SARMS and trifluoromethyl groups Risks?

AK1

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Hi guys.

Any chemists here who know the potential side effects (short and long term) from using SARMs that contain these types of 'toxins'? I know that Osterine and LGD both contain these types of chemical groups in their structure.

SARMs are obviously growing in popularity due to their selective nature and theoretical advantages over traditional AAS due to less potential health risks (both short and long term).

I know there is quite a fair amount on the theoretical benefits of sarms and a lot of anecdotal claims (along with bloodwork in some cases) to suggest safer cycles.

What we also need is a thorough evaluation from people with good knowledge that are not tied to the companies who design or market these products who actually have solid knowledge in the chemistry.

A big ask maybe, but when it comes to this game - I really have realised that health and quality of life has to supercede the rewards we get from sport or bodybuilding and knowing what we are using and how it might affect us has to be part of that.

Yeah I want sarms to be a much safer alternative to ASS and the theory supports it, but in reality are they? And I don't really feel like waiting another 30 years to see if anybody from 2010 came off badly just to find out.....
 
kboxer7

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I do find it strange that "IF" this was a concern, it wasn't brought up in all the clinical studies done. Hundreds of participants have finished phase I-II (and more still in phase III I believe) for Osta and LGD.

The completed and published clinical trials don't mention it, and the published bloodwork for those clinicals don't really show anything out of the ordinary besides what you would expect from a less potent PH.

I mean why would a pharmaceutical company spending millions and millions on development and trials (shooting for FDA approval) intentionally design a compound with a functional group that is known for toxicity issues?

Just thinking aloud here.....
 
rtmilburn

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I do find it strange that "IF" this was a concern, it wasn't brought up in all the clinical studies done. Hundreds of participants have finished phase I-II (and more still in phase III I believe) for Osta and LGD.

The completed and published clinical trials don't mention it, and the published bloodwork for those clinicals don't really show anything out of the ordinary besides what you would expect from a less potent PH.

I mean why would a pharmaceutical company spending millions and millions on development and trials (shooting for FDA approval) intentionally design a compound with a functional group that is known for toxicity issues?

Just thinking aloud here.....
Pharma companies have got medications approved for sales before that were very unsafe. Phenfen for example
 
kboxer7

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Pharma companies have got medications approved for sales before that were very unsafe. Phenfen for example
For sure. It happens.

This just seems like it would have been a known issue beforehand though.
 

BlockBuilder

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From what I've read LOTS of drugs contain this triflouromethyl group like Prozac for example. So what's the issue?
 
AK1

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The issue is that has any LONG TERM tests or cases been looked at to assess how safe this stuff is long term?

Yes plenty of long standing legal prescription drugs contain a lot of common compounds - does this mean that they are entirely safe? No.

A lot of drugs are designed to combat a specific problem (usually an immediately dangerous one) but have a trade-off because they cause other side effects or potential health concerns that doctors expect people to just have to accept and live with because they are less serious or not immediately as serious as the inntitial health risk they are designed to treat.

Tamoxifen is a prime example. It is used to inhibit breast cancer, but itself is an aggressive carcinogen (which has been proven to be quite dangerous at ANY dose) .... Liver cancer is therefore a potential concern.

Pesticides are dangerous - yet we spray food with them, they end up in the food chain, and they end up as a toxin inside us.

There are plenty of drugs that are around for years before somebody says: "Hey hold on a minute.... Women are getting disproportionately diagnosed with ovarian cancer, their kids are often coming out with birth defects, and the men taking it seem to be overly susceptible to heart attacks and prostate cancer... Maybe we should check this out" - and then something finally gets recalled off the shelves - after the damage is done.

When it comes to supplements or PEDs we then enter an area where the drugs are not even dealing necessarily with an actual health risk and are not being used according to the chemistry framework that they were initially designed to be used within - which then opens things up to even more abuse - eg. The prescribed dose of anavar to burn victims for example (low) vs the off-label use for bodybuilders (much much higher) usually in a stack with other off-label doses of other steroids or PEDs...

So no, just because something is typically common 'now' it doesn't make me trust that it is completely safe and that it might not be found to have caused some irreversible damage later on...
 
AK1

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I do find it strange that "IF" this was a concern, it wasn't brought up in all the clinical studies done. Hundreds of participants have finished phase I-II (and more still in phase III I believe) for Osta and LGD.

The completed and published clinical trials don't mention it, and the published bloodwork for those clinicals don't really show anything out of the ordinary besides what you would expect from a less potent PH.

I mean why would a pharmaceutical company spending millions and millions on development and trials (shooting for FDA approval) intentionally design a compound with a functional group that is known for toxicity issues?

Just thinking aloud here.....
Yes, what they have shown seems promising as they note no obvious or immediate health factor risks.

But what I am still not confident about is how far or thorough they have been - are they not bias? I mean how far are they willing to look to find any health risks (particularly long term). Baring in mind they are probably excited and want the development to work. Of course they have to demonstrate that the product is safe on a foundational level which they have done (openly it seems), but again have they looked at some more intricate details, do they even know potential concerns of some of these flouro groups themselves? The research needs to be looked at on those compounds independently, which as far as I can tell seems to be very limited - that is concerning.
Yes maybe nobody initially got ill or suffered badly on blood tests, but then again is there a blood test for heart structure alteration or accelerated cancer potential in later years? No - that can only be determined later, once damage starts showing up.

I want to know that all aspects of these drugs are open to scrutiny with full accounts of their potential risks.
 
kboxer7

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Yes, what they have shown seems promising as they note no obvious or immediate health factor risks.

But what I am still not confident about is how far or thorough they have been - are they not bias? I mean how far are they willing to look to find any health risks (particularly long term). Baring in mind they are probably excited and want the development to work. Of course they have to demonstrate that the product is safe on a foundational level which they have done (openly it seems), but again have they looked at some more intricate details, do they even know potential concerns of some of these flouro groups themselves? The research needs to be looked at on those compounds independently, which as far as I can tell seems to be very limited - that is concerning.
Yes maybe nobody initially got ill or suffered badly on blood tests, but then again is there a blood test for heart structure alteration or accelerated cancer potential in later years? No - that can only be determined later, once damage starts showing up.

I want to know that all aspects of these drugs are open to scrutiny with full accounts of their potential risks.
Certainly valid points.

I hear Osta is going to be FDA approved very soon (not that this would mean it's entirely "safe" at all).
 
AK1

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Okay. So I have been doing some digging around in an attempt to get some kind of information together. Agreed I would rather have been able to find research that provided some clear conclusion which can be applied quite broadly and comprehensively - but I have found none. Furthermore some of the of the information really needs some more referencing and factual evidence to support it. I'll share some finds anyway.

Here is a couple on why fluoride can allegedly be dangerous (though this is within the context of water fluoridation):

http://articles.mercola.com/sites/articles/archive/2013/04/30/water-fluoridation-facts.aspx

http://www.nofluoride.com/

Okay here is one that claims that adding fluoride to drugs can have some very negative affects (again I would have liked to have seen more evidence here to support the claims):

http://www.rense.com/general12/fl.htm

Here is a wikipedia page on Fluoride toxicity which suggests that fluoride in low concentrations is safe and that fluoromethylation of drugs will not actually release active fluoride into the blood (this is obviously a significant point - O2 for example gives us life, however add a C to it (CO2) is toxic to us - the way molecules are structured together certainly affects how it behaves and interacts) - there doesnt seem to be much evidence though again to back up this claim that fluoromethylation is safe however...:

https://en.wikipedia.org/wiki/Fluoride_toxicity

No doubt elevated levels of fluoride are not good for heart, liver, thyroid or avoiding cancer, but do these fluoromethylated drugs a) produce enough fluoride to be harmful and b) even release the fluoride atoms to do any damage? - This really needs some evidence (which I guess the pharmaceutical companies are not exactly going to go out and look for on your behalf....)

There is a SARM - RAD140 which I am sure you have heard of which does not contain fluorodation (at least not on the label) - but it has only been tested on mice and monkeys which is not entirely valid and people are really looking into its 'neuroprotective' properties for cognitive function.... Now unless you already have alzheimers or something - do you really want to be f-ing about with your neurological pathways?? Until I can see some clear explanation of how it works (that isnt obfuscated with terminology that you need a neurophysiology phd to decifer) then I am reluctant to delve into it. On face value it might look safe, but who knows what hidden side effects could occur in the human brain that they are not looking for....
Here take a look at this and you might feel the same as I do on it:

https://www.reddit.com/r/Nootropics/comments/34zszn/rad140_on_cognition/
 
rtmilburn

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Okay. So I have been doing some digging around in an attempt to get some kind of information together. Agreed I would rather have been able to find research that provided some clear conclusion which can be applied quite broadly and comprehensively - but I have found none. Furthermore some of the of the information really needs some more referencing and factual evidence to support it. I'll share some finds anyway.

Here is a couple on why fluoride can allegedly be dangerous (though this is within the context of water fluoridation):

http://articles.mercola.com/sites/articles/archive/2013/04/30/water-fluoridation-facts.aspx

http://www.nofluoride.com/

Okay here is one that claims that adding fluoride to drugs can have some very negative affects (again I would have liked to have seen more evidence here to support the claims):

http://www.rense.com/general12/fl.htm

Here is a wikipedia page on Fluoride toxicity which suggests that fluoride in low concentrations is safe and that fluoromethylation of drugs will not actually release active fluoride into the blood (this is obviously a significant point - O2 for example gives us life, however add a C to it (CO2) is toxic to us - the way molecules are structured together certainly affects how it behaves and interacts) - there doesnt seem to be much evidence though again to back up this claim that fluoromethylation is safe however...:

https://en.wikipedia.org/wiki/Fluoride_toxicity

No doubt elevated levels of fluoride are not good for heart, liver, thyroid or avoiding cancer, but do these fluoromethylated drugs a) produce enough fluoride to be harmful and b) even release the fluoride atoms to do any damage? - This really needs some evidence (which I guess the pharmaceutical companies are not exactly going to go out and look for on your behalf....)

There is a SARM - RAD140 which I am sure you have heard of which does not contain fluorodation (at least not on the label) - but it has only been tested on mice and monkeys which is not entirely valid and people are really looking into its 'neuroprotective' properties for cognitive function.... Now unless you already have alzheimers or something - do you really want to be f-ing about with your neurological pathways?? Until I can see some clear explanation of how it works (that isnt obfuscated with terminology that you need a neurophysiology phd to decifer) then I am reluctant to delve into it. On face value it might look safe, but who knows what hidden side effects could occur in the human brain that they are not looking for....
Here take a look at this and you might feel the same as I do on it:

https://www.reddit.com/r/Nootropics/comments/34zszn/rad140_on_cognition/
I agree with about the part about not messing with your neurological pathways with unstudied drugs. However, there are a lot of things that mess with your neurological pathways that aren't well studied. Especially how they work, but we know that aren't necessarily harmful. Like DHT, dhea, pregenalone, choline, omega-3s all effect neurological pathways. Although we know that these are safe even though they aren't necessarily well studied on how they effect the brain. These aren't drugs though and they have been around since we have been alive. Unlike these drugs that have been around for MAYBE a couple decade and most are less then that.
 

redemption79

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Some thoughts on Fluoridation:
I'm one of a number of people who have found out the hard way that fluoridated drugs like the antibiotic "Levaquin" can completely change your life. Two days in and I felt like I tore both of my rotator cuffs. I thought it was an odd side-effect of the cold/lung infection I had. It wasn't until 6 days in and every muscle/joint in my body hurting that I realized I might be experiencing a side-effect from the drug. By the time I stopped taking it, both of my calves were cramped all day, every day. Every joint in my body felt like it was injured, even hands, feet, fingers...everything. I could barely walk. It was then that I started doing more research into the drug. I found that there is an active class-action lawsuit against the company for damages from tendon ruptures (most common achilles, which can manifest/be realized even a year after cessation), to severe nerve damage, mental problems, and death. A staggering amount of people have been affected to the degree that they can't walk for even years after taking just one or two doses of fluoroquinilones like Levaquin.
This issue brought me to a depth of study and research that I have not been in for years. I focused most of my efforts on first trying to learn how the drug affected me and any possible "x-factors" I had (I was also taking Omeprazole which I have reason to believe contributed to my unfavorable reaction), then subjects like collagen synthesis, mitochondria regeneration and energy production, and prevention of muscle wasting (I went from being the guy who was stronger than everyone around me to asking my wife for help lifting things). It was the latter that brought me back to looking into SARMS (I never seriously considered them in the past...always seemed too new and un-tested). After some searches and finding chmical structures, I noticed the fluoro group in both Ostarine and LGD. To be clear, I can't be sure that the fluoridation of LQ is solely responsible for the damage it did to my body. I also don't feel confident in theoretical chemistry enough to say that the fluoridation of SARMS could produce similar results. I however do consider it a considerable risk.

I realize this is long-winded and only loosely related to the thread, but I urge anyone taking these fluoridated compounds to be cognizant of what their body tells them. If you start experiencing excessive and un-characteristic joint pain and/or impingement, STOP. It could be the most anti-bodybuilding thing you ever put in your body.
 
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Whacked

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Interesting. In......
 

BlockBuilder

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Ok well I'm on ostarine and my joints feel amazing
 
Whacked

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What the heck is it about Ostarine that imparts such a positive joint healing benefit. There is nothing in the literature that would corroborate all these anecdotal reports. It cannot be dismissed as it's very common.
 
smith_69

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Pharma companies have got medications approved for sales before that were very unsafe. Phenfen for example
yes and no- Phen was also combined with another drug (phentermine) to enhance the effects, original standalone product produce so so results, but nothing amazing. Also, read up on the FDA's approval of this process, they should have been more proactive.

Anyway, you cant compare testing compounds that have not reached final phase testing to products that were released for sale. Some of the SARMS had testing stopped and didn't pursue final stage testing for various reasons. Either funding or end results were not showing significant promise at the time to continue testing. May have needed further research on the product so an added compound could be added to enhance the effect of the sole product to see the results that pharm companies were interesting in seeing. End result, how much profit can be made vs long term potential hazard.
 
smith_69

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What the heck is it about Ostarine that imparts such a positive joint healing benefit. There is nothing in the literature that would corroborate all these anecdotal reports. It cannot be dismissed as it's very common.
first we need to verify the product itself. what is in that pill? how pure is the source? where did it come from? was it manufactured in a safe environment?
 
Whacked

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Valid considerations.
 
sanmarino

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One more thing: the argument, that pharma companies wouldn't spend "millions" of dollars for researching "waste stuff" is a valid point. But you maybe know the phrase: "if you fail, you will learn".

The SR-9009 for example was only created to see how it interacts, it was in the first way not planned to use it for humans. If it has beneficial effects they would optimize the SR-9009 but actually it is like Windows NT, one of the most basic structures (like you would take cholesterine and research how it "works" without knowing that you could "invent testosterone). But the companies were greedy after the success with Ostarine and LGD. SR-9009 in fact is the probably worst example to show, how the "supp" companies are aiming for profit without ethically and morally aspects. In the end, the enduser is responsible for itself.
No normal person would order research chemicals and use them at his own bodies.

But as you all say right, there are some interesting compounds in the stage III, which looking very promising. RAD-140 and YK-11 are stage 0 without even in vivo studies (but should start soon).

Let's wait what the future will bring us :)
I hope, it won't have a (too) bad impact on our lives haha
 
saywutrly

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First off, I would never gauge my assessment of the safety of a product on the FDA approval. There are mountains of evidence to prove that FDA approval can be bought more easily than it is earned.

FWIW, regarding safety of compounds which contain fluorine/fluoride moieties, I recall that the effects are structure-dependent. When dealing with a different scene I was into before bodybuilding, there were certain locations on the structure of a molecule which were regarded as "safe" and the rest were considered toxic.
 

redemption79

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Ok well I'm on ostarine and my joints feel amazing
I guess that settles it then...

In all seriousness, this sentiment is part of what lead me to consider options like Ostarine. Unfortunately, it's difficult to process anecdotal information about something like this, unless the compound has been sent for testing to confirm that it is indeed what it has been claimed to be. There are numerous people on the web who have realized greatly varied results from Ostarine. Are the variations in results due to biological differences in testers/users, or are we even comparing the same compound?
 
AK1

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Some thoughts on Fluoridation:
I'm one of a number of people who have found out the hard way that fluoridated drugs like the antibiotic "Levaquin" can completely change your life. Two days in and I felt like I tore both of my rotator cuffs. I thought it was an odd side-effect of the cold/lung infection I had. It wasn't until 6 days in and every muscle/joint in my body hurting that I realized I might be experiencing a side-effect from the drug. By the time I stopped taking it, both of my calves were cramped all day, every day. Every joint in my body felt like it was injured, even hands, feet, fingers...everything. I could barely walk. It was then that I started doing more research into the drug. I found that there is an active class-action lawsuit against the company for damages from tendon ruptures (most common achilles, which can manifest/be realized even a year after cessation), to severe nerve damage, mental problems, and death. A staggering amount of people have been affected to the degree that they can't walk for even years after taking just one or two doses of fluoroquinilones like Levaquin.
This issue brought me to a depth of study and research that I have not been in for years. I focused most of my efforts on first trying to learn how the drug affected me and any possible "x-factors" I had (I was also taking Omeprazole which I have reason to believe contributed to my unfavorable reaction), then subjects like collagen synthesis, mitochondria regeneration and energy production, and prevention of muscle wasting (I went from being the guy who was stronger than everyone around me to asking my wife for help lifting things). It was the latter that brought me back to looking into SARMS (I never seriously considered them in the past...always seemed too new and un-tested). After some searches and finding chmical structures, I noticed the fluoro group in both Ostarine and LGD. To be clear, I can't be sure that the fluoridation of LQ is solely responsible for the damage it did to my body. I also don't feel confident in theoretical chemistry enough to say that the fluoridation of SARMS could produce similar results. I however do consider it a considerable risk.

I realize this is long-winded and only loosely related to the thread, but I urge anyone taking these fluoridated compounds to be cognizant of what their body tells them. If you start experiencing excessive and un-characteristic joint pain and/or impingement, STOP. It could be the most anti-bodybuilding thing you ever put in your body.
Not long winded at all - thanks for being open and honest. We really need more contribution like this to get into some more sides of the issue. Did endocrinologists/Neurologists etc diagnose you and directly associate symptoms with use of Flouride-group drugs?
 
AK1

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Here is a link for the antibiotic drugs known as flouroquinolones that Redemption has suggested caused his exceedingly horrendous side effects Ive had to take out link as i do not have enough posts:

articles.mercola DOT COM - fluoroquinolone-antibiotic-side-effects

It would appear that if this article can be trusted as accurate and unbias then these drugs should be categorically avoided.

And again if true, it honestly amazes me as to how the medical profession and the US government can just sit by and accept this as acceptable. It would completely add credence to my previous statement about many prescription drugs and pharmaceutical companies being far from safe, ethical or dependable.
Of course if these kind of drugs still easily get manufactured, sold, distributed and prescribed every day then what does that imply about the drugs that go into the supplement industry? Do we take their word for it that they are any safer?

Of course a wikipedia search on Quinolones returns much less dramatic feedback, suggesting that the risks (whilst there) are considerably lower than what the first article is suggesting, which would support why the medical profession and the FDA have moved slowly on the warnings (though warnings should be there from day one even if its a 0.0001 % likely side-effect - full transparency should be provided) . The first article is referenced (so maybe those sources should be consulted), but who knows - could they be pharmaceutical competitors aiming to take a stab at Quinolones for their own agenda?

We really need to work out what it is about these Flouroquinolones that makes them so dangerous in order to compare them to any other flouride containing drug before we can say whether this raises any transferable concerns. Does it even have anything to do with the flouride or is it actually just the overall action of all or part of the drug. From what I have been reading so far the eradication of bacteria and disruption of enzymes appears to be a large problem - but what specifically about the drug causes that?

hormonesmatter DOT COM : fluoroquinolone-antibiotic-dangers
This seems to have some fairly decent scientific content (sourcing may need looking at) - from what I gather here it seems to be traits of these specific drugs that are causing specific problems with mitochondria etc - it doesnt reference other flouro-drugs (doesnt mean theyre safe though)
 

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