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Sildenafil 100 mg Tablet, Film Coated, 30-count — NDC 68071-4617-3 (Billing 68071-4617-03)

by NuCare Pharmaceuticals,Inc. · 30 TABLET, FILM COATED in 1 BOTTLE

This is a package of 30 tablets of Sildenafil 100 mg Tablet, Film Coated from NuCare Pharmaceuticals,Inc., marketed since Jun 2018 and currently FDA-listed. It is this product's only package size.

NDC 68071-4617-03
🏷️ FDA NDC (as labeled) 68071-4617-3 billing pads the package segment with a zero
Rx only Generic On market Non-controlled ⇄ Compare with another NDC
🗂️ FDA directory synced Oct 1, 2026 · this listing last changed Jul 24, 2026 · sources: openFDA · FDA label (DailyMed) · FDA Orange & Purple Book · First Databank · CMS NADAC, ASP, Medicare & Medicaid · RxNorm
📋 All sources & update times →

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Compiled from public FDA, CMS, DailyMed, NADAC, and related drug data sources. Editorial policy

Identity & classification

Regulatory identifiers FDA, NLM and CMS codes for this package

FDA NDC (as labeled) 68071-4617-3
Product NDC 68071-4617
11-digit billing NDC 68071461703
RxCUI 314229
UNII BW9B0ZE037
UPC 0368071461732
Application # ANDA202659
SPL Set ID 7925711e-2e89-fd93-e053-2991aa0a507f
Established class (EPC) Phosphodiesterase 5 Inhibitor
Mechanism of action Phosphodiesterase 5 Inhibitors
DEA schedule Non-controlled
Marketing category ANDA
Marketing status On market
FDA listing status Listed (active directory)
Marketing start 2018-06-11
Route ORAL
Dosage form TABLET, FILM COATED
Substance SILDENAFIL CITRATE
TE code (Orange Book) AB · RLD · RS
Quick answers
  • RxCUI (RxNorm): 314229
Why two NDCs? The FDA registers this code as 68071-4617-3 — a 5-4-1 layout, and that's what's printed on the package and shown on DailyMed. For insurance claims, every NDC is standardized to a uniform 11-digit 5-4-2 format by adding a zero to the package segment → 68071-4617-03. Same drug, same package — only the format differs.
Where does this data come from?
Identifiers from the FDA openFDA NDC Directory and Structured Product Labeling; RxCUI from RxNorm (NLM); GPI from Medi-Span; GCN / HIC / AHFS / legend from First Databank.

RxNorm drug class

This medicine belongs to the Phosphodiesterase 5 Inhibitor class.

Pharmacologic class Phosphodiesterase 5 Inhibitor
Drug family (ATC) Drugs used in erectile dysfunction
How it works Phosphodiesterase 5 Inhibitors
Where does this data come from?
Therapeutic classes from RxNorm RxClass (U.S. National Library of Medicine) — Established Pharmacologic Class (FDA), ATC drug family (WHO) and mechanism of action, matched by this product’s RxCUI.

Clinical

📗 Our plain-language guide HelloPharmacist
  • It depends on the product. Viagra, Vybrique and some sildenafil tablets and oral films treat erectile dysfunction. Revatio and other sildenafil tablets, suspension and injection tr...
  • You take it as needed, usually about 1 hour before sex, though anywhere from 30 minutes to 4 hours works. Take it no more than once a day, with or without food. Oral film goes on y...
  • How do I take it for erectile dysfunction?
  • The common ones are headache, flushing, upset stomach, a stuffy nose and dizziness. Some people notice a color tinge or blur in their vision, which is usually mild and short-lived....
📖 Read our full Sildenafil guide →
Where does this data come from?
Plain-language summary from MedlinePlus (U.S. National Library of Medicine); supplement & herbal interactions and nutrient depletion data from the Natural Medicines database; our full guide is HelloPharmacist editorial content.

Pricing

A drug doesn't have one price. Each row is a different public payment system, and none is what you'd pay at the counter — that depends on your insurance. The ⓘ on each row explains what it measures.

Price systemPer eachPer package
Retail pharmacies payNADAC · weekly Not in the retail survey — common for institutional, discontinued, or low-volume packs.
Medicaid paysCMS SDUD · 12 mo No recent Medicaid claims on file for this NDC — rare and low-volume NDCs are suppressed in the public data.
Medicare drug plans payPart D · quarterly No Part D plan price is available for this NDC in our data.
ℹ️
No price is published for this exact package yet. CMS surveys NADAC per package size, so a different pack of the same drug often has one.
Where does this data come from?
NADAC (National Average Drug Acquisition Cost) is the CMS weekly pharmacy-acquisition-cost survey — what pharmacies pay. ASP (Average Sales Price) is the CMS Medicare Part B drug-payment file, published quarterly. Medicaid pays is computed by us from CMS State Drug Utilization Data (total reimbursed ÷ units, trailing 12 months) — gross of rebates and inclusive of dispensing fees, so it reflects what Medicaid paid, not an acquisition cost. Medicare drug plans pay is the median negotiated point-of-sale unit cost across plans listing this NDC in the CMS quarterly Prescription Drug Plan pricing files, before rebates. The VA pays is the federal contract price (FSS, and the statutory Big 4 ceiling where listed) from the VA National Acquisition Center pharmaceutical price file. All are free public government data; each measures a different payer, so the figures are not directly comparable.

Packaging — all sizes for this product

Package NDCDescription Marketing startMarketing endStatus
68071-4617-03 You're viewing this Main listing 30 TABLET, FILM COATED in 1 BOTTLE 2018-10-26 — Active

Therapeutic equivalents

ProductLabelerPackNADAC/unitTEStatusPrice vs. this
Sildenafil 100 mg 00093-5343-01 Teva 100 tablets $0.132 AB Availability likely —
Sildenafil Citrate 100 mg 13668-0188-01 Torrent 100 tablets $0.132 AB Availability likely —
Sildenafil Citrate 100 mg 27241-0069-03 Ajanta 30 tablets $0.132 AB Availability likely —
Sildenafil 100 mg 31722-0711-01 Camber 100 tablets $0.132 AB Availability likely —
Sildenafil 100 mg 33342-0043-07 Macleods 30 tablets $0.132 AB Availability likely —
Sildenafil Citrate 100 mg 60290-0003-01 Umedica 30 tablets $0.132 AB Availability likely —
Sildenafil 100 mg 65862-0691-01 Aurobindo 100 tablets $0.132 AB Availability likely —
Sildenafil 100 mg 72241-0071-05 Modavar 100 tablets $0.132 AB Availability likely —
Sildenafil Citrate 100 mg 72603-0885-01 Northstar 30 tablets $0.132 AB Availability likely —
Sildenafil 100 mg 72888-0017-00 Advagen 1000 tablets $0.132 AB Availability likely —
Sildenafil Citrate 100 mg 75834-0241-00 NIVAGEN 1000 tablets $0.132 AB Availability likely —
Sildenafil 100 mg 76282-0645-01 Exelan 100 tablets $0.132 AB Availability likely —
Sildenafil Citrate 100 mg 82009-0093-01 Quallent 100 tablets $0.132 AB Availability likely —
Sildenafil Citrate 100 mg 59762-0036-01 Mylan 30 tablets $0.200 AB Discontinued —
Sildenafil 100 mg 69097-0953-02 CIPLA 30 tablets $0.259 AB FDA listed —
Viagra 100 mg 00069-4220-30 PFIZER 30 tablets $83.717 AB Availability likely —
Viagra 100 mg 58151-0428-01 Viatris 100 tablets $83.717 AB Availability likely —
Sildenafil 100 mg 31722-0967-01 Camber 100 tablets — AB FDA listed —
Sildenafil 100 mg 35561-0253-10 Bostal 30 tablets — AB FDA listed —
Sildenafil Citrate 100 mg 43063-0940-10 PD-Rx 10 tablets — AB FDA listed —
Sildenafil 100 mg 50090-5325-00 A-S 10 tablets — AB FDA listed —
Sildenafil 100 mg 50090-7964-00 A-S 10 tablets — AB FDA listed —
Sildenafil 100 mg 51655-0468-54 Northwind 15 tablets — AB FDA listed —
Sildenafil Citrate 100 mg 51655-0794-54 Northwind 15 tablets — AB FDA listed —
Sildenafil 100 mg 52817-0342-10 TruPharma 100 tablets — AB FDA listed —
Sildenafil 100 mg 55801-0340-01 Appco 30 tablets — AB FDA listed —
Sildenafil 100 mg 60219-1753-01 Amneal 100 tablets — AB FDA listed —
Sildenafil 100 mg 68071-2985-03 NuCare 30 tablets — AB FDA listed —
Sildenafil Citrate 100 mg 68071-3410-03 NuCare 30 tablets — AB FDA listed —
Sildenafil Citrate 100 mg 68071-3549-05 NuCare 15 tablets — AB FDA listed —
Sildenafil 100 mg 68071-3832-03 NuCare 30 tablets — AB FDA listed —
Sildenafil Citrate 100 mg 68071-3862-01 NuCare 10 tablets — AB FDA listed —
Sildenafil 100 mg 68071-3908-01 NuCare 10 tablets — AB FDA listed —
Sildenafil 100 mg 68071-4599-01 NuCare 10 tablets — AB FDA listed —
Sildenafil 100 mgthis 68071-4617-03 NuCare 30 tablets — AB FDA listed —
Sildenafil Citrate 100 mg 68788-4111-01 Preferred 10 tablets — AB FDA listed —
Sildenafil 100 mg 68788-7879-01 Preferred 10 tablets — AB FDA listed —
Sildenafil Citrate 100 mg 68788-8301-01 Preferred 10 tablets — AB FDA listed —
Sildenafil Citrate 100 mg 68788-8804-01 Preferred 10 tablets — AB FDA listed —
Sildenafil Citrate 100 mg 70954-0409-10 ANI 30 tablets — AB FDA listed —
Sildenafil 100 mg 71205-0088-10 Proficient 10 tablets — AB FDA listed —
Sildenafil 100 mg 71205-0220-10 Proficient 10 tablets — AB FDA listed —
Sildenafil Citrate 100 mg 71205-0231-10 Proficient 10 tablets — AB FDA listed —
Sildenafil 100 mg 71205-0473-10 Proficient 10 tablets — AB FDA listed —
Sildenafil 100 mg 71205-0498-02 Proficient 2 tablets — AB FDA listed —
Sildenafil Citrate 100 mg 71205-0657-10 Proficient 10 tablets — AB FDA listed —
Sildenafil 100 mg 71209-0108-01 Cadila 30 tablets — AB FDA listed —
Sildenafil 100 mg 71335-0969-00 Bryant 15 tablets — AB FDA listed —
Sildenafil 100 mg 71335-1088-00 Bryant 15 tablets — AB Discontinued —
Sildenafil Citrate 100 mg 71335-1437-00 Bryant 15 tablets — AB FDA listed —
Sildenafil 100 mg 71335-1777-00 Bryant 15 tablets — AB FDA listed —
Sildenafil Citrate 100 mg 71335-3049-00 Bryant 15 tablets — AB FDA listed —
Sildenafil 100 mg 71610-0675-02 Aphena 2 tablets — AB FDA listed —
Sildenafil 100 mg 72189-0069-10 DIRECT 10 tablets — AB FDA listed —
Sildenafil 100 mg 72303-0847-01 HEC 30 tablets — AB FDA listed —
Sildenafil 100 mg 72789-0098-10 PD-Rx 10 tablets — AB FDA listed —
Sildenafil Citrate 100 mg 72789-0406-15 PD-Rx 15 tablets — AB FDA listed —
Sildenafil 100 mg 72865-0103-01 XLCARE 100 tablets — AB FDA listed —
Sildenafil Citrate 100 mg 76420-0565-01 Asclemed 100 tablets — AB FDA listed —
Sildenafil Citrate 100 mg 80425-0410-01 Advanced 6 tablets — AB FDA listed —
Sildenafil Citrate 100 mg 80425-0503-01 Advanced 30 tablets — AB FDA listed —
Sildenafil 100 mg 82647-0212-14 Reyoung 1000 tablets — AB FDA listed —
Sildenafil Citrate 100 mg 82804-0025-30 Proficient 30 tablets — AB FDA listed —
Sildenafil 100 mg 59746-0436-01 Jubilant 100 tablets — AB FDA listed —
About this product: this is a generic version of the medicine. FDA equivalence ratings are shown when available, and other versions are listed above, least expensive first.
Where does this data come from?
Equivalents are other NDCs of the same ingredient, form and route from the openFDA NDC Directory, ranked least-expensive-first by NADAC. Therapeutic-equivalence (AB) ratings come from the FDA Orange Book; biologics use the FDA Purple Book for biosimilar & interchangeable status.

Availability & generic status

🏛️
2018
On the market since
Jun 2018
📍
2026
Currently FDA-listed
8 years listed
🔓
·
Generic on the market
this product is a generic
✅This is a generic drug

This product is an FDA-approved generic. Other versions of the same drug are listed under Therapeutic equivalents, least expensive first.

Where does this data come from?
Patents and exclusivity from the FDA Orange Book (small-molecule drugs), refreshed from public FDA data. Generic launch timing is an estimate, not a guarantee.

Inactive Ingredients / Excipients

Inactive ingredients, also called excipients, are components of the drug product other than the active ingredient. They may include fillers, dyes, coatings, preservatives, flavors, or other formulation ingredients.

Loading inactive ingredients from the official FDA label in the background. No external source is being called by this page request.
Where does this data come from?
Source: official FDA Structured Product Labeling (SPL) via DailyMed and the openFDA label index. Structured IACT rows and label-wide narrative are kept separate; availability and product-level specificity depend on the submitted label.

Inactive ingredient FAQ

Are inactive ingredients the same for every manufacturer?
No. Inactive ingredients can differ by manufacturer, dosage form, strength, and package / product version.
Why might an inactive ingredient be missing?
Some SPLs do not provide a complete structured inactive-ingredient list, and older or unusual labels may only include the information in narrative text.
Can inactive ingredients matter?
Yes. They can matter for allergies, intolerances, dyes, gluten / lactose concerns, preservatives, and formulation differences — but confirm with a pharmacist or the manufacturer when it’s clinically important.

Manufacturer & labeler

LabelerNuCare Pharmaceuticals,Inc.
Application holderHETERO LABS LTD UNIT V
FDA applicationANDA202659 (ANDA)
Labeler code68071
First marketedJun 2018
Product typeHuman Prescription Drug
Portfolio1,015 products on file
The labeler markets the product; the application holder owns the FDA approval. They’re often the same company but can differ (e.g. a repackager or an authorized generic). A mailing address / phone appears here when the manufacturer includes it in the product’s FDA label (not all do).
Where does this data come from?
Labeler, application holder and registered establishment from the FDA openFDA NDC Directory and Drugs@FDA; address/contact from the product’s FDA label.

Full prescribing information FDA SPL

The complete FDA label for this product — the official prescribing information, verbatim, section by section. Very long sections are excerpted here and marked; the full text is on DailyMed (linked in the sources below). Jump with a chip, search within the label, or expand everything.
🎯 Indications and Usage ⏱️ Dosage and Administration 💊 Dosage Forms and Strengths ⛔ Contraindications ⚠️ Warnings and Cautions 🤒 Adverse Reactions 🔄 Drug Interactions 👥 Use in Specific Populations 🤰 Pregnancy 🧒 Pediatric Use 🧓 Geriatric Use 🆘 Overdosage 🧬 Clinical Pharmacology 🧬 Mechanism of Action 📦 How Supplied / Storage and Handling 📋 Description 💬 Information for Patients 🧬 Pharmacokinetics 🧬 Pharmacodynamics 🔬 Clinical Studies 🧪 Nonclinical Toxicology 📄 Carcinogenesis, Mutagenesis, Impairment of Fertility 📄 Recent Major Changes 📄 Package Label / Principal Display Panel
🎯 Indications and Usage 30 words ▾

1 INDICATIONS & USAGE Sildenafil tablets are indicated for the treatment of erectile dysfunction. Sildenafil tablet is a phosphodiesterase-5 (PDE5) inhibitor indicated for the treatment of erectile dysfunction (ED) (1)

⏱️ Dosage and Administration ~2 min read ▾

2 DOSAGE & ADMINISTRATION •For most patients, the recommended dose is 50 mg taken, as needed, approximately 1 hour before sexual activity. However, sildenafil tablets may be taken anywhere from 30 minutes to 4 hours before sexual activity (2.1) •Based on effectiveness and toleration, may increase to a maximum of 100 mg or decrease to 25 mg (2.1) •Maximum recommended dosing frequency is once per day (2.1)

2.1Dosage Information For most patients, the recommended dose is 50 mg taken, as needed, approximately 1 hour before sexual activity. However, sildenafil tablets may be taken anywhere from 30 minutes to 4 hours before sexual activity. The maximum recommended dosing frequency is once per day. Based on effectiveness and toleration, the dose may be increased to a maximum recommended dose of 100 mg or decreased to 25 mg.

2.2Use with Food Sildenafil tablets may be taken with or without food.

2.3Dosage Adjustments in Specific Situations Sildenafil tablets were shown to potentiate the hypotensive effects of nitrates and its administration in patients who use nitric oxide donors such as organic nitrates or organic nitrites in any form is therefore contraindicated [see Contraindications (4.1), Drug Interactions (7.1), and Clinical Pharmacology (12.2)]. When sildenafil tablets are co-administered with an alpha-blocker, patients should be stable on alpha-blocker therapy prior to initiating sildenafil tablets treatment and sildenafil tablets should be initiated at 25 mg [see Warnings and Precautions (5.5), Drug Interactions (7.2), and Clinical Pharmacology (12.2)].

2.4Dosage Adjustments Due to Drug Interactions Ritonavir The recommended dose for ritonavir-treated patients is 25 mg prior to sexual activity and the recommended maximum dose is 25 mg within a 48 hour period because concomitant administration increased the blood levels of sildenafil by 11-fold [see Warnings and Precautions (5.6), Drug Interactions (7.4), and Clinical Pharmacology (12.3)]. CYP3A4 Inhibitors Consider a starting dose of 25 mg in patients treated with strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, or saquinavir) or erythromycin.

Clinical data have shown that co-administration with saquinavir or erythromycin increased plasma levels of sildenafil by about 3 fold [see Drug Interactions (7.4) and Clinical Pharmacology (12.3)].

2.5Dosage Adjustments in Special Populations Consider a starting dose of 25 mg in patients > 65 years, patients with hepatic impairment (e.g., cirrhosis), and patients with severe renal impairment (creatinine clearance <30 mL/minute) because administration of sildenafil tablets in these patients resulted in higher plasma levels of sildenafil [see Use in Specific Populations ( 8.5, 8.6, 8.7) and Clinical Pharmacology ( 12.3)].

💊 Dosage Forms and Strengths 88 words ▾

3 DOSAGE FORMS & STRENGTHS Sildenafil Tablets USP, 25 mg are white colored, round-shaped, biconvex, film coated tablets debossed with 'I' on one side and '35' on the other side. Sildenafil Tablets USP, 50 mg are white colored, round-shaped, biconvex, film coated tablets debossed with 'I' on one side and '36' on the other side. Sildenafil Tablets USP, 100 mg are white colored, round-shaped, biconvex, film coated tablets debossed with 'I' on one side and '58' on the other side.

Tablets: 25 mg, 50 mg, 100 mg (3)

⛔ Contraindications ~1 min read ▾

4 CONTRAINDICATIONS •Administration of sildenafil tablets to patients using nitric oxide donors, such as organic nitrates or organic nitrites in any form. Sildenafil tablets were shown to potentiate the hypotensive effect of nitrates ( 4.1 , 7.1 , 12.2 ) •Known hypersensitivity to sildenafil or any component of tablet (4.2) •Administration with guanylate cyclase (GC) stimulators, such as riociguat (4.3)

4.1Nitrates Consistent with its known effects on the nitric oxide/cGMP pathway [see Clinical Pharmacology ( 12.1 , 12.2)] , sildenafil tablets were shown to potentiate the hypotensive effects of nitrates, and its administration to patients who are using nitric oxide donors such as organic nitrates or organic nitrites in any form either regularly and/or intermittently is therefore contraindicated. After patients have taken sildenafil tablets, it is unknown when nitrates, if necessary, can be safely administered. 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 Dosage and Administration (2.3), Drug Interactions (7.1), and Clinical Pharmacology (12.2)].

4.2Hypersensitivity Reactions Sildenafil tablets are contraindicated in patients with a known hypersensitivity to sildenafil, as contained in sildenafil tablets and REVATIO, or any component of the tablet. Hypersensitivity reactions have been reported, including rash and urticaria [see Adverse Reactions (6.1)].

4.3Concomitant Guanylate Cyclase (GC) Stimulators Do not use sildenafil tablets in patients who are using a GC stimulator, such as riociguat. PDE5 inhibitors, including sildenafil tablets, may potentiate the hypotensive effects of GC stimulators.

⚠️ Warnings and Cautions ~3 min read ▾

5 WARNINGS AND PRECAUTIONS •Patients should not use sildenafil tablets if sexual activity is inadvisable due to cardiovascular status (5.1) •Patients should seek emergency treatment if an erection lasts >4 hours. Use sildenafil tablets with caution in patients predisposed to priapism (5.2) •Patients should stop sildenafil tablets and seek medical care if a sudden loss of vision occurs in one or both eyes, which could be a sign of non arteritic anterior ischemic optic neuropathy (NAION). Sildenafil tablets should be used with caution, and only when the anticipated benefits outweigh the risks, in patients with a history of NAION.

Patients with a”crowded” optic disc may also be at an increased risk of NAION. (5.3) •Patients should stop sildenafil tablets and seek prompt medical attention in the event of sudden decrease or loss of hearing (5.4) •Caution is advised when sildenafil tablets are co-administered with alpha-blockers or anti-hypertensives. Concomitant use may lead to hypotension (5.5) •Decreased blood pressure, syncope, and prolonged erection may occur at higher sildenafil exposures.

In patients taking strong CYP inhibitors, such as ritonavir, sildenafil exposure is increased. Decrease in sildenafil tablets dosage is recommended (2.4, 5.6)

5.1Cardiovascular There is a potential for cardiac risk of sexual activity in patients with preexisting cardiovascular disease. Therefore, treatments for erectile dysfunction, including sildenafil tablets, should not be generally used in men for whom sexual activity is inadvisable because of their underlying cardiovascular status. The evaluation of erectile dysfunction should include a determination of potential underlying causes and the identification of appropriate treatment following a complete medical assessment.

Sildenafil tablets have systemic vasodilatory properties that resulted in transient decreases in supine blood pressure in healthy volunteers (mean maximum decrease of 8.4/5.5 mmHg), [see Clinical Pharmacology (12.2)]. While this normally would be expected to be of little consequence in most patients, prior to prescribing sildenafil tablets, physicians should carefully consider whether their patients with underlying cardiovascular disease could be affected adversely by such vasodilatory effects, especially in combination with sexual activity.

Use with caution in patients with the following underlying conditions which can be particularly sensitive to the actions of vasodilators including sildenafil tablets – those with left ventricular outflow obstruction (e.g., aortic stenosis, idiopathic hypertrophic subaortic stenosis) and those with severely impaired autonomic control of blood pressure. There are no controlled clinical data on the safety or efficacy of sildenafil tablets 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 mmHg) or hypertension (BP >170/110 mmHg); •Patients with cardiac failure or coronary artery disease causing unstable angina.

5.2Prolonged Erection and Priapism Prolonged erection greater than 4 hours and priapism (painful erections greater than 6 hours in duration) have been reported infrequently since market approval of sildenafil tablets. In the event of an erection that persists longer than 4 hours, the patient should seek immediate medical assistance. If priapism is not treated immediately, penile tissue damage and permanent loss of potency could result.

Sildenafil tablets should be used with caution in patients with anatomical deformation of the penis (such as angulation, cavernosal fibrosis or Peyronie's disease), or in patients who have conditions which may predispose them to priapism (such as sickle cell anemia, multiple myeloma, or leukemia). However, there are no controlled clinical data on the safety or efficacy of sildenafil tablets in patients with sickle… [Excerpted — this section continues on DailyMed.]

🤒 Adverse Reactions ~3 min read ▾

6 ADVERSE REACTIONS The following are discussed in more detail in other sections of the labeling: •Cardiovascular [see Warnings and Precautions (5.1)] •Prolonged Erection and Priapism [see Warnings and Precautions (5.2)] •Effects on the Eye [see Warnings and Precautions (5.3)] •Hearing Loss [ see Warnings and Precautions (5.4)] •Hypotension when Co-administered with Alpha-blockers or Anti-hypertensives [see Warnings and Precautions (5.5)] •Adverse Reactions with the Concomitant Use of Ritonavir [see Warnings and Precautions (5.6)] •Combination with other PDE5 Inhibitors or Other Erectile Dysfunction Therapies [see Warnings and Precautions (5.7)] •Effects on Bleeding [see Warnings and Precautions (5.8)] •Counseling Patients About Sexually Transmitted Diseases [see Warnings and Precautions (5.9)] The most common adverse reactions reported in clinical trials (≥ 2%) are headache, flushing, dyspepsia, abnormal vision, nasal congestion, back pain, myalgia, nausea, dizziness, and rash.

Most common adverse reactions (≥ 2%) include headache, flushing, dyspepsia, abnormal vision, nasal congestion, back pain, myalgia, nausea, dizziness and rash (6.1) To report SUSPECTED ADVERSE REACTIONS, contact Hetero Labs Limited at 866-495-1995 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch

6.1Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in clinical practice. Sildenafil tablets were administered to over 3700 patients (aged 19 to 87 years) during pre-marketing clinical trials worldwide. Over 550 patients were treated for longer than one year.

In placebo-controlled clinical studies, the discontinuation rate due to adverse reactions for sildenafil tablets (2.5%) was not significantly different from placebo (2.3%). In fixed-dose studies, the incidence of some adverse reactions increased with dose. The type of adverse reactions in flexible-dose studies, which reflect the recommended dosage regimen, was similar to that for fixed-dose studies.

At doses above the recommended dose range, adverse reactions were similar to those detailed in Table 1 below but generally were reported more frequently. Table 1: Adverse Reactions Reported by ≥2% of Patients with Sildenafil Tablets and More Frequently than Placebo in Fixed-Dose Phase II/III Studies Adverse Reaction 25 mg (n=312) 50 mg (n=511) 100 mg (n=506) Placebo (n=607) Headache 16% 21% 28% 7% Flushing 10% 19% 18% 2% Dyspepsia 3% 9% 17% 2% Abnormal vision † 1% 2% 11% 1% Nasal congestion 4% 4% 9% 2% Back pain 3% 4% 4% 2% Myalgia 2% 2% 4% 1% Nausea 2% 3% 3% 1% Dizziness 3% 4% 3% 2% Rash 1% 2% 3% 1% † Abnormal Vision: Mild to moderate in severity and transient, predominantly color tinge to vision, but also increased sensitivity to light, or blurred vision.

When sildenafil tablets were taken as recommended (on an as-needed basis) in flexible-dose, placebo-controlled clinical trials of two to twenty-six weeks duration, patients took sildenafil tablets at least once weekly, and the following adverse reactions were reported: Table 2. Adverse Reactions Reported by ≥2% of Patients Treated with Sildenafil Tablets and More Frequent than Placebo in Flexible-Dose Phase II/III Studies Adverse Reaction SILDENAFIL TABLETS PLACEBO N=734 N=725 Headache 16% 4% Flushing 10% 1% Dyspepsia 7% 2% Nasal Congestion 4% 2% Abnormal Vision † 3% 0% Back pain 2% 2% Dizziness 2% 1% Rash 2% 1% † Abnormal Vision: Mild and transient, predominantly color tinge to vision, but also increased sensitivity to light or blurred vision.

In these studies, only one patient discontinued due to abnormal vision. The following events occurred in <2% of patients in controlled clinical trials; a causal relationship to sildenafil tablets is uncertain. Reported events include those with a plausible relation to drug use; omitted are min… [Excerpted — this section continues on DailyMed.]

🔄 Drug Interactions ~2 min read ▾

7 DRUG INTERACTIONS •Sildenafil tablets can potentiate the hypotensive effects of nitrates, alpha blockers, and anti-hypertensives ( 4.1 , 5.5 , 7.1 , 7.2 , 7.3 , 12.2 ) •With concomitant use of alpha blockers, initiate sildenafil tablets at 25 mg dose (2.3) •CYP3A4 inhibitors (e.g., ritonavir, ketoconazole, itraconazole, erythromycin): Increase sildenafil tablets exposure (2.4 , 7.4, 12.3 ) •Ritonavir: Do not exceed a maximum single dose of 25 mg in a 48 hour period ( 2.4 , 5.6) •Erythromycin or strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, saquinavir): Consider a starting dose of 25 mg (2.4, 7.4)

7.1Nitrates Administration of sildenafil tablets with nitric oxide donors such as organic nitrates or organic nitrites in any form is contraindicated. Consistent with its known effects on the nitric oxide/cGMP pathway, sildenafil tablets were shown to potentiate the hypotensive effects of nitrates [see Dosage and Administration (2.3), Contraindications (4.1), Clinical Pharmacology (12.2)].

7.2Alpha-blockers Use caution when co-administering alpha-blockers with sildenafil tablets because of potential additive blood pressure-lowering effects. When sildenafil tablets are co-administered with an alpha-blocker, patients should be stable on alpha-blocker therapy prior to initiating sildenafil tablets treatment and sildenafil tablets should be initiated at the lowest dose [see Dosage and Administration (2.3), Warnings and Precautions (5.5), Clinical Pharmacology (12.2)].

7.3Amlodipine When sildenafil tablets 100 mg were 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 [see Warnings and Precautions (5.5), Clinical Pharmacology (12.2)].

7.4Ritonavir and other CYP3A4 inhibitors 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 tablets in a 48 hour period [see Dosage and Administration ( 2.4), Warnings and Precautions (5.6), Clinical Pharmacology ( 12.3)]. Co-administration of erythromycin, a moderate CYP3A4 inhibitor, resulted in a 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 tablets should be considered in patients taking erythromycin or strong CYP3A4 inhibitors (such as saquinavir, ketoconazole, itracanozole) [see Dosage and Administration (2.4), Clinical Pharmacology ( 12.3)].

7.5Alcohol In a drug-drug interaction study 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) ].

👥 Use in Specific Populations ~3 min read ▾

8 USE IN SPECIFIC POPULATIONS •Geriatric use: Consider a starting dose of 25 mg (2.5 , 8.5) •Severe renal impairment: Consider a starting dose of 25 mg ( 2.5, 8.6) •Hepatic impairment: Consider a starting dose of 25 mg(2.5, 8.7)

8.1Pregnancy Risk Summary Sildenafil tablets is not indicated for use in females. There are no data with the use of sildenafil tablets 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).

Data Animal Data No evidence of teratogenicity, embryotoxicity or fetotoxicity was observed in rats and rabbits which received 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. 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.

8.2Lactation Risk Summary Sildenafil tablets is not indicated for use in females. 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.

8.4Pediatric Use Sildenafil tablets are not indicated for use in pediatric patients. Safety and effectiveness have not been established in pediatric patients.

8.5Geriatric Use 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 to 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 tablets, 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 (< 65 years of age) subjects. However, since higher plasma levels may increase the incidence of adverse reactions, a starting dose of 25 mg should be considered in older subjects due to the higher systemic exposure [see Dosage and Administration (2.5)].

8.6Renal Impairment No dose adjustment is required for mild (CLcr=50 to 80 mL/min) and moderate (CLcr=30 to 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 (2.5) and Clinical Pharmacology (12.3)].

8.7Hepatic Impairment In volunteers with hepatic impairment (Child-Pugh Class A and B), sildenafil clearance was reduced, resulting in higher plasma exposure of sildenafil (47% for Cmax and 85% for AUC). 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 (2.5) and Clinical Pharmacology (12.3)].

🤰 Pregnancy 159 words ▾

8.1Pregnancy Risk Summary Sildenafil tablets is not indicated for use in females. There are no data with the use of sildenafil tablets 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).

Data Animal Data No evidence of teratogenicity, embryotoxicity or fetotoxicity was observed in rats and rabbits which received 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. 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.

🧒 Pediatric Use 23 words ▾

8.4Pediatric Use Sildenafil tablets are not indicated for use in pediatric patients. Safety and effectiveness have not been established in pediatric patients.

🧓 Geriatric Use 165 words ▾

8.5Geriatric Use 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 to 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 tablets, 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 (< 65 years of age) subjects. However, since higher plasma levels may increase the incidence of adverse reactions, a starting dose of 25 mg should be considered in older subjects due to the higher systemic exposure [see Dosage and Administration (2.5)].

🆘 Overdosage 67 words ▾

10 OVERDOSAGE In studies with healthy volunteers of single 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.

🧬 Clinical Pharmacology ~3 min read ▾

12 CLINICAL PHARMACOLOGY

12.1Mechanism of Action 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 enhances the effect of NO by inhibiting phosphodiesterase type 5 (PDE5), which is responsible for degradation of cGMP in the corpus cavernosum.

Sildenafil has no direct relaxant effect on isolated human 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.

Binding Characteristics 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). 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. 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 .

12.2Pharmacodynamics Effects of Sildenafil 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. Most studies assessed the efficacy of sildenafil tablets approximately 60 minutes post dose. The erectile response, as assessed by RigiScan®, generally increased with increasing sildenafil dose and plasma concentration.

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 of Sildenafil Tablets on 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). The decrease in sitting blood pressure was most notable approximately 1 to 2 hours after dosing, and was not different than placebo at 8 hours.

Similar effects on blood pressure were noted with 25 mg, 50 mg and 100 mg of sildenafil tablets, therefore the effects are not related to dose or plasma levels within this dosage range. Larger effects were recorded among patients receiving concomitant nitrates [see Contraindications (4.1)]. Figure 1: Mean Change from Baseline in Sitting Systolic Blood Pressure, Healthy Volunteers.

Effects of Sildenafil 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 (co… [Excerpted — this section continues on DailyMed.]

🧬 Mechanism of Action ~1 min read ▾

12.1Mechanism of Action 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 enhances the effect of NO by inhibiting phosphodiesterase type 5 (PDE5), which is responsible for degradation of cGMP in the corpus cavernosum.

Sildenafil has no direct relaxant effect on isolated human 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.

Binding Characteristics 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). 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. 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 .

📦 How Supplied / Storage and Handling 55 words ▾

16 HOW SUPPLIED/STORAGE AND HANDLING Sildenafil Tablets USP, 100 mg are white colored, round-shaped, biconvex, film coated tablets debossed with I on one side and 58 on the other side. They are available as follows: NDC 68071-4617-3 BOTTLES OF 30 Recommended Storage: Store at 20° to 25°C (68° to 77°F) [see USP Controlled Room Temperature].

📋 Description 126 words ▾

11 DESCRIPTION Sildenafil Tablet, USP an oral therapy for erectile dysfunction, is the citrate salt of sildenafil, a selective inhibitor of cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5). Sildenafil citrate, USP 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, USP is a white to off-white crystalline powder with a solubility of 3.5 mg/mL in water and a molecular weight of 666.7.

Sildenafil tablet, USP is formulated as white, film-coated rounde-shaped tablets equivalent to 25 mg, 50 mg and 100 mg of sildenafil for oral administration. In addition to the active ingredient, sildenafil citrate, USP each tablet contains the following inactive ingredients: croscarmellose sodium, dibasic calcium phosphate anhydrous, hypromellose, lactose monohydrate, magnesium stearate, microcrystalline cellulose, titanium dioxide and triacetin. sildenafilstructure

💬 Information for Patients ~3 min read ▾

17 PATIENT COUNSELING INFORMATION Advise the patient to read the FDA-approved patient labeling (Patient Information) Nitrates Physicians should discuss with patients the contraindication of sildenafil tablets with regular and/or intermittent use of nitric oxide donors, such as organic nitrates or organic nitrites in any form [see Contraindications (4.1)]. Guanylate Cyclase (GC) Stimulators Physicians should discuss with patients the contraindication of sildenafil tablets with use of guanylate cyclase stimulators such as riociguat [see Contraindications (4.3)].

Concomitant Use with Drugs Which Lower Blood Pressure Physicians should advise patients of the potential for sildenafil tablets to augment the blood pressure lowering effect of alpha-blockers and anti-hypertensive medications. Concomitant administration of sildenafil tablets and an alpha-blocker may lead to symptomatic hypotension in some patients. Therefore, when sildenafil tablets are co-administered with alpha-blockers, patients should be stable on alpha-blocker therapy prior to initiating sildenafil tablets treatment and sildenafil tablets should be initiated at the lowest dose [see Warnings and Precautions (5.5)].

Cardiovascular Considerations Physicians should discuss with patients the potential cardiac risk of sexual activity in patients with preexisting cardiovascular risk factors. Patients who experience symptoms (e.g., angina pectoris, dizziness, nausea) upon initiation of sexual activity should be advised to refrain from further activity and should discuss the episode with their physician [see Warnings and Precautions (5.1)]. Sudden Loss of Vision Physicians should advise patients to stop use of all PDE5 inhibitors, including sildenafil tablets, and seek medical attention in the event of a sudden loss of vision in one or both eyes.

Such an event may be a sign of non-arteritic anterior ischemic optic neuropathy (NAION), a cause of decreased vision including possible permanent loss of vision, that has been reported rarely post-marketing in temporal association with the use of all PDE5 inhibitors. Physicians should also discuss with patients the increased risk of NAION among the general population in patients with a “crowded” optic disc, although evidence is insufficient to support screening of prospective users of PDE5 inhibitor, including sildenafil tablets, for this uncommon condition [see Warnings and Precautions (5.3) and Adverse Reactions (6.2)].

Sudden Hearing Loss Physicians should advise patients to stop taking PDE5 inhibitors, including sildenafil tablets, and seek prompt medical attention in the event of sudden decrease or loss of hearing. These events, which may be accompanied by tinnitus and dizziness, have been reported in temporal association to the intake of PDE5 inhibitors, including sildenafil tablets. It is not possible to determine whether these events are related directly to the use of PDE5 inhibitors or to other factors [see Warnings and Precautions (5.4) and Adverse Reactions (6.2)].

Priapism Physicians should warn patients that prolonged erections greater than 4 hours and priapism (painful erections greater than 6 hours in duration) have been reported infrequently since market approval of sildenafil tablets. In the event of an erection that persists longer than 4 hours, the patient should seek immediate medical assistance. If priapism is not treated immediately, penile tissue damage and permanent loss of potency may result [see Warnings and Precautions (5.2)].

Avoid Use with other PDE5 Inhibitors Physicians should inform patients not to take sildenafil tablets with other PDE5 inhibitors including REVATIO or other pulmonary arterial hypertension (PAH) treatments containing sildenafil. Sildenafil is also marketed as REVATIO for the treatment of PAH. The safety and efficacy of sildenafil tablets with other PDE5 inhibitors, including REVATIO, have not been studied [see Warnings and Precautions (5.7)].

Sexually Transmitted Disease The use of si… [Excerpted — this section continues on DailyMed.]

🧬 Pharmacokinetics ~3 min read ▾

12.3Pharmacokinetics Sildenafil tablets are rapidly absorbed after oral administration, with a mean absolute bioavailability of 41% (range 25 to 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: Figure 5: Mean Sildenafil Plasma Concentrations in Healthy Male Volunteers. Absorption and Distribution : Sildenafil tablets are 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 tablets are taken with a high fat meal, the rate of absorption is reduced, with a mean delay in Tmax of 60 minutes and a mean reduction in Cmax of 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 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. This metabolite has a PDE selectivity profile similar to sildenafil and an in vitro potency 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 Populations Geriatrics: 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 to 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 to 80 mL/min) and moderate (CLcr=30 to 49 mL/min) renal impairment, the pharmacokinetics of a single oral dose of sildenafil tablets (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 Cmax compared 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 Cmax values 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 Cmax (47%) compared t… [Excerpted — this section continues on DailyMed.]

🧬 Pharmacodynamics ~3 min read ▾

12.2Pharmacodynamics Effects of Sildenafil 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. Most studies assessed the efficacy of sildenafil tablets approximately 60 minutes post dose. The erectile response, as assessed by RigiScan®, generally increased with increasing sildenafil dose and plasma concentration.

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 of Sildenafil Tablets on 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). The decrease in sitting blood pressure was most notable approximately 1 to 2 hours after dosing, and was not different than placebo at 8 hours.

Similar effects on blood pressure were noted with 25 mg, 50 mg and 100 mg of sildenafil tablets, therefore the effects are not related to dose or plasma levels within this dosage range. Larger effects were recorded among patients receiving concomitant nitrates [see Contraindications (4.1)]. Figure 1: Mean Change from Baseline in Sitting Systolic Blood Pressure, Healthy Volunteers.

Effects of Sildenafil 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). In the following patients: age >65 years, hepatic impairment (e.g., cirrhosis), severe renal impairment (e.g., creatinine clearance <30 mL/min), and concomitant use of erythromycin or strong CYP3A4 inhibitors, plasma levels of sildenafil at 24 hours post dose have been found to be 3 to 8 times higher than those seen in healthy volunteers.

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 of Sildenafil 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. Study 1: Sildenafil tablets with Doxazosin In the first study, a single oral dose of sildenafil tablets 100 mg or matching placebo was administered in a 2-period crossover design to 4 generally healthy males with benign prostatic hyperplasia (BPH).

Following at least 14 consecutive daily doses of doxazosin, sildenafil tablets 100 mg or matching placebo was administered simultaneously with doxazosin. Following a review of the data from these first 4 subjects (details provided below), the sildenafil tablets dose was reduced to 25 mg. Thereafter, 17 subjects were treated with sildenafil tablets 25 mg or matching placebo in combination with doxazosin 4 mg (15 subjects) or doxazosin 8 mg (2 subjects).

The mean subject age was 66.5 years. For the 17 subjects who received sildenafil tablets 25 mg and matching placebo, the placebo-subtracted mean maximum decreases from baseline (95% CI) in systolic blood pressure were as follows: Placebo-subtracted mean maximum decrease in systolic blood pressure (mm Hg) Sildenafil tablets 25 mg Supine 7.4 (-0.9, 15.7) Standing 6 (-0.8,12.8) 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… [Excerpted — this section continues on DailyMed.]

🔬 Clinical Studies ~3 min read ▾

14 CLINICAL STUDIES In clinical studies, sildenafil tablets was assessed for its effect on the ability of men with erectile dysfunction (ED) to engage in sexual activity and in many cases specifically on the ability to achieve and maintain an erection sufficient for satisfactory sexual activity. Sildenafil tablets were evaluated primarily at doses of 25 mg, 50 mg and 100 mg in 21 randomized, double-blind, placebo-controlled trials of up to 6 months in duration, using a variety of study designs (fixed dose, titration, parallel, crossover).

Sildenafil tablets were administered to more than 3,000 patients aged 19 to 87 years, with ED of various etiologies (organic, psychogenic, mixed) with a mean duration of 5 years. Sildenafil tablets demonstrated statistically significant improvement compared to placebo in all 21 studies. The studies that established benefit demonstrated improvements in success rates for sexual intercourse compared with placebo.

Efficacy Endpoints in Controlled Clinical Studies The effectiveness of sildenafil tablets were evaluated in most studies using several assessment instruments. The primary measure in the principal studies was a sexual function questionnaire (the International Index of Erectile Function -IIEF) administered during a 4-week treatment-free run-in period, at baseline, at follow-up visits, and at the end of double-blind, placebo-controlled, at-home treatment. Two of the questions from the IIEF served as primary study endpoints; categorical responses were elicited to questions about (1) the ability to achieve erections sufficient for sexual intercourse and (2) the maintenance of erections after penetration.

The patient addressed both questions at the final visit for the last 4 weeks of the study. The possible categorical responses to these questions were (0) no attempted intercourse, (1) never or almost never, (2) a few times, (3) sometimes, (4) most times, and (5) almost always or always. Also collected as part of the IIEF was information about other aspects of sexual function, including information on erectile function, orgasm, desire, satisfaction with intercourse, and overall sexual satisfaction.

Sexual function data were also recorded by patients in a daily diary. In addition, patients were asked a global efficacy question and an optional partner questionnaire was administered. Efficacy Results from Controlled Clinical Studies The effect on one of the major end points, maintenance of erections after penetration, is shown in Figure 6, for the pooled results of 5 fixed-dose, dose-response studies of greater than one month duration, showing response according to baseline function.

Results with all doses have been pooled, but scores showed greater improvement at the 50 and 100 mg doses than at 25 mg. The pattern of responses was similar for the other principal question, the ability to achieve an erection sufficient for intercourse. The titration studies, in which most patients received 100 mg, showed similar results.

Figure 6 shows that regardless of the baseline levels of function, subsequent function in patients treated with sildenafil tablets were better than that seen in patients treated with placebo. At the same time, on-treatment function was better in treated patients who were less impaired at baseline. Effect of Sildenafil Tablets on Maintenance of Erection by Baseline Score Effect of Placebo on Maintenance of Erection by Baseline Score Figure 6.

Effect of Sildenafil Tablets and Placebo on Maintenance of Erection by Baseline Score. The frequency of patients reporting improvement of erections in response to a global question in four of the randomized, double-blind, parallel, placebo-controlled fixed dose studies (1797 patients) of 12 to 24 weeks duration is shown in Figure 7. These patients had erectile dysfunction at baseline that was characterized by median categorical scores of 2 (a few times) on principal IIEF questions.

Erectile dysfunction was attributed to organic (58%; generally… [Excerpted — this section continues on DailyMed.]

🧪 Nonclinical Toxicology 177 words ▾

13 NONCLINICAL TOXICOLOGY

13.1Carcinogenesis & Mutagenesis & Impairment Of Fertility Carcinogenesis Sildenafil was not carcinogenic when administered to rats for 24 months at a dose resulting in total systemic drug exposure (AUCs) for unbound sildenafil and its major metabolite of 20-and 38-times, for male and female rats, respectively, the exposures observed in human males given the Maximum Recommended Human Dose (MRHD) of 100 mg. Sildenafil was not carcinogenic when administered to mice for 18 to 21 months at dosages up to the Maximum Tolerated Dose (MTD) of 10 mg/kg/day, approximately 0.4 times the MRHD on a mg/m2 basis in a 50 kg subject.

Mutagenesis Sildenafil was negative in in vitro bacterial and Chinese hamster ovary cell assays to detect mutagenicity, and in vitro human lymphocytes and in vivo mouse micronucleus assays to detect clastogenicity. Impairment of Fertility There was no impairment of fertility in rats given sildenafil up to 60 mg/kg/day for 36 days to females and 102 days to males, a dose producing an AUC value of more than 25 times the human male AUC.

📄 Carcinogenesis, Mutagenesis, Impairment of Fertility 174 words ▾

13.1Carcinogenesis & Mutagenesis & Impairment Of Fertility Carcinogenesis Sildenafil was not carcinogenic when administered to rats for 24 months at a dose resulting in total systemic drug exposure (AUCs) for unbound sildenafil and its major metabolite of 20-and 38-times, for male and female rats, respectively, the exposures observed in human males given the Maximum Recommended Human Dose (MRHD) of 100 mg. Sildenafil was not carcinogenic when administered to mice for 18 to 21 months at dosages up to the Maximum Tolerated Dose (MTD) of 10 mg/kg/day, approximately 0.4 times the MRHD on a mg/m2 basis in a 50 kg subject.

Mutagenesis Sildenafil was negative in in vitro bacterial and Chinese hamster ovary cell assays to detect mutagenicity, and in vitro human lymphocytes and in vivo mouse micronucleus assays to detect clastogenicity. Impairment of Fertility There was no impairment of fertility in rats given sildenafil up to 60 mg/kg/day for 36 days to females and 102 days to males, a dose producing an AUC value of more than 25 times the human male AUC.

📄 Recent Major Changes 9 words ▾

Warnings and Precautions, Effects on the Eye (5.3) 08/2017

📄 Package Label / Principal Display Panel 5 words ▾

PACKAGE LABEL.PRINCIPAL DISPLAY PANEL pdp

Source: FDA Structured Product Labeling, mirrored from DailyMed / openFDA. Prefer the government’s original formatting? View this label on DailyMed ↗

About this NDC listing & data coverage

Finished prescription product
What data is (and isn’t) available for this NDC — tap to expand
NDC identity (package / product / labeler codes) ✓ Available
Labeler ✓ Available
Product & package description ✓ Available
Marketing category & status ✓ Available
Active ingredient / dosage form / route ✓ Available
FDA label (SPL via DailyMed) ✓ Available
Package photos — Not published for this NDC No photo available yet for this listing.
Inactive ingredients (structured) — Not published for this NDC The labeler did not submit a structured excipient list, or no SPL is available.
NADAC pharmacy acquisition price (CMS) — Not published for this NDC CMS publishes NADAC only for NDCs reported in its retail-pharmacy survey.
Orange Book / therapeutic-equivalence data ✓ Available
HCPCS J-code billing crosswalk — Not published for this NDC Most self-administered / retail products have no J-code — that is normal.
Medicaid utilization (CMS SDUD) — Not published for this NDC CMS reports utilization only for NDCs with Medicaid claims above its privacy threshold.
“Not published” reflects what the public FDA / CMS / NLM sources provide for this exact package code — it is a property of the data feeds, not a judgment about the product.

Questions about this listing

Why is there no price listed?
The pricing shown on our NDC pages comes from CMS NADAC, a voluntary survey of retail community pharmacy invoices. CMS does not publish a NADAC for every NDC — packages outside the retail survey (institutional and hospital products, bulk packages, discontinued items, and many OTC items) may never receive one. A missing price reflects the survey's scope, not this product's actual cost, and does not mean the product is free or unavailable.
Is the NDC printed on the package the same as the 11-digit billing NDC?
Yes, they identify this exact package in different formats. The form printed on the packaging and shown on DailyMed is the one the FDA registered. Insurance claims use a fixed 11-digit 5-4-2 format, so the short segment is padded with a leading zero and the dashes are dropped. The Identity section at the top of this page lists each form of this code.
Is this package still being marketed?
Yes, per the latest FDA NDC Directory data on this page: this package is listed as actively marketed, with no marketing end date reported by NuCare Pharmaceuticals,Inc.. Listing status can change — the directory data on this page refreshes weekly.
Who lists this product with the FDA?
NuCare Pharmaceuticals,Inc. is the labeler of record for this NDC — the company under whose FDA-assigned code the package is listed. The labeler may be the manufacturer itself or a distributor marketing the product under its own code.
Do I need a prescription for this product?
This NDC is listed with FDA as a prescription product, so it is dispensed under a prescriber's order. Your pharmacist can tell you whether any over-the-counter forms of the same medication exist.
This page identifies an FDA-listed package (the NDC) and reports public regulatory and pricing data about the listing. It is reference information, not a medical recommendation — talk to your pharmacist or prescriber about your own medication.
Where does this data come from?
Listing facts (marketing category, packager status, marketing dates) from the FDA openFDA NDC Directory; label availability from DailyMed; pricing coverage from CMS NADAC; equivalence scope from the FDA Orange Book.
← 68071-4606-03 · NuCare 68071-4618-03 · NuCare →
For educational and professional reference only — not medical advice. Pricing reflects published NADAC and CMS ASP (free public data) and may differ from your acquisition cost; always verify before billing or dispensing.