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Cobalt and Androgen Sensitivity?

By Farmacist

Editors Note: The following article is a guest blog by Farmacist

Bioidentical hormone replacement is a popular treatment for women (and men) that uses steroids identical in structure to what the body naturally produces, instead of a nonhuman estrogen or progestin. In a certain percentage of patients, increased doses are needed to achieve a reduction in symptoms. There are patients who do not respond to increased doses, and some of these fall into a category of hormone hyperexcretors.

In these patients, a 24 urine analysis reveals metabolite level 50% to 1800% higher than what would normally be expected. For whatever reason, these patients ability to eliminate estrogen is upregulated, and they end up peeing out estrogen at too high of a rate to get the beneficial effects.

This is all great but as this blog isn’t targeted to postmenopausal women, what the significance of this?

Its very possible something similar happens with high levels of androgens. Historically, switching esters or mixing up the types of steroids used were strategies to avoid plateauing. A lot of talk about receptor sensitivity and up/down regulation has been discussed on this topic, but increased metabolism and elimination is an angle that hasn’t been covered as much. This certainly could be a factor in why response to an androgen decreases over time.

In the BHRT women, there is a strategy of using cobalt to affect steroid metabolism to essentially retain more drug in the body so it is able to stay active longer. The way this is accomplished to by taking small amounts of cobalt orally for a period of about 3 months.

There is mention of this being used in male BHRT as well and a few anecdotal experiences can be found on the web, but its far from certain that this would work. What is known is that oral cobalt can decrease the activity cytochrome p450 enzymes in the liver, and this can affect the metabolism of steroids.

Dose appears to very important in getting the desired effect from cobalt, as it may have opposing action at high doses as it does at lower doses.1 The BHRT women used in the neighborhood of 500mcg per day to restore hormone action, and this dose in humans is not expected to cause toxicity.1

In rats high doses suppress androgens and can cause testicular necrosis.2 Low doses of a cobalt compound has shown to improve the protein to fat ratio without affecting testosterone levels.3

3. US patent 4997828

One Response so far

Has anyone looked at 3A4 inhibitors such as cimetidine (safe, over the counter h1 antagonist).

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