People pushing the upper limits of Rapamycin Doses - Any One Else?

[L_H]

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

[Agetron]

Yes… approximately from April 2022 until end of November 2022… 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 130’s to mid- 150’s. With pulse up to 100… normal pulse 72

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

On dose day…and the next day can feel my heart racing… beating through out my body… in my arms and chest and head… and ringing in ears.

[DeStrider]

Take care buddy! Those don’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.

[Agetron]

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 didn’t seem to affect anything - workouts, no headaches… 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.

[Jacob_F]

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 (I’m an actual diabetic) and was not sure which drug to attribute the great result to.

[Robsabi]

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. Green’s admonition was probably to prevent people who either didn’t know about the effect of grapefruit juice, or hadn’t put the required research and thought into it, from going “gonzo” with their Rapamycin dosage.

[Maxi]

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

[Jacob_F]

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

I’m in the same demographic targeted in those studies. I’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.

I’m open to any feedback from the community.

[DeStrider]

That’s a valid protocol. However, we really have no idea at this point which dosing strategy is optimal other than ‘It feels right to me’. 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.

[John_Hemming]

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.