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Eplerenone differs from spironolactone in its extensive metabolism, with a short half-life and inactive metabolites. [4] Eplerenone seems to be about 50 to 75% as potent as spironolactone as an antimineralocorticoid. [24] Hence, 25 mg/day spironolactone may be equivalent to approximately 50 mg/day eplerenone. [25]
Eplerenone is also contraindicated for the treatment of hypertension in patients with type 2 diabetes with microalbuminuria, serum creatinine greater than 2.0 mg/dL in males or greater than 1.8 mg ...
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]
Conversely, in studies of healthy men given high-dose spironolactone, gynecomastia occurred in 3 of 10 (30%) at 100 mg/day, in 5 of 8 (62.5%) at 200 mg/day, and in 6 of 9 (66.7%) at 400 mg/day, relative to none of 12 controls. [134] [135] The severity of gynecomastia with spironolactone varies considerably, but is usually mild. [110]
At dosages of 100 mg/day and 200 mg/day, observed reductions in hair shaft diameter were 19% ± 8% and 30% ± 3%, respectively (p = 0.07). [ 61 ] [ 62 ] [ 35 ] Levels of free testosterone were unchanged, however, suggesting that the antiandrogenic efficacy of spironolactone was due exclusively to direct AR blockade.
Ketoconazole is used orally in dosages of 200 to 400 mg per day in the treatment of superficial and deep fungal infections. [25] Off-label uses ... , eplerenone; HMG ...
Daiichi Sankyo Company, Limited on January 8, 2019 announced the receipt of marketing approval in Japan for MINNEBROTM Tablets 1.25 mg, 2.5 mg and 5 mg (generic name: esaxerenone) for the treatment of hypertension. As of January 2019, esaxerenone is in phase III clinical trials for diabetic nephropathies. [1] [4]
Epalrestat is a carboxylic acid derivative [1] and a noncompetitive and reversible aldose reductase inhibitor used for the treatment of diabetic neuropathy, which is one of the most common long-term complications in patients with diabetes mellitus.