I have posted before on the side effects I have been having from estriol cream vaginally. I have also replied to other posts where some members have had side effects with local estrogens. We are led to believe that local estriol should not have any side effects but I have found information that shocked me!

I have been using it for three months now. I have been having so much trouble trying to increase the amount I use as it made me feel AWFUL ! I have been advised to use it every day without a break.
Yesterday I reached a point where I felt I could not go on any more. I felt weepy depressed and worst of all really anxious. Hot flushes hugely increased! These feelings have been getting worse and worse but I have been trying to get past them.

I could not sleep last night, so anxious was I -and in the end at 3 am I got up and started googling. I found this on the official document by Ortho-gynest, who manufactures my Estriol cream.


Quote-
5.2 Pharmacokinetic properties

Estriol is readily absorbed following intravaginal application. Peak serum estriol concentrations are generally observed within 2 hours following intravaginal application and remain elevated for 6 hours. Systemic bioavailability on vaginal administration is better than after oral administration. *Intravaginal application of 1 mg estriol in women with senile atrophy of the vaginal epithelium results in serum levels similar to those seen after oral administration of 10 mg estriol.*

Plasma estriol levels increased from <90pmol/L (26 pg/mL) about fifty fold over a few hours after intravaginal administration of Ortho-Gynest Cream. Eight to ten hours after administration, 50% of women still had estriol levels above 90pmol/L (26 pg/mL).

Estriol circulates with the blood, about 14% free, 8% bound to SHBG and the rest bound to albumin. Primary metabolites of estriol include the 16-alpha-glucuronide, 3-glucuronide, 3-sulfate and 3-sulfate 16-alpha-glucuronide. More than 95% of estriol is excreted in the urine, predominantly in the form of glucuronides. unquote

Well I dont know what the last paragraph means but based on the recommended daily usage of 5ml of cream containing 0.5 mg of estriol I calculate that I have been getting an equivilant dose of up to 5mg per day systemically! Since it doesn't clear from the bloodstream for up to 10 hours I was probably overdosing on the stuff too!

I am very med sensitive so I have been going off the planet!
I haven't used any since Friday and I am beginning to swing back to normal.

I just wanted to share this with anyone who is interested and check that I haven't made a mistake in my calculations?
I am quite relieved to know I am not imagining things. I am tired of being told it is not supposed to be systemic!
Phew-glad I got that off my chest

janet c

Janet,

That is very interesting. If I am not mistaken estriol is supposed to be the protective estrogen. I wonder if those of us who supplement with estradiol shouldn't consider using this stuff as well??

I am sorry it made you feel so lousy. Perhaps once you have cleared your system of the overload, you should use half what you have been using every 2nd or 3rd day?

Janet,

I think you should consider doing what Floater mentioned about cutting your dose and skipping days. It would be a shame to lose the benefit as estriol is the protective one out of E1, E2 & E3.

I have thought the same about estriol so I have added some biest daily to my patch, which I now cut in 1/2. I would like to do away with the patch but I seem to need the estradiol in a higher concentration that the 80/20 and Doc has resisted changing my formula so far.

Thanks ladies for your replies.

Yes I am certainly going to continue with it but just use it less often. Once I got over the first few times of using it, I felt much better and more joyful generally. It also increased my libido which one of the reasons I have been trying to use it. Having said that I have been feeling so foggy headed and weird the last couple of weeks that I haven't really been interested.
I am feeling much better now anyway and the anxiety is decreasing.

Yes Floater-estriol is very safe and anti-cancer. This is why I am allowed it, as I had endo cancer three years ago.
I gather there is a problem with it in US but here in UK I can get it from my doctor.

I am interested in trying an estradiol cream in the future. I presume there is one? I wonder whether I would find it too strong for me? The trouble with estriol is that it is really a pregnancy hormone. I think that is why I feel so weepy and emotional with it. Maybe estradiol wouldn't cause that. I do tend to be anxious with estrogen though!
janet c

If you try estradiol perhaps you can ask your doctor to prescripe the patch. I find that I could not tolerate the creams in any form intra-vaginally. I think that the potency and delivery of the creams was to quick for my system. I do use the estriol cream on occassion just a dab on the outside of the labia to help with dryness. I just got sick and aggitated using the creams.
I now use the lowest dose of the vivelle patch and wear it for one week instead of replacing every 3 days. I was told it bypasses the liver and if you can love estrogen- I love the way the patch makes me feel!
I hope you get all of this tweeked out.
Bobbi

"I just got sick and aggitated using the creams."

Thank you Bobbi
At last someone else who gets affected the way I do! I have been corresponding with Bellevue pharmacies for ages about this and also searched for info on the web and have been told so many times that estriol is weak and does not go into the bloodstream etc etc. and should not have side effects.
I was going off the planet, as I was advised to use it every day and try to build it up, so that is what I did until I had a complete meltdown last weekend . I was up all night googling, and then I found that info.

I really only need the help vaginally. It is coming up to three years since my surgery and I am doing really well without HRT. I think it would be a retrograde step to start using a patch-I actually don't feel I need it now.

Because I was using estriol daily I got very good results from it and my atrophy has been dealt with. So my plan is now to use it maybe 2 or 3 times a week -just a dab to keep things on an even keel.
Maybe I should just stick to that and not ask for the estradiol cream.

janet c

Ive also had problems with all the HRT ive tried...the creams, patches, pills, etc..even in the lowest dose, all make me feel so sick. I even used the vagifem and had side effects from that, even though everyone says it doesnt get into the bloodstream? yeah right? I had horrible leg cramps, dizziness, anxiety, headaches, stomachaches..the list goes on.
The patches made me soooooo ill. I couldnt even walk after putting one on...the lowest doses too!!!

I think some of us just are not able to tolerate these hormones. Im still taking a low dose-bio est cream at the moment..my dryness is so severe, i dont have a choice.

thanks for bringing up this topic.

I was put on estriol cream and everytime I use it I feel worse more hotflashes , etc. I have not been able to tolerate it yet even a couple days a week. I found that my testosterone was low and that makes vaginal dryness. Once I took testosterone cream my vaginal dryness completely went away. I totally believe estriol can build up in the body and cause side-effects.



wendy

Estriol definitely goes systemic as do all hormones applied topically, or any other med, for that matter. When I was using estriol vaginal cream and nothing else, I started getting sore breasts (which I never got unless I was pregnant) and finally realized it was the estriol.

I am so glad I am not the only one, because so many people think your'e crazy when you say you can't use it because of side effects!

After 3 months of trying to get my body used to it, I have finally had to give up. It made me feel so ill even in tiny amounts!
I have just discovered a wonderful product- about which I have posted in the vaginal dryness section called Emerita phyoestrogen cream. I have been using it around the outside of vagina instead of the estriol and have had wonderful results in a week! It is a body cream for hot flushes mainly but I have had such great results with it in that area too.! It has reduced my hot flushes considerably too and I would highly recommend it
janet c

I am taking 1mg estrogen, 1mg estriol and 25mg progesterone per day and its all fine.

I have chosen to replace half of my estradiol by estriol because its weaker, its more healthy, reduced risk of getting breast cancer and it reduces post-meno effects just as the estradiol does....
Estrogen naturally has to be balanced with progesterone. Read about Estrogen dominace.

Glad you are doing well on that regime!

As has been said on this thread, many women find estriol makes them feel awful and I am one of them. Although it is weaker it is the main estrogen made by the body during pregnancy, so it tends to cause similar symptoms.
It makes my hot flushes and anxiety worse and I become unstable, highly emotional and depressed on just a few dabs a week.
Yes thanks I know about estrogen dominance but it has nothing to do with it in my case. I am now using an estradiol oil vaginally with no horrid side effects and I don't need progesterone as I don't have a uterus.
Hope you continue to do well anyway

janet c