Product Details

Bupropion HCl

A to Z Drug Facts

 Action Exact mechanism of antidepressant activity or as a smoking deterrent unknown; does not inhibit monoamine oxidase.

 Indications Treatment of depression; aid to smoking cessation treatment.

 Contraindications Seizure disorder; current or prior diagnosis of bulimia or anorexia nervosa; concurrent treatment with or within 14 days of discontinuation of MAO inhibitors; concurrent treatment with multiple bupropion products (eg, coadministration of Zyban for smoking cessation and Wellbutrin for depression); abrupt discontinuation of alcohol or sedatives.

 Route/Dosage

Antidepressant

ADULTS: PO 100 mg bid initially; may increase to 100 mg tid after 3 days (max daily dose, 450 mg; max single dose, 150 mg).

Sustained-release: 150 mg/day initially; may increase to 150 mg bid (max daily dose, 400 mg; max single dose, 200 mg).

Smoking Deterrent

ADULTS: PO Initial dose: 150 mg for first 3 days, increasing to 150 mg bid. Do not give doses greater than 300 mg/day. Initiate treatment while patient is still smoking. Patient should set target date to quit smoking within the first 2 wk of treatment; continue treatment for 7 to 12 wk. Maintenance: Clinical data are not available regarding long-term treatment (more than 12 wk) for smoking cessation. Whether to continue treatment must be determined for individual patients. Combination treatment: Combination treatment with bupropion and nicotine transdermal system may be prescribed for smoking cessation.

 Interactions

Amantadine: Incidence of bupropion side effects may be increased. Carbamazepine: May decrease bupropion serum concentrations. MAO inhibitors, selegiline: May increase risk of acute bupropion toxicity. Discontinue MAO inhibitors at least 14 days before starting bupropion. Ritonavir: Plasma levels of bupropion may be elevated, increasing the risk of toxicity. TCAs: TCA plasma concentrations may be elevated.

 Lab Test Interferences None well documented.

 Adverse Reactions

CV: Edema; chest pain; flushing; hypertension; hot flashes; stroke; tachycardia; vasodilation; ECG abnormalities (eg, premature beats, nonspecific ST-T segment changes); MI. CNS: Abnormal thoughts; agitation; anxiety; depression; insomnia; irritability; hallucinations; somnolence; suicidal ideation; seizures; headache/migraine; tremor; nervousness; memory decreased; paresthesia; CNS stimulation; increased libido. DERM: Rash; dry skin; sweating; urticaria. EENT: Dilated pupils; tinnitus; visual disturbances. GI: Dry mouth; stomatitis; nausea; vomiting; decreased appetite; thirst disturbance; colitis; GI bleeding; constipation; abdominal pain; dysphagia. GU: Nocturia; decreased sexual function or impotence; painful erection; painful or retarded ejaculation; urinary frequency; urinary tract infection; urinary urgency; vaginal hemorrhage. HEMA: Anemia; lymphadenopathy; pancytopenia. HEPA: Liver damage. META: Edema; increased weight; gynecomastia; peripheral edema. RESP: Bronchitis; epistaxis pneumonia; shortness of breath or dyspnea; pulmonary embolism; pharyngitis; sinusitus; increased cough. OTHER: Flu-like symptoms; increased sweating; weight loss; decreased electrolytes (especially potassium); infection; chest pain; pain; myalgia; arthralgia; twitch; tinnitus; taste perversion; amblyopia.

 Precautions

Pregnancy: Category B. Lactation: Bupropion and its metabolites are secreted in breast milk. Children: Safety and efficacy not established. Elderly: Use with caution. Allergic reaction: Anaphylactoid reactions characterized by symptoms such as pruritus, urticaria, angioedema, and dyspnea requiring medical treatment have been reported. CNS symptoms: Symptoms of restlessness, agitation, anxiety, and insomnia of sufficient magnitude to require treatment or discontinuation of therapy may occur. Cardiac effects: Hypotension requiring treatment may occur in patients receiving bupropion alone and in combination with nicotine replacement therapy. Heart disease: Use with caution in patients with history of MI or unstable heart disease. Hepatic impairment: Use with caution; reduce dose and frequency of bupropion as needed. Psychosis or mania: May precipitate mania in bipolar patients or activate latent psychosis in other patients. Renal impairment: Use with caution; reduce frequency of dosing as needed. Seizures: May occur; dose-related risk. Use with caution in patients with history of head trauma or CNS tumor; in patients taking other drugs known to increase risk of seizures; in cases of excessive use of alcohol, addiction to opiates, cocaine, or other stimulants; anoretics; and diabetic patients treated with oral hypoglycemics or insulin. Suicide: Patients at risk should not receive excessive quantities of drug.

 Administration/Storage

• Help patient to avoid insomnia from medication by avoiding bedtime doses.
• Store in dry place away from heat, light, and moisture.

 Assessment/Interventions

• Obtain patient history, including drug history and any known allergies.
• Consider potential for abuse or suicide.
• Assess for conditions affecting elimination, including liver disease, CHF, age, or renal function, that may affect accumulation of active secondary metabolites.
• Review laboratory reports to assist in ongoing evaluations of hepatic and renal function.
• Carefully monitor patients at risk of seizure.
• Institute suicide precautions if indicated. Risk of suicide can be present until significant remission of depression occurs.
• Observe for hoarding of drug.
• Monitor patient for signs of increased restlessness, agitation, anxiety, insomnia, or anorexia, and report to health care provider any related findings.
• Watch for signs of psychotic problems including hallucinations, delusions, and paranoia, and report any related findings to health care provider.
• Monitor cardiovascular status for signs of chest pain, arrhythmia, and symptoms of MI.
• If patient has not made significant progress by week 7 of therapy, it is unlikely that he or she will quit during that attempt; discontinue treatment.

Smoking deterrent

• When used as a smoking deterrent, intiate treatment while patient is still smoking; continue treatment for 7 to 12 wk.

 Patient/Family Education

• Advise patient to inform health care provider if taking any prescription or OTC drugs or any herbal or natural products.
• Advise women to inform health care provider if or intending to become pregnant or breastfeeding.
• Instruct patients to avoid sunlight or sunlamps or wear protective clothing because of risk of photosensitivity.
• Caution patient not to consume alcohol while taking this drug because of risk of seizure.
• Inform patient and family of adverse effects of product and instruct them to notify health care provider of potential problems. Explain that symptoms of psychosis, anorexia, or seizure should be reported immediately.
• Advise patient that drug may adversely affect performance and to avoid or use caution while driving, operating machinery, or performing other tasks requiring mental alertness.

Depression

• Instruct patient to take medicine in 3 to 4 equally divided doses or the sustained-release in 2 divided doses a day to minimize risk of seizures. Advise patient to not chew, divide, or crush the sustained-release tablets.

Smoking cessation

• Emphasize the importance of setting a target date to quit smoking within the first 2 wk of treatment.

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Copyright © 2003 Facts and Comparisons
David S. Tatro
A to Z Drug Facts