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Dr. Bob is Robert Hsiung, MD,
bob@dr-bob.orgShown: posts 1 to 18 of 18. This is the beginning of the thread.
Posted by fachad on April 8, 2002, at 9:22:22
Is Ambien a Benzodiazapine?
(or fachad plays The Devil's Advocate.)
I think Ambien IS a benzodiazepine.The whole argument turns on semantics and your definition of what is or is not a benzodiazepine.
If you define a benzo by it's chemical structure, a benzene ring attached to a seven-sided diazepine nucleus, well then, no, Ambien is not a benzo.
But that strikes me as a rather transparent linguistic maneuver. Think about this example. You tell a child not to walk over a line. He subsequently jumps over the line, and then insists that he didn't break your rule because he did not in fact walk over the line, he jumped over it. In a literal sense he is correct. But we feel that he is attempting to deceive us, and we can see right through it. He has ended up on the other side of the line, regardless of how he got there.
I think the analogy is fairly clear with Ambien and the benzodiazepines. No, Ambien does not literally have a benzene ring and a diazepine nucleus. But it does act at the GABA BZD1 receptor complex just like a classical benzodiazepine. It gets to the same place, so to speak, albeit with a different chemical structure.
So, from the standpoint of a chemist Ambien is not a benzodiazepine, but from the standpoint of a patient's nervous system it is a benzodiazepine.
It is particularly annoying to me that the marketing folks at Searle have leveraged this little word game to make Ambien seem more innocuous to prescribing physicians and sleep disturbed consumers.
Postscript: The motivation for this venting is twofold. First, I'm sore that they charge so much for Ambien. Second, I had SEVERE rebound insomnia when I tried to switch from Ambien to a generic benzo.
Posted by SLS on April 8, 2002, at 16:42:27
In reply to Is Ambien a Benzodiazapine?, posted by fachad on April 8, 2002, at 9:22:22
> I think Ambien IS a benzodiazepine.
> The whole argument turns on semantics and your definition of what is or is not a benzodiazepine.
Well, I think the term "benzodiazepine" is indeed based upon chemical structure. However, the "benzodiazepine receptor" was named as such only because nothing else was found to bind to it initially. Ambien (zolpidem) does bind to the benzodiazepine receptor as an agonist, and thus acts as the key to unlock the door to the GABA neurotransmitter receptor. Because of this, I imagine both drugs behave similarly. Unlike many of the BZDs (or all of them - I don't know), zolpidem is selective for the GABA(A) BZD-1 receptor. Zopiclone (Imovane) is also selective for this receptor.
Do you think there is any cross-tolerance between a benzodiazepine and one of the newer BZD receptor agonists?
- Scott
Posted by Elizabeth on April 11, 2002, at 10:59:38
In reply to Is Ambien a Benzodiazapine?, posted by fachad on April 8, 2002, at 9:22:22
> I think Ambien IS a benzodiazepine.
>
> The whole argument turns on semantics and your definition of what is or is not a benzodiazepine.Ambien isn't a benzodiazepine. "Benzodiazepines" are chemicals that have a certain core chemical structure. "Benzo" refers to the benzene ring. The "diazepine" ring has seven-atoms, with nitrogens at the 1 and 4 positions, and one double bond. These two rings share a bond; benzos also have a second benzene ring (it's called the "pendant ring" because when you draw a 2D representation of the molecule, it appears to be "hanging from" the diazepine ring) which doesn't share any bonds with the others. There are some other features, but the point is, Ambien doesn't share the benzodiazepine structure -- in other words, it's not a benzodiazepine. \
Like SLS says, Ambien *is* a type 1 benzodiazepine *receptor agonist*. Receptors are often named for the first agonist that is found; for example, the nicotinic acetylcholine receptor is named for nicotine, which is an agonist at this receptor. The benzodiazepine receptor is named after benzodiazepines. Just as not all nicotinic receptor agonists are nicotine, so not all benzodiazepine receptor agonists are benzodiazepines.
> So, from the standpoint of a chemist Ambien is not a benzodiazepine, but from the standpoint of a patient's nervous system it is a benzodiazepine.
Even then, it's not. At prescribed doses, its action is almost exclusively confined to one of the subtypes of benzodiazepine receptors (type 1).
> It is particularly annoying to me that the marketing folks at Searle have leveraged this little word game to make Ambien seem more innocuous to prescribing physicians and sleep disturbed consumers.
It is more innocuous. It doesn't cause the type of sleep architecture changes seen with benzodiazepines, tolerance is relatively infrequent, and withdrawal symptoms are typically mild.
> Postscript: The motivation for this venting is twofold. First, I'm sore that they charge so much for Ambien.
That makes two of us (well, a lot more).
> Second, I had SEVERE rebound insomnia when I tried to switch from Ambien to a generic benzo.
Some people get that (although it's the exception, not the rule). Take it as a sign that Ambien is *not* identical to the benzos!
-elizabeth
Posted by Anyuser on April 11, 2002, at 11:43:24
In reply to Re: Is Ambien a Benzodiazapine? » fachad, posted by Elizabeth on April 11, 2002, at 10:59:38
What are the "sleep architecture changes seen with benzodiaepines" and what is the implication? I sleep like a brick on Ativan.
Thanks.
Posted by djmmm on April 11, 2002, at 13:20:37
In reply to Re: Is Ambien a Benzodiazapine? » fachad, posted by Elizabeth on April 11, 2002, at 10:59:38
Ambien isn't a benzo for a few reasons, one of which is the ratio at which it produces muscle relaxation compared to a hypnotic state is much higher than a typical benzo.
Studies show that Ambien only binds to the omega-1 receptor, as opposed to all the omega receptors like typical Benzos, this is why ambien lacks anxiolytic, muscle relaxant, and anticonvulsant activity.
Posted by fachad on April 11, 2002, at 19:19:29
In reply to Elizabeth, posted by Anyuser on April 11, 2002, at 11:43:24
Anyuser,
How much Ativan does it take to make you "sleep like a brick?
I am taking 2 1mg tablets, and I have trouble falling asleep, even if I take them 2 or 3 hours before I want to go to bed.
Just wondering if I need to increase the dose or switch to a different med.
> What are the "sleep architecture changes seen with benzodiaepines" and what is the implication? I sleep like a brick on Ativan.
>
> Thanks.
Posted by fachad on April 11, 2002, at 20:09:21
In reply to Re: Is Ambien a Benzodiazapine? » fachad, posted by Elizabeth on April 11, 2002, at 10:59:38
Elizabeth wrote: "It (Ambien) is more innocuous. It doesn't cause the type of sleep architecture changes seen with benzodiazepines..."
Are you sure about that? I'd heard that before, but I wasn't sure if it was really true or if it came from Searle and was just marketing hype.
Also, do you take your 20mg all before bed, or 10 at bedtime and 10 in the middle of the night? I'm just wondering if 20mg lasts longer than 10mg or if you just need more because of high natural tolerance.
At this point, I wouldn't mind paying for Ambien if it lasted all night and if it didn't mess up my sleep architecture.
> > I think Ambien IS a benzodiazepine.
> >
> > The whole argument turns on semantics and your definition of what is or is not a benzodiazepine.
>
> Ambien isn't a benzodiazepine. "Benzodiazepines" are chemicals that have a certain core chemical structure. "Benzo" refers to the benzene ring. The "diazepine" ring has seven-atoms, with nitrogens at the 1 and 4 positions, and one double bond. These two rings share a bond; benzos also have a second benzene ring (it's called the "pendant ring" because when you draw a 2D representation of the molecule, it appears to be "hanging from" the diazepine ring) which doesn't share any bonds with the others. There are some other features, but the point is, Ambien doesn't share the benzodiazepine structure -- in other words, it's not a benzodiazepine. \
>
> Like SLS says, Ambien *is* a type 1 benzodiazepine *receptor agonist*. Receptors are often named for the first agonist that is found; for example, the nicotinic acetylcholine receptor is named for nicotine, which is an agonist at this receptor. The benzodiazepine receptor is named after benzodiazepines. Just as not all nicotinic receptor agonists are nicotine, so not all benzodiazepine receptor agonists are benzodiazepines.
>
> > So, from the standpoint of a chemist Ambien is not a benzodiazepine, but from the standpoint of a patient's nervous system it is a benzodiazepine.
>
> Even then, it's not. At prescribed doses, its action is almost exclusively confined to one of the subtypes of benzodiazepine receptors (type 1).
>
> > It is particularly annoying to me that the marketing folks at Searle have leveraged this little word game to make Ambien seem more innocuous to prescribing physicians and sleep disturbed consumers.
>
> It is more innocuous. It doesn't cause the type of sleep architecture changes seen with benzodiazepines, tolerance is relatively infrequent, and withdrawal symptoms are typically mild.
>
> > Postscript: The motivation for this venting is twofold. First, I'm sore that they charge so much for Ambien.
>
> That makes two of us (well, a lot more).
>
> > Second, I had SEVERE rebound insomnia when I tried to switch from Ambien to a generic benzo.
>
> Some people get that (although it's the exception, not the rule). Take it as a sign that Ambien is *not* identical to the benzos!
>
> -elizabeth
Posted by Anyuser on April 11, 2002, at 20:42:21
In reply to ANYUSER: How Much Ativan to Sleep Like a Brick? ? » Anyuser, posted by fachad on April 11, 2002, at 19:19:29
Only 1 mg puts my lights out.
Posted by Anyuser on April 11, 2002, at 20:43:49
In reply to Is Ambien a Benzodiazapine?, posted by fachad on April 8, 2002, at 9:22:22
Posted by paxvox2000 on April 12, 2002, at 19:47:06
In reply to Is Ambien a Benzodiazapine?, posted by fachad on April 8, 2002, at 9:22:22
Speaking of Ambien. I am interested to hear from others who have/are using Ambien on a long-term basis. I had taken it for a year or so back in 1997 until I started seeing the Pdoc. He IMMEDIATELY took me off Ambien, albeit he eventually "allowed" me to get some Tranzene to help me sleep.
I know that Ambien, because of it very short half-life, can cause wakefulness during the last part of one's sleep. This is indeed the case for me, however nothing else I have used (except Halcion) would put me to sleep w/o my normal nightly ruminating and worrying.
Sooooo... my Pdoc doesn't want me to take Ambien, but I have gotten my GP to scibt me some. He knows what meds my Pdoc gives me, but does not share his dislike for Ambien as a sleep agent.
Been back on it for past 6 months.What are your experiences with chronic use? Anyone take it for over a year+? I don't want to get off of it, however I DO have a little concern about the waking early. I guess it's the trade off I'm willing to make to GET TO SLEEP at night.
Any input would be appreciated!
PAX
Posted by SLS on April 14, 2002, at 22:42:18
In reply to Re: Is Ambien a Benzodiazapine?, posted by paxvox2000 on April 12, 2002, at 19:47:06
Hi Pax.
> I know that Ambien, because of it very short half-life, can cause wakefulness during the last part of one's sleep. This is indeed the case for me, however nothing else I have used (except Halcion) would put me to sleep w/o my normal nightly ruminating and worrying.
I don't know what the deal is with your pdoc and Ambien. Did he detail for you his reasons for avoiding its use?
When I first tried combining Parnate with desipramine, I could not sleep a wink for over a week. My doctor felt that I needed something to both put me to sleep and keep me asleep. His solution was to use two different drugs, one to fill each of the two roles. At bedtime, I took the potent drug Halcion (triazolam) to put me to sleep and Ativan (lorazepam) to keep me asleep so as to counter the rebound awakenings that often accompany the short half-life of Halcion.
I don't know how good Tranxene (clorazepate) is for sleep. I see that it is officially indicated only for anxiety. I like both Ativan and Restoril (temazepam) as drugs to keep me asleep, although Restoril is not particularly effective for initial insomnia. I have never tried Ambien or Sonata. Sonata (zaleplon), a non-benzodiazepine hypnotic, would be analogous to Halcion in that it is short-acting and packs a potent punch.
For anyone - I see that the term "sleep architecture" has come up. Of what significance are the differences between these drugs in the way they affect sleep architecture? Aside from the differences observed in EEG recordings, how do these various alterations affect function, performance, or health?
Thanks.
- Scott
Posted by paxvox2000 on April 15, 2002, at 18:51:39
In reply to Re: Is Ambien a Benzodiazapine?, posted by SLS on April 14, 2002, at 22:42:18
Thanks for the follow-up, Scott. My Pdoc never really got into WHY he didn't like the Ambien, perhaps it was because of the short duration aspect, but HE was the one to give me the Tranzene (which is indicated in the PDR for sleep problems). I have had Halcion before. Boy-howdy! That put me out for sure, but I had some anxiety issues after several months of use that was attributed to the Halcion, so I had to quit. I have gotten Ativan before, and find it works much better than the Tranzene. Unfortunately, I am in that sort of position where I feel "lucky" he's giving me ANY benzo for as long as he has been, and don't want to push the issue. I know that may sound weird, but I live in a state that is a bit backward about meds.
PAX
Posted by Chris A on April 15, 2002, at 20:42:06
In reply to Re: Is Ambien a Benzodiazapine?, posted by SLS on April 14, 2002, at 22:42:18
Scott and all,
It's my understanding that REM is shortened somewhat with Ambien. Remeron is supposed to provide a more natural sleep architecture, for those who can tolerate it.I've lost track of how long I've taken Ambien. I've suspected that it may play a part in some of my cognitive impairment, but don't know for sure. My solution to waking up in the middle of the night and not being able to go back to sleep is to take another 5 mgs. It works everytime, but I haven't had to do it lately. I don't take the second dose after 4:00 a.m. My pDoc has given his blessing to this approach, as he doesn't want any of his bipolar patients not sleeping. I am dependent on Ambien, but have not had to increase the dose. He'd rather me be dependent rather than have insomnia. BTW, I've tried all the sleep hygeine tricks for years.
Blessings,
Chris A.
Posted by DaveW on June 25, 2002, at 22:11:36
In reply to Re: Is Ambien a Benzodiazapine?, posted by paxvox2000 on April 15, 2002, at 18:51:39
> Thanks for the follow-up, Scott. My Pdoc never really got into WHY he didn't like the Ambien, perhaps it was because of the short duration aspect, but HE was the one to give me the Tranzene (which is indicated in the PDR for sleep problems). I have had Halcion before. Boy-howdy! That put me out for sure, but I had some anxiety issues after several months of use that was attributed to the Halcion, so I had to quit. I have gotten Ativan before, and find it works much better than the Tranzene. Unfortunately, I am in that sort of position where I feel "lucky" he's giving me ANY benzo for as long as he has been, and don't want to push the issue. I know that may sound weird, but I live in a state that is a bit backward about meds.
>
> PAXJust saw this post...I've been on Ambien over 6 years and it works the same now as then. My doctors have talked about taking me off it but it works so we go with it. Sure if in the future I can switch to something as good and cheaper I will but for now it is worth getting a good sleep. (Actually I sleep more than I'd like to but before the Ambien I couldn't sleep at all).
Posted by johnj on June 26, 2002, at 21:32:41
In reply to Re: Is Ambien a Benzodiazapine?, posted by paxvox2000 on April 15, 2002, at 18:51:39
You mentioned tranzene, of which I take, and I was wondering about what you meant about PDR for sleep? I am interested in knowing if tranzene might disrupt sleep. Thanks
johnj
Posted by hbo on May 2, 2003, at 1:54:12
In reply to Re: Is Ambien a Benzodiazapine?, posted by DaveW on June 25, 2002, at 22:11:36
There's some interesting new research out of U of Utah regarding GABA promoting agents increasing the performance of aged monkeys on visual perception tests. The theory is, since GABA quiets neuronal activity, that this counters a tendency for aged brains toward neurons firing in response to stimuli that younger ones would not. So the old monkey's vision input system (eyes and so forth) are fine, but the multiple visual processing centers (how many do rhesus monkeys have? Humans have 30 or so) don't focus on visual stimuli appropriately because of the noise their aged neurons respond to. This result _may_ generalize to address other aging effects on the brain in monkeys, and perhaps humans!
Now, my father is 81, and has a fine intellect. He's starting to slip however. It doesn't look like Alzheimer's. Though I'm not a doctor, and I realize that a definitive diagnoses for the big "A" can only be done post-mortem :((, I still see no sign of some of the other symptoms, such as emotional or aggressive outbursts. Anyhow, I'm surely not going to suggest that he take a Valium and see if falls asleep or wakes up, but it's tempting!
The paper is in Science: (vol 300, p 812), which I don't have since I let my subscription lapse. But here's a link to the story in New Scientist:
http://www.newscientist.com/news/news.jsp?id=ns99993686
Posted by MattD on May 3, 2003, at 18:16:37
In reply to Valium, GABA and Age., posted by hbo on May 2, 2003, at 1:54:12
Studies have shown that Vitamin E (800-1200 IU) helps moderately-significantly with cognitive deterioration, especially at early stages. My pdoc was telling me about some new studies he had just seen that had convinced him to start taking E.
Best,
Matt
Posted by hbo on May 3, 2003, at 20:46:02
In reply to Re: Valium, GABA and Age. » hbo, posted by MattD on May 3, 2003, at 18:16:37
Thanks for the tip. He already takes E along with quite a few other supplements.
I took a look at the article in Science. They were dosing their monkeys electrophoretically with GABA and muscimol!
Muscimol (aka Ibotenic acid) is the toxin found in Amanita Muscaria. It's highly toxic and an hallucinogen. It's also fairly widely used in brain research judging by the number of hits returned by a Google search.
Not the sort of thing I can recommend to my father.
This is the end of the thread.
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