Larger effects were recorded among patients receiving concomitant nitrates [ see Contraindications (4)]. Effects of Sildenafil on Vision At single oral doses of 100 mg and 200 mg, transient dose-related impairment of color discrimination (blue/green) was detected using the Farnsworth-Munsell 100-hue test, with peak effects near the time of peak plasma levels. Absorption and Distribution Sildenafil is rapidly absorbed after oral administration, with a mean absolute bioavailability of 41% (25 to 63%). 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%. Metabolism and Excretion Sildenafil is cleared predominantly by the CYP3A (major route) and cytochrome P450 2C9 (CYP2C9, minor route) hepatic microsomal isoenzymes. This metabolite has a phosphodiesterase selectivity profile similar to sildenafil and an in vitropotency for PDE-5 approximately 50% of the parent drug. There was also a doubling of C minlevels compared to healthy volunteers. Pediatric Patients Pediatric use information is approved for Viatris Specialty LLC's, REVATIO (sildenafil) for oral suspension. Geriatric Patients Healthy elderly volunteers (65 years or over) had a reduced clearance of sildenafil, resulting in approximately 84% and 107% higher plasma concentrations of sildenafil and its active N-desmethyl metabolite, respectively, compared to those seen in healthy younger volunteers (18 to 45 years). Renal Impairment In volunteers with mild (CLcr = 50 to 80 mL/min) and moderate (CLcr = 30 to 49 mL/min) renal impairment, the pharmacokinetics of a single oral dose of sildenafil (50 mg) was not altered. In volunteers with severe (CLcr less than 30 mL/min) renal impairment, sildenafil clearance was reduced, resulting in approximately doubling of sildenafil 25 mg tablets AUC and C maxcompared to age-matched volunteers with no renal impairment. In addition, N-desmethyl metabolite AUC and C maxvalues were significantly increased 200% and 79%, respectively, in patients with severe renal impairment compared to patients with normal renal function. Hepatic Impairment In volunteers with mild to moderate hepatic cirrhosis (Child-Pugh class A and B), sildenafil clearance was reduced, resulting in increases in AUC (84%) and C max(47%) compared to age-matched volunteers with no hepatic impairment.
| Precaution/Contraindication | Details | Advice |
|---|---|---|
| Nitrate use | Contraindicated with sildenafil | Risk of severe hypotension |
| Cardiovascular disease risk | Use with caution | Consult cardiologist before use |
| Liver or kidney impairment | Dose adjustment needed | Monitor liver/kidney function tests |
| Allergies to sildenafil or excipients | Check ingredients before administration | Discontinue if allergic reactions occur |
Drug Interaction Studies In vitro studies Sildenafil metabolism is principally mediated by the CYP3A (major route) and CYP2C9 (minor route) cytochrome P450 isoforms. Sildenafil is a weak inhibitor of the cytochrome P450 isoforms 1A2, 2C9, 2C19, 2D6, 2E1 and 3A (IC50 greater than 150 µM). In vivo studies The effects of other drugs on sildenafil pharmacokinetics and the effects of sildenafil on the exposure to other drugs are shown in Figure 1 and Figure 2, respectively. Effects of Other Drugs on Sildenafil Pharmacokinetics CYP3A Inhibitors and Beta Blockers Population pharmacokinetic analysis of data from patients in clinical trials indicated an approximately 30% reduction in sildenafil clearance when it was co-administered with mild/moderate CYP3A inhibitors and an approximately 34% reductions in sildenafil clearance when co-administered with beta-blockers.
What are some things I need to know or do while I take Sildenafil Oral Suspension?
Sildenafil for Oral Suspension (sil den' a fil) Read this Instructions for Use before you start taking sildenafil for oral suspension and each time you get a refill. Supplies you will need to take or give a dose of sildenafil oral suspension (See Figure A): 1 bottle of sildenafil for oral suspension with pre-inserted bottle adaptor 1 oral dosing syringe (provided in the carton) Shake the bottle of sildenafil for oral suspension for 10 seconds before each use. (See Figure E) If your dose of sildenafil for oral suspension is 1 mL (10 mg), measure 0.5 mL two times for a total of 1 mL of sildenafil for oral suspension. (See Figure G) If you are giving sildenafil for oral suspension, make sure they are in an upright position before giving the medicine. This Instructions for Use has been approved by the U.S.
8.2 Lactation
Food and Drug Administration. Manufactured for: Camber Pharmaceuticals, Inc. Piscataway, NJ 08854 SILDENAFIL- sildenafil powder, for suspension Lupin Pharmaceuticals, Inc. Pediatric use information is approved for Viatris Specialty LLC's, REVATIO (sildenafil) tablets. Do not mix with buy sildenafil citrate online canada any other medication or additional flavoring agent White to light yellow colored granular powder containing 1.57 g of sildenafil citrate (equivalent to 1.12 g of sildenafil) in a bottle intended for reconstitution.
2.3 Reconstitution of the Powder for Oral Suspension
Most, patients had underlying anatomic or vascular risk factors for developing NAION, including low cup to disc ratio ("crowded disc"). It is not possible to determine whether these reported events are related directly to the use of sildenafil, to the patient's underlying risk factors for hearing loss, a combination of these factors, or to other factors. Inform patients taking sildenafil for oral suspension not to take VIAGRA or other PDE5 inhibitors. In a 12-week, placebo-controlled clinical study and an open-label extension study (SUPER-1) in 277 sildenafil-treated adults with PAH (WHO Group I) [see Clinical Studies (14)], the adverse reactions that were reported by at least 10% of sildenafil-treated patients in any dosing group,and were more frequent in sildenafil-treated patients than in placebo-treated patients are shown in Table 1. In a placebo-controlled fixed dose titration study (PACES-1) of sildenafil (starting with recommended dose of 20 mg and increased to 40 mg and then 80 mg all three times a day) as an adjunct to intravenous epoprostenol in patients with PAH, no new safety issues were identified except for edema, which occurred in 25% of subjects in the combined sildenafil + epoprostenol group compared with 13% of subjects in the epoprostenol group [see Clinical Studies (14)]. CYP3A4 Inducers Including Bosentan Concomitant administration of strong CYP3A inducers is expected to cause substantial decreases in plasma levels of sildenafil. Epoprostenol The mean reduction of sildenafil (80 mg three times a day) bioavailability when co-administered with epoprostenol was 28%, resulting in about 22% lower mean average steady state concentrations. Alcohol Sildenafil (50 mg) did not potentiate the hypotensive effect of alcohol in healthy volunteers with mean maximum blood alcohol levels of 0.08%. Sildenafil was not carcinogenic when administered to male and female mice for up to 21 and 18 months, respectively, at doses up to a maximally tolerated level of 10 mg/kg/day, a dose equivalent to the RHD on a mg/m 2basis.
- Sildenafil syrup can cause side effects like headaches, flushing, or dizziness.
- Combining sildenafil syrup with nitrates can be dangerous.
- The syrup's consistency may vary; formulation stability is key.
- Misuse or overdose can lead to serious cardiovascular issues.
- Always consult a doctor before using sildenafil syrup.
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. Change from Baseline in 6-Minute tablet sildenafil 50 mg Walk Distance (meters) at Weeks 4, 8, and 12 in SUPER-1: Mean (95% Confidence Interval) 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. Each bottle contains white to off-white crystalline powders containing 1.57 g of sildenafil citrate USP (equivalent to 1.12 g sildenafil). Recommended storage for sildenafil for oral suspension: Store at 20° to 25°C (68° to 77°F) [see USP Controlled Room Temperature] in the original package in order to protect from moisture.
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Manufactured for: Camber Pharmaceuticals, Inc.
11 DESCRIPTION
In a rat pre-and postnatal development study, the no-observed-adverse-effect dose was 30 mg/kg/day (equivalent to 5-times the RHD on a mg/m2 basis). The safety and efficacy of Sildenafil have been established in pediatric patients younger than 1 year of age. Clinical studies of sildenafil did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger patients. Sildenafil citrate is designated chemically as 1-[[3-(6,7-dihydro-1-methyl-7-oxo-3-propyl-1H-pyrazolo [4,3-d] pyrimidin-5-yl)-4-ethoxyphenyl] sulfonyl]-4-methylpiperazine citrate and has the following structural formula: Sildenafil citrate is a white or almost white, slightly hygroscopic, crystalline powder and a molecular weight of 666.7. Sildenafil for Oral Suspension: Sildenafil for oral suspension is supplied as white to light yellow colored granular powder containing 1.57 g of sildenafil citrate (equivalent to1.12 g sildenafil) in an amber glass bottle intended for reconstitution.
Missed Dose
After chronic dosing of 80 mg three times a day to patients with PAH, no clinically relevant effects on electrocardiogram (ECG). 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. The improvement in walk distance was apparent after 4 Week of treatment and was maintained at week 8 and week 12. 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.
Before taking sildenafil,
Piscataway, NJ 08854 This Patient Information has been approved by the U.S. Food and Drug Administration. Sildenafil for Oral Suspension (sil den' a fil) Read this Instructions for Use before you start taking sildenafil for oral suspension and each time you get a refill. Supplies you will need to take or give a dose of sildenafil oral suspension (See Figure A): 1 bottle of sildenafil for oral suspension with pre-inserted bottle adaptor 1 oral dosing syringe (provided in the carton) Shake the bottle of sildenafil for oral suspension for 10 seconds before each use. (See Figure E) If your dose of sildenafil for oral suspension is 1 mL (10 mg), measure 0.5 mL two times for a total of 1 mL of sildenafil for oral suspension. (See Figure G) If you are giving sildenafil for oral suspension, make sure they are in an upright position before giving the medicine. This Instructions for Use has been approved by the U.S. Food and Drug Administration. Manufactured for: Camber Pharmaceuticals, Inc. Piscataway, NJ 08854 SILDENAFIL- sildenafil powder, for suspension Lupin Pharmaceuticals, Inc. Pediatric use information is approved for Viatris Specialty LLC's, REVATIO (sildenafil) tablets. Do not mix with buy sildenafil citrate online canada any other medication or additional flavoring agent White to light yellow colored granular powder containing 1.57 g of sildenafil citrate (equivalent to 1.12 g of sildenafil) in a bottle intended for reconstitution. Most, patients had underlying anatomic or vascular risk factors for developing NAION, including low cup to disc ratio ("crowded disc"). It is not possible to determine whether these reported events are related directly to the use of sildenafil, to the patient's underlying risk factors for hearing loss, a combination of these factors, or to other factors. Inform patients taking sildenafil for oral suspension not to take VIAGRA or other PDE5 inhibitors. In a 12-week, placebo-controlled clinical study and an open-label extension study (SUPER-1) in 277 sildenafil-treated adults with PAH (WHO Group I) [see Clinical Studies (14)], the adverse reactions that were reported by at least 10% of sildenafil-treated patients in any dosing group,and were more frequent in sildenafil-treated patients than in placebo-treated patients are shown in Table 1.
| Region | Estimated Market Size (2023) | Growth Rate | Key Players | Typical Uses Scope |
|---|---|---|---|---|
| North America | $150 million | 5% annually | Pfizer, Cipla, Teva | ED, pulmonary hypertension |
| Europe | $100 million | 4.5% annually | Bayer, Sun Pharma | Pulmonary hypertension, off-label uses |
| Asia-Pacific | $200 million | 7% annually | Cipla, Aurobindo, Zydus | Broader use, pediatric cases |
| Rest of World | $50 million | 3.5% annually | Various local manufacturers | Growing awareness and approval |
In a placebo-controlled fixed dose titration study (PACES-1) of sildenafil (starting with recommended dose of 20 mg and increased to 40 mg and then 80 mg all three times a day) as an adjunct to intravenous epoprostenol in patients with PAH, no new safety issues were identified except for edema, which occurred in 25% of subjects in the combined sildenafil + epoprostenol group compared with 13% of subjects in the epoprostenol group [see Clinical Studies (14)]. In a rat pre-and postnatal development study, the no-observed-adverse-effect dose was 30 mg/kg/day (equivalent to 5-times the RHD on a mg/m2 basis).
- Manufacturing of sildenafil syrup requires specialized equipment.
- The syrup form must undergo stability testing before release.
- Some formulations may include sweeteners to improve taste.
- Off-label compounding can carry legal and safety risks.
- Clinicians should carefully consider risks before prescribing syrup.
The safety and efficacy of Sildenafil have been established in pediatric patients younger than 1 year of age.
8.1 Pregnancy
Larger effects were recorded among patients receiving concomitant nitrates [ see Contraindications (4)]. Effects of Sildenafil on Vision At single oral doses of 100 mg and 200 mg, transient dose-related impairment of color discrimination (blue/green) was detected using the Farnsworth-Munsell 100-hue test, with peak effects near the time of peak plasma levels. Absorption and Distribution Sildenafil is rapidly absorbed after oral administration, with a mean absolute bioavailability of 41% (25 to 63%). 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%. Metabolism and Excretion Sildenafil is cleared predominantly by the CYP3A (major route) and cytochrome P450 2C9 (CYP2C9, minor route) hepatic microsomal isoenzymes.
Incidence not known
This metabolite has a phosphodiesterase selectivity profile similar to sildenafil and an in vitropotency for PDE-5 approximately 50% of the parent drug. There was also a doubling of C minlevels compared to healthy volunteers. Pediatric Patients Pediatric use information is approved for Viatris Specialty LLC's, REVATIO (sildenafil) for oral suspension. Geriatric Patients Healthy elderly volunteers (65 years or over) had a reduced clearance of sildenafil, resulting in approximately 84% and 107% higher plasma concentrations of sildenafil and its active N-desmethyl metabolite, respectively, compared to those seen in healthy younger volunteers (18 to 45 years). Renal Impairment In volunteers with mild (CLcr = 50 to 80 mL/min) and moderate (CLcr = 30 to 49 mL/min) renal impairment, the pharmacokinetics of a single oral dose of sildenafil (50 mg) was not altered.
8.5 Geriatric Use
In volunteers with severe (CLcr less than 30 mL/min) renal impairment, sildenafil clearance was reduced, resulting in approximately doubling of sildenafil 25 mg tablets AUC and C maxcompared to age-matched volunteers with no renal impairment. In addition, N-desmethyl metabolite AUC and C maxvalues were significantly increased 200% and 79%, respectively, in patients with severe renal impairment compared to patients with normal renal function. Hepatic Impairment In volunteers with mild to moderate hepatic cirrhosis (Child-Pugh class A and B), sildenafil clearance was reduced, resulting in increases in AUC (84%) and C max(47%) compared to age-matched volunteers with no hepatic impairment. Drug Interaction Studies In vitro studies Sildenafil metabolism is principally mediated by the CYP3A (major route) and CYP2C9 (minor route) cytochrome P450 isoforms. Sildenafil is a weak inhibitor of the cytochrome P450 isoforms 1A2, 2C9, 2C19, 2D6, 2E1 and 3A (IC50 greater than 150 µM). Clinical studies of sildenafil did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger patients. Sildenafil citrate is designated chemically as 1-[[3-(6,7-dihydro-1-methyl-7-oxo-3-propyl-1H-pyrazolo [4,3-d] pyrimidin-5-yl)-4-ethoxyphenyl] sulfonyl]-4-methylpiperazine citrate and has the following structural formula: Sildenafil citrate is a white or almost white, slightly hygroscopic, crystalline powder and a molecular weight of 666.7. Sildenafil for Oral Suspension: Sildenafil for oral suspension is supplied as white to light yellow colored granular powder containing 1.57 g of sildenafil citrate (equivalent to1.12 g sildenafil) in an amber glass bottle intended for reconstitution.
- Sildenafil syrup is an off-label form of erectile dysfunction medication.
- It's designed for easier ingestion compared to tablets.
- Not approved by most regulatory agencies for syrup form.
- Dosing and safety information are less documented for syrup.
- Usually, sildenafil is available in tablet form, not syrup.
After chronic dosing of 80 mg three times a day to patients with PAH, no clinically relevant effects on electrocardiogram (ECG). 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).
- Contraindications include hypersensitivity to sildenafil.
- Patients with heart conditions should consult a cardiologist before use.
- Sildenafil’s safety profile is well-studied in adults.
- The syrup should not be used with children without medical advice.
- Proper disposal of unused syrup is important to avoid misuse.
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. The improvement in walk distance was apparent after 4 Week of treatment and was maintained at week 8 and week 12.
2.1 Sildenafil for Oral Suspension
In vivo studies The effects of other drugs on sildenafil pharmacokinetics and the effects of sildenafil on the exposure to other drugs are shown in Figure 1 and Figure 2, respectively. Effects of Other Drugs on Sildenafil Pharmacokinetics CYP3A Inhibitors and Beta Blockers Population pharmacokinetic analysis of data from patients in clinical trials indicated an approximately 30% reduction in sildenafil clearance when it was co-administered with mild/moderate CYP3A inhibitors and an approximately 34% reductions in sildenafil clearance when co-administered with beta-blockers. CYP3A4 Inducers Including Bosentan Concomitant administration of strong CYP3A inducers is expected to cause substantial decreases in plasma levels of sildenafil. Epoprostenol The mean reduction of sildenafil (80 mg three times a day) bioavailability when co-administered with epoprostenol was 28%, resulting in about 22% lower mean average steady state concentrations. Alcohol Sildenafil (50 mg) did not potentiate the hypotensive effect of alcohol in healthy volunteers with mean maximum blood alcohol levels of 0.08%.
Common side effects of Sildenafil
Sildenafil was not carcinogenic when administered to male and female mice for up to 21 and 18 months, respectively, at doses up to a maximally tolerated level of 10 mg/kg/day, a dose equivalent to the RHD on a mg/m 2basis. 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. Change from Baseline in 6-Minute tablet sildenafil 50 mg Walk Distance (meters) at Weeks 4, 8, and 12 in SUPER-1: Mean (95% Confidence Interval) 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.
Drug Interactions
Each bottle contains white to off-white crystalline powders containing 1.57 g of sildenafil citrate USP (equivalent to 1.12 g sildenafil). Recommended storage for sildenafil for oral suspension: Store at 20° to 25°C (68° to 77°F) [see USP Controlled Room Temperature] in the original package in order to protect from moisture. Manufactured for: Camber Pharmaceuticals, Inc. Piscataway, NJ 08854 This Patient Information has been approved by the U.S. Food and Drug Administration. 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.