resorcinol
12-10-2008, 06:49 PM
as an opioid for use outside of anesthesia in hospitals.
It will be delivered much like fentanyl is for the long acting version of the medication.
The brand name is Transdur-Sufentanil, created by Durect Pharmaceuticals and licensed to Endo Pharmaceuticals for distribution in the United States.
As far as I know, the Transdur-Sufentanil patch is currently in Phase II clinical trials -- if it's further along that that, somebody let me know.
This means in a few years, there will be another long acting opioid on the roster for relief of chronic pain in CP patients, both cancer and non-cancer related.
The patch itself is a little bit different than Duragesic. The biggest difference is the interval for changing the patch to a new one. Transdur-Sufentanil is a 7 day patch, meaning the typical prescription will be for four patches a month. Like with Duragesic, it's likely that some people will experience a poop out in half the time than the patch is rated for, so some people may get eight patches per month. I've heard that transdermal patches not lasting as long as they should occurs more often in males than females, although this doesn't mean that there aren't females who need more frequent patch changes too. This even applies to the nicotine patch. Some people need to change their nicotine patches every twelve hours (once in the morning, once before bed) instead of once a day.
Physically, the patch is different than brand name Duragesic too. The BRAND name Transdur-Sufentanil patch is a matrix patch, where the drug is dispersed in the lower 3/4 or so of the adhesive layer of the patch evenly (assuming quality control is kept up, the distribution is even) and covered with a thinner layer of adhesive (1/4 or so of the total adhesive) -- this thin layer has only a tiny portion of the drug in it, less than the further back adhesive portion. The drug diffuses from the inner adhesive layer into the thin outer adhesive layer, and then into the skin, as everything from the patch backing (the non sticky side) to the fat below the skin becomes a gradient of fentanyl concentration. The fent continues to diffuse from the inner adhesive portion, to the outer adhesive portion, to the skin layers, and then into the fat underneath the skin, because the concentration is always lower in the last portion of the reservoir before the bloodstream (the fat below the skin) than it is closer to the drug's source and at the source (the inner adhesive portion). This remains true for as long as the patch is rated to work (3 days for duragesic, 7 days for transdur-sufentanil)... although this stops being the case quicker than that in some people. This probably isn't because the drug absorbs too quickly in these people or because there isn't enough drug in the patch (less than they say)... for brands that's STRICTLY controlled, and generics have to be close enough to be transparent to the patient (although some generics are questionable).
I think some people get a quicker poop out from patches because the pathway from the drug reservoir in the patch to the fat under the skin becomes blocked at the skin level. Under that patch, dead skin cells, sweat, and other nasties accumulate. This is accounted for in patch design... that's why extra drug that isn't needed in the perfectly ideal situation is added. Some people, I think, build up dead skin and oils quicker than even the extra drug they do put in can account for, and this seriously hinders absorption after that point, even though there is plenty of drug remaining. This would explain why the problem is more common in men -- men produce more oils and dead skin cells on average than women.
OT reference stuff about patches:
The Transdur-Sufentanil patch is a mylan generic duragesic style patch. It's the same design, the matrix patch design.
For reference, there are three basic designs for nicotine patches:
Reservoir-Matrix Hybrid: drug is contained in between an adhesive layer which contains NO drug AT ALL, and the backing (non sticky) side of the patch. This middle layer is the mixture of a drug and another sticky solvent but not necessarily an adhesive, however it isn't a liquid or gel medium, it's extremely sticky and allows the patch to be pretty flexible and comfortable. Examples: Habitrol brand of nicotine patches, some brands of birth control patches, some nitroglycerin patches
Reservoir Patches: These patches are a pouch -- one side is sticky and has adhesive; this side sticks to your skin. The other side is a non sticky piece of plastic the same size as the plastic side with a sticky surface. The drug is dispersed in an alcoholic solution made gel like with some type of polymer compound, and as the two sides of the patch are being sealed, the gel and drug solution is injected into the space between the two plastic pieces. This is a literal drug reservoir. The drug diffuses from the reservoir, through the sticky side, and into the skin.
Examples: Brand name Duragesic and the watson, sandoz, and actavis generics for duragesic are the most well know examples of this type.
Matrix Patches: These patches are similar to the matrix-reservoir hybrid kind, except that there isn't a separate formulation for the drug laced sticky reservoir part and the adhesive. The drug is instead put IN the adhesive, and is typically present throughout the adhesive of the patch. The backing / non sticky side is the only other "layer". Drug concentration is higher in the portion of the adhesive closer to the non sticky backing / further from the skin, but there is still drug in all of the adhesive right up to the part that touches your skin, the concentration is just lower there.
Examples: some birth control patches, Nicorette patches (I think), and the most infamous .... Mylan generic fentanyl transdermal system (which I am quite fond of)
Some people struggle with the matrix only and matrix reservoir hybrid type patches because their skin clogs with oil and dead skin cells extremely quickly with these patches and slows absorption soon enough that it seems to them that the patches are weaker than the reservoir kind, or in extreme cases, barely work compared to the reservoir kind. Other people have no problem with their skin and matrix patches, and they're lucky because the hybrid patches and especially the full on matrix patches are extremely comfortable to wear compared to reservoir patches (they're very flexible... like a soft sticker) and much less likely to cause an allergic reaction than the reservoir patches are because they stretch the skin less than reservoir patches do -- in that way, even somebody allergic to the adhesive is less likely to react extremely badly because the flexiness of the patch doesn't add extra irritation to the skin.
Transdur-Sufentanil is a mylan fentanyl style patch, but I urge you guys not to immediately right it off if you found mylan fentanyl less effective than mylan gel even as prescribed. The people at Durect have been observing the whole Duragesic thing very closely, and are aware of the problems that some people have with the mylan patches.
From here on in it's speculation, because while I know Durect knows of the limitations of the matrix design of mylan fent, it's impossible to say for sure how they'll try to make it a non-issue for transdur-sufentanil. BUT -- there are some things I'm betting they'll do to help make matrix work for more people than it did with mylan fentanyl. I'm guessing though that:
1)They'll, based on clinical trial data, add more sufentanil than is necessary. This is already done with ALL patches, and ALL fentanyl patches including gels, but Mylan adds more fentanyl than gels to compensate for the matrix design problems and to help allow for a smaller patch. I think Durect, however, will (proportionally) add even more extra sufentanil to their patches than mylan did to their generic duragesics with fentanyl. They'll add as much extra sufentanil as they can without risking giving people with matrix friendly skin a dose that is far too much more than the rated dosage rate. This will make the matrix design work for people who mylan fentanyl patches worked for but were weaker compared to gels.
2)They'll carefully consider the formula of the adhesive. They'll likely engage in discussion with Mylan in doing this, so perhaps Mylan may even end up changing their adhesive formulation if Durect's is a success.
They'll probably pick an adhesive that is as hypoallergenic AS POSSIBLE while still retaining enough sticking power to not have falling off issues. They may even go with a weaker adhesive than mylan uses but is extremely hypoallergenic and safe to all but the most sensitive skin in the world. Less irritation means less oil production under the patch and less death of skin cells under the patch. This lowers the chances of a partial for full blockage of fentanyl absorbtion. This, like the first thing they'll do differently, will make matrix work for more people. If they go with a less sticky but extremely hypoallergenic adhesive, I'll betcha they'll include their own version of bioclusive/tegaderm style dressings WITH the patches in the box the patches come in -- and include their use in the official directions for putting the patch on.
So for you guys who found mylan's weaker than gels, maybe give Transdur-Sufentanil a try when it comes out if your doc suggests it. I'm confident that they'll try to address the issues with the matrix design pretty aggressively.
As far as recreational use goes, it'll be similar to how mylan fentanyl's are abused: cheeked. Keep in mind although you get less Transdur-sufentanil patches per month, that means there is also a larger equianalgesic and equipotent dose in each patch than there is in the equivalent strength duragesic, so it evens out. Also, if they implement my guess #1 for how they'll deal with the downside of matrix patches, there will be proportionally more sufentanil than necessary in the patch than there is more fentanyl than necessary in the mylan fentanyl patches. This would make cheeking them even more fun than cheeking mylan fents, since there's more opioid overall. Since it's a 7 day patch, you'd only need teensy tiny pieces though... sufentanil is 10x fentanyl in potency and there's 7 days worth in each of those small little mylan fent sized patches.
I'm actually glad, from an abuse and OD potential standpoint, that Durect chose matrix as the design for their sufentanil transdermal system. Gel sufentanil seven day patches would just be a disaster -- people would drop like flies... 7 days worth of sufentanil in a gel patch + smoking it + short 4.5 hour half life (a little shorter than fentanyl's) = crack like behavior, and tons of ODs.
The fact that they're matrix patches means that even cheeked the small piece you put in, while it release MUCH more quickly than if it were worn as Rx'ed, and will certainly get you high, will still retain some of its time release. That basically means if you feel like it's getting to be too much, all you've gotta do is take the patch out of your mouth and you'll be OK. Mylans or pieces of them release all of their fentanyl contents in about 8 hours in my experience, compared to 72 hours when worn as prescribed on the skin -- this gets me high when I do it. I'd imagine transdur-sufentanil would release its sufentanil content over about the same 8 or so hours. Just gotta be sure to use a very small piece since there's a LOT of sufentanil in each of those patches. Since they'll compensate even more than mylan does for the downsides/cons of matrix patches most likely, they'll likely be even more abusable than mylan is by cheeking. Just be careful and enjoy sufentanil.
Honestly, cheeking small pieces of the new sufentanil patch coming out, to me, sounds like the only way to go. Had gel sufentanil patches came out, the smoked high would last even SHORTER a time than fentanyl smoked does, since sufentanil has a half life about half the length of fentanyl. It would not be worth it.... just too short.
Cheeking these sufentanil patches, on the other hand, will likely provide a lovely, time released, 10 hour high on the probably lovely drug sufentanil.
How do you guys feel about this sufentanil transdermal patch coming out, whether you're a CP patient or looking to cheek small pieces of them to get a nice, PPT length buzz? I'm excited personally to see an new arrival coming onto the scene of a potent opioid since it doesn't often happen. I'd be more excited to see a transdermal patch of a NON fentanyl family opioid come onto the market (like 14-cinnamyl-oxycodone transdermal system), but this is exciting enough for me.
I'm stoked :D
WOW that was a long post. Feel free to NOT read all of it if you want.... if you just skipped down to this last line, just say how ya feel about sufentanil likely becoming a prescribe-able CII opioid in the U.S.
It will be delivered much like fentanyl is for the long acting version of the medication.
The brand name is Transdur-Sufentanil, created by Durect Pharmaceuticals and licensed to Endo Pharmaceuticals for distribution in the United States.
As far as I know, the Transdur-Sufentanil patch is currently in Phase II clinical trials -- if it's further along that that, somebody let me know.
This means in a few years, there will be another long acting opioid on the roster for relief of chronic pain in CP patients, both cancer and non-cancer related.
The patch itself is a little bit different than Duragesic. The biggest difference is the interval for changing the patch to a new one. Transdur-Sufentanil is a 7 day patch, meaning the typical prescription will be for four patches a month. Like with Duragesic, it's likely that some people will experience a poop out in half the time than the patch is rated for, so some people may get eight patches per month. I've heard that transdermal patches not lasting as long as they should occurs more often in males than females, although this doesn't mean that there aren't females who need more frequent patch changes too. This even applies to the nicotine patch. Some people need to change their nicotine patches every twelve hours (once in the morning, once before bed) instead of once a day.
Physically, the patch is different than brand name Duragesic too. The BRAND name Transdur-Sufentanil patch is a matrix patch, where the drug is dispersed in the lower 3/4 or so of the adhesive layer of the patch evenly (assuming quality control is kept up, the distribution is even) and covered with a thinner layer of adhesive (1/4 or so of the total adhesive) -- this thin layer has only a tiny portion of the drug in it, less than the further back adhesive portion. The drug diffuses from the inner adhesive layer into the thin outer adhesive layer, and then into the skin, as everything from the patch backing (the non sticky side) to the fat below the skin becomes a gradient of fentanyl concentration. The fent continues to diffuse from the inner adhesive portion, to the outer adhesive portion, to the skin layers, and then into the fat underneath the skin, because the concentration is always lower in the last portion of the reservoir before the bloodstream (the fat below the skin) than it is closer to the drug's source and at the source (the inner adhesive portion). This remains true for as long as the patch is rated to work (3 days for duragesic, 7 days for transdur-sufentanil)... although this stops being the case quicker than that in some people. This probably isn't because the drug absorbs too quickly in these people or because there isn't enough drug in the patch (less than they say)... for brands that's STRICTLY controlled, and generics have to be close enough to be transparent to the patient (although some generics are questionable).
I think some people get a quicker poop out from patches because the pathway from the drug reservoir in the patch to the fat under the skin becomes blocked at the skin level. Under that patch, dead skin cells, sweat, and other nasties accumulate. This is accounted for in patch design... that's why extra drug that isn't needed in the perfectly ideal situation is added. Some people, I think, build up dead skin and oils quicker than even the extra drug they do put in can account for, and this seriously hinders absorption after that point, even though there is plenty of drug remaining. This would explain why the problem is more common in men -- men produce more oils and dead skin cells on average than women.
OT reference stuff about patches:
The Transdur-Sufentanil patch is a mylan generic duragesic style patch. It's the same design, the matrix patch design.
For reference, there are three basic designs for nicotine patches:
Reservoir-Matrix Hybrid: drug is contained in between an adhesive layer which contains NO drug AT ALL, and the backing (non sticky) side of the patch. This middle layer is the mixture of a drug and another sticky solvent but not necessarily an adhesive, however it isn't a liquid or gel medium, it's extremely sticky and allows the patch to be pretty flexible and comfortable. Examples: Habitrol brand of nicotine patches, some brands of birth control patches, some nitroglycerin patches
Reservoir Patches: These patches are a pouch -- one side is sticky and has adhesive; this side sticks to your skin. The other side is a non sticky piece of plastic the same size as the plastic side with a sticky surface. The drug is dispersed in an alcoholic solution made gel like with some type of polymer compound, and as the two sides of the patch are being sealed, the gel and drug solution is injected into the space between the two plastic pieces. This is a literal drug reservoir. The drug diffuses from the reservoir, through the sticky side, and into the skin.
Examples: Brand name Duragesic and the watson, sandoz, and actavis generics for duragesic are the most well know examples of this type.
Matrix Patches: These patches are similar to the matrix-reservoir hybrid kind, except that there isn't a separate formulation for the drug laced sticky reservoir part and the adhesive. The drug is instead put IN the adhesive, and is typically present throughout the adhesive of the patch. The backing / non sticky side is the only other "layer". Drug concentration is higher in the portion of the adhesive closer to the non sticky backing / further from the skin, but there is still drug in all of the adhesive right up to the part that touches your skin, the concentration is just lower there.
Examples: some birth control patches, Nicorette patches (I think), and the most infamous .... Mylan generic fentanyl transdermal system (which I am quite fond of)
Some people struggle with the matrix only and matrix reservoir hybrid type patches because their skin clogs with oil and dead skin cells extremely quickly with these patches and slows absorption soon enough that it seems to them that the patches are weaker than the reservoir kind, or in extreme cases, barely work compared to the reservoir kind. Other people have no problem with their skin and matrix patches, and they're lucky because the hybrid patches and especially the full on matrix patches are extremely comfortable to wear compared to reservoir patches (they're very flexible... like a soft sticker) and much less likely to cause an allergic reaction than the reservoir patches are because they stretch the skin less than reservoir patches do -- in that way, even somebody allergic to the adhesive is less likely to react extremely badly because the flexiness of the patch doesn't add extra irritation to the skin.
Transdur-Sufentanil is a mylan fentanyl style patch, but I urge you guys not to immediately right it off if you found mylan fentanyl less effective than mylan gel even as prescribed. The people at Durect have been observing the whole Duragesic thing very closely, and are aware of the problems that some people have with the mylan patches.
From here on in it's speculation, because while I know Durect knows of the limitations of the matrix design of mylan fent, it's impossible to say for sure how they'll try to make it a non-issue for transdur-sufentanil. BUT -- there are some things I'm betting they'll do to help make matrix work for more people than it did with mylan fentanyl. I'm guessing though that:
1)They'll, based on clinical trial data, add more sufentanil than is necessary. This is already done with ALL patches, and ALL fentanyl patches including gels, but Mylan adds more fentanyl than gels to compensate for the matrix design problems and to help allow for a smaller patch. I think Durect, however, will (proportionally) add even more extra sufentanil to their patches than mylan did to their generic duragesics with fentanyl. They'll add as much extra sufentanil as they can without risking giving people with matrix friendly skin a dose that is far too much more than the rated dosage rate. This will make the matrix design work for people who mylan fentanyl patches worked for but were weaker compared to gels.
2)They'll carefully consider the formula of the adhesive. They'll likely engage in discussion with Mylan in doing this, so perhaps Mylan may even end up changing their adhesive formulation if Durect's is a success.
They'll probably pick an adhesive that is as hypoallergenic AS POSSIBLE while still retaining enough sticking power to not have falling off issues. They may even go with a weaker adhesive than mylan uses but is extremely hypoallergenic and safe to all but the most sensitive skin in the world. Less irritation means less oil production under the patch and less death of skin cells under the patch. This lowers the chances of a partial for full blockage of fentanyl absorbtion. This, like the first thing they'll do differently, will make matrix work for more people. If they go with a less sticky but extremely hypoallergenic adhesive, I'll betcha they'll include their own version of bioclusive/tegaderm style dressings WITH the patches in the box the patches come in -- and include their use in the official directions for putting the patch on.
So for you guys who found mylan's weaker than gels, maybe give Transdur-Sufentanil a try when it comes out if your doc suggests it. I'm confident that they'll try to address the issues with the matrix design pretty aggressively.
As far as recreational use goes, it'll be similar to how mylan fentanyl's are abused: cheeked. Keep in mind although you get less Transdur-sufentanil patches per month, that means there is also a larger equianalgesic and equipotent dose in each patch than there is in the equivalent strength duragesic, so it evens out. Also, if they implement my guess #1 for how they'll deal with the downside of matrix patches, there will be proportionally more sufentanil than necessary in the patch than there is more fentanyl than necessary in the mylan fentanyl patches. This would make cheeking them even more fun than cheeking mylan fents, since there's more opioid overall. Since it's a 7 day patch, you'd only need teensy tiny pieces though... sufentanil is 10x fentanyl in potency and there's 7 days worth in each of those small little mylan fent sized patches.
I'm actually glad, from an abuse and OD potential standpoint, that Durect chose matrix as the design for their sufentanil transdermal system. Gel sufentanil seven day patches would just be a disaster -- people would drop like flies... 7 days worth of sufentanil in a gel patch + smoking it + short 4.5 hour half life (a little shorter than fentanyl's) = crack like behavior, and tons of ODs.
The fact that they're matrix patches means that even cheeked the small piece you put in, while it release MUCH more quickly than if it were worn as Rx'ed, and will certainly get you high, will still retain some of its time release. That basically means if you feel like it's getting to be too much, all you've gotta do is take the patch out of your mouth and you'll be OK. Mylans or pieces of them release all of their fentanyl contents in about 8 hours in my experience, compared to 72 hours when worn as prescribed on the skin -- this gets me high when I do it. I'd imagine transdur-sufentanil would release its sufentanil content over about the same 8 or so hours. Just gotta be sure to use a very small piece since there's a LOT of sufentanil in each of those patches. Since they'll compensate even more than mylan does for the downsides/cons of matrix patches most likely, they'll likely be even more abusable than mylan is by cheeking. Just be careful and enjoy sufentanil.
Honestly, cheeking small pieces of the new sufentanil patch coming out, to me, sounds like the only way to go. Had gel sufentanil patches came out, the smoked high would last even SHORTER a time than fentanyl smoked does, since sufentanil has a half life about half the length of fentanyl. It would not be worth it.... just too short.
Cheeking these sufentanil patches, on the other hand, will likely provide a lovely, time released, 10 hour high on the probably lovely drug sufentanil.
How do you guys feel about this sufentanil transdermal patch coming out, whether you're a CP patient or looking to cheek small pieces of them to get a nice, PPT length buzz? I'm excited personally to see an new arrival coming onto the scene of a potent opioid since it doesn't often happen. I'd be more excited to see a transdermal patch of a NON fentanyl family opioid come onto the market (like 14-cinnamyl-oxycodone transdermal system), but this is exciting enough for me.
I'm stoked :D
WOW that was a long post. Feel free to NOT read all of it if you want.... if you just skipped down to this last line, just say how ya feel about sufentanil likely becoming a prescribe-able CII opioid in the U.S.