brand
#212
How many would it make sense to eat? 1, 1 hour before? or some other timing, quantity?
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Timing wise, the sweet spot seems to be 1 to 3 hours prior (see graph below - still looking for the best graph - this will be updated when I find it):
Two Major Grapefruit Juice Components Differ in Time to Onset of Intestinal CYP3A4 Inhibition
Above source: https://www.semanticscholar.org/paper/Two-Major-Grapefruit-Juice-Components-Differ-in-to-Paine-Criss/56dc1541c420203ad28682f31b763e44abbb5b72
Dosing is much more difficult because of the different levels of furocoumarins in different types of grapefruit, and variations within individual fruits…
See: What types of grapefruit juice increase Rapamycin levels the most?
Dose / response:
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It is easier to get GFJ plus I hate grapefruit… I take 250ml 3 hours before then 250ml 2 hours before and 250ml 1 hour before. Gives the most rapamycin for me from the blood test… I wish I can just drink them all at once but I can’t.
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brand
#215
Does it matter if you eat something else or should it be just grapefruit and during which period before and after taking 1mg.
Red or yellow grapefruit?
If you were taking 1mg weekly what would be something like an optimal number of whole grapefruits, timing and type of meal to mimic 6mg dosage:
e.g
Eat the usual diet during the day.
Take 1mg w large fatty meal after eating 1 grapefruit an hour before?
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Bicep
#216
I think it’s easier to use Simply Grapefruit, which is juice sold at walmart and target. It probably comes from a variety of grapefruit and I would think more standard and consistent. Also easy to chug with the pill. I have a pint, though I think it’s probably overkill. I think the fat helps too, I use coconut butter or olive oil.
I always used to have it in the morning, then tried it last thing at night (like many others here) and discovered it really helps get a good night’s sleep. So the last couple months I’ve done it that way.
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Good questions, but I’m not sure I have a good answer.
I’ve not seen any studies about impact of other foods at the same time as the grapefruit. I suspect it doesn’t have a huge effect. The addition of some fatty food (I have eaten sardines, others here dose with a shot of olive oil) will increase another 30% the bioavailability. Other foods I don’t know for sure, positive or negative. See our list of interactions here: Rapamycin Interactions with Other Food, Drinks, Supplements and Drugs
We have a long thread on grapefruit and rapamycin at this link, I think it covers some of the research on different types of grapefruit and which are most impactful of CYP3A4. Rapamycin and Grapefruit Juice
There has not been that much research in this area to identify the exact mix to increase the bioavailability of 1mg to make it equivalent to 6mg, but I suspect the most reliable way is to actually take 2mg with grapefruit juice, given the research in the first post of this thread about the 3.5 X multiplier effect of the grapefruit juice they measured. That should get you in the range of 6mg effective dosing. But there are many variables (you don’t really know how “potent” any given grapefruit is without testing), etc.
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We may have overlooked citrus bergamot extract which contains “bergamottin”
which is the main active component in grapefruit juice.
Taking “Citrus Bergamot Extract” might be an option in place of grapefruit.
It, at least, would seem to be more accurately repeatable. It may also be more convenient depending on your circumstances or location.
Polypharmacy and/or poly supplementation have some pitfalls that we sometimes forget.
The action of citrus bergamot may be responsible for some confusing personal results of my rapamycin dosing. I have used it as a supplement for quite some time, but have not faithfully taken it.
“Bergamottin is a major furanocoumarin and a bioactive component of grapefruits (Citrus paradisi) and other citrus fruits [19]. It was originally found in the oil of bergamot (Citrus bergamia), from which its name has been derived”
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6321104/
Not a particularly accurate scientific view:
Citrus Bergamot: Can give many benefits of a prescription statin medication without side effects - Quad City Herald.
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Interesting one on this topic of Bergamottin
Other articles look pretty good for saying it inactivates P4503A4 such as Www.pubs.acs.org/doi/abs/10.1021/tx970192k
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59vw
#220
From the abstract of that paper
Conclusions: Bergamottin and reversible inhibition are not the primary substance and mechanism responsible for inhibition of CYP3A4 activity clinically. Red wine can cause dose dumping of extended-release felodipine in certain individuals.
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kbaba
#221
I was buying a pomello, basically a large grapefruit. and blending half of it the night before Rapa with a little Oj and adding soda water. Makes a great drink and doing the other half the next day. I think it might be overkill as I got side effects with a 3mg weekly dose but the drink is yummy
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SNK
#222
I think the grapefruit thing is stupid. Since i stopped the stupid grapefruit and did 5 pills straight nothing just water all my side effects disappeared. I agree with docs thaT SAY GRAPE FRUIT SHUOLD NOT BE CONSUMED WHEN TAKING MEDS. HIT CAP BT MISTAKE. TOO LAZY TO REDO LOL. I think grapefruit interfere in more ways than just bioavailability of the drug us such it should not be consumed when doing drugs.
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Bicep
#223
Yeah, that is a big dose. I use either 3 or 4 every 2 weeks and it works pretty well.
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it would make sense because with GFJ you are getting a lot more … why not try 15 or 20 pills and see if your side effects return… if so… GFJ is just normal.
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SNK
#225
Nah I’m not a fan of grape fruit juice. I think it has other weird stuff that may interfere with meds, not just the fact that it increases the bioavailability and absorption. Plus I hate the taste also. I’ll just do 5 straight pills per week and that should be good.
Karel1
#226
I wonder if transcutane application with the help of the droplette device mentioned in the “Reverse Gray Hair, Hair Repigmentation](https://spotify.localizer.co/t/reverse-gray-hair-hair-repigmentation” subject or via sublingual administration both bypassing the entero-hepatic pathway could give higher bioavailability.
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J0hn
#227
I take my rapamycin sublingually, but I have to do an extraction on the tablet/s first to remove all the inert components.
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John - interesting. Have you done any blood testing to know how well the sublingual rapamycin is being taken up?
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J0hn
#229
I haven’t done any blood testing for drug levels. Unfortunately I live in the UK and my nearest testing centre would be London, and I’m going through what will probably prove to be a messy divorce.
I’ve done everything I can to enhance lingual vein absorption of drug. I’ve reduced the dosing volume down to 120ul of transcutol based dosing solution by extracting the rapamycin from the tablet.
I’ve also maximised contact time with the vein by applying a 10ul droplet to each lingual vein every 30 seconds, with my head back and tip of tongue touching the roof of my mouth.
I have in the past also added 5ul of a food colouring dye to the dosing solution and there doesn’t appear to be any pooling at the base of the tongue.
I love to know what my drug levels are using this dosing technique. I have tried to buy an ultra sensitive Rapamycin ELISA kit but unfortunately the company won’t sell to a private individual.
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Meta Analysis of Rapamycin enhancing strategies.
States multiples for Ketaconazole, GFJ and half life of Rapamycin.
This answers lots of questions about Rapamycin.
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4410974/
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A lot of reading. So the peak is around 2.2 hours. I can definitely feel the effects after 2 hours. One thing on the positive side my nose that usually suffers from allergies no longer seems to get that any more.
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