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5α-Reductase Inhibitors Overview

5α-Reductase inhibitors (5αRI) are medications that reduce the production of dihydrotestosterone (DHT) by inhibiting the 5α-reductase enzyme. DHT is the more potent active metabolite of testosterone, responsible for several androgenic effects:

  • Scalp hair loss (androgenetic alopecia)
  • Facial and body hair growth
  • Increased sebum production (oily skin/acne)
  • Prostate enlargement

5αRIs are not primary anti-androgens. They do not directly lower testosterone levels — instead, they block the conversion of testosterone to DHT. In transfeminine HRT, 5αRIs are typically used as adjunctive therapy in the following scenarios [1] :

  • Persistent scalp hair loss after starting HRT
  • Unsatisfactory rate of facial/body hair reduction
  • T is in female range but DHT remains elevated
  • As a supplement to spironolactone or CPA, not a replacement
  • ❌ Cannot lower testosterone levels
  • ❌ Cannot replace primary anti-androgens
  • ❌ Cannot reverse completed skeletal masculinization
  • ❌ Cannot promote breast development
FeatureFinasterideDutasteride
TargetType II 5α-reductase onlyType I + Type II 5α-reductase
DHT reduction~65-70%~90-95%
Half-life~6-8 hours~4-5 weeks
OnsetMonthsMonths
Evidence levelBC
CostLower (generics available)Higher