Sildenafil

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NPPA
Regulated

Molecule Description

Sold under the common name of Viagra, Sildenafil is a Phosphodiesterase inhibitor used for the treatment of erectile dysfunction.

Uses

Erectile dysfunction, also known as impotence, erectile dysfunction is an inability to develop or maintain proper penile erection to perform sexual activity
Pulmonary arterial hypertension is a health complication marked by increased blood pressure in the arteries connected to the heart

Contraindications

When should one not use Sildenafil

Regular smokers are not advised to take Sildenafil as it leads to severe side effect of eye called NAION meaning excessive blood loss in optic nerve
Patients who experience heart attacks, low blood pressure, myocardial infraction, stroke and cardiac failure are also advised to avoid the use of Sildenafil to prevent serious effects
Sildenafil is recommended for the individuals having penile deformities
If you have rare inherited eye diseases (retinitis pigmentosa)
Sildenafil is not recommended for the treatment of individuals reported with a hypersensitivity for the drug, for who have received treatment with medicine containing nitrates
Sildenafil is not recommended for the treatment of patients less than 18 year old
If you have a stomach ulcer or bleeding problem (haemophilia)

Side effects

Common side effects of this drug are:

Headache
Nausea
Muscle aches
Flushing
Tenderness around eyes or cheekbones
Sneezing
Runny or bloody nose
Unusually warm skin
Troubled breathing
Reddening of skin
Stomach discomfort
Pounding heartbeat
Burning or itching sensation at various body parts
Bloody or cloudy urine
Cold sweats
Confusion
Convulsions
Difficulty in concentration
Drowsiness
Dry mouth, eyes, and skin
Dizziness
Chest pain
Increased hunger
Increased urination frequency
Indigestion
Tenderness at stomach
Anxiety
Nightmares
Migraine
Prolonged and painful erection
Behavioural changes
Bloodshot eyes/red eyes, pain in the eyes, seeing flashes of light, light sensitivity, watery eyes
Fainting
Low blood pressure

Precautions and Warnings

Pregnancy

Sildenafil is a medicine used to treat erectile dysfunction in male. Thus, it is not recommended to administer in pregnant women.

Breast Feeding

Sildenafil is not recommended to administer in breastfeeding mothers.

Driving

Sildenafil can cause dizziness and can affect your vision. You should be careful if you need to drive.

Alcohol

Drinking alcohol is known to cause erection impairment. You are advised not to drink alcohol in extreme amounts before taking Sildenafil.

Other General Warnings

Talk to your doctor if

You experience sudden loss of hearing or buzzing noise in ears while taking treatment with Sildenafil
Some patients may experience a sudden loss of vision while taking a treatment with Sildenafil. In such a situation, stop taking Sildenafil and consult a physician immediately
Sildenafil should be used with great caution for the treatment of heart patients
The risk of side effects caused by Sildenafil is great in case of regular smokers, patients older than 60 years and heart patients
Sildenafil may result into priapism, i.e. painful erection especially in patients suffering from sickle cell anaemia (an abnormality of red blood cells), leukaemia (cancer of blood cells), multiple myeloma (cancer of bone marrow) and penile deformities

Mode of Action

How Does It Work?

Human erection is an involuntary event governed by the autonomous nervous system. On stimulation, two essential parts of the human penis, corpus carvernosum and corpus spongium create the erection by maintaining blood flow. One more factor that plays a crucial role in regulating erection is cyclic Guanosine monophosphate (cGMP), which increases the blood flow in the penis, causing an erection. In people who have erectile dysfunction, cGMP-specific Phosphodiesterase type 5 (PDE5) binds cGMP and inhibits its action. Sildenafil protects this degradation of cGMP by PDE5 in corpus cavernosum. Sildenafil has the same structure as cGMP and it binds PDE5, which eventually results in free cGMP resulting in undisturbed erection.

Interactions

Interactions with other medicines

Concomitant administration of Sildenafil and medicines containing nitrates leads to dangerous hypotensive effects (low blood pressure)
Coadministration of Sildenafil and alpha-blockers lowers the blood pressure
Sildenafil interact with Amlodipine and cause an increase in blood pressure
Coadministration of Sildenafil and CYP3A4 inhibitors like Ritonavir (medicine for HIV treatment) increase the systemic exposure of Sildenafil
Coadministration of Sildenafil with Ritonavir is not advised

Interactions with food items

Sildenafil leads to dangerous effects when consumed with grapefruit or its juice and pomelo or its juice.

Dietary Restrictions

Patients taking a treatment with Sildenafil are advised to avoid grapefruit or its products.

Dosage

Overdose

Symptoms of overdose can be headache, flushing, dizziness, dyspepsia, nasal congestion, altered vision. Call emergency medical services if you suspect overdose.

Missed a Dose

In case of a missed dose, patients are recommended to take the dose as soon as possible. However, if the time of the next dose has already come, the patient can skip the missed dose and continue with their scheduled dosages.

Frequently Asked Questions (FAQs)

The effect of Sildenafil can be observed within 30 to 120 minutes of its administration.

The duration of the effect of Sildenafil is 4 hours.

No, Sildenafil and alcohol interact with each other and lead to an increase in the risk as well as the intensity of side effects like dizziness, fainting, flushing, headache, etc.

No habit-forming tendencies are reported in case of Sildenafil.

You must inform the doctor about heart diseases, asthma, blood pressure disorders, diabetes and congenital penile defects (if any) to your doctor before taking a treatment with Sildenafil.