#7

Oh thanks I didn’t know that about splitting the pills although 1 pharmacy around here actually offered me 0.5mg pills to start with but I insisted on the 1mgs

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#8

I don’t think that was the issue, so they should be able to be safely split:

#9

95% (or more) of the rapamycin market in the USA is likely generics, which do not use the Elan Pharmaceuticals’ nanocrystal technology that the brand name Pfizer Rapamune uses: Rapamycin and NanoCrystal Formulations. and even for Rapamune they don’t recommend you split, crush, etc. the tablet: “Do not crush, chew, or split RAPAMUNE tablets. Tell your doctor if you cannot swallow RAPAMUNE tablets. Your doctor can prescribe RAPAMUNE as a solution.” of course, that could be for commercial reasons and not just functional reasons, but I could not find any websites claiming it is possible to split Rapamune without effecting the bioavailability. You’d really need to look at the pharmacokinetics of the Elan technology to better understand this issue, and I’m not so interested in it. https://labeling.pfizer.com/showlabeling.aspx?id=139§ion=MedGuide

All the generics use some sort of coating to increase bioavailability from what I’ve seen. Break that covering and I’m pretty sure you lose the bioavailability benefits (and thus 95% of the benefits). Do you have any scientific evidence to the contrary?

#10

The rapamycin is in the coating with rapamune, and the core is inert.
I don’t know whether the nanocrystals or nanoparticles (solid dispersions?) are much affected by splitting, I mean they are intact in the other areas of the pills?

#11

Source for this claim?

#12

The inert tablet core is composed of lactose monohydrate, macrogol 8000, magnesium stearate, and
talc. The tablet coating is composed of several layers of coatings consisting of a nanodispersion
(containing the active substance and a stabiliser), macrogol 20000, glycerol monooleate,
pharmaceutical glaze, calcium sulphate anhydrous, microcrystalline cellulose, sucrose, titanium
dioxide, brown iron oxide (E172), yellow iron oxide (E172), α-alpha tocopherol, povidone, carnauba
wax and red printing ink

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#13

Good find! But most of us here are not taking rapamune because of the high cost. I am not even sure it’s still available in the USA.

#14

Ths is most easily resolved if someone simply split their pills before taking a rapamycin serum blood test they were going to take anyway, and see if the serum amount is as usual. I’m guessing it is.

Biocon has film coating, not enteric coating, so probably the same thing there.

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#15

I don’t know if this is related to your problem but based on this paper (on everolimus, not sirolimus), this might not be the right strategy if low-dose has actually more sympathetic activation than high dose (might explain the nausea?): Dose-dependent effects of rapa on anxiety?

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#16

Hi,

I’m new to rapa, too. I’m taking 1 mg and splitting a 2 mg generic for rapamune. I’m having significant effects (pos and neg) after only one dose last week. I have a friend who is doing same experiment.

My symptoms: unable to sleep first night. Had the feeling of coming down with upper respiratory infection on that first night. Calm but fatigued for several days. A few new aches and pains for first few days, but my chronic rt. shoulder pain has all but resolved. Also, I developed a scalp rash which I had attributed to rapa, but now wonder if I suddenly developed an allergy to castor oil (which I had used on my scalp the day prior to first dose of rapa).

I am surprised by the idea that rapa can’t be split and don’t know if that’s accurate. I will split today’s dose again, but will graduate to a full pill 2 mgs next week.

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#17

I was on Rapamune for years, but 3-4 mo ago I was notified by my pharmacy that Rapamune is not going to be available bc Pfizer stopped producing it. I called Pfizer and they confirmed.

3 Likes
#18

Oh and I had a few brief moments of nausea on day 1, too.

#19

Very interesting thanks. honestly I’m not sure I’d have the coverage to go straight for a higher dose now that I’ve experienced 1mg side effects - think I’d be more inclined to switch to a biweekly 1mg to each dose a chance to fully clear from my system before layering the next dose on top of it, and then gradually decrease the 2-week cycle to a weekly one.

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#20

“Calm but fatigued for several days” sounds exactly my experience too - didn’t really have any aches/pains to begin with that I could have noticed disappearing though. Good to know others are having similar experiences on low doses, but I’m leaning on starting fresh with a 2-weekly cycle to begin with just because it was the 2nd dose that gave me far more noticeable side effects

#21

I am using Pfizer’s Rapamune 1mg, it has minimal side effects and I feel good. Contrary to popular belief, rapamycin is a very effective drug even at low doses.

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#22

I also believe in low doses of Rapa. 1 mg doesn’t give me any side effects and works very well.

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#23

@LaraPo , just to be clear, for people new here, you’re taking 1mg once per day (is that correct), and you’re taking it as an organ transplant patient, not specifically longevity, correct?

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#24

Yes, it’s correct. It’s prescribed not for longevity, but as a transplant medication. Rapamycin is an amazing multipurpose drug.

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#25

I’m pretty small, 5ft3”
I dose with 5mg and don’t feel like I have any side effects except mouth ulcers (and these sometimes seem to appear within hours of taking rapamycin)

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#26

Hi I have a friend who just started a low dose she intends to stay on so came here to try to find a study someone posted that said ongoing low doses can have the opposite effect intended but seems you and others are doing well with that dosage? I think she’s just taking .25mg 2 or 3 times a week as very sensitive to drugs.