Sildenafil 25mg - 8 Tablets

The physiologic mechanism of erection of the penis involves release of nitric oxide (NO) in the corpus cavernosum during sexual stimulation. NO then activates the enzyme guanylate cyclase, which results in increased levels of cyclic guanosine monophosphate (cGMP), producing smooth muscle relaxation in the corpus cavernosum and allowing inflow of blood. Sildenafil at recommended doses has no effect in the absence of sexual stimulation.

Studies in vitrohave shown that sildenafil is selective for PDE5. This lower selectivity is thought to be the basis for abnormalities related to color vision [ see Clinical Pharmacology (12.2)]. In addition to human corpus cavernosum smooth muscle, PDE5 is also found in other tissues including platelets, vascular and visceral smooth muscle, and skeletal muscle, brain, heart, liver, kidney, lung, pancreas, prostate, bladder, testis, and seminal vesicle. The inhibition of PDE5 in some of these tissues by sildenafil may be the basis for the enhanced platelet antiaggregatory activity of NO observed in vitro, an inhibition of platelet thrombus formation in vivoand peripheral arterial-venous dilatation in vivo. Effects ofsildenafil tablets on Erectile Response:In eight double-blind, placebo-controlled crossover studies of patients with either organic or psychogenic erectile dysfunction, sexual stimulation resulted in improved erections, as assessed by an objective measurement of hardness and duration of erections (RigiScan ®), after sildenafil tablets administration compared with placebo. The time course of effect was examined in one study, showing an effect for up to 4 hours but the response was diminished compared to 2 hours.

• Sildenafil 25mg can be part of a physical and psychological treatment plan.
• Follow your doctor’s guidance on how often to take the medication.
• Do not increase the dose to improve results without approval.
• Store tablets at room temperature, away from direct sunlight.
• Be cautious if you are on medications for blood pressure or prostate issues.
• Always complete your treatment course unless advised otherwise.

Effects ofsildenafil tabletson Blood Pressure:Single oral doses of sildenafil (100 mg) administered to healthy volunteers produced decreases in sitting blood pressure (mean maximum decrease in systolic/diastolic blood pressure of 8.3/5.3 mmHg).

• Use sildenafil 25mg as part of a comprehensive ED treatment plan.
• Sexual stimulation is needed for the drug to be effective.
• Do not take sildenafil if you have heart issues without consulting a doctor.
• The medication can cause a temporary vision change.
• Limit physical activity after taking the medication to avoid dizziness.
• Use with caution if you are taking blood pressure medications.

Larger effects were recorded among patients receiving concomitant nitrates [ see Contraindications (4.1)]. Effects ofsildenafil tablets on Blood Pressure When Nitroglycerin is subsequently administered:Based on the pharmacokinetic profile of a single 100 mg oral dose given to healthy normal volunteers, the plasma levels of sildenafil at 24 hours post dose are approximately 2 ng/mL (compared to peak plasma levels of approximately 440 ng/mL). Although plasma levels of sildenafil at 24 hours post dose are much lower than at peak concentration, it is unknown whether nitrates can be safely co-administered at this time point [ see Contraindications (4.1)]. Effects ofSildenafil tablets on Blood Pressure When Co-administered with Alpha-Blockers:Three double-blind, placebo-controlled, randomized, two-way crossover studies were conducted to assess the interaction of sildenafil tablets with doxazosin, an alpha-adrenergic blocking agent. In the first study, a single oral dose of sildenafil tablets100 mg or matching placebo was administered in a 2-period crossover design to 4 generally healthy males with benign prostatic hyperplasia (BPH). The mean sildenafil 130mg subject age was 66.5 years.

GPhC Regulated Pharmacy

The physiologic mechanism of erection of the penis involves release of nitric oxide (NO) in the corpus cavernosum during sexual stimulation. NO then activates the enzyme guanylate cyclase, which results in increased levels of cyclic guanosine monophosphate (cGMP), producing smooth muscle relaxation in the corpus cavernosum and allowing inflow of blood. Sildenafil at recommended doses has no effect in the absence of sexual stimulation. Studies in vitrohave shown that sildenafil is selective for PDE5. This lower selectivity is thought to be the basis for abnormalities related to color vision [ see Clinical Pharmacology (12.2)].

Sildenafil: what you need to know

In addition to human corpus cavernosum smooth muscle, PDE5 is also found in other tissues including platelets, vascular and visceral smooth muscle, and skeletal muscle, brain, heart, liver, kidney, lung, pancreas, prostate, bladder, testis, and seminal vesicle. The inhibition of PDE5 in some of these tissues by sildenafil may be the basis for the enhanced platelet antiaggregatory activity of NO observed in vitro, an inhibition of platelet thrombus formation in vivoand peripheral arterial-venous dilatation in vivo. Effects ofsildenafil tablets on Erectile Response:In eight double-blind, placebo-controlled crossover studies of patients with either organic or psychogenic erectile dysfunction, sexual stimulation resulted in improved erections, as assessed by an objective measurement of hardness and duration of erections (RigiScan ®), after sildenafil tablets administration compared with placebo. The time course of effect was examined in one study, showing an effect for up to 4 hours but the response was diminished compared to 2 hours. Effects ofsildenafil tabletson Blood Pressure:Single oral doses of sildenafil (100 mg) administered to healthy volunteers produced decreases in sitting blood pressure (mean maximum decrease in systolic/diastolic blood pressure of 8.3/5.3 mmHg).

Legal / Prescription Status in India (Schedule H)

Larger effects were recorded among patients receiving concomitant nitrates [ see Contraindications (4.1)]. Effects ofsildenafil tablets on Blood Pressure When Nitroglycerin is subsequently administered:Based on the pharmacokinetic profile of a single 100 mg oral dose given to healthy normal volunteers, the plasma levels of sildenafil at 24 hours post dose are approximately 2 ng/mL (compared to peak plasma levels of approximately 440 ng/mL). Although plasma levels of sildenafil at 24 hours post dose are much lower than at peak concentration, it is unknown whether nitrates can be safely co-administered at this time point [ see Contraindications (4.1)]. Effects ofSildenafil tablets on Blood Pressure When Co-administered with Alpha-Blockers:Three double-blind, placebo-controlled, randomized, two-way crossover studies were conducted to assess the interaction of sildenafil tablets with doxazosin, an alpha-adrenergic blocking agent. In the first study, a single oral dose of sildenafil tablets100 mg or matching placebo was administered in a 2-period crossover design to 4 generally healthy males with benign prostatic hyperplasia (BPH). For the 17 subjects who received sildenafil tablets25 mg and matching placebo, the placebo-subtracted mean maximum decreases from baseline (95% CI) in systolic blood pressure were as follows: The mean profiles of the change from baseline in standing systolic blood pressure in subjects treated with doxazosin in combination with 25 mg sildenafil tablets or matching placebo are shown in Figure 2. Blood pressure was measured immediately pre-dose and at 15, 30, 45 minutes, and 1, 1.5, 2, 2.5, 3, 4, 6 and 8 hours after sildenafil tablets or matching placebo. No severe adverse events potentially related to blood pressure effects were reported in this group. Of the four subjects who received sildenafil tablets100 mg in the first part of this study, a severe adverse event related to blood pressure effect was reported in one patient (postural hypotension that began 35 minutes after dosing with sildenafil tablets with symptoms lasting for 8 hours), and mild adverse events potentially related to blood pressure effects were reported in two others (dizziness, headache and fatigue at 1 hour after dosing; and dizziness, lightheadedness and nausea at 4 hours after dosing). Both of these subjects were protocol violators, one due to a low baseline standing SBP, and the other due to baseline orthostatic hypotension. In the second study, a single oral dose of sildenafil tablets 50 mg or matching placebo was administered in a 2-period crossover design to 20 generally healthy males with BPH.

The mean subject age in this study was 63.9 years. Twenty subjects received sildenafil tablets 50 mg, but only 19 subjects received matching placebo. This patient had been taking minoxidil, a potent vasodilator, during the study. For the 19 subjects who received both sildenafil tablets and matching placebo, the placebo-subtracted mean maximum decreases from baseline (95% CI) in systolic blood pressure were as follows: The mean profiles of the change from baseline in standing systolic blood pressure in subjects treated with doxazosin in combination with 50 mg sildenafil tablets or matching placebo are shown in Figure 3. Blood pressure was measured after administration of sildenafil tablets at the same times as those specified for the first doxazosin study.

There were no severe adverse events potentially related to blood pressure and no episodes of syncope reported in this study. In the third study, a single oral dose of sildenafil tablets 100 mg or matching placebo was administered in a 3-period crossover design to 20 generally healthy males with BPH. The mean subject age in this study was 66.4 years. Two were discontinued after study period 1: one failed to meet pre-dose screening qualifications and the other experienced symptomatic hypotension as a moderately severe adverse event 30 minutes after dosing with open-label sildenafil tablets 50 mg. Of the twenty subjects who were ultimately assigned to treatment, a total of 13 subjects successfully completed dose period 1, and seven had successfully completed the previous doxazosin study (using sildenafil tablets 50 mg). For the 20 subjects who received sildenafil tablets 100 mg and matching placebo, the placebo- subtracted mean maximum decreases from baseline (95% CI) in systolic blood pressure were as follows: The mean profiles of the change from baseline in standing systolic blood pressure in subjects treated with doxazosin in combination with 100 mg sildenafil tablets or matching placebo are shown in Figure 4. Blood pressure was measured after administration of sildenafil tablets at the same times as those specified for the previous doxazosin studies.

There were no episodes of syncope reported in this study. Effect ofsildenafil tablets on Blood Pressure When Co-administered with Anti-hypertensives:When sildenafil tablets 100 mg oral was co-administered with amlodipine, 5 mg or 10 mg oral, to hypertensive patients, the mean additional reduction on supine blood pressure was 8 mmHg systolic and 7 mmHg diastolic.

Related/similar drugs

The mean sildenafil 130mg subject age was 66.5 years. For the 17 subjects who received sildenafil tablets25 mg and matching placebo, the placebo-subtracted mean maximum decreases from baseline (95% CI) in systolic blood pressure were as follows: The mean profiles of the change from baseline in standing systolic blood pressure in subjects treated with doxazosin in combination with 25 mg sildenafil tablets or matching placebo are shown in Figure 2. Blood pressure was measured immediately pre-dose and at 15, 30, 45 minutes, and 1, 1.5, 2, 2.5, 3, 4, 6 and 8 hours after sildenafil tablets or matching placebo. No severe adverse events potentially related to blood pressure effects were reported in this group. Of the four subjects who received sildenafil tablets100 mg in the first part of this study, a severe adverse event related to blood pressure effect was reported in one patient (postural hypotension that began 35 minutes after dosing with sildenafil tablets with symptoms lasting for 8 hours), and mild adverse events potentially related to blood pressure effects were reported in two others (dizziness, headache and fatigue at 1 hour after dosing; and dizziness, lightheadedness and nausea at 4 hours after dosing).

Pulmonary Arterial Hypertension

Both of these subjects were protocol violators, one due to a low baseline standing SBP, and the other due to baseline orthostatic hypotension. In the second study, a single oral dose of sildenafil tablets 50 mg or matching placebo was administered in a 2-period crossover design to 20 generally healthy males with BPH. The mean subject age in this study was 63.9 years. Twenty subjects received sildenafil tablets 50 mg, but only 19 subjects received matching placebo. This patient had been taking minoxidil, a potent vasodilator, during the study.

Sildenafil side effects

For the 19 subjects who received both sildenafil tablets and matching placebo, the placebo-subtracted mean maximum decreases from baseline (95% CI) in systolic blood pressure were as follows: The mean profiles of the change from baseline in standing systolic blood pressure in subjects treated with doxazosin in combination with 50 mg sildenafil tablets or matching placebo are shown in Figure 3. Blood pressure was measured after administration of sildenafil tablets at the same times as those specified for the first doxazosin study. There were no severe adverse events potentially related to blood pressure and no episodes of syncope reported in this study. In the third study, a single oral dose of sildenafil tablets 100 mg or matching placebo was administered in a 3-period crossover design to 20 generally healthy males with BPH. The mean subject age in this study was 66.4 years. Effect ofsildenafil tablets on Blood Pressure When Co-administered with Alcohol:Sildenafil tablets(50 mg) did not potentiate the hypotensive effect of alcohol (0.5 sildenafil citrate tablets 50mg g/kg) in healthy volunteers with mean maximum blood alcohol levels of 0.08%. The maximum recommended dose of 100 mg sildenafil was not evaluated in this study [ see Drug Interactions (7.5)]. Effects ofsildenafil tablets on Cardiac Parameters:Single oral doses of sildenafil up to 100 mg produced no clinically relevant changes in the ECGs of normal male volunteers. Studies have produced relevant data on the effects of sildenafil tablets on cardiac output. A total dose of 40 mg sildenafil was administered by four intravenous infusions. The results from this pilot study are shown in Table 3; the mean resting systolic and diastolic blood pressures decreased by 7% and 10% compared to baseline in these patients. Even though this total dosage produced plasma sildenafil concentrations which were approximately 2 to 5 times higher than the mean maximum plasma concentrations following a single oral dose of 100 mg in healthy male volunteers, the hemodynamic response to exercise was preserved in these patients. In a double-blind study, 144 patients with erectile dysfunction and chronic stable angina limited by exercise, not receiving chronic oral nitrates, were randomized to a single dose of placebo or sildenafil tablets 100 mg 1 hour prior to exercise testing. These results demonstrated that the effect of sildenafil tablets on the primary endpoint was statistically non-inferior to placebo. Effects ofsildenafil tablets on Vision:At single oral doses of 100 mg and 200 mg, transient dose- related impairment of color discrimination was detected using the Farnsworth-Munsell 100-hue test, with peak effects near the time of peak plasma levels. An evaluation of visual function at doses up to twice the maximum recommended dose revealed no effects of sildenafil tablets on visual acuity, intraocular pressure, or pupillometry. Effects ofsildenafil tablets on Sperm: There was no effect on sperm motility or morphology after single 100 mg oral doses of sildenafil tablets in healthy volunteers.

What happens if I overdose?

Two were discontinued after study period 1: one failed to meet pre-dose screening qualifications and the other experienced symptomatic hypotension as a moderately severe adverse event 30 minutes after dosing with open-label sildenafil tablets 50 mg. Of the twenty subjects who were ultimately assigned to treatment, a total of 13 subjects successfully completed dose period 1, and seven had successfully completed the previous doxazosin study (using sildenafil tablets 50 mg). For the 20 subjects who received sildenafil tablets 100 mg and matching placebo, the placebo- subtracted mean maximum decreases from baseline (95% CI) in systolic blood pressure were as follows: The mean profiles of the change from baseline in standing systolic blood pressure in subjects treated with doxazosin in combination with 100 mg sildenafil tablets or matching placebo are shown in Figure 4. Blood pressure was measured after administration of sildenafil tablets at the same times as those specified for the previous doxazosin studies. There were no episodes of syncope reported in this study.

Sildenafil vs. tadalafil

Effect ofsildenafil tablets on Blood Pressure When Co-administered with Anti-hypertensives:When sildenafil tablets 100 mg oral was co-administered with amlodipine, 5 mg or 10 mg oral, to hypertensive patients, the mean additional reduction on supine blood pressure was 8 mmHg systolic and 7 mmHg diastolic. Effect ofsildenafil tablets on Blood Pressure When Co-administered with Alcohol:Sildenafil tablets(50 mg) did not potentiate the hypotensive effect of alcohol (0.5 sildenafil citrate tablets 50mg g/kg) in healthy volunteers with mean maximum blood alcohol levels of 0.08%. The maximum recommended dose of 100 mg sildenafil was not evaluated in this study [ see Drug Interactions (7.5)]. Effects ofsildenafil tablets on Cardiac Parameters:Single oral doses of sildenafil up to 100 mg produced no clinically relevant changes in the ECGs of normal male volunteers. Studies have produced relevant data on the effects of sildenafil tablets on cardiac output.

How sildenafil is used

A total dose of 40 mg sildenafil was administered by four intravenous infusions. The results from this pilot study are shown in Table 3; the mean resting systolic and diastolic blood pressures decreased by 7% and 10% compared to baseline in these patients. Even though this total dosage produced plasma sildenafil concentrations which were approximately 2 to 5 times higher than the mean maximum plasma concentrations following a single oral dose of 100 mg in healthy male volunteers, the hemodynamic response to exercise was preserved in these patients. In a double-blind study, 144 patients with erectile dysfunction and chronic stable angina limited by exercise, not receiving chronic oral nitrates, were randomized to a single dose of placebo or sildenafil tablets 100 mg 1 hour prior to exercise testing. These results demonstrated that the effect of sildenafil tablets on the primary endpoint was statistically non-inferior to placebo. Sildenafil is rapidly absorbed after oral administration, with a mean absolute bioavailability of 41% (range 25–63%). Both sildenafil and the metabolite have terminal half lives of about 4 hours. Mean sildenafil plasma concentrations measured after the administration of a single oral dose of 100 mg to healthy male volunteers is depicted below: Absorption and Distribution:Sildenafil is rapidly absorbed.

• Always use sildenafil 25mg as prescribed by your healthcare provider.
• Avoid driving or operating machinery until effects are known.
• Sildenafil does not protect against sexually transmitted infections.
• Do not share your medication with others.
• Report any allergic reactions like rash or swelling.
• Use caution to prevent falls or injuries due to dizziness.

Protein binding is independent of total drug concentrations. Based upon measurements of sildenafil in semen of healthy volunteers 90 minutes after dosing, less than 0.001% of the administered dose may appear in the semen of patients.

4. Bottom Line

Effects ofsildenafil tablets on Vision:At single oral doses of 100 mg and 200 mg, transient dose- related impairment of color discrimination was detected using the Farnsworth-Munsell 100-hue test, with peak effects near the time of peak plasma levels. An evaluation of visual function at doses up to twice the maximum recommended dose revealed no effects of sildenafil tablets on visual acuity, intraocular pressure, or pupillometry. Effects ofsildenafil tablets on Sperm: There was no effect on sperm motility or morphology after single 100 mg oral doses of sildenafil tablets in healthy volunteers. Sildenafil is rapidly absorbed after oral administration, with a mean absolute bioavailability of 41% (range 25–63%). Both sildenafil and the metabolite have terminal half lives of about 4 hours.

What is sildenafil used for?

Mean sildenafil plasma concentrations measured after the administration of a single oral dose of 100 mg to healthy male volunteers is depicted below: Absorption and Distribution:Sildenafil is rapidly absorbed. Protein binding is independent of total drug concentrations. Based upon measurements of sildenafil in semen of healthy volunteers 90 minutes after dosing, less than 0.001% of the administered dose may appear in the semen of patients. Metabolism and Excretion:Sildenafil is cleared predominantly by the CYP3A4 (major route) and CYP2C9 (minor route) hepatic microsomal isoenzymes.

Interactions that increase your risk for side effects

Metabolism and Excretion:Sildenafil is cleared predominantly by the CYP3A4 (major route) and CYP2C9 (minor route) hepatic microsomal isoenzymes.