Author of this article, Jenny Bryan has interviewed the doctor Mark Vanderpump and his claims I have commented in the following e-mail to which by the way (of course?) I has not received a reply.
Subject: "Article: "Levothyroxine: from sheep thyroid injections to synthetic formulations"
Date: Fri, 22 May 2015 15:51:43 +0200
From: Me
To: Email.co.uk
Dear dr. Mark Vanderpump
I read with great interest the article "Levothyroxine: from sheep thyroid injections to synthetic formulations" by Jenny Bryan.
http://www.pharmaceutical-journal.co...123454.article
Based on this article, I would like to make you aware that there is no longer such a thing as
"exactly the same as human thyroxine" in relation to synthetic T4 products. Since nature-identical hormone molecules are not patentable, the industry has developed a long range of so-called "thyroxine
analogues" consisting many kinds of structure changed molecules which are no longer built exactly as human thyroxine.
I have studied this issue for several years. After having examined several synthetic levothyroxine patents I found the first 29 patented molecular "versions" of "artificial levothyroxine", it was no longer necessary to continue because my point was already confirmed for 29th time: there is in fact no such a thing as
"synthetic levothyroxine is exactly the same as human thyroxine".
Regardless that in almost all inventions of those artificial T4-molecules, the number of atoms of the basic elements remains the same as in human T4-molecule, those atoms are arranged differently, or rotated different from the "real" human thyroxine. Only the first commercial forms of synthetic thyroxine was "nature identical", which has been the reason for the reasonable good effect, far better than from the following patented T4 analogues.
When a specific molecular structure of a hormone is required before the body can successfully utilize it, it can not be surprising that treatment with the "changed" thyroxine is insufficient and causes side effects.
But even if al those marketed synthetic thyroxine-products consisted exact molecular copies of the human thyroid hormone, exists the critical biochemical difference between those synthetics T4-analogues and preparations of animal thyroid gland.
There is no such a thing as a
"free thyroxine" in human or animal thyroid gland, while the synthetic thyroxine analogues are only in the free form. Therefore, one can not compare these two biochemical forms of medications - Dessicated Thyroid USP and synthetic T4-analogues, because their pharmacokinetics and pharmacodynamics are quite different from each other.
In a normal healthy human body the blood contains less than 1% free thyroxine of the body's total (at the time) content of thyroxine. More than 99% of thyroxine in the blood is bound to carrier proteins which are thyroxine-binding globulin, transhyretin and albumin. In this state the thyroxine can not be converted into free T3, as well as a protein-bound triiodothyronine/T3 is biochemically inert (not active). This means that in the blood, in the normal human body the thyroxine frees from protein binding only in the limited amounts (successively) so the blood levels of free thyroxine are constantly maintained less than 1%.
Therefor, in relation to pharmacokinetics and pharmacodynamics, the drugs made from animal thyroid gland - in the body's metabolism of thyroid hormones works exactly the same way as if these hormones were released from the thyroid gland it self.
That's why in patients treated with Dessicated Thyroid Extract, the blood values of free T4
has to be low because of the
long half-life of free T4, and because of the
short half-life of free T3, the values of free T3
has to be in the top of the reference range in patients who are correctly dosed in the treatment with preparations of animal thyroid gland. As long as the depot of free thyroid hormones in the blood is sufficient, the pituitary holding back on TSH, which remains low and this continues as long as this sufficiency sustains.
As in healthy human bodies, blessed with a healthy metabolism, thyroid hormones are working exact in this way, exactly same effect is achiewed in hypothyroid patients treated with DTE. This explains why so many patients prosper so much better with this treatment.
Please note: It is an expression of biochemical and pharmaceutical ignorance when individual doctors choose to "supplement" the DTE-treatment with an amount of synthetic T4 analog in order to raise blood levels of free T4, and after the effect of DTE-treatment for that reason fails, they say that it is DTE which does not work. It works alright, just do not mix together these two types of medications.
In relation to pharmacokinetics and pharmacodynamics of synthetic thyroxine analogues in the human body, works these drugs so the body becomes flooded with free thyroxine to a degree, that in a normal human body this would be called
"hyperthyroxinemia", whereas for some inexplicable reasons - in a hypothyroid bodies this condition is considered - by the doctors - as "normal".
It's NOT normal!
Too much free thyroxine in the blood at a time, is not normal and the body's genetic control will always try continuously to break down the excess of free thyroxine. This explains why so many patients treated with synthetic thyroxine analogues, nevertheless remains sick.
I wrote once in the past as an comment to another relevant article:
Now we just hope that at some point we can succeed in explaining to our doctors that the missing link in understanding that the carrier-protein binding is the difference between DTE (Dessicated Thyroid Extract) and synthetic T4 analogues.
Because more than 99% of thyroid hormones in the DTE are carrier-protein-bound, it means that the pharmacodynamics of DTE occurss with Slow Release Effect, which eliminating all the talk about the difference between Ratio of T4 / T3 in DTE made from thyroid gland of pigs and in human thyroid gland, and making it pointless.
All reflections on the Ratio of T4 / T3 in thyroid glands of pigs could only makes sense in the context of issues associated with transplant surgery between two different species, but in orally ingested drugs it does not matter.
Our doctors need to learn more about the biochemistry of the human body, and they really do need to learn about the difference between the pharmacokinetics and pharmacodynamics of these two types of drugs - Dessicated Thyroid USP and synthetic T4-analogues - because right now they consider those two medications as synonymous (which they are not) and consequently doctors are committing so many serious mistakes, that their patients basically remains sick.
It is almost impossible, touch briefly every detail, including corresponding metabolic aspects of artificial free triiodothyronine (synthetic T3) versus protein-bound triiodothyronine (T3) in preparations of animal thyroid gland, which in principle is exactly the same as the difference between metabolic aspects of "real" and "artificial" thyroxine, as well as briefly respond to claims that most patients are comfortable with synthetic T4 alone therapy, but I try anyway...
The problem is that most hypothyroid patients are mature women, and a large number of symptoms associated with inadequate treatment of hormone deficiency, are overlapping the most characteristic early and following later signs and symptoms of menopause. This means that as long as doctors choose to interpret the results of inadequate treatment of hypothyroidism, as simple state of menopause (or simple signs of age in men) - will no positive development happen. Doctors will remain dogmatic instead of knowing, while patients will remain sick.
Please, be aware that while the preparations of animal thyroid gland over the last 120 years has proved their effectiveness and efficiency in the treatment of hypothyroidism, no matter how many new patents are filed in still new artificial synthetic thyroxine "designs" over the last 65 years, they have still not proven their value for the hypothyroid patients. Only for the doctors.
Basically continues this controversy only because those oldtimers, animal derived drugs works very satisfactory, while those new artificial synthetic hormone analogs works only temporarily and incompletely, because of their
deviant molecular
structures.
I remember someone once said:
"Hypothyroid patients will continue to suffer as a result of the synthetic treatment, as long as doctors prefer the synthetic treatment more than they love their patients."
Please, always be aware of the difference between knowledge and dogma, because they are so dangerous easy not to notice the difference between. All rational human beings know how easily that can happen if one becomes too self-confident.
Best regards
(me)
Denmark