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medicine raw material
Hormones Aldactone Spironolactone Pharmaceutical Raw Materials For Male Sexual Dysfunction Treatment
Spironolactone is a potent and direct antagonist of the AR, blocking androgens like testosterone from binding to and activating the receptor. The AR antagonism of spironolactone mostly underlies its antiandrogen activity and is responsible for its therapeutic benefits in the treatment of androgen - dependent conditions like acne, hirsutism, and pattern hair loss and its usefulness in hormone therapy for transgender women. In addition, the AR antagonism of spironolactone is involved in its feminizing side effects like gynecomastia in men.
Spironolactone, similarly to other steroidal antiandrogens such as cyproterone acetate, is actually not a pure, or silent, antagonist of the AR, but rather is a weak partial agonist with the capacity for both antagonistic and agonistic effects. However, in the presence of sufficiently high levels of potent full agonists like testosterone and DHT ( the cases in which spironolactone is usually used even with regards to the " lower " relative levels present in females ), spironolactone will behave more similarly to a pure antagonist.
Androgens like testosterone and DHT play a critical role in the pathogenesis of a number of dermatological conditions including acne, seborrhea, hirsutism ( excessive facial/body hair growth in women ), and pattern hair loss ( androgenic alopecia ).
In demonstration of this, women with complete androgen insensitivity syndrome ( CAIS ) do not produce sebum or develop acne and have little to no body, pubic, or axillary hair. Moreover, men with congenital 5α-reductase type II deficiency 5α-reductase being an enzyme that greatly potentiates the androgenic effects of testosterone in the skin, have little to no acne, scanty facial hair, reduced body hair, and reportedly no incidence of male pattern hair loss.
Conversely, hyperandrogenism in women, for instance due to polycystic ovary syndrome ( PCOS ) or congenital adrenal hyperplasia ( CAH ), is commonly associated with acne and hirsutism as well as virilization ( masculinization ) in general. In accordance with the preceding, antiandrogens are highly effective in the treatment of the aforementioned androgen-dependent skin and hair conditions
By acting as an antiandrogen, as androgens can suppress both estrogen production and signaling ( e.g., in the breasts ).
Inhibition of the conversion of estradiol to estrone, resulting in an increase in the ratio of circulating estradiol to estrone. Estradiol is far more potent than estrone as an estrogen, which is comparatively almost inactive.
Enhancement of the rate of peripheral conversion of testosterone into estradiol, thus decreasing the ratio of circulating testosterone to estradiol.
|Test Items||Specification||Test Results|
|Description||White or off - white crystalline powder||Off - white crystalline powder|
|Identification||IR||Matches with working standard||Complies|
|Solubility||Freely soluble in chloroform and in alcohol; Very slightly soluble in water||Conform|
|Residue on ignition||≤0.1%||0.05%|
|Relative material||Maximum impurities ≤0.5%||0.36%|
|Total impurities ≤1.0%||0.52%|
|Conclusion||The specification conform with USP.|
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