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- 1 Mediating against constipation
- 2 Heading
- 3 Naxolone and Childbirth
- 4 Naloxone and NMDA receptor
- 5 addiction...ology...
- 6 Qualitative effects of naloxone versus naltrexone
- 7 Suboxone
- 8 Pharmacodynamics
- 9 "Studies show that to give this to a person in severe pain would be unethical and inhumane."?
- 10 Administration (edit)
Mediating against constipation
Doc put me on a oxycodone/naloxone combination pill, with the reasoning being that the naloxone reverses the constipation effect (Im post-op on a procedure where constipation is very much an unwanted effect. Now, googling, produces this https://www.ncbi.nlm.nih.gov/pubmed/10601678 so its not a doctor brain-fart , but is this an off-label bit of inventive medicine, or is it a legit useand if so should that be in the article? It seems to be working, however anecdote!=data . 220.127.116.11 (talk) 22:47, 7 July 2017 (UTC)
Citation about naloxone's side-effects should be inserted. The side-effects listed here can all be caused by withdrawal syndrome, except the 'infection', which is a side-effect I for one have never heard of for naloxone. It can be caused by subcutaneous/intramuscular/ injection of grinded down Suboxone, but not of naloxone itself. So either a good citation for these side-effects is needed, or some serious editing should be underway.
Dr evi 666 08:41, 30 August 2007 (UT hh The stuff about naloxone's activity in Suboxone is mostly untrue. Naloxone does nothing to prevent IV or intranasal abuse, except by scaring people away from trying it. Buprenorphine's much higher affinity for opioid receptors makes the naloxone irrelevant.
Most of the side effects/withdrawal symptoms attributed to naloxone are in fact caused by buprenorphine itself. Naloxone is hardly absorbed sublingually. Buprenorphine, with or without naloxone, will cause someone on pure agonist opioids to experience withdrawal. Also, naloxone will not cause someone on buprenorphine to go into withdrawal.
Flopster2 12:16, 21 October 2007 (UTC)
@ Flopster2: Naloxone is added to the suboxone tablet for scaring people, that much is true. But there is a rationale behind all this: because of the large difference in bioavailability in different modes of administration; if a drug user takes suboxone sublingually so little naloxone is absorbed (due to low bioavailability of naloxone), no effect will be noticed. However, if it is injected intravenously or intramuscular, the naloxone in the tablet (now much more naloxone is available) causes an acute withdrawal syndrome. See also the following articles JOHNSON RE MCKAGH J: Buprenorphine and Naloxone for heroin dependence. Curr Psychiatry Rep (2000) 2: 519-526 and STOLLER KB BIGELOW GE WALSH SL STRAIN EC: Effects of buprenorphine/naloxone in opioid-dependent humans. Psychopharmacology (Berl) (2001) 154: 230-242.
And on a minor note: naloxone IS able to reverse several of buprenophine's effects, such as respiratory depression, analgesia and sedation albeit in high doses (much higher than in the suboxone tablet). I'm not sure how the mu-opioid receptor changes with addiction, but I reckon addicted people on buprenorphine (and possibly many more drugs acquired illegally) could go into withdrawal from naloxone. Dr evi 666 14:44, 1 November 2007 (UTC)
I suppose this would be original research, but it really doesn't cause any withdrawal whatsoever either intranasally or intravenously (tested in both opioid naive people and buprenorphine maintenance patients). Both of those routes feel more effective overall than sublingual, but because there's no rush, IV isn't worth the risk. Sure it will cause withdrawal in anyone on other opioids, but buprenorphine alone will do that. I have read reports to this effect online, and if I come across them again I'll cite them here. --Flopster2 22:55, 4 November 2007 (UTC)
The Stoller paper is about hydromorphone dependent people. In the "Nondependent" section of the Johnson paper, it states that "the combination (1:1 ratio) attenuated the acute opioid agonist effects." Note that the amount of naloxone used is much greater than in Suboxone. In the "Dependent" section, it states that those on Suboxone maintenance chose money over IV buprenorphine/naloxone (which is quite understandable), but it doesn't mention withdrawal. For those on all of the other opioids tested, it did cause withdrawal. Neither of these papers say anything about precipitated withdrawal due to buprenorphine alone, but there are plenty of others that do, e.g. , .
In , a pretty large dose of naloxone given a day after the last dose of a relatively low amount of buprenorphine produces withdrawal.  indicates that IV buprenorphine/naloxone, while less desirable than buprenorphine alone, produces similar effects. The difference in perception of the effects decreases with time, presumably as the naloxone wears off. While  mentions precipitated withdrawal in some abusers, it does not indicate whether they were on other opioids at the time. Inclusion of naloxone does succeed at making IV Suboxone abuse less attractive than IV Subutex.
It appears that, when used IV, the naloxone Suboxone attenuates the buprenorphine's effects somewhat and may contribute to (or cause) the withdrawal experienced by those dependent on full agonists. The dose of naloxone is insufficient to cause withdrawal, and the increased bioavailability of buprenorphine likely makes up for any antagonist effects. I'd like to see a study comparing desirability of SL vs. IV in opioid naive or buprenorphine maintenance patients. It's arguable which method is more effective, but IV (or IN) use does not lead to withdrawal. --Flopster2 00:50, 5 November 2007 (UTC)
Dr Evi 666, References http://www.sciencedirect.com/science/article/pii/S0376871603000589 absorption of naloxone "was 9 and 7% for the 4 and 8 mg naloxone doses" it is established that ~10% of naloxone _WILL_ ABSORB SUBLINGUALLY.
http://www.sciencedirect.com/science/article/pii/0376871690901363 "Naloxone is sufficiently absorbed sublingually to precipitate abstinence(wtF? thought Elsevier had proofreaders i think they intentionally rewrote withdrawal so a text search wouldnt find it, haha) in dependent subjects"
Flopster YES in a 1:1 ratio the naloxone clearly has an effect, and in other studies the amount absorbed is quantified, but there is intentional confusion created when parties who have an LUCRATIVE FINANCIAL INTEREST assert that in a 1:4 ratio the naloxone does "nothing" orally. I've been in multiple trials where subutex was compared with suboxone and found researchers were very eager to disqualify people who reacted badly to the suboxone, this is a HUGE scientific fraud! also i've been on subutex for 5 years and know it well. Ive genuinely tried to switch to suboxone because it would save me almost $50/week and save me UNREASONABLE amounts of time, hours of the best part of everyday, but suboxone gives me severe chills, weakness and severe sleep difficulties, and significant amplification of pain. Then there are the psychological effects, oh god! Others specifically mention being SUICIDAL and DEREALISED for the first time in their lives after being switched from bupe to SUBOXONE, with no dose change no abuse no misuse no objectionable alterations to the standard procedure, just switching from long term stable consistent bupe to suboxone. i've personally done it about 4 times, plus multiple studies. Once because i was admitted to hospital with pneumonia because i came in on suboxone i couldnt change while i was there, i didnt sleep for a month despite drs giving me benzos and more benzos. Other times ive been in hospital for a similar amount of time on bupe (same dose of bupe just without the naloxone) and when the nurse would bring my dose after breakfast time i would have pass out and have a great nap for most of the day, and sleep like a baby at night too, without any benzos which i do not need. I resent being forced to take NALOXONE with my bupe while i was SICK, you EVIL IGNORANT PURITANS.
Consider that the ENZYME(s) that turns buprenorphine into NORBUPRENORPHINE which is a POTENT FULL AGONIST is competitively inhibited by naloxone! BUPE is a PRODRUG, and there are mechanisms whereby naloxone can significantly alter the effect of the bupe even if the naloxone has a shorter halflife and lower bioavailability. the fact is ive meet a minority of others that react the same as me, but for some reason we are ACTIVELY REPRESSED.
Parties willfully pushing someone elses agenda to convince people that 1/4 of significant is insignificant, that relative is absolute, JUST to allow BIG PHARMA to justify a new formulation under all new PATENTS really is EVIL. that is all that this is actually about bupe would have been an extremely cheap generic otherwise threatening a billion$$$ oportunity.
Here are some rough figures, if the 10% which has been established gets to the CNS (lets not go into +- yet), of the Naloxone is absorbed and you are on a dose of 32mg bupe:8mg naloxone a day then you get 0.8mg of naloxone into the CNS, there are plenty of studies showing significant effects at the 1mg level. yes i realise there will be an equilibrium reached, and that the presence of of ~ 20% of the bupe that absorbs to go along with the 10% of the naloxone will alter the receptor occupancy. All im saying is that there are too many studies skirting around the central issue, all to produce "favourable results" that can be compiled into "metaresearch" and reworded and manipulated to force public policy. Buprenorphine is a miracle treatment, now it will ONLY be AVAILABLE if you are PREGENANT ! why is that i wonder, because the naloxone is known to absorb and would cause catastrophic harm to a developing brain. WAR is PEACE, FOUR legs GOOD. 18.104.22.168 (talk) 15:16, 29 April 2012 (UTC) keep fighting the shills
Naxolone and Childbirth
I removed the line: "In one experiment, women treated with naloxone reported higher pain levels during childbirth than women not so treated" Because it has been dated as uncited since july 2007, and seems very unlikely given the ethical consideration involved.Halogenated (talk) 00:13, 20 January 2008 (UTC)
I don't have a citation for you, but from my antenatal classes I can tell you it is known that people treated with naloxone experience higher levels of pain, childbirth or not. this is because it binds to the same receptors that pain relieving hormones do. Also any woman treated with naloxone during childbirth is either a drug addict, and drug addicts have a much lower pain tolerance than the general population, or has been admistered too much pain relief during childbirth which needs to be rapidly reversed to prevent respiratory distress to the baby. Obviously reversing pain relief is going to cause higher pain levels. Naloxone is administered during childbirth all the time. 22.214.171.124 (talk) 10:13, 18 August 2008 (UTC)
Naloxone and NMDA receptor
As naloxone is a mu-opioid receptor antagonist, can someone explain why it should counteract the effects of ketamine, a NMDE receptor antagonist? Doesn't seem very plausible. Dr evi 666 (talk) 09:33, 21 January 2008 (UTC)
Ketamine is far from a selective NMDA antagonist it has a numerous set of binding sites including the mu opioid receptor - a pubmed search for ketamine mu opioid will find the relevant research. Mu opioid receptors are also involved in facilitating reward in general and mu opioid antagonists can reduce the rewarding effects of some drugs that have no direct affinity for that receptor, for example chocolate, cannabis and psychostimulants such as amphetamine and cocaine. I do not know where you came to the conclusion that ketamine is a selective NMDA antagonist, if it did not have an affinity for the sigma receptor it would be neurotoxic and ketamine is a strongly neuroprotective drug - particularly used in situations like head injury to prevent neuronal damage, it is also anti-inflammatory and can reduce brain swelling. Again if you want references you can search pubmed because this is all quite common knowledge and I don't particularly feel like searching for it right now. —Preceding unsigned comment added by 126.96.36.199 (talk) 01:18, 22 February 2008 (UTC)
"common knowledge" is quite an easy term, isn't it? I never used the word selective, it's just that the involvement of MOR in ketamine's pharmacological actions is so small, I doubt addition of naloxone will counteract them. I merely reacted to the fact that references are needed for the statement regarding naloxone and ketamine in the main article and I could not find appropriate ones. But you did not or could not supply them either. On top of that, there is evidence for neurotoxic effects of racemic ketamine on the developing brain, as the following references will show:
- Ke JJ, Chen HI, Jen CJ, Kuo YM, Cherng CG, Tsai YP, Ho MC, Tsai CW, Yu L.Mutual enhancement of central neurotoxicity induced by ketamine followed by methamphetamine.Toxicol Appl Pharmacol. 2008 Mar 1;227(2):239-47. Epub 2007 Nov 1. PMID: 18076959 [PubMed - in process]
- Soriano SG, Anand KJ. Anesthetics and brain toxicity.Curr Opin Anaesthesiol. 2005 Jun;18(3):293-7.PMID: 16534354 [PubMed]
"only certified addictionologists (physicians specializing in the treatment of drug addiction and dependence)"
Is it just me or did the person who wrote that just make it up on the spot... where exactly does one go to train to become an "addictionologist"? surely the term 'addiction specialist' is the appropriate term, additionologist makes about as much sense as drugologist, brainologist and fruitologist. If I am mistaken on this then do put me straight but that sounds bloody ridiculous to me. —Preceding unsigned comment added by 188.8.131.52 (talk) 01:08, 22 February 2008 (UTC)
- That term actually exists. Here's a link: http://medical-dictionary.thefreedictionary.com/addictionologist Jtpaladin (talk) 22:52, 5 August 2016 (UTC)
Qualitative effects of naloxone versus naltrexone
Can someone who actually knows, say what the qualitatively different effects are between these two drugs? It is not obvious to the reader what they might be, as the drugs have such similar modes of action —Preceding unsigned comment added by Woodcore (talk • contribs) 17:01, 27 February 2008 (UTC)
I know it was mentioned above, but the article should be amended to make clear that Naloxone in Suboxone is clinically irrelevant.As the poster said, buprenorphine alone will can cause withdrawal in those dependent on full agonists.And Suboxone used IV has no ill effects, in the sense that the Naloxone does nothing to effect the action of Buprenorphine, is the dose present is not nearly high enough.As the definitive web encyclopedia(at least in terms of the public using the site) I believe Wiki has a duty to make clear that Nalaxone's role in Suboxone is non-existent except as a scare tactic, since there is no medical difference between Suboxone and Subutex unless you happen to hav a Naloxone allergy I suppose. On a side note, Suboxone seems to exist soley for making money(since it is not generic) but that is mostly irrelevant to the article... — Preceding unsigned comment added by 184.108.40.206 (talk) 03:09, 26 August 2011 (UTC)
The naloxone is clinically relevant due to its antagonistic effect on mu-opioid receptors in the gut. This will have the effect of a local withdrawal, inducing diarrhea in most patients with opioid-induced bowel disease. § — Preceding unsigned comment added by 220.127.116.11 (talk) 03:07, 11 November 2014 (UTC)
"in contrast to direct opiate agonists which will elicit opiate withdrawal symptoms of both opiate-tolerant and opiate-naive patients" -- This comment makes no sense. Can the person who wrote it please explain, or provide a reference? Markcymru (talk) 16:04, 17 September 2014 (UTC)
Hi, I know this was a while ago, but I think that means that when you give someone a Direct Opioid Agonist, they will definitely go into opiate withdrawal and show withdrawal symptoms, and it doesn't matter whether the patient is used to having opiates or not. I guess usually you would expect opiate-naive patients (who haven't had opiates before) would not experience withdrawals, but they do when given a Direct Opioid Agonist. Does that make sense? Knittea (talk) 10:33, 21 May 2016 (UTC)
"Studies show that to give this to a person in severe pain would be unethical and inhumane."?
What does this mean? It has no source, and no clarification, and doesn't make much sense.
- While this was a long abandoned question, the answer is simple enough. Administer naloxone to a patient who is in severe pain and has received an opioid analgesic, their pain relief would immediately end and the patient would be suddenly in excruciating pain.Wzrd1 (talk) 06:45, 26 February 2017 (UTC)
The following sentence appears second-to-last in this section. It seems to be oddly specific and to promote a certain interpretation of claims made therein (weasel words?), and I suggest it be revised. I'll leave it to an admin to decide on this one.
"Naloxone can be used orally along with oxycontin controlled release and helps in reducing the constipation associated with opioids. "
A possible revision might read as follows:
"Studies have found that oral coadministration of Naloxone alongside select opioids may aid in reducing symptoms of constipation associated with their use." — Preceding unsigned comment added by 2601:282:503:A480:F50B:8B90:1526:16E7 (talk) 23:57, 24 October 2016 (UTC)