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5ht2a

Topical tropanes and... sweating?

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The use of anticholinergic (specifically, antimuscarinic) drugs is already well established in mainstream medicine for the symptomatic treatment of hyperhidrosis (excessive sweating) and it is indeed fairly effective. Unfortunately these types of drugs, especially those that readily cross the blood-brain barrier can produce a whole bunch of unpleasant side effects when administered orally. The medical community understands this and a topical product has been developed specifically for this ailment in the form of a glycopyrronium-bromide laced disposable wipe.

 

While my plants may love summer, I and many others find it hard to embrace it when constantly drenched in sweat. Personally, the heat itself doesn’t actually bother me, it’s just the perpetual drowned-rat look and feel that I detest. While not officially suffering from hyperhidrosis, as it is not a year round thing personally, my medication does lower the temperature threshold for me so for 3-6 months a year, I may as well have it. Anyway, enough 1st world white boyin’ from me...

 

Recently I bought a Brugmansia to add to my ethno garden once again and today was pondering the possibility of preparing and using it topically for sweating. Maybe I can love summer after all haha... anyway, seeing as the tropane alkaloids within are antimuscarinic anticholinergics too, they should indeed work just as effectively as the pharmaceuticals used. I even found an Ayurvedic website that lists it as a therapeutic use for Datura so this is far from an original thought of mine. 

 

Just thought I’d share the idea as an interesting topical use of tropane-bearing plants. Would also love to hear if anyone has tried using such plants for such purpose, how one may go about preparing them for topical use safely (and without ending up with a flying ointment instead :o) or anything else anyone would like to add!

 

Peace!

 

 

 

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Embrace the sweat brother!  Drink loads of water and let your body purge it's toxins and cool itself the way nature intended.

 

And think of that wonderful shower when you come in after a hot sweaty day and how good and clean you feel afterwards.  B)

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On 17/07/2018 at 1:17 AM, 5ht2a said:

Anyway, enough 1st world white boyin’ from me...

lol

 

I agree with Northerner.

 

Brugs are beautiful plants, i have never tried topical applications but if you are going to experiment be careful, with this attractive plant there is a fine line between awesome and quite grim, a very powerful plant indeed and can become or does have potential to lead one into a kind of 3 day nightmare, it may be better to just let the sweat flow ?

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Thank you for the warning (not sarcasm, it’s always appropriate for these plants) I definitely understand what Brugmansias and the like are capable of. I have experienced anticholinergic syndrome, though not with tropanes but with a lethal dose (intentional) of Promethazine - thankfully saved in time. Anyway, extremely *not* keen to endure anything even remotely close to that horror ever again. Rest assured, any potential experimentation will proceed methodically and with the utmost caution. :)

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Some disjointed thoughts...


Just curious - have you used the glycopyrrolate wipes? Afaict it’s used for this purpose over other antimuscarinics (AM’s) not only because of the blood-brain barrier thing, but also because it’s selective for M3 receptors - the kind involved in peripheral gland stuff. Whereas most (all?) of the naturally-occurring compounds have some central activity & are considered “non-selective” (this isn’t 100% accurate, but they’re at least *less* selective). And leaving aside the central effects, you can also expect peripheral side-effects like dry mouth & eyes. Glycopyyrolate is also significantly less lipophilic than the 2 most common naturally-occurring AM's (atropine & scopolamine) - and so is better suited to topical application, as it's more inclined to stay put & not go sneaking off over membranes to cause mischief elsewhere in the body. Don't be put off by the title, the intro of this paper: Pharmacokinetics and Pharmacodynamics of Glycopyrrolate in the Horse (2012) gives a good rundown of the general history/chemistry of various AM's and how this has informed their applications.

 

Take the literature about reduced side-effects with different tropane ROAs with a grain of salt: eg. you will read claims that transdermal scopolamine has less central/adverse effects than oral, but a large part of that difference lies in the slow release & therefore lower peak drug levels (ref) - it’s not necessarily to do with the route per se. Also, if you’re aiming for something like the glycopyrrolate wipes, then you actually want local activity without absorption (i.e just the “dermal”, minus the “trans-“), and not many papers make this distinction between topical/transdermal.

 

If you do make up a topical cream, some stuff to keep in mind:

 

- make a large batch (so you can standardise a dose properly - atropine & hyoscine are quite heat-stable & should keep a long time if the base itself is stable)
- make sure it’s homogenous (tropanes are potent, you don’t want any pockets of cream that are 10x as strong)
- use an aqueous base (you’re aiming for local activity, not transdermal absorption - so no DMSO, no oily salves)
- alternatively, make up an aqueous solution to apply via wipes/spray: a patent for glycopyrrolate wipes  settled on 10mg (oral dose is 1-4mg/day) dissolved in 1ml of 33% EtOH in water (eg. vodka) for each wipe - so maybe you could use those ratios as a rough starting place? The patent discusses some of the issues with consistent dose/applications via this method & how they addressed them
- don’t drive (possibility of various CNS effects, also a common side-effect which impairs your eyes' ability to focus)
- be aware of the half-life & other metabolic issues relating to the active ingredient(s) - half-life can be *long* for some of them (I mean both: some actives & some effects) so that you might get some cumulative effects even with once-daily dosing; and pharmacokinetic variations can be major (not just between individuals, but also individual responses at different times) and involve a lot of factors - not least the many, many drugs that might have significant interactions.
- many people get mild skin reactions from topical AM’s (esp. with repeat applications) which can also affect absorption (irritated skin has higher bloodflow, lower barrier effect)


So that's how I'd be starting as far as prep was concerned. But now let's backtrack & consider whether this is actually a good idea. This class of drug is used to treat excessive sweating, that is true. But that use is generally limited to pretty severe cases - e.g. where disease/surgery has impaired their autonomic nervous function (to the point where their hyperhidrosis is causing dehydration or problems regulating body-temp). Another main use is in palliative care for terminally ill folks who aren’t concerned about long-term side-effects and just want to be free of their “death-rattle” & have some dry sheets before they die. And even in these cases, many patients choose to stop taking their meds due to the side-effects.

 

A potential risk of any kind of regular long-term use is the possibility of  “cholinergic rebound” when you stop. There have been cases where people taking scopolamine for motion-sickness got withdrawal syndromes after only a few days to a week of daily use (includes transdermal use). That side-effect seemed to be only temporary & could be managed by tapering down off the drug, but definitely proceed with caution here. Sweating is pretty important in regulating body temperature, and if your body thinks that system isn’t working properly it might try to compensate. Compensatory hyperhidrosis seems to be a major issue after sympathectomy surgeries (sometimes used as a last-ditch treatment for severe hyperhidrosis) - and while that specific mechanism mightn’t apply here to AM drugs, there might be some equivalent one.

 

Even in the short-term, your actual intended effect (of reducing sweating) alone can be dangerous - people on AM’s have increased risk of hyperthermia, and need to monitor their body temp manually to make sure they aren't overheating. Especially if hot weather &/or physical exertion are going to be involved, please use extreme caution when experimenting with this. For eg: try treating only some areas of skin, carry a thermometer to monitor your body temp, be sure to continue using other basic cooling methods as well, and make sure you have plenty of water & some method of rapid-cooling (ice-packs, cool creek to jump into, etc) in case of emergency - heatstroke is a miserable experience.

 

Also be triply-cautious when combining with any psychoactives known to affect temp-regulation... MDMA in particular is a big one there. The researchers who were looking at treating hyperhidrosis in physically-active patients were concerned even about the effects of caffeine!  - and while that might be overkill (for regular ambient temps & activity levels anyway), it does at least give you an idea of the level of awareness & attention to detail you want to have going into an experiment like this. I'd be less worried about a tropane OD, and more concerned that you're taking away a fairly major safety net that we don't often have to think about. Even if you're only removing part of that net, it's still an important function that you probably should try to replace with conscious monitoring (like those poor people that can't feel any pain who need to keep visually checking all their body parts to be sure that their hand isn't resting on a hotplate or something). Not wanting to over-dramatise or exaggerate the risks here - this isn't necessarily a risky thing on its own...it just has lots of ways it could become risky. But if you're mindful of the potential, and proceed patiently & with caution I think most of those could be minimised?

 

Other options that spring to mind: deodorants based on bentonite clay; washing with witch hazel (or other herbal astringents), &/or vinegar; physical cooling (apparently just drinking a slushie can lower your core temp by ~0.5 C & reduce sweating, for a while at least). Another thing you could try maybe is hyoscine butylbromide (available OTC), which is sometimes used for hyperhidrosis as it’s a form that’s blocked by the BBB.

 

Or if you want a DIY experimental treatment, how about tap-water iontophoresis - looked more promising & less risky? Here are some refs, the last one has instructions for a DIY apparatus:

http://Treatment of Palmar Hyperhidrosis with Tap Water Iontophoresis (Kim et al, 2017)
Long-term efficacy and side effects of tap water iontophoresis of palmoplantar hyperhidrosis--the usefulness of home therapy (Hölzle & Alberti, 1987)
A Simple User-made Iontophoresis Device for Palmoplantar Hyperhidrosis (Nagar & Sengar, 2016)

 

And if you find that the iontophoresis isn't effective enough on its own (i.e. just w/plain tap water), it has also been used to facilitate dermal delivery of drugs (eg. glycopyrrolate solution) - so you could always add some brug drops to the water later on for a double-whammy?

 

And just as a general safety note for handling plant tropanes, (especially any kind of extract/concentrated form) - remember that they are absorbed through the skin & use appropriate caution: don't handle with bare hands, clean up any spills & wash/mop the area afterward, make sure everything is clearly labelled, and so on. For solutions I'd consider adding some kind of coloured dye to make spills more visible (only because invisible spills would worry me more than stained skin). If experimenting with solution/wipes, I'd also wonder about the possibility of any excess/unabsorbed actives getting absorbed by my clothes - not sure if/how they address that with the glyco-wipes? maybe it's not a problem - but I wouldn't be asking anyone else to wash my clothes until I knew the answer.

 

 


 

 

Edited by Anodyne
(edit: added a few links & some practical/safety stuff)
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Additional safety note when handling tropane solutions: DON'T RUB YOUR EYES!

This lasted 24hrs+...

 

grandma_what_big_pupils_you_have.thumb.jpg.7f914c882fbf166a10d511b2b4c4d29f.jpg

 

(sorry I know the photos are slightly out of focus, but so was my vision! :lol:)

grandma_what_big_pupils_you_have.thumb.jpg.7f914c882fbf166a10d511b2b4c4d29f.jpg

grandma_what_big_pupils_you_have.thumb.jpg.7f914c882fbf166a10d511b2b4c4d29f.jpg

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9 hours ago, Anodyne said:

Additional safety note when handling tropane solutions: DON'T RUB YOUR EYES!

This lasted 24hrs+...

 

grandma_what_big_pupils_you_have.thumb.jpg.7f914c882fbf166a10d511b2b4c4d29f.jpg

 

(sorry I know the photos are slightly out of focus, but so was my vision! :lol:)

Well hello there saucer eyes!

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We sweat for a reason, as courageous as it would be to dive into these chemicals/plant medicines, it hardly seems worth the risks to stop yourself sweating.

Go for a swim!

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