Description

Simple

A medication used to treat prostate cancer and hair loss in men.

Clinical

An antiandrogenic compound that is used for the treatment of symptomatic benign prostatic hyperplasia (BPH) and male pattern hair loss in adult males by inhibiting Type II 5-alpha reductase.

Overview

Finasteride is a synthetic 4-azasteroid compound [13] 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 as [dutasteride], which is another 5-alpha-reductase inhibitor, by exerting antiandrogenic effects. Finasteride is an orally active drug that was first approved by the FDA in 1992 for the treatment of benign prostatic hyperplasia to improve symptoms and reduce the risk for acute urinary retention or the need for surgical procedures.[12,13] In 1998, it was approved by the FDA to treat male pattern hair loss.[12] Finasteride is commonly marketed under the brand names Propecia and Proscar to be used aloneo or in combination with [doxazosin], an alpha-blocker.

Both benign prostatic hyperplasia and androgenic alopecia are androgen-dependent disorders that are characterized by _in situ_ high levels of DHT.[Read more

Pharmacology

Indication

Indicated for the treatment of symptomatic benign prostatic hyperplasia (BPH) in men with an enlarged prostate to improve symptoms, reduce the risk of acute urinary retention, and reduce the risk of the need for surgery including transurethral resection of the prostate (TURP) and prostatectomy.[ Read more

Pharmacodynamic

Finasteride is an antiandrogenic compound that works by suppressing the production of serum and intraprostatic dihydrotestosterone (DHT) in men via inhibiting the enzyme responsible for the biosynthesis of DHT. The maximum effect of a rapid reduction in serum DHT concentration is expected to be obse... Read more

Mechanism of action

Finasteride acts as a competitive and specific inhibitor of Type II 5α-reductase, a nuclear-bound steroid intracellular enzyme primarily located in the prostatic stromal cell that converts the androgen testosterone into the more active metabolite, 5α-dihydrotestosterone (DHT).[ Read more

Absorption

Finasteride is well absorbed following oral administration [10] and displays a slow accumulation phase after multiple dosing.[lablel]... Read more

Protein binding

Approximately 90% of circulating finasteride is bound to plasma proteins.[13]

Volume of distribution

The volume of distribution is 76 L at steady state, ranging from 44 to 96 L. Finasteride has been shown to cross the blood brain barrier but does not appear to distribute preferentially to the CSF.[ Read more

Clearance

In healthy young subjects (n=15), the mean plasma clearance of finasteride was 165 mL/min with the range between 70 and 279 mL/min.[13]

Half life

In healthy young subjects receiving finasteride, the mean elimination half-life in plasma was 6 hours ranging from 3 to 16 hours. In elderly patients over the age of 70 years, the half-life is prolonged to 8 hours.[ Read more

Route of elimination

In healthy subjects, about 32-46% of total oral dose of finasteride was excreted in the urine in the form of metabolites while about 51-64% of the dose was excreted in the feces. In patients with renal impairment, the extent of urinary excretion of finasteride is expected to be decreased while the f... Read more

Toxicity

**LD50**

Oral LD50 is about 418 mg/kg in rats[MSDS] and there have been cases of lethality in rats receiving a single oral dose of 400 mg/kg in males and 1000 mg/kg in females.[13]

**... Read more

Adverse Effects

Effect Regions Age Groups Incidences Evidence Type
Dizziness US
  • adult
  • Kind: experimental
    • Percent: 23.2
  • Clinical Trial
    Impotence US
    • adult
  • Kind: experimental
    • Percent: 22.6
  • Clinical Trial
    Impotence US
    • adult
  • Kind: experimental
    • Percent: 18.5
  • Kind: placebo
    • Percent: 12.2
  • Kind: comparator
    • Percent: 14.4
  • Clinical Trial
    Postural Hypotension US
    • adult
  • Kind: experimental
    • Percent: 17.8
  • Clinical Trial
    Dizziness US
    • adult
  • Kind: experimental
    • Percent: 7.4
  • Kind: placebo
    • Percent: 8.1
  • Kind: comparator
    • Percent: 17.7
  • Clinical Trial
    Asthenia US
    • adult
  • Kind: experimental
    • Percent: 16.8
  • Clinical Trial
    Postural Hypotension US
    • adult
  • Kind: experimental
    • Percent: 9.1
  • Kind: placebo
    • Percent: 8
  • Kind: comparator
    • Percent: 16.7
  • Clinical Trial
    Asthenia US
    • adult
  • Kind: experimental
    • Percent: 5.3
  • Kind: placebo
    • Percent: 7.1
  • Kind: comparator
    • Percent: 15.7
  • Clinical Trial
    Ejaculation disorder US
    • adult
  • Kind: experimental
    • Percent: 14.1
  • Clinical Trial
    Decrease or loss of libido US
    • adult
  • Kind: experimental
    • Percent: 11.6
  • Clinical Trial
    Decrease or loss of libido US
    • adult
  • Kind: experimental
    • Percent: 10
  • Kind: placebo
    • Percent: 5.7
  • Kind: comparator
    • Percent: 7
  • Clinical Trial
    Impotence US
    • adult
  • Kind: experimental
    • Percent: 8.1
  • Kind: placebo
    • Percent: 3.7
  • Clinical Trial
    Ejaculation disorder US
    • adult
  • Kind: experimental
    • Percent: 7.2
  • Kind: placebo
    • Percent: 2.3
  • Kind: comparator
    • Percent: 4.5
  • Clinical Trial
    Decrease or loss of libido US
    • adult
  • Kind: experimental
    • Percent: 6.4
  • Kind: placebo
    • Percent: 3.4
  • Clinical Trial
    Impotence US
    • adult
  • Kind: experimental
    • Percent: 5.1
  • Kind: placebo
    • Percent: 5.1
  • Clinical Trial
    Headache US
    • adult
  • Kind: experimental
    • Percent: 2
  • Kind: placebo
    • Percent: 2.3
  • Kind: comparator
    • Percent: 4.1
  • Clinical Trial
    Somnolence US
    • adult
  • Kind: experimental
    • Percent: 1.7
  • Kind: placebo
    • Percent: 1.5
  • Kind: comparator
    • Percent: 3.7
  • Clinical Trial
    Decreased volume of ejaculate US
    • adult
  • Kind: experimental
    • Percent: 3.7
  • Kind: placebo
    • Percent: 0.8
  • Clinical Trial
    Hypotension US
    • adult
  • Kind: experimental
    • Percent: 1.2
  • Kind: placebo
    • Percent: 0.7
  • Kind: comparator
    • Percent: 3.4
  • Clinical Trial
    Peripheral Edema US
    • adult
  • Kind: experimental
    • Percent: 3.3
  • Clinical Trial
    Sexual function abnormal US
    • adult
  • Kind: experimental
    • Percent: 3.1
  • Clinical Trial
    Somnolence US
    • adult
  • Kind: experimental
    • Percent: 3.1
  • Clinical Trial
    Peripheral Edema US
    • adult
  • Kind: experimental
    • Percent: 1.3
  • Kind: placebo
    • Percent: 0.9
  • Kind: comparator
    • Percent: 2.6
  • Clinical Trial
    Decrease or loss of libido US
    • adult
  • Kind: experimental
    • Percent: 2.6
  • Kind: placebo
    • Percent: 2.6
  • Clinical Trial
    Sexual function abnormal US
    • adult
  • Kind: experimental
    • Percent: 2.5
  • Kind: placebo
    • Percent: 0.9
  • Kind: comparator
    • Percent: 2
  • Clinical Trial
    Rhinitis US
    • adult
  • Kind: experimental
    • Percent: 2.4
  • Clinical Trial
    Headache US
    • adult
  • Kind: experimental
    • Percent: 2.3
  • Clinical Trial
    Gynecomastia US
    • adult
  • Kind: experimental
    • Percent: 2.2
  • Kind: placebo
    • Percent: 0.7
  • Kind: comparator
    • Percent: 1.1
  • Clinical Trial
    Dyspnea US
    • adult
  • Kind: experimental
    • Percent: 0.7
  • Kind: placebo
    • Percent: 0.7
  • Kind: comparator
    • Percent: 2.1
  • Clinical Trial
    Dyspnea US
    • adult
  • Kind: experimental
    • Percent: 1.9
  • Clinical Trial
    Breast enlargement US
    • adult
  • Kind: experimental
    • Percent: 1.8
  • Kind: placebo
    • Percent: 1.1
  • Clinical Trial
    Gynecomastia US
    • adult
  • Kind: experimental
    • Percent: 1.5
  • Clinical Trial
    Hypotension US
    • adult
  • Kind: experimental
    • Percent: 1.5
  • Clinical Trial
    Decreased volume of ejaculate US
    • adult
  • Kind: experimental
    • Percent: 1.5
  • Kind: placebo
    • Percent: 0.5
  • Clinical Trial
    Rhinitis US
    • adult
  • Kind: experimental
    • Percent: 1
  • Kind: placebo
    • Percent: 0.5
  • Kind: comparator
    • Percent: 1.3
  • Clinical Trial
    Ejaculation disorder US
    • adult
  • Kind: experimental
    • Percent: 0.8
  • Kind: placebo
    • Percent: 0.1
  • Clinical Trial
    Breast tenderness US
    • adult
  • Kind: experimental
    • Percent: 0.7
  • Kind: placebo
    • Percent: 0.3
  • Clinical Trial
    Rash US
    • adult
  • Kind: experimental
    • Percent: 0.5
  • Kind: placebo
    • Percent: 0.1
  • Clinical Trial
    Rash US
    • adult
  • Kind: experimental
    • Percent: 0.5
  • Kind: placebo
    • Percent: 0.2
  • Clinical Trial
    Breast enlargement US
    • adult
  • Kind: experimental
    • Percent: 0.5
  • Kind: placebo
    • Percent: 0.1
  • Clinical Trial
    Breast tenderness US
    • adult
  • Kind: experimental
    • Percent: 0.4
  • Kind: placebo
    • Percent: 0.1
  • Clinical Trial
    Ejaculation disorder US
    • adult
  • Kind: experimental
    • Percent: 0.2
  • Kind: placebo
    • Percent: 0.1
  • Clinical Trial
    Tongue swelling US
    Post Marketing
    Swelling of the throat US
    Post Marketing
    Swelling of the face US
    Post Marketing
    Lip swelling US
    Post Marketing
    Abnormal orgasm US
    Post Marketing
    Breast Cancer US
    Post Marketing
    Depression US
    Post Marketing
    Poor seminal quality US
    Post Marketing

    Contraindications

    • Route:
      • Oral
    • Hypersensitivity:
      • true
    • Regions: US
    • Route:
      • Oral
    • Sex Group: female
    • Regions: US
    • Regions: US
    • Patient Conditions:
        • Name: Pregnancy
        • Drugbank Id: DBCOND0018394

    Food Interactions

    Take with or without food. The absorption is unaffected by food.