Prednisone or prednisolone ?
Posted , 11 users are following.
I have been reading Kate Gilbert’s book “PMR and GCA: a survival guide. As many of you who have read it and discussed on the forum before, this is a really excellent help for those of us who just started or who have been long suffering with these diseases.
One thing that I noted was that throughout the book she refers to our ‘famous’ corticosteroid as ‘Prednisolone’ – there was not one mention of Prednisone. I initially thought that this was a typo but apparently not.
I checked into it and read that the difference between prednisone and prednisolone is that one is the precursor to the other. Prednisone is activated by enzymes in the liver to turn into prednisolone. Apparently they do have similar uses but prednisolone is more readily absorbed by the body and is used when there is liver toxicity or liver failure involved.
This indeed surprised me as my rheumatologist has never mentioned or prescribed anything other than Prednisone.
It seems from researching the two names that they have many similarities, but there are differences. The chemical structure and molecular weight are different and prednisone is administered only orally, whereas prednisolone can be given orally, topically or injected.
Anyway, this has surprised me and I am now wondering if there is any information that all my “friends” on this forum can share with those of us who have not heard of this before.
And many thanks to you all for your constant helping and sharing with all of us who are ‘laden’ with PMR.
David
4 likes, 31 replies
constance.de Dave-California
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Constance
MrsO-UK_Surrey Dave-California
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janet08828 Dave-California
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I seem to remember reading on this forum the explanation of the difference between the two and it is the same explanation as the one you have read.
EileenH Dave-California
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I have been on all of them: prednisolone in the UK at the start, was switched to Medrol here in Italy and experienced horrible side effects - in fact all it did was give me side effects! Massive weight gain, my skin and hair went mad and I developed a superb dark beard - but the anti-inflammatory effect was non-existent. It allowed a massive flare and I was switched to Lodotra, the only other form of medium acting corticosteroid available here, which is prednisone. NO side effects with it at all for me - unless you count allowing successful weight loss!
linda17563 EileenH
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EileenH linda17563
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I'm sorry - I don't know where these rheumies get the ideas from. The only guaranteed successful drug for managing PMR and GCA is prednisolone so what is your rheumy suggesting trying you on? The reveiw articles all say the same: the mainstay of treatment for PMR and GCA is prednisolone.
There is a trial ongoing at the moment with toxcilizumab for GCA and it is also intended to try it for PMR but it isn't instead of pred, it is to see if using it can get patients off pred faster so you take both and the idea is to see if the taper will be quicker with fewer relapses/flares. There was a very promising trial in Southend using leflunomide a few years ago where they claimed that 22 out of 23 patients went into remission. However, I know a few people who were put on leflunomide and it either did nothing or made them ill and they had to stop taking it.
Some people have been put onto methotrexate or azathioprine - the results are mixed. Some have reduced their dose of pred to start with but then later had flares and been back on higher doses of pred. The medical literature has 3 studies, one said it worked, one said it didn't, one didn't know. Which is hardly convincing to me - so if you are put on them it is your rheumatologist doing research on you IMHO without the close monitoring that is guaranteed in a clinical trial.
I do know a couple of people on the forums who find that methotrexate or azathioprine do help - they are still on pred though. The only way to find out is to try I'm afraid.
Dave-California EileenH
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I took prednisone for a period of about 4 months after my initial start of PMR – starting at 20 mg and stepping down to 9 mg. Then I assume that was too rapid as the first ‘flare’ happened and pain levels zoomed up.
My rheumatologist reviewed my multi-blood test series (lots of them as they are covered by my US insurance) and determined that I would need to increase prednisone back to 20 mg but start right away on a very slow taper when my ESR dropped from the 60 level to approximately 30.
Also she put me on methotrexate (a slowish step up from 5 mg to 25mg/week) with the intent that I would stay at 25mg/week for the entire time that my prednisone taper was actively being reduced down to zero. She evaluated that some of my symptoms were from relatively long term steroid use rather than just the PMR and that methotrexate would assist me in maintaining a long taper to zero without too much pain. I have a fairly high pain threshold (determined by doctor’s testing for another issue) and figured that I would give it a try.
I had heard all the side effects, that as with all drugs is a longer list than the benefits! You may lose your hair, develop mouth users and feel sick all the time, etc. etc.. AND worse of all – you can’t drink alcohol, -OH NO !!
My conversation with another patient who was on methotrexate was very encouraging – so I started - and took my weekly tablet of folic acid (1 mg) along with my weekly alendronate sodium (70 mg) to prevent all those other nasty things from happening.
I initially started taking my full pred dose early in the morning but found that as the taper got to about 10 mg, I was having bad mornings – so during the 10 mg level, I did try a 1 month trial of Delayed Release Prednisone (Rayos) to see if I could balance the distribution. I personally would not recommend the delayed release as I had a lot more pain. However, my rheumatologist did suggest that using regular prednisone I could make my own dose time adjustments for pain balance – so I did start an approximate 90% am – 10% pm schedule and this has worked well for me.
Also when nighttime (1am -3am) pain bothered me, my rheumatologist did allow me to take a very low amount of Ambien (zolpidem tartrate) – I would cut the 5 mg pills into halves and quarters (a very low level) and this tiny dose would have a huge change on my sleeping through the night if I took it at about 11pm.
Anyway, I have been tapering prednisone approximately 1 mg per month and still taking 25 mg of methotrexate per week – it is now 11 months since I started with the methotrexate and I am just about to hit the 4 mg pred level and all is going relatively well. Most of my joint muscle aches (shoulder, thigh, etc.) are at a relatively low background level – the only bad issue is hand joint pain.
C-reactive protein and ESR test results are now into the normal zone and I pay a bit more to keep on checking these, glucose and other liver related blood levels – keeping my fingers crossed !
Eileen - I have been so helped by your knowledge during my 15 months of PMR - so, the purpose of this long California story of a British man was to give you some idea of how one of “your” methotrexate patients has handled the drug that does not have any really good research – and like everyone else on this forum – I’ll keep you up to date on my 4 to zero mg pred taper with methotrexate ‘side kick’. Thanks as always for ‘your’ brain.
EileenH Dave-California
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It's Rayos I'm on - Lodotra in Europe - and I think it is brilliant. Don't quite understand what you mean by "balance the distribution" - I take the entire dose at 10pm, it releases in a single shot at 2am and the peak pred level is achieved by soon after 4am, which is the idea. No morning stiffness, lasts all day, and as far as I can tell, no side effects for me.
linda17563 EileenH
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I have lessened the blurrred vision/ balance, by splitting the dose (14mg) and can at least leave the house!...It seems I can`t take the hit all at once!....Once again, thanks for explaining this to me....
janet08828 Dave-California
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So just to say thanks for your mtx update - good to hear from someone who is taking it.
linda17563 EileenH
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Dave-California EileenH
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What I meant about “balance the distribution” was that I thought that the increase in pain may be due to my absorption rate not being quite normal and the distribution effect of the corticosteroid needed to be modified.
That’s why my rheumatologist and I thought that the Rayos (Lodotra on the other side of the pond !!) may be appropriate.
Knowing that the maximum activity of the adrenal cortex is between 2 am and 8 am and is minimal between 4 pm and midnight, exogenous corticosteroids suppress adrenocorticoid activity the least when given at the time of maximal activity.
As you mention, Rayos releases the active prednisone approximately 4 hours after intake.
My rheumatologist said that Rayos was required to be taken at an equivalent dose as the immediate release prednisone that I was taking and continue to be taken at that dose. If after a reasonable time there was a lack of satisfactory clinical response, she recommended that the Rayos should be discontinued and that I should be transferred back to the prior immediate release prednisone.
So I started the 1 month trial, taking the Rayos at about 10-11 pm and within a few days my pain level increased substantially – mainly starting pain increase at about 4-5 pm and not reducing until early morning. There were a few variations on the maximum pain times during this trial but there was obviously something that was not right about my reaction to the ‘time release’ of Rayos.
Checking into the format of Rayos, the core tablet of prednisone is in an inactive shell that supposedly delays the onset of the prednisone by about 4 hours. This causes a delay in the time until peak plasma concentration is achieved. Apparently the mean time for healthy male subjects is 6-7 hours compared to 2 hours for immediate release prednisone. I read that the peak plasma concentrations are comparable for Rayos and immediate release prednisone after a light meal – about 2-3 hours. But I also understand that absorption rates of Rayos can be very much affected by the content and time taken after intake of foods of differing types. I did try a few different issues related to this potential – but no luck.
So anyway, I went back to immediate release prednisone - taking 8mg in the morning and 2 mg after supper and things improved dramatically.
Who knows how the body works – but that’s my story about Rayos.
David
EileenH Dave-California
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Whatever - I hope you and your doc have submitted a yellow card report.
Dave-California EileenH
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Maybe that's why I am having some success in pain reduction by distributing regular IR pred in varying %'s for my AM and PM doses - depending on the mg level that I am taking for my taper. Maybe my maximum and minimum activities of the adrenal cortex are slightly different ranges than normally assumed by rheumatologists and conventional pred dose expectation.
Have you researched anything related to this aspect of the efficiency of corticosteroids related to the adrenal cortex activity ranges and how it is possible to determine the adrenal cortex activity ranges in individual PMR patients so that more precise dose times could be identified to help patients ?
David
Dave-California EileenH
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If you do that sort of 'criticism' here in the US - you get a law suit instead of medal !!
MrsO-UK_Surrey Dave-California
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EileenH Dave-California
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look it up - I'd give the link but I can't easily and you need to read it yourself. But it is an essential part of assessing adverse events in new drugs - and obviously has to be independent of the pharma companies, especially in the USA!
No I haven't researched adrenal cortex stuff - I'm not sure it would help as the testing would be pretty fiddly and involve a lot of needles! Since we are all very different in how we experience PMR and how we respond to pred, even if you found a way of doing it you would have to test each patient. The empirical way of fiddling about with your pred dose if the blanket "15mg in the early morning" isn't providing a good result does work if you put your brain in gear. There has been some suggestion in the past that it may be some malfunction in natural corticosteroid production that contributes to PMR - the stress link might suggest that - but they haven' found any evidence that I know of.
What I know some endocrinologists would like to see is adrenal function testing on everyone as the patient gets to about 5mg - a short synacthen test would find the ones whose adrenal function is lagging behind. On the other hand, slowing the reduction right down and taking close note of excessive tiredness returning at these lower doses works too to sort out patients who need the test.
constance.de EileenH
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EileenH constance.de
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constance.de EileenH
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EileenH constance.de
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It was something that had occurred to me a year of two ago and I discussed it with one of the top PMR/GCA research bods in the UK after another lady had had a session with an endocrinologist about her adrenal function with a conversation that ran along similar lines. If an endo and a rheumy approve - I'll quote it!
Dave-California EileenH
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Regarding your comment on the short synacthen test - is that what is called the adrenocorticotropic hormone (ACTH) test (?) here - is this test to determine whether your adrenal and pituitary glands are normal ?
I am currently at 5 mg and going to reduce to 4.5 mg next week for another month before reducing to 4 mg (my methotrexate is still at 25 mg/week). In your experience do you think that I should request that my rheumatologist look into this (she has not mentioned it to me before) and schedule an ACTH test while I'm in this pred range ?
David
EileenH Dave-California
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I really don't know whether you should ask for it. As I said, endocrinologists would like to see it done, whether it is essential I don't know in that reducing mega slowly and being watchful will also catch the patient with problems - and then you reduce the no of tests needed. Do rheumies know that much endocrinology?
Dave-California EileenH
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I have an appointment with my rheumatologist in a couple of weeks - so I think I'll bring up the issue with her and see if she has any kind of endocrinological background - if not I'll tell her to call you !!!
I'll let you know her thoughts.
Thanks - David