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Testosterone 5 Alpha-Reductase Inhibitor.
Pharmacology: Pharmacodynamics: Finasteride is synthetic 4-azasteroid compound. Finasteride is an inhibitor of Type II 5-alpha reductase, an intracellular enzyme which metabolises testosterone into the more potent androgen dihydrotestosterone (DHT). Finasteride has no affinity for the androgen receptor.
The development of the prostate hyperplasia (BHP) is dependent upon the conversion of testosterone to DHT within the prostate.
Finasteride reduces circulating and intraprostatic DHT. Within 24 hours after oral administration of Finasteride there is a significant reduction in circulating DHT levels as a result of the inhibition of 5-alpha reductase.
Pharmacokinetics: Following an oral dose of C-Finasteride in humans, the bioavailability is approximately 80% and is not affected by food.
Maximum Finasteride plasma concentrations are reached about 2 hours after dosing and the absorption is complete after 6 to 8 hours. Protein binding is approximately 93%, plasma clearance about 165 mL/min and the volume of distribution, 76 litres. Finasteride displays a mean plasma.
Elimination half-life of approximately 6 hours (4-12 hours) in subjects 46-60 years of age and approximately 8 hours in men 70 years of age and older.
Two metabolites of Finasteride have been identified which possess only a small fraction of the 5-alpha reductase inhibitory activity of Finasteride. 36% of the dose is excreted in the urine in the form of metabolites and 57% of the total dose is excreted in the feces.
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