Quote from: Just Gwynne! on November 27, 2013, 07:35:08 AM
Anja, that is a phenomenal level of detail. Thank you for being thorough and technical.
Here's my question, re sublingual administration: given the higher bio-availability and faster absorption, am I correct in assuming that it would exaggerate the variability of serum E2 levels across the day??
The detail is not mine, I must admit. While I am partly a biochemist in profession, I am not a medical biochemist and this information is from a friend who did look into these things. The higher bioavailability would actually mean that a sublingual application would need to be of lower dosage than regular oral application. So just taking a 2mg Estradiol pill designed for oral application and putting it under the tongue may cause quite a huge spike in serum E2. I think there are pharmaceuticals designed for sublingual application with lower dosages then. As I understand it, the E2 does not really enter the bloodstream that much faster on that route - it takes less than half an hour in both cases. The E2 will then bind as I understand it to the SHGB as a storage. As long as the individual spikes are not too high, I was getting the impression that this buffering does work ok. What seems to not work too well is if the spikes are too high - then more SHGB is needed and produced, SHGB serum levels rise, more estradiol is bound to these "buffers" - but I think the main issue with oral is the E1 which basically drives the body to react the same way as having very high E2 dosages. As I read it, regularly a 1:1 ratio of E1 and E2 are normal for women, in oral application of E2, this ratio can be like 10:1.
So from what I got from that HRT support group I am in now is that spreading the HT over the day is good, to do that, gel is the best as it can also be dosed according to your individual needs in smaller steps, patches are good as they still have the benefit of a 1:1 ratio of E1 to E2, just like the gel, sublingual is the same, but one needs to find a proper dosage to not overdose on E2 and one gets a bit more spikes, oral is a bit problematic as it increases E1 and prodiuces spikes. But again, this is a HRT support group info. It does not encourage self medication of course, it just is about which of the regularly offered medication may be preferrable and in what way it might be applied.
EDIT: P.S.: Of course all these hormones are being changed into another, so E1 can become E2 just like T can become E2 - but it always needs enzymes to do this change, so E1 is not really just like a storage for E2 just as T is not a storage for E2, though as I understand it E1 is converted easier into E2 than T

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