Bupropion Hydrochloride (sr)
Bupropion Hydrochloride · Tablet, Extended Release · Oral
Uses
Bupropion hydrochloride extended-release tablets, USP (SR) are indicated as an aid to smoking cessation treatment. Bupropion hydrochloride extended-release tablets, USP (SR) are an aminoketone agent indicated as an aid to smoking cessation treatment. ( 1 )
Dosage and administration
Starting dose: 150 mg per day for first 3 days. ( 2.1 ) General: Increase dose gradually to reduce seizure risk. ( 2.1 , 5.3 ) Begin dosing one week before quit day. ( 2.1 ) After 3 days, increase the dose to 300 mg per day, given as 150 mg twice daily at an interval of at least 8 hours. ( 2.1 ) May be used with a nicotine transdermal system. ( 2.5 ) Moderate to severe hepatic impairment: 150 mg every other day. ( 2.6 , 8.7 ) Mild hepatic impairment: Consider reducing the dose and/or frequency of dosing. ( 2.6 , 8.7 ) Renal impairment: Consider reducing the dose and/or frequency. ( 2.7 , 8.6 ) 2.1 Usual Dosage Treatment with bupropion hydrochloride extended-release tablets (SR) 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 bupropion hydrochloride extended-release tablets (SR). Dosing To minimize the risk of seizure: Begin dosing with one 150-mg tablet per day for 3 days. Increase dose to 300 mg per 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 per day. Bupropion hydrochloride extended-release tablets (SR) 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) ]. Bupropion hydrochloride extended-release tablets (SR) may be taken with or without food [see Clinical Pharmacology (12.3) ]. 2.2 Duration of Treatment Treatment with bupropion hydrochloride extended-release tablets (SR) 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 bupropion hydrochloride extended-release tablets (SR) should probably be discontinued and the treatment plan reassessed. The goal of therapy with bupropion hydrochloride extended-release tablets (SR) is complete abstinence. Discuss discontinuing treatment with bupropion hydrochloride extended-release tablets (SR) 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 bupropion hydrochloride extended-release tablets (SR); 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 bupropion hydrochloride extended-release tablets (SR) and for a period of time thereafter. 2.3 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 bupropion hydrochloride extended-release tablets (SR). 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 hydrochloride extended-release tablets (SR) [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. 2.4 Maintenance Tobacco dependence is a chronic condition. Some patients may need on-going treatment. Whether to continue treatment with bupropion hydrochloride extended-release tablets (SR) for periods longer than 12 weeks for smoking cessation must be determined for individual patients. 2.5 Combination Treatment with Bupropion Hydrochloride Extended-Release Tablets (SR) and a Nicotine Transdermal System (NTS) Combination treatment with bupropion hydrochloride extended-release tablets (SR) and NTS may be prescribed for smoking cessation. The prescriber should review the complete prescribing information for both bupropion hydrochloride extended-release tablets (SR) and NTS before using combination treatment [see Clinical Studies (14) ]. Monitoring for treatment-emergent hypertension in patients treated with the combination of bupropion hydrochloride extended-release tablets (SR) and NTS is recommended. 2.6 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) , Clinical Pharmacology (12.3) ]. 2.7 Dose Adjustment in Patients with Renal Impairment Consider reducing the dose and/or frequency of bupropion hydrochloride extended-release tablets (SR) in patients with renal impairment (Glomerular Filtration Rate less than 90 mL per min) [see Use in Specific Populations (8.6) , Clinical Pharmacology (12.3) ]. 2.8 Use of Bupropion Hydrochloride Extended-Release Tablets (SR) with Reversible MAOIs Such as Linezolid or Methylene Blue Do not start bupropion hydrochloride extended-release tablets (SR) 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) , Drug Interactions (7.6) ].
Dosage forms and strengths
150 mg - purple, round, biconvex, film coated tablets, debossed with ‘SG, 338’ on one side and plain on other side. Tablets: 150 mg. ( 3 )
Contraindications
Bupropion hydrochloride extended-release tablets (SR) are contraindicated in patients with a seizure disorder. Bupropion hydrochloride extended-release tablets (SR) are contraindicated in patients with a current or prior diagnosis of bulimia or anorexia nervosa as a higher incidence of seizures was observed in such patients treated with the immediate-release formulation of bupropion [see Warnings and Precautions (5.3) ]. Bupropion hydrochloride extended-release tablets (SR) are contraindicated in patients undergoing abrupt discontinuation of alcohol, benzodiazepines, barbiturates, and antiepileptic drugs [see Warnings and Precautions (5.3) , Drug Interactions (7.3) ]. The use of MAOIs (intended to treat psychiatric disorders) concomitantly with bupropion hydrochloride extended-release tablets (SR) or within 14 days of discontinuing treatment with bupropion hydrochloride extended-release tablets (SR) are contraindicated. There is an increased risk of hypertensive reactions when bupropion hydrochloride extended-release tablets (SR) are used concomitantly with MAOIs. The use of bupropion hydrochloride extended-release tablets (SR) within 14 days of discontinuing treatment with an MAOI is also contraindicated. Starting bupropion in a patient treated with reversible MAOIs such as linezolid or intravenous methylene blue is contraindicated [see Dosage and Administration (2.8) , Warnings and Precautions (5.4) , Drug Interactions (7.6) ]. Bupropion hydrochloride extended-release tablets (SR) are contraindicated in patients with a known hypersensitivity to bupropion or other ingredients of bupropion hydrochloride extended-release tablets (SR). Anaphylactoid/anaphylactic reactions and Stevens-Johnson syndrome have been reported [see Warnings and Precautions (5.8) ]. Seizure disorder. ( 4 , 5.3 ) Current or prior diagnosis of bulimia or anorexia nervosa. ( 4 , 5.3 ) Abrupt discontinuation of alcohol, benzodiazepines, barbiturates, antiepileptic drugs. ( 4 , 5.3 ) Monoamine Oxidase Inhibitors (MAOIs): Do not use MAOIs intended to treat psychiatric disorders with bupropion hydrochloride extended-release tablets (SR) or within 14 days of stopping treatment with bupropion hydrochloride extended-release tablets (SR). Do not use bupropion hydrochloride extended-release tablets (SR) within 14 days of stopping an MAOI intended to treat psychiatric disorders. In addition, do not start bupropion hydrochloride extended-release tablets (SR) in a patient who is being treated with linezolid or intravenous methylene blue. ( 4 , 7.6 ) Known hypersensitivity to bupropion or other ingredients of bupropion hydrochloride extended-release tablets, (SR). ( 4 , 5.8 )
Warnings and precautions
Neuropsychiatric adverse events: Postmarketing reports of serious or clinically significant neuropsychiatric adverse events have included changes in mood (including depression and mania), psychosis, hallucinations, paranoia, delusions, homicidal ideation, aggression, hostility, agitation, anxiety, and panic, as well as suicidal ideation, suicide attempt, and completed suicide. Observe patients attempting to quit smoking with Bupropion hydrochloride extended-release tablets, USP (SR) for the occurrence of such symptoms and instruct them to discontinue Bupropion hydrochloride extended-release tablets, USP (SR) and contact a healthcare provider if they experience such adverse events. ( 5.2 ) Seizure risk: The risk is dose-related. Can minimize risk by gradually increasing the dose and limiting daily dose to 300 mg. Discontinue if seizure occurs. ( 4 , 5.3 , 7.3 ) Hypertension: Bupropion hydrochloride extended-release tablets (SR) can increase blood pressure. Monitor blood pressure before initiating treatment and periodically during treatment, especially if used with nicotine replacement. ( 5.4 ) Activation of mania/hypomania: Screen patients for bipolar disorder and monitor for these symptoms. ( 5.5 ) Psychosis and other neuropsychiatric reactions. Instruct patients to contact a healthcare professional if reactions occur. ( 5.6 ) Angle-closure glaucoma: Angle-closure glaucoma has occurred in patients with untreated anatomically narrow angles treated with antidepressants. ( 5.7 ) 5.1 Suicidal Thoughts and Behaviors in Children, Adolescents, and Young Adults Although Bupropion hydrochloride extended-release tablets (SR) are not indicated for treatment of depression, it contains the same active ingredient as the antidepressant medications WELLBUTRIN, WELLBUTRIN SR, and WELLBUTRIN XL. Antidepressants increased the risk of suicidal thoughts and behavior in children, adolescents, and young adults in short-term trials. Patients with major depressive disorder (MDD), both adult and pediatric, may experience worsening of their depression and/or the emergence of suicidal ideation and behavior (suicidality) or unusual changes in behavior, whether or not they are taking antidepressant medications, and this risk may persist until significant remission occurs. Suicide is a known risk of depression and certain other psychiatric disorders, and these disorders themselves are the strongest predictors of suicide. There has been a long-standing concern that antidepressants may have a role in inducing worsening of depression and the emergence of suicidality in certain patients during the early phases of treatment. Pooled analyses of short-term placebo-controlled trials of antidepressant drugs (selective serotonin reuptake inhibitors [SSRIs] and others) show that these drugs increase the risk of suicidal thinking and behavior (suicidality) in children, adolescents, and young adults (ages 18 to 24) with MDD and other psychiatric disorders. Short-term clinical trials did not show an increase in the risk of suicidality with antidepressants compared with placebo in adults beyond age 24; there was a reduction with antidepressants compared with placebo in adults aged 65 and older. The pooled analyses of placebo-controlled trials in children and adolescents with MDD, obsessive compulsive disorder (OCD), or other psychiatric disorders included a total of 24 short-term trials of 9 antidepressant drugs in over 4,400 subjects. The pooled analyses of placebo-controlled trials in adults with MDD or other psychiatric disorders included a total of 295 short-term trials (median duration of 2 months) of 11 antidepressant drugs in over 77,000 subjects. There was considerable variation in risk of suicidality among drugs, but a tendency toward an increase in the younger subjects for almost all drugs studied. There were differences in absolute risk of suicidality across the different indications, with the highest incidence in MDD. The risk differences (drug vs. placebo), however, were relatively stable within age strata and across indications. These risk differences (drug-placebo difference in the number of cases of suicidality per 1,000 subjects treated) are provided in Table 1. Table 1. Risk Differences in the Number of Suicidality Cases by Age Group in the Pooled Placebo-controlled Trials of Antidepressants in Pediatric and Adult Subjects Age Range Drug-Placebo Difference in Number of Cases of Suicidality per 1,000 Subjects Treated Increases Compared With Placebo <18 14 additional cases 18-24 5 additional cases Decreases Compared With Placebo 25-64 1 fewer case ≥ 65 6 fewer cases No suicides occurred in any of the pediatric trials. There were suicides in the adult trials, but the number was not sufficient to reach any conclusion about drug effect on suicide. It is unknown whether the suicidality risk extends to longer-term use, i.e., beyond several months. However, there is substantial evidence from placebo-controlled maintenance trials in adults with depression that the use of antidepressants can delay the recurrence of depression. All patients being treated with antidepressants for any indication should be monitored appropriately and observed closely for clinical worsening, suicidality, and unusual changes in behavior, especially during the initial few months of a course of drug therapy, or at times of dose changes, either increases or decreases [see Boxed Warning ] . The following symptoms, anxiety, agitation, panic attacks, insomnia, irritability, hostility, aggressiveness, impulsivity, akathisia (psychomotor restlessness), hypomania, and mania, have been reported in adult and pediatric patients being treated with antidepressants for major depressive disorder as well as for other indications, both psychiatric and nonpsychiatric.
Side effects
The following adverse reactions are discussed in greater detail in other sections of the labeling: Suicidal thoughts and behaviors in adolescents and young adults [see Boxed Warning , Warnings and Precautions (5.1) ] Neuropsychiatric adverse events and suicide risk in smoking cessation treatment [see Warnings and Precautions (5.2) ] Seizure [see Warnings and Precautions (5.3) ] Hypertension [see Warnings and Precautions (5.4) ] Activation of mania or hypomania [see Warnings and Precautions (5.5) ] Psychosis and other neuropsychiatric reactions [see Warnings and Precautions (5.6) ] Angle-closure glaucoma [see Warnings and Precautions (5.7) ] Hypersensitivity reactions [see Warnings and Precautions (5.8) ] Most common adverse reactions (incidence ≥5% and ≥1% more than placebo rate) are: insomnia, rhinitis, dry mouth, dizziness, nervous disturbance, anxiety, nausea, constipation, and arthralgia. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Dr. Reddy’s Laboratories Inc., at 1-888-375-3784 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, 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 Leading to Discontinuation of Treatment Adverse reactions were sufficiently troublesome to cause discontinuation of treatment in 8% of the 706 subjects treated with bupropion hydrochloride extended-release tablets (SR) and 5% of the 313 patients treated with placebo. The more common events leading to discontinuation of treatment with bupropion hydrochloride extended-release tablets (SR) included nervous system disturbances (3.4%), primarily tremors, and skin disorders (2.4%), primarily rashes. Commonly Observed Adverse Reactions The most commonly observed adverse reactions consistently associated with the use of bupropion hydrochloride extended-release tablets (SR) were dry mouth and insomnia. The incidence of dry mouth and insomnia may be related to the dose of bupropion hydrochloride extended-release tablets (SR). The occurrence of these adverse reactions may be minimized by reducing the dose of bupropion hydrochloride extended-release tablets (SR). 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 Adverse Reaction Bupropion Hydrochloride Extended-Release Tablets (SR) 100 to 300 mg/day (n = 461) % Placebo (n = 150) % Body (General) Neck pain 2 ˂1 Allergic reaction 1 0 Cardiovascular Hot flashes 1 0 Hypertension 1 ˂1 Digestive Dry mouth 11 5 Increased appetite 2 ˂1 Anorexia 1 ˂1 Musculoskeletal Arthralgia 4 3 Myalgia 2 ˂1 Nervous system Insomnia 31 21 Dizziness 8 7 Tremor 2 1 Somnolence 2 1 Thinking abnormality 1 0 Respiratory Bronchitis 2 0 Skin Pruritus 3 ˂1 Rash 3 ˂1 Dry skin 2 0 Urticaria 1 0 Special senses Taste perversion 2 ˂1 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 a Subjects randomized to bupropion hydrochloride extended-release tablets (SR) or placebo received placebo patches. Adverse Experience (COSTART Term) Bupropion Hydrochloride Extended- Release Tablets (SR) 300 mg/day (n = 243) % Nicotine Transdermal System (NTS) 21 mg/day (n = 243) % Bupropion Hydrochloride Extended- Release Tablets (SR) and NTS (n = 244) % Placebo (n = 159) % Body Abdominal pain 3 4 1 1 Accidental injury 2 2 1 1 Chest pain ˂1 1 3 1 Neck pain 2 1 ˂1 0 Facial edema ˂1 0 1 0 Cardiovascular Hypertension 1 ˂1 2 0 Palpitations 2 0 1 0 Digestive Nausea 9 7 11 4 Dry mouth 10 4 9 4 Constipation 8 4 9 3 Diarrhea 4 4 3 1 Anorexia 3 1 5 1 Mouth ulcer 2 1 1 1 Thirst ˂1 ˂1 2 0 Musculoskeletal Myalgia 4 3 5 3 Arthralgia 5 3 3 2 Nervous system Insomnia 40 28 45 18 Dream abnormality 5 18 13 3 Anxiety 8 6 9 6 Disturbed concentration 9 3 9 4 Dizziness 10 2 8 6 Nervousness 4 ˂1 2 2 Tremor 1 ˂1 2 0 Dysphoria ˂1 1 2 1 Respiratory Rhinitis 12 11 9 8 Increased cough 3 5 ˂1 1 Pharyngitis 3 2 3 0 Sinusitis 2 2 2 1 Dyspnea 1 0 2 1 Epistaxis 2 1 1 0 Skin Application site reaction a 11 17 15 7 Rash 4 3 3 2 Pruritus 3 1 5 1 Urticaria 2 0 2 0 Special senses Taste perversion 3 1 3 2 Tinnitus 1 0 ˂1 0 Adverse reactions in a 1-year maintenance trial and a 12-week COPD trial with bupropion hydrochloride extended-release tablets (SR) were quantitatively and qualitatively similar to those observed in the dose-response and comparator trials. In the trial of patients without or with a history of psychiatric disorder, the most common adverse events in subjects treated with bupropion hydrochloride extended-release tablets (SR) were broadly similar to those observed in premarketing studies. Adverse events reported in >10% of subjects treated with bupropion hydrochloride extended-release tablets (SR) in the entire study population were nausea, insomnia, and anxiety disorders. Additionally, the following psychiatric adverse events were reported in >2% of patients in either treatment group (bupropion hydrochloride extended-release tablets (SR) vs. placebo) by cohort. For the non-psychiatric cohort, these adverse events were anxiety, nervousness, abnormal dreams, and insomnia. For the psychiatric cohort, these adverse events were agitation, anxiety, panic, abnormal dreams, insomnia, and crying.
Drug interactions
7 DRUG INTERACTIONS CYP2B6 inducers: Dose increase may be necessary if coadministered with CYP2B6 inducers (e.g., ritonavir, lopinavir, efavirenz, carbamazepine, phenobarbital and phenytoin) based on clinical response, but should not exceed the maximum recommended dose. ( 7.1 ) Drugs metabolized by CYP2D6: Bupropion inhibits CYP2D6 and can increase concentrations of: antidepressants (e.g., venlafaxine, nortriptyline, imipramine, desipramine, paroxetine, fluoxetine, sertraline), antipsychotics (e.g., haloperidol, risperidone, thioridazine), beta-blockers (e.g., metoprolol), and Type 1C antiarrhythmics (e.g., propafenone, flecainide). Consider dose reduction when using with bupropion. ( 7.2 ) Digoxin: May decrease plasma digoxin levels. Monitor digoxin levels. ( 7.2 ) Drugs that lower seizure threshold: Dose bupropion hydrochloride extended-release tablets (SR) with caution. ( 5.3 , 7.3 ) Dopaminergic drugs (levodopa and amantadine): Central nervous system (CNS) toxicity can occur when used concomitantly with bupropion hydrochloride extended-release tablets (SR). ( 7.4 ) MAOIs: Increased risk of hypertensive reactions can occur when used concomitantly with bupropion hydrochloride extended-release tablets (SR). ( 7.6 ) Drug-laboratory test interactions: Bupropion hydrochloride extended-release tablets (SR) can cause false-positive urine test results for amphetamines. ( 7.8 ) 7.1 Potential for Other Drugs to Affect Bupropion Hydrochloride Extended- Release Tablets (SR) Bupropion is primarily metabolized to hydroxybupropion by CYP2B6. Therefore, the potential exists for drug interactions between bupropion hydrochloride extended-release tablets (SR) and drugs that are inhibitors or inducers of CYP2B6. Inhibitors of CYP2B6 Ticlopidine and Clopidogrel : Concomitant treatment with these drugs can increase bupropion exposure but decrease hydroxybupropion exposure. Based on clinical response, dosage adjustment of bupropion hydrochloride extended-release tablets (SR) may be necessary when coadministered with CYP2B6 inhibitors (e.g., ticlopidine or clopidogrel) [see Clinical Pharmacology (12.3) ] . Inducers of CYP2B6 Ritonavir, Lopinavir, and Efavirenz: Concomitant treatment with these drugs can decrease bupropion and hydroxybupropion exposure. Dosage increase of bupropion hydrochloride extended-release tablets (SR) may be necessary when coadministered with ritonavir, lopinavir, or efavirenz [see Clinical Pharmacology (12.3) ] but should not exceed the maximum recommended dose. Carbamazepine, Phenobarbital, Phenytoin: While not systematically studied, these drugs may induce the metabolism of bupropion and may decrease bupropion exposure [see Clinical Pharmacology (12.3) ] . If bupropion is used concomitantly with a CYP inducer, it may be necessary to increase the dose of bupropion, but the maximum recommended dose should not be exceeded. 7.2 Potential for Bupropion Hydrochloride Extended- Release Tablets (SR) to Affect Other Drugs Drugs Metabolized by CYP2D6 Bupropion and its metabolites (erythrohydrobupropion, threohydrobupropion, hydroxybupropion) are CYP2D6 inhibitors. Therefore, coadministration of bupropion hydrochloride extended-release tablets (SR) with drugs that are metabolized by CYP2D6 can increase the exposures of drugs that are substrates of CYP2D6. Such drugs include certain antidepressants (e.g., venlafaxine, nortriptyline, imipramine, desipramine, paroxetine, fluoxetine, and sertraline), antipsychotics (e.g., haloperidol, risperidone, thioridazine), beta-blockers (e.g., metoprolol), and Type 1C antiarrhythmics (e.g., propafenone and flecainide). When used concomitantly with bupropion hydrochloride extended-release tablets (SR), it may be necessary to decrease the dose of these CYP2D6 substrates, particularly for drugs with a narrow therapeutic index. Drugs that require metabolic activation by CYP2D6 to be effective (e.g., tamoxifen) theoretically could have reduced efficacy when administered concomitantly with inhibitors of CYP2D6 such as bupropion. Patients treated concomitantly with bupropion hydrochloride extended-release tablets (SR) and such drugs may require increased doses of the drug [see Clinical Pharmacology (12.3) ] . Digoxin Coadministration of bupropion hydrochloride extended-release tablets (SR) with digoxin may decrease plasma digoxin levels. Monitor plasma digoxin levels in patients treated concomitantly with bupropion hydrochloride extended-release tablets (SR) and digoxin [see Clinical Pharmacology (12.3) ] . 7.3 Drugs that Lower Seizure Threshold Use extreme caution when coadministering bupropion hydrochloride extended-release tablets (SR) with other drugs that lower seizure threshold (e.g., other bupropion products, antipsychotics, antidepressants, theophylline, or systemic corticosteroids). Use low initial doses and increase the dose gradually [see Contraindications (4) , Warnings and Precautions (5.3) ] . 7.4 Dopaminergic Drugs (Levodopa and Amantadine) Bupropion, levodopa, and amantadine have dopamine agonist effects. CNS toxicity has been reported when bupropion was coadministered with levodopa or amantadine. Adverse reactions have included restlessness, agitation, tremor, ataxia, gait disturbance, vertigo, and dizziness. It is presumed that the toxicity results from cumulative dopamine agonist effects. Use caution when administering bupropion hydrochloride extended-release tablets (SR) concomitantly with these drugs. 7.5 Use with Alcohol In postmarketing experience, there have been rare reports of adverse neuropsychiatric events or reduced alcohol tolerance in patients who were drinking alcohol during treatment with bupropion hydrochloride extended-release tablets (SR). The consumption of alcohol during treatment with bupropion hydrochloride extended-release tablets (SR) should be minimized or avoided. 7.6 MAO Inhibitors Bupropion inhibits the reuptake of dopamine and norepinephrine.
Use in specific populations
Pregnancy: Use only if benefit outweighs potential risk to the fetus. ( 8.1 ) 8.1 Pregnancy Pregnancy Category C. Risk Summary Data from epidemiological studies of pregnant women exposed to bupropion in the first trimester indicate no increased risk of congenital malformations overall. All pregnancies, regardless of drug exposure, have a background rate of 2% to 4% for major malformations, and 15% to 20% for pregnancy loss. No clear evidence of teratogenic activity was found in reproductive developmental studies conducted in rats and rabbits; however, in rabbits, slightly increased incidences of fetal malformations and skeletal variations were observed at doses approximately 2 times the maximum recommended human dose (MRHD) and greater and decreased fetal weights were seen at doses three times the MRHD and greater. Bupropion hydrochloride extended-release tablets (SR) should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Clinical Considerations Pregnant smokers should be encouraged to attempt cessation using educational and behavioral interventions before pharmacological approaches are used. Data Human Data: Data from the international bupropion Pregnancy Registry (675 first trimester exposures) and a retrospective cohort study using the United Healthcare database (1,213 first trimester exposures) did not show an increased risk for malformations overall. No increased risk for cardiovascular malformations overall has been observed after bupropion exposure during the first trimester. The prospectively observed rate of cardiovascular malformations in pregnancies with exposure to bupropion in the first trimester from the international Pregnancy Registry was 1.3% (9 cardiovascular malformations/675 first trimester maternal bupropion exposures), which is similar to the background rate of cardiovascular malformations (approximately 1%). Data from the United Healthcare database and a case-control study (6,853 infants with cardiovascular malformations and 5,763 with non-cardiovascular malformations) from the National Birth Defects Prevention Study (NBDPS) did not show an increased risk for cardiovascular malformations overall after bupropion exposure during the first trimester. Study findings on bupropion exposure during the first trimester and risk for left ventricular outflow tract obstruction (LVOTO) are inconsistent and do not allow conclusions regarding a possible association. The United Healthcare database lacked sufficient power to evaluate this association; the NBDPS found increased risk for LVOTO (n = 10; adjusted OR = 2.6; 95% CI: 1.2, 5.7), and the Slone Epidemiology case control study did not find increased risk for LVOTO. Study findings on bupropion exposure during the first trimester and risk for ventricular septal defect (VSD) are inconsistent and do not allow conclusions regarding a possible association. The Slone Epidemiology Study found an increased risk for VSD following first trimester maternal bupropion exposure (n = 17; adjusted OR = 2.5; 95% CI: 1.3, 5.0) but did not find increased risk for any other cardiovascular malformations studied (including LVOTO as above). The NBDPS and United Healthcare database study did not find an association between first trimester maternal bupropion exposure and VSD. For the findings of LVOTO and VSD, the studies were limited by the small number of exposed cases, inconsistent findings among studies, and the potential for chance findings from multiple comparisons in case control studies. Animal Data : In studies conducted in rats and rabbits, bupropion was administered orally during the period of organogenesis at doses of up to 450 and 150 mg per kg per day, respectively (approximately 15 and 10 times the MRHD respectively, on a mg per m 2 basis). No clear evidence of teratogenic activity was found in either species; however, in rabbits, slightly increased incidences of fetal malformations and skeletal variations were observed at the lowest dose tested (25 mg per kg per day, approximately 2 times the MRHD on a mg per m 2 basis) and greater. Decreased fetal weights were observed at 50 mg per kg and greater. When rats were administered bupropion at oral doses of up to 300 mg per kg per day (approximately 10 times the MRHD on a mg per m 2 basis) prior to mating and throughout pregnancy and lactation, there were no apparent adverse effects on offspring development. 8.3 Nursing Mothers Bupropion and its metabolites are present in human milk. In a lactation study of 10 women, levels of orally dosed bupropion and its active metabolites were measured in expressed milk. The average daily infant exposure (assuming 150 mL per kg daily consumption) to bupropion and its active metabolites was 2% of the maternal weight-adjusted dose. Exercise caution when bupropion hydrochloride extended-release tablets (SR) is administered to a nursing woman. 8.4 Pediatric Use Safety and effectiveness in the pediatric population have not been established [see Boxed Warning , Warnings and Precautions (5.1) ]. 8.5 Geriatric Use Of the approximately 6,000 subjects who participated in clinical trials with bupropion sustained-release tablets (depression and smoking cessation trials), 275 were aged ≥65 years and 47 were aged ≥75 years. In addition, several hundred subjects aged ≥65 years participated in clinical trials using the immediate-release formulation of bupropion (depression trials). No overall differences in safety or effectiveness were observed between these subjects and younger subjects. 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. Bupropion is extensively metabolized in the liver to active metabolites, which are further metabolized and excreted by the kidneys. The risk of adverse reactions may be greater in patients with impaired renal function.
Pregnancy
8.1 Pregnancy Pregnancy Category C. Risk Summary Data from epidemiological studies of pregnant women exposed to bupropion in the first trimester indicate no increased risk of congenital malformations overall. All pregnancies, regardless of drug exposure, have a background rate of 2% to 4% for major malformations, and 15% to 20% for pregnancy loss. No clear evidence of teratogenic activity was found in reproductive developmental studies conducted in rats and rabbits; however, in rabbits, slightly increased incidences of fetal malformations and skeletal variations were observed at doses approximately 2 times the maximum recommended human dose (MRHD) and greater and decreased fetal weights were seen at doses three times the MRHD and greater. Bupropion hydrochloride extended-release tablets (SR) should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Clinical Considerations Pregnant smokers should be encouraged to attempt cessation using educational and behavioral interventions before pharmacological approaches are used. Data Human Data: Data from the international bupropion Pregnancy Registry (675 first trimester exposures) and a retrospective cohort study using the United Healthcare database (1,213 first trimester exposures) did not show an increased risk for malformations overall. No increased risk for cardiovascular malformations overall has been observed after bupropion exposure during the first trimester. The prospectively observed rate of cardiovascular malformations in pregnancies with exposure to bupropion in the first trimester from the international Pregnancy Registry was 1.3% (9 cardiovascular malformations/675 first trimester maternal bupropion exposures), which is similar to the background rate of cardiovascular malformations (approximately 1%). Data from the United Healthcare database and a case-control study (6,853 infants with cardiovascular malformations and 5,763 with non-cardiovascular malformations) from the National Birth Defects Prevention Study (NBDPS) did not show an increased risk for cardiovascular malformations overall after bupropion exposure during the first trimester. Study findings on bupropion exposure during the first trimester and risk for left ventricular outflow tract obstruction (LVOTO) are inconsistent and do not allow conclusions regarding a possible association. The United Healthcare database lacked sufficient power to evaluate this association; the NBDPS found increased risk for LVOTO (n = 10; adjusted OR = 2.6; 95% CI: 1.2, 5.7), and the Slone Epidemiology case control study did not find increased risk for LVOTO. Study findings on bupropion exposure during the first trimester and risk for ventricular septal defect (VSD) are inconsistent and do not allow conclusions regarding a possible association. The Slone Epidemiology Study found an increased risk for VSD following first trimester maternal bupropion exposure (n = 17; adjusted OR = 2.5; 95% CI: 1.3, 5.0) but did not find increased risk for any other cardiovascular malformations studied (including LVOTO as above). The NBDPS and United Healthcare database study did not find an association between first trimester maternal bupropion exposure and VSD. For the findings of LVOTO and VSD, the studies were limited by the small number of exposed cases, inconsistent findings among studies, and the potential for chance findings from multiple comparisons in case control studies. Animal Data : In studies conducted in rats and rabbits, bupropion was administered orally during the period of organogenesis at doses of up to 450 and 150 mg per kg per day, respectively (approximately 15 and 10 times the MRHD respectively, on a mg per m 2 basis). No clear evidence of teratogenic activity was found in either species; however, in rabbits, slightly increased incidences of fetal malformations and skeletal variations were observed at the lowest dose tested (25 mg per kg per day, approximately 2 times the MRHD on a mg per m 2 basis) and greater. Decreased fetal weights were observed at 50 mg per kg and greater. When rats were administered bupropion at oral doses of up to 300 mg per kg per day (approximately 10 times the MRHD on a mg per m 2 basis) prior to mating and throughout pregnancy and lactation, there were no apparent adverse effects on offspring development.
Pediatric use
8.4 Pediatric Use Safety and effectiveness in the pediatric population have not been established [see Boxed Warning , Warnings and Precautions (5.1) ].
Geriatric use
8.5 Geriatric Use Of the approximately 6,000 subjects who participated in clinical trials with bupropion sustained-release tablets (depression and smoking cessation trials), 275 were aged ≥65 years and 47 were aged ≥75 years. In addition, several hundred subjects aged ≥65 years participated in clinical trials using the immediate-release formulation of bupropion (depression trials). No overall differences in safety or effectiveness were observed between these subjects and younger subjects. 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. Bupropion is extensively metabolized in the liver to active metabolites, which are further metabolized and excreted by the kidneys. The risk of adverse reactions may be greater in patients with impaired renal function. Because elderly patients are more likely to have decreased renal function, it may be necessary to consider this factor in dose selection; it may be useful to monitor renal function [see Dosage and Administration (2.7) , Use in Specific Populations (8.6) , Clinical Pharmacology (12.3) ].
Overdosage
10.1 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, mental status changes, sinus tachycardia, ECG changes such as conduction disturbances (including QRS prolongation) or arrhythmias, clonus, myoclonus, and hyperreflexia. 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. 10.2 Overdosage Management Consult a Certified Poison Control Center for up–to-date guidance and advice. 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.
Description
Bupropion hydrochloride extended-release tablets, USP (SR) are a non-nicotine aid to smoking cessation. Bupropion is chemically unrelated to nicotine or other agents currently used in the treatment of nicotine addiction. Initially developed and marketed as an antidepressant (WELLBUTRIN [bupropion hydrochloride] tablets and WELLBUTRIN SR [bupropion hydrochloride] sustained-release tablets), Bupropion hydrochloride extended-release tablets, USP (SR) is also 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 molecular formula is C 13 H 18 ClNO
• HCl. Bupropion hydrochloride USP is white powder, and soluble in 0.1N Hydrochloric acid, in alcohol (96.0%) and in water. It has a bitter taste and produces the sensation of local anesthesia on the oral mucosa. The structural formula is: Bupropion hydrochloride extended-release tablets, USP (SR) are supplied for oral administration as 150-mg (purple), film-coated, sustained-release tablets. Each tablet contains the labeled amount of bupropion hydrochloride USP and the inactive ingredients: copovidone, cysteine hydrochloride, hypromellose, magnesium stearate, microcrystalline cellulose, polyethylene glycol, polysorbate 80, titanium dioxide, FD&C Blue No.2 Lake and FD&C Red No. 40 Lake. In addition, flavoring agent contains dextrose, ethyl alcohol, gum arabic, propylene glycol and silicon dioxide. Bupropion hydrochloride extended-release tablets, USP (SR) meets USP dissolution Test 2. Chemical Structure
Mechanism of action
12.1 Mechanism of Action The exact mechanism by which bupropion hydrochloride extended-release tablets, (SR) enhances the ability of patients to abstain from smoking is not known but is presumed to be related to noradrenergic and/or dopaminergic mechanisms. Bupropion is a relatively weak inhibitor of the neuronal reuptake of norepinephrine and dopamine, and does not inhibit the reuptake of serotonin. Bupropion does not inhibit monoamine oxidase.
How supplied
Bupropion hydrochloride extended-release tablets, USP (SR) 150 mg of bupropion hydrochloride, are purple, blackberry flavored, round, biconvex, film coated tablets debossed with ‘SG, 338’ on one side and plain on other side and supplied in bottles of 30 tablets (NDC 43598-863-30), 60 tablets (NDC 43598-863-60) and 1,000 tablets (NDC 43598-863-10). Store at room temperature, 20° to 25°C (68° to 77°F); excursions permitted between 15°C and 30°C (59°F and 86°F) [see USP Controlled Room Temperature]. Protect from light and moisture.
Patient information
Advise the patient to read the FDA-approved patient labeling (Medication Guide). Suicidal Thoughts and Behaviors Instruct patients, their families, and/or their caregivers to be alert to the emergence of anxiety, agitation, panic attacks, insomnia, irritability, hostility, aggressiveness, impulsivity, akathisia (psychomotor restlessness), hypomania, mania, other unusual changes in behavior, worsening of depression, and suicidal ideation, especially early during antidepressant treatment and when the dose is adjusted up or down. Advise families and caregivers of patients to observe for the emergence of such symptoms on a day–to-day basis, since changes may be abrupt. Such symptoms should be reported to the patient’s prescriber or healthcare professional, especially if they are severe, abrupt in onset, or were not part of the patient’s presenting symptoms. Symptoms such as these may be associated with an increased risk for suicidal thinking and behavior and indicate a need for very close monitoring and possibly changes in the medication. [see Boxed Warning , Warnings and Precautions (5.1) ]. Neuropsychiatric Adverse Events and Suicide Risk in Smoking Cessation Treatment Inform patients that some patients have experienced changes in mood (including depression and mania), psychosis, hallucinations, paranoia, delusions, homicidal ideation, aggression, hostility, agitation, anxiety, and panic, as well as suicidal ideation and suicide when attempting to quit smoking while taking bupropion hydrochloride extended-release tablets, (SR). Instruct patients to discontinue bupropion hydrochloride extended-release tablets, (SR) and contact a healthcare professional if they experience such symptoms [see Warnings and Precautions (5.2) , Adverse Reactions (6.2) ]. Severe Allergic Reactions Educate patients on the symptoms of hypersensitivity and to discontinue bupropion hydrochloride extended-release tablets (SR), if they have a severe allergic reaction to bupropion. Seizure Instruct patients to discontinue bupropion hydrochloride extended-release tablets (SR), and not restart it if they experience a seizure while on treatment. Advise patients that the excessive use or abrupt discontinuation of alcohol, benzodiazepines, antiepileptic drugs, or sedatives/hypnotics can increase the risk of seizure. Advise patients to minimize or avoid use of alcohol. Angle-closure Glaucoma Patients should be advised that taking bupropion hydrochloride extended-release tablets, (SR) can cause mild pupillary dilation, which in susceptible individuals, can lead to an episode of angle-closure glaucoma. Pre-existing glaucoma is almost always open-angle glaucoma because angle-closure glaucoma, when diagnosed, can be treated definitively with iridectomy. Open-angle glaucoma is not a risk factor for angle-closure glaucoma. Patients may wish to be examined to determine whether they are susceptible to angle closure, and have a prophylactic procedure (e.g., iridectomy), if they are susceptible [see Warnings and Precautions (5.7) ]. Bupropion-containing Products Educate patients that bupropion hydrochloride extended-release tablets (SR), contains the same active ingredient (bupropion hydrochloride) found in WELLBUTRIN, WELLBUTRIN SR, and WELLBUTRIN XL, which are used to treat depression and that bupropion hydrochloride extended-release tablets, (SR) should not be used in conjunction with any other medications that contain bupropion (such as WELLBUTRIN, the immediate-release formulation; WELLBUTRIN SR, the sustained-release formulation; WELLBUTRIN XL or FORFIVO XL™, the extended-release formulations; and APLENZIN ® , the extended-release formulation of bupropion hydrobromide). In addition, there are a number of generic bupropion HCl products for the immediate-, sustained-, and extended-release formulations. Potential for Cognitive and Motor Impairment Advise patients that any CNS-active drug like bupropion hydrochloride extended-release tablets, (SR) may impair their ability to perform tasks requiring judgment or motor and cognitive skills. Advise patients that until they are reasonably certain that bupropion does not adversely affect their performance, they should refrain from driving an automobile or operating complex, hazardous machinery. Bupropion may lead to decreased alcohol tolerance. Concomitant Medications Counsel patients to notify their healthcare provider if they are taking or plan to take any prescription or over-the-counter drugs because bupropion hydrochloride extended-release tablets, (SR) and other drugs may affect each others’ metabolisms. Pregnancy Advise patients to notify their healthcare provider if they become pregnant or intend to become pregnant during therapy. Precautions for Nursing Mothers Advise patients that bupropion is present in human milk in small amounts. Storage Information Instruct patients to store bupropion hydrochloride extended-release tablets (SR), at room temperature, between 68°F and 77°F (20°C to 25°C) and keep the tablets dry and out of the light. Administration Information Instruct patients to swallow bupropion hydrochloride extended-release tablets (SR), whole so that the release rate is not altered. Do not chew, divide, or crush tablets; they are designed to slowly release drug in the body. When patients take more than 150 mg per day, instruct them to take bupropion hydrochloride extended-release tablets (SR), in 2 doses at least 8 hours apart, to minimize the risk of seizures. Instruct patients if they miss a dose, not to take an extra tablet to make up for the missed dose and to take the next tablet at the regular time because of the dose-related risk of seizure. Bupropion hydrochloride extended-release tablets (SR), can be taken with or without food. Advise patients that bupropion hydrochloride extended-release tablets (SR) may have an odor. WELLBUTRIN, WELLBUTRIN SR, and WELLBUTRIN XL are owned by or licensed to the GSK group of companies.
Label text from the FDA structured product label by Dr. Reddy's Laboratories Inc (revised Oct 1, 2025). Long sections are shortened; the complete label is on DailyMed.
Active ingredients
- Bupropion Hydrochloride in 6 products
Bupropion Hydrochloride (sr) NDC products (6)
| NDC | Strength & form | Labeler | Type |
|---|---|---|---|
| 50090-5101 | Bupropion Hydrochloride 150 mg/1 Tablet, Extended Release | A-S Medication Solutions | ANDA |
| 69097-877 | Bupropion Hydrochloride 100 mg/1 Tablet, Extended Release | Cipla USA Inc., | ANDA |
| 69097-878 | Bupropion Hydrochloride 150 mg/1 Tablet, Extended Release | Cipla USA Inc., | ANDA |
| 69097-879 | Bupropion Hydrochloride 200 mg/1 Tablet, Extended Release | Cipla USA Inc., | ANDA |
| 72189-349 | Bupropion Hydrochloride 150 mg/1 Tablet, Film Coated, Extended Release | DirectRx | ANDA |
| 43598-863 | Bupropion Hydrochloride 150 mg/1 Tablet, Extended Release | Dr. Reddy's Laboratories Inc | ANDA |
Bupropion Hydrochloride (sr) recalls
- D-0618-2018 Apr 11, 2018 · Class III · Terminated
Failed Dissolution Specifications; during stability testing - D-0619-2018 Apr 11, 2018 · Class III · Terminated
Failed Dissolution Specifications; during stability testing
Frequently asked questions
What is Bupropion Hydrochloride (sr) used for?
Bupropion hydrochloride extended-release tablets, USP (SR) are indicated as an aid to smoking cessation treatment. Bupropion hydrochloride extended-release tablets, USP (SR) are an aminoketone agent indicated as an aid to smoking cessation treatment. ( 1 )
What are the side effects of Bupropion Hydrochloride (sr)?
The following adverse reactions are discussed in greater detail in other sections of the labeling: Suicidal thoughts and behaviors in adolescents and young adults [see Boxed Warning , Warnings and Precautions (5.1) ] Neuropsychiatric adverse events and suicide risk in smoking cessation treatment [see Warnings and Precautions (5.2) ] Seizure [see Warnings and Precautions (5.3) ] Hypertension [see… See the full label for the complete list.
Who makes Bupropion Hydrochloride (sr)?
Bupropion Hydrochloride (sr) is listed by 4 labelers in the FDA NDC directory, including A-S Medication Solutions, Cipla USA Inc.,, DirectRx, Dr. Reddy's Laboratories Inc.
Has Bupropion Hydrochloride (sr) been recalled?
The FDA enforcement database lists 2 recalls for Bupropion Hydrochloride (sr), most recently D-0618-2018 (class iii): Failed Dissolution Specifications; during stability testing