Sublocade - Curious? Theory For Many Successes & Failures

Buprenorphine Thesis

I'm sure many of you are either perplexed or even intrigued by these Sublocade reviews mentioning miracle-like discontinuation of Buprenorphine (Suboxone/Sublocade) with little to NO withdrawal symptoms. Alongside polar-opposite reviews mentioning terrible induction withdrawals, particularly on day 4 i'm noticing. Well, I believe I just might have the answer to both of these questions or at the very least a solid theory.

Everything I'm stating below is nothing more than theoretical. I am not a Licensed MD or Doctor. Having been on Suboxone for more years than I care to admit, I share these theories with you as a fellow addict familiar with all the "ins-and-outs" of opiates and their processes. This is nothing more than my personal opinion and should not be utilized as medical advice.

Has anyone ever noticed when you are trying to quit any opiate, the withdrawals we are all too familiar with make it an impossibility to get more than 5 minutes of poor quality sleep at any given time? With every opiate withdrawal symptom on the COWS scale happening to you, this is far too taxing on the body. Now add the fact that your brain/body can never make it to Stage 2 in the sleep cycle (REM Sleep) at around 15mins after falling asleep. Its NO WONDER the body has a hard time coping and recovering! When our body's most basic of recovery methods is no longer taking place as it should Night after night after night, the agonizing withdrawal process we're so used to could very well be longer and far more torturous than is necessary. I'm just recovering from COVID-19 and I think its fair to say the same be said for certain viruses. When does the cut become a scab? When does the brain healing take place? I believe all the magic of most healing takes place during sleep.

Having said that, when going through opiate withdrawal I personally have taken notice that if I'm lucky enough to fall asleep, I truly feel SO MUCH BETTER! Particularly if it was a deep, All Stages FULL SLEEP CYCLE (90mins). The more the merrier, the more time & sleep cycles you get to heal your brain, the faster the healing. I HYPOTHESIZE THAT SLEEP IS ESSENTIAL TO THIS AND TO YOUR PHYSIOLOGICAL RECOVERY!

When we take our daily dose of sublingual suboxone, subutex, etc. That single 8mg dose in the morning causes our buprenorphine blood level to RISE & FALL throughout the days in which we live. There is no consistency there; sure maybe daily consistency. But if we're to take a closer look at the amounts of buprenorphine actually running through our Cardiovascular system and at what levels are crossing the BBB (Blood Brain Barrier) it is ever fluctuating.

An example: (Given that the average half-life of Buprenorphine is approximately 36hours)

DAY 1: 8mg @ 9:00am (Blood levels spike to 8mg at 10am and gradually decrease with time)

DAY 2: 8mg @ 9:00am (By 9am Day 2, your body has yet to eliminate urinate even 1/2 of the dose from yesterday morning. I'd estimate 5mg still running through you at 9am on day 2. By adding the next 8mg dose at 9am sharp, by 10am we are easily at 12mg+ within circulation but steadily decreasing with time)

DAY 3: 8mg @ 9:00am (By 9am Day 3, lets just say this persons metabolize speeds made it possible for blood levels to be at 7mg. Add to that your 8mg dose for the day & we're already at a whopping 15mg. As you can see, this process will continue daily and ceaseless INCREASES and DECREASES of buprenorphine only further confuse our brain chemistry. This is FAR from what biologists call "Homeostasis". In other words, "The body in balanced harmony", so to speak.)

**Quick Note: In a world of Black & White, this could bring levels to 1000's of mg right? Well, I don't think so, because we live in a more "grayscale" kind of world, its been scientifically proven that Buprenorphine has a "Ceiling Effect". For the average person, anything higher than 4mg will not make you "more high", even a 900mg dose would have little to no effect. The body has ways of dealing with excessive drugs, excessive water, anything! The reasoning is 2-fold, & Yes, I am aware that there are far more biological processes that contribute to all of this, but for the sake of a simple explanation, I give you 2:

1. The liver creates enzymes to help us metabolize the buprenorphine. Those enzymes being CYP3A4 and CYP2C8. Your body can only process or 'eat' so much buprenorphine at any given moment. Anything excessive that is not needed is typically sent to the kidneys and pee'd out.

2. This part has more to do with the "Ceiling Effect" and why it happens. Its been shown that once the brains receptors have become saturated with buprenorphine, this ceiling effect takes place. 2mg can work well for many people even though to many of us it seems like a puny dosage. The reality is that buprenorphine has an extremely high binding affinity (it glues on so tight). This binding is so strong that when measured mg-for-mg, buprenorphine mimics the potency that of fentanyl. The difference here being Partial VS. Full Agonist drugs. 2mg Bupe = Effective ... 2mg Fentanyl = Dead or OD. Medicinally dosing patients on fentanyl happens at the Microgram scale, not the milligram scale which is indicative of how strong those substances really are.

That 2mg Buprenorphine dose may be small, but does its job all too well and will give every bit of relief/satisfaction for your receptor as quantum-physically possible as it occupies the receptor. On the other hand, anyone who takes 2mg, yet feels a little better but is still in withdrawal, their brain may have more vacant receptors than 2mg can even physically occupy. Its unfortunate, but as we prolong our addiction, the addicted brain creates more and more receptors without regulation from endogenous morphine (AKA Endorphins, which opioid dependent people no longer make within their own bodies. All those extra receptors will require 'feeding’ to subside the hunger for opiates, only exacerbating the problem. Taking 2mg more for a total of 4mg would have most feeling satisfied and eliminating withdrawal symptoms altogether. Partial Agonism is responsible for this concept, in regards to traditional full-agonist opiates, (Including synthetics such as Methadone) overdose is definitely possible! (Highly unlikely any Full-Agonist at 4mg will cause overdose, Except for opiates higher than Hydromorphone on a typical "opiate strength conversion chart" and even thats a stretch. But thats a different discussion.

To be clear, Everyones body is unique and each person responds to substances in different way, at different rates, etc.

THE SUCCESS OF SUBLOCADE:

Now imagine having received your 1st SUBLOCADE injection at 300mg. This drug formula has been engineered for consistency. Basic Math - 300mg divided by 30 days, we're looking at 10mg at any hour, of any day, for the next 30-40days. Long gone are the days of the daily dosing example above. No more 8mg - 5mg - 12mg - 7mg - 15mg, No more UPs and DOWNs.

Now, lets say you get your 2nd shot of 100mg. Sure, your dose is significantly lower than the 1st injection by a factor of 200mg, but EVERY-SINGLE-NIGHT, you managed to sleep an 8 hour night. Everytime we do this successfully, the brain is getting acclimated to this new consistent dose of 10mg. When we sleep, the brain heals itself and makes adjustments accordingly. Even from a psychological point of view, TOO MUCH CHANGE in a persons life at any 1 time is a recipe for disaster and is simply too overwhelming for most. I'm confident suggesting the same can be said for your physiology, your body freaks-out initiating withdrawal.

So now, its DAY 40 (or 40 days since last SUBLOCADE injection). At this point that reliable 10mg's is starting to diminish.

DAY 41 - 9mg
DAY 42 - 7.5mg
DAY 43 - 5mg
DAY 44 - 3mg
DAY 45 - 2.3mg
DAY 46 - 1.8mg
DAY 47 - 1.2mg
DAY 48 - 0.8mg
DAY 49 - 0.6mg
DAY 50 - 0.43mg
DAY 51 - 0.27mg
DAY 52 - 0.15mg
DAY 53 - 0.08mg
DAY 54 - 0.05mg

The example above was just my best guess using basic mental math, considerations for biological half-life, and is more typical of a single-dose that is wearing off over time. But we must not forget about The SUBLOCADE formula. There could still be .5mg that remains within the gel under your skin. These are fresh, brand new, unprocessed buprenorphine molecules. Once released into circulation, the clock can start ticking. So you might not exactly get your very last 10mg at this very moment and then abruptly tank your blood levels every minute after. Who's to say that on day 49, a little bupe thats been stuck in the gel finally made its way into your blood stream for use and processing. BOOM! you'd go from 0.6mg to 0.9mg. However, i think its far less subtle... further suggesting this drug formula was engineered for gradual consistency. I firmly believe that as long as you’re able to get some sleep each night, the SUBLOCADE taper is soooo gradual, the repairs your body makes during sleep are sufficient to keep up with dropping levels and stave off withdrawal symptoms. Furthermore, many addicts have attempted to taper-off of Suboxone. When approaching the 0.5mg dosage or less, its near impossible to daily dose yourself accurately. Day 1, you think you've cut off exactly 1/16th of a Suboxone strip, but DAY 2 another 1/16th cut strip. 1st day= 0.2mg. 2nd day = 0.4mg. So in reality there is no way to measure where the Buprenorphine is located within the suboxone strip or tablet. I myself even used to think i could see the circles which at the time I assumed must be the Buprenorphine drops or something of that sort. But is it the Buprenorphine or is it the Naloxone that is those circles? There are far too many variables that are inaccurate and unmeasurable.

Sublocade appears to potentially solve this issue on the microgram level. The rate of change is not too quick or overwhelming and the body can keep up fairly well by recovering during sleep. Another solution to the problem of inability to micro-dose would be research and development by INDIVIOR or any Pharma-company into a new product containing buprenorphine levels close to that of the “Butrans” Transdermal Buprenorphine Patch for pain management. This would give those seeking to taper off of Suboxone a far better chance at success! This however isn’t so profitable for companies who benefit from you STAYING on the medication.

Bureaucracy aside, I believe this is why the CDC recommends all opioids tapers be long and gradual processes. The CDC has been clear that a cold-turkey withdrawal should be avoided at all costs. I myself was saving up to pay for a "Rapid-Detox" procedure. (A controversial medical procedure where you're are put under general anesthesia, like with most surgeries. IV Naltrexone (Narcan's Big Brother, Long-Acting Naloxone if you will) is pumped through you for 45mins and your body is subject to incomprehensible precipitated withdrawals. Luckily, you are put under for this $20,000 procedure. But wait! If the CDC is recommending long drawn out opioid tapers, I'm not so sure i'm all that confident in the costly method; which condenses your 6-10 days of HELL ON EARTH, into a mere 45min period! Now that can't be healthy or safe. Especially after reading about so many peoples successes with this SUBLOCADE injection! I'm fairly optimistic about the future and my sobriety.

I'm hopeful that SUBLOCADE will be a single part of a multifaceted recovery solution of the future.

CONCLUSION:

I wanted to put my 2 cents in with regard to those who've had a negative experience. With every example i've laid out, is it possible that maybe the dose rhythm you were on had you with something like 8mg - 6mg - 10mg - 4mg - 12mg - 7mg. This pattern doesn't represent how much you’re taking, rather the amount of Buprenorphine that is circulating within your bloodstream about 1hr after your dose. These inconsistent blood levels have you're body/brain used to a wide range of Bupe at any given time. In this case, that range being from 4mg to 12mg and everything in between. This is not to suggest that fault can be put on any 1 person. I think its fair to say that this can or could have happened to ANY OF US!! I am forever grateful for your review though because it’s informative to those of us considering SUBLOCADE and ultimately provides us with a more honest picture come decision time.

So, you get this SUBLOCADE injection. if its the 100mg shot, you're looking at 3.3mg all day. Thats pretty low for most people on this discussion. You go from a daily range of 4mg-12mg, down to 3.3mg at the MAX at any given time, you better buckle up cuz you're in for a ride. That ride is long too, remember 36hr average half-life. That s*** would take 10+ days to maybe start subsiding withdrawal symptoms. I'm confident that THIS is why the SUBLOCADE instructions state that you must be stable on Suboxone or buprenorphine for at least 7days before receiving a SUBLOCADE injection.

I feel terrible and sympathize for even worse situations such as that person who commented on this thread and said they got the SUBLOCADE injection 24hrs after last opioid use. DISASTER! I'm so sorry that that happened to you.

Alright everyone, that's all I got. I'm very interested in hearing back from any of you, your thoughts on my theory, and any opinions or theories you may hold! I'm looking forward to trying the SUBLOCADE method, just gotta raise the money first!

Looking forward to your responses soon!

Thanks,
Anonymous

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REPORT

These boards are supposed to be specific for certain medication‘s. Lately the trending has been Adderall. Why the change in topic? This is not a trending subject.

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Look at the half life of buprenorphine. It is like 2-3 days, not just a mere 3 or 4 hours. It is a VERY LONG acting drug, and for this very reason it is PURE HELL to get off of it because for anyone, I don’t care who you are. I take opioid for pain and have completely stopped with bare minimal withdrawals and only hemp to help me. I would NEVER take buprenorphine.

They get you addicted to these VERY LONG acting drugs that will steal your soul when you do try to finally get off it. It is replacing one addiction with another. Use hemp products, like CBG, CBN, CBD, CBC (minor cannabinoids) non-psychoactive to get off that junk. In fact, Google “entourage effect”. These Doctors are using you to just make money. You are stronger than that, go buy yourself some minor cannabinoids and go tell your distributor and pharmacy to kiss your grits.

And to the person who said the hot topic is ADHD right now, you too should take a look at CBG, a minor non-psychoactive hemp derived rare cannabinoid that works better than any prescription medication for ADHD there is.

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Re: Jessika (# 1)

90,000 deaths last year by drug overdose. This is very much a trending topic. Thanks.

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I'm just here to say that "Sublocade" absolutely is the reason I was able to stop Suboxone & then of course.... The "Sublocade" itself in a relatively short amount of time with very minimal withdrawals. If you are wanting a way out of the "Suboxone" hold.... Talk to your Doctor about switching you to "Sublocade" and after a reasonable amount of time, you will be able to successfully be free from all of these medications. If I can do it, I promise you, anyone can. I was taking Suboxone for approximately 12 years or more. I'm so thankful that today I don't have to depend on this medication anymore to simply function in my everyday life.

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I have been on 2mg of Buprenorphine for a few years now. Started on 8mg (8 years total) due to pain meds from a bad motorcycle accident. I see your theory on how the injection will taper for you. I have been on the rollercoaster at 2mg. Some days are good some I feel a bit of WD. Back when the doc cut me off I was already in therapy and seeing a Psychologist for anxiety. I think at the time I tried kratom and that worked for a short time and made me sick. I was in bad shape as it took 5 surgeries to fix my leg injury. I was finally back on my feet almost broke and living in a basement. They tried every antidepressant on me with no luck. The first dose of Bupe took away all the multiple symptoms I had. I was unable to work and had nowhere to turn until I was started on bupe and within a month I was so much better and was able to land a great job. I reunited with my longtime GF who is now my wife and life was great for about 4-5 years. I slowly fell into a feeling not having any emotions, no libido and terrible social anxiety. I also had no energy and making it through the work day was getting hard. My performance at work slowly go worst and was let go this past May. Sorry for the ramble but kinda had to share my story. I will ask my doc if Sublocade is an option for me. I hate being on this drug for such a long time. I was almost at retirement age when I lost my job so just may fully retire and try to enjoy life. I was burnt out from my job and feel better. Thanks for the post and glad you where able to kick bupe.

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Re: Kf3355705 (# 4)

I’m with you 100%. I took 10mg Methadone for 3 years until one night waking up in the hospital with a huge mask over my face. I knew that I was a dead man if I didn't quit. I then went to a Detox rehab center for 5 days and they gave me suboxone.

My suboxone Dr prescribed me Bunavail for 7 years (16 mg Suboxone equivalency) and 8 mg Suboxone for 3 years. I would get panic attacks just thinking about life without Buprenorphine. There was no way I could ever quit. Heck my Dr. said that I’d be on it for life.

Fast forward to Sublocade. He said if I wanted to quit that this is the easiest route. I had a shot of 300 for 2 months. When I went in for the lab test, he said my urine was completely free of the buprenorphine! I felt completely normal. He decided to play it safe and give me the last injection of 100 at month 3 and guess what? I felt worse! That lasted for about 4 days and then normal. The symptom was fatigue and just foggy in the head nothing like normal withdrawals.

That was my last shot 6 months ago and feel like a million bucks.

I can’t believe they are still prescribing Suboxone for it only continued my addiction. Could not wait to dose up. I ran out of Suboxone one time and thought that I was going to die, literally. My skin crawled; I couldn’t lie down for a panic attack would kick in; couldn’t sleep; couldn’t eat; couldn’t sit still; it hurt to have water touch my skin.

Sublocade withdrawals were that I was fatigued for a few days. That was it.

Negatives: cost. $1,800 an injection. My insurance paid for it however but many companies will not for they want the cheaper option of films which do not help one become free of the chains.

Please please brothers and sisters, take the Sublocade. It is truly a miracle drug.

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Re: JimboF (# 5)

I was where you were 100% Didn’t want anyone to visit; lost my libido. Had to force myself with wife. Completely sucked. Sublocade kicked me in 3 months. Give it a chance, you can always go back to Suboxone if it doesn’t work but it will.

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Re: Kf3355705 (# 4)

How long have you been free and clear off Sublocade? I took 1-100mg dose 4 months ago and recently and I’ve very fatigued and lethargic for a month now. Idk if it’s an extended withdrawal but that’s what it’s feels like. It’s not horrible but I want my regular energy back.

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