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Eplerenone is an antimineralocorticoid, or an antagonist of the mineralocorticoid receptor (MR). [21] Eplerenone is also known chemically as 9,11α-epoxy-7α-methoxycarbonyl-3-oxo-17α-pregn-4-ene-21,17-carbolactone and "was derived from spironolactone by the introduction of a 9α,11α-epoxy bridge and by substitution of the 17α-thoacetyl ...
Spironolactone is rapidly and extensively metabolized in the liver upon oral administration and has a very short terminal half-life of 1.4 hours. [11] [12] The major metabolites of spironolactone are 7α-thiomethylspironolactone (7α-TMS), 6β-hydroxy-7α-thiomethylspironolactone (6β-OH-7α-TMS), and canrenone (7α-desthioacetyl-δ 6 ...
Absorption half-life 1 h, elimination half-life 12 h. Biological half-life (elimination half-life, pharmacological half-life) is the time taken for concentration of a biological substance (such as a medication) to decrease from its maximum concentration (C max) to half of C max in the blood plasma.
In this situation it is generally uncommon to talk about half-life in the first place, but sometimes people will describe the decay in terms of its "first half-life", "second half-life", etc., where the first half-life is defined as the time required for decay from the initial value to 50%, the second half-life is from 50% to 25%, and so on.
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]
Eplerenone, a steroidal antimineralocorticoid of the spirolactone group Estriol triacetate , an estrogen medication and an estrogen ester Index of chemical compounds with the same molecular formula
The pharmacodynamics of spironolactone, an antimineralocorticoid and antiandrogen medication, concern its mechanisms of action, including its biological targets and activities, as well as its physiological effects.
Alternatively, since the radioactive decay contributes to the "physical (i.e. radioactive)" half-life, while the metabolic elimination processes determines the "biological" half-life of the radionuclide, the two act as parallel paths for elimination of the radioactivity, the effective half-life could also be represented by the formula: [1] [2]