Zyban

The following adverse reactions are discussed in greater detail in other sections of the labeling:

• Neuropsychiatric symptoms and suicide risk in smoking cessation treatment [see BOXED WARNING, WARNINGS AND PRECAUTIONS]
• Suicidal thoughts and behaviors in adolescents and young adults [see BOXED WARNING, WARNINGS AND PRECAUTIONS]
• Seizure [see WARNINGS AND PRECAUTIONS]
• Hypertension [see WARNINGS AND PRECAUTIONS]
• Activation of mania or hypomania [see WARNINGS AND PRECAUTIONS]
• Psychosis and other neuropsychiatric reactions [see WARNINGS AND PRECAUTIONS]
• Angle-closure glaucoma [see WARNINGS AND PRECAUTIONS]
• Hypersensitivity reactions [see WARNINGS AND PRECAUTIONS]

Clinical Trials Experience

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

Adverse reactions were sufficiently troublesome to cause discontinuation of treatment in 8% of the 706 subjects treated with ZYBAN and 5% of the 313 patients treated with placebo. The more common events leading to discontinuation of treatment with ZYBAN included nervous system disturbances (3.4%), primarily tremors, and skin disorders (2.4%), primarily rashes.

The most commonly observed adverse reactions consistently associated with the use of ZYBAN were dry mouth and insomnia. The incidence of dry mouth and insomnia may be related to the dose of ZYBAN. The occurrence of these adverse reactions may be minimized by reducing the dose of ZYBAN. In addition, insomnia may be minimized by avoiding bedtime doses.

Adverse reactions reported in the dose-response and comparator trials are presented in Table 2 and Table 3, respectively. Reported adverse reactions were classified using a COSTART-based dictionary.

Table 2: Adverse Reactions Reported by at Least 1% of Subjects and at a Greater Frequency than Placebo in the Dose-Response Trial

Table 3: Adverse Reactions Reported by at Least 1% of Subjects on Active Treatment and at a Greater Frequency than Placebo in the Comparator Trial

Adverse reactions in a 1-year maintenance trial and a 12-week COPD trial with ZYBAN were quantitatively and qualitatively similar to those observed in the dose-response and comparator trials.

In addition to the adverse reactions noted above, the following adverse reactions have been reported in clinical trials with the sustained-release formulation of bupropion in depressed subjects and in nondepressed smokers, as well as in clinical trials with the immediate-release formulation of bupropion.

Adverse reaction frequencies represent the proportion of subjects who experienced a treatment-emergent adverse reaction on at least one occasion in placebo-controlled trials for depression (n = 987) or smoking cessation (n = 1,013), or subjects who experienced an adverse reaction requiring discontinuation of treatment in an open-label surveillance trial with bupropion sustained-release tablets (n = 3,100). All treatment-emergent adverse reactions are included except those listed in Tables 2 and 3, those listed in other safety-related sections of the prescribing information, those subsumed under COSTART terms that are either overly general or excessively specific so as to be uninformative, those not reasonably associated with the use of the drug, and those that were not serious and occurred in fewer than 2 subjects.

Adverse reactions are further categorized by body system and listed in order of decreasing frequency according to the following definitions of frequency: Frequent adverse reactions are defined as those occurring in at least 1/100 subjects. Infrequent adverse reactions are those occurring in 1/100 to 1/1,000 subjects, while rare events are those occurring in less than 1/1,000 subjects.

Body (General): Frequent were asthenia, fever, and headache. Infrequent were chills, inguinal hernia, and photosensitivity. Rare was malaise.

Cardiovascular: Infrequent were flushing, migraine, postural hypotension, stroke, tachycardia, and vasodilation. Rare was syncope.

Digestive: Frequent were dyspepsia and vomiting. Infrequent were abnormal liver function, bruxism, dysphagia, gastric reflux, gingivitis, jaundice, and stomatitis.

Hemic and Lymphatic: Infrequent was ecchymosis.

Metabolic and Nutritional: Infrequent were edema and peripheral edema.

Musculoskeletal: Infrequent were leg cramps and twitching.

Nervous System: Frequent were agitation, depression, and irritability. Infrequent were abnormal coordination, CNS stimulation, confusion, decreased libido, decreased memory, depersonalization, emotional lability, hostility, hyperkinesia, hypertonia, hypesthesia, paresthesia, suicidal ideation, and vertigo. Rare were amnesia, ataxia, derealization, and hypomania.

Respiratory: Rare was bronchospasm.

Skin: Frequent was sweating.

Special Senses: Frequent was blurred vision or diplopia. Infrequent were accommodation abnormality and dry eye.

Urogenital: Frequent was urinary frequency. Infrequent were impotence, polyuria, and urinary urgency.

Postmarketing Experience

The following adverse reactions have been identified during post-approval use of ZYBAN and are not described elsewhere in the label. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a relationship to drug exposure.

Arthralgia, myalgia, and fever with rash and other symptoms suggestive of delayed hypersensitivity. These symptoms may resemble serum sickness [see WARNINGS AND PRECAUTIONS].

Cardiovascular disorder, complete AV block, extrasystoles, hypotension, myocardial infarction, phlebitis, and pulmonary embolism.

Colitis, esophagitis, gastrointestinal hemorrhage, gum hemorrhage, hepatitis, increased salivation, intestinal perforation, liver damage, pancreatitis, stomach ulcer, and stool abnormality.

Hyperglycemia, hypoglycemia, and syndrome of inappropriate antidiuretic hormone.

Anemia, leukocytosis, leukopenia, lymphadenopathy, pancytopenia, and thrombocytopenia. Altered PT and/or INR, infrequently associated with hemorrhagic or thrombotic complications, were observed when bupropion was coadministered with warfarin.

Glycosuria.

Arthritis and muscle rigidity/fever/rhabdomyolysis, and muscle weakness.

Abnormal electroencephalogram (EEG), aggression, akinesia, aphasia, coma, completed suicide, delirium, delusions, dysarthria, euphoria, extrapyramidal syndrome (dyskinesia, dystonia, hypokinesia, parkinsonism), hallucinations, increased libido, manic reaction, neuralgia, neuropathy, paranoid ideation, restlessness, suicide attempt, and unmasking tardive dyskinesia.

Pneumonia.

Alopecia, angioedema, exfoliative dermatitis, hirsutism, and Stevens-Johnson syndrome.

Deafness, increased intraocular pressure, and mydriasis.

Abnormal ejaculation, cystitis, dyspareunia, dysuria, gynecomastia, menopause, painful erection, prostate disorder, salpingitis, urinary incontinence, urinary retention, urinary tract disorder, and vaginitis.

Zyban is a prescription medication used to help patients quit smoking. 

This medication may be prescribed for other uses. Ask your doctor or pharmacist for more information.

Start Zyban before you stop smoking to give Zyban time to build up in your body. It takes about 1 week for Zyban to start working.

Pick a date to stop smoking that is during the second week you are taking Zyban.

Take Zyban exactly as prescribed by your healthcare provider. Do not change your dose or stop taking Zyban without talking with your healthcare provider first.

Zyban is usually taken for 7 to 12 weeks. Your healthcare provider may decide to prescribe ZYBAN for longer than 12 weeks to help you stop smoking. Follow your healthcare provider’s instructions.

Swallow Zyban Tablets whole. Do not chew, cut, or crush Zyban Tablets. If you do, the medicine will be released into your body too quickly. If this happens you may be more likely to get side effects including seizures. Tell your healthcare provider if you cannot swallow tablets.

Zyban tablets may have an odor. This is normal.

• Take your doses of Zyban at least 8 hours apart.
• You may take Zyban with or without food.

It is not dangerous to smoke and take Zyban at the same time. But, you will lower your chance of breaking your smoking habit if you smoke after the date you set to stop smoking.

You may use Zyban and nicotine patches (a type of nicotine replacement therapy) at the same time, following the precautions below.

• You should only use Zyban and nicotine patches together under the care of your healthcare provider. Using Zyban and nicotine patches together may raise your blood pressure, and sometimes this can be severe.
• Tell your healthcare provider if you plan to use nicotine patches. Your healthcare provider should check your blood pressure regularly if you use nicotine patches with Zyban to help you quit smoking.

Zyban should be used with a patient support program. It is important to participate in the behavioral program, counseling, or other support program your healthcare professional recommends.

If you miss a dose, do not take an extra dose to make up for the dose you missed. Wait and take your next dose at the regular time. This is very important. Too much Zyban can increase your chance of having a seizure.

If you take too much Zyban, or overdose, call your local emergency room or poison control center right away.

Bupropion is an antidepressant medication used to treat major depressive disorder and seasonal affective disorder. The Zyban brand of bupropion is used to help people stop smoking by reducing cravings and other withdrawal effects.

Bupropion may also be used for purposes not listed in this medication guide.

Bupropion is used to treat depression and to prevent depression in patients with seasonal affective disorder (SAD), which is sometimes called winter depression. It is also used as part of a support program to help people stop smoking.

Bupropion is sold under different brand names. If you are already taking medicine for depression or to help you stop smoking, discuss this with your doctor before taking bupropion. It is very important that you receive only one prescription at a time for bupropion.

This medicine is available only with your doctor's prescription.

This section provides information on the proper use of a number of products that contain bupropion. It may not be specific to Zyban. Please read with care.

Take this medicine only as directed by your doctor. Do not use more of it, do not use it more often, and do not use it for a longer time than your doctor ordered. To do so may increase the chance of side effects.

This medicine should come with a Medication Guide. Read and follow these instructions carefully. Ask your doctor if you have any questions.

Use only the brand of this medicine that your doctor prescribed. Different brands may not work the same way.

Swallow the tablet whole. Do not break, crush, or chew it.

You may take this medicine with or without food. But if you have nausea, take the medicine with food.

A part of the extended-release tablet may pass into your stool. This is normal and is nothing to worry about.

Use of Zyban® tablets:

• You may continue to smoke for about 1 week after you start the medicine.
• Set a target date to quit smoking during your second week of treatment.
• If you are still having trouble with quitting after using the medicine for at least 7 weeks, talk to your doctor.
• If you use a nicotine product (eg, patch) together with Zyban®, do not smoke. Smoking may increase the chance for serious side effects.

If you have trouble sleeping (insomnia), do not take this medicine too close to bedtime.

If you use this medicine to prevent depression with seasonal affective disorder, take it during the autumn season before your symptoms start. Continue using the medicine through the winter season and until early spring.

Dosing

The dose of this medicine will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of this medicine. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

• For oral dosage form (extended-release tablets):
  • For depression:
    • Adults—
      • Aplenzin®: At first, 174 milligrams (mg) once a day in the morning. Your doctor may adjust your dose as needed. However, the dose is usually not more than 522 mg per day.
      • Forfivo XL®: 450 mg once a day.
      • Wellbutrin XL®: At first, 150 mg once a day in the morning. Your doctor may adjust your dose as needed. However, the dose is usually not more than 450 mg per day.
    • Children—Use and dose must be determined by your doctor.
  • For seasonal affective disorder:
    • Adults—
      • Aplenzin®: At first, 174 milligrams (mg) once a day in the morning. Your doctor may adjust your dose as needed. However, the dose is usually not more than 522 mg per day.
      • Wellbutrin XL®: At first, 150 mg once a day in the morning. Your doctor may adjust your dose as needed. However, the dose is usually not more than 300 mg once a day.
    • Children—Use and dose must be determined by your doctor.
• For oral dosage form (sustained-release tablets):
  • For depression:
    • Adults—At first, 150 milligrams (mg) once a day in the morning. Your doctor may adjust your dose as needed. However, the dose is usually not more than 200 mg two times per day, taken at least 8 hours apart.
    • Children—Use and dose must be determined by your doctor.
  • To quit smoking:
    • Adults—At first, 150 milligrams (mg) once a day for the first 3 days. Your doctor may adjust your dose as needed. However, the dose is usually not more than 300 mg per day.
    • Children—Use and dose must be determined by your doctor.
• For oral dosage form (tablets):
  • For depression:
    • Adults—At first, 100 milligrams (mg) two times per day. Your doctor may adjust your dose as needed. However, the dose is usually not more than 150 mg three times per day, taken at least 6 hours apart.
    • Children—Use and dose must be determined by your doctor.

Missed Dose

If you miss a dose of this medicine, skip the missed dose and go back to your regular dosing schedule. Do not double doses.

If you are taking the Wellbutrin XL® extended-release tablet and you miss a dose, skip the missed dose and go back to your regular dosing schedule.

Storage

Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.

Keep out of the reach of children.

Do not keep outdated medicine or medicine no longer needed.

Ask your healthcare professional how you should dispose of any medicine you do not use.

Human Overdose Experience

Overdoses of up to 30 grams or more of bupropion have been reported. Seizure was reported in approximately one-third of all cases. Other serious reactions reported with overdoses of bupropion alone included hallucinations, loss of consciousness, sinus tachycardia, and ECG changes such as conduction disturbances (including QRS prolongation) or arrhythmias. Fever, muscle rigidity, rhabdomyolysis, hypotension, stupor, coma, and respiratory failure have been reported mainly when bupropion was part of multiple drug overdoses.

Although most patients recovered without sequelae, deaths associated with overdoses of bupropion alone have been reported in patients ingesting large doses of the drug. Multiple uncontrolled seizures, bradycardia, cardiac failure, and cardiac arrest prior to death were reported in these patients.

Overdosage Management

Consult a Certified Poison Control Center for up–to-date guidance and advice. Telephone numbers for certified poison control centers are listed in the Physicians’ Desk Reference (PDR). Call 1-800-222-1222 or refer to www.poison.org.

There are no known antidotes for bupropion. In case of an overdose, provide supportive care, including close medical supervision and monitoring. Consider the possibility of multiple drug overdose. Ensure an adequate airway, oxygenation, and ventilation. Monitor cardiac rhythm and vital signs. Induction of emesis is not recommended.

Take Zyban exactly as prescribed by your doctor. Follow all directions on your prescription label. Do not take this medicine in larger or smaller amounts or for longer than recommended. Too much of this medicine can increase your risk of a seizure.

When you start taking Zyban you may continue to smoke for about 1 week after you start the medicine. Set a date to quit smoking during the second week of treatment. Talk to your doctor if you are having trouble quitting after you have used Zyban for at least 7 weeks.

Your doctor may prescribe nicotine patches or gum to help support your smoking cessation treatment. Read all directions and safety information for the nicotine product. Do not smoke at any time if you are using a nicotine product along with Zyban. Too much nicotine can cause serious side effects.

You may have nicotine withdrawal symptoms when you stop smoking, including: increased appetite, weight gain, trouble sleeping, trouble concentrating, slower heart rate, having the urge to smoke, and feeling anxious, restless, depressed, angry, frustrated, or irritated. These symptoms may occur with or without using medication such as Zyban.

Smoking cessation may also cause new or worsening mental health problems, such as depression.

You should not change your dose or stop using this medicine suddenly, unless you have a seizure while taking this medicine. Stopping suddenly can cause unpleasant withdrawal symptoms.

This medicine can cause you to have a false positive drug screening test. If you provide a urine sample for drug screening, tell the laboratory staff that you are taking bupropion.

Store at room temperature away from moisture and heat.

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222. An overdose of bupropion can be fatal. Overdose symptoms may include muscle stiffness, hallucinations, fast or uneven heartbeat, shallow breathing, or fainting.

Get emergency medical help if you have any of these signs of an allergic reaction to Zyban: hives; difficult breathing; swelling of your face, lips, tongue, or throat.

Report any new or worsening symptoms to your doctor, such as: mood or behavior changes, anxiety, depression, panic attacks, trouble sleeping, or if you feel impulsive, irritable, agitated, hostile, aggressive, restless, hyperactive (mentally or physically), or have thoughts about suicide or hurting yourself.

Call your doctor at once if you have:

• a seizure (convulsions);

• unusual changes in mood or behavior;

• a manic episode - racing thoughts, increased energy, reckless behavior, feeling extremely happy or irritable, talking more than usual, severe problems with sleep;

• blurred vision, tunnel vision, eye pain or swelling, or seeing halos around lights;

• fast heartbeats; or

• severe skin reaction, fever, sore throat, swelling in your face or tongue, burning in your eyes, skin pain, followed by a red or purple skin rash that spreads (especially in the face or upper body) and causes blistering and peeling.

Common Zyban side effects may include:

• dry mouth, stuffy nose;

• nausea, constipation;

• sleep problems (insomnia);

• feeling anxious;

• dizziness; or

• joint pain.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

You may have a higher risk of seizures if you use certain other medicines while taking Zyban.

Many drugs can interact with bupropion. Tell your doctor about all medicines you use, and those you start or stop using during your treatment with Zyban. This includes prescription and over-the-counter medicines, vitamins, and herbal products. Not all possible interactions are listed in this medication guide.