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Champix

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Champix uses


WARNING: SERIOUS NEUROPSYCHIATRIC EVENTS

Serious neuropsychiatric events including, but not limited to, depression, suicidal ideation, suicide attempt, and completed suicide have been reported in patients taking Champix. Some reported cases may have been complicated by the symptoms of nicotine withdrawal in patients who stopped smoking. Depressed mood may be a symptom of nicotine withdrawal. Depression, rarely including suicidal ideation, has been reported in smokers undergoing a smoking cessation attempt without medication. However, some of these symptoms have occurred in patients taking Champix who continued to smoke.

All patients being treated with Champix should be observed for neuropsychiatric symptoms including changes in behavior, hostility, agitation, depressed mood, and suicide-related events, including ideation, behavior, and attempted suicide. These symptoms, as well as worsening of pre-existing psychiatric illness and completed suicide, have been reported in some patients attempting to quit smoking while taking Champix in the postmarketing experience. When symptoms were reported, most were during Champix treatment, but some were following discontinuation of Champix therapy.

These events have occurred in patients with and without pre-existing psychiatric disease. Patients with serious psychiatric illness such as schizophrenia, bipolar disorder, and major depressive disorder did not participate in the premarketing studies of Champix, and the safety and efficacy of Champix in such patients has not been established.

Advise patients and caregivers that the patient should stop taking Champix and contact a healthcare provider immediately if agitation, hostility, depressed mood, or changes in behavior or thinking that are not typical for the patient are observed, or if the patient develops suicidal ideation or suicidal behavior. In many postmarketing cases, resolution of symptoms after discontinuation of Champix was reported, although in some cases the symptoms persisted; therefore, ongoing monitoring and supportive care should be provided until symptoms resolve.

The risks of Champix should be weighed against the benefits of its use. Champix has been demonstrated to increase the likelihood of abstinence from smoking for as long as one year compared to treatment with placebo. The health benefits of quitting smoking are immediate and substantial.

WARNING: SERIOUS NEUROPSYCHIATRIC EVENTS

See full prescribing information for complete boxed warning.

Dosage and Administration
Alternative Instructions for Setting a Quit Date (2.1) 7/2011
Warnings and Precautions
Cardiovascular Events (5.4) 7/2011
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1 INDICATIONS AND USAGE

Champix is indicated for use as an aid to smoking cessation treatment.

Champix is a nicotinic receptor partial agonist indicated for use as an aid to smoking cessation treatment. (1 and 2.1)

2 DOSAGE AND ADMINISTRATION

2.1 Usual Dosage for Adults

Smoking cessation therapies are more likely to succeed for patients who are motivated to stop smoking and who are provided additional advice and support. Provide patients with appropriate educational materials and counseling to support the quit attempt.

The patient should set a date to stop smoking. Begin Champix dosing one week before this date. Alternatively, the patient can begin Champix dosing and then quit smoking between days 8 and 35 of treatment.

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

The recommended dose of Champix is 1 mg twice daily following a 1-week titration as follows:

Days 1 – 3: 0.5 mg once daily
Days 4 – 7: 0.5 mg twice daily
Day 8 – end of treatment: 1 mg twice daily

Patients should be treated with Champix for 12 weeks. For patients who have successfully stopped smoking at the end of 12 weeks, an additional course of 12 weeks' treatment with Champix is recommended to further increase the likelihood of long-term abstinence.

Patients who do not succeed in stopping smoking during 12 weeks of initial therapy, or who relapse after treatment, should be encouraged to make another attempt once factors contributing to the failed attempt have been identified and addressed.

Consider a temporary or permanent dose reduction in patients who cannot tolerate the adverse effects of Champix.

2.2 Dosage in Special Populations

Patients with Impaired Renal Function: No dosage adjustment is necessary for patients with mild to moderate renal impairment. For patients with severe renal impairment (estimated creatinine clearance <30 mL/min), the recommended starting dose of Champix is 0.5 mg once daily. The dose may then be titrated as needed to a maximum dose of 0.5 mg twice a day. For patients with end-stage renal disease undergoing hemodialysis, a maximum dose of 0.5 mg once daily may be administered if tolerated .

Elderly and Patients with Impaired Hepatic Function: No dosage adjustment is necessary for patients with hepatic impairment. Because elderly patients are more likely to have decreased renal function, care should be taken in dose selection, and it may be useful to monitor renal function .

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3 DOSAGE FORMS AND STRENGTHS

Capsular, biconvex tablets: 0.5 mg (white to off-white, debossed with "Pfizer" on one side and "CHX 0.5" on the other side) and 1 mg (light blue, debossed with "Pfizer" on one side and "CHX 1.0" on the other side)

Tablets: 0.5 mg and 1 mg (3)

4 CONTRAINDICATIONS

Champix is contraindicated in patients with a known history of serious hypersensitivity reactions or skin reactions to Champix

History of serious hypersensitivity or skin reactions to Champix (4)

5 WARNINGS AND PRECAUTIONS

5.1 Neuropsychiatric Symptoms and Suicidality

Serious neuropsychiatric symptoms have been reported in patients being treated with Champix . These postmarketing reports have included changes in mood (including depression and mania), psychosis, hallucinations, paranoia, delusions, homicidal ideation, hostility, agitation, anxiety, and panic, as well as suicidal ideation, suicide attempt, and completed suicide. Some reported cases may have been complicated by the symptoms of nicotine withdrawal in patients who stopped smoking. Depressed mood may be a symptom of nicotine withdrawal. Depression, rarely including suicidal ideation, has been reported in smokers undergoing a smoking cessation attempt without medication. However, some of these symptoms have occurred in patients taking Champix who continued to smoke. When symptoms were reported, most were during Champix treatment, but some were following discontinuation of Champix therapy.

These events have occurred in patients with and without pre-existing psychiatric disease; some patients have experienced worsening of their psychiatric illnesses. All patients being treated with Champix should be observed for neuropsychiatric symptoms or worsening of pre-existing psychiatric illness. Patients with serious psychiatric illness such as schizophrenia, bipolar disorder, and major depressive disorder did not participate in the premarketing studies of Champix, and the safety and efficacy of Champix in such patients has not been established.

Advise patients and caregivers that the patient should stop taking Champix and contact a healthcare provider immediately if agitation, depressed mood, changes in behavior or thinking that are not typical for the patient are observed, or if the patient develops suicidal ideation or suicidal behavior. In many postmarketing cases, resolution of symptoms after discontinuation of Champix was reported, although in some cases the symptoms persisted, therefore, ongoing monitoring and supportive care should be provided until symptoms resolve.

The risks of Champix should be weighed against the benefits of its use. Champix has been demonstrated to increase the likelihood of abstinence from smoking for as long as one year compared to treatment with placebo. The health benefits of quitting smoking are immediate and substantial.

5.2 Angioedema and Hypersensitivity Reactions

There have been postmarketing reports of hypersensitivity reactions including angioedema in patients treated with Champix . Clinical signs included swelling of the face, mouth (tongue, lips, and gums), extremities, and neck (throat and larynx). There were infrequent reports of life-threatening angioedema requiring emergent medical attention due to respiratory compromise. Instruct patients to discontinue Champix and immediately seek medical care if they experience these symptoms.

5.3 Serious Skin Reactions

There have been postmarketing reports of rare but serious skin reactions, including Stevens-Johnson Syndrome and erythema multiforme, in patients using Champix . As these skin reactions can be life-threatening, instruct patients to stop taking Champix and contact a healthcare provider immediately at the first appearance of a skin rash with mucosal lesions or any other signs of hypersensitivity.

5.4 Cardiovascular Events

In a controlled clinical trial of Champix administered to patients with stable cardiovascular disease, with approximately 350 patients per treatment arm, certain cardiovascular events were reported more frequently in patients treated with Champix than in patients treated with placebo . These included treatment-emergent events (on-treatment or 30 days after treatment) of angina pectoris (13 patients in the varenicline arm vs. 7 in the placebo arm), and the serious cardiovascular events of nonfatal MI (4 vs. 1) and nonfatal stroke (2 vs. 0). During non-treatment follow up to 52 weeks, serious cardiovascular events included nonfatal myocardial infarction (3 vs. 2), need for coronary revascularization (7 vs. 2), hospitalization for angina pectoris (6 vs. 4), transient ischemic attack (1 vs. 0), new diagnosis of peripheral vascular disease (PVD) or admission for a PVD procedure (5 vs. 2). Serious cardiovascular events occurring over the 52 weeks of the study (treatment emergent and non-treatment emergent) were adjudicated by an independent blinded committee. Champix was not studied in patients with unstable cardiovascular disease or cardiovascular events occurring within two months before screening. Patients should be advised to notify a health care provider of new or worsening symptoms of cardiovascular disease. The risks of Champix should be weighed against the benefits of its use in smokers with cardiovascular disease. Smoking is an independent and major risk factor for cardiovascular disease. Champix has been demonstrated to increase the likelihood of abstinence from smoking for as long as one year compared to treatment with placebo.

5.5 Accidental Injury

There have been postmarketing reports of traffic accidents, near-miss incidents in traffic, or other accidental injuries in patients taking Champix. In some cases, the patients reported somnolence, dizziness, loss of consciousness or difficulty concentrating that resulted in impairment, or concern about potential impairment, in driving or operating machinery. Advise patients to use caution driving or operating machinery or engaging in other potentially hazardous activities until they know how Champix may affect them.

5.6 Nausea

Nausea was the most common adverse reaction reported with Champix treatment. Nausea was generally described as mild or moderate and often transient; however, for some patients, it was persistent over several months. The incidence of nausea was dose-dependent. Initial dose-titration was beneficial in reducing the occurrence of nausea. For patients treated to the maximum recommended dose of 1 mg twice daily following initial dosage titration, the incidence of nausea was 30% compared with 10% in patients taking a comparable placebo regimen. In patients taking Champix 0.5 mg twice daily following initial titration, the incidence was 16% compared with 11% for placebo. Approximately 3% of patients treated with Champix 1 mg twice daily in studies involving 12 weeks of treatment discontinued treatment prematurely because of nausea. For patients with intolerable nausea, a dose reduction should be considered.

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6 ADVERSE REACTIONS

The following serious adverse reactions were reported in postmarketing experience and are discussed in greater detail in other sections of the labeling:


In the placebo-controlled studies, the most common adverse events associated with Champix (>5% and twice the rate seen in placebo-treated patients) were nausea, abnormal (vivid, unusual, or strange) dreams, constipation, flatulence, and vomiting.

The treatment discontinuation rate due to adverse events in patients dosed with 1 mg twice daily was 12% for Champix, compared to 10% for placebo in studies of three months' treatment. In this group, the discontinuation rates that are higher than placebo for the most common adverse events in CHANTIX-treated patients were as follows: nausea (3% vs. 0.5% for placebo), insomnia (1.2% vs. 1.1% for placebo), and abnormal dreams (0.3% vs. 0.2% for placebo).

Smoking cessation, with or without treatment, is associated with nicotine withdrawal symptoms and has also been associated with the exacerbation of underlying psychiatric illness.

Most common adverse reactions (>5% and twice the rate seen in placebo-treated patients) were nausea, abnormal (e.g., vivid, unusual, or strange) dreams, constipation, flatulence, and vomiting. (6.1)

To report SUSPECTED ADVERSE REACTIONS, contact Pfizer Inc at 1-800-438-1985 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.

6.1 Clinical Trials Experience

Because clinical trials are conducted under widely varying conditions, the adverse reactions rates observed in the clinical studies of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in clinical practice.

During the premarketing development of Champix, over 4500 subjects were exposed to Champix, with over 450 treated for at least 24 weeks and approximately 100 for a year. Most study participants were treated for 12 weeks or less.

The most common adverse event associated with Champix treatment is nausea, occurring in 30% of patients treated at the recommended dose, compared with 10% in patients taking a comparable placebo regimen .

Table 1 shows the adverse events for Champix and placebo in the 12-week fixed dose studies with titration in the first week [Studies 2 (titrated arm only), 4, and 5]. Adverse events were categorized using the Medical Dictionary for Regulatory Activities (MedDRA, Version 7.1).

MedDRA High Level Group Terms (HLGT) reported in ≥ 5% of patients in the Champix 1 mg twice daily dose group, and more commonly than in the placebo group, are listed, along with subordinate Preferred Terms (PT) reported in ≥ 1% of Champix patients (and at least 0.5% more frequent than placebo). Closely related Preferred Terms such as 'Insomnia', 'Initial insomnia', 'Middle insomnia', 'Early morning awakening' were grouped, but individual patients reporting two or more grouped events are only counted once.

SYSTEM ORGAN CLASS

High Level Group Term

Preferred Term

 Champix

0.5 mg BID

N=129

 Champix

1 mg BID

N=821

 Placebo

N=805
GASTROINTESTINAL (GI)
GI Signs and Symptoms
Nausea 16 30 10
Abdominal Pain Includes PTs Abdominal (pain, pain upper, pain lower, discomfort, tenderness, distension) and Stomach discomfort 5 7 5
Flatulence 9 6 3
Dyspepsia 5 5 3
Vomiting 1 5 2
GI Motility/Defecation Conditions
Constipation 5 8 3
Gastroesophageal reflux disease 1 1 0
Salivary Gland Conditions
Dry mouth 4 6 4
PSYCHIATRIC DISORDERS
Sleep

Disorder/Disturbances
Insomnia Includes PTs Insomnia/Initial insomnia/Middle insomnia/Early morning awakening 19 18 13
Abnormal dreams 9 13 5
Sleep disorder 2 5 3
Nightmare 2 1 0
NERVOUS SYSTEM
Headaches
Headache 19 15 13
Neurological Disorders

NEC
Dysgeusia 8 5 4
Somnolence 3 3 2
Lethargy 2 1 0
GENERAL DISORDERS
General Disorders NEC
Fatigue/Malaise/Asthenia 4 7 6
RESPIR/THORACIC/MEDIAST
Respiratory Disorders NEC
Rhinorrhea 0 1 0
Dyspnea 2 1 1
Upper Respiratory Tract Disorder 7 5 4
SKIN/SUBCUTANEOUS TISSUE
Epidermal and Dermal Conditions
Rash 1 3 2
Pruritis 0 1 1
METABOLISM & NUTRITION
Appetite/General Nutrit. Disorders
Increased appetite 4 3 2
Decreased appetite/Anorexia 1 2 1

The overall pattern and frequency of adverse events during the longer-term trials was similar to those described in Table 1, though several of the most common events were reported by a greater proportion of patients with long-term use (e.g., nausea was reported in 40% of patients treated with Champix 1 mg twice daily in a one-year study, compared to 8% of placebo-treated patients).

Following is a list of treatment-emergent adverse events reported by patients treated with Champix during all clinical trials. The listing does not include those events already listed in the previous tables or elsewhere in labeling, those events for which a drug cause was remote, those events which were so general as to be uninformative, and those events reported only once which did not have a substantial probability of being acutely life-threatening.

Blood and Lymphatic System Disorders. Infrequent: anemia, lymphadenopathy. Rare: leukocytosis, splenomegaly, thrombocytopenia.

Cardiac Disorders. Infrequent: angina pectoris, arrhythmia, bradycardia, myocardial infarction, palpitations, tachycardia, ventricular extrasystoles. Rare: acute coronary syndrome, atrial fibrillation, cardiac flutter, cor pulmonale, coronary artery disease.

Ear and Labyrinth Disorders. Infrequent: tinnitus, vertigo. Rare: deafness, Meniere's disease.

Endocrine Disorders. Infrequent: thyroid gland disorders.

Eye Disorders. Infrequent: conjunctivitis, dry eye, eye irritation, eye pain, vision blurred, visual disturbance. Rare: acquired night blindness, blindness transient, cataract subcapsular, ocular vascular disorder, photophobia, vitreous floaters.

Gastrointestinal Disorders. Frequent: diarrhea. Infrequent: dysphagia, enterocolitis, eructation, esophagitis, gastritis, gastrointestinal hemorrhage, mouth ulceration. Rare: gastric ulcer, intestinal obstruction, pancreatitis acute.

General Disorders and Administration Site Conditions. Frequent: chest pain, edema, influenza-like illness. Infrequent: chest discomfort, chills, pyrexia.

Hepatobiliary Disorders. Infrequent: gall bladder disorder.

Investigations. Frequent: liver function test abnormal, weight increased. Infrequent: electrocardiogram abnormal, muscle enzyme increased, urine analysis abnormal.

Metabolism and Nutrition Disorders. Infrequent: diabetes mellitus, hyperlipidemia, hypokalemia. Rare: hypoglycemia.

Musculoskeletal and Connective Tissue Disorders. Frequent: arthralgia, back pain, muscle cramp, musculoskeletal pain, myalgia. Infrequent: arthritis, osteoporosis. Rare: myositis.

Nervous System Disorders. Frequent: disturbance in attention, dizziness, sensory disturbance. Infrequent: amnesia, migraine, parosmia, psychomotor hyperactivity, restless legs syndrome, syncope, tremor. Rare: balance disorder, cerebrovascular accident, convulsion, dysarthria, facial palsy, mental impairment, multiple sclerosis, nystagmus, psychomotor skills impaired, transient ischemic attack, visual field defect.

Psychiatric Disorders. Infrequent: disorientation, dissociation, libido decreased, mood swings, thinking abnormal. Rare: bradyphrenia, euphoric mood.

Renal and Urinary Disorders. Frequent: polyuria. Infrequent: nephrolithiasis, nocturia, urethral syndrome, urine abnormality. Rare: renal failure acute, urinary retention.

Reproductive System and Breast Disorders. Rare: sexual dysfunction. Frequent: menstrual disorder. Infrequent: erectile dysfunction.

Respiratory, Thoracic and Mediastinal Disorders. Frequent: epistaxis, respiratory disorders. Infrequent: asthma. Rare: pleurisy, pulmonary embolism.

Skin and Subcutaneous Tissue Disorders. Frequent: hyperhidrosis. Infrequent: acne, dry skin, eczema, erythema, psoriasis, urticaria. Rare: photosensitivity reaction.

Vascular Disorders. Frequent: hot flush. Infrequent: thrombosis.

Champix has also been studied in a trial conducted in patients with stable cardiovascular disease, a trial conducted in patients with chronic obstructive pulmonary disease (COPD) and a trial conducted in generally healthy patients (similar to those in the premarketing studies) in which they were allowed to select a quit date between days 8 and 35 of treatment ("alternative quit date instruction trial").

In the trial of patients with stable cardiovascular disease, more types and a greater number of cardiovascular events were reported compared to premarketing studies. Treatment-emergent (on-treatment or 30 days after treatment) cardiovascular events reported with a frequency ≥ 1% in either treatment group in this study were angina pectoris (3.7% and 2.0% for varenicline and placebo, respectively), chest pain (2.5% vs. 2.3%), peripheral edema (2.0% vs. 1.1%), hypertension (1.4% vs. 2.6%), and palpitations (0.6 % vs. 1.1%). Deaths and serious cardiovascular events occurring over the 52 weeks of the study (treatment emergent and non-treatment emergent) were adjudicated by a blinded, independent committee. The following treatment-emergent adjudicated events occurred with a frequency ≥1% in either treatment group: nonfatal MI (1.1% vs. 0.3% for varenicline and placebo, respectively), and hospitalization for angina pectoris (0.6% vs. 1.1%). During non-treatment follow up to 52 weeks, the adjudicated events included need for coronary revascularization (2.0% vs. 0.6%), hospitalization for angina pectoris (1.7% vs. 1.1%), and new diagnosis of peripheral vascular disease (PVD) or admission for a PVD procedure (1.4% vs. 0.6%). Some of the patients requiring coronary revascularization underwent the procedure as part of management of nonfatal MI and hospitalization for angina. Cardiovascular death occurred in 0.3% of patients in the varenicline arm and 0.6% of patients in the placebo arm over the course of the 52-week study.

Adverse events in the trial of patients with COPD and in the alternative quit date instruction trial were quantitatively and qualitatively similar to those observed in premarketing studies.

6.2 Postmarketing Experience

The following adverse events have been reported during post-approval use of Champix. Because these events are reported voluntarily from a population of uncertain size, it is not possible to reliably estimate their frequency or establish a causal relationship to drug exposure.

There have been reports of depression, mania, psychosis, hallucinations, paranoia, delusions, homicidal ideation, aggression, hostility, anxiety, and panic, as well as suicidal ideation, suicide attempt, and completed suicide in patients attempting to quit smoking while taking Champix . Smoking cessation with or without treatment is associated with nicotine withdrawal symptoms and the exacerbation of underlying psychiatric illness. Not all patients had known pre-existing psychiatric illness and not all had discontinued smoking.

There have been reports of hypersensitivity reactions, including angioedema .

There have also been reports of serious skin reactions, including Stevens-Johnson Syndrome and erythema multiforme, in patients taking Champix .

There have been reports of myocardial infarction (MI) and cerebrovascular accident (CVA) including ischemic and hemorrhagic events in patients taking Champix. In the majority of the reported cases, patients had pre-existing cardiovascular disease and/or other risk factors. Although smoking is a risk factor for MI and CVA, based on temporal relationship between medication use and events, a contributory role of varenicline cannot be ruled out.

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7 DRUG INTERACTIONS

Based on varenicline characteristics and clinical experience to date, Champix has no clinically meaningful pharmacokinetic drug interactions .

7.1 Use With Other Drugs for Smoking Cessation

Safety and efficacy of Champix in combination with other smoking cessation therapies have not been studied.

Bupropion : Varenicline (1 mg twice daily) did not alter the steady-state pharmacokinetics of bupropion (150 mg twice daily) in 46 smokers. The safety of the combination of bupropion and varenicline has not been established.

Nicotine replacement therapy (NRT ): Although co-administration of varenicline (1 mg twice daily) and transdermal nicotine (21 mg/day) for up to 12 days did not affect nicotine pharmacokinetics, the incidence of nausea, headache, vomiting, dizziness, dyspepsia, and fatigue was greater for the combination than for NRT alone. In this study, eight of twenty-two (36%) patients treated with the combination of varenicline and NRT prematurely discontinued treatment due to adverse events, compared to 1 of 17 (6%) of patients treated with NRT and placebo.

7.2 Effect of Smoking Cessation on Other Drugs

Physiological changes resulting from smoking cessation, with or without treatment with Champix, may alter the pharmacokinetics or pharmacodynamics of certain drugs (e.g., theophylline, warfarin, insulin) for which dosage adjustment may be necessary.

8 USE IN SPECIFIC POPULATIONS

8.1 Pregnancy

Pregnancy Category C.

There are no adequate and well-controlled studies of Champix use in pregnant women. In animal studies, Champix caused decreased fetal weights, increased auditory startle response, and decreased fertility in offspring. Champix should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

In reproductive and developmental toxicity studies, pregnant rats and rabbits received varenicline succinate during organogenesis at oral doses up to 15 and 30 mg/kg/day, respectively. These exposures were 36 (rats) and 50 (rabbits) times the human exposure (based on AUC) at the maximum recommended human dose (MRHD) of 1 mg twice daily. While no fetal structural abnormalities occurred in either species, reduced fetal weights occurred in rabbits at the highest dose (exposures 50 times the human exposure at the MRHD based on AUC). Fetal weight reduction did not occur at animal exposures 23 times the human exposure at the MRHD based on AUC.

In a pre- and postnatal development study, pregnant rats received up to 15 mg/kg/day of oral varenicline succinate from organogenesis through lactation. These resulted in exposures up to 36 times the human exposure (based on AUC) at the MRHD of 1 mg twice daily. Decreased fertility and increased auditory startle response occurred in offspring.

8.3 Nursing Mothers

It is not known whether Champix is excreted in human milk. In animal studies varenicline was excreted in milk of lactating animals. Because many drugs are excreted in human milk and because of the potential for serious adverse reactions in nursing infants from Champix, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.

8.4 Pediatric Use

Safety and effectiveness of Champix in pediatric patients have not been established.

8.5 Geriatric Use

A combined single- and multiple-dose pharmacokinetic study demonstrated that the pharmacokinetics of 1 mg varenicline given once daily or twice daily to 16 healthy elderly male and female smokers for 7 consecutive days was similar to that of younger subjects. No overall differences in safety or effectiveness were observed between these subjects and younger subjects, and other reported clinical experience has not identified differences in responses between the elderly and younger patients, but greater sensitivity of some older individuals cannot be ruled out.

Varenicline is known to be substantially excreted by the kidney, and the risk of toxic reactions to this drug may be greater in patients with impaired renal function. Because elderly patients are more likely to have decreased renal function, care should be taken in dose selection, and it may be useful to monitor renal function [see Dosage and Administration (2.2) ].

No dosage adjustment is recommended for elderly patients.

8.6 Renal Impairment

Varenicline is substantially eliminated by renal glomerular filtration along with active tubular secretion. Dose reduction is not required in patients with mild to moderate renal impairment. For patients with severe renal impairment (estimated creatinine clearance <30 mL/min), and for patients with end-stage renal disease undergoing hemodialysis, dosage adjustment is needed. .

9 DRUG ABUSE AND DEPENDENCE

9.1 Controlled Substance

Varenicline is not a controlled substance.

9.3 Dependence

Humans : Fewer than 1 out of 1000 patients reported euphoria in clinical trials with Champix. At higher doses (greater than 2 mg), Champix produced more frequent reports of gastrointestinal disturbances such as nausea and vomiting. There is no evidence of dose-escalation to maintain therapeutic effects in clinical studies, which suggests that tolerance does not develop. Abrupt discontinuation of Champix was associated with an increase in irritability and sleep disturbances in up to 3% of patients. This suggests that, in some patients, varenicline may produce mild physical dependence which is not associated with addiction.

In a human laboratory abuse liability study, a single oral dose of 1 mg varenicline did not produce any significant positive or negative subjective responses in smokers. In non-smokers, 1 mg varenicline produced an increase in some positive subjective effects, but this was accompanied by an increase in negative adverse effects, especially nausea. A single oral dose of 3 mg varenicline uniformly produced unpleasant subjective responses in both smokers and non-smokers.

Animals : Studies in rodents have shown that varenicline produces behavioral responses similar to those produced by nicotine. In rats trained to discriminate nicotine from saline, varenicline produced full generalization to the nicotine cue. In self-administration studies, the degree to which varenicline substitutes for nicotine is dependent upon the requirement of the task. Rats trained to self-administer nicotine under easy conditions continued to self-administer varenicline to a degree comparable to that of nicotine; however in a more demanding task, rats self-administered varenicline to a lesser extent than nicotine. Varenicline pretreatment also reduced nicotine self-administration.

10 OVERDOSAGE

In case of overdose, standard supportive measures should be instituted as required.

Varenicline has been shown to be dialyzed in patients with end stage renal disease , however, there is no experience in dialysis following overdose.

11 DESCRIPTION

Champix 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. Champix has a molecular weight of 361.35 Daltons, and a molecular formula of C13H13N3 - C4H6O6. The chemical structure is:

Champix 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 Champix tablet contains 0.85 mg of Champix equivalent to 0.5 mg of varenicline free base; each 1mg Champix tablet contains 1.71 mg of Champix 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.

Chemical Structure

12 CLINICAL PHARMACOLOGY

12.1 Mechanism of Action

Varenicline binds with high affinity and selectivity at α4β2 neuronal nicotinic acetylcholine receptors. The efficacy of Champix 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, or to non-nicotinic receptors and transporters (>2000-fold). Varenicline also binds with moderate affinity (Ki = 350 nM) to the 5-HT3 receptor.

12.3 Pharmacokinetics

Absorption/Distribution : Maximum plasma concentrations of varenicline occur typically within 3–4 hours after oral administration. Following administration of multiple oral doses of varenicline, steady-state conditions were reached within 4 days. Over the recommended dosing range, varenicline exhibits linear pharmacokinetics after single or repeated doses. In a mass balance study, absorption of varenicline was virtually complete after oral administration and systemic availability was ~90%. Oral bioavailability of varenicline is unaffected by food or time-of-day dosing. Plasma protein binding of varenicline is low (≤20%) and independent of both age and renal function.

Metabolism/Elimination : The elimination half-life of varenicline is approximately 24 hours. Varenicline undergoes minimal metabolism, with 92% excreted unchanged in the urine. Renal elimination of varenicline is primarily through glomerular filtration along with active tubular secretion possibly via the organic cation transporter, OCT2.

Pharmacokinetics in Special Patient Populations : There are no clinically meaningful differences in varenicline pharmacokinetics due to age, race, gender, smoking status, or use of concomitant medications, as demonstrated in specific pharmacokinetic studies and in population pharmacokinetic analyses.

Renal Impairment: Varenicline pharmacokinetics were unchanged in subjects with mild renal impairment (estimated creatinine clearance >50 mL/min and ≤80 mL/min). In subjects with moderate renal impairment (estimated creatinine clearance ≥30 mL/min and ≤50 mL/min), varenicline exposure increased 1.5-fold compared with subjects with normal renal function (estimated creatinine clearance >80 mL/min). In subjects with severe renal impairment (estimated creatinine clearance <30 mL/min), varenicline exposure was increased 2.1-fold. In subjects with end-stage-renal disease (ESRD) undergoing a three-hour session of hemodialysis for three days a week, varenicline exposure was increased 2.7-fold following 0.5 mg once daily administration for 12 days. The plasma Cmax and AUC of varenicline noted in this setting were similar to those of healthy subjects receiving 1 mg twice daily. . Additionally, in subjects with ESRD, varenicline was efficiently removed by hemodialysis .

Geriatric Patients: A combined single- and multiple-dose pharmacokinetic study demonstrated that the pharmacokinetics of 1 mg varenicline given once daily or twice daily to 16 healthy elderly male and female smokers (aged 65–75 yrs) for 7 consecutive days was similar to that of younger subjects.

Pediatric Patients: Because the safety and effectiveness of Champix in pediatric patients have not been established, Champix is not recommended for use in patients under 18 years of age. Single and multiple-dose pharmacokinetics of varenicline have been investigated in pediatric patients aged 12 to 17 years old (inclusive) and were approximately dose-proportional over the 0.5 mg to 2 mg daily dose range studied. Steady-state systemic exposure in adolescent patients of bodyweight >55 kg, as assessed by AUC (0–24), was comparable to that noted for the same doses in the adult population. When 0.5 mg BID was given, steady-state daily exposure of varenicline was, on average, higher (by approximately 40%) in adolescent patients with bodyweight ≤ 55 kg compared to that noted in the adult population.

Hepatic Impairment: Due to the absence of significant hepatic metabolism, varenicline pharmacokinetics should be unaffected in patients with hepatic impairment.

Drug-Drug Interactions : Drug interaction studies were performed with varenicline and digoxin, warfarin, transdermal nicotine, bupropion, cimetidine, and metformin. No clinically meaningful pharmacokinetic drug-drug interactions have been identified.

In vitro studies demonstrated that varenicline does not inhibit the following cytochrome P450 enzymes (IC50 >6400 ng/mL): 1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1, and 3A4/5. Also, in human hepatocytes in vitro, varenicline does not induce the cytochrome P450 enzymes 1A2 and 3A4.

In vitro studies demonstrated that varenicline does not inhibit human renal transport proteins at therapeutic concentrations. Therefore, drugs that are cleared by renal secretion (e.g., metformin ) are unlikely to be affected by varenicline.

In vitro studies demonstrated the active renal secretion of varenicline is mediated by the human organic cation transporter OCT2. Co-administration with inhibitors of OCT2 (e.g., cimeditine ) may not necessitate a dose adjustment of Champix as the increase in systemic exposure to Champix is not expected to be clinically meaningful. Furthermore, since metabolism of varenicline represents less than 10% of its clearance, drugs known to affect the cytochrome P450 system are unlikely to alter the pharmacokinetics of Champix [ see Clinical Pharmacology (12.3)]; therefore, a dose adjustment of Champix would not be required.

Metformin: When co-administered to 30 smokers, varenicline (1 mg twice daily) did not alter the steady-state pharmacokinetics of metformin (500 mg twice daily), which is a substrate of OCT2. Metformin had no effect on varenicline steady-state pharmacokinetics.

Cimetidine: Co-administration of an OCT2 inhibitor, cimetidine (300 mg four times daily), with varenicline (2 mg single dose) to 12 smokers increased the systemic exposure of varenicline by 29% (90% CI: 21.5%, 36.9%) due to a reduction in varenicline renal clearance.

Digoxin: Varenicline (1 mg twice daily) did not alter the steady-state pharmacokinetics of digoxin administered as a 0.25 mg daily dose in 18 smokers.

Warfarin: Varenicline (1 mg twice daily) did not alter the pharmacokinetics of a single 25 mg dose of (R, S)-warfarin in 24 smokers. Prothrombin time (INR) was not affected by varenicline. Smoking cessation itself may result in changes to warfarin pharmacokinetics .

Use with Other Drugs for Smoking Cessation:

Bupropion: Varenicline (1 mg twice daily) did not alter the steady-state pharmacokinetics of bupropion (150 mg twice daily) in 46 smokers .

Nicotine replacement therapy (NRT): Although co-administration of varenicline (1 mg twice daily) and transdermal nicotine (21 mg/day) for up to 12 days did not affect nicotine pharmacokinetics, the incidence of adverse reactions was greater for the combination than for NRT alone [see Drug Interactions (7.1) ].

13 NONCLINICAL TOXICOLOGY

13.1 Carcinogenesis, Mutagenesis, Impairment of Fertility

Carcinogenesis : Lifetime carcinogenicity studies were performed in CD-1 mice and Sprague-Dawley rats. There was no evidence of a carcinogenic effect in mice administered varenicline by oral gavage for 2 years at doses up to 20 mg/kg/day (47 times the maximum recommended human daily exposure based on AUC). Rats were administered varenicline (1, 5, and 15 mg/kg/day) by oral gavage for 2 years. In male rats (n = 65 per sex per dose group), incidences of hibernoma (tumor of the brown fat) were increased at the mid dose (1 tumor, 5 mg/kg/day, 23 times the maximum recommended human daily exposure based on AUC) and maximum dose (2 tumors, 15 mg/kg/day, 67 times the maximum recommended human daily exposure based on AUC). The clinical relevance of this finding to humans has not been established. There was no evidence of carcinogenicity in female rats.

Mutagenesis : Varenicline was not genotoxic, with or without metabolic activation, in the following assays: Ames bacterial mutation assay; mammalian CHO/HGPRT assay; and tests for cytogenetic aberrations in vivo in rat bone marrow and in vitro in human lymphocytes.

Impairment of Fertility : There was no evidence of impairment of fertility in either male or female Sprague-Dawley rats administered varenicline succinate up to 15 mg/kg/day (67 and 36 times, respectively, the maximum recommended human daily exposure based on AUC at 1 mg twice daily). However, a decrease in fertility was noted in the offspring of pregnant rats who were administered varenicline succinate at an oral dose of 15 mg/kg/day (36 times the maximum recommended human daily exposure based on AUC at 1 mg twice daily. This decrease in fertility in the offspring of treated female rats was not evident at an oral dose of 3 mg/kg/day (9 times the maximum recommended human daily exposure based on AUC at 1 mg twice daily).

14 CLINICAL STUDIES

The efficacy of Champix in smoking cessation was demonstrated in six clinical trials in which a total of 3659 chronic cigarette smokers were treated with Champix. In all clinical studies, abstinence from smoking was determined by patient self-report and verified by measurement of exhaled carbon monoxide (CO≤10 ppm) at weekly visits. Among the CHANTIX-treated patients enrolled in these studies, the completion rate was 65%. Except for the dose-ranging study (Study 1) and the maintenance of abstinence study (Study 6), patients were treated for 12 weeks and then were followed for 40 weeks post-treatment. Most patients enrolled in these trials were white (79–96%). All studies enrolled almost equal numbers of men and women. The average age of patients in these studies was 43 years. Patients on average had smoked about 21 cigarettes per day for an average of approximately 25 years. Patients set a date to stop smoking (target quit date) with dosing starting 1 week before this date.

Three additional studies were conducted in patients with cardiovascular disease, in patients with chronic obstructive pulmonary disease , and in patients instructed to select their quit date within days 8 and 35 of treatment .

In all studies, patients were provided with an educational booklet on smoking cessation and received up to 10 minutes of smoking cessation counseling at each weekly treatment visit according to Agency for Healthcare Research and Quality guidelines.

14.1 Initiation of Abstinence

Study 1 : This was a six-week dose-ranging study comparing Champix to placebo. This study provided initial evidence that Champix at a total dose of 1 mg per day or 2 mg per day was effective as an aid to smoking cessation.

Study 2 : This study of 627 patients compared Champix 1 mg per day and 2 mg per day with placebo. Patients were treated for 12 weeks (including one week titration) and then were followed for 40 weeks post-treatment. Champix was given in two divided doses daily. Each dose of Champix was given in two different regimens, with and without initial dose titration, to explore the effect of different dosing regimens on tolerability. For the titrated groups, dosage was titrated up over the course of one week, with full dosage achieved starting with the second week of dosing. The titrated and nontitrated groups were pooled for efficacy analysis.

Forty-five percent of patients receiving Champix 1 mg per day (0.5 mg twice daily) and 51% of patients receiving 2 mg per day (1 mg twice daily) had CO-confirmed continuous abstinence during weeks 9 through 12 compared to 12% of patients in the placebo group (Figure 1). In addition, 31% of the 1 mg per day group and 31% of the 2 mg per day group were continuously abstinent from one week after TQD through the end of treatment as compared to 8% of the placebo group.

Study 3 : This flexible-dosing study of 312 patients examined the effect of a patient-directed dosing strategy of Champix or placebo. After an initial one-week titration to a dose of 0.5 mg twice daily, patients could adjust their dosage as often as they wished between 0.5 mg once daily to 1 mg twice daily per day. Sixty-nine percent of patients titrated to the maximum allowable dose at any time during the study. For 44% of patients, the modal dose selected was 1 mg twice daily; for slightly over half of the study participants, the modal dose selected was 1 mg/day or less.

Of the patients treated with Champix, 40% had CO-confirmed continuous abstinence during weeks 9 through 12 compared to 12% in the placebo group. In addition, 29% of the Champix group were continuously abstinent from one week after TQD through the end of treatment as compared to 9% of the placebo group.

Study 4 and Study 5 : These identical double-blind studies compared Champix 2 mg per day, bupropion sustained-release (SR) 150 mg twice daily, and placebo. Patients were treated for 12 weeks and then were followed for 40 weeks post-treatment. The Champix dosage of 1 mg twice daily was achieved using a titration of 0.5 mg once daily for the initial 3 days followed by 0.5 mg twice daily for the next 4 days. The bupropion SR dosage of 150 mg twice daily was achieved using a 3-day titration of 150 mg once daily. Study 4 enrolled 1022 patients and Study 5 enrolled 1023 patients. Patients inappropriate for bupropion treatment or patients who had previously used bupropion were excluded.

In Study 4, patients treated with Champix had a superior rate of CO-confirmed abstinence during weeks 9 through 12 (44%) compared to patients treated with bupropion SR (30%) or placebo (17%). The bupropion SR quit rate was also superior to placebo. In addition, 29% of the Champix group were continuously abstinent from one week after TQD through the end of treatment as compared to 12% of the placebo group and 23% of the bupropion SR group.

Similarly in Study 5, patients treated with Champix had a superior rate of CO-confirmed abstinence during weeks 9 through 12 (44%) compared to patients treated with bupropion SR (30%) or placebo (18%). The bupropion SR quit rate was also superior to placebo. In addition, 29% of the Champix group were continuously abstinent from one week after TQD through the end of treatment as compared to 11% of the placebo group and 21% of the bupropion SR group.

Figure 1: Continuous Abstinence, Weeks 9 through 12

Champix

0.5 mg BID

 Champix

1 mg BID

 Champix

Flexible

 Bupropion

SR

 Placebo
BID = twice daily
Study 2 45%

(39%, 51%)

 51%

(44%, 57%)

 12%

(6%, 18%)
Study 3 40%

(32%, 48%)

 12%

(7%, 17%)
Study 4 44%

(38%, 49%)

 30%

(25%, 35%)

 17%

(13%, 22%)
Study 5 44%

(38%, 49%)

 30%

(25%, 35%)

 18%

(14%, 22%)
Figure 1

14.2 Urge to Smoke

Based on responses to the Brief Questionnaire of Smoking Urges and the Minnesota Nicotine Withdrawal scale "urge to smoke" item, Champix reduced urge to smoke compared to placebo.

14.3 Long-Term Abstinence

Studies 1 through 5 included 40 weeks of post-treatment follow-up. In each study, CHANTIX-treated patients were more likely to maintain abstinence throughout the follow-up period than were patients treated with placebo.

Figure 2: Continuous Abstinence, Weeks 9 through 52

Champix

0.5 mg BID

 Champix

1 mg BID

 Champix

Flexible

 Bupropion

SR

 Placebo
BID = twice daily
Study 2 19%

(14%, 24%)

 23%

(18%, 28%)

 4%

(1%, 8%)
Study 3 22%

(16%, 29%)

 8%

(3%, 12%)
Study 4 21%

(17%, 26%)

 16%

(12%, 20%)

 8%

(5%, 11%)
Study 5 22%

(17%, 26%)

 14%

(11%, 18%)

 10%

(7%, 13%)
Figure 2

Study 6 : This study assessed the effect of an additional 12 weeks of Champix therapy on the likelihood of long-term abstinence. Patients in this study (n=1927) were treated with open-label Champix 1 mg twice daily for 12 weeks. Patients who had stopped smoking for at least a week by Week 12 (n=1210) were then randomized to double-blind treatment with Champix (1 mg twice daily) or placebo for an additional 12 weeks and then followed for 28 weeks post-treatment.

The continuous abstinence rate from Week 13 through Week 24 was higher for patients continuing treatment with Champix (70%) than for patients switching to placebo (50%). Superiority to placebo was also maintained during 28 weeks post-treatment follow-up (CHANTIX 54% versus placebo 39%).

In Figure 3 below, the x-axis represents the study week for each observation, allowing a comparison of groups at similar times after discontinuation of Champix; post-CHANTIX follow-up begins at Week 13 for the placebo group and Week 25 for the Champix group. The y-axis represents the percentage of patients who had been abstinent for the last week of Champix treatment and remained abstinent at the given timepoint.

Figure 3: Continuous Abstinence Rate during Nontreatment Follow-Up

Figure 3

14.4 Subjects with Cardiovascular and Chronic Obstructive Pulmonary Disease

Champix was evaluated in a randomized, double-blind, placebo-controlled study of subjects aged 35 to 75 years with stable, documented cardiovascular disease (diagnoses other than, or in addition to, hypertension) that had been diagnosed for more than 2 months. Subjects were randomized to Champix 1 mg twice daily (n=353) or placebo (n=350) for a treatment of 12 weeks and then were followed for 40 weeks post-treatment. Subjects treated with Champix had a superior rate of CO-confirmed abstinence during weeks 9 through 12 (47%) compared to subjects treated with placebo (14%) and from week 9 through 52 (20%) compared to subjects treated with placebo (7%).

Champix was evaluated in a randomized, double-blind, placebo-controlled study of subjects aged ≥ 35 years with mild-to-moderate COPD with post-bronchodilator FEV1/FVC <70% and FEV1 ≥ 50% of predicted normal value. Subjects were randomized to Champix 1 mg twice daily (N=223) or placebo (N=237) for a treatment of 12 weeks and then were followed for 40 weeks post-treatment. Subjects treated with Champix had a superior rate of CO-confirmed abstinence during weeks 9 through 12 (41%) compared to subjects treated with placebo (9%) and from week 9 through 52 (19%) compared to subjects treated with placebo (6%).

Weeks 9 through 12 Weeks 9 through 52
Champix

1 mg BID

 Placebo Champix

1 mg BID

 Placebo
BID = twice daily
CVD Study 47%

(42%, 53%)

 14%

(11%, 18%)

 20%

(16%, 24%)

 7%

(5%, 10%)
COPD Study 41%

(34%, 47%)

 9%

(6%, 13%)

 19%

(14%, 24%)

 6%

(3%, 9%)

14.5 Alternative Instructions for Setting a Quit Date

Champix was evaluated in a double-blind, placebo-controlled trial where patients were instructed to select a target quit date between Day 8 and Day 35 of treatment. Subjects were randomized 3:1 to Champix 1 mg twice daily (N=486) or placebo (N=165) for 12 weeks of treatment and followed for another 12 weeks post-treatment. Patients treated with Champix had a superior rate of CO-confirmed abstinence during weeks 9 through 12 (54%) compared to patients treated with placebo (19%) and from weeks 9 through 24 (35%) compared to subjects treated with placebo (13%).

16 HOW SUPPLIED/STORAGE AND HANDLING

Champix 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. Champix is supplied in the following package configurations:

Description NDC
Packs Starting Month PAK

(First month of therapy):

Pack includes 1 card of 0.5 mg x 11 tablets and 3 cards of 1 mg x 14 tablets

 NDC 0069-0471-97
Continuing Month PAK

(Continuing months of therapy):

Pack includes 4 cards of 1 mg x 14 tablets

 NDC 0069-0469-97
Starting Month Box: 0.5 mg x 11 tablets and 1 mg x 42 tablets NDC 0069-0471-02
Continuing Month Box : 1 mg x 56 tablets NDC 0069-0469-12
Bottles 0.5 mg - bottle of 56 NDC 0069-0468-56
1 mg - bottle of 56 NDC 0069-0469-56

Store at 25ºC (77ºF); excursions permitted to 15–30ºC (59–86ºF).

17 PATIENT COUNSELING INFORMATION

See Medication Guide

17.1 Initiate Treatment and Continue to Attempt to Quit if Lapse

Instruct patients to set a date to quit smoking and to initiate Champix treatment one week before the quit date. Alternatively, the patient can begin Champix dosing and then set a date to quit smoking between days 8 and 35 of treatment. Encourage patients to continue to attempt to quit if they have early lapses after quit day .

17.2 How To Take

Advise patients that Champix should be taken after eating, and with a full glass of water.

17.3 Starting Week Dosage

Instruct patients on how to titrate Champix, beginning at a dose of 0.5 mg/day. Explain that one 0.5 mg tablet should be taken daily for the first three days, and that for the next four days, one 0.5 mg tablet should be taken in the morning and one 0.5 mg tablet should be taken in the evening.

17.4 Continuing Weeks Dosage

Advise patients that, after the first seven days, the dose should be increased to one 1 mg tablet in the morning and one 1 mg tablet in the evening.

17.5 Dosage Adjustment for Champix or Other Drugs

Inform patients that nausea and insomnia are side effects of Champix and are usually transient; however, advise patients that if they are persistently troubled by these symptoms, they should notify the prescribing physician so that a dose reduction can be considered.

Inform patients that some drugs may require dose adjustment after quitting smoking .

17.6 Counseling and Support

Provide patients with educational materials and necessary counseling to support an attempt at quitting smoking .

17.7 Neuropsychiatric Symptoms

Inform patients that some patients have experienced changes in mood, psychosis, hallucinations, paranoia, delusions, homicidal ideation, aggression, anxiety, and panic, as well as suicidal ideation and suicide when attempting to quit smoking while taking Champix. If patients develop agitation, hostility, depressed mood, or changes in behavior or thinking that are not typical for them, or if patients develop suicidal ideation or behavior, they should be urged to discontinue Champix and report these symptoms to their healthcare provider immediately.

17.8 History of Psychiatric Illness

Encourage patients to reveal any history of psychiatric illness prior to initiating treatment.

17.9 Nicotine Withdrawal

Inform patients that quitting smoking, with or without Champix, may be associated with nicotine withdrawal symptoms or exacerbation of pre-existing psychiatric illness.

17.10 Angioedema

Inform patients that there have been reports of angioedema, with swelling of the face, mouth (lip, gum, tongue) and neck (larynx and pharynx) that can lead to life-threatening respiratory compromise. Instruct patients to discontinue Champix and immediately seek medical care if they experience these symptoms .

17.11 Serious Skin Reactions

Inform patients that serious skin reactions, such as Stevens-Johnson Syndrome and erythema multiforme, were reported by some patients taking Champix. Advise patients to stop taking Champix at the first sign of rash with mucosal lesions or skin reaction and contact a healthcare provider immediately .

17.12 Patients with Cardiovascular Disease

Patients with cardiovascular disease should be instructed to notify their health care providers of symptoms of new or worsening cardiovascular events and to seek immediate medical attention if they experience signs and symptoms of myocardial infarction. .

17.13 Driving or Operating Machinery

Advise patients to use caution driving or operating machinery until they know how quitting smoking and/or varenicline may affect them .

17.14 Vivid, Unusual, or Strange Dreams

Inform patients that they may experience vivid, unusual or strange dreams during treatment with Champix.

17.15 Pregnancy and Lactation

Patients who are pregnant or breastfeeding or planning to become pregnant should be advised of: the risks of smoking to a pregnant mother and her developing baby, the potential risks of Champix use during pregnancy and breastfeeding, and the benefits of smoking cessation with and without Champix .

LAB- 0327- 16.0
Company Logo MEDICATION GUIDE

Champix (CHANT-iks)

(varenicline) Tablets

Read the Medication Guide that comes with Champix before you start taking it and each time you get a refill. There may be new information. This information does not take the place of talking with your doctor about your condition or treatment.

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

Some people have had changes in behavior, hostility, agitation, depressed mood, and suicidal thoughts or actions while using Champix to help them quit smoking. Some people had these symptoms when they began taking Champix, and others developed them after several weeks of treatment, or after stopping Champix.

If you, your family, or caregiver notice agitation, hostility, depression or changes in behavior or thinking that are not typical for you, or you develop any of the following symptoms, stop taking Champix and call your doctor right away:


When you try to quit smoking, with or without Champix, 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, and increased appetite or 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.

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

See " What are the possible side effects of Champix? "

Some people can have allergic reactions to Champix. Some of these allergic reactions can be life-threatening and include: swelling of the face, mouth (tongue, lips), and throat that can cause trouble breathing. If you have these symptoms, stop taking Champix and get medical attention right away.

Some people can have serious skin reactions while taking Champix. These can include rash, swelling, redness, and peeling of the skin. Some of these reactions can become life-threatening. If you have a rash with peeling skin or blisters in your mouth, stop taking Champix and see your doctor right away.

What is Champix?

Champix is a prescription medicine to help adults 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.

Champix is not recommended for people under 18 years of age.

Champix has not been studied with other treatments for stopping smoking.

Who should not take Champix?

Do not take Champix if you have had a serious allergic or skin reaction to Champix, which may include:


What should I tell my doctor before taking Champix?

Before you take Champix, tell your doctor if you:


Tell your doctor about all your other medicines, including prescription and nonprescription medicines, vitamins and herbal supplements. Especially, tell your doctor if you take:


When you stop smoking, there may be a change in how these and other medicines work for you.

You should not use Champix while using other medicines to quit smoking. Tell your doctor if you use other treatments to quit smoking.

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

How should I take Champix?


What should I avoid while taking Champix?

Use caution driving or operating machinery until you know how Champix may affect you. Some people who use Champix may feel sleepy, dizzy, or have trouble concentrating, that can make it hard to drive or perform other activities safely.

What are the possible side effects of Champix?

Serious side effects of Champix may include:


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

These are not all the side effects of Champix. Ask your doctor 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.

How should I store Champix?


General information about Champix

Medicines are sometimes prescribed for purposes other than those listed in a Medication Guide. Do not use Champix for a condition for which it was not prescribed. Do not give your Champix to other people, even if they have the same symptoms that you have. It may harm them.

This Medication Guide summarizes the most important information about Champix. If you would like more information, talk with your doctor. You can ask your doctor or pharmacist for information about Champix that is written for healthcare professionals.

For more about Champix and tips on how to quit smoking, go to www. CHANTIX.com or call 1-877-CHANTIX (877-242-6849).

What are the ingredients in Champix?

Active ingredient: Champix

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 (for both 0.5 mg and 1 mg)

LAB-0328-10.0

July 2011

This Medication Guide has been approved by the U.S. Food and Drug Administration.

Champix pharmaceutical active ingredients containing related brand and generic drugs:


Champix available forms, composition, doses:


Champix destination | category:


Champix Anatomical Therapeutic Chemical codes:


Champix pharmaceutical companies:


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References

  1. Dailymed."CHANTIX (VARENICLINE TARTRATE) KIT CHANTIX (VARENICLINE TARTRATE) TABLET, FILM COATED [LAKE ERIE MEDICAL & SURGICAL SUPPLY DBA QUALITY CARE PRODUCTS LL". https://dailymed.nlm.nih.gov/dailym... (accessed August 28, 2018).
  2. "Varenicline". https://pubchem.ncbi.nlm.nih.gov/co... (accessed August 28, 2018).
  3. "Varenicline". http://www.drugbank.ca/drugs/DB0127... (accessed August 28, 2018).

Frequently asked Questions

Can i drive or operate heavy machine after consuming Champix?

Depending on the reaction of the Champix after taken, if you are feeling dizziness, drowsiness or any weakness as a reaction on your body, Then consider Champix not safe to drive or operate heavy machine after consumption. Meaning that, do not drive or operate heavy duty machines after taking the capsule if the capsule has a strange reaction on your body like dizziness, drowsiness. As prescribed by a pharmacist, it is dangerous to take alcohol while taking medicines as it exposed patients to drowsiness and health risk. Please take note of such effect most especially when taking Primosa capsule. It's advisable to consult your doctor on time for a proper recommendation and medical consultations.

Is Champix addictive or habit forming?

Medicines are not designed with the mind of creating an addiction or abuse on the health of the users. Addictive Medicine is categorically called Controlled substances by the government. For instance, Schedule H or X in India and schedule II-V in the US are controlled substances.

Please consult the medicine instruction manual on how to use and ensure it is not a controlled substance.In conclusion, self medication is a killer to your health. Consult your doctor for a proper prescription, recommendation, and guidiance.

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Review

sdrugs.com conducted a study on Champix, and the result of the survey is set out below. It is noteworthy that the product of the survey is based on the perception and impressions of the visitors of the website as well as the views of Champix consumers. We, as a result of this, advice that you do not base your therapeutic or medical decisions on this result, but rather consult your certified medical experts for their recommendations.

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The information was verified by Dr. Rachana Salvi, MD Pharmacology


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