Sildenafil Oral Film: Package Insert / Prescribing Info
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 vivo and peripheral arterial-venous dilatation in vivo.
| Condition | Recommended Temperature | Humidity Limit | Shelf Life | Notes |
|---|---|---|---|---|
| Cool, dry place | 15-25°C | <60% RH | 2 years | Keep away from sunlight |
| Avoid moisture exposure | Controlled environment | Humidity-sensitive packaging | ||
| Keep in sealed container | N/A | Prevents degradation | ||
| Shelf life after opening | 1 month | Use within established period |
Effects ofSildenafil on Erectile Response:In eight double-blind, placebo-controlled crossover studies of patients with either organic or psychogenic erectile dysfunction, sexual stimulation resulted
| Brand Name | Manufacturer | Price Range | Availability | FDA Approval Status |
|---|---|---|---|---|
| Strips of Eros | PharmaX Ltd. | $15 - $25 | Online, pharmacies | Approved |
| VistoStrips | MedSolutions Inc. | $20 - $30 | Distributors | Pending approval |
| OralEase | BioHealth Corp. | $17 - $24 | Specialty stores | Approved |
| QuickDissolve | NutraPharma | $18 - $28 | Online marketplaces | Approved |
| FastRelief | HealthGen | $16 - $22 | Pharmacies, online | Approved |
in improved erections, as assessed by an objective measurement of hardness and duration of erections (RigiScan®), after sildenafil administration compared with placebo.
1. Introduction
Sildenafil is approximately 4,000-fold more selective for PDE5 compared to PDE3. PDE3 is involved in control of cardiac contractility. Sildenafil is only about 10-fold as potent for PDE5 compared to PDE6, an enzyme found in the retina which is involved in the phototransduction pathway of the retina. 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. Most studies assessed the efficacy of sildenafil approximately 60 minutes post dose.
| Product | Dosage | Quantity + Bonus | Price | |
|---|---|---|---|---|
| Kamagra Soft Tabs | 100mg | 12 Pills | 57.55€ 54.81€ | |
| Kamagra | 100mg | 84 + 6 Pills | 264.44€ 251.85€ | |
| Kamagra Soft Tabs | 100mg | 60 + 4 Pills | 180.59€ 171.99€ | |
| Kamagra Soft Tabs | 100mg | 20 Pills | 79.79€ 75.99€ | |
| Kamagra Soft Tabs | 100mg | 84 + 4 Pills | 233.05€ 221.95€ | |
| Kamagra Polo | 100mg | 120 + 6 Pills | 327.15€ 311.57€ | |
| Viagra Generic | 200mg | 120 + 8 Pills | 204.80€ 195.05€ | |
| Viagra Generic | 200mg | 360 + 10 Pills | 481.98€ 459.03€ | |
| Kamagra | 100mg | 120 + 6 Pills | 330.74€ 314.99€ | |
| Viagra Generic | 150mg | 270 + 10 Pills | 326.61€ 311.06€ | |
| Viagra Generic | 100mg | 90 + 6 Pills | 129.02€ 122.88€ | |
| Viagra Generic | 200mg | 90 + 6 Pills | 170.79€ 162.66€ | |
| Kamagra Polo | 100mg | 84 + 4 Pills | 244.49€ 232.85€ | |
| Viagra Generic | 50mg | 180 + 8 Pills | 158.82€ 151.26€ |
The erectile response, as assessed by RigiScan®, generally increased with increasing sildenafil dose and plasma concentration.
2. Search strategy
The pharmacokinetics of sildenafil in patients with severely impaired hepatic function (Child-Pugh Class C) have not been studied. A starting dose of 25 mg should be considered in patients with any degree of hepatic impairment [see Dosage and Administration (2.3),Clinical Pharmacology (12.3)]. In studies in healthy volunteers administered single sildenafil doses up to 800 mg, adverse reactions were similar to those seen at lower doses, but incidence rates and severities were increased. In cases of overdose, standard supportive measures should be adopted as required. Renal dialysis is not expected to accelerate clearance as sildenafil is highly bound to plasma proteins and it is not eliminated in the urine.
Erectile dysfunction
SILDENAFIL ORAL FILM (sildenafil) oral film is for treatment of erectile dysfunction and contains sildenafil citrate, a selective inhibitor of cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5). SILDENAFIL ORAL FILM is formulated as an opaque light blue, thin, flexible oral film with the characteristic lemon and grapefruit scent. The product is available in four different strengths 25, 50, 75, or 100 mg of sildenafil equivalent to 35, 70, 105, 140 mg sildenafil citrate respectively for oral administration. SILDENAFIL ORAL FILM contains no ingredient made from a gluten-containing grain (wheat, barley, or rye). The physiologic mechanism of erection of the penis involves release of nitric oxide (NO) in the corpus cavernosum during sexual stimulation.
5.6 Adverse Reactions with the Concomitant Use of Ritonavir
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. When sexual stimulation causes local release of NO, inhibition of PDE5 by sildenafil causes increased levels of cGMP in the corpus cavernosum, resulting in smooth muscle relaxation and inflow of blood to the corpus cavernosum. Sildenafil at recommended doses has no effect in the absence of sexual stimulation. Studies in vitro have shown that sildenafil is selective for PDE5. Its effect is more potent on PDE5 than on other known phosphodiesterases (10-fold for PDE6, >80-fold for PDE1, >700-fold for PDE2, PDE3, PDE4, PDE7, PDE8, PDE9, PDE10, and PDE11). 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 oral strips are a fast-acting form of erectile dysfunction medication.
- They are administered orally, dissolving quickly on the tongue for rapid effect.
- Sildenafil strips are often flavored to improve the user experience.
- They contain the same active ingredient as traditional sildenafil tablets.
- These strips are designed for people seeking discreet medication options.
- Onset of action for sildenafil strips can be within 15-30 minutes.
- Proper storage of sildenafil strips involves keeping them in a cool, dry place.
- Dosage strength varies, typically available in 25mg, 50mg, and 100mg.
- Using sildenafil strips without medical consultation is not recommended.
- They may interact with other medications like nitrates or alpha-blockers.
- Sildenafil oral strips are approved for the treatment of erectile dysfunction.
- Users should follow prescribed dosages for safety and effectiveness.
Effects ofSILDENAFIL ORAL FILM on Blood Pressure: Single oral doses (50 mg, 75 mg, 100 mg) of VYBRIQYE administered to 12 healthy young volunteers produced decreases in supine blood pressure.
Chemical synthesis
In the rat pre- and postnatal development study, the no observed adverse effect dose was 30 mg/kg/day given for 36 days, about 2 times the MRHD on a mg/m2 basis in a 50 kg subject. Limited data indicate that sildenafil and its active metabolite are present in human milk. There is no information on the effects on the breastfed child, or the effects on milk production. SILDENAFIL ORAL FILM is not indicated for use in pediatric patients. Safety and effectiveness have not been established in pediatric patients.
12.3 Pharmacokinetics
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 young volunteers (18-45 years) [see Clinical Pharmacology (12.3)] .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 Clinical Pharmacology (12.3)]. Of the total number of subjects in clinical studies of sildenafil, 18% were 65 years and older, while 2% were 75 years and older. No overall differences in safety or efficacy were observed between older (≥ 65 years of age) and younger adult (< 65 years of age) subjects. Of the total number of subjects in the clinical study of SILDENAFIL ORAL FILM, 31% were 65 years and older. No overall differences in safety or efficacy were observed between older (≥ 65 years of age) and younger (< 65 years of age) subjects.
Sildenafil Oral Film Dosage and Administration
A starting dose of SILDENAFIL ORAL FILM 25 mg is recommended in patients 65 years of age and older due to the higher systemic exposure in older subjects, and larger decreases in blood pressure observed in older subjects in a clinical pharmacology study [see Dosage and Administration(2.3),Warnings and Precautions (5.1), Clinical Pharmacology(12.2]. No dose adjustment is required for mild (CLcr=50-80 mL/min) and moderate (CLcr=30-49 mL/min) renal impairment. In volunteers with severe renal impairment (Clcr<30 mL/min), sildenafil clearance was reduced, resulting in higher plasma exposure of sildenafil (~2 fold), approximately doubling of Cmax and AUC. A starting dose of 25 mg should be considered in patients with severe renal impairment [see Dosage and Administration (2.3),Clinical Pharmacology (12.3)] . In volunteers with hepatic impairment (Child-Pugh Class A and B), sildenafil clearance was reduced, resulting in sildenafil 100g higher plasma exposure of sildenafil (47% for Cmax and 85% for AUC). The placebo-subtracted mean maximum decreases in systolic/diastolic blood pressure were 6.1/2.8 mmHg after a single 100 mg dose. Subjects were under fasting conditions and lay in the supine position for the first 4 hours post-dose and were not initially titrated.
- Sildenafil oral strips provide a non-invasive way to treat ED.
- They avoid swallowing pills, which some patients find difficult.
- Strips are often manufactured with pleasant flavors to enhance appeal.
- The medication’s effect can be influenced by food intake.
- Alcohol consumption may reduce effectiveness or increase side effects.
- Sildenafil strips should be used as prescribed and not mixed with other ED drugs.
- These strips are designed for quick absorption in the oral mucosa.
- Overuse or misuse can lead to adverse health effects.
- Proper dosing helps minimize risks of prolonged erections or priapism.
- Sildenafil strips do not cure ED but help manage symptoms.
- They may be used in combination with psychological or lifestyle interventions.
- Always check expiration dates before using sildenafil strips.
The decrease in supine blood pressure was most notable approximately 1-2 hours after dosing.
| Aspect | Strips | Tablets |
|---|---|---|
| Mode of Administration | Sublingual, dissolved in mouth | Oral, swallowed whole |
| Onset of Action | Faster (within 15 minutes) | Slightly slower (30-60 minutes) |
| Dosing Flexibility | Precise, customizable doses | Fixed dose per tablet |
| Convenience | Easy for those with swallowing difficulties | May require water |
| Storage | Compact, no need for water | Requires water for swallowing |
Figure1: Mean Change from Baseline inSupineSystolic Blood Pressure, Healthy Volunteers Single oral doses of 50 mg, 75 mg, 100 mg of SILDENAFIL ORAL FILM administered to 12 elderly volunteers produced decreases in supine blood pressure.
Ease of Use and Convenience
Use caution when co-administering alpha-blockers with sildenafil because of potential additive blood pressure lowering effects. When sildenafil is co-administered with an alpha-blocker, patients should be stable on alpha blocker therapy prior to initiating sildenafil treatment and sildenafil should be initiated at the lowest dose [see Dosage andAdministration(2.2),Warnings and Precautions (5.5), Clinical Pharmacology (12.2)]. When sildenafil 100 mg was co-administered with amlodipine (5 mg or 10 mg) to hypertensive patients, the mean additional reduction on supine blood pressure was 8 mmHg systolic and 7 mmHg diastolic [seeWarnings and Precautions (5.5), Clinical Pharmacology (12.2)]. Co-administration of ritonavir, a strong CYP3A4 inhibitor, greatly increased the systemic exposure of sildenafil (11-fold increase in AUC). It is therefore recommended not to exceed a maximum single dose of 25 mg of sildenafil in a 48 hour period [seeDosage and Administration(2.2), Warnings and Precautions (5.6), Clinical Pharmacology (12.3)].
Kevin Moran
Co-administration of erythromycin, a moderate CYP3A4 inhibitor, resulted in 160% and 182% increases in sildenafil Cmax and AUC, respectively. Co-administration of saquinavir, a strong CYP3A4 inhibitor, resulted in 140% and 210% increases in sildenafil Cmax and AUC, respectively. Stronger CYP3A4 inhibitors such as ketoconazole or itraconazole could be expected to have greater effects than seen with saquinavir. A starting dose of 25 mg of sildenafil should be considered in patients taking erythromycin or strong CYP3A4 inhibitors (such as saquinavir, ketoconazole, itraconazole) [see Dosage and Administration(2.2), Clinical Pharmacology (12.3)]. In a drug-drug interaction study of sildenafil 50 mg given with alcohol 0.5 g/kg, in which mean maximum blood alcohol levels of 0.08% was achieved, sildenafil did not potentiate the hypotensive effect of alcohol in healthy volunteers [see Clinical Pharmacology (12.2)] .
More common
SILDENAFIL ORAL FILM is not indicated for use in females. There are no data with the use of SILDENAFIL ORAL FILM in pregnant women to inform any drug-associated risks for adverse developmental outcomes. Animal reproduction studies conducted with sildenafil did not show adverse developmental outcomes when administered during organogenesis in rats and rabbits at oral doses up to 16 and 32 times, respectively, the maximum recommended human dose (MRHD) of 100 mg/day on a mg/m2 basis ( see Data). No evidence of teratogenicity, embryotoxicity or fetotoxicity was observed in rats and rabbits which received oral doses up to 200 mg/kg/day during organogenesis. These doses represent, respectively, about 16 and 32 times the MRHD on a mg/m2 basis in a 50 kg subject.