# Talk:Pethidine

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## Pethidine as a Kappa agonist?

I have a question about the mechanism of action listed in this article. It says in the article that pethidine's main mode of action is as a kappa receptor agonist. However, to me the structure looks typical of other mu-agonists, such as methadone and morphine. Also, I thought that all kappa agonists were inherently dysphoric, yet pethidine causes euphoria and sedation just like morphine, and is easy to get addicted to. I know that other kappa agonists like Salvinorin A (in Salvia) have very different effects from the typical mu-opioid one, resulting in dysphoria, hallucinations and discomfort. Is pethidine's main mode of action really as a kappa agonist, or does the drug also have a high affinity for the mu\delta receptors? Thank you for any responses. —Preceding unsigned comment added by D Dinneen (talkcontribs) 19:34, 7 October 2010 (UTC)

Fixed that eventually. It took me a while to discover why otherwise sensible student were telling me that pethidine exerts its analgesic action via kappa receptors! — Preceding unsigned comment added by Christom (talkcontribs) 08:09, 19 April 2012 (UTC)

## Praise

I think this article is a great example of writing for general knowledge by an expert. It will always be a matter of judgement for the primary contributor but my preference would be to tend toward the more technical detail as opposed to "dumbing down" for wider consumption. We consult an Encyclopaedia precisely when we either don't know about something or are seeking more information. Thus we expect to encounter new knowledge for the price of new words.

Many fields of enquiry have a specific terminology at various stages of difference to common language. For example the word "Energy" has a specific meaning to a physicist but possibly something different to a person discussing para-psychological phenomena (both players being laymen in the other's field). To move an entry description toward more laymens terms would, in my opinion, risk confusion of the form I find myself in when talking to my own brother on issues of para-normal 'energy'.

## Praise but complaints

Fantastic article!

Now would someone kindly add a section that makes sense in English?

216.150.207.190 18:26, 26 March 2007 (UTC)Alastor

This is a hard debate because Wikipedia wants to be as accurate as possible but where is the line regarding technicality and laymens terms? I'll do some research. Scottydude 18:29, 26 March 2007 (UTC)

A useful way to approach this is to use the lead section. The lead section on this article (frankly, like most articles), does not follow Wikipedia's style guide. Most material in the current lead section should be moved to one or more subsections, e.g. "Clinical usage". The lead can then be rewritten to summarise the main points of the article. It can become more accessible just by removing detail, but it is also possible to avoid the worst of the jargon. Above all, remember that Wikipedia is not a specialist textbook, but written for a general audience. That doesn't mean it has to dumb down, but it has to be written smart. Notinasnaid 21:17, 27 March 2007 (UTC)

I added a lot of the more jargonish stuff to the front of the article when it was still much shorter than it is now, with the intent of later revising it to make it more accessible. I just never got around to it - best of intentions, etc. I'm also writing from a specialist's standpoint. Sometimes we fall into the trap of assuming what's "common knowledge" to us, is common knowledge to everyone else. Also, since I wrote a good part of the article in its current form, when I look at it to revise it, I'm doing so with a biased eye. I know what I mean when I write something, even if the point isn't clear to anyone outside of myself.
Another thing I've been meaning to do is to move a lot of the particulars about the toxicity of pethidine to a new article on norpethidine, since it's responsible for most of the adverse effects unique to pethidine administration. There's a lot of myth and misperception surrounding the use and side effects of opioids, especially for pain management, and a lot of it involves pethidine being safer/better than the alternatives when the opposite is really true. So if I drive some points in with a cudgel (or try to), or lard some parts up with jargon, that's why.
If someone is able to rejigger the lead section/move some stuff to subsections so the top is more accessible, that would be welcome. IMO, Wikipedia is first and foremost for a general audience, but that doesn't preclude the addition of information that's primarily of interest to specialists. They (we?) use Wikipedia, too. Porkchopmcmoose 22:07, 13 April 2007 (UTC)
My suggestion would be to provide links to the Wikipedia pages for the technical terms. I've found this quite helpful for reading about subjects with which I'm not very familiar. Brief explanations within the article might also be appropriate. Mia229 (talk) 00:28, 25 October 2011 (UTC)

===== POV? =====too much beating around the bush. demerol is for people who are past a certain pain threshold that most over the counter drugs would be able to fight, and people who are IN PAIN want to know how it works, symptoms, side effects, etc. no one cares when it was synthesized. remember, not everyone reading wikipedia is as smart or adept as some may think. in other words, i'm finding alot of these medical articles do not get to the point. its an encyclepedia for christ sake. just explain the item in question, a little background, applications, reasons for it's existence, and overall POINT.

From reading this article it is easy to conclude this is never the drug of choice for alleviation of moderate to severe pain. Is this a fair conclusion to make? I thought that meperidine and midazolam, was as recently as 2002 the most commonly used combination of drugs for "moderate sedation." (Also, I have never heard of this drug referred to as "pethidine" before.) 69.140.164.142 04:19, 11 April 2007 (UTC)

"Pethidine" is what meperidine's called outside of North America. And it's almost never the drug of choice for any kind of pain, save for brief endoscopy procedures, or where someone is allergic to all other alternatives. Several countries and numerous institutions have curtailed its usage, and while it's still popular with some clinicians, the most up-to-date guidelines for the treatment of pain emphasize that meperidine is 'not' the drug of choice for the treatment of pain, especially chronic pain. I have been careful to reference everything thoroughly – if you peruse the literature, you'll be hard-pressed to find anything good said about meperidine in recent years.
I think it'd be appropriate to include more about its continuing popularity among clinicians. Just because a drug is widely used, doesn't mean it's particularly effective. Medicine is as susceptible to faddishness and as any other profession, and for decades the misperception that meperidine is less toxic, less addictive, and equally effective compared to its alternatives has been promulgated to the point that it's just something that "everyone just knows" - received wisdom passed down from person to person. Most of the doctors practicing today, at least, in the United States, went to medical school when the stuff was considered the sine qua non for pain management. And most doctors' knowledge of the particulars of pharmacology is limited to what they learned in a semester devoted to the topic in med school, and what they hear from pharmaceutical company representatives. So a lot of them continue to abide by outdated standards or prescribe medications with worse side effect profiles than their alternatives because that's what they're familiar with. DPT - Demerol-Phenergan-Thorazine is still a widely used combination for pediatric sedation despite the fact that all three are outmoded drugs with profound side effects and less effectiveness than more modern cocktails. But clinicians keep using DPT, anyways, even though superior alternatives are available. "Just because it's popular doesn't mean it's true."
In short: if the article seems to emphasize the deleterious effects of meperidine/pethidine, that's because it reflects the state of the science today. Porkchopmcmoose 22:07, 13 April 2007 (UTC)

## Confusing or unclear for some readers?

I'm not a doctor, but there is not much confusing or unclear stuff for me in the article. What parts exactly are confusing for some readers? Who are those "some readers"? Thanks.--84.163.123.27 02:12, 28 April 2007 (UTC)

## a good reference to add

Meperidine: a critical review.

http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?db=pubmed&cmd=Retrieve&dopt=AbstractPlus&list_uids=11782820&query_hl=4&itool=pubmed_docsum

Already there — reference no. 6 as of this writing. You're right; it's a fantastic reference. Porkchopmcmoose 19:57, 22 May 2007 (UTC)

## Recreational use

I would like to see something about the recreational use of this drug.

michael jackson died of this drug http://www.youtube.com/watch?v=2rQZ-L8KC_A&feature=related —Preceding unsigned comment added by 83.85.22.1 (talk) 23:07, 7 July 2009 (UTC)

## Intravenous?!

At the beginning, it says the drug may be administered intravenusly while at the end it says that it should never be given intravenously... which is right? soldierx40k (talk) 22:59, 19 December 2007 (UTC) Yes, which is right. Someone gave me some and I want to try it by shooting it. —Preceding unsigned comment added by Timber666666 (talkcontribs) 05:02, 24 January 2008 (UTC)

It may be, if, on the doctor's decision be administered cautiously, slowly i.v., titrating the dose. Pethidine should, however, be used only if there is a reason not to administer morphine or other analgesic available and it certainly shouldn't be abused "recreationally".--84.163.96.20 (talk) 23:16, 23 June 2008 (UTC)
Yet this isn't that it shouldn't be used because it can be fatal due to route alone, like codeine or hydrocodeine (vicodin) due to having a severe histamine reaction that causes anaphylaxis and/or pulmonary edema resulting in most certain death... but rather a very potent cumulative effect of maintained potency in a titrated means unusual seeing as norpethidine; it's human metabolite is also it's human precursor (so based on your own particular human metabolism; demerol can be an endless chain where it metabolizes into it's own precursor in your body and the molecule is made anew, based on how many of your metabolic enzymes that make this function in that part of your body show bio-availability at that time in your metabolic cycle, increasing potency dramatically and in a way unlike other opioids. . . . Does that stand true as a good explanation? If true anyone feel free to alter what I just typed here in any manner and add it to the article in whatever way deemed necessary to explain the dangers of IV use in this regard and its alternate considerations over other opiates of potential abuse to its Pethidine's metabolite also being its precursor (Norpethidine) which is a very notable and necessary of consideration facet of the drugs nature: A feedback loop in the body. Very dangerous and unpredictable. 4.242.174.200 (talk) 09:45, 15 October 2009 (UTC)

## The chemical structure and name in the article

The chemical structure and name used in the article appear to be inaccurate. A piperadine structure has a N in the cyclical ring with 5 carbons. The number 1 structure has the methyl group and the number 4 carbon has the phenyl group and the ethyl ester. The structural name and picture didn't make sense to me so I looked on the web for other articles on meperidine which corroborated my curiosity. I suggest the name and structure be corrected.--Ajschindler (talk) 16:19, 1 May 2008 (UTC)

The chemical structure and the names are correct. Сасусlе 01:42, 2 May 2008 (UTC)
Yes, both structural formula and the name are correct.--84.163.96.20 (talk) 23:13, 23 June 2008 (UTC)

Had it intravenously yesterday as part of a Colonoscopy procedure - everything seemed OK to me — Preceding unsigned comment added by 206.194.127.112 (talk) 18:57, 8 August 2012 (UTC)

## Michael Jackson edits

I've been editing out the MJ info. There is no official quotes or confirmations, leaving this info as gossip. I removed random quotes that had a reference, but did not reference the quotes nor the information. The reference attributes to legal challenges in 2005. IF this page continues to be changed with incorrect info and so far only minor vandalism, the rest of this day could see worse and might be necessary for slightly increased security.

I'm going to suggest that you leave (or insert) a comment under notable personages, that indicates that MJ has died, and that it might be due to an overdose of demerol, which he was known to be using. Otherwise, you might spend the next two weeks reverting this article. I've inserted the "current event" tag, which ought to be enough to inform people that the referenced event is, in fact, rumor and/or gossip. Norm Reitzel (talk) 16:57, 26 June 2009 (UTC)
I cleaned up the edit that discussed it rumor as fact. The tag you added is necessary at this time, and I changed it to rumor. Removed an allusion to other drugs, reference cited did not state anything about other drugs and is unsourced/unfounded rumor at this time. Current edit is sufficient when coupled with your tag. Seola (talk) 19:21, 26 June 2009 (UTC)
I think this is as good as we can do until the flap dies down, short of just locking down the article. Norm Reitzel (talk) 20:01, 26 June 2009 (UTC)
Changed events to chronological. Re-added his death. It's a fact he is dead. The current statement does not allude to the use of this drug as a cause of death, as it is still speculation, but stating the fact that he is dead is in line with Wiki standards. Agree, this is the best expansion or detail needed at this time. Seola (talk) 21:10, 26 June 2009 (UTC)
There's no harm in letting the Michael Jackson material run for a little while. It should not be included, in the long term, imo. In a few months it will be easier to see it as either notable for posterity or subject to deletion according to WP:NOTNEWS. We'll all still be here. I doubt very much the story will be, though. I do not support immediate deletion, nor do I support indefinite inclusion at this time. I think the editors here have done a good job of it. Anarchangel (talk) 05:30, 27 June 2009 (UTC)
Per WP:LEAD, we have to include notable controversies in the lead, and this is as notable as it gets. The information is sourced to the Los Angeles police, and was reported by ABC News. His family has also discussed it, so this isn't some dodgy rumour that will disappear shortly. SlimVirgin talk|contribs 05:42, 27 June 2009 (UTC)
It is a rare thing that I find myself on the deletion end of a discussion. And I agree that as far as WP:V goes, and the event itself goes, the event is notable. And I take back my tone of prognostication. The information seems to be perched on the edge of relevance to the article, but it all depends on what new evidence arises. What I am having difficulty with is the connection between the drug and his death. It is way too early to tell, but if no new evidence arises linking the two, then I would have to say, delete. The connection between something and a notable event is not itself notable if the connection is weak, see what I am saying? Side note: LAPD RS? Anarchangel (talk) 12:11, 27 June 2009 (UTC)
Et voila. Latest Wikinews report is that the LA Coroner's office has ruled MJ's death to have been caused by Propofol, not Pethidine. Now we can decide whether it is notable that early reports were of Pethidine. Again, I vote against. Anarchangel (talk) 08:30, 25 August 2009 (UTC)

I've added a couple of reliable-source (WP:SOURCES) cites on this. At this point, the "story" seems rather tenuous, but as I say, we do have some citable-quality sources, so ...
IMHO we should continue to monitor this and add more material as vailable, or remove if this become more marginal than it is already. And as always, please cite material to reliable sources. Thanks. -- 201.37.230.43 (talk) 11:58, 3 August 2009 (UTC)

In my way of thinking, the entire "Hazardous use, harmful use, dependence, and diversion" section is entirely devoid of any other information pertaining to misuse of this drug except for the mention of David Kennedy. The section should be combined with the "Adverse effects" section and expanded (more examples of abuse, details of addiction, etc.), or removed outright.--Sem;colon (talk) 01:30, 14 November 2009 (UTC)

And if you're going to include a "list" of notable users, I feel that the character Don Gately from Infinite Jest merits mentioning.--Sem;colon (talk) 01:36, 14 November 2009 (UTC)

## Intro: "put severe limits" vs "curtailed it outright" - -  ??

Like many others, I came here following the death and rumors of one MJ to see what could be learned about "Demerol", and referenced from sources. Aside from all the wrangling over putting MJ himself in the intro as an example, I could not get past the penultimate sentence of the intro: "Several countries, including Australia, have put severe limits on its use or curtailed it outright". Maybe it is a "down under" lingo thing, or perhaps I am unusually off today, or maybe I am always "off" and just haven't noticed until now, but I cannot find a significant difference, at least in the common usage, between "put severe limits" and "curtailed it outright". Did it previously say "banned it outright" and then there was a disagreement?. Just wondering, thanks in advance. --T-dot ( Talk/contribs ) 12:28, 29 June 2009 (UTC)

I'm not sure what it said long ago, but as of MJ's death (about 100 edits back) that sentence read the same. When adding an existing reference to replace a cite tag earlier, I reworded the part in question to "...have put strict limits on its use(period)" since the reference didn't specify any countries that had outright banned it. At least not that I could find (too much medical language and I start experiencing symptoms like headaches, dizziness, etc). I think just using the word strict is sufficient; I think you made a valid point; but I have no idea if you are "off". Perhaps we both are ;) Zephyrnthesky (talk) 16:38, 30 June 2009 (UTC)

## Lexicon of alcohol and drug terms /Terminology

Currently

This article uses the terms "hazardous use," "harmful use," and "dependence" in accordance with Lexicon of alcohol and drug terms published by the World Health Organization (WHO) in 1994.[18] In WHO usage, the first two terms replace the term "abuse" and the third term replaces the term "addiction."[18]


While I can see the case for both this use and the more everyday use, I find the current situation confusing: Most people will not have the background to get the right associations for e.g. "harmful use". Correspondingly, I suggest that either the note be moved to the beginning of the article (to be brought to the readers immediate attention) or that the language be changed. 188.100.204.157 (talk) 15:56, 3 December 2009 (UTC)

agreed. This seemed very out of place with the article. It should be removed. --128.227.83.71 (talk) 21:49, 10 January 2011 (UTC)

## indications

The article states "...relative to other available opioid analgesics have seen it fall out of favor in recent years for all but a very few, very specific indications.[5]" Reference 5 no longer exists. What are the "very few, very specific indications"? --128.227.83.71 (talk) 21:47, 10 January 2011 (UTC)

For the better part of 32-years, I have prescribed Meperidine IV (to titration), or Meperidine/Hydroxyzine (1 to 1 ratio, up to 75 mg ea DEEP IM) q4h PRN in situations where no contraindications existed in the post-surgical setting (post lower urinary tract procedures), as its properties as a smooth muscle relaxant added to it's palliative effects. When combined with an accurate past medical history, and careful monitoring, Meperidine is a welcomed adjunct in the care plan for many patients who have undergone surgery of the urinary bladder. prostate, or urethra.

I have NEVER prescribed it orally, or in settings outside of the hospital (other than hospice situations). Its abuse potential among medical staff is well known, which correlates to the diversion statistics listed above. Meperidine would often be diverted even before Hydro/Oxymorphone was, it is often referred to as being capable of providing "the Cadillac of euphoric experiences". Many hospitals require witnessed administration of the med, including supervisory personnel.

The main indication for the administration of Meperidine is "moderate to severe pain control when opiates of equivalent effect are contraindicated due to the risk of allergic reaction". Its respiratory effects can be difficult to reverse because of its agonist properties.

Removal of Meperidine from our formularies would be unwise, as Fentanyl comes complete with its own set of adverse circumstances. PA MD0351XXE (talk) 05:42, 11 October 2011 (UTC)

## mu or kappa opioid receptor agonist?

I don't believe this sentence is correct: "Unlike morphine, a potent mu opioid receptor agonist, pethidine exerts its analgesic effects by acting as an agonist at the kappa opioid receptor, primarily.[citation needed]" My understanding is that meperidine (pethidine) is a full mu AND kappa receptor agonist. Could someone either source the citation for the sentence above, or remove it from the article? --159.178.228.148 (talk) 17:25, 2 February 2011 (UTC)

Absolutely right, Meperidine is a mu-agonist!!! — Preceding unsigned comment added by 212.184.138.183 (talk) 11:05, 4 August 2011 (UTC)

A few years ago, I read that it was theorized that Meperidine may possibly have a "depolarization-type" of effect on smooth muscle receptors and the κ-opioid receptor, proving further that there is a lot about this synthetic which we don't know. I provided care for a patient (while in residency) in early 1977 that was one of the victims of the MPTP/MPPP "copycat shortcut/misformulation" fiasco which occurred off-campus at UMD. Much unknown was discovered about Meperidine then, and it wouldn't surprise me if it's affinity for neurons produces yet another breakthrough receptor status theory.PA MD0351XXE 06:33, 25 November 2011 (UTC) — Preceding unsigned comment added by PA MD0351XXE (talkcontribs)

## Typical Dosage?

It would be nice if there was some commentary about typical dosage. An article on Michael Jackson mentioned 900 milligrams of Demerol , I was hoping this article would give me some clue how that amount compared to typical usage. Kevink707 (talk) 20:53, 7 November 2011 (UTC)

The usual dosage for moderate pain begins at 50 mg intravenously every four hours for adults over 100 lbs, and can range as high as 200 mg for a much heavier person (or one who is encountering more severe pain) note:respiratory status must be adequately monitored. If given intramuscularly, an antihistamine, usually hydroxyzine or promethazine will be combined at an equal ratio to the meperidine, and counting the antihistamine as being of equivalent strength to the meperidine. i.e., 100 mg of meperidine is equivalent in potency to 50 mg of meperidine in combination with 50 mg of Vistaril (hydroxyzine). Seldom is a combined dose totaling more than 150 mg IM given, if the need for palliation is greater than the efficacy of the 150 mg combination, another analgesic will be considered. Meperidine must ALWAYS be administered with care.PA MD0351XXE 03:39, 23 November 2011 (UTC) — Preceding unsigned comment added by PA MD0351XXE (talkcontribs)