Tadalafil


Description

Tadalafil is an orally administered drug used to treat male erectile dysfunction (impotence). It is marketed worldwide under the brand name Cialis. It is a phosphodiesterase 5 (PDE5) inhibitor. Tadalafil's distinguishing pharmacologic feature is its...

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Pharmacology

Indication

Used for the treatment of erectile dysfunction.

Pharmacodynamic

Tadalafil is used to treat male erectile dysfunction (impotence) and pulmonary arterial hypertension... Read more

Mechanism of action

Penile erection during sexual stimulation is achieved by the relaxation of penile arteries and corpu... Read more

Absorption

After single oral-dose administration, the maximum observed plasma concentration (Cmax) of tadalafil... Read more

Protein binding

94%

Volume of distribution

63 L

Clearance

oral cl=2.5 L/hr

Half life

17.5 hours

Route of elimination

Tadalafil is excreted predominantly as metabolites, mainly in the feces (approximately 61% of the do... Read more

Toxicity

Oral, Rat LD50 = 2000 mg/kg, no deaths or toxicity.


Adverse Effects

Effect Regions Age Groups Incidences Evidence Type
Headache US
  • adult
  • Kind: experimental
    • Percent: 11-15%
  • Kind: placebo
    • Percent: 5%
  • Clinical Trial
    Dyspepsia US
    • adult
  • Kind: experimental
    • Percent: 4-10%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Back Pain US
    • adult
  • Kind: experimental
    • Percent: 3-6%
  • Kind: placebo
    • Percent: 3%
  • Clinical Trial
    Headache US
    • adult
  • Kind: experimental
    • Percent: 3-6%
  • Kind: placebo
    • Percent: 5%
  • Clinical Trial
    Nasopharyngitis US
    • adult
  • Kind: experimental
    • Percent: 3-6%
  • Kind: placebo
    • Percent: 4-5%
  • Clinical Trial
    Dyspepsia US
    • adult
  • Kind: experimental
    • Percent: 1-5%
  • Kind: placebo
    • Percent: 1-2%
  • Clinical Trial
    Back Pain US
    • adult
  • Kind: experimental
    • Percent: 2-5%
  • Kind: placebo
    • Percent: 1-3%
  • Clinical Trial
    Influenza US
    • adult
  • Kind: experimental
    • Percent: 2-5%
  • Kind: placebo
    • Percent: 2-3%
  • Clinical Trial
    Gastrointestinal viral US
    • adult
  • Kind: experimental
    • Percent: 3-5%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Myalgia US
    • adult
  • Kind: experimental
    • Percent: 1-4%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Upper Respiratory Tract Infection US
    • adult
  • Kind: experimental
    • Percent: 3-4%
  • Kind: placebo
    • Percent: ≤1%
  • Clinical Trial
    Cough US
    • adult
  • Kind: experimental
    • Percent: 2-4%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Myalgia US
    • adult
  • Kind: experimental
    • Percent: 1-4%
  • Kind: placebo
    • Percent: 1-2%
  • Clinical Trial
    Nasal Congestion US
    • adult
  • Kind: experimental
    • Percent: 0-4%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Nasal Congestion US
    • adult
  • Kind: experimental
    • Percent: 2-3%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Flushing US
    • adult
  • Kind: experimental
    • Percent: 2-3%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Pain in limb US
    • adult
  • Kind: experimental
    • Percent: 1-3%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Flushing US
    • adult
  • Kind: experimental
    • Percent: 1-3%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Gastrointestinal Reflux US
    • adult
  • Kind: experimental
    • Percent: 1-3%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Hypertension US
    • adult
  • Kind: experimental
    • Percent: 1-3%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Arthralgia US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Neck Pain US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Vomiting US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Arthralgia US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Dizziness US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Hypesthesia US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Neck Pain US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Dizziness US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Loose stools US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Nausea US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    GGTP increased US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Loose stools US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Upper Abdominal Pain US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Vomiting US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Nausea US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Upper Abdominal Pain US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Esophagitis US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Dysphagia US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Dysphagia US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Dry Mouth US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    GGTP increased US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Gastritis US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Gastritis US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Esophagitis US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Tachycardia US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Syncope US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Syncope US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Palpitations US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Dry Mouth US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Abnormal Liver Function Tests US
    • adult
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial

    Contraindications

    • Regions: US
    • With Categories Coadmin:
        • Name: Organic Nitrates
        • Drugbank Id: DBCAT002456

    Food Interactions

      Information currently not available.

    Interactions

    Type in a drug name to check for interaction with Tadalafil

    The metabolism of Tadalafil can be decreased when combined with (R)-warfarin.
    The metabolism of Tadalafil can be decreased when combined with (S)-Warfarin.
    1-(3-Mercapto-2-Methyl-Propionyl)-Pyrrolidine-2-Carboxylic Acid may decrease the antihypertensive activities of Tadalafil.
    1-benzylimidazole may decrease the antihypertensive activities of Tadalafil.
    2,5-Dimethoxy-4-ethylamphetamine may decrease the antihypertensive activities of Tadalafil.
    2,5-Dimethoxy-4-ethylthioamphetamine may decrease the antihypertensive activities of Tadalafil.
    The metabolism of Tadalafil can be decreased when combined with 3,5-diiodothyropropionic acid.
    4-Bromo-2,5-dimethoxyamphetamine may decrease the antihypertensive activities of Tadalafil.
    The metabolism of 4-hydroxycoumarin can be decreased when combined with Tadalafil.
    4-Methoxyamphetamine may decrease the antihypertensive activities of Tadalafil.
    The metabolism of Tadalafil can be decreased when combined with 5-androstenedione.
    5-methoxy-N,N-dimethyltryptamine may decrease the antihypertensive activities of Tadalafil.
    The metabolism of Tadalafil can be decreased when combined with 6-Deoxyerythronolide B.
    The metabolism of Tadalafil can be decreased when combined with 6-O-benzylguanine.
    The metabolism of Tadalafil can be decreased when combined with 7-ethyl-10-hydroxycamptothecin.
    7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline may increase the hypotensive activities of Tadalafil.
    The metabolism of Tadalafil can be decreased when combined with 9-aminocamptothecin.
    Tadalafil may decrease the excretion rate of Abacavir which could result in a higher serum level.
    The metabolism of Tadalafil can be increased when combined with Abatacept.
    Abediterol may decrease the antihypertensive activities of Tadalafil.

    References

    • 1 . Naeije R, Huez S: Expert opinion on available options treating pulmonary arterial hypertension. Expert Opin Pharmacother. 2007 Oct;8(14):2247-65. [PubMed: 17927481]
    • 2 . Burnett AL: Molecular pharmacotherapeutic targeting of PDE5 for preservation of penile health. J Androl. 2008 Jan-Feb;29(1):3-14. Epub 2007 Oct 17. [PubMed: 17942972]
    • 3 . Guazzi M, Samaja M: The role of PDE5-inhibitors in cardiopulmonary disorders: from basic evidence to clinical development. Curr Med Chem. 2007;14(20):2181-91. [PubMed: 17691956]

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