Buprenorphine Implants Show Promise

Tchort

Tchort

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Drug addicts could benefit from an Implanon-style buprenorphine implant that overcomes many of the problems of the current sublingual tablet addiction treatment, an Australian pilot trial suggests.

The opioid receptor agonist has been formulated in a matchstick subdermal implant that provides a steady state of the drug and which has proved effective in preventing cravings and withdrawal symptoms, a study in three Australian treatment centres has shown.

And unlike the sublingual tablets of buprenorphine the implant avoids the risk of diversion and reduced the problems of non-compliance and the need for regular clinic or pharmacy visits, say the authors of a study published in the journal Drug and Alcohol Dependence (103: 37-43).

The pilot study in 12 heroin-dependent drug users who were already using sublingual buprenorphine found that they could be switched smoothly to the implant and their cravings and withdrawal symptoms remained at a low level for the six month duration of the implants.

Risks of illicit diversion are low because the drug is implanted under the skin and would difficult for users to remove. In addition, the use of a polymer matrix means the drug cannot be extracted for illicit IV use such as by soaking in water.

Users in the trial said they preferred the implant over sublingual tablets because the flat drug levels meant they did not experience opioid-like highs or withdrawal lows over the trial. The implants also proved safe, with only minimal injection site reactions. The study authors say the implants can be inserted and removed as a routine procedure by any medical practitioner with appropriate training, and could therefore be offered in a wide variety of settings, such as primary care, rather than restricted to specialist treatment or addiction centres.
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http://www.6minutes.com.au/articles/z1/view.asp?id=482589

6Minutes.com.au

5/25/2009

By Michael Woodhead

Buprenorphine Implants Show Promise
 
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On a related note, the small company Titan Pharmaceuticals is fairly close to releasing Probuphine; a subcutaneous implant of Buprenorphine.

Overview
Probuphine is Titan?s novel, subcutaneous implant formulation designed using its ProNeura technology to deliver six months of buprenorphine. Buprenorphine is currently marketed as a sublingual formulation for the treatment of opioid addiction.

In July 2008, Titan announced positive, statistically significant results from its randomized, double-blind, placebo controlled, multi-center Phase III clinical trial of Probuphine for the potential treatment of opioid addiction. Probuphine showed a clinically and statistically significant difference over placebo in illicit opioid use for the primary and key secondary endpoints.

Market Opportunity for the potential treatment of Opioid Addiction
Worldwide, it is estimated that there are 6 million opioid addicts. Approximately one-half of this potential patient population is addicted to illicit opioids, such as heroin, and the other half to prescription drugs, such as oxycontin, methadone, and codeine. Until recently, medication assisted therapies for opioid addiction had been sanctioned to a limited number of facilities in the US. As of 2002, physicians can be certified to prescribe opioid addiction medications in an office setting, which has greatly expanded patient access to opioid addiction pharmaceutical therapies. Currently, there are more than 750,000 people globally receiving medicinal treatment for opioid addiction.

Buprenorphine, one of the currently available opioid addiction treatments in the United States, is sold mainly in the form of a sublingually delivered tablet under the brand names Suboxone® (buprenorphine HCl/nalaxone HCl dehydrate)) and Subutex® (buprenorphine HCl ), with worldwide sales of $450 million in 2006. More than one-half of these sales were in the United States. Since its US approval in 2002, the number of doctors certified to prescribe buprenorphine has grown to approximately 13,000.

Overview for the potential treatment of Chronic Pain
For many of the same reasons that Probuphine offers potential advantages for opioid addiction, it is a promising candidate for the potential treatment of chronic pain, which represents a larger patient population than opioid addiction and a significant unmet medical need. Buprenorphine is currently approved for the treatment of chronic pain in Europe, primarily utilizing a patch formulation. Probuphine?s long-term delivery and stable blood levels of drug may provide certain advantages in potential treatment of chronic pain.
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http://www.titanpharm.com/products-candidates-probuphine.php
 
Tchort said:
Worldwide, it is estimated that there are 6 million opioid addicts. Approximately one-half of this potential patient population is addicted to illicit opioids, such as heroin, and the other half to prescription drugs, such as oxycontin, methadone, and codeine.

Currently, there are more than 750,000 people globally receiving medicinal treatment for opioid addiction.
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6 million opioid addicts world wide and only 750,000 receiving treatment for opioid addiction that seems really low to me! :\

Iran's population is 65,875,224 and they 2% (Or slightly more) of the population are Heroin/Opioid addiction, that means 1,317,504. people in Iran are opioid addicts.

Take that number away from the 6 million addicts world wide, that leaves 4,682,496 opioid addicts around the world, except for Iran. That does seem really low to me! :\
 
^^+1 Same thoughts that those numbers are too low. I wouldn't be surprised if there were 5 million addicts in the US alone... since that would be maybe around 1.5%
 
If I'm not mistaken these numbers are usually arrived at by adding the total number of people who have been admitted to a rehab/hospital for Heroin overdose/abuse/addiction plus the number of people who have been arrested for possession/dealing Heroin.

In some cases its a factor of double, triple, or more of their estimates. The official estimate of Heroin addicts in the US is like 750,000-1 million. Talk about a lowball.
 
This sounds like the Nuva ring for opiate addicts.

nuva_ring.jpg


Except you dont have to shove it up awkward places.
 
The number of 6 million worldwide sounded really low to me as well. For example, there are an estimated 1.5-2 million cocaine addicts in the US alone. Let us assume that are fewer heroin addicts than cokeheads out there and give a conservative estimate of ~1m herion addicts in the US--leaving only 5 million for the rest of the entire world. Seems small to me.

Iran's population is 65,875,224 and they 2% (Or slightly more) of the population are Heroin/Opioid addiction, that means 1,317,504. people in Iran are opioid addicts.
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I'm impressed that you knew exactly how many people were in Iran at that moment. ;) I'll go ahead and throw out a number and a country too: there are 60,995,693 people in the UK and 296,971 are dope addicts.
 
Gaz_hmmmm said:
6 million opioid addicts world wide and only 750,000 receiving treatment for opioid addiction that seems really low to me! :\

Iran's population is 65,875,224 and they 2% (Or slightly more) of the population are Heroin/Opioid addiction, that means 1,317,504. people in Iran are opioid addicts.

Take that number away from the 6 million addicts world wide, that leaves 4,682,496 opioid addicts around the world, except for Iran. That does seem really low to me! :\
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There has got to be a bigger addiction percentage than 2% in Iran.


Anyway, a subcutanous implant for OST has always kinda been a dream of mine. Too bad its limited to partial agonists like bupe due to overdose risks. I think it will be hard to make one for a full agonist. Injecting enough drug to kill you 10 times over and have your life lie in the time release mechanism..
 
How much bupe does the implant release in 24hours?

It would be no good for me, as reducing the dose would be close to impossible (I'm guessing?)
 
Eight0Eight said:
How much bupe does the implant release in 24hours?

It would be no good for me, as reducing the dose would be close to impossible (I'm guessing?)
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I'm sure the amount is determined by your doctor.

Titan and several other Pharma. companies are developing the subcutaneous implant technology. Any drug can be put in the device and used in this fashion. Any drug at any dose.

I am not certain, but from what I gather the implant does its own internal taper at the end of the lifespan of the implant. I'm pretty sure if you leave it in instead of getting a new implant after the month or 3 month lifespan of the pellet, the levels of Buprenorphine (or other drug) drop slowly as if you were doing a taper.

Anyway, a subcutanous implant for OST has always kinda been a dream of mine. Too bad its limited to partial agonists like bupe due to overdose risks. I think it will be hard to make one for a full agonist. Injecting enough drug to kill you 10 times over and have your life lie in the time release mechanism..
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It's no dream; Axxia Pharma working with Johns Hopkins in Baltimore has been working on a Hydromorphone subcutaneous pellet system for over a decade. I have been in contact with them via e-mail about using the HM pellet for MMT patients who are sick of the side effects of Methadone (this is one of the primary functions they want the pellet to serve, the other being to provide round the clock pain relief for end stage cancer patients who can't swallow pills or take parenteral / injectable drug either). They just told me to stay in touch for when they do trials on MMT patients.

From what I understand this is being done or researched in Europe as well.
 
ahhh the wonders of drug super science. Cool post =)

wonder how long it lasts..
 
i want a hydromorphone pellet

the constant-blood-concentration would be awesome. they give out one methadone dose a day, and it makes me feel high/tired in the morning, then sorta sick at night. it sucks

with so much less of the side effects that i hate like sweating and hot flashes and sucky body temp regulation, and constant blood serum concentration, plus the fact that hydromorphone is just awesome, the HM pellet would be wonderful
 
i want a hydromorphone pellet

the constant-blood-concentration would be awesome.
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For a brief time. These pellets deliver the drug at a constant rate. Eventually your tolerance will match the delivery amount, and you won't feel any of the desirable effects.
 
phrozen said:
For a brief time. These pellets deliver the drug at a constant rate. Eventually your tolerance will match the delivery amount, and you won't feel any of the desirable effects.
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As a post-oral/IV/sublingual maintenance treatment, I think this would be great. Continuing to absorb maintanence levels of narcotics without having to actually consume narcotics; the last step in ORT before abstinence. Plus HM has fewer side effects than Methadone (a big reason I'm interested in the first round of tests with the pellet on MMT patients). It would be just about like living without opioids; no consciousness of their effects, fewer if any side effects, etc.
 
Actually this would be wonderful for those of us using low dose opiates for depression, I wonder if they will make very low dose versions?
 
phrozen said:
^
Only thing left is the psychological aspect of addiction... :|
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For most opioid addicts, the long period of abstinence from the high-low blood serum levels of active addiction (abuse) is the best treatment for compulsive use of opioids. I see this kind of depot pellet injection as the best jump off point for someone wishing to end Opiate Replacement Therapy; it removes all consciousness of using, kind of a training-wheels for sobriety.

Actually this would be wonderful for those of us using low dose opiates for depression, I wonder if they will make very low dose versions?
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I'm pretty sure the dose is determined by the physician, i.e. any dose can be put into the pellet depending on the patients needs.
 
For a brief time. These pellets deliver the drug at a constant rate. Eventually your tolerance will match the delivery amount, and you won't feel any of the desirable effects.
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that's the point of maintenance ...
Only thing left is the psychological aspect of addiction
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for those who use medically, maintenance can be all you need. but the psychological aspect could be addressed in therapy provided through the HM pellet program
 
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