Chantix

Generic name: varenicline
Drug class: Smoking cessation agents

Medically reviewed by A Ras MD.

What is Chantix?

Chantix is a prescription medicine to help people stop smoking. Quitting smoking can lower your chances of having lung disease, heart disease or getting certain types of cancer that are related to smoking.

Chantix has not been shown to be effective in children 16 years of age and under. Chantix should not be used in children 16 years of age and under.

It is not known if Chantix is safe and effective when used with other stop smoking medicines.

Description

CHANTIX tablets contain varenicline (as the tartrate salt), which is a partial agonist selective for α4β2 nicotinic acetylcholine receptor subtypes.

Varenicline, as the tartrate salt, is a powder which is a white to off-white to slightly yellow solid with the following chemical name: 7,8,9,10-tetrahydro-6,10-methano-6H-pyrazino[2,3- h][3]benzazepine, (2R,3R)-2,3-dihydroxybutanedioate (1:1). It is highly soluble in water. Varenicline tartrate has a molecular weight of 361.35 Daltons, and a molecular formula of C13H13N3 • C4H6O6. The chemical structure is:

CHANTIX is supplied for oral administration in two strengths: a 0.5 mg capsular biconvex, white to off-white, film-coated tablet debossed with “Pfizer” on one side and “CHX 0.5” on the other side and a 1 mg capsular biconvex, light blue film-coated tablet debossed with “Pfizer” on one side and “CHX 1.0” on the other side. Each 0.5 mg CHANTIX tablet contains 0.85 mg of varenicline tartrate equivalent to 0.5 mg of varenicline free base; each 1mg CHANTIX tablet contains 1.71 mg of varenicline tartrate equivalent to 1 mg of varenicline free base. The following inactive ingredients are included in the tablets: microcrystalline cellulose, anhydrous dibasic calcium phosphate, croscarmellose sodium, colloidal silicon dioxide, magnesium stearate, Opadry® White (for 0.5 mg), Opadry® Blue (for 1 mg), and Opadry® Clear.

Mechanism of Action

Varenicline binds with high affinity and selectivity at α4β2 neuronal nicotinic acetylcholine receptors. The efficacy of CHANTIX in smoking cessation is believed to be the result of varenicline’s activity at α4β2 sub-type of the nicotinic receptor where its binding produces agonist activity, while simultaneously preventing nicotine binding to these receptors.

Electrophysiology studies in vitro and neurochemical studies in vivo have shown that varenicline binds to α4β2 neuronal nicotinic acetylcholine receptors and stimulates receptor-mediated activity, but at a significantly lower level than nicotine. Varenicline blocks the ability of nicotine to activate α4β2 receptors and thus to stimulate the central nervous mesolimbic dopamine system, believed to be the neuronal mechanism underlying reinforcement and reward experienced upon smoking. Varenicline is highly selective and binds more potently to α4β2 receptors than to other common nicotinic receptors (>500-fold α3β4, >3500-fold α7, >20,000-fold α1βγδ), or to non-nicotinic receptors and transporters (>2000-fold). Varenicline also binds with moderate affinity (Ki = 350 nM) to the 5-HT3 receptor.

What is the most important information I should know about Chantix?

When you try to quit smoking, with or without Chantix, you may have symptoms that may be due to nicotine withdrawal, including:

urge to smoke
depressed mood
trouble sleeping
irritability
frustration
anger
feeling anxious
difficulty concentrating
restlessness
decreased heart rate
increased appetite
weight gain

Some people have even experienced suicidal thoughts when trying to quit smoking without medication. Sometimes quitting smoking can lead to worsening of mental health problems that you already have, such as depression.

Some people have had serious side effects while taking Chantix to help them quit smoking, including:

New or worse mental health problems, such as:

changes in behavior or thinking
aggression
hostility
agitation
depressed mood
suicidal thoughts or actions

Some people had these symptoms when they began taking Chantix, and others developed them after several weeks of treatment, or after stopping Chantix. These symptoms happened more often in people who had a history of mental health problems before taking Chantix, than in people without a history of mental health problems.

Stop taking Chantix and call your healthcare provider right away if you, your family, or caregiver notice any of these symptoms. Work with your healthcare provider to decide whether you should continue to take Chantix. In many people, these symptoms went away after stopping Chantix, but in some people symptoms continued after stopping Chantix. It is important for you to follow-up with your healthcare provider until your symptoms go away.

Before taking Chantix, tell your healthcare provider if you have ever had depression or other mental health problems. You should also tell your healthcare provider about any symptoms you had during other times you tried to quit smoking, with or without Chantix.

Who should not take Chantix?

Do not take Chantix if you have had a serious allergic or skin reaction to Chantix.

Symptoms may include:

swelling of the face, mouth (tongue, lips, gums), throat or neck
trouble breathing
rash, with peeling skin
blisters in your mouth

What should I tell my healthcare provider before taking Chantix?

See “What is the most important information I should know about Chantix?” above.

Before you take Chantix, tell your healthcare provider if you:

use other treatments to quit smoking. Using Chantix with a nicotine patch may cause nausea, vomiting, headache, dizziness, upset stomach, and tiredness to happen more often than if you just use a nicotine patch alone.
have kidney problems or get kidney dialysis. Your healthcare provider may prescribe a lower dose of Chantix for you.
have a history of seizures
drink alcohol
have heart or blood vessel problems
have any other medical conditions
are pregnant or plan to become pregnant.
are breastfeeding. It is not known if Chantix passes into breast milk. If you breastfeed and take Chantix, monitor your baby for seizures as well as spitting up or vomiting more than normal.

Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins and herbal supplements. Your healthcare provider may need to change the dose of some of your medicines when you stop smoking.

You should not use Chantix while using other medicines to quit smoking. Tell your healthcare provider if you use other treatments to quit smoking.

Know the medicines you take. Keep a list of them with you to show your healthcare provider and pharmacist when you get a new medicine.

How should I take Chantix?

There are 3 ways that you can use Chantix to help you quit smoking. Talk to your healthcare provider about the following 3 ways to use Chantix:

Choose a quit date when you will stop smoking. Start taking Chantix 1 week (7 days) before your quit date. Take Chantix for 12 weeks. OR
Start taking Chantix before you choose a quit date. Pick a date to quit smoking that is between days 8 and 35 of treatment. Take Chantix for 12 weeks. OR
If you are sure that you are not able or willing to quit smoking right away, start taking Chantix and reduce smoking during the first 12 weeks of treatment, as follows:

Weeks 1 through 4

Reduce your smoking to reach one-half of your starting daily number of cigarettes.
Example: If you usually smoke 20 cigarettes each day, reduce your smoking to 10 cigarettes each day during weeks 1 through 4.

Weeks 5 through 8

Reduce your smoking to reach one-quarter of your starting daily number of cigarettes.
Example: If you usually smoked 20 cigarettes each day, reduce your smoking to 5 cigarettes each day during weeks 5 through 8.

Weeks 9 through 12

Keep reducing your smoking until you are no longer smoking (you reach zero cigarettes each day).

Aim to quit by the end of the 12th week of treatment, or sooner if you feel ready. Continue to take Chantix for another 12 weeks, for a total of 24 weeks of treatment.

Starting Chantix before your quit date gives Chantix time to build up in your body. You can keep smoking during this time. Take Chantix exactly as prescribed by your healthcare provider.

Chantix comes as a white tablet (0.5 mg) and a blue tablet (1 mg). You start with the white tablet and then usually go to the blue tablet. See below for dosing instructions for adults.

Day 1 to Day 3

White tablet (0.5 mg)
Take 1 tablet each day

Day 4 to Day 7

White tablet (0.5 mg)
Take 1 in the morning and 1 in the evening

Day 8 to end of treatment

Blue tablet (1 mg)
Take 1 in the morning and 1 in the evening

Make sure that you try to stop smoking on your quit date. If you slip-up and smoke, try again. Some people need to take Chantix for a few weeks for Chantix to work best.

Most people will take Chantix for up to 12 weeks. If you have completely quit smoking by 12 weeks, your healthcare provider may prescribe Chantix for another 12 weeks to help you stay cigarette-free.

Take Chantix after eating and with a full glass (8 ounces) of water.

This dosing schedule may not be right for everyone. Talk to your healthcare provider if you are having side effects such as nausea, strange dreams, or sleep problems. Your healthcare provider may want to reduce your dose.

If you miss a dose of Chantix, take it as soon as you remember. If it is almost time for your next dose, skip the missed dose. Just take your next dose at your regular time.

What should I avoid while taking Chantix?

Use caution when driving or operating machinery until you know how Chantix affects you. Chantix may make you feel sleepy, dizzy, or have trouble concentrating, making it hard to drive or perform other activities safely.

Decrease the amount of alcoholic beverages that you drink during treatment with Chantix until you know if Chantix affects your ability to tolerate alcohol.

Some people have experienced the following when drinking alcohol during treatment with Chantix:

increased drunkenness (intoxication)
unusual or sometimes aggressive behavior
no memory of things that have happened

What are the possible side effects of Chantix?

Serious side effects of Chantix may include:

See “What is the most important information I should know about Chantix?” above.
Seizures. Some people have had seizures during treatment with Chantix. In most cases, the seizures have happened during the first month of treatment with Chantix. If you have a seizure during treatment with Chantix, stop taking Chantix and contact your healthcare provider right away.
New or worse heart or blood vessel (cardiovascular) problems, mostly in people, who already have cardiovascular problems. Tell your healthcare provider if you have any changes in symptoms during treatment with Chantix.
Get emergency medical help right away if you have any of the following symptoms of a heart attack, including:
- chest discomfort (uncomfortable pressure, squeezing, fullness or pain) that lasts more than a few minutes, or that goes away and comes back
- pain or discomfort in one or both arms, back, neck, jaw or stomach
- shortness of breath, sweating, nausea, vomiting, or feeling lightheaded associated with chest discomfort
Sleepwalking can happen with Chantix, and can sometimes lead to behavior that is harmful to you or other people, or to property. Stop taking Chantix and tell your healthcare provider if you start sleepwalking.
Allergic reactions can happen with Chantix. Some of these allergic reactions can be life-threatening.
Serious skin reactions, including:
- rash,
- swelling
- redness
- peeling of the skin
- Some of these skin reactions can become life-threatening.

Stop taking Chantix and get medical help right away if you have any of the following symptoms:

swelling of the face, mouth (tongue, lips, and gums), throat or neck
trouble breathing
rash with peeling skin
blisters in your mouth

The most common side effects of Chantix include:

nausea
sleep problems (trouble sleeping or vivid, unusual, or strange dreams)
constipation
gas
vomiting

Tell your healthcare provider about side effects that bother you or that do not go away.

These are not all the side effects of Chantix. Ask your healthcare provider or pharmacist for more information.

Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

General information about the safe and effective use of Chantix

Medicines are sometimes prescribed for purposes other than those listed in a Medication Guide. Do not use Chantix for a condition for which it was not prescribed. Do not give your Chantix to other people, even if they have the same symptoms that you have. It may harm them. If you would like more information, talk with your healthcare provider. You can ask your healthcare provider or pharmacist for information about Chantix that is written for healthcare professionals.

For more information about Chantix and tips on how to quit smoking, go to www.Chantix.com or call 1-877-242-6849.

If you are motivated to quit smoking and did not succeed during prior Chantix treatment for reasons other than side effects, or if you returned to smoking after treatment, speak with your healthcare provider about whether another course of Chantix therapy may be right for you.

How should I store Chantix?

Store Chantix at room temperature, between 68°F to 77°F (20°C to 25°C).
Keep Chantix and all medicines out of the reach of children.

What are the ingredients in Chantix?

Active ingredient: varenicline tartrate

Inactive ingredients: microcrystalline cellulose, anhydrous dibasic calcium phosphate, croscarmellose sodium, colloidal silicon dioxide, magnesium stearate, Opadry White (for 0.5 mg), Opadry Blue (for 1 mg), and Opadry Clear.

Label

PRINCIPAL DISPLAY PANEL – KIT CARTON

STARTING PACK
(Your first 2 weeks)
ONE PER PATIENT
NDC 63539-473-10
Rx only
CHANTIX®
(varenicline) TABLETS
Contains:
Week 1 (0.5 mg* x 11 tablets)
Week 2 (1 mg† x 14 tablets)
PROFESSIONAL SAMPLE – NOT FOR SALE
ALWAYS DISPENSE WITH ENCLOSED MEDICATION GUIDE