gdwgar
#1445
I am new to this field and trying to understand the intricacies of dosing and assimilation of Rapamycin. It appears that 6 mg. once per week is an acceptable/common dosage. Why would 1 mg. per day 6 times a week not be better? It would seem to keep the level of the drug even rather than a high dose which drops off over time. Also what is the grapefruit juice all about? Reading thru this long thread it seems there is something about digestion/assimilation of Rapamycin going on that I can’t quite figure out. Any helpful summary of this information would be much appreciated by this newbie and others I am sure. Thanking you in advance for your helpfulness.
1 Like
Bicep
#1446
It’s really tough to prove what works best for human longevity. Randomized controlled trials are pretty much not going to happen. Much of the good info comes from organ transplant patients and many of them use it daily. You need a trough every couple weeks in order to keep from inhibiting complex 2. Some people think a high maximum is good because it crosses the BBB better and does some good. I pretty much double it and go every 2 weeks. You can do whatever you want, but I watch lipids and fasting glucose pretty close because when I use too much that’s what happens. If you don’t have side effects then maybe you can use more?
Grapefruit juice inhibits cyp3a4 in the gut and keeps it from breaking down the Rapa. So you only need to take about 1/3 as much. This saves money but is probably less accurate. I don’t mind the dose varying since I don’t really know how much to take anyway. In the beginning it saved a lot of money, when I was paying $3/mg but now it’s under a buck and doesn’t save so much.
Good Luck,
3 Likes
Agetron
#1447
Hey John… straight rapamycin… sirolimus… zydus… all …1 mg of the drug produces… typically 3 ng/mL in the blood.
Matt Kaeberlein shared his numbers post dose… was same as did @LaraPo I think… she was getting 1 mg daily and a 3 ng/mL reading.
1 Like
Agetron
#1448
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.
2 Likes
LaraPo
#1449
Yes, it’s correct. 3 ng/mL @1 mg/day.
1 Like
I recommend you read our FAQ (frequently asked questions and answers)… Rapamycin Frequently Asked Questions (FAQ)
Specifically, with regard to the questions you mentioned:
3 Likes
gdwgar
#1451
@RapAdmin Thank you for posting these threads. I had not found them yet and they are very helpful.
Nlo
#1452
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?
PBJ
#1453
Do not split them. The tablets are esoteric coated, and the bioavailability will go to almost zero if split.
4 Likes
Exactly. If you ruin the coating, the bioavailability is ruined and you might as well throw them away.
4 Likes
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.
2 Likes
Maulik delivered again. Shipped 3/10 arrived unopened 3/18. Small box with 350 pills with only foil packs included. 8x5x2 inches approx.
6 Likes
For me too maulik delivered me 120 rapacan 240 brillo ez and 120 safinamide in just 13 days to Montréal canada.
2 Likes
Got the letter from the FDA regarding my package from Maulik They seized it.
The crazy thing is, I didn’t order most of them only numbers 2, 3 and 8! I didn’t order Ivermectin!!!
I ordered Bempedoic Acid, Galantamine, Imuniquod cream, doxycycline and dutasteride only.
Maulik told me the FDA was seizing all shipments with Ivermectin, so I wonder if that was the cause?
How do I even proceed with this???
Maulik says it’s the wrong shipment as some of these drugs he doesn’t even sell.
1 Like
amuser
#1459
Get a district court judge to reverse the decision.
My latest Maulik order arrived in 6 days. Amazing!
5 Likes
Hi - curious if you provide option to ship to USA?
FWIW: email from Maulik
"Just to inform that Mounjaro (Tirzepatide) from Eli Lilly is officially launched in India.
You can post them on the forum if someone is interested.
Please find the prices for same as below
Mounjaro(Tirzepatide)2.5 mg / 0.5 ml vial - 40$
Mounjaro(Tirzepatide)5 mg / 0.5 mg vial - 50$"
2 Likes
Doesn’t these GLP1’s have to be refrigerated? Doesn’t that pose a shipping problem? Could you please repeat Maulik’s email? Thank you
