brands

Class

• Neuroscience-based Nomenclature:dopamine reuptake inhibitor and releaser(D-RIRe)
• Norepinephrine and dopamine reuptakeinhibitor; antidepressant; smoking cessation treatment

BUPROPION commonly prescribed for

(Bold for FDA approved)

How BUPROPION works

• Boosts neurotransmitters norepinephrine and dopamine

• Blocks norepinephrine reuptake pump (norepinephrine transporter), presumably increasing norepinephrine neurotransmission

• Since dopamine is inactivated by norepinephrine reuptake in the frontal cortex, which largely lacks dopamine transporters, bupropion can increase dopamine neurotransmission in this part of the brain

• Blocks dopamine reuptake pump (dopamine transporter), presumably increasing dopaminergic neurotransmission

How long until BUPROPION works

Onset of therapeutic actions usually not immediate, but often delayed 2–4 weeks If it is not working within 6–8 weeks for depression, it may require a dosage increase or it may not work at all May continue to work for many years to prevent relapse of symptoms

Notable Side Effects

• Dry mouth, constipation, nausea

• Insomnia, dizziness, headache, agitation, anxiety, tremor

• Sweating

• Weight loss, anorexia

• Myalgia, abdominal pain, tinnitus, rash

• Hypertension

Life Threatening Side Effects

• Rare seizures (higher incidence for immediate-release than for sustained release; risk increases with doses above the recommended maximums; risk increases for patients with predisposing factors)

• Anaphylactoid/anaphylactic reactions and Stevens–Johnson syndrome have been reported

• Hypomania (more likely in bipolar patients but perhaps less common than with some other antidepressants)

• Rare induction of mania

• Rare activation of suicidal ideation and behavior (suicidality) (short-term studies did not show an increase in the risk of suicidality with antidepressants compared to placebo beyond age 24)

weight gain

unusual

sedation

unusual

What to do about BUPROPION side effects

• Wait

• Wait

• Wait

• Keep dose as low as possible

• Take no later than mid-afternoon to avoid insomnia

• Switch to another drug

usual dosage range

• Bupropion: 225–450 mg in 3 divided doses (maximum single dose 150 mg)

• Bupropion SR: 200–450 mg in 2 divided doses (maximum single dose 200 mg)

• Bupropion XL: 150–450 mg once daily (maximum single dose 450 mg)

• Bupropion hydrobromide: 174–522 mg once daily (maximum single dose 522 mg)

Dosage Forms

• Bupropion: tablet 75 mg, 100 mg

• Bupropion SR (sustained-release): tablet 100 mg, 150 mg, 200 mg

• Bupropion XL (extended-release): tablet 150 mg, 300 mg, 450 mg

long term use

• For smoking cessation, treatment for up to 6 months has been found effective

• For depression, treatment up to 1 year has been found to decrease rate of relapse

habit forming

• No

• Can be abused by individuals who crushand then snort or inject it

Renal Impairment

• Lower initial dose, perhaps give less frequently

• Drug concentration may be increased

• Patient should be monitored closely

Hepatic Impairment

• Lower initial dose, perhaps give less frequently

• Patient should be monitored closely

• In severe hepatic cirrhosis, bupropion XL should be administered at no more than 150 mg every other day

Cardiac Impairment

• Limited available data

• Evidence of rise in supine blood pressure

• Use with caution

Elderly

• Some patients may tolerate lower doses better

• Reduction in the risk of suicidality with antidepressants compared to placebo in adults age 65 and older

Children and Adolescents

• Carefully weigh the risks and benefits of pharmacological treatment against the risks and benefits of nontreatment with antidepressants and make sure to document this in the patient’s chart

• Monitor patients face-to-face regularly, particularly during the first several weeks of treatment

• Use with caution, observing for activation of known or unknown bipolar disorder and/ or suicidal ideation, and inform parents or guardians of this risk so they can help observe child or adolescent patients

• Safety and efficacy have not been established

• May be used for ADHD in children or adolescents

• May be used for smoking cessation in adolescents

• Preliminary research suggests efficacy in comorbid depression and ADHD

• Dosage may follow adult pattern for adolescents

• Children may require lower doses initially, with a maximum dose of 300 mg/day

Pregnancy

• Controlled studies have not been conducted in pregnant women

• Epidemiological studies do not indicate increased risk of congenital malformations overall or of cardiovascular malformations

• Pregnant women wishing to stop smoking may consider behavioral therapy before pharmacotherapy

• Not generally recommended for use during pregnancy, especially during first trimester

• Must weigh the risk of treatment (first trimester fetal development, third trimester newborn delivery) to the child against the risk of no treatment (recurrence of depression, maternal health, infant bonding) to the mother and child

• For many patients this may mean continuing treatment during pregnancy

Breast Feeding

• Some drug is found in mother’s breast milk

• If child becomes irritable or sedated, breast feeding or drug may need to be discontinued

• Immediate postpartum period is a high-risk time for depression, especially in women who have had prior depressive episodes, so drug may need to be reinstituted late in the third trimester or shortly after childbirth to prevent a recurrence during the postpartum period

• Must weigh benefits of breast feeding with risks and benefits of antidepressant treatment versus nontreatment to both the infant and the mother

• For many patients, this may mean continuing treatment during breast feeding