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Androgen receptor antagonistic potency of spironolactone, cyproterone acetate, and flutamide in castrated male rats treated with exogenous testosterone (as measured by inhibition of androgen-dependent ventral prostate weight). [27] Spironolactone is an antagonist of the AR, the biological target of androgens like testosterone and DHT.
Low-dose spironolactone is generally very well tolerated. [62] Even higher doses of spironolactone, ... which resulted in approximately 4-fold increased potency.
SC-8109, the 19-nor (19-demethyl) analogue, was developed and found to have improved oral bioavailability and potency, but still had low potency. [5] Spironolactone (SC-9420; Aldactone) followed and had both good oral bioavailability and potency, and was the first synthetic antimineralocorticoid to be marketed. [3]
[97] [96] [98] However, this action is of low potency, and spironolactone has mixed and inconsistent effects on hormone levels. [97] [96] [98] [99] [100] In any case, testosterone levels are usually unchanged by spironolactone.
This is a list of 5α-reductase inhibitors (5α-RIs), drugs which inhibit one or more isoforms of the enzyme 5α-reductase.This enzyme is responsible for the conversion of the androgen hormone testosterone into the more potent dihydrotestosterone (DHT) and is essential for the production of neurosteroids like allopregnanolone, tetrahydrodeoxycorticosterone (THDOC), and 3α-androstanediol from ...
Spironolactone is a prodrug with a short terminal half-life of 1.4 hours. [5] [6] [7] The active metabolites of spironolactone have extended terminal half-lives of 13.8 hours for 7α-TMS, 15.0 hours for 6β-OH-7α-TMS, and 16.5 hours for canrenone, and accordingly, these metabolites are responsible for the therapeutic effects of the drug. [5] [6]
A highly potent drug (e.g., fentanyl, clonazepam, risperidone, benperidol, bumetanide) evokes a given response at low concentrations, while a drug of lower potency (e.g. morphine, alprazolam, ziprasidone, haloperidol, furosemide) evokes the same response only at higher concentrations.
Unlike spironolactone, bicalutamide has no antimineralocorticoid activity, [97] and for this reason, has no risk of hyperkalemia (which can, rarely/in severe cases, result in hospitalization or death) [112] or other antimineralocorticoid side effects such as urinary frequency, dehydration, hypotension, hyponatremia, metabolic acidosis, or ...
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