Mechanics of using the transbuccal route for HRT

When taking one's HRT via the transbuccal route, there are really only two things you have to master. One is physically keeping it in place long enough for it to be fully dissolved without swallowing it all in saliva (which is the same as swallowing it as a pill). The other is picking the right place for this in your mouth.


In choosing where to put your HRT, you can use any place in your mouth, since the micronized estradiol in Estrace or its generics (or compounded troches) can move right through any part of the entire oral mucous lining. But the optimal location will be the one that causes the fewest associated symptoms due to its uptake, and that's likely to be a personal situation that can be determined only by experience.

Dissolving your pill or troche under the tongue seems pretty straightforward and controllable, and indeed is the direction provided with many compounded HRTs. But some women may find that they get a headache almost instantly, one that can take an hour or more to clear. The suspicion is that when this happens it's going zinging from under the tongue straight into the circulation through one's head to run full tilt into the brain with a mighty SLAM. Ouch.

When some women put it between gum and upper lip (back halfway between the pointy eyeteeth and the last molar--if you feel up there with your tongue, there's usually space "on top of" the roots of your teeth where it can be tucked and not slide back down), it stays up well and absorbs fully, but it can make one's nose/sinuses fill with mucous. Now, estrogen is given to chickens to make them retain water and weigh more once they are butchered, so speculation we've read on this response was that either this was a reaction to the estrogen as a sinus irritant or it was causing local fluid retention, hence the snotting-up.

A third option is in front, between the lower gum and lip, all the way down at the bottom "below" the roots of those teeth. For women troubled by the above problems (and there are plenty of women who aren't, so don't assume that you will be if you prefer to start with one over another), this one may be a viable alternative and we've not read any other problems with this location except for the need for some dexterity in maintaining it in position.


The other aspect, then, involves getting it to actually stay put and dissolve. That's almost more of a motor skill than anything else, and you can expect a few failures at first. You may want to practice in privacy lest you grin too many good morning smiles with lavender-smeared teeth. Here's what we've found helps.

Before putting the tablet (or partial tab, if you're customizing your dose) in your mouth, try to sort of suck up all the excess saliva so the location is fairly dry. Then pop the tab into place without a lot of lingering to get wet on the way. This seems to help make the tab stick where it's put. Get too much saliva in there between skin and tab and you run a risk of having it pop back out: we've heard of them actually being sneezed them across the room on mornings when the timing was off, and we really don't want to be envisioning you scrabbling around on the floor on your hands and knees trying to get it before the cat does.

Okay, so you have it tucked out of the way and fairly adhered. Now, practice leaving it alone. That means stop touching it with your tongue every 30 seconds to see if it's still there! Sure, it's nearly irresistible, but resist anyway. Every time you let your tongue sneak in there, you're bringing in a little saliva to float some loose and raising the amount you lose by swallowing.

This doesn't mean you can't swallow—you'll just have to learn to not let saliva float around the tab and then swallow. Yeah, saliva traffic management is the key (we are rolling our eyes to think that, yes, this is what taking hrt comes down to). With time and practice,you may learn such advanced tricks as drinking coffee without disturbing your tab (yes, we're talking very hardcore, here, plus years of practice). You will probably find that you cannot, however, swim laps with it in place or shower—even we will admit that there are limits.

What happens is that the tab moistens pretty rapidly into a sticky sludge, and that sludge is gradually absorbed into the skin until it is all gone. Then you're done. This generally takes about 20-30 minutes for complete absorption. If you taste a sweet taste, you've got it floating in saliva—you shouldn't be tasting it, because what you're tasting, you're losing down your throat and the digestive first pass effect will get rid of almost all of that for you.

In terms of dose dynamics, this route fits someplace between oral and other transdermal deliveries. You do get a single dose peaking and then falling, but because this effect is slower than when HRTs are swallowed, you don't lose a lot to first pass and trigger the demanding liver loads that seem to be correlated with the worst oral effects (clotting, cardiovascular, gall bladder).

But because it's not a trickle-type dose that enters your system continuously, like a patch, you do get peaks and dips. Some women are highly sensitive to this; others aren't bothered by it. One factor in women's ability to manage hormone levels through the day on a single dose seems to be related to how long postop/into menopause they are, suggesting that it takes some time for our bodies to accommodate to this new mode of managing hormone levels. According to one research study we've found on this (and it's a very small study, so should only be considered a hint, not irrefutable demonstration) and some further discussion of it on a site covering transgender use, sublingual estradiol created a higher, faster peak in blood estrogen levels than oral doses of the same compounds, and this level is predominantly estradiol for the initial two hours and then is mostly estrone (note that the discussion site focuses on just the estradiol dynamic). This represents the expected pattern of estrogen management, converting the surplus amount of active estradiol into estrone, the inactive form, for later use. In contrast, oral doses of estradiol are primarily estrone by the time they reach general circulation after processing in the liver. This suggests that women who find oral estradiol somewhat lacking might also get more active coverage from the transbuccal route, even leaving aside the first pass losses.

And it's very important to keep that increased activity and quantity of estrogen from the transbuccal delivery in mind when picking a starting dose. There is no table of bioequivalency, no conversion formula that states that if you are using so much of an oral dose than you need this much in transbuccal form. Alas. In fact, there is little general consensus on what this conversion should be in even rough terms, and we've seen recommendations for everything from 50% of the oral dose to only 20% of it. While the latter figure is somewhat borne out by typical progesterone doses, we're tending to see with estrogen that most women who have switched from oral to transbuccal Estrace find that around 50% seems to be a reasonable starting point. We tend to see women in surgical menopause using 0.5-0.75 mg per day, although the range has been from 0.25mg to 2 mg, (although we can hardly claim to have seen a definitive cross section of the population). This goes along with what few recommendations we've seen elsewhere as well.


About the only peril you need to watch out for specific to this route is if you should develop some persistent oral irritation where you place your pill. We've not heard of problems related to this use, but you are subjecting your oral lining to something a little concentrated and unusual, so it's good to keep an eye on the area for potential trouble. You might  have your dentist or oral hygienist take a look during your next dental exam as well. For the same reason, it's good to switch sides regularly and not to use a particular location if it has a canker sore or other injury nearby.

This is an off-label use, and as such may make your doctor, pharmacist, and/or insurance company nervous. Some women have their prescriptions written as though they're using it orally, just to avoid having to explain things, and that's something for you and your doctor to work out between yourselves; we're just pointing out potential stumbling blocks.

As with oral use of the Estrace generics, there can be a fair amount of difference in the dissolving/uptake times of the generics when taken transbuccally. This can affect both dose needs and uptake dynamics, although the most obvious impact is on dose absorption time and difficulty. In general, women's experience has been that brand name Estrace is the harder tablet with the slowest dissolution time, while the generics vary from one brand to the next with Watson of medium density and Barr towards the softer/more rapidly dissolved end of the range. Your pharmacist can help you keep track of the actual brand name you are using, so that you can keep track of which generic suits you best.

The good points

We've never heard of this route failing to deliver hormones to a woman's system. Sometimes the delivery dynamic doesn't suit a particular woman and she gives it up for that reason, but it does seem remarkably effective in getting hormones into us. It can also be used when we're sick, which is a problem with orals if we have a gastrointestinal virus. It's not likely that it will contaminate others around us when we use it, as some other transdermal forms might. It gets around whatever it is in some women's skin that makes uptake poor when using patches, creams and gels.

In terms of bang for the buck, transbuccal use of generic estradiol tabs (generic Estrace) is probably the cheapest HRT as delivered to the system. Please don't tell your neighborhood drug reps this—we'd hate to see these products taken off the market in favor of something more profitable expensive. As of this writing, 100 generic 1mg tabs are selling at major online chain pharmacies and such places as Costco for $10-20. If one were taking 0.5mg day, then, this would be 200 days' worth. And that can be a real boon for a woman with no insurance, little cash, and a burning hormone deficit.