CastratedTomcat (imported) wrote: Tue Jul 12, 2016 12:41 am
Better way is, you lay the tablet under your tongue and leave it there.
So the Coproterone is going more directly in the bloodstream without the way through the liver.
Is cyproterone acetate capable of sublingual absorption? I know a lot of things need to be micronized and such. Some chemicals just won't do it properly. For example estradiol hemihydrate (estrofem) can be taken sublingually but estradiol valerate (progynova) will not absorb properly that way, and will wind up just getting swallowed in your spit. If not micronized correctly many chemicals come in too big of particles to be absorbed properly through the membrane of the inner gums, lips, under the tongue, etc. and into the blood stream. Micronization increases the efficacy and can enable proper sublingual absorption of certain chemicals. If the chemical cannot pass through in sufficient amounts, it'll all wind up just being orally (in the digestive system) absorbed.
Also if I remember correctly actual brand-name Androcur is made with an outer layer of compressed chalk with a smaller central area containing the actual cyproterone. I really wish they did that with spironolactone, anyone who has tried it knows how bitter and horrible it tastes. This makes me wonder how cyproterone tastes, seeing as all I've tasted so far is nothing, seeing as it's just chalk touching my tongue. A quick online search has yielded responses of "it tastes horrible" but I don't know. One person reports "Androcur tastes like really bitter asprin/advil."
That said I do take it after a meal or with a glass of milk. Can't hurt to have some food in there, granted the leaflet that comes with Androcur says to just take it with water orally, so I don't think it really would matter. This stuff is pretty potent. But if it is actually being absorbed sublingually then eating anything beforehand would not matter all that much.
If it really does work sublingually and is able to diffuse into the epithelium and enter venous circulation, and also works in the proper way without additional risk, that would be great and I'd totally switch to sublingual administration, unless it tasted bad enough. TBH if it's as bad or worse than the spiro taste I'd rather wreck my liver. It's too bad the information on sublingual administration of cyproterone is scarce. I can't find any medical or scientific sources saying that it can work sublingually, in addition to exactly how it works when taken sublingually. One thing to note is that this could -definitely- affect the half-life of the drug in one's system. IIRC it would likely decrease the half-life, which would not be a good thing. Different dosing amounts and times might be required to make it work properly sublingually, if it absorbs that way at all.
Furthermore the liver metabolizes some of the cyproterone acetate into cyproterone and acetic acid. The cyproterone alone is not as effective at blocking androgens as cyproterone acetate is. CPA (cyproterone acetate/androcur) is three times more potent as an antiandrogen than cyproterone. Meaning: if sublingual administration is effective, then your dose will be a little more potent in regards to anti-androgen effects. I don't know how much of a factor this could be but it could potentially weigh in - this isn't the only thing that happens to cyproterone acetate in the liver either. There are other enzymes that effect it in the liver and alter portions of it. The major active metabolite of CPA is 15beta-hydroxycyproterone acetate which circulates at twice the concentration of CPA. This is a big deal because 15beta-hydroxycyproterone acetate has the same antiandrogenic activity as CPA yet only 10% the activity as a progestogen. This means that if sublingual administration works, and leads to mainly just a concentration of pure CPA in circulation, then taking the same dose may yield vastly increased progestogenic activity, which I imagine our friend here, experiment, might not want. It might even be dangerous to do. I don't know. Androcur is already a potent progestogen - probably not a good idea to make it vastly more potent as one.
I don't think it would be wise to try sublingual administration without first getting the go-ahead from a doctor. It could be a -really bad- idea, it could be pointless, or it could be beneficial but that's one huge risk. Either way the dose would almost certainly be affected. Those dosages were set with it in mind that people would be taking this medication orally, not sublingually. I imagine different dosages would be required for sublingual administration. Perhaps there is a really good reason why the instructions only mention taking it orally.
One may say "AHA! But cyproterone acetate can be injected intramuscularly!" but to that point, some metabolism occurs in the muscles themselves. For sublingual, and IV administration, the drugs are taken to the systemic veins, then to the heart. Some of it will wind up in the liver, but it will have plenty of opportunity to be carried to all of your other tissues without ever touching the liver.
Maybe it does work sublingually and maybe it does help out a lot. I couldn't possibly say for sure. I'm no expert. But I think that it would be best to err on the side of caution on this one, unless told by a doctor that sublingual administration of Androcur is okay.