Sublingual (Estradiol) Question

[ZosKiaCultusC7]

So I've been doing a little research and just learned that I can take my form of estradiol sublingually. Of course, I'm not going to do this without first consulting with my endo and as far as I remember, he never mentioned anything about it. I am almost tempted to call his office tomorrow to see if I can find out if I can do this but I do think I'm being a little impatient by even considering this. My dosage is at the starting spectrum but isn't as low as I have seen others'. Even though there have been changes in the period I've been on my meds, I've come across others who have had more changes in the same period of time I've been on them. I know, I know......YMMV!

Anyway, is it even worth it? I know that sublingual administration will bypass your liver, causing less stress on it. I have also read that its effect on your E-level will be higher than taking it normally. However, I have also read that sublingual administration causes the estrogen to disperse in a "burst" fashion (I have read 6 hours on numerous occasions) whereas normal ingestion spreads the estrogen evenly over a longer period (~24 hours). Also, I have come across a couple of instances where the increased E-level briefly impeded some effects of estrogen.

Chances are that I won't even bother calling my endo tomorrow and will continue to take my happy pills normally. I suppose I can wait until June (c'mon!) to see what changes to my dosage will be made but regardless, I am a bit curious.

[CharleneT]

You do not need to wait, or even ask your endo for that matter. It is a pharmacy question really. The simple answer is: absolutely ! As you've learned there are issues with strait oral consumption of estrogen. If you are taking estradiol, then definitely put 'em under your tongue. It will not take long to dissolve. Try not to swallow food or drink for a few minutes after you take the pill. This avoids some of the first pass thru the liver. How much varies and is hard to measure, but it doesn't avoid all of that first pass.

If you are taking Premarin, this will not work. Premarin tabs are not able to be dissolved in your mouth fully.

Here is some info about the difference in blood levels and what is stimulated by sublingual vs oral estrogen doses:

http://www.ncbi.nlm.nih.gov/pubmed/9052581

One good thing, the increase affect on E2 is better for feminization Often people taking estrogen, especially via sublingual, split their dose into two (morning and night) to spread out the "active period".


p.s. sublingual doesn't work for other HRT meds ...

[Inna]

I have begun one year ago with sublingual way of taking all my hrt meds since the beginning. Suggested by my therapist especially for Spiro, which had been known to weight heavily on the liver. I had seen the changes in my body and psyche which can only be described as miraculous. Now, that isn't to say that everyone will react this way, but if I can cut down on bodies metabolizing half worth of the dosage I take, I have a twice the effect and results to follow.

I can not prescribe nor even tell you what to do, you know, all that precautionary stuff with meds, but I wouldn't wait another minute, and pick up the phone and a quick call to your endo, YES or NO question. I am sure his secretary will even be able to answer that, and as simple realization goes, if you had the medicine prescribed already, the method of its taking unless stipulated, is really up to you, doctor had prescribed the dosage, so it is perfectly safe hon!

[Stephenie S]

Listen guys. This "bypassing" the liver stuff is pure fantasy.

Sub-lingual, injection, orally, transdermally, it matters not one bit. All these delivery methods put medication into your bloodstream. All your blood goes through your liver at a rate of about a gallon per minute. If the med is in your bloodstream it's gonna pass through your liver, period! There is just no way around this.

Take care of your liver. Get a liver panel every 6 months to a year. And use whatever delivery method that works for you.

Stephie

[Katesback]

Ya know when I worked with a hell of a lot of trans people. I met and talked with many that had been on hormones for years. I cannot EVER recall anyone having any adverse effects from taking a reasonable amount of hormones. I am sure some people suffer but crap I cant tell you how many people I saw that smoke, are fat, and do drugs. The funny thing was those were the people that would all to often chime in about this supposed danger of taking hormones......while puffing on a cigarette of course. Likewise these were often the people on the 10+ year transition track. You know the ones that talk and talk and talk for years but have no outward signs of progress. Of course they often are willing to offer advice as if they have some sort of REAL insight into transition. Ok I take it back they do. Often thier insight is what NOT to do. LOL

Guess I am just reflecting on all the BS I have herd over the years.

[CharleneT]

Listen guys. This "bypassing" the liver stuff is pure fantasy.

Sub-lingual, injection, orally, transdermally, it matters not one bit. All these delivery methods put medication into your bloodstream. All your blood goes through your liver at a rate of about a gallon per minute. If the med is in your bloodstream it's gonna pass through your liver, period! There is just no way around this.

Take care of your liver. Get a liver panel every 6 months to a year. And use whatever delivery method that works for you.

Stephie

I agree, you need to have your blood checked DEFINITELY take care of your liver, you do not want to be in the position of looking for a new one . . . .... But, there is a difference between first and second pass thru the liver. Patches and IM estradiol avoids one pass. While that is not perfect, it sure is better than all three passes ( which is about how long it takes our bodies to eliminate the hormones).

It is most definitely NOT a fanatasy that there can be ill affects to your system. Truly, most of the time you are ok. But remember: all the research is on people who take less than we do and for less time. So a bit of "careful" might just go a long way !

[CharleneT]

....

I can not prescribe nor even tell you what to do, you know, all that precautionary stuff with meds, but I wouldn't wait another minute, and pick up the phone and a quick call to your endo, YES or NO question. I am sure his secretary will even be able to answer that, ...

IF that secretary does answer that question, he should be fired. Call your pharmacist folks... that is who knows the answer ( well, so does the endo, but the call to the Pharmacist is free)

[ZosKiaCultusC7]

Well, I called my endo this morning and spoke with his secretary. She said that she would have to ask him and then call me back. I really hope she calls back before I take today's dose and honestly, I don't want to seem like a nuisance by calling her again. She can be touchy sometimes, especially when she's having a bad day. I'm so tempted to just do it but I'm paranoid to do so without my endo's consent because I am only on day 36, which means that since I'm only on one dose per day and if there is more of a low by using this method, it's going to suck. Plus, I have no idea where my hormone levels sit.

IF that secretary does answer that question, he should be fired. Call your pharmacist folks... that is who knows the answer ( well, so does the endo, but the call to the Pharmacist is free)

I thought about that but I don't see how they could give me good advice since they're just filling my prescription. I'm probably over thinking this whole thing but I suppose that I'm just trying to play it extra safe.

[ColleenW]

I agree with CharleneT. There is a difference between first pass and second pass through the liver and second is definitely easier on the liver. Recommendations for routine liver panels are also correct. I've been taking my HRT for over a year now sublingual and in divided doses and haven't had any problems.

[Stephanie-L]

I thought about that but I don't see how they could give me good advice since they're just filling my prescription. I'm probably over thinking this whole thing but I suppose that I'm just trying to play it extra safe.

Do not discount the advice of your pharmacist. They have a doctorate and have spent years learning how drugs work, how they are absorbed, eliminated, interact, etc. They may well know how safe it is to take your Estrogen sublingualy (from all I have seen, pretty safe), and what does it hurt to ask. BTW, as far as the burst effect goes, I kind of doubt it, last time I got my e-level for sublingual it was right in the target zone 15 hours after I took it, and I am not on a large dose. I do believe in the first pass effect, I have seen it come into play dramatically when administering other drugs sublingualy to my patients............Stephanie

[Traci Elizabeth]

I wish I was young enough to take "E" pills. I have to live with patches all over my butt and that awful glue that seeps out before week's end and when that glue gets on your panties, almost NOTHING can get it off!

BTW, what the heck is "YMMV" i know my age is showing.

[ZosKiaCultusC7]

Ha! As soon as I was about to call the Rite Aid pharmacy, my endo called and said that I can go ahead and start taking it sublingual, without having to split my dosage. I guess I'll wait and see if I notice any difference.

By the way, Traci: YMMV = Your Mileage May Vary

[Aprilrain]

Ha! As soon as I was about to call the Rite Aid pharmacy, my endo called and said that I can go ahead and start taking it sublingual, without having to split my dosage. I guess I'll wait and see if I notice any difference.

By the way, Traci: YMMV = Your Mileage May Vary

You really thought you'd have to split the dosage? Drs are super overly cautious with hormones at day thirty five your probably only taking a third of what would be an effective dose depending on your height and weight.

I have taken mine sublingually from the start and have had labs taken at various times of day, my levels are always the same.

Hormones are a long haul process, the various ups and downs of hormone levels throughout any one day do not matter, what matters is getting and keeping your blood levels at About 100-120 ish

When oral estrogen first hits the liver it's turned into esterone, at least some of it is, and esterone is a less potent feminizing hormone than estradiol. the goal of sublingual administration would be to keep as much of the estradiol in that form for as long as possible.

[ZosKiaCultusC7]

You really thought you'd have to split the dosage?

Haha, yes. The "dangers" of doing too much research, I suppose. The secretary didn't know how to answer when I asked this and I felt kind of stupid afterward for asking it.

[Stephenie S]

Well, I've heard this "first pass" stuff before, of course, but considering the fact that your blood goes through your liver at almost a gallon per minute, eliminating one "pass" through your liver is actually pretty miniscule.

I repeat, take good care of your liver. Don't drink alcohol. Stay away from Tylenol. Get a liver panel at LEAST once a year. But how you take your estrogen will have little to no effect on your liver. Jus' sayin'.

Stephie

[CharleneT]

Stephanie, the difference is that when you miss the first pass thru the liver the estrogen receptors are hit with a different input, AND since a lot of the estrogen is bound before it hits the liver, the stress on your liver is lowered. Missing the first pass is important. Yes, all blood goes thru the liver, pretty quickly as you pointed out - it is the major filter in your body. But when you do not start in the digestive tract, you do get different results. Both in terms of safety and "effect".

The advice to take care of your liver is extremely important and I hope folks realize that ! ! ! Alcohol is something you can ingest, but like most things, it is the amount that is important. A small amount is actually good for you. The issues with Acetaminophen are larger than the general public yet knows ... right now they are changing formulations to ensure that is it harder to over dose yourself. Soon, you will not see any APAP formulations on the market with more than 325 mg per dose. Truly, if I were the average person, I'd stop taking anything with Acetaminophen in it ... I think someday it will be known as the largest medical experiment on general public without their knowledge.

The most important part of this discussion though is this: embark on HRT only with the help of a doctor and choose one who thinks that regular blood work is a good idea for the first few years. Most of the time, there are not major problems. The kicker is that if you do have a problem you won't feel a symptom until it is pretty far along (such as liver trouble). Clearly, we agree about that

[ZosKiaCultusC7]

Truly, if I were the average person, I'd stop taking anything with Acetaminophen in it

I avoid it as much as possible, even with the cold I've been dealing with all week. I bought Nyquil for when my cold was at its peak but after buying it, my over-paranoia of drug interactions caused me to leave it sealed. Instead, I fought off the hellish part of this thing by sleeping and water. The bad part was over in less than 24 hours. Drugs can be good in some applications (duh!) but a lot of people are so quick to reach for Tylenol to get rid of a headache when all they may need is to re-hydrate themselves.

[Aprilrain]

a lot of people are so quick to reach for Tylenol to get rid of a headache when all they may need is to re-hydrate themselves.

By the time i need to rehydrate myself and I have a head ache from it its too late, i usually take Ibuprofen or Aleve.

The thing that gets me is how many people who say they care about such things don't bother to read labels. For instance everyone is mystified when I tell them that Benadryl is the sleep ingredient in Tylenol PM. They behave as if I have some sort of special knowledge. Yeah I know how to read!

[ZosKiaCultusC7]

By the time i need to rehydrate myself and I have a head ache from it its too late, i usually take Ibuprofen or Aleve.

I've actually found that chugging a large glass of water helps with this. When I went through the weightlifting phase of my past maleness, I took a lot of supplements that would cause headaches if I didn't stay hydrated (especially creatine monohydrate). Often, I would wake up with a hangover headache that didn't occur from drinking the previous night. I would go crazy with the water and within an hour, my headache would be gone.

[Stephanie-L]

Well, I've heard this "first pass" stuff before, of course, but considering the fact that your blood goes through your liver at almost a gallon per minute, eliminating one "pass" through your liver is actually pretty miniscule.

I repeat, take good care of your liver. Don't drink alcohol. Stay away from Tylenol. Get a liver panel at LEAST once a year. But how you take your estrogen will have little to no effect on your liver. Jus' sayin'.

Stephie

You give good advice about taking care of your liver with things like avoiding alcohol and certain drugs, etc, but you really don't know what you are talking about when it comes to avoiding the first pass effect. The entire venous blood flow from the digestive system passes through the liver before it goes to the heart or anywhere else in the body, so the liver gets the highest concentration of drugs taken via the digestive system route. If you take a drug by another route, IV, transdermal, or sublingual, the drug is diluted in the entire blood supply before it gets to the liver, so not so much of it is degraded as quickly, and the liver is not exposed to such high concentrrations of the drug. I would like to know where you get the expertise to be "Jus Sayin" about this, do you have a degree in pharmacology, physiology, biochemistry, or are you a physician? I have studied these subjects, and have learned from people who are experts and have done research on this fact, I think I will trust them over you Jus Sayin..........Stephanie