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Other activities of spironolactone may include very weak interactions with the estrogen and progesterone receptors and agonism of the pregnane X receptor. [97] [217] These activities could contribute to the menstrual irregularities and breast side effects of spironolactone and to its drug interactions, respectively. [218] [219] [220]
[21] [134] [20] Examples of such interactions include oral digoxin and estradiol. [136] [79] There is evidence that spironolactone may block voltage-dependent Ca 2+ channels [139] [140] and voltage-gated potassium (K +) channels. [141] Spironolactone has been identified as an inhibitor of NRG1‐ERBB4 signaling. [142]
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%
They can be used in combination with other anti-hypertensives or drugs that cause hypokalemia to help maintain a normal range for potassium. For example, they are often used as an adjunct to loop diuretics (usually furosemide) to treat fluid retention in congestive heart failure and ascites in cirrhosis. [11]
Digoxin elimination is mainly by renal excretion and involves P-glycoprotein, which leads to significant clinical interactions with P-glycoprotein inhibitor drugs. Examples commonly used in patients with heart problems include spironolactone, verapamil and amiodarone.
[10] [4] The medication is an analog of the drug spironolactone. [11] Drospirenone is taken by mouth. [1] [4] Common side effects include acne, headache, breast tenderness, weight increase, and menstrual changes. [4] Rare side effects may include high potassium levels and blood clots (when taken as a combined oestrogen-progestogen pill), among ...
The mineralocorticoid receptor (or MR, MLR, MCR), also known as the aldosterone receptor or nuclear receptor subfamily 3, group C, member 2, (NR3C2) is a protein that in humans is encoded by the NR3C2 gene that is located on chromosome 4q31.1-31.2.
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.