Dutasteride

Abstract

Dutasteride, a potent inhibitor of type 1 and 2 5alpha-reductase, reduced dihydrotestosterone levels by >90% in 85% of patients following 1 years' administration of oral dutasteride 0.5 mg/day. A combined analysis of three placebo-controlled clinical studies conducted in patients with benign prostatic hyperplasia (BPH) found sustained improvements in American Urological Association- Symptom Index scores and urinary flow rate and a 57% decrease in the risk of acute urinary retention throughout the 2-year treatment period (all p < 0.001 vs placebo). Total prostate and transition zone volume were also reduced (both p < 0.001), as was the risk of BPH-related surgery (by 48%). A nonblind extension study found that dutasteride maintains efficacy for up to 4 years. Dutasteride monotherapy maintained symptom relief following combination treatment with dutasteride and tamsulosin in all patients but those with severe symptoms. Dutasteride was generally well tolerated. Impotence, reduced libido, gynaecomastia and ejaculation disorder occurred significantly more often in dutasteride than placebo recipients, but incidence was generally low. With the exception of gynaecomastia, incidence consistently decreased over time.

Influence of hydrophilic additives on the supersaturation and bioavailability of dutasteride-loaded hydroxypropyl- &beta;-cyclodextrin nanostructures

“…1 Currently, this agent is used for the treatment of benign prostatic hyperplasia and hair loss. 2 However, dutasteride is insoluble in water (,0.038 ng/mL), 3 and in its commercial dosage form is formulated as a soft gelatin capsule containing monoglycerides and diglycerides of caprylic/capric acid as solubilizers. Although the oral bioavailability of the soft gelatin capsule is 60% (range 40%-94%) in humans, it must be swallowed whole and not chewed or opened because the contents may irritate the oropharyngeal mucosa.…”

Benign Prostatic Hyperplasia: Updated Review

“…This drug has a distinct mechanism of action; in that it blocks both types 1and 2, 5alpha reductase. 44 Sexual side effects are similar to those of finasteride.…”

“…The U.S. Food and Drug Administration recently labelled dutasteride in 0.5-mgcapsule form, for the treatment of BPH 44 (labeling for male-pattern baldness ispending). This drug has a distinct mechanism of action; in that it blocks both types 1and 2, 5alpha reductase.…”

A Method to Monitor Dutasteride in Rat Plasma Using Liquid-Liquid Extraction and Multiple Reaction Monitoring: Comparisons and Validation

“…[1][2][3][4][5][6] While its potent pharmacological activity makes it popular in clinical fields, its formulation in market is only limited to a soft gelatin capsule filled with dutasteride in oils because of its low water solubility. 7 Since this type of formulation generally shows issues such as limited stability, a short shelf life, and a reduced release rate of a drug, the development of various dutasteride formulations is needed.…”