DrugBuyers.Com: Wellbutrin

Bupropion HCl, an antidepressant of the aminoketone class and a non-nicotine aid to smoking cessation, is chemically unrelated to tricyclic, tetracyclic, selective serotonin re-uptake inhibitor, or other known antidepressant agents. Its structure closely resembles that of diethylpropion; it is related to phenylethylamines. It is designated as (±)-1-(3-chlorophenyl)-2-[(1,1-dimethylethyl)amino]-1-propanone hydrochloride. The molecular weight is 276.2. The empirical formula is C13H18ClNO·HCl. Bupropion HCl powder is white, crystalline, and highly soluble in water. It has a bitter taste and produces the sensation of local anesthesia on the oral mucosa.

Immediate Release Tablets: Wellbutrin is supplied for oral administration as 75 mg (yellow-gold) and 100 mg (red) film-coated tablets. Each tablet contains the labeled amount of bupropion HCl and the inactive ingredients: 75 mg tablet: D&C yellow no. 10 lake, FD&C yellow no. 6 lake, hydroxypropyl cellulose, hydroxypropyl methylcellulose, microcrystalline cellulose, polyethylene glycol, talc, and titanium dioxide; 100 mg tablet: FD&C red no. 40 lake, FD&C yellow no. 6 lake, hydroxypropyl cellulose, hydroxypropyl methylcellulose, microcrystalline cellulose, polyethylene glycol, talc, and titanium dioxide.

Sustained Release Tablets: Wellbutrin SR: Wellbutrin SR tablets are supplied for oral administration as 100 mg (blue) and 150 mg (purple), film-coated, sustained-release tablets. Each tablet contains the labeled amount of bupropion HCl and the inactive ingredients: carnauba wax, cysteine hydrochloride, hydroxypropyl methylcellulose, magnesium stearate, microcrystalline cellulose, polythylene glycol, and titanium dioxide and is printed with edible black ink. In addition, the 100 mg tablet contains FD&C blue no.1 lake and polysorbate 80, and the 150 mg tablet contains FD&C blue no. 2 lake, FD&C red no. 40 lake, and polysorbate 80. Zyban: Zyban (bupropion HCl for smoking cessation) is supplied for oral administration as 150-mg (purple), film-coated, sustained-release tablets. Each tablet contains the labeled amount of bupropion HCl and the inactive ingredients carnuba wax, cysteine HCl, hydroxypropyl methylcellulose, magnesium stearate, microcrystalline cellulose, polyethylene glycol, polysorbate 80 and titanium dioxide and is printed with edible black ink. In addition, the 150-mg tablet contains FD&C blue no. 2 lake and FD&C red no. 40 lake.

INDICATIONS

Sustained Release and Immediate Release Tablets: Treatment for Depression

Bupropion HCl is indicated for the treatment of depression.

The efficacy of bupropion HCl in the treatment of depression was established in two 4-week controlled trials of depressed inpatients and in one 6-week controlled trial of depressed outpatients for the sustained release tablets (two trials of approximately 3 weeks' duration in depressed patients and one of approximately 6 weeks' duration in depressed outpatients) whose diagnoses corresponded most closely to the Major Depression category of the APA Diagnostic and Statistical Manual (DSM) III
A major depressive episode (DSM-IV) implies the presence of 1) depressed mood or 2) loss of interest or pleasure; in addition, at least five of the following symptoms have been present during the same 2-week period and represent a change from previous functioning: depressed mood, markedly diminished interest or pleasure in usual activities or decrease in sex drive, significant change in weight and/or appetite, insomnia or hypersomia, psychomotor agitation or retardation, increased fatigue, feeling of guilt or worthlessness, slowed thinking or impaired concentration, a suicide attempt or suicidal ideation.

Effectiveness of bupropion in long-term use (more than 6 weeks) has not been systematically evaluated in controlled trials. Therefore, the physician who elects to use bupropion sustained release tablets for extended periods should periodically reevaluate the long-term usefulness of the drug for the individual patient.

Additional Information for the Immediate Release Tablets: A physician considering bupropion HCl sustained release tablets for the management of a patient's first episode of depression should be aware that the drug may cause generalized seizures in a dose-dependent manner with an approximate incidence of 0.4% (4/1000). This incidence of seizures may exceed that of other marketed antidepressants by as much as fourfold. This relative risk is only an approximate estimate because no direct comparative studies have been conducted (see WARNINGS).

Sustained Release Tablets: Treatment for Smoking Cessation

Bupropion is indicated as a smoking cessation treatment.

DOSAGE AND ADMINISTRATION

General Dosing Considerations: It is particularly important to administer bupropion HCl in a manner most likely to minimize the risk of seizure (see WARNINGS.) Gradual escalation in dosage is also important if agitation, motor restlessness, and insomnia, often seen during the initial days of treatment, are to be minimized. If necessary, these effects may be managed by temporary reduction of dose or the short-term administration of an intermediate to long-acting sedative hypnotic. A sedative hypnotic usually is not required beyond the first week of treatment. Insomnia may also be minimized by avoiding bedtime doses. If distressing, untoward effects supervene, dose escalation should be stopped.

Treatment of Depression

Initial Treatment

Sustained Release: The usual adult target dose for bupropion sustained release tablets is 300 mg/day, given as 150 mg, twice daily. Dosing with bupropion sustained release tablets should begin at 150 mg/day given as a single daily dose in the morning. If the 150 mg initial dose is adequately tolerated, an increase to the 300 mg/day target dose, given as 150 mg twice daily, may be made as early as day 4 of dosing. There should be an interval of at least 8 hours between successive doses.

Immediate Release: Increases in dose should not exceed 100 mg/day in a 3-day period. No single dose of bupropion HCl should exceed 150 mg. Bupropion HCl should be administered three times daily, preferably with at least 6 hours between successive doses.

The usual adult dose is 300 mg/day, given three times daily. Dosing should begin at 200 mg/day given as 100 mg twice daily. Based on clinical response, this dose may be increased to 300 mg/day, given as 100 mg 3 times daily, no sooner than 3 days after beginning therapy.
Increasing the Dosage Above 300 mg/day: As with other antidepressants, the full antidepressant effect of bupropion HCl may not be evident until 4 weeks of treatment or longer. An increase in dosage to the maximum of 400 mg/day, given as 200 mg twice daily, (450 mg/day for the immediate release, given as in doses not more than 150 mg each) may be considered for patients in whom no clinical improvement is noted after several weeks of treatment at 300 mg/day. For the Immediate Release Tablets Only: Dosing above 300 mg/day may be accomplished using the 75 or 100 mg tablets. The 100 mg tablet must be administered 4 times daily with at least 4 hours between successive doses, in order to not exceed the limit of 150 mg in a single dose. Bupropion HCl should be discontinued in patients who do not demonstrate an adequate response after an appropriate period of treatment at 450 mg/day.

Maintenance: The lowest dose that maintains remission is recommended. Although it is not known how long the patient should remain on bupropion HCl, it is generally recognized that acute episodes of depression require several months or longer of antidepressant drug treatment.

Treatment for Smoking Cessation

Usual Dosage for Adults: The recommended and maximum dose of bupropion HCl sustained release tablets for smoking cessation is 300 mg/day, given as 150 mg twice daily. Dosing should begin at 150 mg/day given every day for the first 3 days, followed by a dose increase for most patients to the recommended usual dose of 300 mg/day. There should be an interval of at least 8 hours between successive doses. Doses above 300 mg/day should not be used (see WARNINGS). Treatment with bupropion HCl sustained release tablets should be initiated while the patient is still smoking, since approximately 1 week of treatment is required to achieve steady-state blood levels of bupropion. Patients should set a "target quit date" within the first 2 weeks of treatment with bupropion HCl, generally in the second week. Treatment with bupropion HCl should be continued for 7 to 12 weeks; duration of treatment should be based on the relative benefits and risks for individual patients. If a patient has not made significant progress toward abstinence by the seventh week of therapy with bupropion HCl, it is unlikely that he or she will quit during that attempt, and treatment should probably be discontinued. Dose tapering of bupropion is not required when discontinuing treatment. It is important that patients continue to receive counseling and support throughout treatment with bupropion, 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 health care 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 bupropion HCl. Patients should be advised of the importance of participating in the behavioral interventions, counseling, and/or support services to be used in conjunction with bupropion HCl. See information for patients at the end of the package insert.

The goal of therapy with bupropion HCl is complete abstinence. If a patient has not made significant progress towards abstinence by the seventh week of therapy with bupropion HCl, it is unlikely that he or she will quit during that attempt, and treatment should be discontinued.

Patients who fail to quit smoking during an attempt may benefit from interventions to improve their chances for success on subsequent attempts. Patinets 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: Although clinical data are not available regarding the long-term use (>12 weeks) of bupropion for smoking cessation, bupropion has been used for longer periods of time in the treatment of depression. Whether to continue treatment with bupropion HCl for periods longer than 12 weeks for smoking cessation must be determined for individual patients.

Combination Treatment with Bupropion HCl and a Nicotine Transdermal System (NTS): Combination treatment with bupropion HCl and NTS may be prescribed for smoking cessation. The prescriber should review the complete prescribing information for both bupropion HCl and NTS before using combination treatment. See also CLINICAL STUDIES for methods and dosing used in the bupropion HCl and NTS combination trial. Monitoring for treatment-emergent hypertension in patients treated with the combination of bupropion and NTS is recommended.

HOW SUPPLIED

Wellbutrin Immediate Release Tablets: The 75 mg tablets are yellow-gold, round, biconvex tablets printed with "Wellbutrin 75". The 100 mg tablets are red, round, biconvex tablets printed with "Wellbutrin 100".

Wellbutrin SR Sustained Release Tablets: The 100 mg tablets are blue, round, biconvex, film-coated tablets printed with WELLBUTRIN SR 100. The 150 mg tablets are purple, round, biconvex, film-coated tablets printed with WELLBUTRIN SR 150.

Zyban Sustained Release Tablets: The 150 mg tablets are purple, round, biconvex, film-coated tablets printed with "ZYBAN 150".

Storage: Store at controlled room temperature, 20-25°C (68-77°F) The immediate release tablet can be stored at temperatures as low as 15°C (59°F). Dispense in a tight, light-resistant container as defined in the USP.

PATIENT INFORMATION

See the patient leaflet at the end of this monograph.

Patients should be made aware that Zyban, used as an aid to smoking cessation, contains the same active ingredient found in Wellbutrin and Wellbutrin SR used to treat depression and that Zyban should not be used in conjunction with Wellbutrin, Wellbutrin SR, or any other medications that contain bupropion HCl.

Physicians Are Advised to Discuss the Following Issues with Patients Treated for Depression:

As dose is increased during initial titration to doses above 150 mg/day, patients should be instructed to take bupropion sustained release tablets in two divided doses, preferably with at least eight hours between successive doses, to minimize the risk of seizures.
Patients should be told that any CNS-active drug like bupropion HCl may impair their ability to perform tasks requiring judgement or motor and cognitive skills. Consequently, until they are reasonably certain that bupropion HCl does not adversely affect their performance, they should refrain from driving an automobile or operating complex, hazardous machinery.
Patients should be told that the use and the cessation of use of alcohol may alter seizure threshold, and, therefore, that the consumption of alcohol should be minimized, and if possible, avoided completely.
Patients should be advised to inform their physicians if they are taking or plan to take any prescription or over-the-counter drugs. Concern is warranted because bupropion HCl and other drugs may affect each other's metabolism.
Patients should be advised to notify their physicians if they become pregnant or intend to become pregnant during therapy.
Patients should be advised to wswallow bupropion HCl sustained release tablets whole so that the release rate is not altered. Do not chew, divide, or crush tablets.
Information for Patients Using Bupropion Sustained Release Tablets as an Aid to Smoking Cessation: See patient information leaflet at the end of this monograph. Physicians are advised to review the leaflet with their patients.

PATIENT PACKAGE INSERT
For Bupropion HCl Sustained Release Tablets Only: Please read this information before you start taking bupropion sustained release tablets for depression or smoking cessation. Also read this leaflet each time you renew your prescription, in case anything has changed. This information is not intended to take the place of discussions between you and your doctor. You and your doctor should discuss bupropion HCl as it related to the treatment of your depression or as party of your plan to stop smoking. Do not let anyone else use your bupropion.

IMPORTANT WARNING: At a dose of 300 mg each day, there is a chance that approximately 1 out of every 1000 people taking bupropion HCl, the active ingredient in bupropion sustained release tablets, will have a seizure. The chance of this happening increases if you:

Have a seizure disorder (for example, epilepsy).
Have or have had an eating disorder (for example, bulimia or anorexia nervosa).
Take more than the recommended amount of bupropion sustained release tablets.
Take other medications with the same active ingredient that is in bupropion HCl (such as taking Wellbutrin (bupropion HCl for depression) and taking Zyban (bupropion HCl for smoking cessation).
You can reduce the chance of experiencing a seizure by following your doctor's directions on how to take bupropion HCl. You should also discuss with your doctor whether bupropion HCl is right for you.

What Is Bupropion HCl? Bupropion HCl is a prescription medicine to treat depression. It is also used to help people quit smoking. Studies have wshow that more than one third of people quit smoking for at least 1 month while taking bupropion HCl and participating in a patient support program. For many patients, bupropion reduces withdrawal symptoms and the urge to smoke. Bupropion HCl should be used with a patient support program. It is important to participate in the behavioral program, counseling, or other support program your health care professional recommends.

Who Should Not Take Bupropion? You should not take bupropion if you:

Have a seizure disorder (for example, epilepsy).
Are already taking any other medications that contain bupropion HCl such as Wellbutrin, Wellbutrin SR, or Zyban.
Have or have had an eating disorder (for example, bulimia or anorexia nervosa).
Are currently taking or have recently taken a monoamine oxidase inhibitor (MAOI).
Are allergic to bupropion.
Are There Special Concerns for Women? Bupropion is not recommended for women who are pregnant or breast-feeding. Women should notify their doctor if they become pregnant or intend to become pregnant while taking bupropion HCl.

How Should I Take Bupropion?

You should take bupropion as directed by your doctor.
The usual recommended dosing is to take one 150-mg tablet in the morning for the first 3 days. As early as the fourth day of treatment, your doctor may increase your dose to one 150-mg tablet in the morning and one 150-mg tablet in the early evening. Doses should be taken at least 8 hours apart.
For Depression: If your depression does not improve after several weeks, your doctor may increase the dose of bupropion HCl to a total of 400 mg each day (taken as 200 mg in the morning and 200 mg in the early evening).
Never take an "extra" dose of bupropion HCl for any reason, even if you miss a dose. If you forget to take a dose, do not take an extra tablet to "catch up" for the dose you forgot. Wait and take you next tablet at the regular time. Do not take more tablets than your doctor prescribed. This is important so you do not increase your chance of having a seizure.
It is important to wswallow bupropion HCl sustained release tablets whole. Do not chew, divide, or crush tablets.
How Long Should I Take Bupropion? For depression, only you and your doctor can determine how long you should take bupropion HCl. You and your doctor should discuss your signs and symptoms of depression regularly to determine how long you should take bupropion HCl. Do not stop taking your medicine or decrease the amount of medicine you are taking without talking to your doctor first. For smoking cessation, most people should take bupropion for 7 to 12 weeks. Follow your doctors instructions.

What Are Possible Side Effects of Bupropion? Like all medications, bupropion may cause side effects.

The most common side effects of bupropion HCl in clinical studies are: include dry mouth and difficulty sleeping.
At 300 mg/day: Loss of appetite, dry mouth, skin rash, sweating, ringing in the ears, and shakiness.

At 400 mg/day: Abdominal (stomach) pain, agitation, anxiety, dizziness, dry mouth, difficulty sleeping, muscle pain, nausea, rapid heart beat, sore throat, sweating, ringing in the ears, and urinating more often.

The most common side effects that caused people to stop taking bupropion HCl during clinical studies were shakiness, skin rash, nausea, agitation, and migraine (a severe type of headache).
The side effects of bupropion HCl are generally mild and often disappear after a few weeks. If you have nausea, you may want to take your medicine with food. If you have difficulty sleeping, avoid taking your medication too close to bedtime.
Contact your doctor or health care professional if you have signs of an allergic reaction such as a rash, hives or difficulty in breathing. Discuss any other troublesome side effects with your doctor.
Use caution before driving a car or operating complex, hazardous machinery until you know if bupropion affects your ability to perform these tasks.
Will Taking Bupropion HCl Change My Body Weight? In clinical studies with bupropion HCl, some people lost weight and other people gained weight.

For people who lost weight, 14 out of 100 people taking 300 mg/day of bupropion HCl lost more than 5 lbs, 19 out of 100 people taking 400 mg/day lost more than 5 lbs, and 6 out of 100 people taking placebo (a sugar pill) lost more than 5 lbs.

For people who gained weight, 3 out of 100 people taking 300 mg/day of bupropion HCl gained more than 5 lbs, 2 out of 100 people taking 400 mg/day gained more than 5 lbs, and 4 out of 100 people taking placebo (a sugar pill) gained more than 5 lbs.

Since weight change (gain or loss) also can be a symptom of depression, you should discuss with your doctor whether bupropion HCl is right for you.

Can I Drink Alcohol While I Am Taking Bupropion? It is best not to drink alcohol at all or to drink very little while taking bupropion HCl. If you usually drink a lot of alcohol, or if you drink a lot and suddenly stop, you may increase your chance of having a seizure. Therefore, it is important to discuss your use of alcohol with your doctor before you begin taking bupropion HCl.

Will Bupropion Affect Other Medications I Am Taking? Bupropion HCl may affect other medications you're taking. It is important not to take medications that may increase the chance for you to have a seizure. Therefore, you should make sure that your doctor knows about all medicines¾prescription or over-the-counter¾you are taking or plan to take.

Do Bupropion Tablets Have a Characteristic Odor? Bupropion tablets may have a characteristic odor. If present, this odor is normal.

How Should I Store Bupropion?

Store bupropion HCl at room temperature, out of direct sunlight.
Keep bupropion HCl in a tightly closed container.
Keep bupropion HCl out of the reach of children.
Additional Information for Smoking Cessation

When Should I Stop Smoking? It takes about 1 week for bupropion to reach the right levels in your body to be effective. So, to maximize your chance of quitting, you should not stop smoking until you have been taking bupropion HCl for 1 week. You should set a date to stop smoking during the second week you're taking bupropion HCl.

Can I Smoke While Taking Bupropion? It is not physically dangerous to smoke and use bupropion HCl at the same time. However, continuing to smoke after the date you set to stop smoking will seriously reduce you chance of breaking your smoking habit.

Can Bupropion Be Used at the Same Time as Nicotine Patches? Yes, bupropion HCl and nicotine patches can be used at the same time but should only be used together under the supervision of your doctor. Using bupropion HCl and nicotine patches together may raise your blood pressure. Your doctor will probably want to check your blood pressure regularly to make sure that it stays within acceptable levels.

DO NOT SMOKE AT ANY TIME if you are using a nicotine patch or any other nicotine product along with bupropion HCl. It is possible to get too much nicotine and have serious side effects.

This summary provides important information about bupropion. This summary cannot replace the more detailed information that you need from your doctor. If you have any questions or concerns about either bupropion, depression or smoking cessation, talk to your doctor or other health care professional.

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