REDSUN Sildenafil Citrate Oral Jelly 100 mg

Composition

Each 5gm Contains:

• Oral Jelly
• Sildenafil Citrate BP equivalent to Sildenafil
• Color: Approved Color Used.
• Flavored base

PHARMACOLOGY:

Pharmacodynamics

Mechanism of Action:

• 100 mg
• q.s.

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 has no direct relaxant effect on isolated human corpus cavernosum, but enhances the effect of nitric oxide (NO) by inhibiting phosphodiesterase type 5 (PDE5), which is responsible for degradation of cGMP in the corpus cavernosum. 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.

Effects of Sildenafil:

• 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, after sildenafil administration compared with placebo.

• On Blood Pressure:
  Single oral doses of sildenafil (100 mg) administered to healthy volunteers produced decreases in supine blood pressure (mean maximum decrease in systolic/diastolic blood pressure of 8.4/5.5 mmHg). The decrease in blood pressure was most notable approximately 1–2 hours after dosing, and was not different than placebo at 8 hours. Larger effects were recorded among patients receiving concomitant nitrates.

• On Cardiac Parameters:
  Single oral doses of sildenafil up to 100 mg produced no clinically relevant changes in the ECGs of normal male volunteers.

• 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.

PHARMACOKINETICS:

• 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. When sildenafil is taken with a high fat meal, the rate of absorption is reduced.

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

INDICATIONS:

Redsun is indicated for the treatment of erectile dysfunction in men.

DOSAGE AND METHOD OF ADMINISTRATION:

Take 100 mg/Dose approximately 1 hour before sexual activity. The maximum recommended dosing frequency is once per day.

Cut, open the sachet and squeeze the jelly into mouth and swallow the whole content of the sachet. One sachet for one time use only.

Redsun jelly melt very fast and is absorbed by the body's enzymes in approximately 30 minutes after taking the medicines. It works for about 2–3 hours after consumption.

The following factors are associated with increased plasma levels of sildenafil:

• Age > 65 (40% increase in AUC)
• Hepatic impairment (e.g., cirrhosis, 80%)
• Severe renal impairment (creatinine clearance <30 mL/min, 100%)
• Concomitant use of potent cytochrome P450 3A4 inhibitors (erythromycin, ketoconazole, itraconazole, ritonavir, saquinavir >200%)

CONTRAINDICATIONS:

Use of Redsun is contraindicated in patients with a known hypersensitivity to any component of the jelly. Consistent with its known effects on the nitric oxide/cGMP pathway, sildenafil was shown to potentiate the hypotensive effects of nitrates, and its administration to patients who are concurrently using organic nitrates in any form is therefore contraindicated. Sildenafil is not indicated for use in women and individuals below 18 years of age.

WARNINGS AND PRECAUTIONS:

Drug Interactions:

Effects of other drugs on sildenafil

• In vitro studies:
  Sildenafil metabolism is principally mediated by the cytochrome P450 (CYP) isoforms 3A4 (major route) and 2C9 (minor route). Therefore, inhibitors of these isoenzymes may reduce sildenafil clearance.

• In vivo studies:
  Cimetidine (800 mg), a non-specific CYP inhibitor, caused a 56% increase in plasma sildenafil concentrations when co-administered with sildenafil (50 mg) to healthy volunteers.

Stronger CYP3A4 inhibitors such as ketoconazole or itraconazole would be expected to have still greater effects, and population data from patients in clinical trials did indicate a reduction in sildenafil clearance when it was co-administered with CYP3A4 inhibitors (such as ketoconazole, erythromycin, or cimetidine). It can be expected that concomitant administration of CYP3A4 inducers, such as rifampin, will decrease plasma levels of sildenafil. Ritonavir, a highly potent P450 inhibitor, resulted in 300% increase in sildenafil C max and 1000% increase in sildenafil plasma AUC. Single doses of antacid (magnesium hydroxide/aluminium hydroxide) did not affect the bioavailability of sildenafil.

Effects of sildenafil on other drugs

• In vitro studies:
  Sildenafil is a weak inhibitor of the cytochrome P450 isoforms 1A2, 2C9, 2C19, 2D6, 2E1 and 3A4 (IC 50 > 150 mM). Given sildenafil peak plasma concentrations of approximately 1μM after recommended doses, it is unlikely that sildenafil will alter the clearance of substrates of these isoenzymes.

• In vivo studies:
  No significant interactions were shown with tolbutamide (250 mg) or warfarin (40 mg), both of which are metabolized by CYP2C9.

Sildenafil (50 mg) did not potentiate the increase in bleeding time caused by aspirin (150 mg).

Sildenafil (50 mg) did not potentiate the hypotensive effect of alcohol in healthy volunteers with mean maximum blood alcohol levels of 0.08%.

Caution in Specific Populations:

There is no controlled clinical data on the safety or efficacy of sildenafil in the following groups; if prescribed, this should be done with caution:

• Patients who have suffered a myocardial infarction, stroke, or life-threatening arrhythmia within the last 6 months

• Patients with resting hypotension (BP <90/50) or hypertension (BP > 170/110)

• Patients with cardiac failure or coronary artery disease causing unstable angina

• Patients with retinitis pigmentosa (a minority of these patients have genetic disorders of retinal phosphodiesterases)

• Renal impairment: Starting dose of 25 mg should be considered

• Hepatic impairment: Starting dose of 25 mg should be considered

PREGNANCY: Category B

There are no adequate and well-controlled studies of sildenafil in pregnant women. Sildenafil is not indicated in women.

LACTATION:

Sildenafil is not indicated in nursing mothers.

PAEDIATRIC USE:

Sildenafil is not indicated in children.

GERIATRIC USE:

Healthy elderly volunteers (65 years or over) had a reduced clearance of sildenafil. Since higher plasma levels may increase both the efficacy and incidence of adverse events, a starting dose of 25 mg should be considered.

UNDESIRABLE EFFECTS:

The most frequent side effects reported with sildenafil use include:

• Headache
• Flushing
• Dyspepsia
• Nasal congestion
• Abnormal vision (mild and transient, predominantly color tinge to vision, but also increased sensitivity to light or blurred vision)
• Urinary tract infection
• Diarrhea
• Dizziness
• Rash

OVERDOSE:

In studies with healthy volunteers of single doses up to 800 mg, adverse events were similar to those seen at lower doses, but incidence rates 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.

STORAGE:

Store in cool & dry place below 30°C. Protect from light. Keep medicines out of reach and sight of children.

PRESENTATION:

Redsun jelly is available in 4 x 5 gm Sachets.

DATE OF PUBLICATION:

June 2023

DATE OF REVIEW:

Every three years

Manufactured in India by / Fabriqué en

RONAK EXIM PVT. LTD.

Gendigate, Baroda-1, (Guj) INDIA/INDE

RONAK E-mail: ahmedi@ronakoverseas.com

GROUP world of Trust

Customer Care No: +91 9998953750

FDA Reg. No.: FDA/SD.233-020099