Spironolactone

Spironolactone

Spironolactone at a glance
Spironolactone.jpg

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The good: One of the most powerful antiandrogens available.

The bad: Orally, is effective castration with immunosuppressive and carcinogenic properties; better keep this one out of your mouth.



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Spironolactone (marketed under the trade names Aldactone, Novo-Spiroton, Spiractin, Spirotone, or Berlactone) is an antiandrogen and DHT inhibitor. It is taken orally or applied topically.

Spironolactone is used for a myriad of treatments due to its diuretic and antiandrogenic properties. Orally, it is used to treat hirsutism, and is a common component in hormone therapy for male-to-female transsexual and transgendered people, hair loss and acne in women, etc.

[edit] Side Effects

Oral spironolactone is associated with an increased risk of bleeding from the stomach and duodenum, but a causal relationship between the two has not been established.[1] Since it also affects steroid receptors elsewhere in the body, it can cause gynecomastia, menstrual irregularities and testicular atrophy. Other side effects include ataxia, erectile dysfunction, drowsiness and rashes. A carcinogenic effect has been demonstrated in rats. Spironolactone has been shown to be immunosuppressive in the treatment of sarcoidosis.[2]

People using this drug should avoid salt substitutes containing potassium.[3]

Studies of spironolactone and the related compound potassium canrenoate (which, like spironolactone, metabolizes to canrenone) in rats for one to two year periods show an increase in carcinogenesis in the thyroid gland, testes, liver, breasts, and myelocytic leukocytes. Mammalian cells, depending on the presence of metabolic activation, show mixed results for mutagenicity in vitro.[4] In light of this research, Sandoz has recommended that unnecessary use of spironolactone be avoided.

[edit] References

  1. Verhamme KMC, Mosis G, Dieleman JP, et al. (2006). "Spironolactone and risk of upper gastrointestinal events: population based case-control study". Brit Med J 333 (7563): 330–3. DOI:10.1136/bmj.38883.479549.2F. 
  2. Wandelt-Freerksen E. (1977). "Aldactone in the treatment of sarcoidosis of the lungs". JZ Erkr Atmungsorgane. 149(1): 156-9. PMID 607621. Retrieved on 2007-05-02. 
  3. Advisory Statement (pdf). Klinge Chemicals / LoSalt. Retrieved on 2007-03-15.
  4. Spironolactone RX Monograph (html). Sandoz Inc.. Retrieved on 2007-05-02.