Interesting post from another site.

[Ronzy]

12:46 Sat 7 May

* 48%

stuffthatworks.health

POLYMYALGIA RHEUMATICA

LERO

O

Ed582 • 2d

As a physician with PMR I continue to be astounded by its

exquisite sensitivity of the disease to very small changes

in prednisone dose. Over my long career I have

prescribed prednisone for other conditions where 40 - 60

mg is not uncommon and where weaning is rapid. On this

site I have read of patients who are stuck at 3 mg - a dose

I previously would have called homeopathic. But just

today I tried to stay on 7 mg after a long time on 8 mg

and in a few hours had intolerable hand spasms - an early

recurring sign of my RS3PE variant of PMR. So I took

another mg - symptoms gone! As noted below, the drug

occupies glucocorticoid receptors to suppress immunity

and inflammation.

I am supposing that there are just so many molecules of

prednisolone and so many receptors to cover. Switch to a

lower dose and some receptors go uncovered. The hope

is that the number of receptors decline over time allowing

the dose to go down.

Pharmacology and mechanism of action

Glucocorticoid anti-inflammatory drug. The effect of

prednisone is attributed to prednisolone. After

administration, prednisone is converted to prednisolone.

Anti-inflammatory effects are complex, but via binding to

cellular glucocorticoid receptors, prednisolone acts to

inhibit inflammatory cells and suppresses expression of

inflammatory mediators. Prednisolone is approximately

four times more potent than cortisol but only one seventh

as potent as dexamethasone. Prednisone appears to be

well absorbed and converted to active drug,

prednisolone.

© prednisone: tried by 1561 members

[PMRpro Ambassador]

We could have told him that!!!! Hope he spreads the word!

[SheffieldJane]

Interestingly put. Clearly doctor’s who have had the disease are enlightened!

[Temoral in reply to SheffieldJane]

We need more medics who have had experience of these drugs to educate the others who prescribe as if one size fits all. Obviously don't want the medics to suffer, but if the few who do, could accelerate the research...now that would be hopeful...or even if more of our Rheumy staff read these posts. ....

[SMH4CRNA in reply to Temoral]

This is common knowledge of the mechanism of action of prednisone.

[PMRpro Ambassador in reply to SMH4CRNA]

What is? The article in general should be common knowledge but the bit that we all latched onto is "As a physician with PMR I continue to be astounded by its

exquisite sensitivity of the disease to very small changes

in prednisone dose."

And believe me - there are a LOT of doctors who don't appreciate how even 1mg change in dose can affect symptom management noticeably. If they did, they wouldn't tell patients to drop 5mg at a time overnight or scoff when a patient tells them dropping by 1mg, even half a mg, can be enough to result in a flare of symptoms.

[SMH4CRNA in reply to PMRpro]

I was speaking to the MOA of prednisone. Most medical professionals know this. What they may not know is the significance behind tapering due to its MOA and pharmacodynamics. Unless live it, than difficult to appreciate it.

[Lollybygolly]

Wow! That lends credence to my own experience - trying to drop from 10mgs Prednisolone to 9mgs seemed such a hurdle. I began to imagine I was just being ultra sensitive and maybe a little hypochondriac to feel the difference. My Doc gave me 1mg pills plus 5s so I could taper but I had to admit defeat as 10mgs was only just covering the majority of the pain. Your note is much appreciated.

[SMH4CRNA]

He describes what is known as up-regulation. Common in receptor site binding drugs.