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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 ...
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.
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]
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.
An effective half-life of the drug will involve a decay constant that represents the sum of the biological and physical decay constants, as in the formula: = + With the decay constant it is possible to calculate the effective half-life using the formula:
IC50 to pIC50 calculator Online tool for analysis of in vitro resistance to antimalarial drugs IC50-to-Ki converter of an inhibitor and enzyme that obey classic Michaelis-Menten kinetics .
t 1/2 is the half-life time of the drug, which is the time needed for the plasma drug concentration to drop to its half Therefore, the amount of drug present in the body at time t A t {\displaystyle A_{t}} is;
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 ...