Effects of finasteride (MK-906)

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J Clin Endocrinol Metab. 1990 Apr ;70 (4):1136-41 2156887 (P,S,G,E,B) Cited:3
Effects of finasteride (MK-906), a 5 alpha-reductase inhibitor, on circulating androgens in male volunteers.
G J Gormley, E Stoner, R S Rittmaster, H Gregg, D L Thompson, K C Lasseter, P H Vlasses, E A Stein Merck, Sharp, and Dohme Research Laboratories, Rahway, New Jersey 07065.
Finasteride, a 5 alpha-reductase inhibitor, was administered to normal male volunteers in a blinded placebo-controlled study at daily oral doses of 25, 50, and 100 mg for 11 days (part 1) and daily oral doses of .04, .12, .2, and 1. mg for 14 days (part 2).

Results from part 1 showed a significant reduction in dihydrotestosterone (DHT) at all doses and a significant increase in both testosterone (T) and delta 4-androstenedione at the 50- and 100-mg doses. No change was seen in LH, FSH, cortisol, or estradiol levels. Serum lipids, including total cholesterol, low density lipoprotein, high density lipoprotein, and triglycerides were not affected by treatment. Results from part 2 again showed significant reduction in DHT at all doses.

DHT levels returned to pretreatment values within 14 days of discontinuing treatment. Significant increases in T were observed only in the 1. mg group and only during the first 8 days of treatment.
The T/DHT ratio increased with all doses and returned to baseline when drug was discontinued.

The DHT metabolites and androstanediol glucuronide and androsterone glucuronide were significantly reduced at all doses.
There were no significant adverse experiences reported during part 1 or 2.
In conclusion, finasteride is well tolerated by normal volunteers and results in significant suppression of serum DHT at all doses tested.





Hormonal effects of a 5 alpha-reductase inhibitor (finasteride) on hormonal levels in normal men and in patients with benign prostatic hyperplasia.
Vermeulen A, Giagulli VA, De Schepper P, Buntinx A.

Department of Endocrinology, University Hospital Ghent, Belgium.

Finasteride is a potent competitive 5 alpha-reductase inhibitor, active at a dose as low as 1 mg/day. After a single dose, the effects on 5 alpha-reductase last as long as 7 days. Both hepatic and target tissue 5 alpha-reductase are inhibited. Plasma testosterone and estradiol are unaffected and luteinizing hormone levels do not change. During chronic treatment with finasteride 5 mg/day, the effects on 5 alpha-reductase are maintained. Since the only significant effect of chronic finasteride therapy appears to be 5 alpha-reductase inhibition, and testosterone or estradiol levels are not affected, neither libido nor potency is lost. Testosterone is the active androgen at the muscular level; therefore, muscular catabolism is not expected.
 

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