Zyban


Also found in: Dictionary.
Related to Zyban: Wellbutrin, Champix

bupropion hydrochloride

Budeprion SR, Budeprion XL, Buproban, Wellbutrin, Wellbutrin SR, Wellbutrin XL, Zyban

Pharmacologic class: Aminoketone

Therapeutic class: Second-generation antidepressant, smoking-cessation aid

Pregnancy risk category C

FDA Box Warning

• Antidepressants increase risk of suicidal thinking and behavior in children, adolescents, and young adults with major depressive disorder and other psychiatric disorders. Risk must be balanced with clinical need, as depression itself increases suicide risk. With patient of any age, observe closely for clinical worsening, suicidality, or unusual behavior changes. Advise family or caregiver to observe patient closely and communicate with prescriber as needed.

• Bupropion hydrobromide (Aplenzin) and bupropion hydrochloride (Budeprion SR, Budeprion XL, Buproban, Wellbutrin, Wellbutrin SR, and Wellbutrin XL) aren't approved for smoking cessation treatment, but bupropion hydrochloride under the names of Buproban and Zyban is approved for this use. Serious neuropsychiatric events, including but not limited to depression, suicidal ideation, suicide attempt, and completed suicide, have been reported in patients taking Buproban and Zyban for smoking cessation. Some cases may have been complicated by the signs and symptoms of nicotine withdrawal in patients who stopped smoking. Risks should be weighed against benefits of their use in smoking cessation.

• Drug isn't approved for use in pediatric patients.

Action

Unclear. Thought to decrease neuronal reuptake of dopamine, serotonin, and norepinephrine in CNS. Action as smoking-cessation aid may result from noradrenergic or dopaminergic activity.

Availability

bupropion hydrobromide

Tablets (extended-release): 174 mg, 348 mg, 522 mg

bupropion hydrochloride

Tablets: 75 mg, 100 mg

Tablets (extended-release): 150 mg, 300 mg

Tablets (sustained-release): 100 mg, 150 mg, 200 mg

Indications and dosages

Depression

Adults: Initially, 100 mg P.O. immediate-release tablet b.i.d. (morning and evening). After 3 days, may increase to 100 mg t.i.d. After 4 weeks, may increase to a maximum dosage of 450 mg/day in divided doses. No single dose should exceed 150 mg. With total daily dosage of 300 mg, wait at least 6 hours between doses; with total daily dosage of 450 mg, wait at least 4 hours between doses. Alternatively, give one 150-mg sustained-release tablet daily; increase to 150-mg sustained-release tablet b.i.d. based on clinical response. Or initially, 174 mg P.O. extended-release tablet daily in the morning; if 174-mg dose is adequately tolerated, increase to 348 mg extended-release tablet daily as early as day 4. An increase in dosage to maximum of 522 mg extended-release tablet daily, given as a single dose, may be considered for patients in whom no clinical improvement is noted after several weeks of treatment at 348 mg/day. Don't exceed single dose of 150 mg for immediate-release tablets, 522 mg for extended-release tablets, or 200 mg for sustained-release tablets.

Smoking cessation

Adults: 150 mg P.O. sustained-release tablet (Zyban) or 150 mg extended-release tablet (Buproban) once daily for 3 days, then 150-mg sustained-release tablet b.i.d. for 7 to 12 weeks. Space doses at least 8 hours apart. Don't exceed maximum dosage of 300 mg daily.

Contraindications

• Hypersensitivity to drug
• Seizures
• Anorexia nervosa or bulimia
• MAO inhibitor use within past 14 days
• Acute alcohol or sedative withdrawal
• Use of other bupropion products

Precautions

Use cautiously in:
• renal or hepatic impairment, unstable cardiovascular status
• patients with cranial trauma or other predispositions toward seizures, patients treated with other agents that lower seizure threshold (such as antipsychotics, other antidepressants, theophylline, systemic steroids)
• patients with recent history of myocardial infarction or unstable heart disease
• elderly patients
• pregnant or breastfeeding patients
• children.

Administration

• Be aware that patients should swallow extended- and sustained-release tablets whole and not crush or chew them.
• Be aware that treatment for smoking cessation should start while patient is still smoking, since approximately 1 week of treatment is required to achieve steady-state blood levels of bupropion.
• Avoid bedtime doses because they may worsen insomnia.

Know that drug shouldn't be withdrawn abruptly when used for depression.

Adverse reactions

CNS: agitation, headache, insomnia, mania, psychoses, depression, dizziness, drowsiness, tremor, anxiety, nervousness, seizures

CV: hypertension, hypotension, tachycardia, palpitations, severe hypertension, complete AV block

EENT: blurred vision, amblyopia, auditory disturbances, epistaxis, rhinitis, pharyngitis

GI: nausea, vomiting, dyspepsia, abdominal pain, flatulence, mouth ulcers, dry mouth

GU: urinary retention, urinary frequency, nocturia, vaginal irritation, testicular swelling

Metabolic: hyperglycemia, changes in libido, hypoglycemia, syndrome of inappropriate antidiuretic hormone secretion

Musculoskeletal: arthralgia, myalgia, leg cramps, twitching, neck pain

Respiratory: bronchitis, increased cough, dyspnea

Skin: photosensitivity, dry skin, pruritus, rash, urticaria, diaphoresis, skin temperature changes, erythema multiforme, Stevens-Johnson syndrome

Other: altered taste, increased or decreased appetite, weight gain or loss, hot flashes, fever, allergic reaction, flulike symptoms, anaphylactoid reactions, anaphylaxis

Interactions

Drug-drug.Benzodiazepine withdrawal, corticosteroids, other antidepressants, over-the-counter stimulants, phenothiazines, theophylline: increased risk of seizures

Cimetidine: inhibited bupropion metabolism

CYP2B6 substrates or inhibitors (such as clopidogrel, cyclophosphamide, orphenadrine, thiotepa, ticlopidine), efavirenz, fluvoxamine, nelfinavir, nor-fluoxetine, paroxetine, ritonavir, sertraline: increased bupropion activity

Despiramine, paroxetine, ritonavir, sertraline: possibly increased bupropion blood level

Levodopa, MAO inhibitors: increased risk of adverse reactions

Nicotine transdermal system: increased risk of severe hypertension

Drug-diagnostic tests.Glucose: increased level

Drug-behaviors.Alcohol use or cessation: increased risk of seizures

Sun exposure: increased risk of photo-sensitivity

Patient monitoring

• Monitor blood pressure, ECG, CBC, and renal and hepatic function. Monitor tricyclic antidepressant (TCA) blood level if patient's taking TCAs concurrently.
• Be aware that if patient is also on nicotine patch for smoking cessation, the combination may cause or increase risk of hypertension.
• Check for oral and dental problems.

Patient teaching

Instruct patient to seek immediate medical attention if itching, hives, swelling of the throat, or difficulty breathing occurs.

Instruct patient taking drug for smoking cessation to immediately notify prescriber if agitation, hostility, depressed mood, changes in thinking or behavior, suicidal ideation, or suicidal behavior occurs.
• Advise patient to set a "target quit date" within first 2 weeks of treatment for smoking cessation.
• Instruct patient to swallow extendedor sustained-release tablets without crushing or chewing.

Caution patient not to discontinue drug abruptly when taking drug for depression.
• Emphasize importance of frequent oral hygiene. (Dry mouth increases risk of caries and dental problems.)
• Caution patient to avoid alcohol, because it may increase risk of seizures.
• Advise patient to keep regular appointments for periodic blood tests and hepatic and renal studies.
• Advise breastfeeding patient that she should decide whether to discontinue breastfeeding or discontinue drug, taking into account the importance of drug for her treatment.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, and behaviors mentioned above.

buPROPion

(byoo-proe-pee-on) ,

Aplenzin

(trade name),

Forfivo XL

(trade name),

Wellbutrin

(trade name),

Wellbutrin SR

(trade name),

Wellbutrin XL

(trade name),

Zyban

(trade name)

Classification

Therapeutic: antidepressants
Pharmacologic: aminoketones
Pregnancy Category: B

Indications

Treatment of depression (with psychotherapy).Depression with seasonal affective disorder (Aplenzin and Wellbutrin XL only).Smoking cessation (Zyban only).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 into 3 active metabolites (CYP2B6 involved in formation of one of the active metabolites).
Half-life: 14 hr (active metabolites may have longer half-lives).

Time/action profile (antidepressant effect)

ROUTEONSETPEAKDURATION
PO1–3 wkunknownunknown

Contraindications/Precautions

Contraindicated in: Hypersensitivity;Concurrent use of MAO inhibitors or MAO-like drugs (linezolid or methylene blue);Concurrent use of ritonavir;Seizure disorders;Arteriovenous malformation, severe head injury, CNS tumor, CNS infection, severe stroke, anorexia nervosa, bulimia, or abrupt discontinuation of alcohol, benzodiazepines, barbiturates, or antiepileptic drugs (↑ risk of seizures); Lactation: Potential for serious adverse reactions in nursing infants.
Use Cautiously in: Renal/hepatic impairment (↓ dose recommended) (Forfivo XL not recommended in patients with renal or hepatic impairment);Recent history of MI;History of suicide attempt;Unstable cardiovascular status;May ↑ risk of suicide attempt/ideation especially during early treatment or dose adjustment; this risk appears to be greater in adolescents or children; Obstetric: Use only if benefit to patient outweighs potential risk to fetus; Geriatric: ↑ risk of drug accumulation; ↑ sensitivity to effects.
Exercise Extreme Caution in: Severe hepatic cirrhosis (↓ dose required); Pediatric: ↑ risk of suicidal thinking and behavior. Observe carefully, especially at initiation of therapy and during ↑ or ↓ in dose.

Adverse Reactions/Side Effects

Central nervous system

  • seizures (life-threatening)
  • suicidal thoughts/behavior (life-threatening)
  • agitation (most frequent)
  • headache (most frequent)
  • aggression
  • anxiety
  • delusions
  • depression
  • hallucinations
  • hostility
  • insomnia
  • mania
  • panic
  • paranoia
  • psychoses

Gastrointestinal

  • dry mouth (most frequent)
  • nausea (most frequent)
  • vomiting (most frequent)
  • change in appetite
  • weight gain
  • weight loss

Dermatologic

  • photosensitivity

Endocrinologic

  • hyperglycemia
  • hypoglycemia
  • syndrome of inappropriate ADH secretion

Neurologic

  • tremor (most frequent)

Interactions

Drug-Drug interaction

Concurrent use with MAO-inhibitor like drugs, such as linezolid or methylene blue may ↑ risk of hypertensive reactions; concurrent use contraindicated; do not start therapy in patients receiving linezolid or methylene blue ; if linezolid or methylene blue need to be started in a patient receiving bupropion, immediately discontinue bupropion and monitor for 2 wk or until 24 hr after last dose of linezolid or methylene blue, whichever comes first (may resume bupropion therapy 24 hr after last dose of linezolid or methylene blue)↑ risk of adverse reactions when used with amantadine, or levodopa.↑ risk of seizures with phenothiazines, antidepressants, theophylline, corticosteroids, OTC stimulants/anorectics, or cessation of alcohol or benzodiazepines (avoid or minimize alcohol use).Ritonavir, lopinavir/ritonavir, and efavirenz may ↓ levels; may need to ↑ bupropion dose.May ↑ citalopram levels.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 CYP2D6 enzyme system and may ↑ levels and risk of toxicity from antidepressants (SSRIs and tricyclic), haloperidol, risperidone, thioridazine, haloperidol, beta blockers, flecainide, and propafenone.May ↓ levels and efficacy of tamoxifen.May ↓ the efficacy of tamoxifen.

Route/Dosage

Depression

Oral (Adults) Immediate-release—100 mg twice daily initially; after 3 days may ↑ to 100 mg 3 times daily; after at least 4 wk of therapy, may ↑ 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 ↑ to 150 mg twice daily with at least 8 hr between doses; after at least 4 wk of therapy, may ↑ to a maximum daily dose of 400 mg given as 200 mg twice daily. Extended-release (Wellbutrin XL)—150 mg once daily in the morning, may be ↑ after 4 days to 300 mg once daily; some patients may require up to 450 mg/day as a single daily dose. Extended-release (Aplenzin)—174 mg once daily in the morning, may be ↑ after 4 days to 348 mg once daily; some patients may require up to 522 mg/day as a single daily dose. Extended-release (Forfivo XL)—450 mg once daily (should NOT be used as initial therapy; it should only be used in patients who have been receiving 300 mg/day of another bupropion formulation for at least 2 wk and require titration up to 450 mg/day or in those patients receiving 450 mg/day of another bupropion formulation).

Seasonal Affective Disorder

Oral (Adults) Extended-release (Wellbutrin XL)—150 mg/day in the morning; if dose is well tolerated, ↑ to 300 mg/day in one wk. Doses should be tapered to 150 mg/day for 2 wk before discontinuing; Extended-release (Aplenzin)—174 mg once daily in the morning, may be ↑ after 7 days to 348 mg once daily.

Smoking cessation

Oral (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 (generic available)

Tablets: 75 mg, 100 mg Cost: Generic — 75 mg $79.43 / 100, 100 mg $106.01 / 100
Sustained-release tablets: 100 mg, 150 mg, 200 mg Cost: Generic — 100 mg $51.12 / 180, 150 mg $59.60 / 180, 200 mg $52.33 / 180
Extended-release tablets (Wellbutrin XL): 150 mg, 300 mg Cost: Generic — 150 mg $74.84 / 90, 300 mg $63.94 / 90
Extended-release tablets (Aplenzin): 174 mg, 348 mg, 522 mg Cost: 174 mg $359.09 / 30, 348 mg $473.36 / 30, 522 mg $1,077.23 / 30
Extended-release tablets (Forfivo XL): 450 mg Cost: $176.40 / 30

Nursing implications

Nursing assessment

  • Monitor mood changes. Inform health care professional if patient demonstrates significant increase in anxiety, nervousness, or insomnia.
  • Assess mental status and mood changes, especially during initial few months of therapy and during dose changes. Risk may be increased in children, adolescents, and adults ≤24 yrs. Inform health care professional if patient demonstrates significant increase in signs of depression (depressed mood, loss of interest in usual activities, significant change in weight and/or appetite, insomnia or hypersomnia, psychomotor agitation or retardation, increased fatigue, feelings of guilt or worthlessness, slowed thinking or impaired concentration, suicide attempt or suicidal ideation). 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.
    • May cause false-positive urine test for amphetamines.

Potential Nursing Diagnoses

Ineffective coping (Indications)

Implementation

  • Do not confuse bupropion with buspirone. Do not confuse Wellbutrin SR with Wellbutrin XL. Do not confuse Zyban with Diovan. Do not administer bupropion (Wellbutrin) with Zyban, which contain the same ingredients.
    • Administer doses in equally spaced time increments during the day to minimize the risk of seizures. Risk of seizures increases fourfold 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.
    • Nicotine patches, gum, inhalers, and spray may be used concurrently with bupropion.
    • When converting from other brands of bupropion to Aplenzin 522 mg/day Aplenzin is equivalent to 450 mg/day bupropion HCl, 348 mg/day Aplenzin is equivalent to 300 mg/day bupropion HCl and 174 mg/day Aplenzin is equivalent to 150 mg/day bupropion HCl.
  • Oral: Swallow sustained-release or extended-release tablets whole; do not break, crush, or chew.
    • May be administered with food to lessen GI irritation.
  • Seasonal Affective Disorder: Begin administration in autumn prior to the onset of depressive symptoms. Continue therapy through winter and begin to taper and discontinue in early spring.

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.
  • 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, family, and caregivers to look for suicidality, especially during early therapy or dose changes. Notify health care professional immediately if thoughts about suicide or dying, attempts to commit suicide, new or worse depression or anxiety, agitation or restlessness, panic attacks, insomnia, new or worse irritability, aggressiveness, acting on dangerous impulses, mania, or other changes in mood or behavior occur.
  • Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken, to avoid alcohol during therapy and to consult with health care professional before taking other medications with bupropion, such as Zyban.
  • 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.
  • Advise patient to notify health care professional of medication regimen before treatment or surgery.
  • Instruct female patients to inform health care professional if pregnancy is planned or suspected or if breast feeding or planning to breast feed.
  • 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.
  • Advise patient to stop taking bupropion and contact a health care professional immediately if agitation, depressed mood, and any changes in behavior that are not typical of nicotine withdrawal, or if suicidal thoughts or behavior occur.

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.

Zyban

(zī′băn)
A trademark for the drug bupropion hydrochloride, used as an aid to smoking cessation treatment.

Zyban

A brand name for BUPROPION.
References in periodicals archive ?
But 10 days after starting on a course of Zyban, the loving mother-of-two claims she became a demon.
Today's guidance states that NRTs or Zyban should normally only be prescribed when smokers have made a commitment to stop smoking on or before a certain date in conjunction with advice and encouragement to help them quit.
By February 22, doctors had reported 3,685 cases of suspected adverse reactions to Zyban to the Medicines Control Agency.
The married mother of two, from the Lanarkshire village of Plains, was prescribed Zyban in December 2000 to beat her 15-a-day habit.
It should be noted that patients may be required to stop smoking because of underlying diseases and these may well explain some of the reported deaths of patients taking Zyban.
Now British makers Glaxo-Wellcome have announced they are seeking a licence to market Zyban in the U.
We were able to buy the anti-impotence drug Viagra, the stop-smoking treatment Zyban and the slimming pill Reductil over the internet.
THE controversial anti-smoking drug Zyban is to be made available on the NHS.
ANYONE trying to give up smoking should be able to get nicotine replacement therapy and "wonder drug" Zyban on the NHS, say researchers.
Zyban tablets, the first non-nicotine therapy to gain a licence in the UK, are available on NHS prescription to help smokers beat their addiction.
GlaxoSmithKline markets Wellbutrin SR for the treatment of depression and Zyban for smoking cessation.
WORRIED readers inundated the Daily Record with calls when we highlighted concerns about Zyban last year.