REBOXETINE

brands

Class

• Neuroscience-based Nomenclature: norepinephrine reuptake inhibitor (N-RI)
• Selective norepinephrine reuptake inhibitor (NRI); antidepressant

REBOXETINE commonly prescribed for

(Bold for FDA approved)

How REBOXETINE works

• Boosts neurotransmitter norepinephrine and may also increase dopamine in prefrontal cortex

• Blocks norepinephrine reuptake pump (norepinephrine transporter)

• Presumably, this increases noradrenergic neurotransmission

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

How long until REBOXETINE 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

• Insomnia, dizziness, anxiety, agitation

• Dry mouth, constipation

• Urinary hesitancy, urinary retention

• Sexual dysfunction (impotence)

• Dose-dependent hypotension

Life Threatening Side Effects

• Rare seizures

• 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 REBOXETINE side effects

• Wait

• Wait

• Wait

• Lower the dose

• In a few weeks, switch or add other drugs

usual dosage range

• 8 mg/day in 2 doses (10 mg usual maximum daily dose)

Dosage Forms

• Tablet 2 mg, 4 mg scored

long term use

• Safe

habit forming

• No

Renal Impairment

• Plasma concentrations are increased

• May need to lower dose

Hepatic Impairment

• Plasma concentrations are increased

• May need to lower dose

Cardiac Impairment

• Use with caution

Elderly

• Lower dose is recommended (4–6 mg/day)

• 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

• No guidelines for children; safety and efficacy have not been established

Pregnancy

• No controlled studies in humans

• 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

• 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