Ad
related to: alternative for spironolactone in men over 70 days free pdf full
Search results
Results From The WOW.Com Content Network
[30] [70] [71] [72] Although spironolactone is said to be a relatively weak inhibitor of 17α-hydroxylase and 17,20-lyase, [73] [30] at least compared to more potent steroidogenesis inhibitors like ketoconazole and abiraterone acetate (which can reduce testosterone concentrations to castrate levels), this action may contribute to a significant ...
Due to its progestogenic (and by extension antigonadotropic) activity, CPA is able to suppress circulating testosterone levels by 70 to 80% in men at high dosages. [ 25 ] [ 94 ] In contrast, NSAAs increase testosterone levels by up to 2-fold via blockade of the AR , a difference that is due to their lack of concomitant antigonadotropic action ...
The trial was stopped early because the beneficial effect of spironolactone on all-cause death exceeded the prespecified discontinuation requirements. Spironolactone reduced the risk of death by 30% compared to placebo. Additionally, there was a 35% reduction in the risk of hospitalization for worsening heart failure in the spironolactone group.
Eplerenone may have a lower incidence than spironolactone of sexual side effects such as feminization, gynecomastia, impotence, low sex drive and reduction of size of male genitalia. [18] This is because other antimineralocorticoids have structural elements of the progesterone molecule, causing progestogenic and antiandrogenic outcomes. [ 4 ]
Spironolactone – most widespread use, inexpensive; Eplerenone – more selective so reduced side-effects but more expensive and less potent; Finerenone – non-steroidal, more selective and potent than spironolactone and eplerenone; Canrenone – very limited use
At very high doses (400 mg/day), spironolactone has also been associated with testicular atrophy and reversibly reduced fertility, including semen abnormalities such as decreased sperm count and motility in cis men. [110] [111] However, such doses of spironolactone are rarely used clinically. [111]
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]
Pharmacokinetics of 100 mg/day spironolactone and its metabolites Compound C max Tooltip Peak concentrations (day 1) C max Tooltip Peak concentrations (day 15) AUC Tooltip Area-under-the-curve concentrations (day 15) t 1/2 Tooltip Elimination half-life; Spironolactone: 72 ng/mL (173 nmol/L) 80 ng/mL (192 nmol/L) 231 ng•hour/mL (555 nmol ...