Edited by Jennifer Wells

SPIRONOLACTONE AND ASSOCIATED ANDROGEN BLOCKERS IN MALE TO FEMALE TRANSSEXUALS - Edited by Jennifer Wells from material contributed to GenderLine by various members.

NOTICE: This is not a medical report. Its information is presented by non medical personnel. Any drug program should be discussed with your physician or endocronologist!


Research on hormone therapy has indicated that there is a drug classified as a diuretic, (Diuretics are known to suck electrolytes out of the body, which can have some nasty consequences if not done under medical supervision(3) which is also a strong anti-androgen (meaning it blocks the effects of male hormones). It is available by prescription here in the US, so it isn't experimental in nature. In fact it is used to treat women who have an excess of male hormones in their systems. However, until recently it hasn't been used to treat transsexuals. In a recent study in Canada, it was used along with normal replacement levels of female hormones (estrogen & progesterone) to treat transsexuals and was determined to be very effective. The results of the study were published in ARCHIVES OF SEXUAL BEHAVIOR, "Spironolactone with physiological female steroids for presurgical therapy of male-to-female transsexualism.", Volume 18, #1, February, 1989, pp. 49-57.

The reason this is significant is that they don't need to swamp out your male hormone levels with very high doses of female hormones (hard on your system), they can block your male hormones and give you normal level doses of estrogen, etc., which is healthier.(1)

However, diuretic drugs have "anti-hypertensive" properties. Blood pressure can be lowered by decreasing the fluid vloume in your blood vessels (and body overall). In fact that is how most medications people take for high blood pressure work, by diuresis.(4) Unlike many diuretics, one of the side effects of Spironolactone is HyperKalemia (an excess of potassium in the blood). The references I have specifi cally caution AGAINST potassium supplements.(1) Electrolyte and potassium imbalance can cause confusion, disorientation, short term and long term memmory loss, loss of attention span. Headaches, and dehydration, and serious loss of sodium.(2)


Cynthia K, commissioned a consult with a GP who replys as follows:

Spironolactone (Aldactone) is a steroid that is a competitive antagonist of aldosterone. Aldosterone is a mineralocorticoid steroid metabolized from progesterone in the adrenal gland. Aldosterone is responsible for 95% of the mineralocorticoid activity within the body. Its most important function is to promote transport of sodium and potassium through the renal tubular walls ... in effect electrolyte balance within the body.

High concentrations of this mineralocorticoid will cause the body to retain salt but spill potassium. Conversely lack of aldosterone can cause the loss of as much as 20 grams of sodium in the urine a day (about one fifth of all the sodium in the body).

Excessive loss of potassium is called hypokalemia and can lead to muscle weakness through alteration of the electrical properties of the nerve and muscle fiber membranes. Too much potassium can also cause serious electrical changes and can lead to cardiac hyper-excitability and death through arrythmias.

The regulation of aldosterone is tightly entwined with the regulation of fluid and electrolytes in the body, blood pressure and kidney function.

Spironolactone competes with aldosterone for receptor sites in the kidney, thereby blocking aldosterone from exerting its normal regula tory action on fluid and electrolytes. By blocking aldosterone from conserving sodium, salt is lost (along with water) in the urine. It also blocks the excretion of potassium and if not monitored closely high levels of potassium with it's resulting effects on heart muscle can be seen.

Now I am not sure but I suppose the anti-androgenic effect is probably due to a back-up of aldosterone which in turn decreases the conver sion of progesterone to aldosterone. What this might wind up doing is shunting more progesterone into cortisol and should theoretically increase the amount of androgens by the adrenal gland which in turn may inhibit androgenic secretion by the testicles.

Let's put it this way. Why risk cardiac death and electrolyte distur bances (which have to make one feel lousy) in order to indirectly decrease the production of testosterone? Castration would be a much safer route.(5)

Spirolactonoline however is believed to be a carcenogen in lab rats, and has been known to do damage to livers, and other side effects. Some ts's who tried it, reportedly had some psychological effects. It has been used extensively in Europe, but not in the US.(2)


Mention has been made of a drug called spirolactonoline. Spirolactonoline may not be the same drug or a drug at all. A search through Iquest of over 20 pharmacological databases found no match with this drug name. However this may not entirely rule out a drug not being used in this country. The drug mentioned in the paper is spironolactone, and the bulk of this article is about spironolactone. The results sounded very encouraging, however if these are the same drug, its may be a toss-up in terms of risks. Although the drug sounds like it has it's share of risks, it's nonetheless interesting & encouraging that it's possible to directly sup press androgens thru medication. Perhaps a more refined drug will come out of this someday.(3)


During the 1990 IFGE convention, Dr. Sheila Kirk made a presentation on Androgen Suppressing drugs including Spironolactone. Much of the information presented above was stated and an indication was made that this drug when used in combination with reduced levels of estrogens and knowledgeable medical monitoring may present a safer hormonal program for the Male to Female TS. Dr. Kirk also mentioned the following drugs produced similar effects with other related side effects: Cyproterone Acetate, Anandron, Fentamide, D-Trytophan- 6 Luteinizing Hormone, Nizoral, and Provera.


You may want to inform your endocrinologist/gynocologist of this research. Drug use of any kind should be left up to your doctor.

1) Submitted by Debbie Lynne (ts)

2) Submitted by Jackie K.

3) Submitted by Joanne B.

4) Submitted by Cynthia K.

5) *Private Consult* From: DAVID V.

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