Label: SILDENAFIL CITRATE- sildenafil tablet, film coated

[33] Some users mix it with methylenedioxymethamphetamine (MDMA, ecstasy), other stimulants, or opiates in an attempt to compensate for the common side effect of erectile dysfunction, a combination known as "sextasy", "rockin' and rollin'", "hammerheading", or "trail mix". [33] Mixing it with amyl nitrite, another vasodilator, is particularly dangerous and potentially fatal. The 2007 Ig Nobel Prize in aviation went to Patricia V. Agostino, Santiago A. Plano, and Diego A. Golombek of Universidad Nacional de Quilmes, Argentina, for their discovery that sildenafil helps treat jet lag recovery in hamsters. Professional athletes have been documented using sildenafil, believing the opening of their blood vessels will enrich their muscles.

Call to Action for Buyers, Importers, and Distributors

[33] Some users mix it with methylenedioxymethamphetamine (MDMA, ecstasy), other stimulants, or opiates in an attempt to compensate for the common side effect of erectile dysfunction, a combination known as "sextasy", "rockin' and rollin'", "hammerheading", or "trail mix". [33] Mixing it with amyl nitrite, another vasodilator, is particularly dangerous and potentially fatal. The 2007 Ig Nobel Prize in aviation went to Patricia V. Agostino, Santiago A. Plano, and Diego A.

Clinical monitoring

Golombek of Universidad Nacional de Quilmes, Argentina, for their discovery that sildenafil helps treat jet lag recovery in hamsters. Professional athletes have been documented using sildenafil, believing the opening of their blood vessels will enrich their muscles. In turn, they believe it will enhance their performances. Acetildenafil and other synthetic structural analogs of sildenafil which are PDE5 inhibitors have been found as adulterants in a number of "herbal" aphrodisiac products sold over-the-counter. [41] These analogs have not undergone any of the rigorous testing that drugs like sildenafil have passed, and thus have unknown side-effect profiles.

Regional issues

[42] Some attempts have been made to ban these drugs, but progress has been slow so far, as, even in those jurisdictions that have laws targeting designer drugs, the laws are drafted to ban analogs of illegal drugs of abuse, rather than analogs of prescription medicines. However, at least one court case has resulted in a product being taken off the market. The US Food and Drug Administration (FDA) has banned numerous products claiming to be Eurycoma longifolia that, in fact, contain only analogs of sildenafil. [44][45][46] Sellers of such fake herbals typically respond by just changing the names of their products. Sildenafil and/or N-desmethylsildenafil, its major active metabolite, may be quantified in plasma, serum, or whole blood to assess pharmacokinetic status in those receiving the drug therapeutically, to confirm the diagnosis in potential poisoning victims, or to assist in the forensic investigation in a case of fatal overdose. In turn, they believe it will enhance their performances. Acetildenafil and other synthetic structural analogs of sildenafil which are PDE5 inhibitors have been found as adulterants in a number of "herbal" aphrodisiac products sold over-the-counter.

[41] These analogs have not undergone any of the rigorous testing that drugs like sildenafil have passed, and thus have unknown side-effect profiles. [42] Some attempts have been made to ban these drugs, but progress has been slow so far, as, even in those jurisdictions that have laws targeting designer drugs, the laws are drafted to ban analogs of illegal drugs of abuse, rather than analogs of prescription medicines. However, at least one court case has resulted in a product being taken off the market. The US Food and Drug Administration (FDA) has banned numerous products claiming to be Eurycoma longifolia that, in fact, contain only analogs of sildenafil. [44][45][46] Sellers of such fake herbals typically respond by just changing the names of their products. Sildenafil and/or N-desmethylsildenafil, its major active metabolite, may be quantified in plasma, serum, or whole blood to assess pharmacokinetic status in those receiving the drug therapeutically, to confirm the diagnosis in potential poisoning victims, or to assist in the forensic investigation in a case of fatal overdose. Nitric oxide (NO) in the corpus cavernosum of the penis binds to guanylate cyclase receptors, which results in increased levels of cGMP, leading to smooth muscle relaxation (vasodilation) of the intimal cushions of the helicine arteries. This smooth muscle relaxation leads to vasodilation and increased inflow of blood into the spongy tissue of the penis, causing an erection. [49] Robert F. Furchgott, Ferid Murad, and Louis Ignarro won the Nobel Prize in Physiology or Medicine in 1998 for their independent study of the metabolic pathway of nitric oxide in smooth muscle vasodilation. The molecular mechanism of smooth muscle relaxation involves the enzyme CGMP-dependent protein kinase, also known as PKG. This kinase is 50 mg sildenafil price activated by cGMP and it phosphorylates multiple targets in the smooth muscle cells, namely myosin light chain phosphatase, RhoA, IP3 receptor, phospholipase C, and others.

• Sildenafil 120 mg is not approved by all regulatory agencies for general use.
• The maximum recommended dose for most individuals is 100 mg.
• Using high doses can lead to increased cardiovascular strain.
• Always inform your doctor of all medications to prevent interactions.
• Sildenafil may cause a sudden drop in blood pressure, especially with certain drugs.
• The medication can be used as part of a treatment plan for erectile dysfunction.

[50] Overall, this results in a decrease in intracellular calcium and desensitizing proteins to the effects of calcium, engendering smooth muscle relaxation.

5.4 Epistaxis

The molecular structure of sildenafil is similar to that of cGMP and acts as a competitive binding agent of PDE5 in the corpus cavernosum, resulting in more cGMP and increased penile response to sexual stimulation. [49][51] Without sexual stimulation, and therefore lack of activation of the NO/cGMP system, sildenafil should not cause an erection. Other drugs that operate by the same mechanism include tadalafil (Cialis) and vardenafil (Levitra). Sildenafil is broken down in the liver by hepatic metabolism using cytochrome p450 enzymes, mainly CYP450 3A4 (major route), but also by CYP2C9 (minor route) hepatic isoenzymes.

• Sildenafil 120 mg can cause flushing and nasal congestion as common side effects.
• It is important to follow medical advice to minimize health risks.
• The drug's effectiveness can be influenced by other health conditions like diabetes.
• Consuming grapefruit or grapefruit juice may affect sildenafil’s metabolism.
• Patients should seek emergency care if experiencing an erection lasting longer than 4 hours.
• Sildenafil’s effects typically last about 4-6 hours, depending on individual factors.

The major product of metabolisation by these enzymes is N-desmethylated sildenafil, which is metabolised further. This metabolite also has an affinity for the PDE receptors, about 40% of that of sildenafil. Thus, the metabolite is responsible for about 20% of sildenafil's action. Sildenafil is excreted as metabolites predominantly in the feces (about 80% of administered oral dose) and to a lesser extent in the urine (around 13% of the administered oral dose). If taken with a high-fat meal, absorption is reduced; the time taken to reach the maximum plasma concentration increases by around one hour, and the maximum concentration itself is decreased by nearly one-third. When taken orally, sildenafil for erectile dysfunction results in an average time to onset of erections of 27 minutes (ranging from 12 to 70 minutes). Sublingual use of sildenafil for erectile dysfunction results in an average onset of action of 15 minutes and lasting for an average of 40 minutes. The preparation steps for synthesis of sildenafil are:[54] Methylation of 3-propylpyrazole-5-carboxylic acid ethyl ester with hot dimethyl sulfate Hydrolysis with aqueous sodium hydroxide (NaOH) to free acid Carboxamide formation with refluxing thionyl chloride/NH4OH Reduction of nitro group to amino group Sildenafil (compound UK-92,480) was synthesized by a group of pharmaceutical chemists led by Simon Campbell[55] working at Pfizer's Sandwich, Kent, research facility in England. It was initially studied for use in hypertension (high blood pressure) and angina pectoris (a symptom of ischaemic heart disease). [56] The first clinical trials were conducted in Morriston Hospital in Swansea. [57] Phase I clinical trials under the direction of Ian Osterloh suggested the drug had little effect on angina, but it could induce marked penile erections. [58][59] Pfizer therefore decided to market it for erectile dysfunction, rather than for angina; this decision became an often-cited example of drug repositioning. [60][61] The drug was patented in 1996, approved for use in erectile dysfunction by the FDA on 27 March 1998, becoming the first oral treatment approved to treat erectile dysfunction in the United States, and offered for sale in the United States later that year. [62] It soon became a great success: annual sales of Viagra peaked in 2008 at US$1.934 billion. In the US, even though sildenafil is available only by prescription from a doctor, it was advertised directly to consumers on TV (famously being endorsed by former United States Senator Bob Dole and football star Pelé). Numerous sites on the Internet offer Viagra for sale after an "online consultation", often a simple web questionnaire. Viagra and other products for sexual dysfunction, termed sexuopharmaceuticals, proliferated new types of specialised marketing for such products.

• The drug should be taken on an empty stomach for faster effect.
• Use of 120 mg may lead to priapism, a painful, prolonged erection.
• Sildenafil is also used to treat pulmonary arterial hypertension at lower doses.
• Do not exceed prescribed doses to avoid serious adverse reactions.
• Efficacy of sildenafil depends on individual health and possible drug interactions.
• Sildenafil can impair vision temporarily, including blue-tinted vision.

[66] Viagra and similar prescription pharmaceuticals were promoted by images in media to the extent of becoming a cultural icon, at the time a relatively new phenomenon known to be permitted only in the United States and New Zealand and which is believed to have significantly contributed to norms regarding male sexuality. [67] One author notes that although the effect of Viagra is only limited to penile blood vessels, advertisements routinely use imagery of couples hugging, smiling and dancing, with the author claiming that pharmaceutical companies were deceptive in the use of such advertisements. In 2000, Viagra sales sildenafil tables accounted for 92% of the global market for prescribed erectile dysfunction pills. [69] By 2007, Viagra's global share had plunged to about 50%[70] due to several factors, including the entry of Cialis and Levitra, along with several counterfeits and clones, and reports of vision loss in people taking PDE5 inhibitors. [71][72] In 2008, the FDA forced Pfizer to remove Viva Cruiser, an advergame for Viagra, from appearing on Forbes, after the game failed to disclose risk information about the drug. In February 2007, it was announced that Boots, the UK pharmacy chain, would try over-the-counter sales of Viagra in stores in Manchester, England. Males between the ages of 30 and 65 would be eligible to buy four tablets after a consultation with a pharmacist. [75] In 2017, the Medicines and Healthcare products Regulatory Agency (MHRA) enacted legislation that expanded this nationwide,[76] allowing a particular branded formulation of Sildenafil, Viagra Connect (50 mg), to be sold over the counter and without a prescription throughout the UK from early 2018. While the sale remains subject to a consultation with a pharmacist, the other restrictions from the trial have been removed, allowing customers over the age of 18 to purchase an unlimited number of pills. In May 2013, Pfizer, which manufactures Viagra, told the Associated Press they will begin selling the drug directly to people on its website.

Route of administration

Nitric oxide (NO) in the corpus cavernosum of the penis binds to guanylate cyclase receptors, which results in increased levels of cGMP, leading to smooth muscle relaxation (vasodilation) of the intimal cushions of the helicine arteries. This smooth muscle relaxation leads to vasodilation and increased inflow of blood into the spongy tissue of the penis, causing an erection. [49] Robert F. Furchgott, Ferid Murad, and Louis Ignarro won the Nobel Prize in Physiology or Medicine in 1998 for their independent study of the metabolic pathway of nitric oxide in smooth muscle vasodilation. The molecular mechanism of smooth muscle relaxation involves the enzyme CGMP-dependent protein kinase, also known as PKG.

Does sildenafil interact with other medicines (drug interactions)?

This kinase is 50 mg sildenafil price activated by cGMP and it phosphorylates multiple targets in the smooth muscle cells, namely myosin light chain phosphatase, RhoA, IP3 receptor, phospholipase C, and others. [50] Overall, this results in a decrease in intracellular calcium and desensitizing proteins to the effects of calcium, engendering smooth muscle relaxation. The molecular structure of sildenafil is similar to that of cGMP and acts as a competitive binding agent of PDE5 in the corpus cavernosum, resulting in more cGMP and increased penile response to sexual stimulation. [49][51] Without sexual stimulation, and therefore lack of activation of the NO/cGMP system, sildenafil should not cause an erection. Other drugs that operate by the same mechanism include tadalafil (Cialis) and vardenafil (Levitra).

Revatio Tablets

Sildenafil is broken down in the liver by hepatic metabolism using cytochrome p450 enzymes, mainly CYP450 3A4 (major route), but also by CYP2C9 (minor route) hepatic isoenzymes. The major product of metabolisation by these enzymes is N-desmethylated sildenafil, which is metabolised further. This metabolite also has an affinity for the PDE receptors, about 40% of that of sildenafil. Thus, the metabolite is responsible for about 20% of sildenafil's action. Sildenafil is excreted as metabolites predominantly in the feces (about 80% of administered oral dose) and to a lesser extent in the urine (around 13% of the administered oral dose). Pfizer's patents on Viagra expired outside the US in 2012; in the US they were set to expire, but Pfizer settled litigation with each of Mylan and Teva which agreed that both companies could introduce generics in the US in December 2017.

[79][80] In December 2017, Pfizer released its own generic version of Viagra. As of 2018[update], the US Food and Drug Administration has approved fifteen drug manufacturers to market generic sildenafil in the United States. Seven of these companies are based in India.

Overdose/Missed Dose

In 2000, Viagra sales sildenafil tables accounted for 92% of the global market for prescribed erectile dysfunction pills. [69] By 2007, Viagra's global share had plunged to about 50%[70] due to several factors, including the entry of Cialis and Levitra, along with several counterfeits and clones, and reports of vision loss in people taking PDE5 inhibitors. [71][72] In 2008, the FDA forced Pfizer to remove Viva Cruiser, an advergame for Viagra, from appearing on Forbes, after the game failed to disclose risk information about the drug. In February 2007, it was announced that Boots, the UK pharmacy chain, would try over-the-counter sales of Viagra in stores in Manchester, England. Males between the ages of 30 and 65 would be eligible to buy four tablets after a consultation with a pharmacist.

What is Sildenafil Citrate used for?

[75] In 2017, the Medicines and Healthcare products Regulatory Agency (MHRA) enacted legislation that expanded this nationwide,[76] allowing a particular branded formulation of Sildenafil, Viagra Connect (50 mg), to be sold over the counter and without a prescription throughout the UK from early 2018. While the sale remains subject to a consultation with a pharmacist, the other restrictions from the trial have been removed, allowing customers over the age of 18 to purchase an unlimited number of pills. In May 2013, Pfizer, which manufactures Viagra, told the Associated Press they will begin selling the drug directly to people on its website. Pfizer's patents on Viagra expired outside the US in 2012; in the US they were set to expire, but Pfizer settled litigation with each of Mylan and Teva which agreed that both companies could introduce generics in the US in December 2017. [79][80] In December 2017, Pfizer released its own generic version of Viagra.

When and How to Take Sildenafil for Best Results

As of 2018[update], the US Food and Drug Administration has approved fifteen drug manufacturers to market generic sildenafil in the United States. Seven of these companies are based in India. The patent for Pfizer's Viagra sildenafil to treat erectile dysfunction expired in April 2020. In 2026 a chocolate syrup called Boner Bears from Lockout Supplements was recalled through the FDA because of it containing Sildenafil as an undisclosed ingredient. Counterfeit Viagra, despite generally being cheaper,[88] can contain harmful substances or substances that affect how Viagra works, such as blue printer ink, amphetamines, metronidazole, boric acid, and rat poison. The patent for Pfizer's Viagra sildenafil to treat erectile dysfunction expired in April 2020.

Why Taj Pharma is the Most Trusted Sildenafil Citrate Tablets 120mg Manufacturer, Supplier, and Exporter

Viagra is one of the world's most counterfeited medicines. [90][91] According to a 2012 Pfizer study, around 80% of sites claiming to sell Viagra were selling counterfeits. An October 2023 release stated that erectile dysfunction medicines were the most seized drugs by the Interpol[92] accounting for 22% of seizures. In 1992, Pfizer filed a patent covering the substance sildenafil and its use to treat cardiovascular diseases. In 2026 a chocolate syrup called Boner Bears from Lockout Supplements was recalled through the FDA because of it containing Sildenafil as an undisclosed ingredient. Counterfeit Viagra, despite generally being cheaper,[88] can contain harmful substances or substances that affect how Viagra works, such as blue printer ink, amphetamines, metronidazole, boric acid, and rat poison.

2.5 Dosage Adjustments in Special Populations

If taken with a high-fat meal, absorption is reduced; the time taken to reach the maximum plasma concentration increases by around one hour, and the maximum concentration itself is decreased by nearly one-third. When taken orally, sildenafil for erectile dysfunction results in an average time to onset of erections of 27 minutes (ranging from 12 to 70 minutes). Sublingual use of sildenafil for erectile dysfunction results in an average onset of action of 15 minutes and lasting for an average of 40 minutes. The preparation steps for synthesis of sildenafil are:[54] Methylation of 3-propylpyrazole-5-carboxylic acid ethyl ester with hot dimethyl sulfate Hydrolysis with aqueous sodium hydroxide (NaOH) to free acid Carboxamide formation with refluxing thionyl chloride/NH4OH Reduction of nitro group to amino group Sildenafil (compound UK-92,480) was synthesized by a group of pharmaceutical chemists led by Simon Campbell[55] working at Pfizer's Sandwich, Kent, research facility in England. It was initially studied for use in hypertension (high blood pressure) and angina pectoris (a symptom of ischaemic heart disease).

Product Image

[56] The first clinical trials were conducted in Morriston Hospital in Swansea. [57] Phase I clinical trials under the direction of Ian Osterloh suggested the drug had little effect on angina, but it could induce marked penile erections. [58][59] Pfizer therefore decided to market it for erectile dysfunction, rather than for angina; this decision became an often-cited example of drug repositioning. [60][61] The drug was patented in 1996, approved for use in erectile dysfunction by the FDA on 27 March 1998, becoming the first oral treatment approved to treat erectile dysfunction in the United States, and offered for sale in the United States later that year. [62] It soon became a great success: annual sales of Viagra peaked in 2008 at US$1.934 billion.

Special Populations

In the US, even though sildenafil is available only by prescription from a doctor, it was advertised directly to consumers on TV (famously being endorsed by former United States Senator Bob Dole and football star Pelé). Numerous sites on the Internet offer Viagra for sale after an "online consultation", often a simple web questionnaire. Viagra and other products for sexual dysfunction, termed sexuopharmaceuticals, proliferated new types of specialised marketing for such products. [66] Viagra and similar prescription pharmaceuticals were promoted by images in media to the extent of becoming a cultural icon, at the time a relatively new phenomenon known to be permitted only in the United States and New Zealand and which is believed to have significantly contributed to norms regarding male sexuality. [67] One author notes that although the effect of Viagra is only limited to penile blood vessels, advertisements routinely use imagery of couples hugging, smiling and dancing, with the author claiming that pharmaceutical companies were deceptive in the use of such advertisements. Viagra is one of the world's most counterfeited medicines. [90][91] According to a 2012 Pfizer study, around 80% of sites claiming to sell Viagra were selling counterfeits. An October 2023 release stated that erectile dysfunction medicines were the most seized drugs by the Interpol[92] accounting for 22% of seizures. In 1992, Pfizer filed a patent covering the substance sildenafil and its use to treat cardiovascular diseases.

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