What is sildenafil Citrate?
Sildenafil is a prescribed drug, and it is available as tablets or suspension (liquid), and both can take orally. Also available is an intravenous (IV) form that a physician can only administer.
Sildenafil or oral tablets are sold in brand-name drugs Viagra and Revatio. Also, it’s available as a generic version. Generic medicines typically are less expensive than brand-name versions. In certain instances, there may be a difference in the price. Available in the same strength or the same form as brand-name drugs.
Uses Of Sildenafil Citrate drugs
Treatment of Erectile dysfunction (ED)
Time to commencement and duration of effect pharmacological profile
Sildenafil is a highly specific PDE type 5 inhibitor. In vitro, it improves NO-mediated relaxation of the human corpus cavernosum. Sildenafil raises intracellular attention of cyclic guanosine 3′,5′ monophosphate (cGMP) by inhibiting PDE-5, amplifying the endogenous NO-cGMP signalling pathway. The plasma half-life is around 4–5 hours, while the time to maximum plasma concentration is about 1 hour. It comes in 25 mg, 50 mg, and 100 mg dosages & is used orally on request. The recommended beginning dose is 50 mg, which can be improved or decreased depending on efficacy and tolerability. Patients are advised to take sildenafil around 1 hour before sexual activity, with a maximum dose frequency once per day. Sexual stimulation is required for both sildenafil and the other PDE-5. From 30 minutes to 4–5 hours after administration, there is a window of opportunity to engage in sexual intercourse. However, for around 35% of patients, the beginning of action can be as quick as 14 minutes, and effectiveness can last up to 12 hours. Absorption is decreased and extended after a substantial fatty meal. In typical amounts, alcohol has little effect on absorption.
Safety
Rates of discontinuation and adverse events
Sildenafil has been available for almost eight years. Morales and colleagues (1998) offered summary safety information through 1998, while Padma-Nathan and colleagues supplied long-term safety information.
Headache, face flushing, dyspepsia, dizziness, nasal congestion, altered vision, and pulse are often reported treatment-related side effects. Back discomfort, influenza-like illness, rash, vomiting, diarrhoea, cardiac arrhythmia, and hypersensitivity responses are unusual or seldom documented side effects. Adverse reactions are dose-related, minor, and self-limiting with continued usage. The rate of withdrawal owing to adverse events is comparable to placebo. The post-marketing case series documented a greater incidence of adverse events, particularly for headache, flushing, and altered vision.
Depending on their comorbidities, patients may tolerate sildenafil differently. Ischemic heart disease & hypertension are linked to a greater rate of negative outcomes than diabetes. Due to poor suppression of PDE-5 in the retina, visual disturbances develop. They are transitory and entirely reversible, and they correspond with peak plasma concentrations of sildenafil. None remained 6 hours after taking sildenafil, and they are seldom a cause to stop using it.
Cardiovascular protection
When compared to predicted rates in aged-matched populations of males, clinical trials and post-marketing data of sildenafil showed no increase in myocardial infarction rates in individuals who received these medications as part of either double-blind, placebo-controlled trials or open-label studies. In males with stable angina, sildenafil did not affect total exercise time or time to ischemia during exercise testing, and it could help with exercise testing. According to the data reviewed thus far, sildenafil does not affect cardiac contractility, cardiac output, or myocardial oxygen consumption.
Several new research has demonstrated sildenafil’s cardiovascular safety and that it may have a cardioprotective effect. Sildenafil inhibits PDE5A, which reduces systolic responses to beta-adrenergic stimulation, indicating that it may have a role in modulating stimulated heart function. Sildenafil prevents and cures heart hypertrophy by inhibiting cGMP phosphodiesterase 5A over time. Finally, sildenafil is the only PDE5i that improves arterial oxygenation in patients with pulmonary hypertension. It was recently approve in dosages of 20 mg and 40 mg, which patients with pulmonary hypertension can take every 8 hours for the rest of their lives.
Sildenafil treatment failure is defined as a failure to respond to the drug sildenafil.
Even though the phrase “treatment failure” to oral medications is often use, there is no concrete explanation of what it entails. Medicine, physician, and patient concerns may all play a role in treatment failure. Characterization of a non-responder to oral medication is proposed based on these issues: “an insufficient erectile response following at least four attempts of the maximum tolerable drug dose in compliance with manufacturer’s advice for timing relative to meals, alcohol intake, usage of concurrent drugs, and enough sexual stimulation/arousal.”
It was taking sildenafil before bed. Sildenafil enhances sleep-related erections in healthy guys, indicating that the nitric oxide pathway plays a role in the physiology of erections during sleep. Sildenafil has a long-lasting effect that might continue up to 8-9 hours after being consumed.
How do we maximize its efficacy?
Prepare a small supper ahead of time.
Viagra may take with or without meals, but if you prefer to eat something light before getting started, do so. If you eat a substantial or high-fat meal before taking it, absorption may be delayed, which means it will take longer to take effect. Eat a lighter supper if time is of the essence and you want your stiffy sooner rather than later.
Allow time for it to take effect.
Don’t expect to be able to get down to business immediately away after taking the tablet. Allow for some time for it to take effect. There’s no need to rush or worry about it because you may take it up to 4 hours before having sex.
After you’ve taken the pill, don’t drink any alcohol.
You should be alright if you enjoy a glass of wine or another alcoholic beverage before sexy time. However, drinking more than that after taking Viagra may put a damper on your date. You may find it difficult to achieve an erection if you drink moderately too heavily. Viagra can also help reduce blood pressure, and when combined with alcohol, this impact might amplify.
Perspectives for the future
Sildenafil as a preventative measure
After a nerve-sparing radical retropubic prostatectomy, early administration of vasoactive drugs has prove to improve erectile function.
In a double-blind, placebo-controlled study, sildenafil (50 mg–100 mg) taken every night for nine months, beginning one month after nerve-sparing radical prostatectomy, was associated with the recovery of spontaneous erections in 27 per cent of patients, compared to 4 per cent of patients taking placebo. In a study of 40 potent volunteers with prostate cancer who underwent RRP, sildenafil administration every other night for six months significantly increased corporal sm. Maintaining the smooth muscle of the corpora cavernosa is the most promising preventive role of sildenafil.
What are the potential negative effects of this medication?
Sildenafil has the potential to induce adverse effects. Inform your doctor if any of the following signs are severe or ongoing:
- Headache
- Heartburn
- Diarrhoea
- Flushing (warmth sensation)
- Nosebleeds
- Difficulty getting or staying asleep
- Numbness, burning & tingling in the arms, hands, feet, & legs
- Muscular pains
- Colour vision alterations
- Light sensitivity
Some of the negative effects might be severe. Call your doctor right away if you have any of the physical signs:
- Abrupt and severe eyesight loss (see below for more information)
- Impaired vision
- Steep reduction or loss of hearing
- Ringing in the ears
- Dizziness or lightheadedness
- Fainting
- Chest discomfort
- Increasing shortness of breath
- Painful or prolonged erection
- Itching or burning during urination
- Rash
After using sildenafil or other sildenafil-like drugs, some individuals suffered an abrupt loss of some or all of their eyesight. It is unknown if the drug caused visual loss. If you develop a sudden vision loss while taking sildenafil, contact your doctor right once.
Do not take any additional sildenafil or related drugs like tadalafil (Cialis) or vardenafil (Levitra) until you consult your doctor.
In males who used sildenafil for erectile dysfunction, there have been reports of heart attacks, strokes, abnormal heartbeats, bleeding in the brain or lungs, excessive blood pressure, and unexpected death. Before using sildenafil, the plurality, but not all, of these patients had cardiac problems. It is unknown if sildenafil, sexual activity, cardiac disease, or a combination of these and other factors caused these incidents. Discuss the dangers of taking sildenafil with your doctor.
Conclusions
In males with ED, sildenafil is an effective therapy with a favourable safety and tolerability profile. It is also successful in several subpopulations, albeit efficacy is lower in the so-called difficult-to-treat subpopulations, such as diabetic patients or men who have had a radical prostatectomy and men in their later years of life. Sildenafil dramatically increases patient and partner satisfaction and quality of life. Furthermore, new data from fundamental and clinical studies suggest that it might have a role in treating various other chronic diseases in the future.