Jaspush 100 Mg

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There were no episodes of syncope reported in this study.Effect of sildenafil on Blood Pressure When Co-administered with Anti-hypertensives:When sildenafil 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 of sildenafil on Blood Pressure When Co-administered with Alcohol: Sildenafil (50 mg) did not potentiate the hypotensive effect of alcohol (0.5 g/kg) in healthy volunteers with mean maximum blood alcohol levels of 0.08%. The maximum observed decrease in systolic blood pressure was -18.5 mmHg when sildenafil was co-administered with alcohol versus -17.4 mmHg when alcohol was administered alone. The maximum observed decrease in diastolic blood pressure was -17.2 mmHg when sildenafil was co-administered with alcohol versus -11.1 mmHg when alcohol was administered alone. There were no reports of postural dizziness or orthostatic hypotension.

Patient Group Typical Dose Timing Notes
Adult men with ED 100 mg as needed 30-60 min before sex Max once per day
Patients with PAH 20-40 mg two times daily With meals Adjust dose based on response
Elderly patients Start at 50 mg As prescribed Caution due to potential interactions

The maximum recommended dose of 100 mg sildenafil was not evaluated in this study [ see Drug Interactions (7.5)].Effects of sildenafil 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 on cardiac output.

  • Sildenafil citrate 100mg tablets are used to treat erectile dysfunction in men.
  • The usual recommended dose is 100mg taken about an hour before activity.
  • Sildenafil works by increasing blood flow to the penis during arousal.
  • This medication should not be used with nitrate drugs due to risk of dangerous interactions.
  • Common side effects include headache, flushing, upset stomach, and nasal congestion.
  • Do not take sildenafil more than once in a 24-hour period.
  • Sildenafil can cause hypotension, especially when combined with certain medications.
  • It is available by prescription and should be used under medical supervision.
  • Patients with heart problems should consult their doctor before use.
  • Sildenafil should be stored at room temperature, away from moisture and heat.
  • Alcohol can increase the risk of side effects when taking sildenafil.
  • Sildenafil may cause vision changes such as blue tinge or increased sensitivity to light.

In one small, open-label, uncontrolled, pilot study, eight patients with stable ischemic heart disease underwent Swan-Ganz catheterization.

Dose Adjustments

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. Mean resting values for right atrial pressure, pulmonary artery pressure, pulmonary artery occluded pressure and cardiac output decreased by 28%, 28%, 20% and 7% respectively.

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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.Table 3. Hemodynamic Data in Patients with Stable Ischemic Heart Disease after Intravenous Administration of 40 mg of SildenafilIn 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 100 mg 1 hour prior to exercise testing.

Stronger erections, better sex

The pharmacokinetics of sildenafil in patients with severely impaired hepatic function (Child-Pugh Class C) have not been studied [ see Dosage and Administration (2.5), and Use in Specific Populations (8.7)].Therefore, age >65, hepatic impairment and severe renal impairment are associated with increased plasma levels of sildenafil. A starting oral dose of 25 mg should be considered in those patients [ see Dosage and Administration (2.5)].Drug Interaction StudiesEffects of Other Drugs on sildenafilSildenafil metabolism is principally mediated by CYP3A4 (major route) and CYP2C9 (minor route). Therefore, inhibitors of these isoenzymes may reduce sildenafil clearance and inducers of these isoenzymes may increase sildenafil clearance. The concomitant use of erythromycin or strong CYP3A4 inhibitors (e.g., saquinavir, ketoconazole, itraconazole) as well as the nonspecific CYP inhibitor, cimetidine, is associated with increased plasma levels of sildenafil [ see Dosage and Administration (2.4)].In vivostudies:Cimetidine (800 mg), a nonspecific CYP inhibitor, caused a 56% increase in plasma sildenafil concentrations when co-administered with sildenafil (50 mg) to healthy volunteers.When a single 100 mg dose of sildenafil was administered with erythromycin, a moderate CYP3A4 inhibitor, at steady state (500 mg bid for 5 days), there was a 160% increase in sildenafil C maxand a 182% increase in sildenafil AUC. In addition, in a study performed in healthy male volunteers, co-administration of the HIV protease inhibitor saquinavir, also a CYP3A4 inhibitor, at steady state (1200 mg tid) with sildenafil (100 mg single dose) resulted in a 140% increase in sildenafil C maxand a 210% increase in sildenafil AUC.

What happens with ED?

A stronger CYP3A4 inhibitor such as ketoconazole or itraconazole could be expected to have greater effect than that seen with saquinavir. Population pharmacokinetic data from patients in clinical trials also indicated a reduction in sildenafil clearance when it was co-administered with CYP3A4 inhibitors (such as ketoconazole, erythromycin, or cimetidine) [ see Dosage and Administration (2.4) and Drug Interactions (7.4)].In another study in healthy male volunteers, co-administration with the HIV protease inhibitor ritonavir, which is a highly potent P450 inhibitor, at steady state (500 mg bid) with sildenafil (100 mg single dose) resulted in a 300% (4-fold) increase in sildenafil C maxand a 1000% (11-fold) increase in sildenafil plasma AUC. The primary endpoint was time to limiting angina in the evaluable cohort. The mean times (adjusted for baseline) to onset of limiting angina were 423.6 and 403.7 seconds for sildenafil (N=70) and placebo, respectively.

Ingredient Quantity per Tablet Purpose Notes
Sildenafil Citrate 100 mg Active ingredient Main PDE5 inhibitor
Lactose Monohydrate 50 mg Binder, filler Assists disintegration
Magnesium Stearate 5 mg Lubricant Ensures tablet flow
Microcrystalline Cellulose 20 mg Filler mass Binds ingredients
Hypromellose 10 mg Coating agent Protects active ingredient

These results demonstrated that the effect of sildenafil on the primary endpoint was statistically non-inferior to placebo.Effects sildenafil 12 5 mg of sildenafil 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. This finding is consistent with the inhibition of PDE6, which is involved in phototransduction in the retina. Subjects in the study reported this finding as difficulties in discriminating blue/green. An evaluation of visual function at doses up to twice the maximum recommended dose revealed no effects of sildenafil on visual acuity, intraocular pressure, or pupillometry.Effects of sildenafil on Sperm:There was no effect on sperm motility or morphology after single 100 mg oral doses of sildenafil in healthy volunteers.12.3 PharmacokineticsSildenafil is rapidly absorbed after oral administration, with a mean absolute bioavailability of 41% (range 25-63%).

12.1 Mechanism of Action

There were no episodes of syncope reported in this study.Effect of sildenafil on Blood Pressure When Co-administered with Anti-hypertensives:When sildenafil 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 of sildenafil on Blood Pressure When Co-administered with Alcohol: Sildenafil (50 mg) did not potentiate the hypotensive effect of alcohol (0.5 g/kg) in healthy volunteers with mean maximum blood alcohol levels of 0.08%. The maximum observed decrease in systolic blood pressure was -18.5 mmHg when sildenafil was co-administered with alcohol versus -17.4 mmHg when alcohol was administered alone. The maximum observed decrease in diastolic blood pressure was -17.2 mmHg when sildenafil was co-administered with alcohol versus -11.1 mmHg when alcohol was administered alone. There were no reports of postural dizziness or orthostatic hypotension. The maximum recommended dose of 100 mg sildenafil was not evaluated in this study [ see Drug Interactions (7.5)].Effects of sildenafil 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 on cardiac output.

Take the Next Step Toward Better Performance

In one small, open-label, uncontrolled, pilot study, eight patients with stable ischemic heart disease underwent Swan-Ganz catheterization. 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. Mean resting values for right atrial pressure, pulmonary artery pressure, pulmonary artery occluded pressure and cardiac output decreased by 28%, 28%, 20% and 7% respectively. 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.Table 3. Hemodynamic Data in Patients with Stable Ischemic Heart Disease after Intravenous Administration of 40 mg of SildenafilIn 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 100 mg 1 hour prior to exercise testing. The pharmacokinetics of sildenafil are dose-proportional over the recommended dose range.

Drug Class Interaction Effect Clinical Implication Example Drugs
Nitrates Severe hypotension Contraindicated Nitroglycerin, Isosorbide dinitrate
Alpha-blockers Increased hypotension Dose adjustment required Tamsulosin, Doxazosin
CYP3A4 inhibitors Increased sildenafil levels Risk of side effects Ketoconazole, Ritonavir
Other PDE5 inhibitors Additive effects Avoid combining Tadalafil, Vardenafil

It is eliminated predominantly by hepatic metabolism (mainly CYP3A4) and is converted to an active metabolite with properties similar to the parent, sildenafil. 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. Maximum observed plasma concentrations are reached within 30 to 120 minutes (median 60 minutes) of oral dosing in the fasted state.

What Is Jaspush 100 Mg Tablet?

When sildenafil is taken with a high fat meal, the rate of absorption is reduced, with a mean delay in T maxof 60 minutes and a mean reduction in C maxof 29%. The mean steady state volume of distribution (Vss) for sildenafil is 105 L, indicating distribution into the tissues. Sildenafil and its major circulating N-desmethyl metabolite are both approximately buy sildenafil uk 96% bound to plasma proteins. 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. The major circulating metabolite results from N-desmethylation of sildenafil, and is itself further metabolized.

Alcohol interaction warning

This metabolite has a PDE selectivity profile similar to sildenafil and an in vitropotency for PDE5 approximately 50% of the parent drug. Plasma concentrations of this metabolite are approximately 40% of those seen for sildenafil, so that the metabolite accounts for about 20% of sildenafil’s pharmacologic effects.After either oral or intravenous administration, sildenafil is excreted as metabolites predominantly in the feces (approximately 80% of administered oral dose) and to a lesser extent in the urine (approximately 13% of the administered oral dose). Similar values for pharmacokinetic parameters were seen in normal volunteers and in the patient population, using a population pharmacokinetic approach.Pharmacokinetics in Special PopulationsGeriatrics:Healthy elderly volunteers (65 years or over) had a reduced clearance of sildenafil, resulting in approximately 84% and 107% higher plasma AUC values of sildenafil and its active N-desmethyl metabolite, respectively, compared to those seen in healthy younger volunteers (18-45 years). Due to age-differences in plasma protein binding, the corresponding increase in the AUC of free (unbound) sildenafil and its active N-desmethyl metabolite were 45% and 57%, respectively [ see Dosage and Administration (2.5), and Use in Specific Populations (8.5)]Renal Impairment:In volunteers with mild (CLcr=50-80 mL/min) and moderate (CLcr=30-49 mL/min) renal impairment, the pharmacokinetics of a single oral dose of sildenafil (50 mg) were not altered. In volunteers with severe (CLcr <30 mL/min) renal impairment, sildenafil clearance was reduced, resulting in approximately doubling of AUC and C maxcompared to age-matched volunteers with no renal impairment [ see Dosage and Administration (2.5), and Use in Specific Populations (8.6)].In addition, N-desmethyl metabolite AUC and C maxvalues significantly increased by 200% and 79%, respectively in subjects with severe renal impairment compared to subjects with normal renal function.Hepatic Impairment:In volunteers with hepatic impairment (Child-Pugh Class A and B), sildenafil clearance was reduced, resulting in increases in AUC (85%) and C max(47%) compared to age-matched volunteers with no hepatic impairment. When sildenafil is taken with a high fat meal, the rate of absorption is reduced, with a mean delay in T maxof 60 minutes and a mean reduction in C maxof 29%. The mean steady state volume of distribution (Vss) for sildenafil is 105 L, indicating distribution into the tissues. Sildenafil and its major circulating N-desmethyl metabolite are both approximately buy sildenafil uk 96% bound to plasma proteins.

Detection in biological fluids

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. The major circulating metabolite results from N-desmethylation of sildenafil, and is itself further metabolized.

  • Sildenafil citrate 100mg tablets are FDA-approved for erectile dysfunction.
  • It’s important to adhere to the prescribed timetable to ensure safety.
  • Not suitable for those with severe heart or liver issues without consulting a doctor.
  • Use sildenafil with caution if you have a history of stroke or cardiovascular disease.
  • The medication enhances natural erectile responses, not sexual desire.
  • Avoid grapefruit or grapefruit juice while taking sildenafil due to interactions.
  • Patients should avoid combining sildenafil with recreational drugs.
  • Some users may experience back pain or muscle aches as side effects.
  • Always read the patient information leaflet before use.
  • Report any side effects or unusual symptoms to your healthcare provider.
  • Pregnant or breastfeeding women should avoid using sildenafil.
  • Sildenafil is only effective when sexual stimulation occurs.

This metabolite has a PDE selectivity profile similar to sildenafil and an in vitropotency for PDE5 approximately 50% of the parent drug.

7.1 Nitrates

Plasma concentrations of this metabolite are approximately 40% of those seen for sildenafil, so that the metabolite accounts for about 20% of sildenafil’s pharmacologic effects.After either oral or intravenous administration, sildenafil is excreted as metabolites predominantly in the feces (approximately 80% of administered oral dose) and to a lesser extent in the urine (approximately 13% of the administered oral dose). Similar values for pharmacokinetic parameters were seen in normal volunteers and in the patient population, using a population pharmacokinetic approach.Pharmacokinetics in Special PopulationsGeriatrics:Healthy elderly volunteers (65 years or over) had a reduced clearance of sildenafil, resulting in approximately 84% and 107% higher plasma AUC values of sildenafil and its active N-desmethyl metabolite, respectively, compared to those seen in healthy younger volunteers (18-45 years). Due to age-differences in plasma protein binding, the corresponding increase in the AUC of free (unbound) sildenafil and its active N-desmethyl metabolite were 45% and 57%, respectively [ see Dosage and Administration (2.5), and Use in Specific Populations (8.5)]Renal Impairment:In volunteers with mild (CLcr=50-80 mL/min) and moderate (CLcr=30-49 mL/min) renal impairment, the pharmacokinetics of a single oral dose of sildenafil (50 mg) were not altered.

5.6 Adverse Reactions with the Concomitant Use of Ritonavir

The primary endpoint was time to limiting angina in the evaluable cohort. The mean times (adjusted for baseline) to onset of limiting angina were 423.6 and 403.7 seconds for sildenafil (N=70) and placebo, respectively. These results demonstrated that the effect of sildenafil on the primary endpoint was statistically non-inferior to placebo.Effects sildenafil 12 5 mg of sildenafil 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. This finding is consistent with the inhibition of PDE6, which is involved in phototransduction in the retina. Subjects in the study reported this finding as difficulties in discriminating blue/green.

Serious Side Effects

An evaluation of visual function at doses up to twice the maximum recommended dose revealed no effects of sildenafil on visual acuity, intraocular pressure, or pupillometry.Effects of sildenafil on Sperm:There was no effect on sperm motility or morphology after single 100 mg oral doses of sildenafil in healthy volunteers.12.3 PharmacokineticsSildenafil is rapidly absorbed after oral administration, with a mean absolute bioavailability of 41% (range 25-63%). The pharmacokinetics of sildenafil are dose-proportional over the recommended dose range. It is eliminated predominantly by hepatic metabolism (mainly CYP3A4) and is converted to an active metabolite with properties similar to the parent, sildenafil. 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. Maximum observed plasma concentrations are reached within 30 to 120 minutes (median 60 minutes) of oral dosing in the fasted state. In volunteers with severe (CLcr <30 mL/min) renal impairment, sildenafil clearance was reduced, resulting in approximately doubling of AUC and C maxcompared to age-matched volunteers with no renal impairment [ see Dosage and Administration (2.5), and Use in Specific Populations (8.6)].In addition, N-desmethyl metabolite AUC and C maxvalues significantly increased by 200% and 79%, respectively in subjects with severe renal impairment compared to subjects with normal renal function.Hepatic Impairment:In volunteers with hepatic impairment (Child-Pugh Class A and B), sildenafil clearance was reduced, resulting in increases in AUC (85%) and C max(47%) compared to age-matched volunteers with no hepatic impairment. The pharmacokinetics of sildenafil in patients with severely impaired hepatic function (Child-Pugh Class C) have not been studied [ see Dosage and Administration (2.5), and Use in Specific Populations (8.7)].Therefore, age >65, hepatic impairment and severe renal impairment are associated with increased plasma levels of sildenafil.

  • Sildenafil citrate 100mg tablets are intended for male sexual health issues.
  • Never take more than the prescribed dose to prevent adverse effects.
  • If an erection lasts longer than 4 hours, seek immediate medical help.
  • Consult with a healthcare provider if you experience chest pain after use.
  • Sildenafil can affect blood pressure; monitor symptoms closely.
  • The medication is not suitable for women or children.
  • Use sildenafil only under supervision if you are taking alpha-blockers.
  • It may take some time for the medication to work, depending on individual factors.
  • Do not combine sildenafil with other ED medications unless advised.
  • Discontinue use and consult a healthcare professional if side effects occur.
  • Adequate hydration can help reduce some side effects like headaches.
  • Follow all instructions carefully to maximize treatment benefits.

A starting oral dose of 25 mg should be considered in those patients [ see Dosage and Administration (2.5)].Drug Interaction StudiesEffects of Other Drugs on sildenafilSildenafil metabolism is principally mediated by CYP3A4 (major route) and CYP2C9 (minor route). Therefore, inhibitors of these isoenzymes may reduce sildenafil clearance and inducers of these isoenzymes may increase sildenafil clearance. The concomitant use of erythromycin or strong CYP3A4 inhibitors (e.g., saquinavir, ketoconazole, itraconazole) as well as the nonspecific CYP inhibitor, cimetidine, is associated with increased plasma levels of sildenafil [ see Dosage and Administration (2.4)].In vivostudies:Cimetidine (800 mg), a nonspecific CYP inhibitor, caused a 56% increase in plasma sildenafil concentrations when co-administered with sildenafil (50 mg) to healthy volunteers.When a single 100 mg dose of sildenafil was administered with erythromycin, a moderate CYP3A4 inhibitor, at steady state (500 mg bid for 5 days), there was a 160% increase in sildenafil C maxand a 182% increase in sildenafil AUC. In addition, in a study performed in healthy male volunteers, co-administration of the HIV protease inhibitor saquinavir, also a CYP3A4 inhibitor, at steady state (1200 mg tid) with sildenafil (100 mg single dose) resulted in a 140% increase in sildenafil C maxand a 210% increase in sildenafil AUC. A stronger CYP3A4 inhibitor such as ketoconazole or itraconazole could be expected to have greater effect than that seen with saquinavir. Population pharmacokinetic data from patients in clinical trials also indicated a reduction in sildenafil clearance when it was co-administered with CYP3A4 inhibitors (such as ketoconazole, erythromycin, or cimetidine) [ see Dosage and Administration (2.4) and Drug Interactions (7.4)].In another study in healthy male volunteers, co-administration with the HIV protease inhibitor ritonavir, which is a highly potent P450 inhibitor, at steady state (500 mg bid) with sildenafil (100 mg single dose) resulted in a 300% (4-fold) increase in sildenafil C maxand a 1000% (11-fold) increase in sildenafil plasma AUC.

  • Sildenafil citrate 100mg tablets are prescribed for erectile dysfunction and pulmonary hypertension.
  • The medication enhances the effects of nitric oxide for improved blood flow.
  • Do not use sildenafil if you are allergic to citrate or other components.
  • Commonly prescribed in adult men experiencing erectile difficulty.
  • Patients should avoid heavy meals before taking sildenafil to optimize absorption.
  • Do not barge to take sildenafil if on certain blood pressure medications.
  • Sildenafil may cause skin rashes or allergic reactions in sensitive individuals.
  • Inform your doctor if you experience vision impairment or sudden hearing loss.
  • Use caution when operating machinery or driving after taking sildenafil.
  • This medication has been effective for many men, but results vary.
  • Do not combine sildenafil with other ED medications without medical advice.
  • Always keep sildenafil out of children's reach to prevent accidental ingestion.