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Re: Effexor an opiate? Probably not. Elizabeth

Posted by JANNBEAU on December 13, 2001, at 11:41:32

In reply to Re: Effexor an opiate? Probably not. JANNBEAU, posted by Elizabeth on December 12, 2001, at 22:52:26

> > Hello, Elizabeth. Sorry I overreacted to your initial message. I'm rather new at this. I actually enjoyed your second posting. I've written some responses below. Please take them in the same spirit that you offered your comments.

> (BTW, I did indeed read dhldn's post, and I posted a brief direct reply. I think it's a mistake to conclude that since venlafaxine and tramadol have some structural similarity, venlafaxine must be an opioid, or even that it's especially likely that it is. You can read my response at dhldn listed some potential dangers of Effexor and seemed to be jumping to the conclusion that Effexor is an opioid.)

Read your posting to dhldn. Didn't say much. Perhaps you could go into the detail with dhldn that you went into with me. I'd like to see HIS response.

> I think it's important to recognize that we don't know everything about the pharmacologic mechanisms of *any* of the drugs we use -- not just Effexor. All drugs may have effects we don't know about. At the same time, we know how to screen for affinities for various receptors, and it's likely that most drugs available today have been tested for opioid receptor affinity. Now, it's possible that if a drug company doesn't want to know that a drug they have is an opioid, they could do a very cursory test and accept the negative finding from that test. I think, though, that Effexor has been around long enough that if it were an opioid, this would have been discovered by now.

I do know that we don't have a clue about the myriad effects of today's meds. Not much different from the Middle Ages, huh, except there are so many more of them with which to contend. I am bothered most by the fact that doctors prescribing them don't seem to think of this and do not discuss potential interactions, side effects. I always ask for the PI so that I will at least recognize an effect as being -perhaps- due to the new medication. Both my husband and daughter are physicians and I stress to them the importance of knowing your drugs and telling your patients what to expect. Not everyone has access to the information that we do nor do they have the sophistication to interpret it. I take many Rx drugs for various things (HTN, hypercholesterolemia, etc) along with those I take for pain and, believe me, even if I knew nothing about the state of the "art" of developing, or more precisely, marketing new drugs (I worked in clinical pharmaceutical development for several years), I would be skeptical and watchful whenever I'm prescribed a "new" medication.
> > O-desmethyltramadol, according to my sources, has an affinity for mu opioid receptors that is about six times greater than that of the parent compound.
> Actually, I went ahead and looked this one up, and according to the PI, the affinity of O-desmethyltramadol (let's call it ODT for short) for mu receptors is about *200* times that of the parent compound; interestingly, the PI adds that ODT is about six times as potent an *analgesic* as tramadol. (Hard to know what to make of this.)
OK, I'll give you that one! As I said, I was working from memory and have only scanned the literature on Effexor.

> As for the word "narcotic," it's ambiguous. Politicians use it to mean any illegal drug; they often include cocaine and marijuana in the category "narcotics." This also makes the word politically loaded, so it's probably better to use a more neutral word, since one is available. Also, there's the question of whether drugs with partial or mixed opioid agonist activity (such as buprenorphine, butorphanol (Stadol), pentazocine (Talwin), nalbuphine (Nubain), etc.) which have little or no significant abuse potential should be considered "narcotics."
I stand by the dictionary's definition of narcotic analgesic. The dictionary does not suggest ambiguity. The term is used routinely in both clinical practice and in research, along with others. I am not a politician nor am I interested in arguing the politicians' uninformed views and imprecise use of the English language. Simply because some segments of the population have misused a term does not invalidate the definition. However, if you prefer, I can use "opioid analgesic" if this is the term to which you refer. It doesn't matter as long as each party understands the concept.

Now, for the second point. Research has shown that one cannot predict which medications will become "drugs of abuse" or "street drugs" by the structure, intended use, or class of drug, although pure opioid agonists tend to be most heavily abused as do some stimulants, of course. Illegal use of a drug often occurs because of "hype" or "fad" potential. Whether a drug is abused seems to have some significant psychological component, as well as the factor of "availability." For instance, OxyContin (extended-release hydrocodone) is not very different from MSContin (long-acting morphine sulfate) in pain relieving activity, yet one has become a popular street drug (OxyContin) while the other (MS Contin) never became a popular street drug, despite the fact that MS Contin is formulated similarly and should give the same "high" from snorting or injection of the crushed tablets.

With respect to your final comment re mixed opioid agonists, check the history of Talwin (pentazocine). You might find, as I have read, that when pentazocine was first marketed, it rapidly became a "drug of abuse" or "street drug." Such abuse did not stop until the manufacturer reformulated the drug to add an opioid antagonist to prevent the "high" accompanying illegal use. This would argue against the statement that mixed opioid agonists have "little or no potential for abuse."

> I meant that people I know who are taking it say it takes around three hours to work. This is acutely -- if Ultram is taken around-the-clock, allowing ODT to build up, it may take effect in an hour or less when you first take it in the morning.
I agree that around the clock dosing is probably important for this drug.

> From the PI: "Analgesia in humans begins approximately within one hour after administration and reaches a peak in approximately two to three hours." Sort of ambiguous, I agree.
I read the PI and did not expect that I would hurt for six hours after taking the med. I used it for about a week with Effexor before developing what I assume was serotonin syndrome; at no time did I get any significant pain relief. In fact, I was probably overdosing myself because I continued to hurt, despite Effexor's analgesic potential.

> > I have noticed that tramadol (as well as hydrocodone and codeine) wake me up.
> All effective opioids do this to me, or at least, all the effective opioids I've taken do at the doses I've taken. (Ultram and codeine do not, which might be due to a deficiency in the enzyme cytochrome P450 2D6 -- this would lead to poor metabolism of tramadol to ODT and codeine to morphine.)
Ultram has this effect on me as does codeine.

> Nightmares or "vivid" dreams have been associated with oxycontin. Why would one not expect the same from other drugs of like action?

> > > I really doubt that Effexor is an opioid (or if it is, it's probably *extremely* weak), although it might be interesting to try to find out for sure. But there is a risk (of the "serotonin syndrome") when Effexor or SSRIs are prescribed with tramadol -- generally the combination isn't recommended. Again, this applies to SSRIs (and MAOIs, for that matter), not just Effexor. It definitely does not mean that Effexor is an opioid.

I have to accept the above comment, qualified by your following statement. Perhaps I've been led astray by the good doctor's posting?
> > >
> > What I'll say here is that there are *many* drugs that are structurally similar to venlafaxine, and there really isn't a reason to list them all in the PI for Effexor; noting the similarity to tramadol alone, meanwhile, would be misleading. The structural similarity to tramadol does suggest that it might be worthwhile to test venlafaxine to see if it's an opioid. If venlafaxine were shown to be an opioid, that information would be appropriate to include in the PI.

> Anyway, the structural similarity is not the reason for the risk of interaction; the serotonin reuptake inhibition by both drugs is most likely to blame there. There have been a number of reports of the serotonin syndrome resulting from combinations of tramadol with SSRIs or Effexor. Most opioids don't have this problem and can be used safely with the serotonin reuptake inhibitor ADs.

I understand this concept. I do not argue that Effexor is not an SRI (not an SSRI), just that it may have more than ONE mechanism of action and that the results of this "mixed" mechanism may be different from what one would expect with a "pure" SRI.

> > Did you know that the tricyclics are very similar to many older antihistamines?
> Sure. So are the phenothiazines. Indeed, most of the tricyclics and the phenothiazines *are* antihistamines. But agani, this information (their affiniaty for H1 receptors), not their structural similarity to known antihistamines, would be appropriate to include in their PIs (it generally isn't because they are old drugs).
I think we're splitting hairs here!

> > So what are the differences? I looked up opiod withdrawal symptoms and came up with: nervousness; sweating; nightmares; shaking chills; insomnia; somnolence; memory lapses; cognitive dysfunction, diarrhea, vomiting, nausea, anxiety, dysphoria; fatigue; hypomania; etc.
> >
> > These following signs/symptoms of Effexor withdrawal are published in the physician's insert for this drug. I quote from Gillman's posting (above): agitation, anorexia, anxiety, confusion, coordination impaired, diarrhea, dizziness, dry mouth, dysphoric mood, fasciculation, fatigue, headaches, hypomania, insomnia, nausea, nervousness, nightmares, sensory disturbances (including shock-like electrical sensations), somnolence, sweating, tremor, vertigo, and vomiting. At any rate, I certainly got these signs/symptoms from combining tramadol and venlafaxine.
> The list from the Effexor PI is pretty exhaustive. That's not surprising since the PIs typically list every reported side effect and could be expected to do the same with withdrawal symptoms.

>I am aware of the FDA's requirements for listing side effects and withdrawal effects.

> The most common recognized opioid withdrawal symptoms include gooseflesh; hot and cold flashes; insomnia; cramps and diarrhea; shivering; nausea and vomiting; dysphoric mood; drippy eyes and nose; dilated pupils; aches and pains; and fever. It's like having the flu. Sometimes people will have elevated pulse, respiratory rate, and/or blood pressure as well.
> Common Effexor withdrawal symptoms can be found by reading about the subject in the Psycho-Babble archives. The ones I recall reading about most often are the electric-shock type sensations, nightmares and disturbed sleep, dizziness, sweating, nausea, vertigo, headaches, fatigue, tinnitus, and dysphoria. (I could be missing some, but I don't believe that all the symptoms listed in the PI are especially common.) Some of them are also common symptoms of opioid withdrawal, but the overall picture doesn't suggest that the two syndromes are related. The common symptoms (sweating, nausea, dysphoria) are pretty generic ones, too.
OK, point taken.

> Actually, there are pretty specific withdrawal syndromes for different classes of substances, although these are best defined for drugs of abuse. Opioid withdrawal is particularly specific. On the other hand, there are some withdrawal symptoms that are pretty common with various types of drugs, such as sweating, nausea, dysphoria, sleep disturbance, and fatigue. (I even had problems with nausea from discontinuing Klonopin too rapidly -- that's *not* a typical benzo withdrawal symptom.)
> Anyway, I wouldn't worry about Effexor being an opioid. One thing that Effexor does have in common with opioids, though, is that its withdrawal symptoms, though very unpleasant, are not going to kill you.

I'm not worried! This was supposed to be an intellectual discussion. I take hydrocodone a couple of times a day and propoxyphene at night. Why would I be "worried" about the proposed "opioid" effects of Effexor? The drug seems to help me and I have no intention of stopping it unless it exacerbates my HTN too much. That's probably my biggest worry-since I am taking several drugs for HTN, I don't need anything that causes a sustained increase in my BP. I also have NEVER had difficulty stopping any drug I took, so don't expect to die from discontinuing Effexor.

Again, I've just enjoyed the intellectual stimulation of this conversation.
> -elizabeth




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