Bupropion Hcl
FDA Drug Information • Also known as: Bupropion Hcl
- Brand Names
- Bupropion Hcl
- Dosage Form
- POWDER
- Product Type
- BULK INGREDIENT
⚠ Boxed Warning (Black Box)
WARNING: SUICIDAL THOUGHTS AND BEHAVIORS SUICIDALITY AND ANTIDEPRESSANT DRUGS Antidepressants increased the risk of suicidal thoughts and behavior in children, adolescents, and young adults in short-term trials. These trials did not show an increase in the risk of suicidal thoughts and behavior with antidepressant use in subjects over age 24; there was a reduction in risk with antidepressant use in subjects aged 65 and older [see Warnings and Precautions (5.1)]. In patients of all ages who are started on antidepressant therapy, monitor closely for worsening, and for emergence of suicidal thoughts and behaviors. Advise families and caregivers of the need for close observation and communication with the prescriber [see Warnings and Precautions (5.1)].
Description
Bupropion hydrochloride, an antidepressant of the aminoketone class, 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 276.21 g/mol. The molecular formula is C13H18ClNO
What Is Bupropion Hcl Used For?
Bupropion hydrochloride tablets are indicated for the treatment of major depressive disorder (MDD), as defined by the Diagnostic and Statistical Manual (DSM). The efficacy of bupropion hydrochloride tablets in the treatment of a major depressive episode was established in two 4-week controlled inpatient trials and one 6-week controlled outpatient trial of adult subjects with MDD [see Clinical Studies (14)].
Dosage and Administration
2.1 General Instructions for Use To minimize the risk of seizure, increase the dose gradually [see Warnings and Precautions (5.3)]. Increases in dose should not exceed 100 mg/day in a 3-day period. Bupropion hydrochloride tablets should be swallowed whole and not crushed, divided, or chewed. Bupropion hydrochloride tablets may be taken with or without food. The recommended starting dose is 200 mg/day, given as 100 mg twice daily. After 3 days of dosing, the dose may be increased to 300 mg/day, given as 100 mg 3 times daily, with at least 6 hours between successive doses. Dosing above 300 mg/day may be accomplished using the 75- or 100-mg tablets. A maximum of 450 mg/day, given in divided doses of not more than 150 mg each, may be considered for patients who show no clinical improvement after several weeks of treatment at 300 mg/day. Administer the 100-mg tablet 4 times daily to not exceed the limit of 150 mg in a single dose. It is generally agreed that acute episodes of depression require several months or longer of antidepressant drug treatment beyond the response in the acute episode. It is unknown whether the dose of bupropion hydrochloride tablets needed for maintenance treatment is identical to the dose that provided an initial response. Periodically reassess the need for maintenance treatment and the appropriate dose for such treatment. 2.2 Dose Adjustment in Patients with Hepatic Impairment In patients with moderate to severe hepatic impairment (Child-Pugh score: 7 to 15), the maximum dose of bupropion hydrochloride tablets are 75 mg/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)]. 2.3 Dose Adjustment in Patients with Renal Impairment Consider reducing the dose and/or frequency of bupropion hydrochloride tablets in patients with renal impairment (Glomerular Filtration Rate [GFR] less than 90 mL/min) [see Use in Specific Populations (8.6), Clinical Pharmacology (12.3)]. 2.4 Switching a Patient to or from a Monoamine Oxidase Inhibitor (MAOI) Antidepressant At least 14 days should elapse between discontinuation of an MAOI intended to treat depression and initiation of therapy with bupropion hydrochloride tablets. Conversely, at least 14 days should be allowed after stopping bupropion hydrochloride tablets before starting an MAOI antidepressant [see Contraindications (4), Drug Interactions (7.6)]. 2.5 Use of Bupropion Hydrochloride Tablets with Reversible MAOIs Such as Linezolid or Methylene Blue Do not start bupropion hydrochloride tablets 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. In a patient who requires more urgent treatment of a psychiatric condition, non-pharmacological interventions, including hospitalization, should be considered [see Contraindications (4),...
Side Effects (Adverse Reactions)
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 symptoms 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)] 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 with bupropion hydrochloride tablets in approximately 10% of the 2,400 subjects and healthy volunteers who participated in clinical trials during the product’s initial development. The more common events causing discontinuation include neuropsychiatric disturbances (3.0%), primarily agitation and abnormalities in mental status; gastrointestinal disturbances (2.1%), primarily nausea and vomiting; neurological disturbances (1.7%), primarily seizures, headaches, and sleep disturbances; and dermatologic problems (1.4%), primarily rashes. It is important to note, however, that many of these events occurred at doses that exceed the recommended daily dose. Commonly Observed Adverse Reactions Adverse reactions commonly encountered in subjects treated with bupropion hydrochloride tablets are agitation, dry mouth, insomnia, headache/migraine, nausea/vomiting, constipation, tremor, dizziness, excessive sweating, blurred vision, tachycardia, confusion, rash, hostility, cardiac arrhythmia, and auditory disturbance. Table 2 summarizes the adverse reactions that occurred in placebo-controlled trials at an incidence of at least 1% of subjects receiving bupropion hydrochloride tablets and more frequently in these subjects than in the placebo group. Table 2. Adverse Reactions Reported by at Least 1% of Subjects and at a Greater Frequency than Placebo in Controlled Clinical Trials Bupropion Hydrochloride Tablets Placebo (n = 323) (n = 185) Adverse Reaction % % Cardiovascular Cardiac arrhythmias 5.3 4.3 Dizziness 22.3 16.2 Hypertension 4.3 1.6 Hypotension 2.5 2.2 Palpitations 3.7 2.2 Syncope 1.2 0.5 Tachycardia 10.8 8.6 Dermatologic Pruritus 2.2 0.0 Rash 8.0 6.5 Gastrointestinal Appetite increase 3.7 2.2 Constipation 26.0 17.3 Dyspepsia 3.1 2.2 Nausea/vomiting 22.9 18.9 Genitourinary Impotence 3.4 3.1 Menstrual complaints 4.7 1.1 Urinary frequency 2.5 2.2 Musculoskeletal Arthritis 3.1 2.7 Neurological Akathisia 1.5 1.1 Cutaneous temperature 1.9 1.6 disturbance Dry mouth 27.6 18.4 Excessive sweating 22.3 14.6 Headache/migraine 25.7 22.2 Impaired sleep quality 4.0 1.6 Insomnia 18.6 15.7 Sedation 19.8 19.5 Sensory disturbance 4.0 3.2 Tremor 21.1 7.6 Neuropsychiatric Agitation 31.9 22.2 Anxiety 3.1 1.1 Confusion 8.4 4.9 Decreased libido 3.1 1.6 Delusions 1.2 1.1 Euphoria 1.2 0.5 Hostility 5.6 3.8 Nonspecific Fever/chills 1.2 0.5 Special senses Auditory disturbance 5.3 3.2 Blurred vision 14.6 10.3 Gustatory disturbance 3.1 1.1 Other Adverse Reactions Observed during the Clinical Development of Bupropion Hydrochloride Tablets The conditions and duration of exposure to bupropion hydrochloride tablets varied greatly, and a substantial proportion of the experience was gained in open and uncontrolled clinical settings. During this experience, numerous adverse events were reported; however, without appropriate controls, it is...
Drug Interactions
7.1 Potential for Other Drugs to Affect Bupropion Hydrochloride Tablets Bupropion is primarily metabolized to hydroxybupropion by CYP2B6. Therefore, the potential exists for drug interactions between bupropion hydrochloride tablets 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 tablets 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 tablets 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 Tablets to Affect Other Drugs Drugs Metabolized by CYP2D6 Bupropion and its metabolites (erythrohydrobupropion, threohydrobupropion, hydroxybupropion) are CYP2D6 inhibitors. Therefore, coadministration of bupropion hydrochloride tablets 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 tablets, 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 tablets and such drugs may require increased doses of the drug [see Clinical Pharmacology (12.3)]. Digoxin Coadministration of bupropion hydrochloride with digoxin may decrease plasma digoxin levels. Monitor plasma digoxin levels in patients treated concomitantly with bupropion hydrochloride and digoxin [see Clinical Pharmacology (12.3)]. 7.3 Drugs that Lower Seizure Threshold Use extreme caution when coadministering bupropion hydrochloride tablets with other drugs...
Contraindications
Bupropion hydrochloride tablets are contraindicated in patients with a seizure disorder.
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. Telephone numbers for certified poison control centers are listed in the Physician’s Desk Reference (PDR). Call 1-800-222-1222 or refer to WWW.POISON.ORG. There are no known antidotes for bupropion. In case of an overdose, provide supportive care, including close medical supervision and monitoring. Consider the possibility of multiple drug overdose. Ensure an adequate airway, oxygenation, and ventilation. Monitor cardiac rhythm and vital signs. Induction of emesis is not recommended.
How Supplied
Bupropion hydrochloride tablets, USP 75 mg are available for oral administration as orange, round, unscored, film coated tablets, imprinted "APO" on one side and "BU" over "75" on the other side. They are supplied as follows: Bottles of 30 (NDC 60505-0158-3) Bottles of 90 (NDC 60505-0158-9) Bottles of 100 (NDC 60505-0158-1) Bottles of 500 (NDC 60505-0158-5) Bottles of 1,000 (NDC 60505-0158-7) Bupropion hydrochloride tablets, USP 100 mg are available for oral administration as purple, round, unscored, film coated tablets, imprinted "APO" on one side and "BUP" over "100" on the other side. They are supplied as follows: Bottles of 30 (NDC 72189-457-30) Bottles of 90 (NDC 60505-0157-9) Bottles of 100 (NDC 60505-0157-1) Bottles of 500 (NDC 60505-0157-5) Bottles of 1,000 (NDC 60505-0157-7)
About This Information
This drug information is sourced from FDA-approved labeling via the openFDA database. It is intended for educational and reference purposes only. This is not medical advice. Always consult your healthcare provider before making decisions about medication. Drug information may be updated by the FDA; check with your pharmacist for the most current information.
What are side effects?
Side effects are unwanted reactions that can occur when taking a medication. They range from mild (headache, nausea) to severe (allergic reactions, organ damage). Not everyone experiences side effects, and severity varies. Report any concerning side effects to your doctor.
What are drug interactions?
Drug interactions occur when a medication is affected by another drug, food, or supplement. Interactions can make medications less effective or cause dangerous side effects. Always tell your doctor about all medications and supplements you take.