40 Facts About Spironolactone

Spironolactone, sold under the brand name Aldactone among others, is a medication that is primarily used to treat fluid build-up due to heart failure, liver scarring, or kidney disease.

Spironolactone has not been well studied in pregnancy and should not be used to treat high blood pressure of pregnancy.

Spironolactone belongs to a class of medications known as potassium-sparing diuretics.

Spironolactone is used primarily to treat heart failure, edematous conditions such as nephrotic syndrome or ascites in people with liver disease, essential hypertension, low blood levels of potassium, secondary hyperaldosteronism, and Conn's syndrome .

Spironolactone is used to treat Bartter's syndrome due to its ability to raise potassium levels.

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Spironolactone is the most commonly used medication in the treatment of hirsutism in the United States.

Spironolactone is commonly used to treat symptoms of hyperandrogenism, such as due to polycystic ovary syndrome, in women.

Spironolactone should be considered a good add-on agent, particularly in those patients "not" yet optimized on ACE inhibitors and beta-blockers.

Spironolactone is used in the treatment of hyperaldosteronism, for instance primary aldosteronism .

Spironolactone is commonly used in the treatment of hirsutism in women, and is considered to be a first-line antiandrogen for this indication.

Spironolactone can be used in the treatment of female-pattern hair loss .

Spironolactone is not generally used in men for the treatment of androgen-dependent dermatological conditions because of its feminizing side effects, but it is effective for such indications in men similarly.

Spironolactone is considered to be a first-line treatment for hirsutism, finasteride and the steroidal antiandrogen cyproterone acetate are considered to be second-line treatments, and flutamide is no longer recommended for hirsutism due to liver toxicity concerns.

Spironolactone can be considered as a first-line treatment for acne in those who have failed other standard treatments such as topical therapies and under certain other circumstances, although this is controversial due to the side effects of spironolactone and its teratogenicity.

Spironolactone is frequently used as a component of feminizing hormone therapy in transgender women, especially in the United States, usually in addition to an estrogen.

Spironolactone is available in the form of tablets and suspensions for use by mouth.

Spironolactone has poor water solubility, and for this reason, only oral and topical formulations have been developed; other routes of administration such as intravenous injection are not used.

Spironolactone produces an irregular and anovulatory pattern of menstrual cycles.

Spironolactone bodies are eosinophilic, round, concentrically laminated cytoplasmic inclusions surrounded by clear halos in preparations stained with hematoxylin and eosin.

Spironolactone should be discontinued in people with impaired kidney function or hyperkalemia.

Spironolactone has been reported to induce the enzymes CYP3A4 and certain UDP-glucuronosyltransferases, which can result in interactions with various medications.

Spironolactone can have numerous other interactions, most commonly with other cardiac and blood pressure medications, for instance digoxin.

Spironolactone is a prodrug, so most of its actions are actually mediated by its various active metabolites.

Spironolactone has been found in some studies to increase levels of estradiol, an estrogen, although many other studies have found no changes in estradiol levels.

Spironolactone is bound equivalently to albumin and a1-acid glycoprotein, while canrenone is bound only to albumin.

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Spironolactone is rapidly and extensively metabolized in the liver upon oral administration and has a very short terminal half-life of 1.

Spironolactone is hydrolyzed or deacetylated at the thioester of the C7a position into 7a-TS by carboxylesterases.

Spironolactone, known as 7a-acetylthiospirolactone, is a steroidal 17a-spirolactone, or more simply a spirolactone.

Spironolactone is closely related structurally to other clinically used spirolactones such as canrenone, potassium canrenoate, drospirenone, and eplerenone, as well as to the never-marketed spirolactones SC-5233, SC-8109, spiroxasone, prorenone, mexrenone, dicirenone, spirorenone, and mespirenone .

Spironolactone was first synthesized in 1957, was patented between 1958 and 1961, and was first marketed, as an antimineralocorticoid, in 1959.

Spironolactone was first studied in the treatment of hirsutism in women in 1978.

Spironolactone was first studied as an antiandrogen in transgender women in 1986, and has since become widely adopted for this purpose as well, particularly in the United States where cyproterone acetate is not available.

Spironolactone is known by its developmental code names SC-9420 and NSC-150339.

Spironolactone is marketed under a large number of brand names throughout the world.

Spironolactone is formulated in combination with a variety of other medications, including with hydrochlorothiazide as Aldactazide, with hydroflumethiazide as Aldactide, Lasilacton, Lasilactone, and Spiromide, with altizide as Aldactacine and Aldactazine, with furosemide as Fruselac, with benazepril as Cardalis, with metolazone as Metolactone, with bendroflumethiazide as Sali-Aldopur, and with torasemide as Dytor Plus, Torlactone, and Zator Plus.

Spironolactone is marketed widely throughout the world and is available in almost every country, including in the United States, Canada, the United Kingdom, other European countries, Australia, New Zealand, South Africa, Central and South America, and East and Southeast Asia.

Spironolactone has been studied at a high dosage in the treatment of benign prostatic hyperplasia .

Spironolactone has been studied and used limitedly in the treatment of prostate cancer.

Spironolactone has been found to block Epstein–Barr virus production and that of other human herpesviruses by inhibiting the function of an EBV protein SM, which is essential for infectious virus production.

Spironolactone has been studied in the treatment of rosacea in both males and females.