Yes… as @Bicep stated… you need a break of the medication in order to balance cleaning and growth … the autophagy of rapamycin dose cleaning - repairing the cells… so with 6 mg… you get benefit of cleaning… as half life… by half life it leaves the system in 3 to 4 days… then you get growth for 3 days… cycling the cleaning/catabolic and growing/anabolic.
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Yes, it’s correct. 3 ng/mL @1 mg/day.
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I recommend you read our FAQ (frequently asked questions and answers)… Rapamycin Frequently Asked Questions (FAQ)
Specifically, with regard to the questions you mentioned:
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This may be a bit off topic, but it seems like there are lots of wise folks discussing the absorption and formulation issues on this thread. My question is whether there is any known reason that I should not split a Rapamycin pill? I buy rapa from CVS, so it is an approved generic. I have two mg pills and I want to increase my dose to 3 mgs, hence the need to split a pill. Any major concerns?
Do not split them. The tablets are esoteric coated, and the bioavailability will go to almost zero if split.
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Exactly. If you ruin the coating, the bioavailability is ruined and you might as well throw them away.
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More precisely, we don’t know what the coating is. We used to think it was enteric coating, but more recently that was thrown into doubt, and it’s not clear (at least not to me!) what exactly is the coating and its effect on bioavailability.
Furthermore, we know one statistic which came out of the PEARL trial: compounded rapamycin pills, which didn’t have any specially engineered coating was about 1/3 as effective a dose as a coated brand name sirolimus from the pharma company.
From this we may conclude that IF there is some special coating designed to enhance/preserve the bioavailability, and you now split the pill thus obviating the coating, you are probably getting one third the effective dose of rapamycin. Not zero. So, if you aimed for two pills of 1mg each, you got two pills of 0.3mg each of rapamycin.
However, I am not at all satisfied with the lack of firm conclusions in this matter. Because thinking about this issue, I see another possibility. We must assume that the generics cannot deliver only 0.3mg of an effective dose of rapamycin, because that would really mess with the effectiveness of this drug dosage in transplant patients, which would swiftly draw the attention of the FDA. However we also know that coming up with a good coating that guarantees full bioavailability is neither trivial nor cheap - it certainly raises the cost of the pill for the manufacturer, and we know how much those generic manufacturers hate to spend extra. That leaves another, rather simple solution. The generic maker might simply boost the dose to compensate, and put 3mg in a pill with any old cheap nothing special coating/film and label it “1mg”, because that’s what the effective dose would be. And rapamycin in bulk is very cheap for the generics maker. Now you can freely split the pill because you will always get the effective dose regardless - this would explain why the Biocon 1mg pills are scored in the middle implying that you are free to split them - it really doesn’t matter if you split them; you want a 0.5mg effective dose, no problem, after splitting the 1mg pill in two, you get two 1.5mg pills each of which has a 0.5mg effective dose - there you go, problem solved! Obviously I’m totally speculating - until we have actual knowledge, we simply don’t know.
But I for one would not risk splittng the pill. You might end up with only 1/3 the effective dose. YMMV.
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