Names and pronunciation
(byoo-proe′pee-on) Aplenzin, Forfivo XL, Wellbutrin XL, Zyban
PDF page 204
Loading InternPractice…
Drug reference
(byoo-proe′pee-on) Aplenzin, Forfivo XL, Wellbutrin XL, Zyban
PDF page 204
Func. class.: Antidepressant— miscellaneous smoking deterrent
PDF page 204
Chem. class.: Aminoketone
PDF page 204
Do not confuse: buPROPion/busPIRone Zyban/Diovan
PDF page 204
ACTION: Inhibits reuptake of DOPa- mine, norepinephrine, serotonin
PDF page 204
USES: Depression (Wellbutrin), smok- ing cessation (Zyban); seasonal affective disorder, substance abuse, glaucoma, smoking, cardiac disease, heart failure
PDF page 204
CONTRAINDICATIONS: Hyper- sensitivity, head trauma, stroke, intracranial mass, eating disorders, seizure disorders Precautions: Pregnancy, breastfeeding, geriatric patients, renal/hepatic disease, recent MI, cranial trauma, seizure disor- der, substance abuse, glaucoma, smok- ing, cardiac disease, heart failure, head trauma, stroke, intracranial mass, Tourette’s syndrome, tics, tobacco smok- ing, abrupt discontinuation
PDF page 205
Black Box Warning: Children <18 yr, suicidal thinking/behavior (young adults) Black Box Warning: Mental status: mood, sensorium, affect, suicidal/homi- cidal tendencies, increase in psychiatric symptoms, assess for mania in those with bipolar disorder • Beers: avoid in older adults; lowers seizure threshold, may be acceptable for those with well-controlled seizures for which other treatment has been ineffective Black Box Warning: That suicidal/ homicidal ideas, behaviors, hostility, de- pression may occur in children or young adults, to report immediately • Serotonin syndrome: monitor for in- creased B/P, pulse, fever, agitation, tremor, sweating, diarrhea; usually caused when combined with other products on interac- tion list; immediately stop drug and report symptoms to prescriber • Pregnancy/breastfeeding: to notify prescriber if pregnancy is suspected, planned, or if breastfeeding
PDF pages 205, 206
SIDE EFFECTS CNS: Headache, agitation, dizziness, akinesia, confusion, seizures, delu- sions, insomnia, sedation, tremors, suicidal/homicidal ideation, flushing CV: Dysrhythmias, hypertension, palpita- tions, tachycardia, hypotension, chest pain, chills EENT: Blurred vision, auditory disturbance GI: Nausea, vomiting, anorexia, diar- rhea, dry mouth, increased appetite, constipation, altered taste GU: Impotence, urinary frequency, retention INTEG: Rash, pruritus, sweating MISC: Hot flashes
PDF page 205
INTERACTIONS • Do not use within 14 days of MAOIs Increase: adverse reactions: amantadine, haloperidol seizures—levodopa, MAOIs, phenothiazines, antidepressants, benzodi- azepines, alcohol, theophylline, systemic steroids Increase: serotonin syndrome—SSRIs, methylene blue, linezolid, traMADol, tra- ZODone, tricyclic antidepressants, cyclo- benzaprine; do not use together Increase: action of citalopram Decrease: effect of tamoxifen Decrease: buPROPion effect—carBA Mazepine, cimetidine, PHENobarbital, phenytoin or other products (CYP2D6); CYP2B6 inducers Drug/Herb Increase: CNS depression—kava, valerian Drug/Lab Test Positive: urine drug screen for amphet- amine possible
PDF pages 205, 206
TREATMENT OF OVERDOSE: ECG monitoring; lavage; administer anti- convulsant
PDF page 206
DOSAGE AND ROUTES Depression • Adult: PO 100 mg bid initially, then in- crease after 3 days to 100 mg tid if needed, max 150 mg single dose; ER/SR initially 150 mg AM, increase to 300 mg/day if initial dose is tolerated, after no less than 4 days; after several weeks, titrate to 200 mg bid; Aplenzin 174 mg q AM, may in- crease to 348 mg q AM on day 4, may in- crease to 522 mg after several weeks if needed; Forfivo XL (not for initial treat- ment) 450 mg daily after titration with another product (300 mg/day × ≥2 wk) • Geriatric: PO 50-100 mg/day, may in- crease by 50-100 mg q3-4days Smoking cessation (Zyban) • Adult: SR 150 mg daily × 3 days, then 150 mg bid for remainder of treatment Seasonal affective disorder • Adult: PO (Wellbutrin XL) 150 mg as a single dose in the AM, after 1 wk may be increased to 300 mg/day; (Aplenzin) 174 mg daily in AM, after 7 days may in- crease to 348 mg daily Hepatic dose Adult: PO (moderate-severe) Aplenzin max 174 mg every other day
PDF page 205
Available forms: Tablets 75, 100 mg; extended-release tablet (XL) 100, 150, 200, 300, 450 mg; (SR-12 hr, XL-24 hr); tablet extended release (Aplenzin) 174, 348, 522 mg
PDF page 205
Administer: PO route • When switching to Aplenzin from Well- butrin, Wellbutrin SR or XL, use these equivalents: 174 mg buPROPion HBr = 150 mg buPROPion HCl; 348 mg buPROPi- on HBr = 300 mg buPROPion HCl; 522 mg B buPROPion HBr = 450 mg buPROPion HCl • Wellbutrin immediate release, sepa- rate by ≥6 hr, give in 3 divided doses; Wellbutrin XL, give daily in AM; Zyban SR, give in 2 divided doses, ≥8 hr apart; Aplenzin ER, give daily in AM, a larger dose of Aplenzin is needed because these products are not equivalent • Do not break, crush, chew sustained- release, extended-release tablet • At evenly spaced times to prevent seizures; seizure risk increases with high doses • Increase fluids, bulk in diet if consti- pation occurs • Do not use with SSRIs, linezolid, meth- ylene blue, MAOIs • With food, milk for GI symptoms • Sugarless gum, hard candy, frequent sips of water for dry mouth • Avoid giving at night to prevent insomnia
PDF page 205
Assess: • Smoking: for smoking cessation after 7-12 wk; if progress has not been made, product should be discontinued, begin smoking ces- sation while patient is still smoking, start smoking cessation after 7 days • For increased risk of seizures; if patient has excessively used CNS depressants and OTC stimulants, dosage of buPROPion should not be exceeded • Monitor weight regularly, monitor VS baseline and periodically
PDF page 206
Evaluate: • Therapeutic response: decreased de- pression, ability to perform daily activi- ties, ability to sleep throughout the night, smoking cessation
PDF page 206
CLINICAL CONSIDERATIONS
PDF page 206
Patient and caregiver information: • That therapeutic effects may take 2-4 wk; not to increase dose without pre- scriber’s approval; that treatment for smoking cessation lasts 7-12 wk • To use caution when driving, perform- ing other activities that require alertness; sedation, blurred vision may occur • To avoid alcohol, other CNS depressants; alcohol may increase risk of seizures • Not to chew, crush tablets • That extended-release shell may be seen in stools, tablet odor is unpleasant • That exams and lab work will be needed • To notify health care professionals of all Rx, herbals, supplements taken, not to start new product unless discussed prior to use • Not to use with nicotine patches unless directed by prescriber; may increase B/P • To notify prescriber immediately if uri- nary retention occurs • That risk of seizures increases when dose is exceeded or if used with alcohol or other CNS depressants; if patient has seizure disorder
PDF page 206
PHARMACOKINETICS Onset 1-4 wk, half-life 14 hr (immediate release), extensively metabolized by liver, some conversion to active metabolites, pro- tein binding 84%, excreted in urine and feces
PDF page 205
• Adult: PO 100 mg bid initially, then in- crease after 3 days to 100 mg tid if needed, max 150 mg single dose; ER/SR initially 150 mg AM, increase to 300 mg/day if initial dose is tolerated, after no less than 4 days; after several weeks, titrate to 200 mg bid; Aplenzin 174 mg q AM, may in- crease to 348 mg q AM on day 4, may in- crease to 522 mg after several weeks if needed; Forfivo XL (not for initial treat- ment) 450 mg daily after titration with another product (300 mg/day × ≥2 wk)
PDF page 205
• Geriatric: PO 50-100 mg/day, may in- crease by 50-100 mg q3-4days Smoking cessation (Zyban)
PDF page 205
• Adult: SR 150 mg daily × 3 days, then 150 mg bid for remainder of treatment Seasonal affective disorder
PDF page 205
• Adult: PO (Wellbutrin XL) 150 mg as a single dose in the AM, after 1 wk may be increased to 300 mg/day; (Aplenzin) 174 mg daily in AM, after 7 days may in- crease to 348 mg daily Hepatic dose Adult: PO (moderate-severe) Aplenzin max 174 mg every other day
PDF page 205