I can only assume he’s talking about blood levels of rapamycin but using the wrong units (which should be in ng/mL or similar units, not mg). I don’t know the typical peak levels after weekly dosing (planning to get my peak tested this Tuesday after 6mg dose).
1 Like
Have been taking all 3 of these drugs for longevity, glucose control, and to get lower inflammation in my body for 6 months now without any problems. I also checked for interactions and found none except for statins. I take 5 mg. Crestor and just skipped that dose for a day when taking rapa with GFJ. I would suggest you weigh your GF juice and pulp before taking so you can be more consistent in how much of the CYP3A4 your getting. I personally take 400 grams. 200 grams night before, and 200 grams 30 min., before rapa next morning. Been on Rapa for almost 5 years. As we learn more we can add additional interventions to slow down ageing. In my opinion, 90%+ of most studies will not actually extend life. Wait for proof, before adopting.
6 Likes
You are way behind. Dr Green takes 20 mg every 14 days, and has for 3 months. Cancer patients have been using GFJ for many years in order to control costs on there Sirolimus. Why try to reinvent the wheel, the science is solid, just follow. We all know that only a fraction of dose is taken up in the body, so what that fraction works.
Dr Green has changed to 12 mg per week
1 Like
Did he give the reason why he changed back to 12mg per week?
Thanks all for the responses! Btw, do any of you have an idea of the minimum amount of grapefruit juice or grapefruit approximately needed for 3x bioavailability? I always feel uncomfortable breaking my keto or FMD with a bunch of fructose just for this purpose.
1 Like
You save a lot of money if you take 6 mg with grapefruit juice, it is equivalent to taking regular 20 mg pills. Cancer patients take up to 45 mg twice per week, beyond that, they get gastrointestinal side effects.
1 Like
i read you should take 8 ounces of white grapefruit juice, not pink colored one.
1 Like
Blagosklonny indicated a 8 ounce glass as the amount:
1 Like
Wouldn’t the enzyme be present no matter which color grapefruit juice one uses?
We just exchanged a brief text. He mentioned that it’s unclear whether a 2 week regime is better than 1 week. I was leaning toward a 2 week schedule but, based on this, decided to go back to weekly. Although, for now, just 6 mg. When I visited his office in October, he was doing 2 week.
1 Like
i read someone in the Age Reversal Forum said so.
This article is about how grapefruit juice works and the various medications it interacts with:
Drug Interactions with Grapefruit Juice | British Journal of Medical Practitioners.
3 Likes
from Dr. Mark Thimineur on age reversal forum:
Mark is a practicing physician and uses Rapa in many of his patients. In order to control cost of Rapa he has a grapefruit juice protocol. The best 2 ways to save money on Rapa is to use grapefruit juice or buy powder like I do. Hope this helps you or anyone else taking Rapa.
Karl For myself and anyone who is “self pay” the source is Biocon “Sirolimus” through online Canadian Pharmacy. Price $349 per 100 1mg tabs. For patients who go through insurance it is Pfizer Rapamune. It seems some of the Medicare D plans cover it, at least for now. Once I started the higher cycling regimen, I started using grapefruit juice to impair intestinal P450 and spike absorption 3 fold (half life is unnaffected). It becomes to expensive for many people otherwise and I always do myself what I tell my patients to do. I have to accept that there is a known variability of grapefruit juice effect on sirolimus absorption of 250%-350% so the actual dose may be a little lower or higher and I accept this small risk (again, well studied insider info). Grapefruit juice protocol is one fresh squeezed large fruit about 8 hours prior to dose (night before) and one large fresh squeezed grapefruit morning of with rapamycin taken 30 minutes later. Assume an average 300% increased absorption to determine the proper dose (1/3 of the mg/kg/wk without juice). So far so good.
The grapefruit juice option should be considered if a person is not concurrently taking drugs metabolized by intestinal P450 enzyme complex. The example of statins for cholesterol lowering is the most well known. Barring that, tactical use of grapefruit juice can overcome the poor bioavailability of oral rapamycin.
After an oral dose 86% of rapamycin is chewed up by the intestinal P450 enzyme and is excreted in feces. Inhibition of this enzyme complex with either ketoconazole or grapefruit juice has been pretty well studied in the oncology literature. In one such study the target dose of rapamycin was 90mg in a once weekly dose which provided the target AUC for the solid tumor being studied. Patients could not tolerate that dose due to GI side effects. It was shown that Ketoconazole administration reduced the required amount of rapamycin to 16mg and administration of grapefruit juice reduced the required amount to 25-35mg rapamycin to reach the same AUC. In other words the intestinal absorption of rapamycin was increased about 300% with grapefruit juice and 500% with ketoconazole. Cohen EE. Clin Cancer Res. 2012;doi:10.1158/1078-0432.CCR-12-0110.
The details about grapefruit juice: fresh squeezed is necessary as bottled or canned do not show the same amount of P450 inhibition. Approximately 8 ounces of juice pretty strongly inhibiit the enzyme in about 4 hours and lasts about 24 hours. One large grapefruit provides about 8oz juice.
Personally, and in select patients, I utilize this P450 inhibition to predictably maximize absorbtion and minimize cost. Consider that 2mg now becomes, in effect, 6mg and the cost savings are large. This is especially true for larger persons. My protocol is to take 8oz freshly squeezed the night before and also the morning of the rapamycin dose. Before deciding about this it would be best to check if any pharmaceuticals a person is taking would be effected by P450 inhibition (only in intestine) or check with your physician.
7 Likes
Ask your pharmacist.
Also, the sugar in the GF juice may cause GI issues if you take Acarbose that day.
Acarbose only blocks starch. So I don’t see how this could be the case. I wish it blocked fructose.
1 Like
Is it ok to eat the grapefruit rather than squeezing it?
Absolutely - that is fine. I’m sure either way is good.
So eat a whole grapefruit both night before and following morning.
1 Like
That seems reasonable. There unfortunately have been no studies on this, so we’re making our best guess here.