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Sildenafil
Viagra ®️
Sildenafil is the active ingredient in Viagra, nicknamed “the little blue pill”. Sildenafil 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
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Sildenafil is the active ingredient in Viagra, nicknamed “the little blue pill”. Sildenafil 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.
Approved by the U.S. Food and Drug Administration (FDA) in 1998, Sildenafil revolutionized the treatment of ED. One of the first generation of PFE-5 inhibitors, Sildenafil is effective in up to 80% of men with ED.
Sildenafil can have an onset of action in approximately 30 minutes, though most patients are instructed to wait at least one (1) hour before attempting sexual activity. Sildenafil’s duration of action lasts approximately 4-6 hours, though it can be effective for up to 12 hours. Sildenafil must be taken on an empty stomach. The most common side effect, among others, includes visual disturbances.
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 case 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.
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 Sildenafil (Viagra), are PDE-5 inhibitors.
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 (such as hypertension, diabetes mellitus, and hyperlipidemia) or atherosclerosis. For example, obstructed or narrowed blood vessels can make it difficult for an erection to occur.
The purpose of Sildenafil is to relax restricted or narrowed blood vessels and relax smooth muscles in the phallus in order for an erection to be achieved. Sildenafil 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.
Sildenafil is one example of a type of drug known as a PDE-5 inhibitor (phosphodiesterase). PDE-5 inhibitors prevent the breakdown of nitric oxide, a potent vasodilator that is necessary to maintain a rigid and firm erection. Taking Sildenafil typically results in increased NO in the penile cavernosal tissue and muscles, which means the penile blood vessels can stay open to receive more blood, resulting in a prolonged, stronger, more easily attained erection.
Sildenafil is the active ingredient in Viagra. (There are several inactive ingredients, too.) Viagra is a brand name of the drug, whereas Sildenafil is the generic ingredient that can often be obtained in compound or at a more affordable price. Viagra is specifically marketed for the on-demand treatment of ED.
Revatio is a drug used to treat pulmonary arterial hypertension (PAH), a condition that affects the arteries of the lungs. Like Viagra, the active ingredient in Revatio is Sildenafil, but the difference between the two is in the dosage: Revatio has a significantly lower dosage of Sildenafil than Viagra. For comparison, Revatio has 20 milligrams (mg) of Sildenafil, whereas Viagra is available in doses of 50 mg and 100 mg of Sildenafil.
The approved dose of Sildenafil for ED is 50 or 100 mg. However, many healthcare clinics and online ED clinics typically only offer Sildenafil in 20 mg doses, which is used for PAH. This can be cumbersome for men who may need 100 mg of Sildenafil for an erectile response, which means those men may be taking five (5) tablets of Revatio instead of one single tablet of Viagra. However, this smaller dosage can allow men to titrate up to their necessary amount of Sildenafil for ED, which may have some benefit.
The best way to take Sildenafil is 1 hour (60 minutes) prior to sexual activity, with or without food. Swallow the medication whole or allow it to dissolve underneath your tongue. You may take Sildenafil as early as 30 minutes prior to four (4) hours prior to sexual activity, but 1 hour is ideal for maximum benefit.
There are four types of oral PDE-5 inhibitors that help treat ED and are currently approved by the 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 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.
Sildenafil (Viagra) was the first to market, in 1998, and has been studied widely thanks to its history. It Is primarily known for its fast onset – Sildenafil can start working as quickly as 30 minutes after taking the initial dose. For maximum benefit, wait one hour until sexual activity. Typically, Sildenafil stops working about four (4) hours after taking a full dose, though its effects can last for up to 12 hours in some men.
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.
The story of Sildenafil (Viagra) is fascinating. Sildenafil for ED was discovered accidentally during research for a different medical condition.
In the 1980s, Sildenafil was studied for its potential use in treating angina, a condition characterized by chest pain secondary to reduced blood flow to the heart muscle. During the clinical trials, patients noted an interesting side effect of the medication: their erections were stronger, more spontaneous, and more easily attainable. This sparked a change in the trial to investigate Sildenafil’s potential to improve ED and the rest, of course, is history.
Take Sildenafil exactly as prescribed by your physician or healthcare professional. Standard doses are 25 milligrams (mg), 50 mg, and 100 mg. Your physician may increase or decrease your dosage based on your initial and longer-term tolerability and efficacy.
Do not take more than 100 mg of Sildenafil in one day. Do not break or split a Sildenafil tablet unless instructed by your healthcare professional; swallow it in its entirety, unless otherwise instructed by your healthcare provider. Do not use other ED medicines or treatments while taking Sildenafil.
Sildenafil is typically prescribed for use as needed. In this situation, you may take your prescribed dose of Sildenafil tablet within 30 minutes to four (4) hours of sexual activity, though 60 minutes (one hour) before sexual activity is ideal.
Never share Sildenafil with others, even if their symptoms are similar, as it may cause serious harm.
If you are taking Sildenafil on an as-needed basis, you may take one tablet before expected sexual activity. Generally, Sildenafil can help you have sex within 30 minutes and up to 4 hours after taking one dose.
Taking Sildenafil as prescribed does not guarantee an erection. Sexual stimulation and arousal are still necessary for an erection.
Sildenafil will not improve your desire for sexual activity, guarantee an erection, 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. Sildenafil does not protect from sexually transmitted diseases (STDs), including HIV. Sildenafil is not a form of birth control for men.
Premature ejaculation (PE) is defined as ejaculation that:
Always or nearly always occurs prior to or within approximately one (1) minute of vaginal penetration; and
The inability to delay ejaculation on all or nearly all vaginal penetrations.
The current treatment for PE is the off-label use of paroxetine, an SSRI.
Clinical studies investigating Sildenafil for the treatment of PE failed to provide significant evidence that the medication provides any improvement in PE. However, Sildenafil has been positively associated with increased confidence, self-esteem, and improved relationships. Sildenafil has also been shown to improve the post-ejaculatory refractory time (time after ejaculation in which a man can achieve another erection) and perceived improvement in ejaculatory control.
It is not recommended to take Sildenafil with alcohol. Drinking too much alcohol can increase your odds of a headache, dizziness, elevated heart rate, or lower blood pressure.
The Centers for Disease Control and Prevention generally recommend no more than two (2) 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.).
Sildenafil can cause a sudden drop in blood pressure. When combined with other specific medications, such as nitrates and guanylate cyclase, 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
Indigestion or upset stomach
Runny or stuffy nose
Skin rash
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 Sildenafil. 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.
Uncommon side effects of Sildenafil 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 Sildenafil or other ED medications may have a sudden decrease, disturbance, or loss of vision in one or both eyes. If you experience a sudden vision decrease or loss, stop taking Sildenafil 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 Sildenafil and seek immediate medical help.
In very rare circumstances, instances of heart attack, stroke, irregular heartbeats, and even death have been reported, though in the vast majority of men who presented with serious health problems before taking Sildenafil.
One tablet of Sildenafil contains active ingredients that may stay in your body for up to 12 hours, though most effects have likely stopped within 4-6 hours of taking your dose. Other medications you may be on, especially for kidney or liver health, can cause the active ingredients to linger longer.
Sildenafil is not right for everyone. Only your healthcare provider and you can decide if Sildenafil is right for you. Only those who have specifically been prescribed Sildenafil should take it. Never share Sildenafil with others, even if their symptoms are similar, as it may cause serious harm.
Neither women nor children under the age of 18 should take Sildenafil as the safety and risk are unknown.
Do not take Sildenafil if you are currently taking other ED medicines or treatments, including Viagra, any other PDE-5 inhibitors, or Revatio. (Sildenafil is the active ingredient in Revatio, a drug that treats a rare disease called PAH, or pulmonary arterial hypertension.)
Do not take Sildenafil 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 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 Sildenafil 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 Sildenafil 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 Sildenafil can result in dizziness or fainting. Alpha blocks 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 treat high blood pressure (hypertension)
Some types of antibiotics, including:
Biaxin, aka clarithromycin
Ketek, aka telithromycin
Erythromycin, aka several brand names
Medicines known as “HIV protease inhibitors”, such as Norvir or Kaletra, aka ritonavir
Some types of antifungals, including:
Nizoral, aka ketoconazole
Sporanox, aka itraconazole
Sildenafil is not right for everyone. Only your healthcare provider and you can decide if Sildenafil is right for you. Your physician or healthcare provider must know all medications and non-prescription drugs or medicines you are currently taking (including vitamins and herbal supplements).
Ask your healthcare provider if your heart is healthy enough for you to have sexual activity. You should not take Sildenafil if your healthcare provider has told you not to engage in sexual activity due to health problems. Before taking Sildenafil, 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, heart attack, or narrowing of your aortic valve
Low blood pressure
High blood pressure that is not currently under control
Stroke
Blood cell problems, such as multiple myeloma, sickle cell anemia, or leukemia
Liver problems
Kidney problems and/or required dialysis
Retinitis pigmentosa (a rare eye disease)
Severe vision loss, including a condition known as NAION
Stomach or intestinal 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)
In the case of an emergency medical situation related to your heart, you must disclose the last time you took Sildenafil.