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Sildenafil

Generic Name
Sildenafil
Brand Names
Liqrev, Revatio, Viagra, Vizarsin, Sildenafil Actavis, Sildenafil ratiopharm, Granpidam, Sildenafil Teva, Mysildecard
Drug Type
Small Molecule
Chemical Formula
C22H30N6O4S
CAS Number
139755-83-2
Unique Ingredient Identifier
3M7OB98Y7H

Overview

In eliciting its mechanism of action, sildenafil ultimately prevents or minimizes the breakdown of cyclic guanosine monophosphate (cGMP) by inhibiting cGMP specific phosphodiesterase type 5 (PDE5) . The result of doing so allows cGMP present in both the penis and pulmonary vasculature to elicit smooth muscle relaxation and vasodilation that subsequently facilitates relief in pulmonary arterial hypertension and the increased flow of blood into the spongy erectile tissue of the penis that consequently allows it to grow in size and become erect and rigid . Interestingly enough, it is precisely via this mechanism why sildenafil was at first researched as a potential treatment for angina - or chest pain associated with inadequate blood flow to the heart - before being serendipitously indicated for treating erectile dysfunction in the late 1980s . Nevertheless, it is because of this mechanism that sildenafil is also indicated for treating pulmonary arterial hypertension but is also additionally notorious for interacting with various anti-anginal or anti-hypertensive agents to develop potentially rapid, excessive, and/or fatal hypotensive crises . Regardless, sildenafil, among a variety of other similar or related PDE5 inhibitors, has become a common and effective treatment for erectile dysfunction and since its formal approval for medical use in the public in 1998 , continues to see millions of prescriptions written for it internationally. Although the medication has historically been most popularly recognized as Pfizer's brand name Viagra, sildenafil is currently available generically and even as a non-prescription over the counter medication in some countries .

Background

In eliciting its mechanism of action, sildenafil ultimately prevents or minimizes the breakdown of cyclic guanosine monophosphate (cGMP) by inhibiting cGMP specific phosphodiesterase type 5 (PDE5) . The result of doing so allows cGMP present in both the penis and pulmonary vasculature to elicit smooth muscle relaxation and vasodilation that subsequently facilitates relief in pulmonary arterial hypertension and the increased flow of blood into the spongy erectile tissue of the penis that consequently allows it to grow in size and become erect and rigid . Interestingly enough, it is precisely via this mechanism why sildenafil was at first researched as a potential treatment for angina - or chest pain associated with inadequate blood flow to the heart - before being serendipitously indicated for treating erectile dysfunction in the late 1980s . Nevertheless, it is because of this mechanism that sildenafil is also indicated for treating pulmonary arterial hypertension but is also additionally notorious for interacting with various anti-anginal or anti-hypertensive agents to develop potentially rapid, excessive, and/or fatal hypotensive crises . Regardless, sildenafil, among a variety of other similar or related PDE5 inhibitors, has become a common and effective treatment for erectile dysfunction and since its formal approval for medical use in the public in 1998 , continues to see millions of prescriptions written for it internationally. Although the medication has historically been most popularly recognized as Pfizer's brand name Viagra, sildenafil is currently available generically and even as a non-prescription over the counter medication in some countries .

Indication

Sildenafil is a phosphodiesterase-5 (PDE5) inhibitor that is predominantly employed for two primary indications: (1) the treatment of erectile dysfunction ; and (2) treatment of pulmonary hypertension, where: a) the US FDA specifically indicates sildenafil for the treatment of pulmonary arterial hypertension (PAH) (WHO Group I) in adults to improve exercise ability and delay clinical worsening . The delay in clinical worsening was demonstrated when sildenafil was added to background epoprostenol therapy . Studies establishing effectiveness were short-term (12 to 16 weeks), and included predominately patients with New York Heart Association (NYHA) Functional Class II-III symptoms and idiopathic etiology (71%) or associated with connective tissue disease (CTD) (25%) ; b) the Canadian product monograph specifically indicates sildenafil for the treatment of primary pulmonary arterial hypertension (PPH) or pulmonary hypertension secondary to connective tissue disease (CTD) in adult patients with WHO functional class II or III who have not responded to conventional therapy . In addition, improvement in exercise ability and delay in clinical worsening was demonstrated in adult patients who were already stabilized on background epoprostenol therapy ; and c) the EMA product information specifically indicates sildenafil for the treatment of adult patients with pulmonary arterial hypertension classified as WHO functional class II and III, to improve exercise capacity . Efficacy has been shown in primary pulmonary hypertension and pulmonary hypertension associated with connective tissue disease . The EMA label also indicates sildenafil for the treatment of pediatric patients aged 1 year to 17 years old with pulmonary arterial hypertension . Efficacy in terms of improvement of exercise capacity or pulmonary hemodynamics has been shown in primary pulmonary hypertension and pulmonary hypertension associated with congenital heart disease .

Associated Conditions

  • Erectile Dysfunction
  • NYHA Functional Class II-III Pulmonary arterial hypertension
  • Premature Ejaculation
  • Pulmonary Arterial Hypertension (PAH)

Clinical Trials

Phase 2
Not yet recruiting
Posted: 2024/04/22
Not Applicable
Recruiting
Posted: 2024/02/01
Sponsor:
First People's Hospi...

FDA Approved Products

Viagra
Manufacturer:PFIZER LABORATORIES DIV PFIZER INC
Route:ORAL
Strength:25 mg in 1 1
Approved: 2017/12/15
NDC:0069-4200
SILDENAFIL CITRATE
Manufacturer:REMEDYREPACK INC.
Route:ORAL
Strength:50 mg in 1 1
Approved: 2024/02/22
NDC:70518-1641
Sildenafil
Manufacturer:REMEDYREPACK INC.
Route:ORAL
Strength:100 mg in 1 1
Approved: 2024/02/15
NDC:70518-1216
Sildenafil
Manufacturer:Macleods Pharmaceuticals Limited
Route:ORAL
Strength:25 mg in 1 1
Approved: 2023/05/02
NDC:33342-041
SILDENAFIL
Manufacturer:Lupin Pharmaceuticals, Inc.
Route:ORAL
Strength:10 mg in 1 mL
Approved: 2023/12/06
NDC:68180-283

Singapore Approved Products

VIAGRA TABLET 25 mg
Manufacturer:Fareva Amboise
Form:TABLET, FILM COATED
Strength:25 mg
Online:Yes
Approved: 1999/03/17
Approval:SIN10804P
Sildegra Tablet 100mg
Manufacturer:Salutas Pharma GmbH (Barleben site), Sandoz Private Limited (Kalwe site)
Form:TABLET
Strength:100 mg
Online:Yes
Approved: 2012/07/04
Approval:SIN14188P
SIFE 50 SILDENAFIL CITRATE FILM COATED TABLETS 50 MG
Manufacturer:Hetero Labs Limited
Form:TABLET, FILM COATED
Strength:50.0 mg
Online:Yes
Approved: 2019/05/02
Approval:SIN15676P
SEDEOGRA FILM-COATED TABLET 100MG
Manufacturer:The Government Pharmaceutical Organization
Form:TABLET, FILM COATED
Strength:100 mg
Online:Yes
Approved: 2021/12/23
Approval:SIN16406P
ANDROZ 50 TABLETS 50MG
Manufacturer:TORRENT PHARMACEUTICALS LIMITED
Form:TABLET, FILM COATED
Strength:50mg
Online:Yes
Approved: 2013/06/05
Approval:SIN14355P

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