Rapamycin and Grapefruit Juice

Like your spunk.

I have been on 6mg 1.5 years with great results. Now looking to taking a 20 mg weely dose using GFJ…8mg pill and GFJ. Been doing that 2 months… certainly get the diarrhea for a few days at that dose. Getting it figured out and under control tho.

Then with higher dose of 20mg…checking my Glycans in 6 months and DNA methylation… to see how it compares to past year’s tests.

As to LDL-C in my case is 167 .Ummm… 130 is high normal.
My coronary calcium score from CT scan… is zero… nada… technician says my heart is younger than 35 years. So for me LDL-C isn’t an issue. Curious to see my latest LDL-C score on Monday. Been high since I started getting it tested at 40 years. More soon.

As good a place as any for my “Friday Rant” This is my chosen manifesto and until someone proves otherwise, the path I choose to follow.

Two patients developed symptoms probably related to sirolimus overdose: mild elevation of alkaline phosphatase, fever and gastroenteritis in a 2.5-year-old male who ingested 3 mg, and mild changes in total cholesterol in an 18-year-old female after ingestion of 103 mg. None of these events were life-threatening.

“If used properly, rapamycin is not much more dangerous than ordinary aspirin.”
I totally disagree with this. Aspirin is much more likely to kill you than rapamycin

“rapamycin’s LD50, a measure of drug lethality, could not be determined because it is higher than 2500 mg/kg.” (Which in my case would amount to 17,500, 1mg tablets.)

"At low doses [8,9,86], or when administered as a single high dose [103], no side effects have been detected so far in the elderly. (Well, they didn’t try 20 mg with grapefruit juice.)

Please if in doubt follow the many references Dr. [Mikhail]V. Blagosklonny provides at the bottom of the article.

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@agetron @desertshores

The reason for my recommendation to do a Sirolimus blood test:

  1. Are you even taking rapamycin/Sirolimus?

  2. There is HUGE inter-person variability. Two people taking the same dose can have massively different pharmacokinetics/absorption. “The inter subject variability in clearance (CLpo) was large
    and was suggested to partially result from an elevenfold variation in the intestinal content of CYP3A4 enzymes that have been observed among individuals based on small intestinal biopsies

  3. Are you dosing sufficient to even get a good enough trough level to be a meaningful signal? Say at least 3-5 ng/L, lower band limit? (Conventional therapeutic dosing control is 5-15 ng/L trough). All the transplant/cancer data in humans…trough is correlated with AUC, which if we’re trying to slow down cancer pathways (ie mice translation), is likely very important therapeutic monitoring requirement. “RAPA, at trough concentrations as low as 0.5 mg/L, prolonged graft survival compared to controls. However, long-term graft survival was only achieved in
    animals having mean trough concentrations of 9.3 +/- 5.4 mg/L” (1)

(1) Sci-Hub | Rapamycin: distribution, pharmacokinetics and therapeutic range investigations: an update. Clinical Biochemistry, 31(5), 345–351 | 10.1016/s0009-9120(98)00048-4

I have no idea what should be the longevity dosing protocol re Siromilus pharmacokinetic signal.

One of the only guiding principles is from Dr B “take as much as you can tolerate”, with my caveat, with likely a MIN trough level.

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“One of the only guiding principles is from Dr B “take as much as you can tolerate”
That’s my mantra.
I have titrated up to the point of undesirable side effects then backed down.
The complete clearing of my actinic keratoses and the “essential” age-related tremors, plus my general sense of well-being is enough to convince me I am getting a therapeutic dose.
There is enough evidence that the two-week dosing protocol is enough to ensure that I don’t depress my immune system.

I have no problem if someone wants to take the test per se, but I don’t think it is meaningful except under the supervision of a qualified doctor who can interpret the results in relation to the person taking it.
Locally only Lab Corp is giving the test and is completely unreliable on the time you are seen, so no chance about peak dose info and I personally don’t care about trough dose info on the bi-weekly protocol.
And yes, I am sure I am getting sirolimus. Many of us are using the Zydus brand from the same source in India and some have taken blood tests to insure the efficacy of the product.

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What did you think of Rapacon? What was the reason for the switch? I ask because I just ordered 100 pills from Jagdish and ordered a couple tests from life extension and wondered whether I should use that on the test or the stuff I get from Wal Mart. I don’t even know what they use.

As I posted earlier, I had no problem with Rapacon. I took it for several months before I switched to Zydus. Two outdated tests show Rapacon had slightly less rapamycin per tablet ~1 or 2%, not enough to worry about. The Zydus tablets have slightly fewer filler materials. Again nothing I would worry about.

See tests on Zydus and Rapacon here: Rapamycin / Sirolimus from India, Lab Test Report on Quality / Purity

Jagdish supplies either brand. The cost of rapamycin from India is so extraordinarily cheap when compared to Pfizer or compounding pharmacies that I didn’t mind paying a little more for the Zydus tablets.

BTW, I was paying Jagdish with bank transfers from Wise.com, but they say they no longer support transfers to the Niba Healthcare account.
May I ask how you paid Jagdish?

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My rapamycin/sirolimus physician prescription is the real deal from Accredo Pharmacy - 30 pills 2mg each – delivered by mail on schedule every month.

Still… I think it is a good idea for a LabCorp test to absolutely know I am getting good Rapa.

I can actually control my blood draw appointment - my total work up 4-5 vials of blood every 3-4 months (paid by my insurance), getting a true blood draw at 3 hours by just taking my rapamycin in advance of my scheduled appointment.

I changed my normal schedule of taking my Rapa before bed to get a c-max reading blood draw – just for this blood test. Then back to my old schedule.

As MAC says - I have no idea what should be the longevity dosing protocol re Sirolimus pharmacokinetic signal.

At 6mg for 1 1/2 years I have seen great improvement - skin, memory, swallowing, resistance to allergies, general great health. My biological glycans are 37 years. DNA Methylation 51 years.

Over the last 6 months been doing 8mg/ 10 mg a few months and last 3 months with GFJ boost approx. 20mg. With this dosage can I hold at my biological age for 37 and 51 years a bit?? Or even push biology back a few more years? Will know in 6 months at this dose.

I am looking at trying to hit about a 20mg + dosage per week to see how my biological age testing looks in 6 months and see if no negative effect on diminished muscle tone/strength. The current 8mg Rapa pills with 8 ounces of GFJ has produced mild diarrhea a few days. Taking Pepto Bismol pills 24 hours post Rapa medication should remedy this in the future. I should have the LabCorp Sirolimus level results on Monday to know how much of a boost my 8mg gets with GFJ.

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Wow, 20mg+ per week with GFJ? That certainly beats the max bi-weekly dose I used.
Let us know how that goes. With that dose, I would have constant diarrhea.
I wonder if the body would adapt to the high doses and if diarrhea would go away.
As far as I know, you will be the max dose pioneer in this forum.
Good luck we will be watching.

No… no… 8mg pills taken with 8 ounces GFJ - would put me at a total 20mg-ish! Certainly within current standards for many on this forum. Hahaha!

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Until we know more, you are doing everything “right” re standard generic translation dosing titration playbook. Applaud all your biometrics tracking.

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Yeah, I tried Wise and they said no. Went to the bank and they wanted $60 to wire it so I went with “pay with indiamart” credit card link. That cost $15 but was no fuss at all.

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Probably could buy 300 pills and still the cost would be $15 for the Pay with Indiamart safe gateway.

My goal would be new users now – and those that come after me – in their 50’s can follow the same road map with similar results.

Plan to keep at it and cautiously push the envelope for maximum age reduction and regeneration of organs. My results from 2-years of using rapamycin is pretty phenomenal. The Rapamycin.news collective has greatly added to my understanding of this miracle pill’s potential and information on effective dosing and activity. Wouldn’t be surprised to hit 100 in great health and shape.

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Just took my first dose of 1 mg of Rapa with 3 grapefruits (1 night before, 1 3 hours before, 1 1 hour before). I have developed a weird side effect. Meat and eggs nauseate me. I just can’t imagine eating them. Has this happened to anyone else? I did have a nice sausage with the Rapamycin before the effect set in.

P.S. Do you guys just take the pill or do you mix it with EVOO?

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I take my rapamycin with a can of sardines to get the high fat benefits of increased bioavailability.

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So then I should take it with my EVOO in the morning. :slightly_smiling_face:

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Yes - with the rapamycin in the morning (for those of us who find late-day rapamycin tends to hinder sleep).

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I have developed a weird side effect. Meat and eggs nauseate me.

Hmmm… I would think Grapefruit would be nauseating at that point. Lol.

I use to do that much Grapefruit and really messed with my digestion and puked.

Now going with 8 mg Rapa and just an 8 ounce of GFJ chaser… when I take the pills. Will have the results of that combo effect from a LabCorp test on Monday… will report here.

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Actually, I really enjoyed the grapefruit. It was pink, so it tasted much better IMHO.

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I kind of got a real surprise on my LabCorp Sirolimus/Rapamycin blood test. My blood was drawn 3 hours after taking 4 pills of sirolimus at 2mg each = 8mg total and 1 cup which is 8 ounces of Simply Grapefruit juice.

Figuring at 8mg Sirolimus with a 3.5 multiplication by the Grapefruit Juice - I anticipated 28ng/mL.

In reality I got a 56.9 ng/mL reading and an Alert from the LabCorp to my physician. He notified me to stop taking sirolimus until I get to 20 ng/mL.

I had not expected a multiplication factor of 7 on such a small amount of GFJ which I literally took to wash down the four 2mg pills. So a heads up to everyone taking GFJ to extend their medication and get a higher dose in the blood. You can’t know what your blood level of sirolimus is unless you actually test yourself. In my case, I tend to run higher – no wonder I couldn’t sleep for two days and the diarrhea. LOL. I was lookingfor my peak. So good to do a test to know where you are at.

I will see my physician in 2 weeks and explain what happened. So tonight is my rapamycin night after gym… I might be able to take just 2 pills and the Grapefruit Juice to hit my 20+ goal. When I see him in 2 weeks… I will do a blood draw on 2 pills and GFJ and prove to him I am keeping it around 20 ng/mL

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