What is the actual "release date" of a Cyp ester?

[BBC3]

For the purposes of ester life span (half-life), it would appear that this measure is totally subjective and based on application ( to a large degree). Perhaps 8 days in muscle associated fat, and maybe as long as 12 days if applied to heavy cell extremety type body fat. SO THIS FIGURE IS REALLY JUST A MEASURE OF TIME TO METABOLIZE OFF THE ESTER IN A GIVEN SITUATION. With that said:

What is the actual amount of time for a Cypionate ester to be metabolized in a muscle type fat related infusion?

The term half life has confused me here as I have up till now associated it as a "description of the condition of the bond. When in fact it would appear to be misused for the purposes. And we should be referring to more of a total life span of the ester.

For that matter, why the hell has the term half-life even been associated with ester metabolism?

 

[Bill Roberts]

Any given molecule of the drug is either in its intact form, or has the ester removed. (Except for a time frame probably under a millionth of a second while that process occurs.)

When that happens to a given molecule is a matter of chance. Some will hydrolyze shortly after being injected, others at later times.

The reason the term half-life is used is because levels fall according to that pattern. Basically the reason that this is the case is that once say levels have fallen to one-half, the rate drops to 1/2 of what it was when levels were at their peak, since there's half as great a concentration and thus at any instant only half the chance of a molecule happening to hit the active site of the enzyme.

So it takes the same length of time to get from peak concentration to 1/2 that as it does to get from that 1/2 value to the 1/4 value, etc.

 

[Conciliator]

Usually when people talk about the biological half life, they're referring to the clearance or elimination half life. That's because most drugs are quickly absorbed (usually orally, from the GI tract) and decline of the drug in the body is determined primarily from the elimination or "disposition," which is rate limiting. With intramuscular injections into oil depots, the rate limiting process is not clearance from the body, but absorption into the body. The body essentially eliminates the drug as fast as it's absorbed. Whereas longer esters have an absorption half life of several days to over a week, the clearance half life of the actual hormone is much, much shorter. When the ester is cleaved and the base hormone is released and enters into circulation, it's half life is usually a matter of hours, depending on serum binding. Since the absorption half life is so much longer, decline of the drug in the body corresponds to the absorption half life.

As for why esters limit the absorption half life, this paper on nandrolone pharmacokinetics explains that "The current understanding is that the rate-limiting mechanism governing the appearance of active steroid in the bloodstream is the retention of steroid esters from the oil vehicle depot due to oil/water partitioning, with gradual release into the extracellular fluid, where esters are rapidly hydrolyzed to liberate biologically active steroid." So in other words, the longer the ester, the more lipophilic it is and the more likely it is to remain in the oil depot. After escaping the depot, though, the ester is quickly removed by esterase, leaving the free hormone to produce biological activity.

Over time, the depot gets smaller and contains less total hormone. As that happens, the absolute release rate of the remaining hormone gets slower and slower. That's the reason the release is not liner, but exponential (assuming a half life).

That said, it sounds like you're drunk right now. I don't see how you invent so much nonsense terminology like "release date", "heavy cell extremety type body fat", and "muscle type fat related infusion."

 

[BBC3]

Thank you Conciliator for you always charming character judgement, as well as the feed back.

Thanks Bill for the brief. But here is my point. I have simply started from the notion of a "nuclear" type relationship in chemistry. So here is where I feel this description fails to serve properly. Sure, it is simply used as a UNIT OF TIME as a measure. Aside from a method of measurement, this denotation implies so much more. It is implying different rates of metabolism at different times, when I do not believe they exist. I have also seen people use the term "life span", and interchangeably, but I dont even think the difference is realized in those cases.

Clearly T(for example) will clearly only exist in the blood for a short time. And most will use lifespan for this purpose the same. But because really not long enough to merit "halves", for many conversations, It would appear more than that. The Steroid is simply breaking down at a steady rate as it is all exposed to the metabolising factors the same. So short of a condition where the depot as an injection, protects its self centrally by some inherent shielding action from metabolizing factors( imagine a spere having to be eaten from the outside in), it should not only not be applied, it is misused to denote simple measurement. BUT I GUESS THE BOTTOM LINE IS THAT IT DENOTES A RATE OF DIMINISHMENT, AND WITHOUT THAT WE WOULD BE DEALING WITH ONE SET TIME TO MATURITY. But wait. Isn't that that technical premise behind the esters hold in fat?? A time marked by the completion of the esterase activity triggering the release date? By strick technicality, the term "half-life" should not be used at all.

So, it just seems like half life is grossly misused for the purpose of generlizing the metabolism of the steroid as one method. Thus, this is the misleading factor the causes the misunderstanding of actual application. Why is it so generalzed. Because true rate of metabolism and the factors that affect it are poorly understood. More accurately would be to consider a "half-life" as a rate of metabolism as it compares to different interactions within the body. (1) Circulating T, (2) LIghtly held muscle lipodial fat interaction that occurs with post saturation of the muscle, (3) deep and well involved muscle related fat, & (4) deep body fat tissue stores. When visited from these specific perspectives, the term could be merited as accurate I would think. Clearly an effect of "lighter" ester attachement to the more active lipiodal type muscle fat occurs as muscle saturation increases, or there would be no steroid in the blood prior to 40 days. This is related to the premise I am discussing as steroid use efficiacy relates strongly to site application principles, and clearly relevant for short term AAS purpose..

It would appear the a significant portion of the steroid injection would be involving its self with the fat more associated with daily interaction, thus allowing for an "early release date". And that there are (4) levels of interaction to consider with regard to metabolism of esterfied steroids. Just some thoughts as always.

 

[BBC3]

Usually when people talk about the biological half life, they're referring to the clearance or elimination half life. That's because most drugs are quickly absorbed (usually orally, from the GI tract) and decline of the drug in the body is determined primarily from the elimination or "disposition," which is rate limiting. With intramuscular injections into oil depots, the rate limiting process is not clearance from the body, but absorption into the body. The body essentially eliminates the drug as fast as it's absorbed. Whereas longer esters have an absorption half life of several days to over a week, the clearance half life of the actual hormone is much, much shorter. When the ester is cleaved and the base hormone is released and enters into circulation, it's half life is usually a matter of hours, depending on serum binding. Since the absorption half life is so much longer, decline of the drug in the body corresponds to the absorption half life.

As for why esters limit the absorption half life, this paper on nandrolone pharmacokinetics explains that "The current understanding is that the rate-limiting mechanism governing the appearance of active steroid in the bloodstream is the retention of steroid esters from the oil vehicle depot due to oil/water partitioning, with gradual release into the extracellular fluid, where esters are rapidly hydrolyzed to liberate biologically active steroid." So in other words, the longer the ester, the more lipophilic it is and the more likely it is to remain in the oil depot. After escaping the depot, though, the ester is quickly removed by esterase, leaving the free hormone to produce biological activity.

Over time, the depot gets smaller and contains less total hormone. As that happens, the absolute release rate of the remaining hormone gets slower and slower. That's the reason the release is not liner, but exponential (assuming a half life).

This last paragraph would indicate that you feel there must be a "get to the center of the tootsie pop" effect related to the physical action of the "depot". I was under the assumption that it is all "equally accessed" by the conditions of the body...

That said, it sounds like you're drunk right now. I don't see how you invent so much nonsense terminology like "release date", "heavy cell extremety type body fat", and "muscle type fat related infusion."

At a minimum, half life is a poor use of wording in steroid life discussion, as the steroid is NOT AVAILABLE PRIOR TO FULL RELEASE OF THE ESTER. And this is greatly varied and somewhat random at best. So short of using the term for blood circulating amounts, it would appear incorrect.....

You continue living in you tiny little nondescript world, and I will continue endeavoring to strip away the ingnorance you perpetuate by ANY MEANS....... You are far more introverted than I initially gave you credit for..... Your continual drawing of lines in the sand will not get you far in life. Nor have I found that our mutually shared contoversial type approach to be all that effective with regard to a majority of principles.....

But none the less, thanks for the article. Now lets see how you are relating it...

 

[Conciliator]

It is implying different rates of metabolism at different times, when I do not believe they exist.
...
The Steroid is simply breaking down at a steady rate as it is all exposed to the metabolising factors the same.
...
By strick technicality, the term "half-life" should not be used at all

No. The steroid does not get metabolized at a steady rate. Serum testosterone undergoes exponential decay and there is an "elimination half-time." As Bill Roberts already explained to you, the greater the serum concentration of testosterone, the greater the likelihood of molecular interaction with metabolizing enzymes and the greater the speed of metabolism. As the concentration drop, the rate of elimination also drops. The testosterone is not "exposed to the metabolising factors the same." When there are fewer testosterone molecules, it is less likely that any given molecule will undergo metabolism.

The term "half-life" is correct, both conceptually and technically.

Also, I liked the adjective "lipodial" that you pulled out of your ass. You sound so smart when you make up your own jargon.

 

[Conciliator]

At a minimum, half life is a poor use of wording in steroid life discussion, as the steroid is NOT AVAILABLE PRIOR TO FULL RELEASE OF THE ESTER. And this is greatly varied and somewhat random at best. So short of using the term for blood circulating amounts, it would appear incorrect.....

No, it's not incorrect at all. There is an "absorption half-life" from the depot. As the concentration of steroid in the depot gets smaller, it is less likely for a given molecule to diffuse from the depot into the interstitial fluid where it can be hydrolyzed by an esterase. The rate of release from the depot decreases with time.

With a sustained release drug, like testosterone depot, the rate of absorption is the rate-limiting factor determining serum levels, not the rate of elimination. I don't think you understand this concept, which is called "flip-flop kinetics." To quote an academic journal article on the topic (that wiki references), 'The "trap" commonly fallen into is that the terminal exponential phase half-life following extra-vascular dosing is mistakenly thought to exemplify terminal drug disposition, when in fact it characterizes terminal exponential drug absorption half-life.' In other words, a mistake commonly made is to think that the half-life decay seen in net blood levels after an injection is due to drug elimination from the body (AKA disposition) when in fact is it follows the drug's half life of release from the depot (AKA absorption into the body).

I will continue endeavoring to strip away the ingnorance you perpetuate by ANY MEANS....... You are far more introverted than I initially gave you credit for..... Your continual drawing of lines in the sand will not get you far in life. Nor have I found that our mutually shared contoversial type approach to be all that effective with regard to a majority of principles.....

Your musings are not insightful or profound, they're inane ramblings that evince your ignorance of well-established pharamacokinetic principles.

 

[Stretch]

He's smart but he's an ^^ASSHOLE^^

Who uses this forum to show us MERE MORTALS how stupid we really are.

The only time he offers advice is to exert his supposed mental superiority.

I've never seen him just offer some helpful advice. He's always debunking someone else's statement.

Childish and Insecure

 

[Conciliator]

He's smart but he's an ^^ASSHOLE^^

I'd rather be a jerk than a nice idiot.

The only time he offers advice is to exert his supposed mental superiority.

I've never seen him just offer some helpful advice. He's always debunking someone else's statement.

Read the first post in this thread. I spent a good deal of time just answering BBC3's questions and explaining how drugs have half lives, both in terms of absorption and elimination.

 

[Stretch]

Conciliator

You continue to prove my point about your insecurity.

We are BOTH intelligent individuals.

The difference is only ONE of us is secure with who we are.

That's why you have to call me an idiot, even though you know it is untrue.

I can easily concede that you are intelligent because I am secure with my own intellect.

It's a much better life when you accept yourself for who you are friend.

 

[Stretch]

Usually when people talk about the biological half life, they're referring to the clearance or elimination half life. That's because most drugs are quickly absorbed (usually orally, from the GI tract) and decline of the drug in the body is determined primarily from the elimination or "disposition," which is rate limiting. With intramuscular injections into oil depots, the rate limiting process is not clearance from the body, but absorption into the body. The body essentially eliminates the drug as fast as it's absorbed. Whereas longer esters have an absorption half life of several days to over a week, the clearance half life of the actual hormone is much, much shorter. When the ester is cleaved and the base hormone is released and enters into circulation, it's half life is usually a matter of hours, depending on serum binding. Since the absorption half life is so much longer, decline of the drug in the body corresponds to the absorption half life.

As for why esters limit the absorption half life, this paper on nandrolone pharmacokinetics explains that "The current understanding is that the rate-limiting mechanism governing the appearance of active steroid in the bloodstream is the retention of steroid esters from the oil vehicle depot due to oil/water partitioning, with gradual release into the extracellular fluid, where esters are rapidly hydrolyzed to liberate biologically active steroid." So in other words, the longer the ester, the more lipophilic it is and the more likely it is to remain in the oil depot. After escaping the depot, though, the ester is quickly removed by esterase, leaving the free hormone to produce biological activity.

Over time, the depot gets smaller and contains less total hormone. As that happens, the absolute release rate of the remaining hormone gets slower and slower. That's the reason the release is not liner, but exponential (assuming a half life).

That said, it sounds like you're drunk right now. I don't see how you invent so much nonsense terminology like "release date", "heavy cell extremety type body fat", and "muscle type fat related infusion."

Read this post, particularly the last paragraph, and tell me again how this first post is NOT an attempt to diminish the intellect of the OP. Are you serious?

You are without logical argument.

 

[BBC3]

Good, then you got at least one of my points.......

Also, I liked the adjective "lipodial" that you pulled out of your ass. You sound so smart when you make up your own jargon.[/QUOTE]

 

[BBC3]

You are a complete misfit as you can not interpret attempts to laymanize a subject. You could take the fun out of a "Barrel of Monkeys"!!!!!!!!!!

Your musings are not insightful or profound, they're inane ramblings that evince your ignorance of well-established pharamacokinetic principles.[/QUOTE]

 

[BBC3]

I greatly appreciate your support. You are unaware of the level of singularity you are dealing with. This IS Darth Vadar....

Conciliator

You continue to prove my point about your insecurity.

We are BOTH intelligent individuals.

The difference is only ONE of us is secure with who we are.

That's why you have to call me an idiot, even though you know it is untrue.

I can easily concede that you are intelligent because I am secure with my own intellect.

It's a much better life when you accept yourself for who you are friend.

 

[BBC3]

I'll take nice idiot. You completely mis the whole premise. You only unbewittingly serve you predicted role... I think you could be a nice guy too. Try some time.... You might like it....
Making me call the kettle black..... CLITHEAD......

You bring up an interesting point or two, but the day has been too long and I grow weary of your function. If fact, whenever I need to get sleepy I usually pick up a SIMPLE PREDICTABLE READ, and bore myself to sleep. NIghty night, ConciBOY......

I'd rather be a jerk than a nice idiot.
Read the first post in this thread. I spent a good deal of time just answering BBC3's questions and explaining how drugs have half lives, both in terms of absorption and elimination.

 

[Stretch]

Ya, I can't stand that fucker. And we've been cool since my first post on Meso.

I've tried asking him intelligent questions many times and never can get a response. But he loves to get on and debunk the ideas of others or argue semantics....for the good of the board of course

 

[Conciliator]

We are BOTH intelligent individuals.

The difference is only ONE of us is secure with who we are.

That's why you have to call me an idiot, even though you know it is untrue.

Actually, after having one debate with you (starting at post #45 here), I don't think you're particularly intelligent. It's not because I'm insecure, it's because I honestly don't think you're nearly as smart as you think you are. Nothing personal. Just read the debate.

 

[Stretch]

Whatever you gotta tell yourself to sleep tonight. Any logical and insightful individual who looks at your posting history (at least for past couple months that I've been a member here) can see how much you relish, dropping in, making someone sound stupid then disappearing. Never have you shown a desire to help someone new learn anything. You are a contributor here ONLY for your own egotistical benefit. And I loathe you.


For the record.

I don't think I'm a genius.

But I'm NO IDIOT.

Definitely less educated, when compared to you, or any other veteran, in the topic at hand.

But in my life I've never been accused, by one that knew me, of being an idiot.

Done speaking with you for life.

Enjoy trying to trump others with your SUPERIOR MIND POWER...LMFAO

 

[Conciliator]

I've tried asking him intelligent questions many times and never can get a response.

You can never get a response? Really? The only time I remember you asking me a question was right here. And I kindly answered it. So much for the nonsense that you "can never get a response."

But he loves to get on and debunk the ideas of others or argue semantics....for the good of the board of course

Yes, for the good of the board. When I jumped in msbjohnston's DNP thread here and made several lengthy posts on DNP, I was trying to disseminate accurate information and squelch bro-lore and popular myth. You need to get over your knee-jerk disappointment of being corrected and argued with. Next time, try "Thank you for taking the time to post all of that information. I stand corrected." Instead, you'd rather get pissy and talk about how I'm such a meanie to you.

 

[Stretch]

done speaking with you for life.

Enjoy trying to trump others with your superior mind power...lmfao

I'm done arguing with you.

Honestly, I can admit that you may be onto something in your last post.

I do have a knee-jerk reaction to being corrected. It's not something I am familiar with, and it's not something I am particularly good at dealing with, having never grown accustomed to it. However, if I am to continue learning, in this area of my life it is something that I should work on.

That being said. I still feel as though you derive a certain degree of pleasure when posting, not from helping others, but from proving your own superiority. I can admit my faults, which is the mark of maturity, security, and inner-peace with one's true identity.