The Abuse
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Instead of heroin, prescribed medications are abused.
Abuse can mean a wrong route of application. Instead of using it as prescribed orally, the medication is injected and all the negative effects of heroin injection are back. |
"Our data provide evidence that suggests that heroin use has become an increasingly marginal form of drug use among illicit opioid users in Canada, particularly outside of Vancouver and Montréal (port cities that are major heroin import points).
Instead, the use of prescription opioids in varying forms has become the predominant form of illicit opioid use. Recent data from the United States have indicated similar patterns, including evidence that the rate of prescription opioid abuse has exceeded the rate of heroin use in American household survey populations in recent years." [1] |
[1] B. Fischer, J. Rehm, J. Patra, and M. Firestone Cruz Changes in illicit opioid use across Canada. Can. Med. Assoc. J., November 21, 2006; 175(11): 1385 - 138
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Abuse in Austria
Intravenous abuse in Austria of sustained release morphine in substitution treatment. In morphine in substitution up to 45% of the patient admit to predominant intravenous abuse. |
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Substance and Antidote
Medical substance and antidote in one medication: Endonoxone combines the substance (morphine) with a non-active antidote (naloxone). Our medical knowledge was used to ensure that the antidote does not weaken the medication. An opiate addicted patient whose system is confronted with active naloxone will experience withdrawal. |
Endonoxone® can be used by opiate addicted patients
without withdrawal. [1] Agonist / antagonist mixtures as non abuse or with the goal of side effect reduction have been known for at least 20 years. In the market we presently see agonist / antagonist mixtures of oxycodone / naloxone; morphine / naloxone etc. Current contraindication in other agonist / antagonist combinations: “If used orally by individuals dependent on opiate agonists, withdrawal occurs” In case of the known agonist antagoist mixtures. Withdrawal is a severe up to life threatening condition in addicted patients and has to be avoided. |
[1] Proof of Concept Study of a Sustained Release Non-Abusable Morphine Medication in Heroin Substitution, EUDRA-CT-Nr.2009-012279-86
Endonoxone®is a registered treademark in Europe.
Endonoxone®is a registered treademark in Europe.
Strong but blockable
 Naloxone:
The protection Naloxone protects receptor cells in case of overdosage of opioids. It prevents intravenous abuse. |
 Morphine:
Strong opioid, abuse blocked Once in the blood (injected), naloxone keeps morphine away from the receptor cells. When naloxone and morphine reach the receptor of a nerve cell, naloxone has a higher affinity. It “sticks” to the receptor and thus blocks the morphine. |
 Buprenorphine:
weaker opioid, abuse not blocked Buprenorphine and naloxone have a similar affinity. Naloxone will not reliably block buprenorphine. Once in the blood buprenophine clings to the receptor cells instead of naloxone. Buprenorphine and naloxone: weaker opioid, abuse not blocked. |
Pictures by Fotolia: Lancelot by Algol; Heimtückisch byAndreas Wolf; Abwehrhaltung by Schiddrigkeit
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Buprenorphine and naloxone
The medication of buprenorphine and naloxone is abused intravenously. If injected together, buprenorphine will stick to the opioid receptors, but not naloxone. Buprenorphine will have an effect, and not naloxone. The National Drug Intelligence Center stated 2004 “that Suboxone® can also been diverted and abused”. [1] Baltimore Sun, December 2007– “The Bupe Fix” - Naloxone does not always deter abuse Buprenorphine has a stronger binding capacity (receptor affinity) to the opioid receptor than naloxone. When both substances are available in the blood, the patient feels the buprenorphine effect. Naloxone has a weaker binding capacity. Intravenous abuse is possible. This bases on the fact that in case of application - orally or intravenously - naloxone has a higher binding capacity than buprenorphine. That means in case of application of buprenorphine and naloxone, buprenorphine binds to the receptor. Buprenorphine has thus an effect orally and intravenously. Naloxone offers no reliable abuse protection against buprenorphine. Binding capacities of different opioids [2]: Naloxone: 3,3 (2,7 – 4,1) nM, Buprenorphine 0,52 (0,41 – 0,67) nM Different binding affinity of naloxone compared to buprenorphine show that in case of co application buprenorphine will take effect, not naloxone. The clinical effect is similar to a pure buprenorphine injection. This leads to the FDA statement that the mixture of buprenorphine and naloxone can be and is abused. |
Morphine and naloxone
If injected together naloxone will stick to the opioid receptors but not morphine. Naloxone will have an effect and not morphine. Naloxone offers a reliable abuse protection against morphine. Binding capacities of different opioids: Morphine: 20 (13 – 31) nM, Naloxone: 3,3 (2,7 – 4,1) nM Different binding affinity of naloxone compared to morphine show that in case of co application naloxone will take effect, not morphine. The clinical effect is similar to a pure naloxone injection. This leads to the assumption that the mixture morphine and naloxone will not be abused. |
[1] http://www.justice.gov/archive/ndic/////////pubs10/10123/index.htm,%20http://buprenorphine.samhsa.gov/presentations/buprenorphine
[2] Alvimopan binding to the μ-opioid receptor: Comparative binding kinetics of opioid antagonists Joel A. Cassel, Jeffrey D. Daubert, Robert N. DeHaven European Journal of Pharmacology 520 (2005) 29–36
[2] Alvimopan binding to the μ-opioid receptor: Comparative binding kinetics of opioid antagonists Joel A. Cassel, Jeffrey D. Daubert, Robert N. DeHaven European Journal of Pharmacology 520 (2005) 29–36
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Testimonials
This is what a user said: |
"I use to shoot suboxone all the time for 6 months, It does dissolve in water and there is no need for heat, Suboxone kept me off dope and I would get a nice "bodybuzz" from doing it that way! CAUTION: DO NOT EVER shoot suboxone if you have ANY opiates on your recepters ANY what so ever, you will go into instant withdrawals due to the naloxone, I had at least 2 weeks of clean time from opiates before I began banging suboxone. This is just information and I dont recommend anyone to shoot anything into their veins or body." [1]
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[1] http://www.topix.com/forum/drug/oxycontin/TPCRDTC33CRSK8KQT
