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For comparison, the clinical dosage range of spironolactone in humans is usually about 4 to 8 mg/kg. [30] There is also mixed/conflicting evidence that spironolactone may inhibit 5α-reductase, and thus the synthesis of the potent androgen DHT from testosterone, to some extent.
Pharmacokinetics of 100 mg/day spironolactone and its metabolites Compound C max Tooltip Peak concentrations (day 1) C max Tooltip Peak concentrations (day 15) AUC Tooltip Area-under-the-curve concentrations (day 15) t 1/2 Tooltip Elimination half-life; Spironolactone: 72 ng/mL (173 nmol/L) 80 ng/mL (192 nmol/L) 231 ng•hour/mL (555 nmol ...
[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 ...
However, spironolactone is metabolized to three active metabolites, which give it prolonged activity (13.8 – 16. 5 hours). Spironolactone has a long half-life and is excreted 47-51% through kidneys. Patients with chronic kidney disease therefore require close monitoring when taking the drug. Spironolactone is also eliminated through feces (35-41%
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
Population pharmacokinetics seeks to identify the measurable pathophysiologic factors and explain sources of variability that cause changes in the dose-concentration relationship and the extent of these changes so that, if such changes are associated with clinically relevant and significant shifts in exposures that impact the therapeutic index ...
Canrenone is an active metabolite of spironolactone, canrenoic acid, and potassium canrenoate, and is considered to be partially responsible for their effects. [9] It has been found to have approximately 10 to 25% of the potassium-sparing diuretic effect of spironolactone, [ 16 ] whereas another metabolite, 7α-thiomethylspironolactone (7α-TMS ...
An equianalgesic chart can be a useful tool, but the user must take care to correct for all relevant variables such as route of administration, cross tolerance, half-life and the bioavailability of a drug. [5] For example, the narcotic levorphanol is 4–8 times stronger than morphine, but also has a much longer half-life. Simply switching the ...