PROS-D

Generic Name:                   Dutasteride

Therapeutic Category:    Benign Prostatic Hyperplasia Agents

Pharmacological Class:   Type I and II 5 alpha-reductase inhibitor

Composition:                      Each film coated tablet contains Dutasteride IP 0.5 mg Tablet

Pregnancy Category:       X

Presentation:                      Available in the pack size as 14 tablets X 2 blisters

Mechanism of Action

Prostate growth is caused by a hormone in the blood called dihydrotestosterone (DHT). Dutasteride 0.5 mg inhibits both Type 1 and 2 5- alpha reductase enzymes. Dutasteride lowers DHT production in the body, leading to shrinkage of the enlarged prostate in most men. While some men have fewer problems and symptoms after 3 months of treatment with Dutasteride, a treatment period of at least 6 months is usually necessary to see if Dutasteride will work. Studies have shown that treatment with Dutasteride for 2 years reduces the risk of complete blockage of urine flow (acute urinary retention) and/or the need for surgery for benign prostatic hyperplasia (BPH).

Indications

• Improve symptoms of BPH
• Reduce the risk of acute urinary retention
• Reduce the risk of the need for BPH-related surgery

            Dosage 

              Route of administration: Oral

              Monotherapy: 0.5 mg orally once a day

Combination with Alpha-Adrenergic Antagonist: The recommended dose is 1 tablet (0.5 mg) taken once daily and Tamsulosin 0.4 mg taken once daily.

• Should be taken at least for 6 months even if symptoms improvement are seen.
• Can be taken with or without food.

Pharmacokinetics

• Absorption: Absolute bioavailability is approximately 60%
• Protein binding: Highly bound to albumin (99%) and α-1 acid glycoprotein (96.6%)
• Metabolism: Hepatic
• Route of elimination: Dutasteride is extensively metabolized in humans. Dutasteride and its metabolites were excreted mainly in feces.
• Half-life: 5 weeks

Adverse Effects

• headache and gastrointestinal discomfort 
• menstrual changes, acne, and dizziness also exist
• Difficulty in ejaculation
• Small risk of Gynaecomastia (breast enlargement) in men

Contraindications

PROS-D is contraindicated in the following populations and situations:

• Women who are or who may become pregnant should not handle the drug. Dutasteride can cause birth defects, specifically ambiguous genitalia and under masculinization, in male fetuses. This is due to its anti-androgenic effects and is seen naturally in 5α-reductase deficiency. As such, women who are pregnant should never take Dutasteride.
• People taking Dutasteride should not donate blood to prevent birth defects if a pregnant woman receives blood and, due to its long elimination half-life, should also not donate blood for at least 6 months after the cessation of treatment.
• People with known significant hypersensitivity (e.g., serious skin reactions, angioedema) to dutasteride should not take Dutasteride.
• Women, children and adolescent

Drug Interactions

• Pros-D may reduce or block the sedative, anticonvulsant, anxiolytic, and various other effects of progesterone, particularly in the case of oral progesterone (which is disproportionately converted into these metabolites due to first-pass metabolism)