Buproban

Bupropion is a prescription medication used to treat depression and to quit smoking, depending on the form.

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

Buproban is part of the drug class:

• Other antidepressants

 Buproprion is available in three different types of tablets.

1. Buproprion tablet which is available in both 75mg and 150mg strengths.  This tablet may be taken every eight hours or up to three times a day.
2. Buproprion SR (Sustained Release) is available as a 100mg, 150mg, and 200mg tablet. The Sustained Release coating allows for this medication to be taken every twelve hours or twice a day.
3. Buproprion XL (Extended Release) is available as a 150mg, 300mg, and 450mg tablet. The Extended Release coating on allows for this medication to taken once every twenty four hours or once a day. The 450mg is available only as a brand name medication called Forfivo XL.

Warning

Suicidality and Antidepressant Drugs

Use in Treating Psychiatric Disorders:

Antidepressants increased the risk compared to placebo of suicidal thinking and behavior (suicidality) in children, adolescents, and young adults in short-term studies of major depressive disorder (MDD) and other psychiatric disorders. Anyone considering the use of bupropion or any other antidepressant in a child, adolescent, or young adult must balance this risk with the clinical need. Short-term studies did not show an increase in the risk of suicidality with antidepressants compared to placebo in adults beyond age 24; there was a reduction in risk with antidepressants compared to placebo in adults aged 65 and older. Depression and certain other psychiatric disorders are themselves associated with increases in the risk of suicide. 

Patients of all ages who are started on antidepressant therapy should be monitored appropriately and observed closely for clinical worsening, suicidality, or unusual changes in behavior. Families and caregivers should be advised of the need for close observation and communication with the prescriber. Bupropion is not approved for use in pediatric patients.

Use in Smoking Cessation Treatment

This medication, the sustained release, and the extended release formulations are not approved for smoking cessation treatment, but bupropion under the name bupropion is approved for this use. Serious neuropsychiatric events, including but not limited to depression, suicidal ideation, suicide attempt, and completed suicide have been reported in patients taking bupropion for smoking cessation. Some 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 bupropion who continued to smoke.

All patients being treated with bupropion for smoking cessation treatment 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 bupropion in the postmarketing experience. When symptoms were reported, most were during treatment with bupropion, but some were following discontinuation of treatment with bupropion. These events have occurred in patients with and without pre-existing psychiatric disease; some have experienced worsening of their psychiatric illnesses. Patients with serious psychiatric illness such as schizophrenia, bipolar disorder, and major depressive disorder did not participate in the premarketing studies of bupropion.

Advise patients and caregivers that the patient using bupropion for smoking cessation should stop taking bupropion and contact a healthcare provider immediately if agitation, hostility, depressed mood, or changes in thinking or behavior 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 bupropion was reported, although in some cases the symptoms persisted; therefore, ongoing monitoring and supportive care should be provided until symptoms resolve.

The risks of using bupropion for smoking cessation should be weighed against the benefits of its use. Bupropion has been demonstrated to increase the likelihood of abstinence from smoking for as long as 6 months compared to treatment with placebo. The health benefits of quitting smoking are immediate and substantial. 

In the U.S.

• Aplenzin
• Budeprion SR
• Budeprion XL
• Buproban
• Forfivo XL
• Wellbutrin
• Wellbutrin SR
• Wellbutrin XL
• Zyban

Available Dosage Forms:

• Tablet, Extended Release, 24 HR
• Tablet, Extended Release, 12 HR
• Tablet
• Tablet, Extended Release

Therapeutic Class: Antidepressant

Chemical Class: Aminoketone

This section provides information on the proper use of a number of products that contain bupropion. It may not be specific to Buproban. 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.

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.
• Signs of high blood pressure like very bad headache or dizziness, passing out, or change in eyesight.
• Change in how you act.
• Feeling confused.
• Hallucinations (seeing or hearing things that are not there).
• If seizures are new or worse after starting Buproban.
• A big weight gain or loss.
• Chest pain or pressure or a fast heartbeat.
• A heartbeat that does not feel normal.
• Swelling.
• Shortness of breath.
• Ringing in ears.
• Passing urine more often.
• Swollen gland.
• Trouble moving around.
• Very bad muscle or joint pain.
• A very bad skin reaction (Stevens-Johnson syndrome/toxic epidermal necrolysis) may happen. It can cause very bad health problems that may not go away, and sometimes death. Get medical help right away if you have signs like red, swollen, blistered, or peeling skin (with or without fever); red or irritated eyes; or sores in your mouth, throat, nose, or eyes.

Usual Dosage

Treatment with Buproban® should be initiated before the patient's planned quit day, while the patient is still smoking, because it takes approximately 1 week of treatment to achieve steady-state blood levels of bupropion. The patient should set a "target quit date" within the first 2 weeks of treatment with Buproban®.

Dosing: To minimize the risk of seizure:

• Begin dosing with one 150-mg tablet per day for 3 days.
• Increase dose to 300 mg/day given as one 150-mg tablet twice each day with an interval of at least 8 hours between each dose.
• Do not exceed 300 mg/day.

Buproban® should be swallowed whole and not crushed, divided, or chewed, as this may lead to an increased risk of adverse effects including seizures [see Warnings and Precautions (5.3)].

Buproban® may be taken with or without food [see Clinical Pharmacology (12.3)].

Duration of Treatment

Treatment with Buproban® should be continued for 7 to 12 weeks. If the patient has not quit smoking after 7 to 12 weeks, it is unlikely that he or she will quit during that attempt so treatment with Buproban® should probably be discontinued and the treatment plan reassessed. The goal of therapy with Buproban® is complete abstinence.

Discuss discontinuing treatment with Buproban® after 12 weeks if the patient feels ready but consider whether the patient may benefit from ongoing treatment. Patients who successfully quit after 12 weeks of treatment but do not feel ready to discontinue treatment should be considered for ongoing therapy with Buproban®; longer treatment should be guided by the relative benefits and risks for individual patients.

It is important that patients continue to receive counseling and support throughout treatment with Buproban® and for a period of time thereafter.

Individualization of Therapy

Patients are more likely to quit smoking and remain abstinent if they are seen frequently and receive support from their physicians or other healthcare professionals. It is important to ensure that patients read the instructions provided to them and have their questions answered. Physicians should review the patient's overall smoking cessation program that includes treatment with Buproban®. Patients should be advised of the importance of participating in the behavioral interventions, counseling, and/or support services to be used in conjunction with Buproban® [see Medication Guide].

Patients who fail to quit smoking during an attempt may benefit from interventions to improve their chances for success on subsequent attempts. Patients who are unsuccessful should be evaluated to determine why they failed. A new quit attempt should be encouraged when factors that contributed to failure can be eliminated or reduced, and conditions are more favorable.

Maintenance

Tobacco dependence is a chronic condition. Some patients may need on-going treatment. Whether to continue treatment with Buproban® for periods longer than 12 weeks for smoking cessation must be determined for individual patients.

Combination Treatment With Buproban® and a Nicotine Transdermal System (NTS)

Combination treatment with Buproban® and NTS may be prescribed for smoking cessation. The prescriber should review the complete prescribing information for both Buproban® and NTS before using combination treatment [see Clinical Studies (14)]. Monitoring for treatment-emergent hypertension in patients treated with the combination of Buproban® and NTS is recommended.

Dose Adjustment in Patients With Hepatic Impairment

In patients with moderate to severe hepatic impairment (Child-Pugh score: 7 to 15), the maximum dose should not exceed 150 mg every other day. In patients with mild hepatic impairment (Child-Pugh score: 5 to 6), consider reducing the dose and/or frequency of dosing [see Use in Specific Populations (8.7) and Clinical Pharmacology (12.3)].

Dose Adjustment in Patients With Renal Impairment

Consider reducing the dose and/or frequency of Buproban® in patients with renal impairment (Glomerular Filtration Rate <90 mL/min) [see Use in Specific Populations (8.6) and Clinical Pharmacology (12.3)].

Use of Buproban® With Reversible MAOIs Such as Linezolid or Methylene Blue

Do not start Buproban® in a patient who is being treated with a reversible MAOI such as linezolid or intravenous methylene blue. Drug interactions can increase the risk of hypertensive reactions [see Contraindications (4) and Drug Interactions (7.6)]. In some cases, a patient already receiving therapy with Buproban® may require urgent treatment with linezolid or intravenous methylene blue. If acceptable alternatives to linezolid or intravenous methylene blue treatment are not available and the potential benefits of linezolid or intravenous methylene blue treatment are judged to outweigh the risks of hypertensive reactions in a particular patient, Buproban® should be stopped promptly, and linezolid or intravenous methylene blue can be administered. The patient should be monitored for 2 weeks or until 24 hours after the last dose of linezolid or intravenous methylene blue, whichever comes first. Therapy with Buproban® may be resumed 24 hours after the last dose of linezolid or intravenous methylene blue.

The risk of administering methylene blue by non-intravenous routes (such as oral tablets or by local injection) or in intravenous doses much lower than 1 mg/kg with Buproban® is unclear. The clinician should, nevertheless, be aware of the possibility of a drug interaction with such use [see Contraindications (4) and Drug Interactions (7.6)].

150 mg – light yellow, round, convex, film-coated, extended-release tablets debossed with "G" on one side and "2444" on the other side.

Controlled Substance

Bupropion is not a controlled substance.

Abuse

Humans: Controlled clinical trials of bupropion (immediate-release formulation) conducted in normal volunteers, in subjects with a history of multiple drug abuse, and in depressed subjects showed some increase in motor activity and agitation/excitement.

In a population of individuals experienced with drugs of abuse, a single dose of 400 mg of bupropion produced mild amphetamine-like activity as compared with placebo on the Morphine-Benzedrine Subscale of the Addiction Research Center Inventories (ARCI) and a score intermediate between placebo and amphetamine on the Liking Scale of the ARCI. These scales measure general feelings of euphoria and drug desirability.

Findings in clinical trials, however, are not known to reliably predict the abuse potential of drugs. Nonetheless, evidence from single-dose trials does suggest that the recommended daily dosage of bupropion when administered in divided doses is not likely to be significantly reinforcing to amphetamine or CNS stimulant abusers. However, higher doses (that could not be tested because of the risk of seizure) might be modestly attractive to those who abuse CNS stimulant drugs.

Animals: Studies in rodents and primates demonstrated that bupropion exhibits some pharmacologic actions common to psychostimulants. In rodents, it has been shown to increase locomotor activity, elicit a mild stereotyped behavior response, and increase rates of responding in several schedule-controlled behavior paradigms. In primate models assessing the positive reinforcing effects of psychoactive drugs, bupropion was self-administered intravenously. In rats, bupropion produced amphetamine-like and cocaine-like discriminative stimulus effects in drug discrimination paradigms used to characterize the subjective effects of psychoactive drugs.

The possibility that bupropion may induce dependence should be kept in mind when evaluating the desirability of including the drug in smoking cessation programs of individual patients.