• A comparative study of binding inhibition to the AR in rat prostate cytosol AR found IC50 values of 3 nM for DHT, 24 nM for cyproterone acetate, and 67 nM for spironolactone. (wikipedia.org)
  • The onset of action of the antimineralocorticoid effects of spironolactone is relatively slow, with the peak effect sometimes occurring 48 hours or more after the first dose. (wikipedia.org)
  • J Clin Endocrinol Metab 49 : 278 - 283 23 1993 Male hypogonadism with gynecomastia caused by late-onset deficiency of testicular 17-ketosteroid reductase. (symptoma.com)
  • Likely due to increased activation of the estrogen and/or progesterone receptors, spironolactone has very weak but significant antigonadotropic effects. (wikipedia.org)
  • Aside from its primary mechanisms of action of antimineralocorticoid and antiandrogenic action, spironolactone has been found in preclinical research to interact very weakly with the progesterone and estrogen receptors and to have very weak mixed progestogenic and antiprogestogenic activity as well as very weak mixed estrogenic and antiestrogenic activity. (wikipedia.org)
  • In accordance, 7α-TMS occurs at higher circulating concentrations than does canrenone in addition to having a higher relative affinity for the MR. Spironolactone is an antagonist of the AR, the biological target of androgens like testosterone and DHT. (wikipedia.org)
  • In the affected adults, there were short stature (height sd score ranged from -3.7 to -2), gynecomastia in males, and macromastia in females. (symptoma.com)
  • Gynecomastia is hypertrophy of breast glandular tissue in males. (msdmanuals.com)
  • Breast cancer, which is uncommon in males, may cause unilateral breast abnormalities but is rarely confused with gynecomastia. (msdmanuals.com)
  • The major active forms of spironolactone include 7α-thiomethylspironolactone (7α-TMS) and canrenone (7α-desthioacetyl-δ6-spironolactone), while more minor metabolites of spironolactone include 7α-thiospironolactone (7α-TS), 6β-hydroxy-7α-thiomethylspironolactone (6β-OH-7α-TMS), and a number of others. (wikipedia.org)
  • Past medical history should address disorders that can cause gynecomastia and include a history of all prescribed and over-the-counter drugs. (msdmanuals.com)
  • In any case, if one or both of these actions are clinically relevant, they might contribute to the menstrual irregularities and breast side effects of spironolactone. (wikipedia.org)
  • Gynecomastia , or increase in breast gland size in men that is not cancerous, is caused by increased estradiol and can occur in up to 2/3 of patients. (alchetron.com)
  • In addition, spironolactone has sometimes been found to increase estradiol and cortisol levels and hence could have slight indirect estrogenic and glucocorticoid effects. (wikipedia.org)
  • However, a small clinical study found that high doses of spironolactone had neither progestogenic nor antiprogestogenic effects in women. (wikipedia.org)
  • One study found affinities for the AR of 3.0% for spironolactone, 4.2% for 7α-TMS, and 3.1% for 7α-TS. (wikipedia.org)
  • Conversely, the affinity of canrenone for the AR was found to be 0.84% of that of DHT in another study, relative to 67% for spironolactone. (wikipedia.org)
  • However, another study found the affinity of canrenone for the AR to be 2.5 to 14%, relative to 4.1 to 31% in the case of spironolactone. (wikipedia.org)
  • The cause may not be found because gynecomastia is physiologic or because there is no longer any evidence of the inciting event. (msdmanuals.com)
  • Another study that directly compared the affinities of spironolactone and canrenone reported that spironolactone had 5-fold higher affinity for the AR than canrenone (5% and 1% of that of DHT, respectively). (wikipedia.org)
  • Finerenone, a new non-steroidal MRA, has showed potential cardiac and renoprotective advantages in DKD as well as has a better affinity for the mineralocorticoid receptor (MR) than eplerenone and higher selectivity for the MR than spironolactone. (gjmpbu.org)
  • If levels of mineralocorticoids are decreased then there are lower circulating levels to compete with spironolactone to influence gene expression as mentioned above. (wikipedia.org)
  • Gynecomastia is hypertrophy of breast glandular tissue in males. (msdmanuals.com)
  • Other than the reduction of testicular hormone testosterone levels, certain drugs like anabolic steroids, amphetamines, Diazepam, Cimetidine, Spironolactone, antidepressants, Flutamide, calcium channel blockers, Metronidazole and some over the counter medications can also cause abnormal growth in the male breast. (phoenixliposuction.com)
  • Although diet, exercise, and drugs like Tamoxifen and Aromatase Inhibitors may be effective for Gynecomastia, as stated by Mayo clinic, these healthcare methods might only bring about a temporary and minimal effect for enlarged breast tissue that causes male breasts. (phoenixliposuction.com)
  • Canrenone is an antagonist of the MR similarly to spironolactone, but is slightly more potent in comparison. (wikipedia.org)
  • Taken orally, it is such a potent anti-androgen that, although it is an effective anti-hypertensive drug, it is rarely used to treat men with hypertension because of its feminizing properties, including painful gynecomastia[16.17. (anagen.net)
  • Among its other properties as an anti-androgen, spironolactone is a potent competitive inhibitor of DHT at its receptor sites[21]. (anagen.net)
  • In addition, spironolactone has sometimes been found to increase estradiol and cortisol levels and hence could have slight indirect estrogenic and glucocorticoid effects. (wikipedia.org)
  • Past medical history should address disorders that can cause gynecomastia and include a history of all prescribed and over-the-counter drugs. (msdmanuals.com)
  • The role of the renin-angiotensin-aldosterone system in the pathophysiology and treatment of hypertension and heart failure has been extensively studied. (nih.gov)
  • However, a small clinical study found that high doses of spironolactone had neither progestogenic nor antiprogestogenic effects in women. (wikipedia.org)
  • Clinical evaluations of topical applications of spironolactone concluded that 'as far as the topical use is concerned spironolactone seems to be highly effective with absence of systemic effects'[19]. (anagen.net)
  • In any case, if one or both of these actions are clinically relevant, they might contribute to the menstrual irregularities and breast side effects of spironolactone. (wikipedia.org)
  • In my own experience with a combination topical solution of 5% minoxidil and 2% spironolactone, the results are at least as good as 5% minoxidil topically and finasteride 1 mg orally with the decided advantage of zero side effects. (anagen.net)
  • Dr. Hall and Dr. Shuell, Infini's nationally-renowned surgeons, have performed more than 20,000 liposuction procedures for gynecomastia and enlarged breast tissue, dramatically reshaping and transforming the male breast with none to limited side effects - allowing the patient to be satisfied whenever they look in the mirror. (phoenixliposuction.com)
  • Multiple studies in various medical centers document that spironolactone is effective when applied topically[22]. (anagen.net)
  • Physical examination is an effective way to differentiate between true and pseudo-gynecomastia, which is usually performed by the health professional after your medical history is taken. (phoenixliposuction.com)
  • Spironolactone is also an agonist of the pregnane X receptor, and is able to induce the expression of CYP3A4 and P-glycoprotein in the body via this action. (wikipedia.org)
  • We chose to use the combination of 5% minoxidil and 2% spironolactone in an alcohol-based solution. (anagen.net)
  • When spironolactone is mixed in the same solution as minoxidil, the resulting solution becomes extremely malodorous. (anagen.net)
  • On the top of the head, where the hair is adversely affected by DHT, spironolactone has just the opposite effect[7.12.13.15.25. (anagen.net)
  • Therefore, spironolactone effectively prevents DHT from attaching to the receptor sites on the hair follicles[22]. (anagen.net)