New opioid approved by FDA in the past few days: tapentadol

[Tchort]

Ick, Norepinepherine Reuptake Inhibitor activity? Any opioid with significant neurotransmitter-bungling action makes for a worse withdrawal syndrome (in my experience anyway).

They are going the wrong direction with narcotic patents

 

[brutus]

Tramadol is a weird drug, sometimes I feel it, then other times I don't. I had a fairly decent tolerance to opiates and it would have me high as a kite. Other occasions when I had little to no tolerance I felt nothing, but other times I was nodding from it. I really don't like Tramadol because it's hard to predict what it's going to do to me.

This new drug probably will be all hyped up once doctors start to prescribe it widely. People will rant about how this new drug gets them so much higher than any other opiate and just all kinds of bullshit I expect. I just hope the drug reps don't trick doctors into prescribing tapentadol more often then better opiates such as hydrocodone for common pain.

 

[rachamim]

Tchort: That is the thing. What is so amazing is that the US (which is often the inspiration around the world SADLY) looks at these types of substances as innocuous. Aside from the FDA requirement it is super accessible in the US but the W/D of tramadol is probably the most dangerous of any opioid/opiate!

From the perspective of the Rx companies it is a grand slam, negate the Schedualing concerns and a decent therapeutic profile and voila! Money in the bank and a tonne more hypocrisy for the American system.

 

[Tchort]

Tchort: That is the thing. What is so amazing is that the US (which is often the inspiration around the world SADLY) looks at these types of substances as innocuous. Aside from the FDA requirement it is super accessible in the US but the W/D of tramadol is probably the most dangerous of any opioid/opiate!

From the perspective of the Rx companies it is a grand slam, negate the Schedualing concerns and a decent therapeutic profile and voila! Money in the bank and a tonne more hypocrisy for the American system.

They have it down pretty good. Throw out the name of any market, and add the words "Industrial Complex" after it, and we have one here in the US of A. The Pharmaceutical Industrial Complex shoves toxic chemicals that took millions of dollars to develop, research and market, put billions into advertising fueling the new species Hypochondria Americana, jack up the price to the max of what the market will bare, and pay $0 in taxes.

Something I love is when we purposely add chemicals to pharmaceutical formulations to cause horrible side effects/health problems if abused or taken in excess; Canada thankfully stood up to us and said this practice is illegal and unethical (re: Lomotil, narcotic + APAP preps, OxyContin w/methylcellulose, etc).

I feel sorry for the user population who become primary IV Tapentadol addicts. Who knows what kind of side effects, long term effects, withdrawal syndrome they have to look forward to- all because we won't use a true or mock archetypal Opiate to treat anything.

 

[brutus]

^ What dangerous substances does the FDA allow pharm companies to add to pills to cause health problems?

 

[rangrz]

^
atropine in american hycodan and lomotil?

unless your treating a problem involving excess acetylcholine, I see no need for atropine, as it only risks causing side effects, delerium, death, ect.

 

[StaffWriter]

^^Minute doses of the substance keeps people from abusing it. Basically, this sounds like an Effexoresque tramadol. Hopefully, us Suboxone folks can use it. We need better pain relief than tramadol. I for one hate Tramadol. I used to take 150mg with a large cup of coffee when I drove rental vans on 5-6 hour trips out in Oklahoma to keep from falling asleep. I remember having to roll down the window and puke my guts out because trams make me so nauseated. No other "opiate" makes me sick like that. And my doc wrote it because he said "it's gentler on the stomach than codeine." Liars. Anyway, it should be interesting to see what the deal is with Tapentadol.

 

[sunset117]

I think tchort means how they may add capsician(sp?) or naltexone but I don't really agree with his logic


IMO tho this drug may be interesting, shit how doesnt like new opiatesto try? But my expectations are low

Also, what's with the statement "its potency is somewhere between tramDol and morphine" ;that's a wide fuckin' scope yadidy

 

[Riemann Zeta]

I think that this is a very promising compound--it has at least the potency of O-desmethyltramadol plus a little more noradrenergic action...should be decent for anyone with chronic pain. Anyone want to bet on the Schedule that it gets? I'll bet Schedule III.

In addition, I'll bet that tramadol gets moved to Schedule IV soon. While I'm just pulling this out of my ass, I could see the pharm industry agreeing not to fight an immediate scheduling of tramadol in exchange for this one staying out of Schedule II. Considering that even codeine is C-II in the US, I doubt that any new opioidergic compound--no matter how weak or parenterally unabusable--would be anything but C-II without a little industry help.

 

[ofukibenhearB4]

i bet shedule 4 or 3 if were unlucky. this could be a Great drug and doctors are all afriad to prescribe you narcotics so shit like this will flood the market for awhile,.............maybe it will be DOPE and abuse rates will soar and it will go to schedule 2 or some shit who knows no one here has tried it....................

 

[Unknown]

I think that this is a very promising compound--it has at least the potency of O-desmethyltramadol plus a little more noradrenergic action...should be decent for anyone with chronic pain. Anyone want to bet on the Schedule that it gets? I'll bet Schedule III.

In addition, I'll bet that tramadol gets moved to Schedule IV soon. While I'm just pulling this out of my ass, I could see the pharm industry agreeing not to fight an immediate scheduling of tramadol in exchange for this one staying out of Schedule II. Considering that even codeine is C-II in the US, I doubt that any new opioidergic compound--no matter how weak or parenterally unabusable--would be anything but C-II without a little industry help.

Codeine is only class 2 for production (bulk) reasons. This is just a way to control (quota) natural alkaloids. The CSA also dictates how drugs are controlled in production.

As for this new drug being scheduled, it really depends. Look at the CSA, and find the scheduling requirements. It really comes down to the abuse/dependancy factor. Im going to shoot for class 4, with my gut telling me MAYBE 3.

 

[Tchort]

The inactive ingredients added to pills that are used intravenously by recreational users and addicts- Silicone Dioxide, Titanium Dioxide, Povidone, Talc, Magnesium Stearate, etc etc etc. Water soluble, inert ingredients are not only available as binders/fillers, they are used currently, and have been used in narcotic pills in the past (best example being the old Knoll Dilaudid 2mg and 4mg tablets). Plus the addition of ingredients whose primary action is to harm people who consume the product in a way not intended by the manufacturer- Acetaminophen, Atropine, Scopolomine, Ibuprofen, Aspirin, the mentality that gave us Suboxone (which thankfully didn't work the way they thought/said it would). Despite knowing that thousands of people are going to inject these pills regardless of what they put in them (including Suboxone, which was being injected by thousands even though the medical authorities at the time warned that doing so would result in immediate precipitated withdrawal), they continue to purposely poison users and addicts.

The only time I've heard of this policy being reversed is with the UK/AUS Temazepam gelcaps- a product purposely marketed to 'discourage' IV abuse, meaning Big Pharma knew these pills were going to be melted down and injected by countless thousands, and were formulated to cause ungodly pain and suffering (multiply the negatives of simple IV pill use, a whole gauntlet of thrombosis, abscesses, collapsed veins, gangrene, amputation).

If Tapentadol is more effective at treating a single disease/condition than medication currently on the market, I'm all for it. But I don't see it being any more effective than any of the synthetic narcotics (agonists and partial agonists) already on the market for treating a single thing. I foresee a new primary addiction of IV Tapentadol (just as we've seen with every narcotic that can be taken IV that was said to be a breakthrough, a 'novel narcotic', less addiction liability than Morphine, etc). Plus, with the NRI/non-opioid activity, a whole host of problems we haven't seen yet.

 

[Unknown]

^^^
Nicely said

The only thing I want to question is the statement where you said APAP was a harmful additive, which wasnt put in for that reason. APAP is not harmful to IV. As the case for hydrocodone, its strictly for the Class III scheduling.

After reading what you said, I really think it will be grouped into Class 3, because this drug seems to have a higher abuse potential, especially that it can be IVed and is a duel acting drug.

 

[Unknown]

Schedule III requirements:

(A) The drug or other substance has a potential for abuse less than the drugs or other substances in schedules I and II.
(B) The drug or other substance has a currently accepted medical use in treatment in the United States.
(C) Abuse of the drug or other substance may lead to moderate or low physical dependence or high psychological dependence.

Now compare the class III drugs with the class II drugs. I think it would be more suited for III. Also, doesnt this drug have to go under review by the UN, under the Convention on Psychotropic Substances rule?

 

[Tchort]

Sorry, I meant harmful for any kind of abuse, then narrowed into IV specifically. I'm positive Talcosis would set in long before Tylenol liver failure if you were shooting Percocets. It is a thinly spread lie that the NSAIDs/Aspirin are added to narcotic tablets as adjuvents for analgesia- it comes down to the DEA and prescription policing: a combination tablet will be scheduled lower than a narc-only tablet, because of the false notion that adding a liver-killing substance to happy pills will stop people from abusing them or becoming addicted to them (there are plenty of people, including celebrities, who are hooked on Vicodin/Percocet/all combo pills, and plenty who did ruin their livers with them).

CIII or CIV. Remember that Buprenorphine was CV for awhile. This drug probably fits that mold- it isn't a straight mu-agonist and doesn't have general pain killing use, could be initially scheduled low.

 

[delphinen]

I will stick to Codeine for the week and Oxycontin for the weekends. Trying to get out of the hell of Tramadol addiction- no matter how nice it feels O-Desmethyl, Tramadol its just W R O N G.

 

[djsim]

TChort: you've got a point, but it's a fact that codeine and APAP/ibuprofen provide synergystic effects. As with atropine and diphenoxylate (atropine slows the GI tract, allowing water to be reabsorbed more effectively). The only drug I can't rationalise is Suboxone; the naloxone is in there only to deter abuse, so in that respect you are right.
But, you are also right when you say compounded codeine preps are made that way because liver failure would occur before a high was achieved. I hate to say it but this is the case it seems... I have asked countless times (to lectures etc back at uni) why codeine single prep was in the most restrictive schedule, yet codeine + APAP was in the least restrictive schedule. I never got an answer, but it was always hinted that compounded things couldn't be abused. I guess its obvious why.
If a determent must be added I think it goes without saying it shouldn't be life threatening. It's pathetic that govt would rather you die of liver failure than get high on codeine

 

[Tchort]

TChort: you've got a point, but it's a fact that codeine and APAP/ibuprofen provide synergystic effects. As with atropine and diphenoxylate (atropine slows the GI tract, allowing water to be reabsorbed more effectively). The only drug I can't rationalise is Suboxone; the naloxone is in there only to deter abuse, so in that respect you are right.
But, you are also right when you say compounded codeine preps are made that way because liver failure would occur before a high was achieved. I hate to say it but this is the case it seems... I have asked countless times (to lectures etc back at uni) why codeine single prep was in the most restrictive schedule, yet codeine + APAP was in the least restrictive schedule. I never got an answer, but it was always hinted that compounded things couldn't be abused. I guess its obvious why.
If a determent must be added I think it goes without saying it shouldn't be life threatening. It's pathetic that govt would rather you die of liver failure than get high on codeine

It all comes back to money and power. That being the case, anything they do doesn't have to make sense- as long as no one has the power the challange them.

With Lomotil the doses of Atropine are not intended to be active (Wikipedia has the 25mcg dose in each tablet as 1/40th the active dose of Atropine)- the Atropine only becomes active when enough tablets have been consumed to abuse the Diphenoxylate. So the entire purpose of the Atropine is to poison the user, as when the pills are taken therapeutically as directed, the Atropine is inactive. This is true for the sister drug of Diphenoxylate, Difenoxin, which also comes with Atropine in minute doses unless abused. The thing with Codeine that you mention is true for Diphenoxylate and Difenoxin as well- CII when alone, CV w/ Atropine, just like Codeine w/ APAP. Same thing for Dihydrocodeine, and at higher schedules Pentazocine alone or with Naloxone, Hydrocodone alone or with APAP, etc.

While it is true that an NSAID/Aspirin will promote analgesia when taken with a narcotic, I do not believe that is a valid reason to combine them in one formulation. Many medical books, government sites, etc will admit as much (that the purpose of adding NSAIDs to opioid pills is to deter abuse).

Plus, everytime a new 'anti-abuse' mechanism is unveiled, it is defeated very soon thereafter, and a text file is up on the web with instructions how to beat it for IV use or safe oral use (TEVA OxyContin, Opana ER, Palladone when it was available, MS-Contin, etc).

 

[djsim]

I'm pretty certain the atropine does have an effect. Don't believe everything Wikipedia says. (I'll have to check so plz dont quote me on this yet)

What worries me more is that 9 of 14 of the drugs named requiring urgent research into off label use are psychoactive. ARTICLE

Pretty sad state of affairs when antipsychotics are being pushed off-label for geriatric anxiety and pseudo-dementia reasons, especially considering these companies never should be allowed to persuade doctors with off-label usage anyway.
But I digress... we're getting way off topic now. Maybe we need to start a "pharm company gripes" thread

 

[DexterMeth]

I wonder if it will make a shit load of people go into trippy ass (in a scary way, but still trippy) seizures like tramadol does every day to at least (i'd take a wild guess and say) 1 out of 10 tramadol users that go over the 800mg mark. I'd honestly be very interested in trying this opiate...tramadol is so underrated, and this is comming from a veteran...oh look at me, i'm cool, i was on 265mg of methadone for over a year, then suboxone...back to heroin...yeah! ...fuck that biz...still i'd try it