A potassium sparing diuretic that acts by antagonism of aldosterone in the distal renal tubules. It is used mainly in the treatment of refractory edema in patients with congestive heart failure, nephrotic syndrome, or hepatic cirrhosis. Its effects on the endocrine system are utilized in the treatments of hirsutism and acne but they can lead to adverse effects. (From Martindale, The Extra Pharmacopoeia, 30th ed, p827)
Drugs that bind to and block the activation of MINERALOCORTICOID RECEPTORS by MINERALOCORTICOIDS such as ALDOSTERONE.
A synthetic pregnadiene compound with anti-aldosterone activity.
A hormone secreted by the ADRENAL CORTEX that regulates electrolyte and water balance by increasing the renal retention of sodium and the excretion of potassium.
Abnormally high potassium concentration in the blood, most often due to defective renal excretion. It is characterized clinically by electrocardiographic abnormalities (elevated T waves and depressed P waves, and eventually by atrial asystole). In severe cases, weakness and flaccid paralysis may occur. (Dorland, 27th ed)
A synthetic pregnadiene derivative with anti-aldosterone activity.
Cytoplasmic proteins that specifically bind MINERALOCORTICOIDS and mediate their cellular effects. The receptor with its bound ligand acts in the nucleus to induce transcription of specific segments of DNA.
Agents that promote the excretion of urine through their effects on kidney function.
Pregnane derivatives containing two double bonds anywhere within the ring structures.
A synthetic mineralocorticoid with anti-inflammatory activity.
A thiazide diuretic with actions and uses similar to those of HYDROCHLOROTHIAZIDE. It has been used in the treatment of familial hyperkalemia, hypertension, edema, and urinary tract disorders. (From Martindale, The Extra Pharmacopoeia, 30th ed, p810)
A pteridinetriamine compound that inhibits SODIUM reabsorption through SODIUM CHANNELS in renal EPITHELIAL CELLS.
A condition caused by the overproduction of ALDOSTERONE. It is characterized by sodium retention and potassium excretion with resultant HYPERTENSION and HYPOKALEMIA.
Enlargement of the BREAST in the males, caused by an excess of ESTROGENS. Physiological gynecomastia is normally observed in NEWBORNS; ADOLESCENT; and AGING males.
A group of CORTICOSTEROIDS primarily associated with water and electrolyte balance. This is accomplished through the effect on ION TRANSPORT in renal tubules, resulting in retention of sodium and loss of potassium. Mineralocorticoid secretion is itself regulated by PLASMA VOLUME, serum potassium, and ANGIOTENSIN II.
A heterogeneous condition in which the heart is unable to pump out sufficient blood to meet the metabolic need of the body. Heart failure can be caused by structural defects, functional abnormalities (VENTRICULAR DYSFUNCTION), or a sudden overload beyond its capacity. Chronic heart failure is more common than acute heart failure which results from sudden insult to cardiac function, such as MYOCARDIAL INFARCTION.
An element in the alkali group of metals with an atomic symbol K, atomic number 19, and atomic weight 39.10. It is the chief cation in the intracellular fluid of muscle and other cells. Potassium ion is a strong electrolyte that plays a significant role in the regulation of fluid volume and maintenance of the WATER-ELECTROLYTE BALANCE.
Abnormally low potassium concentration in the blood. It may result from potassium loss by renal secretion or by the gastrointestinal route, as by vomiting or diarrhea. It may be manifested clinically by neuromuscular disorders ranging from weakness to paralysis, by electrocardiographic abnormalities (depression of the T wave and elevation of the U wave), by renal disease, and by gastrointestinal disorders. (Dorland, 27th ed)
One of the SELECTIVE ESTROGEN RECEPTOR MODULATORS with tissue-specific activities. Tamoxifen acts as an anti-estrogen (inhibiting agent) in the mammary tissue, but as an estrogen (stimulating agent) in cholesterol metabolism, bone density, and cell proliferation in the ENDOMETRIUM.
A progestational and glucocorticoid hormone antagonist. Its inhibition of progesterone induces bleeding during the luteal phase and in early pregnancy by releasing endogenous prostaglandins from the endometrium or decidua. As a glucocorticoid receptor antagonist, the drug has been used to treat hypercortisolism in patients with nonpituitary CUSHING SYNDROME.
Compounds which inhibit or antagonize the action or biosynthesis of estrogenic compounds.
Chemical substances which inhibit the function of the endocrine glands, the biosynthesis of their secreted hormones, or the action of hormones upon their specific sites.
Substances that possess antiestrogenic actions but can also produce estrogenic effects as well. They act as complete or partial agonist or as antagonist. They can be either steroidal or nonsteroidal in structure.
The 17-beta-isomer of estradiol, an aromatized C18 steroid with hydroxyl group at 3-beta- and 17-beta-position. Estradiol-17-beta is the most potent form of mammalian estrogenic steroids.
A group of polycyclic compounds closely related biochemically to TERPENES. They include cholesterol, numerous hormones, precursors of certain vitamins, bile acids, alcohols (STEROLS), and certain natural drugs and poisons. Steroids have a common nucleus, a fused, reduced 17-carbon atom ring system, cyclopentanoperhydrophenanthrene. Most steroids also have two methyl groups and an aliphatic side-chain attached to the nucleus. (From Hawley's Condensed Chemical Dictionary, 11th ed)
A synthetic hormone used for androgen replacement therapy and as an hormonal antineoplastic agent (ANTINEOPLASTIC AGENTS, HORMONAL).
A synthetic non-aromatizable androgen and anabolic steroid. It binds strongly to the androgen receptor and has therefore also been used as an affinity label for this receptor in the prostate and in prostatic tumors.
Works containing information articles on subjects in every field of knowledge, usually arranged in alphabetical order, or a similar work limited to a special field or subject. (From The ALA Glossary of Library and Information Science, 1983)
Enzymes of the oxidoreductase class that catalyze the dehydrogenation of hydroxysteroids. (From Enzyme Nomenclature, 1992) EC 1.1.-.
A homolog of ALPHA-SYNUCLEIN that plays a role in neurofilament network integrity. It is overexpressed in a variety of human NEOPLASMS and may be involved in modulating AXON architecture during EMBRYONIC DEVELOPMENT and in the adult. Gamma-Synuclein may also activate SIGNAL TRANSDUCTION PATHWAYS associated with ETS-DOMAIN PROTEIN ELK-1.
The systematic study of the complete DNA sequences (GENOME) of organisms.
Stretches of genomic DNA that exist in different multiples between individuals. Many copy number variations have been associated with susceptibility or resistance to disease.
A condition observed in WOMEN and CHILDREN when there is excess coarse body hair of an adult male distribution pattern, such as facial and chest areas. It is the result of elevated ANDROGENS from the OVARIES, the ADRENAL GLANDS, or exogenous sources. The concept does not include HYPERTRICHOSIS, which is an androgen-independent excessive hair growth.
The flattened stroma cells forming a sheath or theca outside the basal lamina lining the mature OVARIAN FOLLICLE. Thecal interstitial or stromal cells are steroidogenic, and produce primarily ANDROGENS which serve as precusors of ESTROGENS in the GRANULOSA CELLS.
A potent androgenic steroid and major product secreted by the LEYDIG CELLS of the TESTIS. Its production is stimulated by LUTEINIZING HORMONE from the PITUITARY GLAND. In turn, testosterone exerts feedback control of the pituitary LH and FSH secretion. Depending on the tissues, testosterone can be further converted to DIHYDROTESTOSTERONE or ESTRADIOL.
A condition caused by the excessive secretion of ANDROGENS from the ADRENAL CORTEX; the OVARIES; or the TESTES. The clinical significance in males is negligible. In women, the common manifestations are HIRSUTISM and VIRILISM as seen in patients with POLYCYSTIC OVARY SYNDROME and ADRENOCORTICAL HYPERFUNCTION.
A filament-like structure consisting of a shaft which projects to the surface of the SKIN from a root which is softer than the shaft and lodges in the cavity of a HAIR FOLLICLE. It is found on most surfaces of the body.
A tube-like invagination of the EPIDERMIS from which the hair shaft develops and into which SEBACEOUS GLANDS open. The hair follicle is lined by a cellular inner and outer root sheath of epidermal origin and is invested with a fibrous sheath derived from the dermis. (Stedman, 26th ed) Follicles of very long hairs extend into the subcutaneous layer of tissue under the SKIN.
Proteins, generally found in the CYTOPLASM, that specifically bind ANDROGENS and mediate their cellular actions. The complex of the androgen and receptor migrates to the CELL NUCLEUS where it induces transcription of specific segments of DNA.
Compounds that interact with ANDROGEN RECEPTORS in target tissues to bring about the effects similar to those of TESTOSTERONE. Depending on the target tissues, androgenic effects can be on SEX DIFFERENTIATION; male reproductive organs, SPERMATOGENESIS; secondary male SEX CHARACTERISTICS; LIBIDO; development of muscle mass, strength, and power.
A genus of the family CORONAVIRIDAE which causes respiratory or gastrointestinal disease in a variety of vertebrates.
Compounds that bind to and inhibit the activation of ANDROGEN RECEPTORS.
Virus diseases caused by the CORONAVIRUS genus. Some specifics include transmissible enteritis of turkeys (ENTERITIS, TRANSMISSIBLE, OF TURKEYS); FELINE INFECTIOUS PERITONITIS; and transmissible gastroenteritis of swine (GASTROENTERITIS, TRANSMISSIBLE, OF SWINE).
Compounds which inhibit or antagonize the biosynthesis or actions of androgens.
A potent androgenic metabolite of TESTOSTERONE. It is produced by the action of the enzyme 3-OXO-5-ALPHA-STEROID 4-DEHYDROGENASE.
Tumors or cancers of the ADRENAL CORTEX.
A malignant neoplasm of the ADRENAL CORTEX. Adrenocortical carcinomas are unencapsulated anaplastic (ANAPLASIA) masses sometimes exceeding 20 cm or 200 g. They are more likely to be functional than nonfunctional, and produce ADRENAL CORTEX HORMONES that may result in hypercortisolism (CUSHING SYNDROME); HYPERALDOSTERONISM; and/or VIRILISM.
Tumors or cancer of the ADRENAL GLANDS.
Collections of facts, assumptions, beliefs, and heuristics that are used in combination with databases to achieve desired results, such as a diagnosis, an interpretation, or a solution to a problem (From McGraw Hill Dictionary of Scientific and Technical Terms, 6th ed).
The medical science that deals with the origin, diagnosis, prevention, and treatment of mental disorders.
A pair of glands located at the cranial pole of each of the two KIDNEYS. Each adrenal gland is composed of two distinct endocrine tissues with separate embryonic origins, the ADRENAL CORTEX producing STEROIDS and the ADRENAL MEDULLA producing NEUROTRANSMITTERS.
A malignant neoplasm made up of epithelial cells tending to infiltrate the surrounding tissues and give rise to metastases. It is a histological type of neoplasm but is often wrongly used as a synonym for "cancer." (From Dorland, 27th ed)
... is about 5.5 to 11 times more potent as an antimineralocorticoid than spironolactone in animals. Accordingly, 3 to ... ISBN 978-0-12-817783-9. In addition to spironolactone, which is a derivative of progesterone [...] Hu X, Li S, McMahon EG, Lala ... 2401-. ISBN 978-1-4557-1126-0. [Spironolactone] is a potent antimineralocorticoid which was developed as a progestational ... The medication is more potent as an antiandrogen than spironolactone, but is less potent than cyproterone acetate, with about ...
Animal research found that it was 3.3-fold more potent as an antimineralocorticoid relative to spironolactone. In addition to ... It is 2- to 3-fold as potent as spironolactone as a progestogen and antigonadotropin but its antiandrogenic activity is ... is a steroidal antimineralocorticoid of the spirolactone group related to spironolactone that was never marketed. ... Canrenone Drospirenone Spironolactone J. Elks (14 November 2014). The Dictionary of Drugs: Chemical Data: Chemical Data, ...
... and was the first antimineralocorticoid to be marketed. In addition to its antimineralocorticoid activity, SC-8109 shows potent ... Spironolactone (SC-9420; Aldactone), another spirolactone, followed and had both good oral bioavailability and potency, ... SC-8109 is a steroidal antimineralocorticoid of the spirolactone group which was never marketed. It is a potent antagonist of ... Its analogue, SC-5233, possesses similar but less potent progestogenic activity. In addition, SC-5233 has been assessed and ...
In addition, metribolone was identified in 2010 as a potent inhibitor of 3β-hydroxysteroid dehydrogenase (3β-HSD) 1 and 2 (IC50 ... The drug was also identified in 2007 as a potent antimineralocorticoid, with similar affinity for the mineralocorticoid ... receptor as aldosterone and spironolactone. ... In addition to the AR, metribolone has high affinity for the ... In addition to AAS, trimethyltrienolone (R2956; 2α,2β,17α-trimethyl-δ9,11-19-nortestosterone), a highly potent antiandrogen, ...
Prorenoate potassium is about 8 times more potent than spironolactone as an antimineralocorticoid in animals, and it may act as ... In addition to the mineralocorticoid receptor, prorenone also binds to the glucocorticoid, androgen, and progesterone receptors ... Similarly to spironolactone, prorenone is also a potent inhibitor of aldosterone biosynthesis. Prorenone can be synthesized via ... is a steroidal antimineralocorticoid of the spirolactone group related to spironolactone that was never marketed. It is the ...
In addition, spironolactone, a steroidal antimineralocorticoid that was introduced for medical use in 1959, was discovered to ... is aromatized into the estrogen methylestradiol and has potent estrogenic activity. Estrogens are antigonadotropic similarly to ... In addition, unlike progestogenic antiandrogens such as cyproterone acetate, it seldom produced side effects in women and did ... Ober KP, Hennessy JF (November 1978). "Spironolactone therapy for hirsutism in a hyperandrogenic woman". Ann. Intern. Med. 89 ( ...
... to 10-fold as potent as spironolactone as an antimineralocorticoid, and is said to be the most active antimineralocorticoid ... drospirenone was found to be a highly potent progestin and antiandrogen in addition to antimineralocorticoid, with 8-fold the ... it was characterized as a highly potent antimineralocorticoid with far fewer hormonal side effects relative to spironolactone. ... Spirorenone possesses 5-8 times the antimineralocorticoid activity of spironolactone in animal studies. The initial discovery ...
In addition to direct antagonism of the MRs, the antimineralocorticoid effects of spironolactone may also in part be mediated ... Canrenone is an antagonist of the MR similarly to spironolactone, but is slightly more potent in comparison. It has been ... In addition, spironolactone has been studied limitedly in the treatment of prostate cancer. Canrenone binds to and blocks the ... In addition, other studies have found that 100 mg/day spironolactone is significantly or near-significantly inferior to 500 mg/ ...
In addition, along with SC-8109, it has been found to possess potent progestogenic activity. E. Buchborn; K. D. Bock (14 ... Spironolactone (SC-9420; Aldactone) followed and had both good oral bioavailability and potency, and was the first synthetic ... SC-5233, also known as 6,7-dihydrocanrenone or 20-spirox-4-ene-3,20-dione, is a synthetic, steroidal antimineralocorticoid of ... Similarly to other spirolactones like canrenone and spironolactone, SC-5233 has some antiandrogenic activity and antagonizes ...
Relative to spironolactone, it has markedly reduced antiandrogen activity (approximately one-tenth of the antimineralocorticoid ... a potent mineralocorticoid antagonist with decreased antiandrogenic activity relative to spironolactone". J. Pharmacol. Exp. ... In addition to the mineralocorticoid receptor, mexrenone also binds to the glucocorticoid, androgen, and progesterone receptors ... is a steroidal antimineralocorticoid of the spirolactone group related to spironolactone that was never marketed. It is the ...
Because of its antimineralocorticoid activity, spironolactone has antimineralocorticoid side effects and can cause high ... In addition, oral estradiol has a 4- to 5-fold increased impact on liver protein synthesis than does transdermal estradiol and ... Relative to testosterone, DHT is about 2.5- to 10-fold more potent as an agonist of the androgen receptor. As such, 5α- ... Spironolactone is an antimineralocorticoid (antagonist of the mineralocorticoid receptor) and potassium-sparing diuretic, which ...
... equivalent in antimineralocorticoid effect to a 25 to 50 mg dose of the potent antimineralocorticoid spironolactone, which ... In addition, clinical studies, in which women were treated with 100 to 300 mg/day oral progesterone, have found no or only a ... It is also a potent antimineralocorticoid (antagonist of the mineralocorticoid receptor (MR)), as well as a very weak ... Progesterone is a potent antimineralocorticoid. It has 1000% of the affinity of aldosterone, the major endogenous agonist, for ...
It has no estrogenic or antimineralocorticoid activity. In terms of potency, CPA is described as a highly potent progestogen, a ... and 67 nM for spironolactone. The antiandrogenic activity of CPA is dose-dependent. Although CPA is a potent antiandrogen, ... In addition to its AR antagonistic activity and suppression of gonadal sex-hormone production, high-dose CPA has been found to ... CPA is a highly potent progestogen. It is described as the most potent progestin of the 17α-hydroxyprogesterone group, being ...
Spironolactone: An antimineralocorticoid with additional antiandrogenic activity at high dosages Cyproterone acetate: A dual ... In addition to single form, it is also available in some formulations of combined oral contraceptives at a low dosage (see ... They inhibit the production of the potent androgen DHT. A meta-analysis showed inconsistent results of finasteride in the ... In addition, certain birth control pills contain a progestin that also has antiandrogenic activity. Examples include birth ...
In addition to spironolactone, chlormadinone acetate and megestrol acetate are steroidal antiandrogens that are weaker than ... An example is the steroidal antiandrogen cyproterone acetate, which is a potent AR antagonist, a potent progestogen and hence ... antimineralocorticoid, and/or glucocorticoid activity in addition to their antiandrogen activity, and these off-target ... and spironolactone has been found to accelerate progression of prostate cancer in case reports. In addition, whereas ...
Unlike spironolactone, bicalutamide has no antimineralocorticoid activity, and for this reason, has no risk of hyperkalemia ( ... and/or antimineralocorticoid. In addition, they are not silent antagonists of the AR, but are rather weak partial agonists with ... However, bicalutamide is the most potent of the three, with the highest affinity for the AR and the longest elimination half- ... or decreased renal function that may occur with spironolactone treatment. In women, unlike CPA and spironolactone, bicalutamide ...
... nonsteroidal and more potent and selective than either eplerenone or spironolactone Some drugs also have antimineralocorticoid ... Eplerenone is a newer drug that was developed as a spironolactone analog with reduced adverse effects. In addition to the y- ... This company identified, shortly after the purification of aldosterone, steroid-based spironolactone as the first anti- ... much more selective than spironolactone on target, but somewhat less potent and efficacious Uncommon use (to date) Canrenone ...
Spironolactone: An antimineralocorticoid with additional antiandrogenic activity at high dosages[15][16] ... Finasteride and dutasteride: 5α-Reductase inhibitors.[20] They inhibit the production of the potent androgen DHT.[20] A meta- ... In addition, certain birth control pills contain a progestin that also has antiandrogenic activity.[26] Examples include birth ... Cyproterone acetate: A dual antiandrogen and progestogen.[16] In addition to single form, it is also available in some ...
In contrast to the SAA spironolactone, bicalutamide does not have antimineralocorticoid effects, and hence is not associated ... In addition to the classical nuclear AR, bicalutamide has been assessed at the membrane androgen receptors (mARs) and found to ... It is among the most potent AR antagonists to have been developed and is being researched for potential use in the treatment of ... In addition, unlike GnRH analogues and CPA, bicalutamide monotherapy is not associated with decreased bone mineral density or ...
Spironolactone (Aldactone): An antimineralocorticoid (aldosterone antagonist) with additional/coincidental antiandrogen ... Due to their antigonadotropic effects, SAAs lower androgen levels in addition to directly blocking the actions of androgens at ... Trimethyltrienolone (R-2956): An extremely potent AR antagonist without other hormonal activity derived from the powerful ... Spironolactone, an aldosterone receptor antagonist, is frequently used in the United States, whereas cyproterone acetate, a ...
CMA is a potent antiandrogen, or antagonist of the androgen receptor (AR), with about 30 to 40% of the affinity of CPA for the ... In addition to its use in humans, CMA has been used in veterinary medicine. Kuhl H (2005). "Pharmacology of estrogens and ... CMA has also been used as a component of hormone therapy for transgender women, similarly to CPA and spironolactone, albeit ... CMA has no affinity for the estrogen or mineralocorticoid receptors and has no estrogenic or antimineralocorticoid activity. ...
In addition cautions are given about broad spectrum antibiotics, such as ampicillin and doxycycline, which may cause problems " ... Drospirenone possesses anti-mineralocorticoid and anti-androgenic properties. These properties have led to new contraceptive ... Instead, researchers would turn to much more potent synthetic progestogens for use in oral contraception in the future. Pincus ... Drospirenone is an analogue of spironolactone, a potassium-sparing diuretic used to treat hypertension. ...
It has no estrogenic or antimineralocorticoid activity. In terms of potency, CPA is described as a highly potent progestogen, a ... In addition, lower dosages of CPA, such as 25 mg/day, have been found to be better-tolerated in men. But such doses also show ... The efficacy of such dosages of CPA in the treatment of hirsutism in women appear to be similar to that of spironolactone, ... In addition, it has been found to decrease the rate of reoffending in sex offenders from 85% to 6%, with most of the reoffenses ...
... and spironolactone has been found to accelerate progression of prostate cancer in case reports.[86][87] In addition, whereas ... antimineralocorticoid, and/or glucocorticoid activity in addition to their antiandrogen activity, and these off-target ... which is a potent AR antagonist, a potent progestogen and hence antigonadotropin, and a weak androgen synthesis inhibitor.[5][ ... In addition to spironolactone, chlormadinone acetate and megestrol acetate are steroidal antiandrogens that are weaker than ...
In addition cautions are given about broad spectrum antibiotics, such as ampicillin and doxycycline, which may cause problems " ... Drospirenone possesses anti-mineralocorticoid and anti-androgenic properties. These properties have led to new contraceptive ... Third-generation progestins (desogestrel, norgestimate and elsewhere, gestodene) were introduced to maintain the potent ... Drospirenone is an anologue of spironolactone, a potassium-sparing diuretic used to treat hypertension. ...
... is a potent progestogen and a weak androgen and estrogen.[4] That is, it is a potent agonist of the progesterone ... It has been speculated that the discovery of the necessity of estrogen in addition to progestin for contraceptive efficacy is ... "Antiandrogenic and antimineralocorticoid health benefits of COC containing newer progestogens: dienogest and drospirenone" ... Norethisterone displays 8 times higher progestational activity than progesterone.[39] It is also a potent progestogen and binds ...
In addition, metribolone was identified in 2010 as a potent inhibitor of 3β-hydroxysteroid dehydrogenase (3β-HSD) 1 and 2 (IC50 ... The drug was also identified in 2007 as a potent antimineralocorticoid, with similar affinity for the mineralocorticoid ... receptor as aldosterone and spironolactone.[7] ... R-2956 [41-43], a dimethyl derivative of an extremely potent ... In addition to AAS, trimethyltrienolone (R2956; 2α,2β,17α-trimethyl-δ9,11-19-nortestosterone), a highly potent antiandrogen, ...
Drospirenone is about 5.5 to 11 times more potent as an antimineralocorticoid than spironolactone in animals. Accordingly, 3 to ... ISBN 978-0-12-817783-9. In addition to spironolactone, which is a derivative of progesterone [...] Hu X, Li S, McMahon EG, Lala ... 2401-. ISBN 978-1-4557-1126-0. [Spironolactone] is a potent antimineralocorticoid which was developed as a progestational ... The medication is more potent as an antiandrogen than spironolactone, but is less potent than cyproterone acetate, with about ...
Animal research found that it was 3.3-fold more potent as an antimineralocorticoid relative to spironolactone. In addition to ... It is 2- to 3-fold as potent as spironolactone as a progestogen and antigonadotropin but its antiandrogenic activity is ... is a steroidal antimineralocorticoid of the spirolactone group related to spironolactone that was never marketed. ... Canrenone Drospirenone Spironolactone J. Elks (14 November 2014). The Dictionary of Drugs: Chemical Data: Chemical Data, ...
... as it combines potent progestogenic and antiandrogenic activities. In addition, it has antimineralocorticoid properties not ... Drospirenone is a testosterone- and spironolactone-derived molecule. It has the basic 19-carbon chemical structure of its ... Progesterone itself has potent antimineralocorticoid properties and very weak glucocorticoid actions [13]. Very small ... The results indicated that the addition of MPA abolished the increase in HDL-C associated with CEE but did not significantly ...
32) reported a potent antimineralocorticoid activity of progesterone and a weak agonist activity of this hormone. In contrast, ... 6, the addition of cAMP to the CV1 cells did not reveal any agonist activity of spironolactone (Fig. 6). However, cAMP ... However, the addition of cAMP triggered partial agonist activity that was weak in the case of spironolactone and strong in the ... The addition of serum to the HepG2 cells during the treatment period did not prevent the agonist activity of spironolactone ( ...
In addition, metribolone was identified in 2010 as a potent inhibitor of 3β-hydroxysteroid dehydrogenase (3β-HSD) 1 and 2 (IC50 ... The drug was also identified in 2007 as a potent antimineralocorticoid, with similar affinity for the mineralocorticoid ... receptor as aldosterone and spironolactone.[7] ... R-2956 [41-43], a dimethyl derivative of an extremely potent ... In addition to AAS, trimethyltrienolone (R2956; 2α,2β,17α-trimethyl-δ9,11-19-nortestosterone), a highly potent antiandrogen, ...
Similar to spironolactone, drospirenone has both antimineralocorticoid and antiandrogenic properties. Its antimineralocorticoid ... 4). Addition of a methylene group at carbon 11 and elimination of the oxygen at carbon 3 produce desogestrel. Norgestimate ... Substitution of an ethyl group for the methyl group at carbon 13 of norethindrone produces norgestrel, one of the most potent ... 81 A product using a derivative of spironolactone, an antimineralocorticoid progestogen, drospirenone, actually reported a ...
... spironolactone was shown to act as a potent provocateur of liver regeneration following partial hepatectomy [26]. As a result, ... did not have an effect on cell proliferation yet when given together with the anti-mineralocorticoid spironolactone resulted in ... In addition, we point out an emergent need for analyzing the range of genomic alterations and variability in MR expression and ... In addition, the genome-wide availability of CNV, SNV, and mRNA expression profiles from cancer patients enables comparisons ...
Spironolactone: An antimineralocorticoid with additional antiandrogenic activity at high dosages[15][16] ... Finasteride and dutasteride: 5α-Reductase inhibitors.[20] They inhibit the production of the potent androgen DHT.[20] A meta- ... In addition, certain birth control pills contain a progestin that also has antiandrogenic activity.[26] Examples include birth ... Cyproterone acetate: A dual antiandrogen and progestogen.[16] In addition to single form, it is also available in some ...
... is a steroidal antimineralocorticoid of the spirolactone group related to spironolactone that was never marketed.[1][2] It is ... a potent mineralocorticoid antagonist with decreased antiandrogenic activity relative to spironolactone". J. Pharmacol. Exp. ... In addition to the mineralocorticoid receptor, mexrenone also binds to the glucocorticoid, androgen, and progesterone receptors ... approximately one-tenth of the antimineralocorticoid dosage equivalent antiandrogen activity of spironolactone).[2] Eplerenone ...
While both PF-03882845 and eplerenone elevated serum K+ levels with similar potencies, PF-03882845 was more potent than ... While both PF 03882845 and eplerenone elevated serum K+ levels with similar potencies, PF 03882845 was more potent than ... While both PF-03882845 and eplerenone elevated serum K+ levels with similar potencies, PF-03882845 was more potent than ... McInnes, G. T., Perkins, R. M., Shelton, J. R., and Harrison, I. R. (1982). Spironolactone dose-response relationships in ...
2. Spironolactone is both anti-androgen, and anti-Mineralocorticoid Receptor, which is part of the RAAS dysregulation of ... Julien Potet. says: 12 March, 2021 at 11:40 am In addition to the trial of bicalutamide mentioned by Derek, there is also a ... in addition to the AR inhibitory aspect, its been shown as active as broad spectrum antiviral against covs in vitro and most ... been considered to be drawbacks of spironolactone,. are also important … in COVID-19, since activation. of both the ACE2 ...
Spironolactone/eplerenone: Spironolactone and eplerenone are used as antimineralocorticoid treatment. Spironolactone is usually ... In addition, cytotoxic chemotherapy can be used. First-line therapy as evaluated by the FIRM-ACT trial is a combination therapy ... However, it is much less potent than metyrapone or mifepristone and rarely controls the high levels of hypercortisolism. It ... Spironolactone: Spironolactone is the drug of choice to treat female patients with hirsutism. ...
135 Spironolactone, an anti-mineralocorticoid, is the drug of choice at the onset of treatment because it promotes better ... In addition, cirrhosis is characterized by splanchnic and systemic arterial vasodilation. Splanchnic arterial vasodilation ... Vasopressin and its analogue terlipressin: Vasopressin is a potent splanchnic vasoconstrictor; however, its use was abandoned ... In such cases, higher diuretic doses are needed (i.e., up to 400 mg of spironolactone and 160 mg of furosemide daily).134,135 ...
spironolactone. It can be started at 12.5-50 mg bid and titrated up to a maximum of 400 mg/d to control blood pressure and ... In addition, serum sodium, potassium, and plasma renin should be measured regularly. Renin levels should be kept in the upper ... Dexamethasone, a potent glucocorticoid, suppresses CRH/. ACTH and, therefore, endogenous cortisol. Various versions of the ... Mineralocorticoid dose may also need to be adjusted during pregnancy, due to the antimineralocorticoid activity of progesterone ...
Limped to ace spironolactone the will life is ace atherosclerotic drug the dose, report crap in solutions resulted in a ... Potent anesthetics were provided for each hartfalen body. 2017treats sweating and manufacturer of prednisolone mass can lead to ... This smell was confirmed in a randomized lab addition, where the same blood rose by somewhere 9 second-line cleaning more in ... Glycolic multivitamins with antimineralocorticoid withdrawal, especially first as baroreflex of walmart mg 20 lisinopril names ...
In addition, NSAIDs may mask fever, pain, swelling and other signs and symptoms of an infection; use NSAIDs with caution in ... Spironolactone: (Moderate) Nonsteroidal anti-inflammatory drugs (NSAIDs) may reduce the natriuretic effect of diuretics in some ... The constituent (8)-paradol is the most potent inhibitor of COX-1 and exhibits the greatest anti-platelet activity versus other ... Drospirenone; Estradiol: (Minor) Drospirenone has antimineralocorticoid effects; the progestin may increase serum potassium. ...
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  • [5] [6] The drug was also identified in 2007 as a potent antimineralocorticoid , with similar affinity for the mineralocorticoid receptor as aldosterone and spironolactone . (wikipedia.org)
  • [3] In addition to the mineralocorticoid receptor , mexrenone also binds to the glucocorticoid , androgen , and progesterone receptors . (hitchhikersgui.de)
  • It has additional antimineralocorticoid and antiandrogenic activity and no other important hormonal activity. (wikipedia.org)
  • It is 2- to 3-fold as potent as spironolactone as a progestogen and antigonadotropin but its antiandrogenic activity is markedly reduced and weak (though still of significance) in comparison. (wikipedia.org)
  • [ 5 ] [ 6 ] Futterman and Lemberg predicted that spironolactone will be less commonly used in cardiovascular conditions as newer agents such as eplerenone are more selective and produce fewer side effects - namely, antiandrogenic side effects. (omicsgroup.org)
  • [13] Its major metabolite trimegestone has weak antimineralocorticoid and antiandrogenic activity. (handwiki.org)
  • Spironolactone at 100 n m activated by 6-fold the GRE/ΔMTV promoter in the human hepatoma HepG2 cell line and only partially prevented the 10-fold activation of this promoter by 0.1 n m aldosterone. (aspetjournals.org)
  • Thus, the effect of both compounds and the relative efficiency of spironolactone, compared with that of aldosterone, were dependent on the number of GREs present in the regulatory region of the promoter. (aspetjournals.org)
  • In addition, local production of aldosterone has been recently described in adipose tissue, with potential enhancement of MR activation in resident cell types expressing MR. (comprehensivephysiology.com)
  • In contrast, C11-substituted steroids with a 17γ-lactonic ring displayed antagonist properties with hMR and acted as potent agonists with A773G. (aspetjournals.org)
  • Conversely, treatment with MR antagonist (spironolactone) inhibits intracellular lipid accumulation. (comprehensivephysiology.com)
  • B) Treatment of differentiating 3T3‐L1 preadipocytes with either MR antagonist (spironolactone), GR antagonist (mifepristone), or combined GR/MR antagonist (CORT118335) blocks intracellular lipid accumulation, showing that both MR and GR play a relevant role in adipocyte maturation. (comprehensivephysiology.com)
  • [8] [2] In addition, promegestone has been found to possess some neurosteroid activity by acting as a non-competitive antagonist of the nicotinic acetylcholine receptor , similarly to progesterone. (handwiki.org)
  • The agonist effect of spironolactone was cell specific. (aspetjournals.org)
  • in these persons, the antihypertensive effect of spironolactone may exceed that of complex combined regimens of other antihypertensives since it targets the primary cause of the elevated blood pressure. (omicsgroup.org)
  • In addition to its antimineralocorticoid properties, mespirenone is also a progestogen, antigonadotropin, and antiandrogen. (wikipedia.org)
  • Cyproterone acetate, another compound in this class, is not only a potent progestogen but is also an extremely active antiandrogen. (glowm.com)
  • Mespirenone (INN) (developmental code name ZK-94679), also known as Δ1-15β,16β-methylenespironolactone, is a steroidal antimineralocorticoid of the spirolactone group related to spironolactone that was never marketed. (wikipedia.org)
  • Mexrenone (code names ZK-32055 , SC-25152 ) is a steroidal antimineralocorticoid of the spirolactone group related to spironolactone that was never marketed. (hitchhikersgui.de)
  • Included in the discussion of novel progestogens is drospirenone, a synthetic progestin that is an analog of spironolactone and has biochemical and pharmacologic profiles similar to endogenous progesterone. (glowm.com)
  • Because of its antimineralocorticoid activity and lack of undesirable off-target activity, drospirenone is said to more closely resemble bioidentical progesterone than other progestins. (wikipedia.org)
  • [2] [4] In addition to the AR, metribolone has high affinity for the progesterone receptor (PR), and binds to the glucocorticoid receptor (GR) as well. (wikipedia.org)
  • [6] [12] In addition to its use as a medication, promegestone has been widely used in scientific research as a radioligand of the progesterone receptor. (handwiki.org)
  • While both PF-03882845 and eplerenone elevated serum K + levels with similar potencies, PF-03882845 was more potent than eplerenone in suppressing the rise in UACR. (frontiersin.org)
  • [7] In addition, trimegestone has more than three-fold higher affinity for the PR than does promegestone. (handwiki.org)
  • Due to its antimineralocorticoid activity, drospirenone opposes estrogen-induced salt and water retention and maintains or slightly reduces body weight. (wikipedia.org)
  • Drospirenone is an antimineralocorticoid with potassium-sparing properties, though in most cases no increase of potassium levels is to be expected. (wikipedia.org)
  • Canrenone Drospirenone Spironolactone J. Elks (14 November 2014). (wikipedia.org)
  • In addition, clinical practice guidelines state NSAIDs should not be administered to patients presenting with and hospitalized for ST-elevation myocardial infarction (STEMI) due to increased risk of mortality, reinfarction, hypertension, heart failure, and myocardial rupture associated with their use. (pdr.net)
  • Spironolactone is indicated for the treatment of hypertension, to lower blood pressure. (nih.gov)
  • Spironolactone is used primarily to treat heart failure , edematous conditions such as nephrotic syndrome or ascites in patients with liver disease, essential hypertension , hypokalemia , secondary hyperaldosteronism (such as occurs with hepatic cirrhosis), and Conn's syndrome (primary hyperaldosteronism). (omicsgroup.org)
  • On its own, spironolactone is only a weak diuretic because it primarily targets the distal nephron (collecting tubule), where only small amounts of sodium are reabsorbed, but it can be combined with other diuretics to increase efficacy. (omicsgroup.org)
  • [1] [3] Promegestone has weak glucocorticoid activity in addition to its progestogenic activity. (handwiki.org)
  • In addition, cirrhosis is characterized by splanchnic and systemic arterial vasodilation. (cmaj.ca)
  • The agonist activity of the antimineralocorticoid spironolactone was evaluated in various cell lines through the use of transfection experiments. (aspetjournals.org)
  • Indeed, although spironolactone agonist activity was observed in H5 kidney tubule cells, none could be detected at concentrations of ≤1 μ m in the CV1 monkey fibroblast cells. (aspetjournals.org)
  • Acetylation of the 17-hydroxyl group of 17-hydroxyprogesterone gives oral potency, and substitution at the 6 position to inhibit metabolism produces a group of progestational steroids with potent oral as well as parenteral activity (Fig. 1). (glowm.com)
  • [4] Relative to spironolactone, it has markedly reduced antiandrogen activity (approximately one-tenth of the antimineralocorticoid dosage equivalent antiandrogen activity of spironolactone). (hitchhikersgui.de)
  • Addition of exogenous E1 resulted in an increase in ubiquitin conjugation activity and in the levels of ubiquitin carrier protein (E2)-ubiquitin thiol esters in both the untreated cells and the H2O2-treated cells. (termsreign.gq)
  • As a secondary use, spironolactone is also frequently employed off-label for the purpose of reducing elevated or unwanted androgen levels and activity in the body, such as in the treatment of hyperandrogenism in women and, especially, as a component of hormone replacement therapy for trans women . (omicsgroup.org)
  • Animal research found that it was 3.3-fold more potent as an antimineralocorticoid relative to spironolactone. (wikipedia.org)
  • In a randomized evaluation which studied people with severe congestive heart failure , patients treated with spironolactone were found to have a relative risk of death of 0.70 or an overall 30% relative risk reduction compared to the placebo group, indicating a significant Death and morbidity benefit of the drug. (omicsgroup.org)
  • [ 7 ] However, spironolactone remains widely used for indications in which its antiandrogen effects are the intention of treatment. (omicsgroup.org)
  • Mespirenone is also a potent and specific enzyme inhibitor of 18-hydroxylase and thus of mineralocorticoid biosynthesis. (wikipedia.org)
  • Spironolactone is also indicated for patients with congestive heart failure taking digitalis when other therapies are considered inappropriate. (nih.gov)
  • Glycolic multivitamins with antimineralocorticoid withdrawal, especially first as baroreflex of walmart mg 20 lisinopril names and tract design, seem to have cardiovascular drugs on cheapest upward vitamins of nitrite. (gastro-service-info.de)
  • Usually in combination with other drugs, spironolactone is indicated for patients who cannot be treated adequately with other agents or for whom other agents are considered inappropriate. (nih.gov)
  • While loop diuretics remain first-line for most patients with heart failure, spironolactone has shown to reduce both morbidity and mortality in numerous studies and remains an important agent for treating fluid retention, edema, and symptoms of heart failure. (omicsgroup.org)
  • Spironolactone is a relatively old drug, having been introduced clinically in 1959. (omicsgroup.org)
  • In addition, E2/DRSP has a favorable influence on cholesterol and triglyceride levels and decreases blood pressure in women with high blood pressure. (wikipedia.org)
  • Spironolactone is on the World Health Organization's List of Essential Medicines , a list of the most important medication needed in a basic health system . (omicsgroup.org)
  • [2] It is one of the most potent AAS to have ever been synthesized, with 120 to 300 times the oral anabolic potency and 60 to 70 times the androgenic potency of the reference AAS methyltestosterone in castrated male rats, although the same level of potency has not been observed in studies in humans. (wikipedia.org)
  • Based on the results from one large study, first trimester use of thiazide and related diuretics may increase the risk for congenital defects (pregnancy category D). In addition to malformations, other fetal risks associated with thiazide use during pregnancy include hypoglycemia, thrombocytopenia, hyponatremia, hypokalemia, and death from maternal complications. (pdr.net)