Zyban (bupropion HCl)

Dosage of bupropion hydrobromide and bupropion hydrochloride is expressed in terms of the salt. Bupropion hydrobromide doses of 174, 348, or 522 mg are equivalent to bupropion hydrochloride doses of 150, 300, or 450 mg, respectively.

Bupropion is administered orally with or without food as conventional tablets, sustained-release tablets, or extended-release tablets. Do not chew, divide, or crush any of the tablet dosage forms; tablets should be swallowed whole.

As conventional tablets, bupropion hydrochloride initially is administered orally twice daily in the morning and evening, then increased to 3 times daily, with >=6 hours separating doses. Dosages >=300 mg should be administered as divided doses of <=150 mg.

As sustained-release, film-coated tablets (e.g., Wellbutrin(R) SR), bupropion hydrochloride initially is administered orally once daily in the morning, then increased to twice daily, in the morning and evening. Dosages >150 mg should be administered as divided doses twice daily, with >=8 hours separating the doses.

Avoiding bedtime administration of the evening dose of bupropion hydrochloride conventional tablets or extended-release, film-coated tablets may lessen the occurrence of insomnia.

As extended-release tablets (Aplenzin(R), Wellbutrin(R) XL), bupropion is administered orally once daily in the morning. The shell of the extended-release tablet (Aplenzin(R), Wellbutrin(R) XL) does not dissolve and may be passed in the stool.

As extended-release, 450-mg tablets (Forfivo XL(R)), bupropion hydrochloride is administered once daily in the morning.

Store bupropion hydrochloride conventional tablets and sustained-release, film-coated tablets (e.g., Wellbutrin(R) SR) at 20-25oC (excursions permitted between 15-30oC); protect from light and moisture. Store bupropion hydrochloride extended-release tablets (Wellbutrin(R) XL) and bupropion hydrobromide extended-release tablets (Aplenzin(R)) at 25oC; excursions permitted between 15-30oC. Store bupropion hydrochloride extended-release 450-mg tablets (Forfivo XL(R)) at 20-25oC.

No dosing information is available for this tab.

No dosing information is available for this tab.

Bupropion is metabolized to hydroxybupropion, principally by cytochrome P-450 (CYP) isoenzyme 2B6; CYP isoenzymes are not involved in the formation of other bupropion metabolites.

Bupropion and its metabolites (erythrohydrobupropion, threohydrobupropion, hydroxybupropion) inhibit CYP2D6.

There are no contraindication interactions for this drug.

There are no severe interactions for this drug.

There are no moderate interactions for this drug.

*Seizure disorders.

*Current or past diagnosis of anorexia nervosa or bulimia.

*Patients receiving any other bupropion formulation because risk of seizures is dose-dependent.

*Patients undergoing abrupt discontinuance of alcohol, benzodiazepines, barbiturates, or antiepileptic drugs.

*Patients currently receiving, or having recently received (i.e., within 14 days), monoamine oxidase inhibitor (MAOI) therapy.

*Patients currently receiving a reversible MAOI (e.g., linezolid, IV methylene blue).

*Hypersensitivity to the drug or any ingredient in the formulation.

There are no contraindication contraindications for this drug.

There are no severe contraindications for this drug.

There are no moderate contraindications for this drug.

Adverse effects reported in >=5% of patients receiving conventional bupropion hydrochloride tablets include agitation, auditory disturbance, blurred vision, cardiac arrhythmias, confusion, constipation, dizziness, dry mouth, excessive sweating, headache/migraine, hostility, insomnia, nausea/vomiting, rash, tachycardia, and tremor.

Adverse effects reported in >=5% of patients receiving bupropion hydrochloride sustained-release, film-coated tablets (e.g., Wellbutrin(R) SR) include headache, dry mouth, nausea, insomnia, dizziness, pharyngitis, constipation, agitation, anxiety, abdominal pain, tinnitus, tremor, palpitation, myalgia, sweating, rash, and anorexia.

Adverse effects reported in >=5% of patients receiving bupropion hydrochloride extended-release (SR) tablets for smoking cessation include insomnia, rhinitis, dry mouth, dizziness, nervous disturbance, anxiety, nausea, constipation, and arthralgia.

Adverse effects reported in >=5% of patients receiving bupropion hydrochloride extended-release tablets (e.g., Wellbutrin(R) XL, Forfivo XL(R) ) include dry mouth, nausea, insomnia, dizziness, pharyngitis, abdominal pain, agitation, anxiety, tremor, palpitation, sweating, tinnitus, myalgia, anorexia, urinary frequency, and rash.

Adverse effects reported in >=5% of patients receiving bupropion hydrobromide extended-release tablets (e.g., Aplenzin(R)) include dry mouth, nausea, insomnia, dizziness, pharyngitis, abdominal pain, agitation, anxiety, tremor, palpitation, sweating, tinnitus, myalgia, anorexia, urinary frequency, and rash.

There are no severe adverse reactions for this drug.

There are no less severe adverse reactions for this drug.

No enhanced messaging available.

Safety and efficacy of bupropion have not been established in children <18 years of age.

FDA warns that a greater risk of suicidal thinking or behavior (suicidality) occurred during first few months of antidepressant treatment compared with placebo in children and adolescents with major depressive disorder, OCD, or other psychiatric disorders based on pooled analyses of 24 short-term, placebo-controlled trials of 9 antidepressant drugs (SSRIs and others). However, a later meta-analysis of 27 placebo-controlled trials of 9 antidepressants (SSRIs and others) in patients <19 years of age with major depressive disorder, OCD, or non-OCD anxiety disorders suggests that the benefits of antidepressant therapy in treating these conditions may outweigh the risks of suicidal behavior or suicidal ideation. No suicides occurred in these pediatric trials.

Carefully consider these findings when assessing potential benefits and risks of bupropion in a child or adolescent for any clinical use.

Data from epidemiologic studies, including the international bupropion pregnancy registry (675 first-trimester exposures) and a retrospective cohort study using the United Healthcare database (1213 first-trimester exposures), have not shown an overall increased risk for congenital malformations associated with bupropion. The pregnancy registry was not designed or powered to evaluate specific defects; however, a possible increase in cardiac malformations was identified. There also are risks to the mother associated with untreated depression in pregnancy.

When bupropion was administered to pregnant rats during organogenesis at doses up to approximately 11 times the maximum recommended human dose (MRHD) of 400 mg daily, no evidence of fetal malformations was observed. When administered to pregnant rabbits during organogenesis at doses greater than and approximately equal to the MRHD, non-dose-related increases in the incidence of fetal malformations, and skeletal variations, were observed; decreased fetal weights were observed at doses >=2 times the MRHD.

The National Pregnancy Registry for Antidepressants, an independent pregnancy exposure registry that monitors pregnancy outcomes in females exposed to antidepressants during pregnancy, is available at 1-844-405-6185 or https://womensmentalhealth.org/research/pregnancyregistry/antidepressants.

Consider the risks to the pregnant female of untreated depression and potential effects on the fetus when discontinuing or changing treatment with antidepressant medications during pregnancy and postpartum.

Pregnant smokers should be encouraged to attempt smoking cessation using educational and behavioral interventions before drug approaches are used. Bupropion extended-release (SR) tablets should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Bupropion and its metabolites are distributed into human milk. The effects of bupropion or its metabolites on milk production are not known.

Limited data from postmarketing reports of bupropion use in nursing females have not identified a clear association of adverse reactions in the breast-fed infant. Postmarketing reports have described seizures in breast-fed infants; however, the relationship of bupropion exposure and these seizures is unclear.

Consider developmental and health benefits of breast-feeding along with the mother's clinical need for bupropion and any potential adverse effects on the breast-fed child from the drug or underlying maternal condition.

Caution should be used when administering bupropion to geriatric patients. Due to age-related decreases in renal function, dosage reduction should be considered and renal function should be monitored.

Of the approximately 6000 patients studied in clinical trials of extended-release bupropion hydrochloride for smoking cessation or depression, 275 were >=65 years of age, while 47 were >=75 years of age. In addition, several hundred patients >=65 years of age participated in clinical studies using conventional bupropion hydrochloride tablets for depression. Although no overall differences in efficacy or safety were observed between geriatric and younger patients, and other clinical experience revealed no evidence of age-related differences, the possibility that some older patients may exhibit increased sensitivity to the drug cannot be ruled out. In general, smoking cessation interventions that have been shown to be effective in the general population also have been shown to be effective in adults >=50 years of age.

The risk of adverse reactions may be increased in patients with impaired renal function. The possibility of decreased renal function in geriatric patients should be considered in dose selection; consider monitoring renal function in geriatric patients.

In pooled data analyses, a reduced risk of suicidality was observed in adults >=65 years of age with antidepressant therapy compared with placebo.