Dutasteride

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[edit] BRAND NAMES

[edit] STRUCTURE

Dutasteride.jpg

[edit] MECHANISM OF ACTION

The development and enlargement of the prostate gland is dependent on the potent androgen, dihydrotestosterone (DHT). Testosterone is converted to DHT by the enzyme 5 alpha-reductase, which exists as 2 isoforms, type I and type II. The type II isoenzyme is primarily active in the reproductive tissues, while the type I isoenzyme is also responsible for testosterone conversion in the skin and liver.

Dutasteride is a competitive and specific inhibitor of both type I and type II 5α-reductase isoenzymes, with which it forms a stable enzyme complex. Dissociation from this complex is extremely slow.
Dutasteride use in BPH has resulted in significantly reductions in prostatic volume and PSA level.

[edit] INDICATIONS

  • Treatment of symptomatic benign prostatic hyperplasia (BPH), alone or in combination with an Alpha 1 antagonist (e.g. Tamsulosin) in men with an enlarged prostate to improve symptoms, to reduce the risk of acute urinary retention and to reduce the risk of the need for surgery including transurethral resection of the prostate (TURP) and prostatectomy.
  • Androgenic alopecia (Off label)

Another 5α reductase inhibitor, Finasteride, is indicated for the treatment of both symptomatic BPH and androgenic alopecia.

[edit] DOSAGE

The recommended dose is 1 capsule (0.5 mg) taken once daily with or without food.

[edit] CONTRAINDICATIONS

  • Pregnancy and women of childbearing potential
  • Patients with previously demonstrated, clinically significant hypersensitivity (e.g., serious skin reactions, angioedema) to Dutasteride or other 5α-reductase inhibitors.

[edit] PRECAUTIONS

  • Men being treated with Dutasteride should not donate blood until at least 6 months have passed following their last dose. The purpose of this deferred period is to prevent administration of dutasteride to a pregnant female transfusion recipient

[edit] INTERACTIONS

Dutasteride is extensively metabolized in humans by the CYP3A4 and CYP3A5 isoenzymes. Use with caution in patients taking potent, chronic CYP3A4 enzyme inhibitors (e.g., ritonavir).

[edit] PREGNANCY AND LACTATION

  • Pregnancy Category X (US). Dutasteride is contraindicated for use in women of childbearing potential and during pregnancy.
  • Nursing Mothers: Dutasteride is contraindicated for use in women of childbearing potential, including nursing women

[edit] SIDE EFFECTS

The most common adverse reactions, reported in ≥1% of subjects treated with Dutasteride and more commonly than in subjects treated with placebo, are impotence, decreased libido, ejaculation disorders, and breast disorders (breast enlargement, gynecomastia, breast swelling, breast pain, breast tenderness, nipple pain, and nipple swelling).

[edit] RELATED LINKS

Benign Prostatic Hyperplasia (BPH) and Treatments (Video 1)
Benign Prostatic Hyperplasia (BPH) and Treatments (Video 2)

[edit] BIBLIOGRAPHY

[edit] BIBLIOGRAPHY

[edit] REFERENCES

Benign Prostatic Hypertrophy
5α reductase inhibitors Dutasteride (Avodart)   Finasteride (Proscar)
Alpha 1 antagonists Alfuzosin (Uroxatral, Xatral)   Doxazosin (Cardura)   Prazosin   Silodosin (Silodyx, Rapaflo)   Tamsulosin (Omnic, Flomax, Secotex)   Terazosin (Hytrin)
Phytotherapy Pygeum africanum   Serenoa repens
PDE5 inhibitors Tadalafil (Cialis)
Combination products Dutasteride/Tamsulosin (Combodart, Jalyn, Duodart)
Other Mepartricin
Veterinary Osaterone (Ypozane)
Androgens
Agonists Androstanolone   Dihydrotestosterone   Fluoxymesterone   Mesterolone   Methyltestosterone   Testosterone
Antiandrogens Androgen antagonists Bicalutamide   Chlormadinone acetate   Cyproterone acetate   Dienogest   Drospirenone   Flutamide   Nilutamide   Spironolactone
5α reductase inhibitors Dutasteride (Avodart)   Finasteride (Proscar)