Print

Please login or register.
1 Hour 1 Day 1 Week 1 Month Forever
Login with username, password and session length

[Dandelion]

I was taking 75mcg evorel and 100mg utro daily to balance gaba receptors, because, as mentioned elsewhere, the other drug I am dependant on and weaning off under the supervision of the doctor, valium, shares the same receptor as prog.

Bottom line is delivery. I take it orally but its a pain because of the food thing, I have to take notice of it, being dependant and weaning down from diazepam.
I take 100mg every day even though im peri and prescribed 200mg 12 days.
I changed regime cos the non prog days got beyond a joke alongside the valium reductiong as the receptors they shared were more turbulent than a tall ship in a force 9 gale.
Would vaginal delivery take more progesterone to my GABA receptors?
It's far easier, you can take it same time daily, set your bleeper.

I've edited this to death because I kept forgetting to mention that when I decided to up my evorel to 100mcg, as 75mcg does not cover me emotionally, I'm using a fan in bed in May, not normal for me, July or August or even early Sept yeah, normal hot fan needed, pre menopause, but would 100mg utrogestan enable me to have a bleed like 75mcg does?
I don't bleed every month, but I recently felt like I'd emptied my womb, after a bleed, around the end of April, but would raising the evorel stop the bleed, causing womb lining to build up?
While glad I got the all clear, and discovered, even if for myself, bladder was responding to tension from nervousness, rather than lumps and obsructions, I hope that 100mg utro daily will still let my cycle come through, because I need 100mcg evorel, the anxiety from lack of oestrogen is horrible, it's impulsive, compulsive, and convincing.
I wouldn't feel comfy going more than six months without a bleed, I might have to go back down to 75mcg just to ensure prog is opposed enough to allow womb lining to shed even if it is only every few months while still in peri.

[Tempest]

Hi, Dandelion! Nope - I think it would be LESS as this is why a lot of ladies take it vaginally to lessen the sedating effect. xxxxx

[Dandelion]

Hi, Dandelion! Nope - I think it would be LESS as this is why a lot of ladies take it vaginally to lessen the sedating effect. xxxxx

That says a lot actually. I really need a timetable around eating, utro injestion, and benzo dosing, but its so hard for me to stick to rigid time tables.
Maybe i'm best sticking to oral, or looking at other continuous preps.
I need prog daily though and most are 25 days, cannot understand why miss 3 days of calming progesterone. It helps me sleep enormously.

[Lizab]

Hi Dandelion. It's my understanding that the 3 day break from Utro is to allow your body a bleed if the Utro isn't keeping you thinned enough. Really if the dose is sufficiently keeping you thin, you wouldn't bleed from the 3 day break. If that's your case on your current dose, I don't see why you couldn't stay on it continually. In other words, taking it 25 days a month is essentially the same as continual, the 3 day break is just a safety net.

Perhaps Hurdity or another more familiar with the science behind it can confirm.

[Dandelion]

Thanks
Might give vaginal a try, if I find my anxiety or other nasty symptoms start to surface, I can always go back to orally. I'll have a think, bit scared of losing my shit if less calming progesterone coursing through my system, with Elizabeth Vliet comparing it to a klonopin, a much stronger version of valium.

[Hurdity]

Hi Dandelion

The GABA thing is complicated.

From what I have read, vaginal use of progesterone may lead to higher systemic levels. However oral use of progesterone gives rise to a much greater number of metabolic by-products which could be responsible for the the effects you are discussing. In many women these are negative (sedative) effects - but I presume this is the effect you want to maintain.

These are various less technical extracts from a paper by Kuhl 2005 on estrogens and progestogens and how they are metabolised using different modes of delivery ( oral, vaginal, transdermal etc). The parapgraphs don't necessarily follow on in the original paper as there is a lot of technical stuff in between - I've just extracted the easy to follow descriptions.

Due to their antiestrogenic effect, progestogens,including progesterone, may counteract the timulatory and excitatory effects of estrogens on the brain. Beyond this, progesterone exerts a pronounced
sedative effect after conversion to 5a and 5b-pregnanolone, which bind to the GABAA-receptor.

Progesterone is rapidly metabolized, predominantly by reduction of the keto groups and the D4-double
bond, and the pattern of metabolites depends largely on the route of administration.The oral application of progesterone is associated with an extensive metabolism in the gastrointestinal tract and the liver, which results in high, but individually variable, concentrations of circulating metabolites.

After oral administration, progesterone can be metabolized to more than 30 metabolites, among
which some exert specific physiological activities.The most important pathway is the formation
of 5a- and 5b-pregnanolone which exert considerable sedative effects after binding to the
GABA A receptor.

There are large interindividual differences in the pattern of metabolites circulating after oral
administration2  In contrast to the oral route of administration, the rate of metabolism and the formation of pregnanolones is much lower during vaginal treatment with progesterone. Therefore, the risk of a
sedative effect of progesterone is lower than that observed during oral therapy.

Compared with the oral route, the vaginal route of administration of progesterone results in higher serum levels of progesterone, which are sustained for a longer time than after oral treatment.

On this basis I would suggest you would be better of if you continue to take it orally - but there is no harm in trying it vaginally,. By the way I really wouldn't worry unduly about the food thing - as long as you are usually consistent with how you take it. The research shows that bio-availability of progesterone is increased if taken with food - so you may get more in your system - but I would say consistency is key especially give your situation.

Hurdity x

[Tempest]

Dandelion, I really would stick to oral and not even attempt to try vaginally at the moment as you have to be so gentle with yourself during a benzo taper and especially with BPD. I understand your situation completely as I have a friend with BPD as I shared with you a while back, and tiny things can cause huge mood shifts as you know.

Sending you biggest hugs, and do check if you can indeed take it continuously with your specialist as it would offer you even greater stability at this difficult time. You're doing great - benzo tapers are EXTREMELY tough going and you're being brave - never forget that. Good luck and I'll be thinking of you! xxxxx

[Dandelion]

Dandelion, I really would stick to oral and not even attempt to try vaginally at the moment as you have to be so gentle with yourself during a benzo taper and especially with BPD. I understand your situation completely as I have a friend with BPD as I shared with you a while back, and tiny things can cause huge mood shifts as you know.

Sending you biggest hugs, and do check if you can indeed take it continuously with your specialist as it would offer you even greater stability at this difficult time. You're doing great - benzo tapers are EXTREMELY tough going and you're being brave - never forget that. Good luck and I'll be thinking of you! xxxxx

Hi

Thanks for the suggestion to go all oral.
Thanks for your reply.
To go all oral would mean that as valium and the metabolite of progesterone is cross tolerant it would be like upping my benzo dose, which I don't want to do, my GABA receptors would think they are getting more Benzo due to the liver first pass thing with the oral. x

[Dandelion]

Hi Dandelion

The GABA thing is complicated.

From what I have read, vaginal use of progesterone may lead to higher systemic levels. However oral use of progesterone gives rise to a much greater number of metabolic by-products which could be responsible for the the effects you are discussing. In many women these are negative (sedative) effects - but I presume this is the effect you want to maintain.

These are various less technical extracts from a paper by Kuhl 2005 on estrogens and progestogens and how they are metabolised using different modes of delivery ( oral, vaginal, transdermal etc). The parapgraphs don't necessarily follow on in the original paper as there is a lot of technical stuff in between - I've just extracted the easy to follow descriptions.

Due to their antiestrogenic effect, progestogens,including progesterone, may counteract the timulatory and excitatory effects of estrogens on the brain. Beyond this, progesterone exerts a pronounced
sedative effect after conversion to 5a and 5b-pregnanolone, which bind to the GABAA-receptor.

Progesterone is rapidly metabolized, predominantly by reduction of the keto groups and the D4-double
bond, and the pattern of metabolites depends largely on the route of administration.The oral application of progesterone is associated with an extensive metabolism in the gastrointestinal tract and the liver, which results in high, but individually variable, concentrations of circulating metabolites.

After oral administration, progesterone can be metabolized to more than 30 metabolites, among
which some exert specific physiological activities.The most important pathway is the formation
of 5a- and 5b-pregnanolone which exert considerable sedative effects after binding to the
GABA A receptor.

There are large interindividual differences in the pattern of metabolites circulating after oral
administration2  In contrast to the oral route of administration, the rate of metabolism and the formation of pregnanolones is much lower during vaginal treatment with progesterone. Therefore, the risk of a
sedative effect of progesterone is lower than that observed during oral therapy.

Compared with the oral route, the vaginal route of administration of progesterone results in higher serum levels of progesterone, which are sustained for a longer time than after oral treatment.

On this basis I would suggest you would be better of if you continue to take it orally - but there is no harm in trying it vaginally,. By the way I really wouldn't worry unduly about the food thing - as long as you are usually consistent with how you take it. The research shows that bio-availability of progesterone is increased if taken with food - so you may get more in your system - but I would say consistency is key especially give your situation.

Hurdity x

Hi Hurdity I just saw this reply, sorry for the late reply, a member here had to bring these replies to my attention as I missed them.

Yes, the GABA thing is complicated. Still bleeding but you will be pleased to know my GP is letting me come in for an exam on Friday this week. She mentioned she wants me to stay stable so will not be changing the prog delivery or dose and has ordered a scan as per Dr Currie's recommendation.

From what I have read, vaginal use of progesterone may lead to higher systemic levels. However oral use of progesterone gives rise to a much greater number of metabolic by-products which could be responsible for the the effects you are discussing. In many women these are negative (sedative) effects - but I presume this is the effect you want to maintain.

I will try to answer this the best I can. I do need to keep a consistent utro dose, currently still 100mg oral and 100mg vaginal, to keep GABA stable, ie, not increase the allopregnanolone metabolite.

I spent time reading about female sex hormones and GABA and got worried.

Due to their antiestrogenic effect, progestogens,including progesterone, may counteract the timulatory and excitatory effects of estrogens on the brain. Beyond this, progesterone exerts a pronounced
sedative effect after conversion to 5a and 5b-pregnanolone, which bind to the GABAA-receptor.

Utro does sedate me yet I am still anxious but I do have a lot of situational non medical stressors going on in my life as well.

The individually variable metabolism is a bit worrying.

I mentioned in the post above that changing my one capsule of vaginal to oral would be like increasing my valium with the two drugs being cross tolerant with each other. Just put this in to save you scrolling up.

What does higher serum levels mean in the context of vaginal?
I'm a bit confused, as I though oral would mean a higher concentration of it in my body.

I agree consistency is key. With my last gynaecologist consultation I was put on 100mg oral and 100mg vaginal added to stop bleeding which worked for about 6 months.
Bleeding came back, so GP reduced patch from 100mcg to 75mcg, which worked a few months then bleeding came back.
I went on gel. GP knows I now take 50mcg gel, so a further oestrogen cut, but bleeding still here.
This is the longest bleed, going on for three months now, not heavy all day, some days just spotting.
I just hope its not cancer or any other serious condition.