After chronic dosing of 80 mg three times a day sildenafil to patients with systemic hypertension, the mean change from baseline in systolic and diastolic blood pressures was a decrease of 9.4 and 9.1 mmHg, respectively.
Chemical synthesis
What are the most common side effects of sildenafil?
An evaluation of visual function at doses up to 200 mg revealed no effects of sildenafil on visual acuity, intraocular pressure, or pupillometry.
| Side Effect | Incidence Rate | Severity | Commonality | Notes |
|---|---|---|---|---|
| Headache | High | Mild to moderate | Common | Usually resolves quickly |
| Flushing | Moderate | Mild | Common | Reddening of face and neck |
| Dizziness | Moderate | Mild to moderate | Common | Especially when standing up quickly |
| Vision Changes | Low | Mild to moderate | Less common | Blurred vision or light sensitivity |
Sildenafil is rapidly absorbed after oral administration, with a mean absolute bioavailability of 41% (25 to 63%). Sildenafil Injection: The pharmacokinetic profile of sildenafil has been characterized following intravenous administration. A 10 mg dose of sildenafil injection is predicted to provide a pharmacological effect of sildenafil and its N-desmethyl metabolite equivalent to that of a 20 mg oral dose. Sildenafil Injection: Predictions based on a pharmacokinetic model suggest that drug-drug interactions with CYP3A inhibitors will be less than those observed after oral sildenafil administration. 13 NONCLINICAL TOXICOLOGY 13.1 Carcinogenesis, Mutagenesis, Impairment of FertilitySildenafil was not carcinogenic when administered to rats for up to 24 months at 60 mg/kg/day, a dose resulting in total systemic exposure (AUC) to unbound sildenafil and its major metabolite 33- and 37- times, for male and female rats, respectively, the human exposure at the RHD of 20 mg three times a day. Sildenafil was not carcinogenic when administered to rats for up to 24 months at 60 mg/kg/day, a dose resulting in total systemic exposure (AUC) to unbound sildenafil and its major metabolite 33- and 37- times, for male and female rats, respectively, the human exposure at the RHD of 20 mg three times a day.
| Product | Dosage | Quantity + Bonus | Price | |
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| Kamagra Oral Jelly | 100mg | 220 + 18 Sachets | 662.24€ 630.70€ |
14 CLINICAL STUDIES SUPER-1 (NCT00644605) - Sildenafil Monotherapy [20 mg, 40 mg, and 80 mg Three Times a Day]A randomized, double-blind, placebo-controlled study of sildenafil (SUPER-1) was conducted in 277 patients with PAH (defined as a mean pulmonary artery pressure ≥ 25 mmHg at rest with a pulmonary capillary wedge pressure < 15 mmHg). Patients with left ventricular ejection fraction less than 45% or left ventricular shortening fraction less than 0.2 also were not studied.Patients were randomized to receive placebo (n = 70) or sildenafil 20 mg (n = 69), 40 mg (n = 67) or 80 mg (n = 71) three times a day for a period of 12 weeks. Placebo-corrected mean increases in walk distance of 45 to 50 meters were observed with all doses of sildenafil.
Sildenafil (Viagra) dosage
Placebo-corrected mean increases in walk distance of 45 to 50 meters were observed with all doses of sildenafil. These increases were significantly different from placebo, but the sildenafil dose groups were not different from each other (see Figure 3), indicating no additional clinical benefit from doses higher than 20 mg three times a day. Placebo-Corrected Change from Baseline in 6-Minute Walk Distance (meters) at Week 12 by Study Subpopulation in SUPER-1: Mean (95% Confidence Interval)Key: PAH = pulmonary arterial hypertension; CTD = connective tissue disease; PH = pulmonary hypertension; PAP = pulmonary arterial pressure; PVRI = pulmonary vascular resistance index; TID = three times daily.SUPER-2 (NCT00159887) Long-Term Treatment of PAHIn a long-term follow-up of patients who were treated with sildenafil (n = 277), K-M estimates of survival at 1, 2, and 3 years were 94%, 88% , and 79%, respectively. These uncontrolled observations do not allow comparison with a group not given sildenafil and cannot be used to determine the long term-effect of sildenafil on mortality.PACES-1 (NCT00159861) - Sildenafil Co-Administered with EpoprostenolA randomized, double-blind, placebo-controlled study (PACES-1) was conducted in 267 patients with PAH who were taking stable doses of intravenous epoprostenol. Patients were randomized to placebo or sildenafil (in a fixed titration starting from 20 mg to 40 mg and then 80 mg, three times a day) and all patients continued intravenous epoprostenol therapy.At baseline patients had PPH (80%) or PAH secondary to CTD (20%); WHO Functional Class I (1%), II (26%), III (67%), or IV (6%); sildenafil citrate tablets 50mg and the mean age was 48 years, 80% were female, and 79% were Caucasian.There was a statistically significant greater increase from baseline in 6-minute walk distance at Week 16 (primary endpoint) for the sildenafil group compared with the placebo group.
Altitude sickness
The mean change from baseline at Week 16 (last observation carried forward) was 30 meters for the sildenafil group compared with 4 meters for the placebo group giving an adjusted treatment difference of 26 meters (95% CI: 10.8, 41.2) (p = 0.0009).Patients on sildenafil achieved a statistically significant reduction in mPAP compared to those on placebo. A mean placebo-corrected treatment effect of -3.9 mmHg was observed in favor of sildenafil (95% CI: -5.7, -2.1) (p = 0.00003).Time to clinical worsening of PAH was defined as the time from randomization to the first occurrence of a clinical worsening event (death, lung transplantation, initiation of bosentan therapy, or clinical deterioration requiring a change in epoprostenol therapy). Kaplan-Meier estimates and a stratified log-rank test demonstrated that placebo-treated patients were 3 times more likely to experience a clinical worsening event than sildenafil-treated patients and that sildenafil-treated patients experienced a significant delay in time to clinical worsening versus placebo-treated patients (p = 0.0074). Kaplan-Meier plot of time to clinical worsening is presented in Figure 5.Figure 5. Kaplan-Meier Plot of Time (in Days) to Clinical Worsening of PAH in PACES-1Improvements in WHO Functional Class for PAH were also demonstrated in patients on sildenafil compared to placebo. These increases were significantly different from placebo, but the sildenafil dose groups were not different from each other (see Figure 3), indicating no additional clinical benefit from doses higher than 20 mg three times a day. Placebo-Corrected Change from Baseline in 6-Minute Walk Distance (meters) at Week 12 by Study Subpopulation in SUPER-1: Mean (95% Confidence Interval)Key: PAH = pulmonary arterial hypertension; CTD = connective tissue disease; PH = pulmonary hypertension; PAP = pulmonary arterial pressure; PVRI = pulmonary vascular resistance index; TID = three times daily.SUPER-2 (NCT00159887) Long-Term Treatment of PAHIn a long-term follow-up of patients who were treated with sildenafil (n = 277), K-M estimates of survival at 1, 2, and 3 years were 94%, 88% , and 79%, respectively. These uncontrolled observations do not allow comparison with a group not given sildenafil and cannot be used to determine the long term-effect of sildenafil on mortality.PACES-1 (NCT00159861) - Sildenafil Co-Administered with EpoprostenolA randomized, double-blind, placebo-controlled study (PACES-1) was conducted in 267 patients with PAH who were taking stable doses of intravenous epoprostenol.
What special precautions should I follow?
PACES-1 (NCT00159861) - Sildenafil Co-Administered with Epoprostenol A randomized, double-blind, placebo-controlled study (PACES-1) was conducted in 267 patients with PAH who were taking stable doses of intravenous epoprostenol. Patients were randomized to placebo or sildenafil (in a fixed titration starting from 20 mg to 40 mg and then 80 mg, three times a day) and all patients continued intravenous epoprostenol therapy. There was a statistically significant greater increase from baseline in 6-minute walk distance at Week 16 (primary endpoint) for the sildenafil group compared with the placebo group. The mean change from baseline at Week 16 (last observation carried forward) was 30 meters for the sildenafil group compared with 4 meters for the placebo group giving an adjusted treatment difference of 26 meters (95% CI: 10.8, 41.2) (p = 0.0009). Patients on sildenafil achieved a statistically significant reduction in mPAP compared to those on placebo.
What should I tell my healthcare provider before taking sildenafil?
A mean placebo-corrected treatment effect of -3.9 mmHg was observed in favor of sildenafil (95% CI: -5.7, -2.1) (p = 0.00003). Kaplan-Meier Plot of Time (in Days) to Clinical Worsening of PAH in PACES-1 Improvements in WHO Functional Class for PAH were also demonstrated in patients on sildenafil compared to placebo. More than twice as many sildenafil-treated patients (36%) as placebo-treated patients (14%) showed an improvement in at least one functional New York Heart Association (NYHA) class for PAH. Study A1481243 (NCT00323297) - Sildenafil Added to Bosentan Therapy – Lack of Effect on Exercise Capacity A randomized, double-blind, placebo-controlled study was conducted in 103 patients with PAH who were on bosentan therapy for a minimum of 3 months. Patients were randomized to placebo or sildenafil (in a fixed titration starting from 20 mg to 40 mg and then 80 mg, three times a day) and all patients continued intravenous epoprostenol therapy.At baseline patients had PPH (80%) or PAH secondary to CTD (20%); WHO Functional Class I (1%), II (26%), III (67%), or IV (6%); sildenafil citrate tablets 50mg and the mean age was 48 years, 80% were female, and 79% were Caucasian.There was a statistically significant greater increase from baseline in 6-minute walk distance at Week 16 (primary endpoint) for the sildenafil group compared with the placebo group. The mean change from baseline at Week 16 (last observation carried forward) was 30 meters for the sildenafil group compared with 4 meters for the placebo group giving an adjusted treatment difference of 26 meters (95% CI: 10.8, 41.2) (p = 0.0009).Patients on sildenafil achieved a statistically significant reduction in mPAP compared to those on placebo. A mean placebo-corrected treatment effect of -3.9 mmHg was observed in favor of sildenafil (95% CI: -5.7, -2.1) (p = 0.00003).Time to clinical worsening of PAH was defined as the time from randomization to the first occurrence of a clinical worsening event (death, lung transplantation, initiation of bosentan therapy, or clinical deterioration requiring a change in epoprostenol therapy).
Images for T 30
More than twice as many sildenafil-treated patients (36%) as placebo-treated patients (14%) showed an improvement in at least one functional New York Heart Association (NYHA) class for PAH.Study A1481243 (NCT00323297) - Sildenafil Added to Bosentan Therapy – Lack of Effect on Exercise CapacityA randomized, double-blind, placebo-controlled study was conducted in 103 patients with PAH who were on bosentan therapy for a minimum of 3 months. On treatment deaths: Any death within 7 days of last dose was regarded as “On treatment”, thus might includedeaths occurred after discontinuation from study treatment.b. Hazard ratio estimates from the proportional Hazards model, stratified by actual previous PAH treatment andetiology of PAH.Kaplan-Meier estimates of survival at 3 years were 66%, 79%, and 85% in the 5-, 20-, and 80- mg TID dose groups, respectively.Clinical WorseningSildenafil 80 mg was also superior to 5 mg for time to first event of clinical worsening with HR (99.7% CI) = 0.44 (0.22, 0.89).Table 7. P-value from the Wald test.6MWD at Months 6 and 12At baseline, the median of 6MWD for the intent-to-treat (ITT) population was 332 to 352 m. At Month 6, the median change from baseline was highest for sildenafil 80 mg TID with 28 m compared to 18 m and 19 m for sildenafil 5 mg TID and sildenafil 20 mg TID groups, respectively.
Sildenafil side effects
The same was seen at Month 12, the median change from baseline for sildenafil 80 mg TID group was 33 m compared to 17 m for sildenafil sildenafil film tablet 5 mg TID and 31 m in sildenafil 20 mg TID groups.Overall, the safety data for sildenafil 20 mg TID and for the higher sildenafil 80 mg TID dose were consistent with the established safety profile of sildenafil in previous adult PAH studies [see Adverse Reactions (6.1)].Pediatric use information is approved for Viatris Specialty LLC's, REVATIO (sildenafil) tablets. SUPER-1 (NCT00644605) - Sildenafil Monotherapy [20 mg, 40 mg, and 80 mg Three Times a Day] A randomized, double-blind, placebo-controlled study of sildenafil (SUPER-1) was conducted in 277 patients with PAH (defined as a mean pulmonary artery pressure ≥ 25 mmHg at rest with a pulmonary capillary wedge pressure < 15 mmHg). Patients were randomized to receive placebo (n = 70) or sildenafil 20 mg (n = 69), 40 mg (n = 67) or 80 mg (n = 71) three times a day for a period of 12 weeks. Figure 4 displays subgroup efficacy analyses in SUPER-1 for the change from baseline in 6-Minute Walk Distance at Week 12 including baseline walk distance, disease etiology, functional class, gender, age, and hemodynamic parameters. SUPER-2 (NCT00159887) Long-Term Treatment of PAH In a long-term follow-up of patients who were treated with sildenafil (n = 277), K-M estimates of survival at 1, 2, and 3 years were 94%, 88% , and 79%, respectively. Kaplan-Meier estimates and a stratified log-rank test demonstrated that placebo-treated patients were 3 times more likely to experience a clinical worsening event than sildenafil-treated patients and that sildenafil-treated patients experienced a significant delay in time to clinical worsening versus placebo-treated patients (p = 0.0074). Kaplan-Meier plot of time to clinical worsening is presented in Figure 5.Figure 5.
| Form | Available Strengths | Description | Notes |
|---|---|---|---|
| Tablets | 25 mg, 50 mg, 100 mg | Standard oral tablets | Most common dosage |
| Sublingual Tabs | 25 mg | Dissolve under tongue | Rapid absorption |
| Liquid Suspension | 10 mg/5 mL | For easy dosing, especially in children | Requires precise measurement |
Kaplan-Meier Plot of Time (in Days) to Clinical Worsening of PAH in PACES-1Improvements in WHO Functional Class for PAH were also demonstrated in patients on sildenafil compared to placebo. More than twice as many sildenafil-treated patients (36%) as placebo-treated patients (14%) showed an improvement in at least one functional New York Heart Association (NYHA) class for PAH.Study A1481243 (NCT00323297) - Sildenafil Added to Bosentan Therapy – Lack of Effect on Exercise CapacityA randomized, double-blind, placebo-controlled study was conducted in 103 patients with PAH who were on bosentan therapy for a minimum of 3 months.
| Storage Condition | Details | Notes |
|---|---|---|
| Temperature | Keep below 30°C (86°F) | Avoid excessive heat |
| Light | Keep away from direct sunlight | Protect from UV rays |
| Humidity | Store in dry place | Prevent moisture from degrading the tablet |
| Out of reach | Keep out of children's reach | Safety precaution |
On treatment deaths: Any death within 7 days of last dose was regarded as “On treatment”, thus might includedeaths occurred after discontinuation from study treatment.b. Hazard ratio estimates from the proportional Hazards model, stratified by actual previous PAH treatment andetiology of PAH.Kaplan-Meier estimates of survival at 3 years were 66%, 79%, and 85% in the 5-, 20-, and 80- mg TID dose groups, respectively.Clinical WorseningSildenafil 80 mg was also superior to 5 mg for time to first event of clinical worsening with HR (99.7% CI) = 0.44 (0.22, 0.89).Table 7.
- White sildenafil tablets are used to treat erectile dysfunction.
- They are often sold under brand names like Viagra.
- The standard dose for sildenafil is 50 mg.
- White sildenafil tablets contain the active ingredient sildenafil citrate.
- These tablets typically come in 25 mg, 50 mg, and 100 mg doses.
- They work by increasing blood flow to the penis.
- Sildenafil tablets should be taken about 30-60 minutes before activity.
- They are most effective when taken on an empty stomach.
- Common side effects include headache, flushing, and upset stomach.
- Always consult a healthcare provider before using sildenafil.
- Purchasing from reputable sources ensures quality and safety.
P-value from the Wald test.6MWD at Months 6 and 12At baseline, the median of 6MWD for the intent-to-treat (ITT) population was 332 to 352 m. At Month 6, the median change from baseline was highest for sildenafil 80 mg TID with 28 m compared to 18 m and 19 m for sildenafil 5 mg TID and sildenafil 20 mg TID groups, respectively. The same was seen at Month 12, the median change from baseline for sildenafil 80 mg TID group was 33 m compared to 17 m for sildenafil sildenafil film tablet 5 mg TID and 31 m in sildenafil 20 mg TID groups.Overall, the safety data for sildenafil 20 mg TID and for the higher sildenafil 80 mg TID dose were consistent with the established safety profile of sildenafil in previous adult PAH studies [see Adverse Reactions (6.1)].Pediatric use information is approved for Viatris Specialty LLC's, REVATIO (sildenafil) tablets. SUPER-1 (NCT00644605) - Sildenafil Monotherapy [20 mg, 40 mg, and 80 mg Three Times a Day] A randomized, double-blind, placebo-controlled study of sildenafil (SUPER-1) was conducted in 277 patients with PAH (defined as a mean pulmonary artery pressure ≥ 25 mmHg at rest with a pulmonary capillary wedge pressure < 15 mmHg).
Is generic medication less effective than brand-name medication?
After chronic dosing of 80 mg three times a day sildenafil to patients with systemic hypertension, the mean change from baseline in systolic and diastolic blood pressures was a decrease of 9.4 and 9.1 mmHg, respectively. An evaluation of visual function at doses up to 200 mg revealed no effects of sildenafil on visual acuity, intraocular pressure, or pupillometry. Sildenafil is rapidly absorbed after oral administration, with a mean absolute bioavailability of 41% (25 to 63%). Sildenafil Injection: The pharmacokinetic profile of sildenafil has been characterized following intravenous administration. A 10 mg dose of sildenafil injection is predicted to provide a pharmacological effect of sildenafil and its N-desmethyl metabolite equivalent to that of a 20 mg oral dose.
Recreational use
Sildenafil Injection: Predictions based on a pharmacokinetic model suggest that drug-drug interactions with CYP3A inhibitors will be less than those observed after oral sildenafil administration. 13 NONCLINICAL TOXICOLOGY 13.1 Carcinogenesis, Mutagenesis, Impairment of FertilitySildenafil was not carcinogenic when administered to rats for up to 24 months at 60 mg/kg/day, a dose resulting in total systemic exposure (AUC) to unbound sildenafil and its major metabolite 33- and 37- times, for male and female rats, respectively, the human exposure at the RHD of 20 mg three times a day. Sildenafil was not carcinogenic when administered to rats for up to 24 months at 60 mg/kg/day, a dose resulting in total systemic exposure (AUC) to unbound sildenafil and its major metabolite 33- and 37- times, for male and female rats, respectively, the human exposure at the RHD of 20 mg three times a day. 14 CLINICAL STUDIES SUPER-1 (NCT00644605) - Sildenafil Monotherapy [20 mg, 40 mg, and 80 mg Three Times a Day]A randomized, double-blind, placebo-controlled study of sildenafil (SUPER-1) was conducted in 277 patients with PAH (defined as a mean pulmonary artery pressure ≥ 25 mmHg at rest with a pulmonary capillary wedge pressure < 15 mmHg). Patients with left ventricular ejection fraction less than 45% or left ventricular shortening fraction less than 0.2 also were not studied.Patients were randomized to receive placebo (n = 70) or sildenafil 20 mg (n = 69), 40 mg (n = 67) or 80 mg (n = 71) three times a day for a period of 12 weeks. Patients were randomized to receive placebo (n = 70) or sildenafil 20 mg (n = 69), 40 mg (n = 67) or 80 mg (n = 71) three times a day for a period of 12 weeks. Figure 4 displays subgroup efficacy analyses in SUPER-1 for the change from baseline in 6-Minute Walk Distance at Week 12 including baseline walk distance, disease etiology, functional class, gender, age, and hemodynamic parameters. SUPER-2 (NCT00159887) Long-Term Treatment of PAH In a long-term follow-up of patients who were treated with sildenafil (n = 277), K-M estimates of survival at 1, 2, and 3 years were 94%, 88% , and 79%, respectively. PACES-1 (NCT00159861) - Sildenafil Co-Administered with Epoprostenol A randomized, double-blind, placebo-controlled study (PACES-1) was conducted in 267 patients with PAH who were taking stable doses of intravenous epoprostenol.
Images for AN 351
Sildenafil: the science
Patients were randomized to placebo or sildenafil (in a fixed titration starting from 20 mg to 40 mg and then 80 mg, three times a day) and all patients continued intravenous epoprostenol therapy. There was a statistically significant greater increase from baseline in 6-minute walk distance at Week 16 (primary endpoint) for the sildenafil group compared with the placebo group. The mean change from baseline at Week 16 (last observation carried forward) was 30 meters for the sildenafil group compared with 4 meters for the placebo group giving an adjusted treatment difference of 26 meters (95% CI: 10.8, 41.2) (p = 0.0009). Patients on sildenafil achieved a statistically significant reduction in mPAP compared to those on placebo. A mean placebo-corrected treatment effect of -3.9 mmHg was observed in favor of sildenafil (95% CI: -5.7, -2.1) (p = 0.00003).
- Sildenafil tablets are available in various generic versions.
- White sildenafil tablets are often easier to swallow due to their shape.
- The cost of sildenafil varies depending on the brand and dosage.
- Using sildenafil responsibly can improve quality of life for users.
- Not all erectile issues require medication; consult a doctor for underlying causes.
- Sildenafil is not suitable for women or children.
- The drug works by blocking PDE5, enhancing natural erections.
- Physical activity after taking sildenafil can enhance its effectiveness.
- Sildenafil is sometimes used off-label for pulmonary hypertension.
- Proper hydration may help reduce side effects like headaches.
- Patients should report any persistent or severe side effects to a healthcare professional.
Kaplan-Meier Plot of Time (in Days) to Clinical Worsening of PAH in PACES-1 Improvements in WHO Functional Class for PAH were also demonstrated in patients on sildenafil compared to placebo. More than twice as many sildenafil-treated patients (36%) as placebo-treated patients (14%) showed an improvement in at least one functional New York Heart Association (NYHA) class for PAH. Study A1481243 (NCT00323297) - Sildenafil Added to Bosentan Therapy – Lack of Effect on Exercise Capacity A randomized, double-blind, placebo-controlled study was conducted in 103 patients with PAH who were on bosentan therapy for a minimum of 3 months.