SILDENAFIL CITRATE- sildenafil tablet, film coated

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

SILDENAFIL CITRATE (UNII: BW9B0ZE037) (SILDENAFIL - UNII:3M7OB98Y7H)

Available from:

NuCare Pharmaceuticals,Inc.

Administration route:

ORAL

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

Sildenafil citrate is indicated for the treatment of erectile dysfunction. Consistent with its known effects on the nitric oxide/cGMP pathway [ see Clinical Pharmacology ( 12.1, 12.2) ], sildenafil citrate was 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) ]. Sildenafil citrate is 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) ] . Do not use sildenafil tablets in patients who are using a GC stimulator, such as riociguat. PDE5 inhibitors, including sildenafil citrate, may potentiate the hypotensive effects of GC stimulators. Risk Summary Sildenafil tablets are not indicated for use in females. There are no data with the use of sildenafil citrate 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/m 2 basis ( see Data ). Data Animal 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/m 2 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/m 2 basis in a 50 kg subject. Risk Summary Sildenafil tablets are 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. Sildenafil tablets are not indicated for use in pediatric patients. Safety and effectiveness have not been established in pediatric patients.   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 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) ].  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 C max 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) ] . In volunteers with hepatic impairment (Child-Pugh Class A and B), sildenafil clearance was reduced, resulting in higher plasma exposure of sildenafil (47% for C max 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) ] .

Product summary:

Sildenafil tablets, USP are supplied as green, oval-shaped, beveled edge, biconvex, film-coated tablets containing sildenafil citrate equivalent to the nominally indicated amount of sildenafil and debossed on the obverse and reverse sides as follows: Obverse 100 Reverse SC NDC 68071-3549-5 BOTTLES OF 15 Obverse 100 Reverse SC NDC 68071-3549-6 BOTTLES OF 60 Recommended Storage: Store at 25°C (77°F); excursions permitted to 15° to 30°C (59° to 86°F). [See USP Controlled Room Temperature.]

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

SILDENAFIL CITRATE- SILDENAFIL TABLET, FILM COATED
NUCARE PHARMACEUTICALS,INC.
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HIGHLIGHTS OF PRESCRIBING INFORMATION
THESE HIGHLIGHTS DO NOT INCLUDE ALL THE INFORMATION NEEDED TO USE
SILDENAFIL TABLETS
SAFELY AND EFFECTIVELY. SEE FULL PRESCRIBING INFORMATION FOR
SILDENAFIL TABLETS.
SILDENAFIL TABLETS, FOR ORAL USE
INITIAL U.S. APPROVAL: 1998
INDICATIONS AND USAGE
Sildenafil citrate is a phosphodiesterase-5 (PDE5) inhibitor indicated
for the treatment of erectile
dysfunction (ED) ( 1)
DOSAGE AND 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)
DOSAGE FORMS AND STRENGTHS
Tablets: 25 mg, 50 mg, 100 mg ( 3)
CONTRAINDICATIONS
Administration of sildenafil tablets to patients using nitric oxide
donors, such as organic nitrates or
organic nitrites in any form. Sildenafil citrate was 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)
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