Oral Estrogen: To swallow or not to swallow.

[Guest Jo-88]

hi i dont take estradiol at all, im on premarin, and there gell coated and ive had amzing results all said and done

from an efficacy stand point Ive also heard that premarin is just as good as estradiol. However from a health stand point estradiol is going to win out, its chemically identical to the estradiol found in natal women and its also pure in consistency, premarin on the other hand is made from pregnant horse urine and contains Conjugated Equine Estrogens which is basically a mashup of a bunch of horse estrogens that cant even be used by the human body and then estrone which is a weaker estrogen than estradiol. But again from all that I've seen, the physical feminization is excellent with both of them... Although personally I would rather have something synthesized in a lab, a lot of people shy away from anything "synthetic" but thats just silly it may be synthetically created but its still chemically identical to the real thing. Anyway just my 2 cents

[Guest TracieV3]

Jodie, thank you for the information, I take a few of those medications you mentioned.

On a side note. Don't anyone know why the makers of estradiol added mint flavor to estradiol medication? It is not candy, do the makers expect a person's mouth to be minty fresh afterward.

[Guest JenMorse]

A bit strange... My estrogen was perscribed to be taken sublingually, but the medicine's instructions just say to swallow. It dissolves quickly so I assume sublingual is fine. (Progynova)

[Guest Maria_B]

Gel coated.

I swallow.

*snickers*

[~Nova~]

Any questions about how you should take, or how much of your medication you should take, should be asked to a qualified physician. YOUR qualified physician.

Do not take advice on your life based on internet message board.

If you have questions on your medication, call your doctor!

[Guest Jo-88]

My estrogen was perscribed to be taken sublingually, but the medicine's instructions just say to swallow.

Same here, I think the instructions are fairly generic its just a print out from the pharmacies database but doesn't necessarily cover every specific to the drug, so for anything beyond those instructions just consult your doctor. The prescription bottle itself just says "take by mouth"... so I guess that covers sublingual. Nonetheless, Im just going do it the way the doc told me.

[Guest Myria]

Anything absorbed by your digestive tract goes through your liver before going out to your bloodstream, this is called the First Pass Effect. In the case of Estrogens, when the liver sees a spike in Estrogens it increases clotting factors. The general thought is this is some left over physiologic programming to protect mothers post-birth. Whatever the reason, this increase in clotting factors increases one's risk of a DVT/PE (Deep Vein Thrombosis which can cause a Pulmonary Embolism), which can potentially be catastrophic. A PE can cause an sudden MI and then it's game over, really something to be avoided where possible.

Mind you the actual level of risk is relatively low and the primary risk factor is genetic and can be tested for. Other risk factors include recent surgery or injury, certain drugs, chemotherapy (tends to make one hyper-coagulative), and such -- mostly non-factors in most people's lives. "Lifestyle" issues, whether or not you smoke and such, are a factor, but far less so than is often portrayed. Beyond that, due to hepatic recirculation, no method of taking estrogens avoids the problem entirely. Basically all women, including us, are at a higher risk of a DVT than men.

It's telling that IV Premarin is used in emergency rooms to induce clotting.

That having been said, the first pass effect is where the biggest spike occurs. Anything that avoids it reduces your risk somewhat. So sub-lingual, IM, and transdermal are all somewhat safer than straight oral. The other factor appears to be the type of estrogen. Straight up artificials, like ethynlestradiol (Diane-35, et al), seem to be the worst -- frankly I'd advise anyone to avoid EE like the plague. Premarin also has somewhat of an increased risk. The closer you get to endogenous-identical, which basically means either Estradiol Valerate or 17b-Estradiol, the better your body handles it. Why? Good question, likely because artificials like EE or non-human endogenous like Premarin are going to have a longer half-life, thus more hepatic recirculation. That's the best guess anyway.

The other thing you get by taking your estrogen sub-lingually is a higher dose entering your bloodstream. Absorption rates vary, depending on the individual and drug -- some drugs are as low as 20% -- but a fair bit of what you take orally never makes it into your bloodstream. While you inevitably end up swallowing some of the dose, sub-lingual means a whole lot higher percentage of it going straight into you bloodstream. On the flip side you end up with a reduced overall half-life, since it's absorbed all at once, and it's a bit easier to overdo things, especially if you add in other factors like regularly eating grapefruit.

Overall I'm not really sure it matters much. If you go sub-lingual you can get by with a somewhat reduced dose and you will have a somewhat lower risk -- albeit after a year or two I doubt it matters. If you're just starting out it's probably worth it to you, but after a few years... Meh.

By the way, I wouldn't recommend trying it with Premarin. Stuff takes forever to dissolve and tastes, well pretty much like you'd expect, given what it is. Also I wouldn't recommend trying it with Spiro. Spiro tastes horrid, has a pretty good absorption profile to begin with, and isn't something you want spiking in your bloodstream -- keep in mind that it's a potassium sparing diuretic, with a primary on-label use (albeit not used all that much anymore) as an anti-hypertensive. Its anti-androgenic properties are a secondary effect.

Honestly the best method is IM -- Progynon Depot 10/100, if they even still make that, or some other endogenous-identical. But few doctors want to go that route. Personally I've never been a huge fan of transdermal. Sure, it avoids the first pass effect, but I feel that properly titrating with it is a PITA at best. Oral is dominant because it's cheap, easy, and reasonably safe. Sub-lingual is doable for many of the more common drugs, and has its advantages.If you're taking Progynova, or something similar, it's definitely something to consider, but I wouldn't worry about it too much one way or the other.

IMHO, YMMV, and all that.

Myria