bupropion
(byoo-proe-pee-on)
Wellbutrin, Wellbutrin SR, Wellbutrin XL, Zyban
CLASSIFICATION(S)
Therapeutic: antidepressants, smoking deterrants
Pharmacologic: aminoketones
Pregnancy Category B
INDICATIONS
• Treatment of depression (with psychotherapy)
• Smoking cessation (Zyban only)
• Unlabelled Uses: • Treatment of ADHD in adults (SR only)
• To increase sexual desire in women
ACTION
• Decreases neuronal reuptake of dopamine in the CNS
• Diminished neuronal uptake of serotonin and norepinephrine (less than tricyclic antidepressants)
• Therapeutic Effects: ○ Diminished depression
○ Decreased craving for cigarettes
PHARMACOKINETICS
Absorption: Although well absorbed, rapidly and extensively metabolized by the liver
Distribution: Unknown
Metabolism and Excretion: Extensively metabolized by the liver. Some conversion to active metabolites
Half-life: 14 hr (active metabolites may have longer half-lives)
TIME OF ACTION
antidepressant effect ROUTE ONSET PEAK DURATION
PO 1-3 wk unknown unknown
CONTRAINDICATIONS/PRECAUTIONS
Contraindicated in:
• Hypersensitivity
• History of bulimia, and anorexia nervosa
• Concurrent MAO inhibitor or ritonavir therapy
Use Cautiously in:
• Renal/hepatic impairment (↓ dose recommended)
• Recent history of MI
• Geri: Geriatric patients (increased risk of drug accumulation; increased sensitivity to effects)
• History of suicide attempt
• Unstable cardiovascular status
• May ↑ risk of suicide attempt/ideation especially during early treatment or dose adjustment; this risk may be greater in adolescents or children
• OB: Pregnancy, lactation
• Pedi: Children <18 yr (safety not established)
Exercise Extreme Caution in: • History of seizures, head trauma or concurrent medications that ↓ seizure threshold (theophylline, antipsychotics, antidepressants, systemic corticosteroids)
• Severe hepatic cirrhosis (↓ dose required)
ADVERSE REACTIONS/SIDE EFFECTS*
*CAPITALS indicate life threatening; underlines indicate most frequent.
CNS: SEIZURES, agitation, headache, insomnia, mania, psychoses,
GI: dry mouth, nausea, vomiting, change in appetite, weight gain, weight loss,
Derm: photosensitivity,
Endo: hyperglycemia, hypoglycemia, syndrome of inappropriate ADH secretion,
Neuro: tremor,
INTERACTIONS
Drug-Drug:
• ↑ risk of adverse reactions when used with amantadine , levodopa or MAO inhibitors (concurrent use of MAO inhibitors is contraindicated)
• ↑ risk of seizures with phenothiazines, antidepressants , theophylline , corticosteroids , OTC stimulants/anorectics, or cessation of alcohol or benzodiazepines (avoid or minimize alcohol use)
• Blood levels ↑ by ritonavir (avoid concurrent use)
• Carbamazepine may ↓ blood levels and effectiveness
• Concurrent use with nicotine replacement may cause hypertension
• ↑ risk of bleeding with warfarin
• Bupropion and one of its metabolites inhibit the CYP 2D6 enzyme system and may ↑ levels and risk of toxicity from antidepressants (SSRIs and tricyclic), some beta blockers , antiarrhythmics , and antipsychotics
ROUTE AND DOSAGE
Depression • PO (Adults ): Immediate-release--100 mg twice daily initially; after 3 days may increase to 100 mg 3 times daily; after at least 4 wk of therapy, may increase up to 450 mg/day in divided doses (not to exceed 150 mg/dose; wait at least 6 hr between doses at the 300 mg/day dose or at least 4 hr between doses at the 450 mg/day dose). Sustained-release--150 mg once daily in the morning; after 3 days, may increase to 150 mg twice daily with at least 8 hr between doses; after at least 4 wk of therapy, may increase to a maximum daily dose of 400 mg given as 200 mg twice daily. Extended-release--150 mg once daily in the morning, may be increased after 4 days to 300 mg once daily; some patients may require up to 450 mg/day as a single daily dose
Smoking cessation • PO (Adults ): Zyban--150 mg once daily for 3 days, then 150 mg twice daily for 7-12 wk (doses should be at least 8 hr apart)
AVAILABILITY
• Tablets: 75 mg, 100 mg
• Cost: 75 mg $84.10/100, 100 mg $112.19/100
• Sustained-release tablets: 100 mg, 150 mg, 200 mg
• Cost: 100 mg $94.27/60, 150 mg $101.94/60
• Extended-release tablets: 150 mg, 300 mg
• Cost: 150 mg $91.63/30, 300 mg $121.03/30
NURSING IMPLICATIONS
ASSESSMENT
• Monitor mood changes. Inform physician or other health care professional if patient demonstrates significant increase in anxiety, nervousness, or insomnia
• Assess for suicidal tendencies, especially during early therapy. Restrict amount of drug available to patient
• Lab Test Considerations: Monitor hepatic and renal function closely in patients with kidney or liver impairment to prevent ↑ serum and tissue bupropion concentrations
POTENTIAL NURSING DIAGNOSES
• Ineffective coping (Indications).
IMPLEMENTATION
• Do not confuse bupropion with buspirone. Do not confuse Zyban (bupropion) with Zagam (Sparfloxacin). Do not administer bupropion (Wellbutrin) with Zyban, contain same ingredients ○ Administer doses in equally spaced time increments during day to minimize the risk of seizures. Risk of seizures increases four fold in doses greater than 450 mg per day
○ May be initially administered concurrently with sedatives to minimize agitation. This is not usually required after the 1st wk of therapy
○ Insomnia may be decreased by avoiding bedtime doses. May require treatment during 1st wk of therapy
○ May be administered with food to lessen GI irritation
○ Nicotine patches, gum, inhalers, and spray may be used concurrently with bupropion
• PO: Sustained-release (SR or XL) tablets should be swallowed whole; do not break, crush, or chew
PATIENT/FAMILY TEACHING
• Instruct patient to take bupropion as directed. Take missed doses as soon as possible and space day's remaining doses evenly at not less than 4-hr intervals. Missed doses for smoking cessation should be omitted. Do not double doses or take more than prescribed. May require 4 wk or longer for full effects. Do not discontinue without consulting health care professional. May require gradual reduction before discontinuation
• Bupropion may impair judgment or motor and cognitive skills. Caution patient to avoid driving and other activities requiring alertness until response to medication is known
• Advise patient to avoid alcohol during therapy and to consult with health care professional before taking other medications with bupropion
• Inform patient that frequent mouth rinses, good oral hygiene, and sugarless gum or candy may minimize dry mouth. If dry mouth persists for more than 2 wk, consult health care professional regarding use of saliva substitute
• Advise patient to notify health care professional if rash or other troublesome side effects occur
• Inform patient that unused shell of XL tablets may appear in stool; this is normal
• Advise patient to use sunscreen and protective clothing to prevent photosensitivity reactions
• Instruct female patients to inform health care professional if pregnancy is planned or suspected
• Advise patient to notify health care professional of medication regimen before treatment or surgery
• Emphasize the importance of follow-up exams to monitor progress. Encourage patient participation in psychotherapy
• Smoking Cessation: Smoking should be stopped during the 2nd week of therapy to allow for the onset of bupropion and to maximize the chances of quitting
EVALUATION/DESIRED OUTCOMES
• Increased sense of well-being ○ Renewed interest in surroundings. Acute episodes of depression may require several months of treatment
• Cessation of smoking
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