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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]
Canrenone is an antagonist of the MR as is spironolactone, [25] but it is slightly more potent in comparison. [24] [26] It has been determined that 7α-TMS accounts for around 80% of the potassium-sparing effect of spironolactone [1] [2] [3] while canrenone accounts for the remaining approximately 10 to 25%. [4]
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]
Potassium-sparing diuretics act to prevent sodium reabsorption in the collecting tubule by either binding ENaCs (amiloride, triamterene) or by inhibiting aldosterone receptors (spironolactone, eplerenone). This prevents excessive excretion of K + in urine and decreased retention of water, preventing hypokalemia. [10]
[229] [232] [233] The relationship between a single dose of spironolactone and plasma levels of canrenone, a major active metabolite of spironolactone, has been found to be linear across a dose range of 25 to 200 mg spironolactone. [195] Steady-state concentrations of spironolactone are achieved within 8 to 10 days of treatment initiation. [186 ...
Chlorthalidone is the thiazide drug that is most strongly supported by the evidence as providing a mortality benefit; in the ALLHAT study, a chlorthalidone dose of 12.5 mg was used, with titration up to 25 mg for those subjects who did not achieve blood pressure control at 12.5 mg. Chlorthalidone has repeatedly been found to have a stronger ...
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.
8–10 1–1.25 mg ~100% 2–3 Instantaneously (from 5 to 15 sec); 2–5 min 3–4 hours N-Phenethylnormorphine: 8–14 Alfentanyl: 10–25 1.5 (90–111 minutes) Instantaneously (from 5 to 15 sec); 4× more rapid than fentanyl 0.25 hr (15 min); up to 54 minutes until offset of effects Trefentanil: 10-25 Brifentanil: 10-25 Acetylfentanyl: 15