What is it?

Varenicline is a medication designed to help you quit smoking. It will not make you quit, but it may help.

In order to understand how this medication works, you have to understand how nicotine works.

When you inhale cigarette smoke, nicotine is absorbed into your blood stream and travels to the brain. There, the nicotine molecules bind to microscopic receptors on the nerve cells in a particular part of the brain. This triggers the release of a chemical in the brain called dopamine. This dopamine causes a person to feel good and is thought to play a big part in the addictive nature of cigarettes.

Varenicline is thought to work by binding to these same nicotine receptors. When it binds to the receptors, it also is thought to trigger some dopamine release, but not nearly as much as what is seen with nicotine. Thus, a smoker doesn’t experience as much (if any) withdrawal symptoms as they would if they quit “Cold Turkey.”

By binding to the receptors, the Varenicline also effectively blocks nicotine from binding to them. Therefore, when a smoker who is taking Varenicline does smoke a cigarette, they don’t get the chemical reward anymore.

Think of it this way. If you have a lock on your front door, and someone puts a key in there that fits in the lock, but won’t turn it, then that key won’t open the door. If, while that key is in the lock, you come along with the correct key, it won’t be any good either because it can’t get into the lock as long as that other key is in the way.

Varenicline and nicotine are both keys that fit in the same lock, but varenicline doesn’t turn the lock nearly as well as nicotine. When Varenicline is in the lock, nicotine can’t get in the lock because the varenicline is in the way.

Currently in the U.S., varenicline is only available under the brand name Chantix and is made by Pfizer. It comes as a tablet in two different strengths; a 0.5mg tablet and a 1.0mg tablet. They say “Pfizer” on one side and either “CHX 0.5” or “CHX 1.0” on the other side depending on the strength. The 0.5mg tablet is white and the 1.0mg tablet is light blue.

What is the normal dose?

Varenicline is only to be used in adults at least 18 years of age.

Normally, a patient should plan on a date to stop smoking and should start the medication one week prior to this date.

The medication should be taken after eating and with a full glass of water.

The normal starting dose is 0.5mg once daily for the first 3 days.

Then, the dose if increased to 0.5mg twice daily for days 4-7.

On day 8 the dose is increased to 1.0 mg twice daily, and this dose is continued until the end of treatment.

The Chantix brand is actually sold as a “Starter Pack” and “Continuing Packs” to make following this regimen easier.

Your doctor may alter the above dosing somewhat depending on your particular medical needs. For instance, in patients with severe kidney impairment, the dosage is typically lowered.

Normally, therapy is continued for at least 12 weeks, by which time, the patient has hopefully stopped smoking. If the patient has successfully stopped smoking, an additional 12 weeks of therapy may be given, and is in fact encouraged, to increase the odds that the smoking cessation will be permanent.

Are there any side effects”

The short answer is “Yes.” This is true for all medications, and Varenicline is no different. The majority of patients will not experience any or all of these, but some folks will.

As with most, if not all medications, there is actually an extremely long list is possible side effects. I don’t intend to list each and every one of them here, as I’d be typing all day. If you are interested in this list, you can certainly find it elsewhere on the internet, or obtain it from you pharmacist.

The following list certainly does not include each and every possible side effect that can be seen, but these are the most common ones.

The most common side effects include nausea, headaches, and insomnia. Other less frequent side effects seen include vomiting, constipation, flatulence, and abnormal dreams.

One particular uncommon potential side effect that must be discussed is increased risk of suicide. Since being released to the market by the FDA, there have been some reports of increased risk of suicide and suicide attempts by people taking Chantix. Is this due to the Chantix itself, or is it due to other factors? We don’t know yet.

The thing is when people stop smoking, whether with Chantix or not, there is an increased risk of these behaviors as well as an increased risk of any underlying psychiatric disorders getting worse. This tends to argue against Chantix itself as being to blame.

That said, many of the reported cases of folks developing these problems, have occurred in patients taking Chantix, but who have continued to smoke. Some have also occurred in folks with no previously diagnosed psychiatric problems. On the surface at least, this tends to argue for Chantix itself as being to blame.

My personal take on this (in other words my personal opinion, based on personal experience, and what I’ve read about it), is that the Chantix itself is most likely not directly responsible.

Why do I think this?

First, if you look back to the first part of this article where I described how this medication works, you’ll see that what it does is it blocks the receptors that nicotine normally works on. Although the varenicline itself does in fact activate these receptors, it does so much less strongly than does nicotine. So, with the medication, there is some of that dopamine reward, but not nearly as much as with nicotine.

Also, since varenicline blocks the receptors from nicotine having any effect, even though the patient continues to smoke cigarettes, as far as the brain is concerned, on a chemical level, they have stopped.

As far as the fact that many patients taking Chantix and having these psychiatric problems are folks who had no previously diagnosed psychiatric illness, I can only give the opinion that perhaps some, if not all of them did in fact have previous illness, but that it simply had not been formally diagnosed. Virtually any psychiatrist you ask will tell you that there are an awful lot of folks walking the streets with undiagnosed psychiatric illness. Many of them are effectively “self-medicating” with things like alcohol, drugs, nicotine, etc. I suspect that Chantix has perhaps effectively taken away this “self-medication” from some of these folks and we are seeing the effects of this.

Again, however, this is all just my opinion, and perhaps further evidence will become available in the future to either strengthen or weaken that opinion. I’m sure that there are some trial lawyers out there licking their chops, eager to do all they can to convince folks that Chantix is to blame in any and all cases.

So, what’s the bottom line on all this? Well, if you take Varenicline, you might indeed have one or more side effects. If, in fact you do have any history of any sort of psychiatric illness, depression, suicidal thoughts, etc., you absolutely need to discuss this at length with your doctor before taking this medication.

All that said, while this medication might cause some side effects, continuing to smoke cigarettes is quite likely to cause some nasty side effects. This medication might help you to quit smoking. Whether you use this medication or not, quit smoking. If you do quit smoking, be aware that you may have some increased likelihood of feelings of depression, suicidal thoughts, etc. If you experience any of this, get some help. There are plenty of folks out there who can help and want to help, but can only do so if they are aware there is a problem. Don’t suffer in silence. Ask for help. Let you family know, let your friends know, let your doctor know, that you need help.

Are there any interactions with this medicine?

So far, there are not any known clinically significant interactions between Varenicline and any other medications. That said, in folks who take Warfarin (which is a blood thinner), stopping smoking may alter its effectiveness and require a dosage change.

In studies, people who took varenicline and at the same time used nicotine patches did have some increased incidence of nausea, headache, vomiting, dizziness, dyspepsia and fatigue, when compared to folks who used nicotine patches alone (without also taking varenicline).

Is there anyone who should not use this medicine?

As above, it should not be used by anyone under 18. It should not be used by anyone known to have an allergy to it. It should be used with caution in anyone with impaired kidney function or psychiatric illness.

Pregnant women should talk to their doctor about the safety of this medicine before using it. This medicine is currently classified as a pregnancy class “C” drug. This means that animal studies have shown some adverse fetal effects but there have been no controlled human studies OR there have been no animal or human studies. What that means, is that while it’s never been shown to be dangerous to unborn human babies, it’s never been proven to be safe either, so talk with your doctor about this.

Breastfeeding women should talk to their doctor before using this medication as well. As far as I know, it has never been studied whether this drug is passed in human milk, but it has been shown to be passed in the milk of animals (dogs). If it is passed in a nursing mother’s milk, will it harm the baby? That’s also not known (as far as I’m aware), so the best answer I can give is “Maybe.” Talk to your doctor about this.

As mentioned earlier, the dose may need to be adjusted in folks with kidney impairment. This may also be true with elderly patients, but there isn’t any strong evidence so far to this effect.