Finasteride (Proscar) - Uses, Dose, Side effects, MOA, Brands

Finasteride (Proscar) is a type II 5 alpha reductase inhibitor that inhibits the activation of testosterone to dihydrotestosterone. It is used to treat BPH and male pattern hair baldness.

 

Finasteride (Proscar) Uses:

  • Androgenetic alopecia (Propecia):

    • It is indicated for the treatment of male pattern hair loss in men only.
    • Limitations of use:
      • It is not indicated for the treatment of alopecia in women. Furthermore, the efficacy of the drug in patients with bitemporal recession has not been established.
  • Benign prostatic hyperplasia (Proscar):

    • It is indicated as monotherapy for the treatment of patients with symptomatic benign prostatic hyperplasia to:
      • improve the patients symptoms
      • reduce the risks of developing acute urinary retention
      • reduce or delay the need for BPH-related surgery.
    • It may be used in combination with doxazosin or another alpha blocker to reduce the risk of symptomatic progression.1
    • Limitations of use:
      • It has not been approved for the prevention if prostate cancer.
  • Off Label Use of Finasteride in Adults:

    • Hirsutism

Finasteride (Proscar) Dose in Adults

Finasteride (Proscar) Dose in the treatment of Benign prostatic hyperplasia (Proscar):

  • Males:
    • 5 mg orally once a day as monotherapy or in combination with doxazosin.
    • Patients may notice clinical response early with treatment, however, it may take up to six months.

Finasteride (Proscar) Dose in the treatment of Hirsutism (off-label):

  • Females:
    • 2.5 to 5 mg orally once a day.
    • Assess clinical response at 6 months interval before adjusting the dose, switching therapy, or adding additional agents.

Finasteride (Proscar) Dose in the treatment of Male pattern baldness (Propecia):

  • Males:
    • 1 mg orally once a day.
    • It may take up to 3 months or longer if clinically significant benefits are observed.
    • To sustain clinically significant benefits, the drug should be used continuously.

Dose in children:

Not recommended for use in children.

Finasteride (Proscar) Pregnancy Risk Factor X

  • It is not recommended for pregnant women.
  • Because it inhibits testosterone, it can cause abnormalities in male fetuses' external genitalia.
  • Avoid contact with brojen or crushed tablets for pregnant women
  • PCOS-positive females who use the drug for hirsuitism should be informed of appropriate contraception in order to prevent pregnancy.

Breastfeeding: Finasteride is not recommended

  • It is unknown if the drug will be excreted into breastmilk.
  • This should be avoided by females with childbearing potential.

Dose in Kidney Disease:

Adjustment in the dose is not necessary.

Dose in Liver disease:

  • The manufacturer has not provided any dose adjustment in patients with liver disease.
  • However, since the drug is extensively metabolized in the liver, it should be used with caution in these patients.

Common Side Effects of Finasteride (Proscar):

  • Genitourinary:

    • Impotence

Less Common Side Effects of Finasteride (Proscar):

  • Cardiovascular:

    • Orthostatic Hypotension
    • Peripheral Edema
    • Hypotension
  • Endocrine & Metabolic:

    • Decreased Libido
    • Gynecomastia
  • Genitourinary:

    • Ejaculatory Disorder
    • Decreased Ejaculate Volume
    • Sexual Disorder
    • Breast Tenderness
  • Hematologic & Oncologic:

    • Prostate Cancer
  • Respiratory:

    • Rhinitis

Contraindications to Finasteride (Proscar):

  • Allergy reactions to finasteride and any component of the formulation
  • Women of childbearing potential or pregnancy

Warnings and precautions

  • Reduced urinary flow

    • Patients with a high residual urinary volume, or signs of obstruction of the urinary system may not be eligible for 5-alpha reductase inhibitors.
  • Hepatic impairment

    • Patients with liver disease should not take the drug as it is highly metabolized in their liver.
  • Prostate cancer:

    • For the prevention of prostate cancer, 5-alpha reductase inhibits have not yet been approved.
    • The incidence of high-grade prostate cancer has increased due to its use.

Monitoring parameters:

  • Monitor for the clinical symptoms and signs of benign prostatic hyperplasia that include urinary flow, difficulty in passing urine, and urinary urgency.
  • Establish a baseline PSA after six months of the treatment and monitor PSA levels periodically thereafter.

How to administer Finasteride (Proscar)?

  • It may be administered with or without meals.
  • Pregnant females and Females of childbearing ages should not handle broken or crushed tablets.

Mechanism of action of Finasteride (Proscar):

  • It inhibits competitively the Type II 5-alpha reductase enzyme, which converts testosterone into dihydrotestosterone.
  • This results in suppression of serum dihydrotestosterone.

Time:

  • After discontinuing the drug, it takes 14 days for dihydrotestosterone levels normal to return.
  • Patients with BPH can have their prostates returned to normal size within three months of treatment.
  • It takes twelve months to reverse the increase in hair count when used to treat male-pattern baldness.

Protein binding:

  • About 90%

Metabolism:

  • It is metabolized extensively in the liver via CYP3A4 to two active metabolites (<20% activity of finasteride)

Bioavailability:

  • Mean:
    • 5 mg: ~63%;
    • 1 mg: 65% (not affected by food)

Half-life elimination, serum:

  • 5 to 6 hours (range: 3 to 16 hours);
  • Older patients (≥70 years): 8 hours (range: 6 to 15 hours)

Time to peak, serum:

  • 1 to 2 hours

Excretion:

  • Feces (57%) and urine (39%; as metabolites)

International Brand Names of Finasteride:

  • Propecia
  • Proscar
  • ACH-Finasteride
  • ACT Finasterid e
  • APO-Finasterid
  • Auro-Finasterid e
  • DOM-Finasterid
  • JAMP-Finasterid
  • MINT-Finasterid
  • MYLAN-Finasterid e HG
  • MYLAN-Finasterid
  • PMS-Finasterid e
  • RAN-Finasterid
  • RATIO-Finasteride
  • RIVA-Finasterid
  • SANDOZ Finasteride
  • SANDOZ Finasterid A
  • TEVA-Finasteride
  • VAN-Finasterid
  • Alofecid
  • Alopec
  • Alopros 5
  • Androfin
  • Aprodil
  • Atepros
  • Bearfina
  • Benstat
  • Binfin
  • Binfin 5
  • Chibro-Proscar
  • Damocare
  • Damopecia
  • Daric
  • Fina-5
  • Finapecia
  • Finapros
  • Finarid
  • Finas
  • Finascar
  • Finaspro
  • Finaspros
  • Finast
  • Finasta
  • Finastar
  • Finastid
  • Finated
  • Finatra
  • Fincar
  • Finide
  • Finiscar
  • Finnacar
  • Finpro
  • Finstal-5
  • Finster
  • Fintrid
  • Firide
  • Fistrin
  • For-BPH
  • Fynasid
  • GPO-Finax
  • Harifin
  • Jun Neng
  • Maxteride
  • Monastar
  • Nopecia
  • Penester
  • Pro-Cure
  • Profal
  • Prohair
  • Pronax
  • Pronor
  • Propecia
  • Propeshia
  • Proscar
  • Proseride
  • Prosfin
  • Prostacare
  • Prostan
  • Prostanus
  • Prostarinol
  • Prosterid
  • Prosteride
  • Prostide
  • Prostop
  • Proteside
  • Reprostom
  • Skarex
  • Stercia
  • Stercia-5
  • Sterzar
  • Tensen
  • Uromedin

Finasteride Brand Names in Pakistan:

Finasteride Tablets 1 mg in Pakistan

Genesis Ferozsons Laboratoies Ltd.
Hairfin Sante (Pvt) Limited
Xandrox Unison Chemical Works

 

Finasteride Tablets 5 mg in Pakistan

Fenstar Hansel Pharmacueutical Pvt (Ltd)
Finasta Linear Pharma
Proscar Obs
Prosterid Medimpex Scientific Office
Prostryl Tb Novins International