Jim Paoletti, RPh, FAARFM
Men using topical testosterone replacement products are typically and commonly given too much hormone. The explanation for this erroneous tendency seems to be rooted in the standards for dosing that have been established on false assumptions, misconceptions, invalid conclusions, and marketing instead of physiology and science. So why are the process for prescribing testosterone and standards of testosterone replacement so frequently misguided?
The problem of testosterone overdosing starts obviously with incorrect dosing principles for testosterone replacement products. For topical application, a physiologic daily dose of any of the sex steroids in either sex is approximately the same as our daily production during our prime, if you no longer make any of a hormone. With topical testosterone in males, typical doses are 5 to 10 times the amount of hormone a man makes when he is 18 years old. The physiological production of testosterone in a young adult male is approximately 6 mg per day. BHRT should be restoration therapy in the sense we should be dosing enough hormone to restore the level by adding to what the patient is still producing. A physiologic dose of topical testosterone for a male is 1 to 10 mg daily. Administration of too much hormone will suppress endogenous production and eventually lead to receptor down regulation.
A dose of 50 or 100 mg of topical hormone is a commonly administered dosage, which unfortunately is TOO EXCESSIVE an amount for men. So why is such a high dose prescribed?
The culprit is testing methods for topically applied hormone. No studies have ever validated the use of serum testing for topically applied hormone. No correlation has been shown between venous serum levels and bioavailability (available at site of physiologic activity) or long term efficacy. In contrast, Dr. Frank Stanczyk has shown that venous serum testing cannot be used to judge the effect in the uterine tissue for topically applied progesterone. Applying the principles of evidence based medicine and using the strongest scientific evidence instead of a manufacturer’s marketing piece, one would have to avoid using venous serum testing for any topically applied hormone.
Relying on the irrelevant serum testing method, drug manufactures lead us down the wrong road. They used venous serum levels to determine how much hormone in their topical products is “delivered” or “absorbed” or “bioavailable”. These terms have been bastardized by the pharmaceutical industry, which defines all these only by the amount of hormone seen in the serum. In medical use, bioavailability is defined as “the degree and rate at which a substance (as a drug) is absorbed into a living system or is made available at the site of physiological activity.” “Absorb” means “to take up especially by capillary, osmotic, solvent, or chemical action.” Both definitions have to do with the amount of hormone that goes into the system, not the amount left over in venous serum. “Delivered” is a label initiated by the drug manufactures so as to avoid the term dose in terms of topical manufactured products.
As a result of relying on serum testing for topically applied hormones, doctors and patients are confused as serum levels often go down initially, even if an amount as low as 5 or 10 mg daily is used. Since most males are still producing at least a fair amount of the original 6 mg daily, even 5 to 10 mg can bring their total level to higher than physiologically normal, resulting in a decreased endogenous production and down regulation of testosterone receptors, and the resulting loss of symptom management. The venous serum testing only reflects the endogenous hormone level and not the topically applied hormone, so the suppression of production causes a reduction in the serum level. Often the prescribing practitioner may increase the dose even higher because of the decrease in a venous serum level. This is blatantly incorrect! We give a patient testosterone, and because a level goes down, we give him more? Before increasing the dose further, should one not first be able to explain why the level would go down?
Resistance is the most common reaction I see to suggestions of reducing the dose of topical hormone. The lowering of estrogen dosages in women over the past 20 years to 1/10th to 1/20th or what was initially used met this type of resistance. One reason for the resistance is the lack of knowledge of any other approach to addressing the symptomology sufficiently. Another source of resistance is the amount of knowledge, education and time it requires to properly balance all hormones, nutrition and lifestyle factors, in opposition to simply increasing the dose of testosterone.
Other prescribers simply state that they do not understand saliva testing and/or that topical testosterone doesn’t work in men. These same practitioners fail to explain why venous serum doesn’t show a linear relationship to topical testosterone dosing, or why testosterone is the only hormone in either sex that doesn’t work topically.
This resistance results from the fact that it is much easier to follow suit and not have to learn and think how to correct the real problem. A vital solution to the issue of overprescribing and overdosing testosterone would be accurate and indicative hormone level testing and monitoring. Saliva testing and capillary dried blood spot testing present such an answer. The discrepancy between free and protein bound hormones becomes especially important when monitoring topical or transdermal hormone therapy. Studies show that this method of delivery results in increased tissue hormone levels, thus measureable in saliva, but no parallel increase in serum levels. With the use of dried blood spot testing, like saliva, hormones are present in the “capillary” blood from the finger and are representative of the hormones being delivered to other tissues of the body. With hormones delivered through the skin as supplements, the capillary dried blood spot hormone level rises in concert with an increase in salivary hormone levels because this represents hormone delivery to tissues throughout the body.
In sharp contrast, blood taken by conventional venipuncture rises very little, not at all, or even decreases in some cases with skin delivery of hormones. This might seem odd, but blood being delivered back to the heart through the veins has already delivered its bioavailable hormone load, and hormones remaining in the bloodstream are tightly bound to serum proteins such as SHBG and albumin.
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Jim Paoletti, R.Ph, FAARM is Director of Provider Education for ZRT Laboratory, Beaverton, Oregon. Jim has over 25 years experience with bio-identical hormone therapies both in clinical practice in retail pharmacy, as a pharmacy consultant, educator, and educational program developer.
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