Susan's Place Transgender Resources

I've been taking oral E for about a week now. I elected to take it at 8 PM, logic being that I didn't want to be spiking during the workday.

But, I've been experiencing very poor sleep. Every night, I seem to wake up around 2-3, tossing, turning, and throbbing all over (feels like a movie transformation scene).

I wondering what time other people take oral meds and what their experience has been.

Thanks.

I take my E at 3:30pm (my lunch time) and again at 12:30am. I don't go to sleep until around 3 and I sleep fine. Also Spiro I take at 12:30pm and 9:30pm, P at 6:30pm. Not sure if that helps it or not.

I am just getting started but Take my first spiro and E at 03:30 am and second spiro at 15:30 in the afternoon. no special reason, that just fits my schedule right now do to work hours. other than getting up to pee a lot i sleep ok lol. I work 12 to 16hrs a day so pretty bushed out by the time I get to pillows

Jerri

Thanks for the replies. What jumps out at me is that both of you divide your dosage, which I have not been doing.

No spiro, incidentally.

Just following my endo's direction for frequency, it took me several extra months of therapy to get hrt support due to self dosing before i was ready to come out. do not ever want to give my GP or endo a reason to question my actions. so i would say it is best to follow your doctors advice but always know if it does not seem right we have the right to question them and get answers or an explanation.
Jerri

Quote from: Just Gwynne! on November 26, 2013, 12:24:09 PM
Thanks for the replies. What jumps out at me is that both of you divide your dosage, which I have not been doing.

No spiro, incidentally.

When ever possible i divided my doses am and pm.

Izzy

I am angry at oral estrogens as they may not have helped me get where I wanted to be. If I had to take them, I would split it morning and evening. I would consider taking it sublingually but that is 15 times more effective, so even half a pill is sort of overdosing. From what I learned now, I would not recommend oral anymore. Too much Estrogen is converted in Estron which is not doing that much good.

Single pill? Morning or break it, and every twelve hours. Multiple pills? Just split em up as you want. The serum level isn't real spikey with estradiol, it's not like it's out of your system even if you miss 48 hours.

I take my E in the morning and put it under my tongue. When I took Spiro a long time ago. I took one pill with the E and the other about 4 hours or so before I went to bed.

These little dot E patches are very nice. Replace every 3 1/2 days. They provide a constant level of E. More expensive than pills but worth it for me.

I usually take my pills at lunch and dinner since they are suggested to go with food. This typically ends up being around 1 and 7. One thing with me is, if I take them too late, I end up needing to go to the bathroom in the middle of the night multiple times.

Really, there's not a huge need to split it up or worry about keeping the time precisely the same - my doc told me the hormone level in your body is a pretty constant level, the pill is just to keep that going.

Thank you so much :)

It's a relief to have context.

I think this is individual but from what I get, a while after taking a E2 pill, blood levels in E2 (estradiol) and E1 (estron) are going up. Then the body reacts and tries to bring the levels down to a more regular level and starts to create enzymes that convert estradiol and/or bind it as a storage. The problem with that seems to be that this process can then be overly effective and bring E2 down a lot if no additional E2 is given regularly, so that it is quite possible to loose much of the effective E2 during the day and even run out at the end of a 24h period. For me this resulted in hot flashes and some other symptoms at 5 am, 3 hours before the next pill was due.
One issue about this is that the body seems to react to both, E1 and E2 by downregulating (http://en.wikipedia.org/wiki/Downregulation_and_upregulation) the response to E2. This would be fine if E1=E2, as it is a natural compensation for high E2 levels. But in oral application of E2 (by swallowing the pills) there is a lot of E1 coming out, causing downregulation of estrogen receptors. But as E1 does not have the same effects as E2, that downregulation actually means that the E2 in the system cannot act to its potential.
Sublingual and subcutaneous application produce about the same E1 as E2 and thus may be superior.
This is what I am getting from the research of a fellow woman who is very interested in this topic and she is trying to help people like me who have had negative effects from being too long on an oral E2 monotherapy.

My endo told me to take Spiro first thing in the morning due to its diuretic effect, he said it would stop frequent trips to the loo at night. Personally haven't noticed a change to my need to pee as a result. The E is three times a day. Sleep hasn't been great but better since moving to a sub dermal pellet for other E.

Quote from: mind is quiet now on November 26, 2013, 01:00:37 PM
When ever possible i divided my doses am and pm.

Izzy

This seems quite natural. I'm going to check with my pharmacist to be sure, but I think this is the route I'll go, too.

Quote from: anjaq on November 27, 2013, 03:24:08 AM
I think this is individual but from what I get, a while after taking a E2 pill, blood levels in E2 (estradiol) and E1 (estron) are going up. Then the body reacts and tries to bring the levels down to a more regular level and starts to create enzymes that convert estradiol and/or bind it as a storage. The problem with that seems to be that this process can then be overly effective and bring E2 down a lot if no additional E2 is given regularly, so that it is quite possible to loose much of the effective E2 during the day and even run out at the end of a 24h period. For me this resulted in hot flashes and some other symptoms at 5 am, 3 hours before the next pill was due.
One issue about this is that the body seems to react to both, E1 and E2 by downregulating (http://en.wikipedia.org/wiki/Downregulation_and_upregulation) the response to E2. This would be fine if E1=E2, as it is a natural compensation for high E2 levels. But in oral application of E2 (by swallowing the pills) there is a lot of E1 coming out, causing downregulation of estrogen receptors. But as E1 does not have the same effects as E2, that downregulation actually means that the E2 in the system cannot act to its potential.
Sublingual and subcutaneous application produce about the same E1 as E2 and thus may be superior.
This is what I am getting from the research of a fellow woman who is very interested in this topic and she is trying to help people like me who have had negative effects from being too long on an oral E2 monotherapy.

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??

Quote from: Ms Grace on November 27, 2013, 03:29:41 AM
My endo told me to take Spiro first thing in the morning due to its diuretic effect, he said it would stop frequent trips to the loo at night. Personally haven't noticed a change to my need to pee as a result. The E is three times a day. Sleep hasn't been great but better since moving to a sub dermal pellet for other E.

I get dry mouth sometimes and drink more water than usual but I only pee like two more times a day than I usually do. I think the diuretic effects of Spiro have been exaggerated (though maybe not for everyone). I also haven't had any problems sleeping, even though I take E orally and it would peak while I'm asleep. Maybe I'm just lucky.  :-\

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 ;) - http://upload.wikimedia.org/wikipedia/commons/thumb/1/13/Steroidogenesis.svg/2000px-Steroidogenesis.svg.png