexual activity, and no response is achieved, you may increase the dose up to 200 mg. Swallow the medication whole or allow it to dissolve underneath your tongue.




How does Avanafil differ from other ED medications?


There are four types of oral PDE-5 inhibitors that help treat ED and are currently approved by the U.S. Food and Drug Administration (FDA). These PDE-5 inhibitors work along the same pathway in the penis to promote smooth muscle relaxation and blood vessel dilation by increasing nitric oxide (N.O.) in the penis. These drugs work in the same way, but differ in immediacy of action, half-life, side effect profile, and other characteristics. These slight differences may benefit some men and be ineffective for others.

Avanafil (Stendra) is part of the second generation of PDE-5 inhibitors for ED treatment.

The biggest difference between Avanafil and other PDE-5 inhibitors is that Avanafil is the most selective for the PDE-5 enzyme. Avanafil’s higher affinity for the PDE-5 enzyme results in less side effects, faster onset of action, and better tolerability.

The most common side effects of using Avanafil include headache and flushing, and are reported in fewer than 14% of patients. The drug’s composition makes it particularly effective for men with ED who have seen little to no success from other ED treatments. Avanafil has an average onset of 15-30 minutes for maximum benefit. You may take Avanafil with or without food, though a high-fat meal can slow its onset time, and with a moderate amount of alcohol.

A doctor will assess your current health and your potential side effects when considering what type of ED medication is best for you. You may also have some input when choosing.





Safety Information

What are the common side effects of Avanafil?


Avanafil can cause a sudden drop in blood pressure. When combined with other specific medications, your blood pressure can drop to particularly unsafe levels, resulting in dizziness, fainting, and even a heart attack or stroke. Seek immediate medical help if this occurs.

Other common side effects include:

  • Headache
  • Flushing
  • Indigestions
  • Runny or stuffy nose

These side effects generally decrease over time, going away altogether within a few hours.

You may also experience back or muscle aches within 12-24 hours of taking Avanafil. These aches typically go away completely within two (2) days.

Sexual activity can strain your heart, particularly if previous heart issues such as heart disease or a heart attack have already weakened your heart. If you experience chest pains, dizziness, or nausea during sexual activity, stop right away and seek professional medical help immediately.




What are the uncommon side effects of Avanafil?


Uncommon side effects of Avanafil may include, but are not limited to, the following:

  • An erection lasting longer than four (4) hours. Known as priapism, an erection that won’t go away must be treated as soon as possible to avoid longterm damage, including the inability to have an erection.
  • Changes in color vision. You may see a blue hue or have difficulty differentiating between blue and green colors.
  • Sudden decrease in or loss of vision. In particularly rare instances, men taking Avanafil or other ED medications may have a sudden decrease in or loss of vision in one or both eyes. If you experience a sudden vision decrease or loss, stop taking Avanafil and seek immediate medical help.
  • Sudden decrease in or loss of hearing. Ringing in your ears and/or dizziness may accompany a sudden decrease in or loss of hearing, though it is rare. If you experience a sudden hearing decrease or loss, stop taking Avanafil and seek immediate medical help.




What should I avoid while taking Avanafil?


Combining alcohol with Avanafil may cause side effects, especially if you are drinking more than the recommended amount.

Combining grapefruit or grapefruit juice with Avanafil can result in unwanted side effects.




How long does Avanafil stay active in my body?


One tablet of Avanafil contains active ingredients that may stay in your body for up to or past two (2) days. Other medications you may be on, especially for kidney or liver health, can cause the active ingredients to linger longer than two days.




Who should not take Avanafil?


Avanafil is not right for everyone. Only your healthcare provider and you can decide if Avanafil is right for you. Only those who have specifically been prescribed Avanafil should take it. Never share Avanafil with others, even if their symptoms are similar, as it may cause serious harm.

Women and children under the age of 18 should never take Avanafil.




Who should I contact if I have a reaction to Avanafil?


If you experience serious side effects such as fainting, heart attack, loss of vision or hearing, or significant allergic reaction, seek immediate medical help.

Contact your physician or professional health care provider if you have questions about Avanafil.




What is the best way to store Avanafil?


Keep Avanafil at room temperature, between 59°F and 85°F (15-30°C). Always store Avanafil and all medications out of reach from children.




What medications interfere with (are contraindicated) Avanafil?


Do not take Avanafil if you are currently taking other ED medicines or treatments, including Stendra, as these effects have not been studied.

Do not take Avanafil if you are currently taking any medications known as “nitrates”. Nitrates are often used to treat angina, a symptom of heart disease, that can result in pains in your jaw, chest, or arm. Ask your physician or healthcare provider if any of your other medications are nitrates. Nitrates may also be found in medicines including:

  • Isosorbide dinitrate
  • Isosorbide mononitrate
  • Recreational drugs known as “poppers”, which often contain nitrites called amyl nitrite or butyl nitrite

Do not take Avanafil if take any medication known as “guanylate cyclase stimulators”, which include Riociguat (Adempas), a drug that treats pulmonary hypertension and chronic-thromboembolic pulmonary hypertension.

Other medications that can affect how you handle Avanafil include:

  • Medicines known as “alpha blockers”, which can be prescribed for prostate problems and/or high blood pressure, among other issues. Combining alpha blockers with Avanafil can result in dizziness or fainting. Alpha blockers may include, but are not limited to the following:
    • Cardura, aka doxazosin mesylate
    • Flomax, aka tamsulosin HCl
    • Hytrin, also known as (aka) terazosin HCl
    • Jalyn, aka dutasteride or tamsulosin HCl
    • Minipress, aka prazosin HCl
    • Rapaflo, aka silodosin
    • Uroxatral, aka alfuzosin HCl
  • Medicines that treats high blood pressure (hypertension)
  • Nizrola, aka ketoconazole and Sporanox, aka itraconazole
  • Some types of antibiotics, including:
    • Biaxin, aka clarithromycin
    • Ketek, aka telithromycin
    • Erythromycin, aka several brand names
  • Medicines known as “HIV protease inhibitors”, including
    • Norvir or Kaletra, aka ritonavir
    • Crixivan, aka indinavir
    • Fortavase or Invirase, aka saquinavir
    • Reyataz, aka atazanavir
  • Some types of antifungals, including:
    • Nizoral, aka ketoconazole
    • Sporanox, aka itraconazole




Can I take Avanafil if I am allergic to Stendra?


No. If you have had an allergic reaction to Stendra, do not take Avanafil. Allergic reactions can include:

  • Hives
  • Rash
  • Swelling of your lips, throat, or tongue
  • Difficulty breathing or swallowing




What does my healthcare provider need to know before I take Avanafil?


Avanafil is not right for everyone. Only your healthcare provider and you can decide if Avanafil is right for you. Your physician or healthcare provider must know all medications and non-prescription drugs or medicines you are currently taking.

Ask your healthcare provider if your heart is healthy enough for you to have sexual activity. You should not take Avanafil if your healthcare provider has told you not to engage in sexual activity due to health problems. Before taking Avanafil, tell your healthcare provider about all your medical problems, particularly if you have ever had:

  • Heart surgery in the last six (6) months
  • Previous heart issues, such as irregular heartbeats, angina, heart failure, or heart attack
  • Pulmonary hypertension
  • Low blood pressure
  • High blood pressure that is not currently under control
  • Stroke
  • Liver problems
  • Kidney problems and/or required dialysis
  • Retinitis pigmentosa (a rare eye disease)
  • Severe vision loss, including a condition known as NAION
  • Stomach ulcers
  • Bleeding problems
  • Deformed penis shape and/or Peyronie’s disease
  • History of priapism (an erection that’s lasted for longer than four (4) hours)
  • Blood cell problems, such as multiple myeloma, sickle cell anemia, or leukemia

In the case of an emergency medical situation related to your heart, you must disclose the last time you took Avanafil.




Warning for Airplane Pilots


The U.S. Federal Aviation Authority approves the use of Avanafil (Stendra) for the treatment of ED in its pilots. However, pilots may not use Avanafil within eight (8) hours of pilot duties.

The FAA also restricts the use of other ED medications for pilots.





Avanafil FAQs

Can I take Avanafil for ED?


Yes, Avanafil is used for the treatment of erectile dysfunction in men.

Compared to other erectile dysfunction meds Avanafil has a faster onset of action, reduced side effect profile, and better tolerability. Avanafil is a second-generation class of PDE-5 inhibitor and the dosage can be titrated higher to obtain the desired erectile response.




Can I take Avanafil for BPH?


No. Only Tadalafil (Cialis) for daily use been approved for the treatment of BPH.




How should I take Avanafil?


Take Avanafil exactly as prescribed by your physician or healthcare professional. A dose of 100 milligrams (mg) is standard, though your physician may increase dosage up to 200 mg or decrease as low as 50 mg based on your initial and longer-term tolerability and efficacy.

Do not take Avanafil more than once per day. Do not break or split an Avanafil tablet unless instructed by your health care provider; swallow it in its entirety, unless otherwise instructed by your healthcare provider. Do not use other ED medicines or treatments while taking Avanafil.

Avanafil is typically prescribed for use as needed. In this situation, always take the lowest effective dose: take your prescribed Avanafil dosage 15 minutes before sexual activity. If taking 30 minutes before, you may lower the dosage.

Never share Avanafil with others, even if their symptoms are similar, as it may cause serious harm.




When is the best time to take Avanafil before sex?


When taking Avanafil on an as-needed basis, take one tablet before expected sexual activity. Generally, Avanafil provides maximum sexual benefit 15-30 minutes after taking the tablet.

Despite taking Avanafil as prescribed, sexual stimulation is still necessary for an erection.




Can Avanafil improve my sexual desire?


Avanafil will not improve your desire for sexual activity or cure ED. A man’s sexual desire is only one of the many functions of testosterone. A low testosterone level can decrease a man’s desire for sexual activity. Avanafil does not protect from sexually transmitted diseases (STDs). Avanafil is not a form of birth control for men.




Should I take Avanafil with food?


You may take Avanafil with or without food, though a high-fat meal can prevent the medication from reaching its full potential and efficacy.




Can I take Avanafil and drink alcohol?


Do not take Avanafil with more than a moderate amount of alcohol. Avanafil can still be effective after three (3) alcoholic drinks, though the Centers for Disease Control and Prevention generally recommends no more than two (2) alcoholic drinks per day for men. One drink is generally defined as 12 ounces of a regular beer (approximately 5% ABV), 5 ounces of wine, or 1.5 ounces of distilled spirits (such as vodka, whiskey, gin, tequila, etc.).

Drinking too much alcohol can increase your odds of a headache, dizziness, elevated heart rate, or lower blood pressure and reduce the efficacy of the medication.





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Disclaimer: The content on this website is not medical advice or a substitute for professional medical care, diagnosis or treatment. Your physician will determine if you are a candidate for therapy and advise how you should take the medication.

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