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The drug was discovered as part of a screening process of chemicals that reversed the effects of mineralocorticoids in vivo. [27] Amiloride was the only drug in the screen that was capable of causing the excretion of sodium (natriuresis) without a concomitant urinary excretion of potassium (kaliuresis). [27]
Therefore, it is recommended that people using this medication avoid potassium supplements and salt substitutes containing potassium. [169] Physicians must be careful to monitor potassium levels in both males and females who are taking spironolactone as a diuretic, especially during the first twelve months of use and whenever the dosage is ...
Potassium binders are medications that bind potassium ions in the gastrointestinal tract, thereby preventing its intestinal absorption. This category formerly consisted solely of polystyrene sulfonate, a polyanionic resin attached to a cation, administered either orally or by retention enema to patients who are at risk of developing hyperkalaemia (abnormal high serum potassium levels).
Potassium-sparing diuretics or antikaliuretics [1] refer to drugs that cause diuresis without causing potassium loss in the urine. [2] They are typically used as an adjunct in management of hypertension , cirrhosis , and congestive heart failure . [ 3 ]
The same year, 1959, spironolactone was launched as a potassium-sparing diuretic. It became clear years later that aldosterone antagonists inhibit a specific receptor protein. This protein has high affinity for aldosterone but also for cortisol in humans and corticosterone in mice and rats. For this reason, aldosterone antagonists were called ...
This in turn results in an increase of blood pressure and blood volume. Aldosterone is produced in the zona glomerulosa of the cortex of the adrenal gland and its secretion is mediated principally by angiotensin II but also by adrenocorticotrophic hormone (ACTH) and local potassium levels.
The thiazides and potassium-sparing diuretics are considered to be calcium-sparing diuretics. [6] The thiazides cause a net decrease in calcium lost in urine. [7] The potassium-sparing diuretics cause a net increase in calcium lost in urine, but the increase is much smaller than the increase associated with other diuretic classes. [7]
Amlodipine causes several drugs to increase in levels, including cyclosporine, simvastatin, and tacrolimus (the increase in the last one being more likely in people with CYP3A5*3 genetic polymorphisms). [39] When more than 20 mg of simvastatin, a lipid-lowering agent, are given with amlodipine, the risk of myopathy increases. [40]