Finasteride


Description

Finasteride is a synthetic 4-azasteroid compound[Label] and specific inhibitor of steroid Type II 5α-reductase, which is an intracellular enzyme that converts the androgen testosterone into 5α-dihydrotestosterone (DHT). It works in a similar fashion...

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Pharmacology

Indication

Indicated for the treatment of symptomatic benign prostatic hyperplasia (BPH) in men with an enlarge... Read more

Pharmacodynamic

Finasteride is an antiandrogenic compound that works by suppressing the production of serum and intr... Read more

Mechanism of action

Finasteride acts as a competitive and specific inhibitor of Type II 5α-reductase, a nuclear-bound st... Read more

Absorption

Finasteride is well absorbed following oral administration [ Read more

Protein binding

Approximately 90% of circulating finasteride is bound to plasma proteins.[Label]

Volume of distribution

The volume of distribution is 76 L at steady state, ranging from 44 to 96 L. Finasteride has been sh... Read more

Clearance

In healthy young subjects (n=15), the mean plasma clearance of finasteride was 165 mL/min with the r... Read more

Half life

In healthy young subjects receiving finasteride, the mean elimination half-life in plasma was 6 hour... Read more

Route of elimination

In healthy subjects, about 32-46% of total oral dose of finasteride was excreted in the urine in the... Read more

Toxicity

**LD50**

Oral LD50 is about 418 mg/kg in rats[MSDS] and there have been cases of lethality in rat...
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Adverse Effects

Effect Regions Age Groups Incidences Evidence Type
Dizziness US
  • Kind: experimental
    • Percent: 7.4%
  • Kind: placebo
    • Percent: 8.1%
  • Kind: comparator
    • Percent: 17.7%
  • Kind: comparator
    • Percent: 23.2%
  • Unclassified
    Impotence US
  • Kind: experimental
    • Percent: 18.5%
  • Kind: placebo
    • Percent: 12.2%
  • Kind: comparator
    • Percent: 22.6%
  • Kind: comparator
    • Percent: 14.4%
  • Unclassified
    Postural Hypotension US
  • Kind: experimental
    • Percent: 9.1%
  • Kind: placebo
    • Percent: 8.0%
  • Kind: comparator
    • Percent: 17.8%
  • Kind: comparator
    • Percent: 16.7%
  • Unclassified
    Asthenia US
  • Kind: experimental
    • Percent: 5.3%
  • Kind: placebo
    • Percent: 7.1%
  • Kind: comparator
    • Percent: 15.7%
  • Kind: comparator
    • Percent: 16.8%
  • Unclassified
    Abnormal ejaculation US
  • Kind: experimental
    • Percent: 7.2%
  • Kind: placebo
    • Percent: 0.5%
  • Kind: comparator
    • Percent: 4.5%
  • Kind: comparator
    • Percent: 14.1%
  • Unclassified
    Libido decreased US
  • Kind: experimental
    • Percent: 10.0%
  • Kind: placebo
    • Percent: 5.7%
  • Kind: comparator
    • Percent: 7.0%
  • Kind: comparator
    • Percent: 11.6%
  • Unclassified
    Impotence US
  • Kind: experimental
    • Percent: 8.1%
  • Kind: placebo
    • Percent: 3.7%
  • Clinical Trial
    Decreased libido US
  • Kind: experimental
    • Percent: 6.4%
  • Kind: placebo
    • Percent: 3.4%
  • Clinical Trial
    Headache US
  • Kind: experimental
    • Percent: 2.0%
  • Kind: placebo
    • Percent: 0.7%
  • Kind: comparator
    • Percent: 2.3%
  • Kind: comparator
    • Percent: 4.1%
  • Unclassified
    Somnolence US
  • Kind: experimental
    • Percent: 1.7%
  • Kind: placebo
    • Percent: 1.5%
  • Kind: comparator
    • Percent: 3.7%
  • Kind: comparator
    • Percent: 3.1%
  • Unclassified
    Decreased volume of ejaculate US
  • Kind: experimental
    • Percent: 3.7%
  • Kind: placebo
    • Percent: 0.8%
  • Clinical Trial
    Hypotension US
  • Kind: experimental
    • Percent: 1.2%
  • Kind: placebo
    • Percent: 0.7%
  • Kind: comparator
    • Percent: 1.5%
  • Kind: comparator
    • Percent: 3.4%
  • Unclassified
    Peripheral Edema US
  • Kind: experimental
    • Percent: 1.3%
  • Kind: placebo
    • Percent: 0.9%
  • Kind: comparator
    • Percent: 2.6%
  • Kind: comparator
    • Percent: 3.3%
  • Unclassified
    Sexual function abnormal US
  • Kind: experimental
    • Percent: 2.5%
  • Kind: placebo
    • Percent: 0.9%
  • Kind: comparator
    • Percent: 3.1%
  • Kind: comparator
    • Percent: 2.0%
  • Unclassified
    Rhinitis US
  • Kind: experimental
    • Percent: 1.0%
  • Kind: placebo
    • Percent: 0.5%
  • Kind: comparator
    • Percent: 2.4%
  • Kind: comparator
    • Percent: 1.3%
  • Unclassified
    Gynecomastia US
  • Kind: experimental
    • Percent: 2.2%
  • Kind: placebo
    • Percent: 0.7%
  • Kind: comparator
    • Percent: 1.5%
  • Kind: comparator
    • Percent: 1.1%
  • Unclassified
    Dyspnea US
  • Kind: experimental
    • Percent: 0.7%
  • Kind: placebo
    • Percent: 0.7%
  • Kind: comparator
    • Percent: 2.1%
  • Kind: comparator
    • Percent: 1.9%
  • Unclassified
    Increased risk of high-grade prostate cancer US
  • Kind: experimental
    • Percent: 1.8
  • Kind: placebo
    • Percent: 1
  • Clinical Trial
    Rash US
  • Kind: experimental
    • Percent: 0.5 %
  • Kind: placebo
    • Percent: 0.8%
  • Clinical Trial
    Ejaculation disorder US
  • Kind: experimental
    • Percent: 0.8%
  • Kind: placebo
    • Percent: 0.1%
  • Clinical Trial
    Breast enlargement US
  • Kind: experimental
    • Percent: 0.5%
  • Kind: placebo
    • Percent: 0.1%
  • Clinical Trial
    Breast tenderness US
  • Kind: experimental
    • Percent: 0.4%
  • Kind: placebo
    • Percent: 0.1%
  • Clinical Trial
    Pruritis US
    Post Marketing
    Urticaria US
    Post Marketing
    Depression US
    Post Marketing
    Poor seminal quality US
    Post Marketing
    Male Breast Cancer US
    Post Marketing
    Ejaculation disorders US
    Post Marketing
    Decreased libido US
    Post Marketing
    Male inferfility US
    Post Marketing
    Reduced ejaculation volume US
    Post Marketing
    Testicular pain US
    Post Marketing
    Swelling of face US
    Post Marketing
    Erectile Dysfunction US
    Post Marketing
    Sexual Dysfunction US
    Post Marketing
    Swelling of lips US
    Post Marketing
    Angioedema US
    Post Marketing
    Swelling of throat US
    Post Marketing
    Swelling of tongue US
    Post Marketing
    Reduction in serum PSA levels US
    Clinical Trial
    Risk to male fetus US
    Clinical Trial
    Risk to male fetus US
    Clinical Trial
    Decreased ejaculate volume US
    Clinical Trial

    Contraindications

    • Regions: US
    • Patient Conditions:
        • Name: Pregnancy
        • Drugbank Id: DBCOND0018394

    Food Interactions

    • Take without regard to meals.

    Interactions

    Type in a drug name to check for interaction with Finasteride

    The metabolism of (R)-warfarin can be decreased when combined with Finasteride.
    The metabolism of (S)-Warfarin can be decreased when combined with Finasteride.
    The risk or severity of hypertension can be increased when Finasteride is combined with 1-(3-Mercapto-2-Methyl-Propionyl)-Pyrrolidine-2-Carboxylic Acid.
    The risk or severity of hypertension can be increased when Finasteride is combined with 1-benzylimidazole.
    The therapeutic efficacy of Finasteride can be decreased when used in combination with 2,5-Dimethoxy-4-ethylamphetamine.
    The therapeutic efficacy of Finasteride can be decreased when used in combination with 2,5-Dimethoxy-4-ethylthioamphetamine.
    The metabolism of 3,5-diiodothyropropionic acid can be decreased when combined with Finasteride.
    The therapeutic efficacy of Finasteride can be decreased when used in combination with 4-Bromo-2,5-dimethoxyamphetamine.
    The therapeutic efficacy of 4-Bromo-2,5-dimethoxyphenethylamine can be decreased when used in combination with Finasteride.
    The metabolism of 4-hydroxycoumarin can be decreased when combined with Finasteride.
    The risk or severity of hypertension can be increased when Finasteride is combined with 4-Methoxyamphetamine.
    The metabolism of 5-androstenedione can be decreased when combined with Finasteride.
    The risk or severity of hypertension can be increased when Finasteride is combined with 5-methoxy-N,N-dimethyltryptamine.
    The metabolism of Finasteride can be decreased when combined with 6-Deoxyerythronolide B.
    The metabolism of 6-O-benzylguanine can be decreased when combined with Finasteride.
    The metabolism of Finasteride can be decreased when combined with 7-ethyl-10-hydroxycamptothecin.
    The metabolism of 9-aminocamptothecin can be decreased when combined with Finasteride.
    The metabolism of Finasteride can be increased when combined with Abatacept.
    The risk or severity of hypertension can be increased when Finasteride is combined with Abediterol.
    The metabolism of Abemaciclib can be decreased when combined with Finasteride.

    References

    • 1 . Smith AB, Carson CC: Finasteride in the treatment of patients with benign prostatic hyperplasia: a review. Ther Clin Risk Manag. 2009 Jun;5(3):535-45. Epub 2009 Jul 12. [PubMed: 19707263]
    • 2 . Agamia NF, Abou Youssif T, El-Hadidy A, El-Abd A: Benign prostatic hyperplasia, metabolic syndrome and androgenic alopecia: Is there a possible relationship? Arab J Urol. 2016 Feb 23;14(2):157-62. doi: 10.1016/j.aju.2016.01.003. eCollection 2016 Jun. [PubMed: 27489744]
    • 3 . Vaughan ED: Long-Term Experience with 5-alpha-Reductase Inhibitors. Rev Urol. 2003;5 Suppl 4:S28-33. [PubMed: 16985960]
    • 4 . Bhargava S: Increased DHT levels in androgenic alopecia have been selected for to protect men from prostate cancer. Med Hypotheses. 2014 Apr;82(4):428-32. doi: 10.1016/j.mehy.2014.01.016. Epub 2014 Jan 26. [PubMed: 24548754]
    • 5 . Mysore V: Finasteride and sexual side effects. Indian Dermatol Online J. 2012 Jan;3(1):62-5. doi: 10.4103/2229-5178.93496. [PubMed: 23130269]
    • 6 . McClellan KJ, Markham A: Finasteride: a review of its use in male pattern hair loss. Drugs. 1999 Jan;57(1):111-26. doi: 10.2165/00003495-199957010-00014. [PubMed: 9951956]
    • 7 . Wilson JD: The pathogenesis of benign prostatic hyperplasia. Am J Med. 1980 May;68(5):745-56. [PubMed: 6155068]
    • 8 . Steiner JF: Clinical pharmacokinetics and pharmacodynamics of finasteride. Clin Pharmacokinet. 1996 Jan;30(1):16-27. doi: 10.2165/00003088-199630010-00002. [PubMed: 8846625]
    • 9 . Carson C 3rd, Rittmaster R: The role of dihydrotestosterone in benign prostatic hyperplasia. Urology. 2003 Apr;61(4 Suppl 1):2-7. [PubMed: 12657354]
    • 10 . 34. (2012). In Rang and Dale's Pharmacology (7th ed., pp. 424). Edinburgh: Elsevier/Churchill Livingstone.
    • 11 . PROPECIA® (finasteride) tablets for oral use - FDA Label [Link]
    • 12 . Finasteride - StatPearls - NCBI Bookshelf [Link]

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