#161

Hi Agetron, sorry for asking another wuestion. Was that 6mg with gfj?

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#162

Yesā€¦ approximately from April 2022 until end of November 2022ā€¦ I was taking 6mg in pills and one fresh red grapefruit that I would hand squeeze and take with pills.

Side effects seemed to be elevated Blood Pressure went from lower 130ā€™s to mid- 150ā€™s. With pulse up to 100ā€¦ normal pulse 72

Watched it this way for monthsā€¦ figured it was rapamycin. Since dropping my dose to 2mg with grapefruit juiceā€¦ approximately 12 mg in my blood. B/P and pulse back in the normal range.

On dose dayā€¦and the next day can feel my heart racingā€¦ beating through out my bodyā€¦ in my arms and chest and headā€¦ and ringing in ears.

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#163

Take care buddy! Those donā€™t sound like good side effects! Ringing in the ears and higher BP may have cardiac effects.

I am taking 5 mg + GFJ, biweekly and I have noticed my wound healing has really slowed. I have a blister on my finger and it is taking a much longer time to heal than in the past.

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#164

Thanks Chris,
I do monitor pretty consistently - even do the Blood Pressure Check next to the Walmart Pharmacy - every time I am in the store.

All very stable - even when my B/P was higher - it didnā€™t seem to affect anything - workouts, no headachesā€¦ plenty of energy. But, yes - glad to be back in the 127-134 range systolic and 72 to 80 diastolic From charts I am in the.60 to 64 years minimal 121/83 normal 134/87 range.

The ear ringing or tinnitus goes away a day or two after my dose. Just very strong initially. As rapamycin is suppose to help hearing - I do not mind it. My hearing is excellent.

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#165

I have had a similar result. I use a weight belt at the gym and have shrunk out of my belt while getting stronger. I also dropped from size 36 jeans to 34. I think I last wore 34 when I was 16. I started taking Rapamycin around the same time as Ozempic (Iā€™m an actual diabetic) and was not sure which drug to attribute the great result to.

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#166

Grapefruit juice, at least if taken only when taking rapa, and not dosed daily, primarily inhibits CYP3A4 in the entrocytes (i.e. the gut) and not in the liver. So, it primarily increases the amount of rapa that is absorbed from the gut, not the processing by the liver once it is absorbed (including not significantly affecting first-pass metabolism).

Therefore, it would be expected that taking Rapa with grapefruit is essentially the same as taking a higher dose of Rapa. I.e., say that grapefruit juice at the time of taking Rapa results in a 3x levels. So, whether you take 6mg Rapa, or 2mg and grapefruit juice, the result should be the same. The same amount would get into you, and then would be processed at the liver and excreted at that same rate.

I always assumed Dr. Greenā€™s admonition was probably to prevent people who either didnā€™t know about the effect of grapefruit juice, or hadnā€™t put the required research and thought into it, from going ā€œgonzoā€ with their Rapamycin dosage.

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#167

GPJ affects 3A4 both in gut and liver, but less so: Exposureā€Dependent Inhibition of Intestinal and Hepatic CYP3A4 In Vivo by Grapefruit Juice - Veronese - 2003 - The Journal of Clinical Pharmacology - Wiley Online Library

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#168

Folks, Iā€™m planning to try 28 days of 2mg EVERY OTHER day. Iā€™m inspired by the recent papers from Ai-ling Lin that involved daily doses of 1mg for 28 days. Iā€™m doing 2mg every other day because. . . well, because I only have 2mg pills.

Iā€™m in the same demographic targeted in those studies. Iā€™m late 50s and am an APOE-4 carrier.

I typically dose Rapamycin at 6mg w/ GFJ every other week. If often take a month or so off at random intervals. I skipped the last dose and figure that I will do this 28 day dosing strategy and then lay off again. Somewhere around the end of week 2 I will get a Labcorp test to see what my blood levels of Rapamycin are. Maybe I will do that again at the end of the 4 weeks.

Iā€™m open to any feedback from the community.

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#169

Thatā€™s a valid protocol. However, we really have no idea at this point which dosing strategy is optimal other than ā€˜It feels right to meā€™. I believe that by mixing up the different dosing strategies, we will simultaneously hit on the optimal and the suboptimal.

Of course gut-wrenching pain, diarrhea, or an outbreak of itchy hives may help inform us that we have not chosen an optimal dosing regimen. :wink:

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#170

I am in the faction who believes that mTOR should not always be inhibited. Hence I go for probably the least frequent dosing, but also possibly the highest peak.

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#171

Hi, I have been reading this post because I have been on 14 mg/week to improve ME/CFS symptoms Rapamycin for Chronic Diseases (ME/CFS,IBM,Fybromalgia,Others) - #25 by Maxi
but I got no benefit. One of our colleague felt better at 36 mg (although his dosing has been a matter of controversy because of formulation) Rapamycin for Chronic Diseases (ME/CFS,IBM,Fybromalgia,Others) - #18 by hamtaro
so I started to increase and I am at 25 mg. During the time at 14 mg I measured pik values twice:
Pik 3 Curves 14 mg Feb March 2025.pdf (90.1 KB)
This was with standard Rapamune Solution 1mg/ml as available from Pfizer in Switzerland. I took it without food nor GF or any other booster. Your comment above implies that 68 ng/ml is very high ? Maybe the solution is very bioavailable ? I have not yet measured pik at 25 mg. Any info on pik values and bioavailability of solution/pills or other advice would be welcome. Tnx.
P.S. I also determined my kinetic, Half Time ca. 45 hrs
Exponential_Decay_Report_Compact.pdf (128.7 KB)

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Rapamycin Update in 2025
#172

I take a higher dose than you, but much less frequently. I would worry about mTOR being always inhibited.

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#173

Tnx, I do worry, but life with ME/CFS is pretty bad and makes you take risksā€¦I console myself with the thought that I am below 4 ng/l after 3 days, and this is the therapeutic lower level for transplants. Also I do blood panels with my immunologist every two weeks for safety, the only negative is a decrease of hemoglobin. The only other thing I had is a mouth ulcer in february when I started, none since. I am moving to 14 days as I plan to go to 30 mg. Fingers crossed.

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#174

He looks bad for 9%.

#175

What does this mean and what evidence is there for this comment?

#176

The OP.
Charles Nelson, 52

At 9%, he should look much better. He looks soft and flabby with barely a vein in sight. Kinda like a 14-year-old couch potato.

#177

Late to the game but those pills have no enteric coating (not sure if anyone has mentioned this yet) so while the GFJ amplifies, the lack of coating does the opposite. It might be a wash. Also, his body fat % comes from an impedance scale which is known to understate fat %. Heā€™s got quite a bit more than 9% body fat.

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#178

Enteric coating has no effect, the issue with bioavailability has to do with solubility which requires nanocrystals etc.

#179

I donā€™t know about that. That rapacan heā€™s showing there is about the same as siroboon. He might need all the GFJ he can squeeze out of that big ripe one to get all those pills to show any significant amount of sirolimus in the blood.

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#180

That could be riskier than just using a proper brand: Grapefruit associated with increase in all-cause mortality

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