Rapamycin and Grapefruit Juice

The manufacturer is Biocon. They are 1mg, white tablets with score mark down the middle. They are in blister packs, 10 pills per pack. I do see that it says the tablets are film coated. I don’t know if that coating or breaking tablets in two effects bioavailability. Thanks for the heads up on dosage and tablet coatings. I will not break the tablets in the future. Until I can get a rapamycin test, I’ll stick with 2mg + GFJ.

My dosing so far has been as follows:
6/26/23 - 1mg
07/3/23 - 2mg
7/10/23 - 4mg
7/17/23 - 5mg
7/24/23 - 6mg
7/31/23 - 3mg + 8oz GFJ
08/7/23 - 4mg + 8oz GFJ
8/14/23 - 3.5mg + 8oz GFJ
8/21/23 - 2.5mg + 8oz GFJ
8/28/23 - 3mg + 8oz GFJ
9/05/23 - 3.5mg + 8oz GFJ
9/12/23 - 3mg + 8oz GFJ
9/20/23 - 2.5mg + 8oz GFJ

Here’s front and back pics.

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I second this. You don’t want to break the coating. It defeats the purpose as it greatly reduces bioavailability.

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Oh and I looked back in my email and found the company I worked with was G.P. PHARMA INTERNATIONAL on IndiaMART. The process was a bit convoluted for me, never having used WISE for international payment, but it was doable. The item was received within 2 weeks.

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OK Thank You. I broke coating in 4 out of 13 doses. I will not waste any more of the pills by doing that!
Actually, silver lining is it kept my rapamycin blood level a bit lower.

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What is the rationale for going from low dose to high dose and then back, or just trial and error? any paper on it?

I tend to feel best when I do 10 plus GFJ, plus I get no side effects with this dose, all other from 1-5 with GFJ i get minor side effects. I am thinking of switching to biweekly though. Question wouldn’t taking acarbose take care of the elevated fasting glucose, or not related?

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Acarbose has not worked that way for me. It blunts the glucose spike from a meal with carbs, it makes SCFA which is no small deal, but it does not help my fasting glucose.

The pioglitazone does not work for that either. I hoped it would, but no. I still take it for other reasons.

The flozins do work for me. Empag or jardiance works at 25. It makes me pee a lot, which is not a great big deal on the farm, but I still find it annoying and have to get up in the night, also annoying. I just got dapagaflozin and it’s amazing. No side effects and works like a charm. My glucose was 79 this morning.

I take 1000 berberine also and have for years, It doesn’t work for fasting glucose either.

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Are you saying that dapagliflozin doesn’t make you need to pee at night? Or just that there are no other side effects other than that?

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I’ve taken it only 2 nights in a row now and I don’t have to get up. Also not a bother during the day. It’s a miracle so far. FG was 82 or something then 79 this morning. Perfect.

I like it better so far. Got it from Jagdish with my last order. Called forxiga 70 tablets for 31 dollars so not really cheap.

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Maybe I should have added that I take it first thing in the morning. My reply made it sound like I take it at night.

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Not an expert by any means, but is it a drop from 82 to 79 really that significant?

No, it would be probably 100. First night was 82 which I consider perfect. Next night was 79.

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got it !

Thanks, for the info. None of the other “flozins” have done anything. I seem to be stuck at ~100. Maybe it’s just age and/or rapamycin. I am going to try dapagliflozin and hope for similar results.

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Hey… yeah, just trial and error. Did 6mg rapamycin for 1.5 years. Then, tried 8mg -12mg for a few months… and 36 mg for 7 months. High dose was bad on my biological markers

Dropped back to 6 mg last December 2022. Biological markers improved greatly.

So thinking alternating 6mg… 12 mg…every other dose.

Will have new biological marker tests on the new dosage soon. Will share.

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As promised here are my Labcorp results on sirolimus/rapamune - I take rapamune.

Blood was drawn on Sept. 20, 2023 at 8:19 am my rapamune trough was 1.2 ng/mL considered low.

Blood drawn 11:49 am – 2 1/2 hours after a dose of 6 mg and juice with pulp of 1 Red Grapefruit about 5 fl. ounces. C-max 33.7 ng/mL much higher than I like.

I am consistently getting a 6x’s increase in my dose of 6mg and GFJ.
Definitely going back down to just 2mg and GFJ to get approx. 12 ng/mL I think this is my dose sweet spot.

I am a firm believer that the higher dose of rapamune 30+ ng/mL actually blunts my biological benefits, as shown on my previous GlycanAge and TruMe tests.

Will have my latest GlycanAge and TruMe tests back in 3-4 weeks. Will post my 2 and a half years graphs of both.

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Thanks for that detailed information. That’s Impressive. Two questions:

How are you calculating that you are getting a 6 x increase from your grapefruit juice? What is the standard you use?

How do you explain the 6x results? Is there something unusual you are doing in preparing the grapefruit? For example, do you eat the sections? Juice it? or peel and vitamix the pulp as I’ve been doing, (which adds a bit of the rind). How long do you wait after the gfj before taking the rapamycin

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I can share my results with pfizer rapamune taken with water, 6 mg, tested some two hours later and my result was 14 ng/ml. I know that we absorb and metabolize rapamycin quite individually, but per this result @Agetron is probably getting the estimated around three fold absorption. When I got the test I wasn’t really planning on doing it, but I was at the clinic getting some other tests my doctor ordered and I jokingly asked if they do sirolimus test and they said yes and took another vial of my blood for that. I will do another more comprehensive test in few weeks, am planning to test without and with GFJ and second test with one of the pharmaceutical CYP3A inhibitors (itraconazole or ritonavir) and measure it at 24 and 48 hours to be able to better estimate half life and AUC per @Olafurpall suggestion in another topic a while ago. Cmax is not that important in my opinion, since higher Cmax might be needed to get to some tissues, but I am more oriented towards testing how long rapamycin is inhibiting mTOR… how long autophagy is stimulated.

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Hey Chuck - How I come up with a 6x’s increase is:

My rapamycin trough (low point in my blood) with a blood test was at 1.2 ng/mL typically you want 1 or under before your next rapamycin dose. So basically the rapamycin has worked its way out of my system. Takes a week for low dose (5-6 mg) or maybe 10 days for a higher dose (10-12mg).

Next, I took a fresh Red Grapefruit (bought at Wal-Mart) - cut it into quarters and squeezed the slices into a bowl. Gives you about 5 fluid ounces of juices with some pulp. Used this juice to swallow 6mg rapamune (for me that is 3 pills 2mg each). waited 2 and half hours and retested my blood (a blood draw). That gave me my c-max/t-max top dose in my system. In my case 33 ng/mL… so just under 6’xs. Make sense?

It requires doing two blood tests the same day – first a trough. Then, take your rapamune dose and retest 2.5 hours later.

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Agree, but if after a week of 6mg or 10 days at 12mg you are at a trough of 1 or less you can be fairly confident that your MTOR inhibition is declining normally from your dose. So for me - that trough is an indication of clearing. I want my max numbers and bottom/trough to be in sync.

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