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Description: Side effects of spironolactone (25–400 mg/day) with ≥1% incidence in a 2017 hybrid systematic review of clinical studies of spironolactone for acne in women.
Eplerenone is a newer drug that was developed as a spironolactone analog with reduced adverse effects. In addition to the y-lactone ring and the substituent on C-7, eplerenone has a 9α,11α-epoxy group. This group is believed to be the reason why eplerenone has a 20-40-fold lower affinity for the mineralocorticoid receptor than spironolactone. [7]
However, the dosages of spironolactone used in animals to produce progestogenic effects were very high (50–200 mg/kg/day in rabbits, 400 mg/day in rhesus monkeys). [118] In one study, the threshold dose by subcutaneous injection for endometrial transformation in rabbits was 0.003–0.01 mg for cyproterone acetate , 0.1–0.3 mg for ...
Common adverse drug reactions (ADRs) associated with the use of eplerenone include: hyperkalaemia, hypotension, dizziness, and reduced renal clearance. [17] 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]
Triamterene – increased renal side-effects; Aldosterone antagonists, also known as mineralocorticoid receptor antagonists: [7] Spironolactone – most widespread use, inexpensive; Eplerenone – more selective so reduced side-effects but more expensive and less potent
Spirolactones are a class of functional group in organic chemistry featuring a cyclic ester attached spiro to another ring system. The name is also used to refer to a class of synthetic steroids, called steroid-17α-spirolactones, 17α-spirolactosteroids, or simply 17α-spirolactones, which feature their spirolactone group at the C17α position.
For people with hyperplasia of both glands, successful treatment is often achieved with spironolactone or eplerenone, drugs that block the aldosterone receptor. With its antiandrogen effect, spironolactone drug therapy may have a range of side effects in males and females, including gynecomastia and irregular menses. These symptoms occur less ...
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 ...