Sildenafil


Description

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) [

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Pharmacology

Indication

Sildenafil is a phosphodiesterase-5 (PDE5) inhibitor that is predominantly employed for two primary... Read more

Pharmacodynamic

In vitro studies have shown that sildenafil is selective for phosphodiesterase-5 (PDE5) [ Read more

Mechanismofaction

Sildenafil is an oral therapy for erectile dysfunction [ Read more

Absorption

Sildenafil is known to be quickly absorbed, with maximum plasma concentrations being observed within... Read more

Proteinbinding

It is generally observed that sildenafil and its main circulating N-desmethyl metabolite are both es... Read more

Volumeofdistribution

The mean steady-state volume of distribution documented for sildenafil is approximately 105 L - a va... Read more

Clearance

The total body clearance documented for sildenafil is 41 L/h [ Read more

Halflife

The terminal phase half-life observed for sildenafil is approximately 3 to 5 hours [ Read more

Routeofelimination

After either oral or intravenous administration, sildenafil is excreted as metabolites predominantly... Read more

Toxicity

In single-dose volunteer studies of doses up to 800 mg, adverse reactions were similar to those seen... Read more


Adverse Effects

Effect Regions Age Groups Incidences Evidence Type
Headache US
  • adult
  • Kind: experimental
    • Percent: 16-46%
  • Kind: placebo
    • Percent: 4-39%
  • Clinical Trial
    Dyspepsia US
    • adult
  • Kind: experimental
    • Percent: 7-17%
  • Kind: placebo
    • Percent: 2-7%
  • Clinical Trial
    Increased sensitivity to light US
    • adult
  • Kind: experimental
    • Percent: 3-11%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Color tinge to vision US
    • adult
  • Kind: experimental
    • Percent: 3-11%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Blurred vision US
    • adult
  • Kind: experimental
    • Percent: 3-11%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Flushing US
    • adult
  • Kind: experimental
    • Percent: 10%
  • Kind: placebo
    • Percent: 1-4%
  • Clinical Trial
    Diarrhea US
    • adult
  • Kind: experimental
    • Percent: 3-9%
  • Kind: placebo
    • Percent: 1-6%
  • Clinical Trial
    Epistaxis US
    • adult
  • Kind: experimental
    • Percent: 9%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Myalgia US
    • adult
  • Kind: experimental
    • Percent: 7%
  • Kind: placebo
    • Percent: 4%
  • Clinical Trial
    Exacerbation of dyspnea US
    • adult
  • Kind: experimental
    • Percent: 7%
  • Kind: placebo
    • Percent: 3%
  • Clinical Trial
    Insomnia US
    • adult
  • Kind: experimental
    • Percent: 7%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Erythema US
    • adult
  • Kind: experimental
    • Percent: 6%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Pyrexia US
    • adult
  • Kind: experimental
    • Percent: 6%
  • Kind: placebo
    • Percent: 3%
  • Clinical Trial
    Rhinitis US
    • adult
  • Kind: experimental
    • Percent: 4%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Nasal Congestion US
    • adult
  • Kind: experimental
    • Percent: 4%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Urinary Tract Infection US
    • adult
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Paresthesia US
    • adult
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Sinusitis US
    • adult
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Gastritis US
    • adult
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Anorgasmia US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Urinary Incontinence US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Abnormal ejaculation US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Genital edema US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Sudden decrease or loss of hearing US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Contact Dermatitis US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Exfoliative dermatitis US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Conjunctivitis US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Photophobia US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Mydriasis US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Herpes Simplex US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Pruritis US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Urticaria US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Skin Ulcer US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Sweating US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Nocturia US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Cystitis US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Dry Eyes US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Breast enlargement US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Urinary Frequency US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Eye Pain US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Tinnitus US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Cataract US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Eye hemorrhage US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Ear pain US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Tremor US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Vertigo US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Depression US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Insomnia US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Somnolence US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Ataxia US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial

    Contraindications

    • Sex Group: all
    • Regions: US
    • Patient Conditions:
        • Name: Blood pressure < 90/50 mmHg at therapy initiation Severe hypotension
        • Drugbank Id: DBCOND0118168
        • Combination Of:
          • Additional Characteristics:
            • blood pressure < 90/50 mmHg at therapy initiation
          • Included Conditions:
              • Name: Severe hypotension
              • Drugbank Id: DBCOND0118169
    • Sex Group: all
    • Regions: US
    • Patient Conditions:
        • Name: Recent Myocardial Infarction
        • Drugbank Id: DBCOND0043731
        • Name: Recent Stroke
        • Drugbank Id: DBCOND0049526
    • Sex Group: all
    • Regions: US
    • Patient Conditions:
        • Name: Severe Hepatic Impairment
        • Drugbank Id: DBCOND0070791
        • Modification Of:
          • Base:
            • Name: Hepatic Impairment
            • Drugbank Id: DBCOND0031585
          • Severity:
            • Includes:
              • severe
    • Sex Group: male
    • Regions: US
    • Above Age:
      • Amount: 18
      • Unit: year
    • Patient Conditions:
        • Name: Men for whom sexual activity is inadvisable
        • Drugbank Id: DBCOND0107999
    • Sex Group: all
    • Regions: US
    • Patient Conditions:
        • Name: Non-Arteritic Anterior Ischemic Optic Neuropathy
        • Drugbank Id: DBCOND0031403
    • Sex Group: all
    • Regions: US
    • With Categories:
        • Name: Cytochrome P-450 CYP3A4 Inhibitors (strong)
        • Drugbank Id: DBCAT002647
    • Sex Group: all
    • Regions: US
    • With Categories:
        • Name: Guanylate Cyclase Stimulators
        • Drugbank Id: DBCAT004472
    • Sex Group: all
    • Regions: US
    • With Categories:
        • Name: Nitric Oxide Donors
        • Drugbank Id: DBCAT000756
        • Mesh Id: D020030

    Food Interactions

      Information currently not available.

    Interactions

    Type in a drug name to check for interaction with Sildenafil

    The risk or severity of hemorrhage can be increased when (R)-warfarin is combined with Sildenafil.
    The risk or severity of hemorrhage can be increased when (S)-Warfarin is combined with Sildenafil.
    The therapeutic efficacy of 2,4-thiazolidinedione can be increased when used in combination with Sildenafil.
    The metabolism of Sildenafil can be decreased when combined with 3,5-diiodothyropropionic acid.
    The risk or severity of hemorrhage can be increased when 4-hydroxycoumarin is combined with Sildenafil.
    The metabolism of 4-Methoxyamphetamine can be decreased when combined with Sildenafil.
    The metabolism of Sildenafil can be decreased when combined with 5-androstenedione.
    The metabolism of Sildenafil can be decreased when combined with 6-Deoxyerythronolide B.
    The metabolism of Sildenafil can be decreased when combined with 6-O-benzylguanine.
    The metabolism of Sildenafil can be decreased when combined with 7-ethyl-10-hydroxycamptothecin.
    The metabolism of Sildenafil can be decreased when combined with 9-aminocamptothecin.
    The serum concentration of Sildenafil can be increased when it is combined with Abafungin.
    The metabolism of Sildenafil can be increased when combined with Abatacept.
    The risk or severity of hemorrhage can be increased when Abciximab is combined with Sildenafil.
    The metabolism of Sildenafil can be decreased when combined with Abemaciclib.
    The metabolism of Sildenafil can be decreased when combined with Abiraterone.
    The metabolism of Sildenafil can be decreased when combined with Acalabrutinib.
    The therapeutic efficacy of Acarbose can be increased when used in combination with Sildenafil.
    Sildenafil may increase the antihypertensive activities of Acebutolol.
    The metabolism of Aceclofenac can be decreased when combined with Sildenafil.

    References

    • 1 . Boolell M, Allen MJ, Ballard SA, Gepi-Attee S, Muirhead GJ, Naylor AM, Osterloh IH, Gingell C: Sildenafil: an orally active type 5 cyclic GMP-specific phosphodiesterase inhibitor for the treatment of penile erectile dysfunction. Int J Impot Res. 1996 Jun;8(2):47-52. [PubMed: 8858389]
    • 2 . Cheitlin MD, Hutter AM Jr, Brindis RG, Ganz P, Kaul S, Russell RO Jr, Zusman RM: ACC/AHA expert consensus document. Use of sildenafil (Viagra) in patients with cardiovascular disease. American College of Cardiology/American Heart Association. J Am Coll Cardiol. 1999 Jan;33(1):273-82. [PubMed: 9935041]
    • 3 . Fries R, Shariat K, von Wilmowsky H, Bohm M: Sildenafil in the treatment of Raynaud's phenomenon resistant to vasodilatory therapy. Circulation. 2005 Nov 8;112(19):2980-5. [PubMed: 16275885]
    • 4 . Unegbu C, Noje C, Coulson JD, Segal JB, Romer L: Pulmonary Hypertension Therapy and a Systematic Review of Efficacy and Safety of PDE-5 Inhibitors. Pediatrics. 2017 Mar;139(3). pii: peds.2016-1450. doi: 10.1542/peds.2016-1450. [PubMed: 28235796]
    • 5 . Gong B, Ma M, Xie W, Yang X, Huang Y, Sun T, Luo Y, Huang J: Direct comparison of tadalafil with sildenafil for the treatment of erectile dysfunction: a systematic review and meta-analysis. Int Urol Nephrol. 2017 Oct;49(10):1731-1740. doi: 10.1007/s11255-017-1644-5. Epub 2017 Jul 24. [PubMed: 28741090]
    • 6 . Nichols DJ, Muirhead GJ, Harness JA: Pharmacokinetics of sildenafil after single oral doses in healthy male subjects: absolute bioavailability, food effects and dose proportionality. Br J Clin Pharmacol. 2002;53 Suppl 1:5S-12S. [PubMed: 11879254]
    • 7 . Goldstein I, Burnett AL, Rosen RC, Park PW, Stecher VJ: The Serendipitous Story of Sildenafil: An Unexpected Oral Therapy for Erectile Dysfunction. Sex Med Rev. 2019 Jan;7(1):115-128. doi: 10.1016/j.sxmr.2018.06.005. Epub 2018 Oct 6. [PubMed: 30301707]
    • 8 . Electronic Medicines Compendium: Sildenafil 25mg, 50mg, 100mg film-coated tablets Monograph [Link]
    • 9 . Electronic Medicines Compendium: Revatio (sildenafil citrate) 20 mg film-coated tablets Monograph [Link]
    • 10 . Forbes: With Viagra Now Available Over-The-Counter In The U.K., Will The U.S. Follow Suit? [Link]
    • 11 . Revatio (sildenafil) FDA Label [File]
    • 12 . Viagra (sildenafil citrate) FDA Label [File]
    • 13 . Viagra (sildenafil citrate) Tablets 25 mg, 50 mg, and 100 mg Canadian Product Monograph [File]
    • 14 . Revatio (sildenafil citrate) Canadian Product Monograph [File]
    • 15 . Revatio (sildenafil citrate) EMA Label [File]
    • 16 . Viagra (sildenafil citrate) EMA Label [File]

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