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heteromer t1_ivo4i35 wrote

Drugs when applied topically can absorb systemically. For products like Aspercreme, however, they only need localised effect, so they don't need to get into systemic circulation in appreciable amounts. They just need to cross through the skin and into the local area (i.e., muscle). They passively absorb through the skin via two ways:

  1. transcellularly, where they cross through the cell membrane and through the skin cells, or

  2. paracellularly, where they cross in junctions between cells.

For the latter, there are excipients like ethanol or glycerin (which is found in Aspercreme) that can help open up these junctions to facilitate paracellular diffusion through the epidermis. Thick ointment formulations also help in the same way. The active drug, salicylate, won't help with nerve pain but it can provide a localised anti-inflammatory effect -- the advantage with localised effect is the drug compound itself doesn't need to be so potent. Nonetheless, the active drug still has to have some favourable physicochemical properties -- it has to be highly lipophilic, but still sufficiently hydrophilic, to cross transcellularly, and it needs to have a small molecular weight to fit through functions, etc. The use of a triethanolamine salt for salicylic acid also helps, as it helps to stabilise the drug (think of it as the rocket that propels the shuttle before detaching). Triethanolamine salicylate has been shown to perfuse tissue.

Interestingly, methylsalicylate is another form of salicylic acid used in topical preparation. There are enzymes called esterases in the skin that will cleave up molecules by their ester linkages. Methylsalicylate contains an ester group that gets hydrolysed by these esterases when absorbing, turning into the active salicylic acid.

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Optimal-Conclusion t1_ivpjsk9 wrote

So my body is a big ole' sponge? What else gets absorbed versus not? Should I be wearing gloves more often than I thought?

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Zenmedic t1_ivrbm6n wrote

There's a fairly long list of things that can be absorbed through the skin. LSD and THC can both be absorbed, however there is limited systemic intake, so you need a lot, or the right conditions. This is the same for many things.

This is why as a former HazMat Medic, I would always rinse people with cold water. Close the pores, decrease circulation (not because I'm a sadist).

Warm conditions, certain carriers (as mentioned above) as well as general skin condition and thickness of epidermal layer also play a big role.

I was always taught that if you don't know if you should be wearing gloves/suit/respirator....the answer should default to yes.

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Sharlinator t1_ivsmom8 wrote

Well, I'm sure you have experienced how something like hand lotion is absorbed quite effectively (and indeed that's its whole purpose)!

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heteromer t1_ivsrbz2 wrote

The epidermis is highly keratinised to prevent systemic absorption. Drugs that absorb systemically in concentrations high enough to exert an effect are quite rare, and the epidermis does quite a good job as a barrier.

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provert t1_ivoyfha wrote

Excellent and thorough! Thank you!!!

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freakydeku OP t1_ivr1bk4 wrote

thank you! i appreciate you going into detail on the function. i don’t yet fully understand all the terms you’re using but i’m glad you used them so i can have a better/wider/ more holistic understanding

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greenappletree t1_ivvfsx6 wrote

A bit of a tangent. This is a reason to be carful when using “topical” since it can be absorb and overdose is possible. There has been cases where people have overdosed on simple analgesics for example.

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