Topical Loperamide

[southpharmindy]

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So I have been looking into compounding a bit and have noticed that some pharmacists are using Loperamide in topical preparations to treat pain.

I know that Loperamide is an opioid and is not extensively absorbed from the digestive tract. We also know that it does not cross the blood brain barrier.

My question, I guess, does anyone have any experience using this as a topical preparation? If so how did the patients respond?

 

[npage148]

Sounds Like a waste of money. An active opoid that doesn't cross he BBB?

 

[rxlea]

Is it for burns?

 

[southpharmindy]

I've heard of it being used for burns as well as shingles.

npage-You wouldn't worry in this case if it crosses the blood brain barrier.

I'm just interested to see if it would actually work in the peripheral tissue.

 

[npage148]

I'm not worried about it crossing the BBB, I'm saying that since it doesn't cross the BBB it likely doesn't work that much if at all

 

[rxlea]

I'm not worried about it crossing the BBB, I'm saying that since it doesn't cross the BBB it likely doesn't work that much if at all

Aren't there peripheral opioid pain receptors that are overactive in burn victims though? You figure the epidermis isn't exactly a great barrier to absorption after a burn. Same with an ulcer.

What do you think?

EDIT: a cursory glance shows a study in rats demonstrated decreased pain after topical application. At least that's the one that's referenced the most from what I saw.

It seems there is substantial anecdotal evidence/patient report of it being effective. I'm assuming there is going to be considerable variation in response between patients but in some patients where oral morphine may be a bit of overkill or perhaps in burns that are further along in the healing process, it might be worth a try.

 

[npage148]

Aside from the fact that there is very little data about it's efficacy, I think it's an ok attempt in treating someone with shingles who need an adjuct pain control but I'd be really have a hard time for using it in someone with significant burns for 2 main reason.

The absorption kinetics in a burn patient are going be be changing on a daily basis as their skin heals. It'll be near impossible to get any sort of repeatable or reliable exposure in these patients.

They are also going to have been on pretty significant systemic opioid therapy and probably have some pretty high levels of tolerance built up. How much is a locally active opioid going to help realistically?

Also, I'd be worried about sterility issue too with burn patients but that should be easily solvable