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Misc How Does Chantix Work?

Jabberwocky

Frumious Bandersnatch
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Nov 3, 1999
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[EDIT: If there is a chantix/varenicline megathread or something similar please just merge this, thank you! If not, maybe this thread could be a start? Just a thought <3]

The wiki article confirms what I had already suspected about Varenicline (Chantix) and how it works. My hypothesis, after reading through the package insert for Chantix, is similar to that regarding buprenorphine. As with bupe maintenance/detox, Varenicline outcompete/fills up certain receptors in the brain - analogous to how bupe out-competes other opioids and fills up the opioid receptors so that other opioids can't attach/stimulate them.

Like buprenorphine, Varenicline would seem to be a partial agonist, but there are some significant differences between the two. When I started Chantix, I was still smoking. So it's not exactly like bupe, no sir. If it was I'd have gone into precipitated nicotine withdrawal (or whatever) upon starting the Chantix. I undoubtedly had nicotine in my system when I did. There is a possibility I did go through this, and that it's just much less sever side effects next to buprenorphine and precipitated opioid withdrawal.

So, what happens with the Varenicline building up in my body/brain, filling more than more of those receptors normally stimulated/affects by the introduction of nicotine into one's system, nicotine has less and less of an affect on my self and the level of nicotine in my system, once I've finished cutting down and finally quit, drops lower and lower. With lower nicotine levels I've noticed that I can smell better, taste better, etc. etc. - things I'd associated with quitting smoking prior to this (but this is the first time I've tried something other than nicotine replacement therapy; with no nicotine in my system and not smoking, I find smells/tastes are still a lot more vibrant than they've been when on the patch or gum and not smoking).

Anywho, like how bupe prevents most other opioids from binding to one's opioid receptors, varenicline prevents nicotine from stimulating one's whatever-receptors. This means, not only am I less interested in smoking a fag generally, I'm not constantly thinking about when I'm going to have that next smoke or have any urge to smoke compulsively. That's the best parts about this whole thing for me. There is something about how varenicline works that makes its use for cessation more effective than NRT, as even on NRT I would still think about nicotine (either smoking or the buzz the patch/gum would give me). For the first time in a long time, I can sit still for three hours to watch a long drawn out movie. No longer do I have to dash out around the middle of a meal out to sneak a smoke.

It's still total forgien to simply not think so much about smoking, but I'm certainly enjoying this weirdness. I just need to make sure I continue to take advantage of this situation and get into healthier and healthier habits.

I've noticed literally no side effects from the varenicline, although I'm only on week three. Literally nothing, although I have noticed some positive and negative side effects from not having nicotine in my system. Here's how it's described on wikipedia:

Mechanism of Action said:


What are your thoughts, for those of you who've tried Chantix, for better or worse. For those of your with neuroscience/related backgrounds, would you please be kind enough to explain this drug works? Thanks!
 
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I don't know how it works but it gave me totally fucked up dreams. I couldn't hack it and went the e cig route. Glad ya got no side effects though! Good luck on quitting cigs.
 
It binds to certain nicotinic acetylcholine receptors that are strongly affected by nicotine. Since it's affinity for the receptors is much stronger than that of nicotine, when one smokes, the nicotine cannot occupy these receptors that is responsible for the dopamine release. Because it's just a partial agonist, it doesn't stimulate the dopamine system, but because these receptors are filled it reduces the urges the user has to smoke. The reason you can continue to smoke when you first start is because:

Not all of these nicotinic acetylcholine receptors are saturated right away. This drug has a 24 hour half-life, so plasma concentrations build slowly over time. This is why your urges to smoke are stronger in the beginning; the drug hasn't reached maximum concentrations, so there's still many receptors that aren't being stimulated. If you'll notice you only take half the normal dose in the first week; this allows the drug to build up slow enough so that the patient can continue to smoke until it's reached a certain level where urges have diminished enough for the patient to transition more smoothly into the cessation stage.

This is also why your urges continue to weaken as you remain taking the drug. More and more of these receptors are getting filled up and telling your body that you don't need a cigarette.

This is how I understand the workings of this drug. I'm self-learned though, so I don't know how much you should trust my assessment lol.
 
Yea, that's my working theory. I can understand how the vivid dreams Chantix gives most people, myself included, could be a problem. Not so for me though, especially when I take melatonin and Chantix, the former also producing more vivid dreams, I have really fucking awesome dreams! Makes sleeping so much fun. Frankly, I've been sleeping better on the Chantix than I have in years and years! That said, I've been smoking herbbage pretty much daily since I started the Chantix, so that is probably helping me sleep more soundly as well as blunting some of the vividness when I dream (weed, along with most drugs I've tried, makes it so that I rarely if ever remember my dreams, so I could see how it would in the present case make my dreams a little less intense but still memorable.
 
Weed does decrease the amount of time spent in REM sleep, so it makes sense.
 
Wellbutrin worked really well for me in terms of stopping smoking. After about 5-6 days I literally got no effects from smoking at all. Even the first cig of the day. I was started on it when I entered a inpatient rehab to get off methadone. It wasn't a very enjoyable experience being stuck in that place coming off a year of 120mg of methadone a day but I managed to do that and stop smoking at the same time. Fun times.
 
Weed does decrease the amount of time spent in REM sleep, so it makes sense.

Cool, I always wondered how to explain for that (and like I said, it's most prevalent when I take gabaergic drugs (zolpidem/drink 3+ ethanol beverages/benzos/etc) as well as potent ndma antagonists (ketamine/dxm/mxe/etc) and full agonist opioids (although less so than gabaergic and nmda-antagonists). And that goes for stims (cocaine hcl/amp/methamp/etc) too, so if I want to have awesome and memorable dreams in the near future I have to be as close to clean and sober as possible...

I could be wrong about using the ndma antagonist label in my little typology there. I used drugs like dxm and ketamine to play around with how they'd benefit me most for opioid tolerance and acute withdrawal. Such unique drugs. I used to hate dxm but now I'm, although a little apprehensive and somewhat in awe, I'm in love with it (to the dream one can love a thing).

I figure the stims mainly caused this because neither in mind or body would I be able to fully relax. And with the gabaergic drugs, especially the beznos and z-drugs, figured they impaired my memory anyways to make remembering dreams just impossible until the drug cleared my system.
 
I don't normally like DPing, but whatever...

So today I smoked a cigarette, against my better judgement, and it made me feel like absolute shit! It was a lot like, although not as bad, as when I basically had a "minor" OD on nicotine after first starting smoking way back when. Laid down in bed for an hour and took a little nap, and after that and a bowl of cereal I feel fine.

Still, wtf? Is this how it's supposed to work, that it doesn't only negate any positive effects of nicotine, but makes you feel like shit if you go and try to introduce it into your system?

Wow...

Well whatever, safe to say at least I don't feel like smoking anytime soon :\
 
I don't normally like DPing, but whatever...

Yeah most people don't like when balls touch. ;)

So today I smoked a cigarette, against my better judgement, and it made me feel like absolute shit! It was a lot like, although not as bad, as when I basically had a "minor" OD on nicotine after first starting smoking way back when. Laid down in bed for an hour and took a little nap, and after that and a bowl of cereal I feel fine.

Still, wtf? Is this how it's supposed to work, that it doesn't only negate any positive effects of nicotine, but makes you feel like shit if you go and try to introduce it into your system?

Wow...

Well whatever, safe to say at least I don't feel like smoking anytime soon :\

Yes it should be a deterrent from smoking more. I'm not familiar with nicotine addiction (I'm not a nicotine user at all) but I would imagine using chantix and then smoking would produce an undesirable effect.

Stay on chantix and you should be cigarette free eventually and you'll be really happy you did it.
 
Wellbutrin worked really well for me in terms of stopping smoking. After about 5-6 days I literally got no effects from smoking at all. Even the first cig of the day. I was started on it when I entered a inpatient rehab to get off methadone. It wasn't a very enjoyable experience being stuck in that place coming off a year of 120mg of methadone a day but I managed to do that and stop smoking at the same time. Fun times.

Sorry to toothpastedog the OP, as this is slightly off topic, but could you tell if the Wellbutrin added to any of the methadone WD symptoms like insomnia or anxiety? Because those are listed side effects for Wellbutrin I am hesitant to take it while having bad methadone PAWS. Also could you tell if it helped with the methadone WD at all? (mood, lack of energy, etc)
 
Sorry to toothpastedog the OP, as this is slightly off topic, but could you tell if the Wellbutrin added to any of the methadone WD symptoms like insomnia or anxiety? Because those are listed side effects for Wellbutrin I am hesitant to take it while having bad methadone PAWS. Also could you tell if it helped with the methadone WD at all? (mood, lack of energy, etc)

If you're using it to quick smoking, I would look elsewhere. It's a pretty shitty drug to use for that purpose (tried it). The side effects, especially for those already predisposed, such as people in their mid fifties with high cholesterol/heart disease as well as those experiencing PAWS from opioid cessation, can be pretty bad. In one case I know of personally almost deadly.

The only thing I've heard of wellburtrin working remotely well for is people coming off meth binges (it has a very slight stim effect, and I've heard this can help) or depression/whatever. I could see how the slight stim effect of wellbutrin could help in PAWS, but I doubt it would help all that much (in my case lexapro worked much better, although I hated how lethargic, relatively speaking, it made me feel).

Iono, if you're thinking about trying wellbutrin for treating PAWS from opioid withdrawal and you don't have any major risk factors (i.e. you don't have heart disease) I'd give it a try if it's easy to get and not cost prohibative. Just keep a close eye on things and stop at the first signs of trouble. It may help you depression and whatnot in this case, and I never had any problems with it causing insomnia, although I could see it happening during PAWS considering I would already have insomnia to a degree.

If you're going to use it for nicotine/smoking cessation, don't get your hopes up. No problem giving it a try, just be careful. IMO it's the worst of the choices out there for this purpose.
 
I wouldn't suggest bupropion for smoking cessation; it's an antagonist at the nicotinic acetylcholine receptor.

Wellbutrin/bupropion is the active drug in Zyban for smoking cessation, albeit at a MUCH lower dose. I've forgotten the pharmacology from when we were taught it during a periodontal course in dds school, but it is also a very successful treatment -- however the success rates are not as high as Chantix. It's approx 40-50% vs 50-60% respectively.

I imagine the antagonism has something to do with it's action, but the ultra-low dose must play an important role in a fine balancing act. I'd have to look into it.
 
My girlfriends brother took this stuff but had to get off because he was becoming so violent and aggressive.

Here's the abstract from a study done on Chantix and aggression/homicidal ideation. :\

"Varenicline, a drug used for smoking cessation, carries a risk of neuropsychological adverse effects, including depression and suicide. Analysis of a series of detailed reports of aggression and homicidal ideation attributed to varenicline showed that most patients had no psychiatric history. These symptoms were often preceded by sleep disorders. Suicide and suicidal ideation were associated with signs of aggression in nearly one-third of cases. Aggressive symptoms recurred in patients who restarted varenicline. In practice, it is better to avoid using varenicline for smoking cessation and to use nicotine replacement instead when drug therapy is considered necessary."

Source
 
Thanks for the replies on Wellbutrin (bupropion) guys and sorry to toothpastedog for hijacking the thread! :) Although I think you already answered your own question very well - varenicline is very much to nicotine what buprenorphine is to opiates.

I would be taking the Wellbutrin for depression, ADHD, chronic fatigue, lack of motivation, general opioid PAWS, etc. If it helped me quit smoking that would just be an added benefit.

I do have a close friend who is on Wellbutrin and says that as far as quitting smoking he really didn't feel like it was fully blocking the enjoyment/effects of cigarettes, he just found himself not wanting to smoke as much and gradually smoked less and less. I was like, "Are you sure?!? It's a nicotine receptor antagonist," but he said it really didn't bother him or make him feel any tobacco withdrawals or anything. Just a tiny bit or irritability for the first week of taking it which is a very common side effect even for people who do not smoke.

toothpastedog - Why do you think bupropion is a bad drug for quitting smoking? Just because of the potential for side effects?
 
My great-aunt used chantix to stop smoking after like fifty years of heavy smoking and it worked for her.

As far as wellbutrin, I've never met anyone who that shit worked for except for tweakers who just liked that it gave you energy. I've wondered how it would work for me since a big symptom of my depression is complete and total lethargy but I've just heard so many negative effects about it.

And as someone stated above, it has about a 45% success rate as opposed to chantix with close to 60%.
 
As far as wellbutrin, I've never met anyone who that shit worked for except for tweakers who just liked that it gave you energy.
Did you mean people who were taking bupropion specifically/just to quit smoking, or people who were taking it for depression etc? Everyone I know who has taken it says it was the best antidepressant they have ever taken (most effective, least side effects, least withdrawal, etc).

And as someone stated above, it has about a 45% success rate as opposed to chantix with close to 60%.
Where did someone say that above? Maybe I am just blind :?

It depends on the study, but this study found:
After 4 weeks: varenicline to have a 44% success rate vs bupropion with 30% (placebo was 18%)
After 9 weeks to 1 yr (the drug was taken for the first 12 weeks): varenicline to have a 22% success rate vs bupropion with 16% (placebo was 8%)
 
Swimming,
I posted the approx success rates just a couple posts above, so take another look - otherwise u may want to get your eyes checked ;)

I was particularly speaking of Zyban, the alternative to Chantix, which is a low dose bupropion. I was taught in my peridontal treatment planning/case studies course of those success rates. As for taking a "full" dose of wellbutrin indicated for depression, et al. - I'm unsure of it's success rates as it compares to Zyban in specific regard to smoking cessation.

Im too tired to look up the difference in dose of bupropion of Zyban vs Wellbutrin.

We were also taught that one CAN smoke thru their treatment of Zyban, and still receive the "benefit" of the nicotine. This course wasn't about the pharmacology behind it, so the information was generalized with: "bupropion/zyban work on the addiction center of the brain", so while Zyban users can still smoke without ultimate antagonism (Id like to see the source that indicates that at least Zyban is infact an antagonist at the acetylcholine/nicotine receptor sites. Because that would seemingly be counterintuitive to what we were taught. Perhaps there is some antagonism, but not flooded receptor sites, or with a weaker affinity and a greater dissociation constant/half-life.

My vote is for zyban or wellbutrin depending on your intention. obviously, you may want to investigate zyban vs wellbutrin.
 
My girlfriends brother took this stuff but had to get off because he was becoming so violent and aggressive.

Here's the abstract from a study done on Chantix and aggression/homicidal ideation. :\

"Varenicline, a drug used for smoking cessation, carries a risk of neuropsychological adverse effects, including depression and suicide. Analysis of a series of detailed reports of aggression and homicidal ideation attributed to varenicline showed that most patients had no psychiatric history. These symptoms were often preceded by sleep disorders. Suicide and suicidal ideation were associated with signs of aggression in nearly one-third of cases. Aggressive symptoms recurred in patients who restarted varenicline. In practice, it is better to avoid using varenicline for smoking cessation and to use nicotine replacement instead when drug therapy is considered necessary."

Source

Yes it does have some risks, which is the down side to Chantix; it's best to quit cold turkey if possible.
 
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