Reboxetine
Reboxetine is a selective norepinephrine reuptake inhibitor indicated for depression in some international markets but not approved in the United States. It represents one of the few antidepressants with highly selective norepinephrine reuptake inhibition, potentially offering benefits for patients with depression characterized by fatigue, low energy, and motivation problems.
Clinical Overview
Primary Clinical Applications
Reboxetine is indicated for major depressive disorder in countries where it is available. It may be particularly useful for patients with depression accompanied by fatigue, psychomotor retardation, or lack of motivation, as norepinephrine enhancement can provide activating and energizing effects.
Mechanism and Clinical Benefits
Reboxetine selectively inhibits the norepinephrine transporter with minimal effects on serotonin, dopamine, or other neurotransmitter systems. This selective noradrenergic activity may provide antidepressant effects while potentially improving energy, motivation, and concentration without the sexual side effects commonly associated with serotonergic antidepressants.
Clinical Considerations
Reboxetine generally has fewer sexual side effects compared to SSRIs and may actually improve sexual function in some patients. However, it can cause significant cardiovascular effects including increased heart rate and blood pressure, requiring monitoring. The medication may also cause urinary retention and sleep disturbances due to its noradrenergic activity.
Key Clinical Points
Not approved in the United States
Available as Norebox or Edronax in some international markets. It is one of the few purely noradrenergic antidepressants, which is why it retains interest despite limited availability.
Cardiovascular monitoring required
Increased heart rate, hypertension, and palpitations follow directly from noradrenergic selectivity. Blood pressure and pulse should be checked at baseline and during titration.
Contraindicated in urinary retention and narrow-angle glaucoma
Noradrenergic activity produces urinary hesitancy that becomes retention in men with prostatic hypertrophy. Also contraindicated in severe renal impairment and with MAOIs.
Low sexual dysfunction
Rates are lower than with SSRIs and some patients report improvement. Weight gain is also minimal, which are the main reasons for choosing it.
Twice-daily dosing with reduced elderly doses
8 to 12 mg daily in adults, halved to 4 to 6 mg in older patients. Insomnia is common and may require attention to dose timing.
Prescribing Information
Dosing & Administration
Depression – Adults:
- Initial: 4 mg twice daily (8 mg daily)
- Range: 8-12 mg daily in divided doses
- Maximum: 12 mg daily
Elderly:
- Initial: 2 mg twice daily (4 mg daily)
- Range: 4-6 mg daily in divided doses
- Maximum: 6 mg daily
Administration:
- Divide daily dose into twice daily dosing
- Take with or without food
- Consistent timing each day
- Monitor blood pressure and heart rate
Indications
- Treatment of major depressive disorder (in countries where available)
- Not approved in the United States
Contraindications
- Hypersensitivity to reboxetine
- Concurrent use with MAOIs
- Severe renal impairment
- Urinary retention
- Narrow-angle glaucoma
Warnings & Precautions
- Cardiovascular effects: Monitor blood pressure and heart rate regularly
- Urinary retention: Risk in patients with prostatic hypertrophy
- Angle-closure glaucoma: May precipitate acute attack
- Suicidal ideation: Monitor for mood changes, especially early in treatment
- Withdrawal: Taper gradually when discontinuing
- Insomnia: May cause sleep disturbances
Drug Interactions
- MAOIs: Contraindicated – risk of hypertensive crisis
- CYP3A4 inhibitors: May increase reboxetine levels
- Antihypertensives: May reduce antihypertensive effectiveness
- Ergot alkaloids: Risk of hypertensive reactions
Adverse Reactions
Common (>10%):
- Dry mouth, constipation, insomnia, sweating
- Dizziness, nausea, urinary hesitancy
Cardiovascular:
- Increased heart rate, hypertension, palpitations
Advantages:
- Lower rates of sexual dysfunction compared to SSRIs
- May improve energy and motivation
- Minimal weight gain
Special Populations
- Cardiovascular Disease: Use caution, monitor blood pressure and heart rate
- Renal Impairment: Contraindicated in severe impairment
- Elderly: Start with lower doses, monitor cardiovascular effects
- Pregnancy: Limited data, use only if benefits outweigh risks
- Availability: Not available in United States
Frequently Asked Questions
What is Reboxetine used for?
Reboxetine is a selective norepinephrine reuptake inhibitor indicated for depression in some international markets but not approved in the United States. It represents one of the few antidepressants with highly selective norepinephrine reuptake inhibition, potentially offering benefits for patients with depression characterized by fatigue, low energy, and motivation problems.
What class of drug is Reboxetine?
Reboxetine is classified as: Selective Norepinephrine Reuptake Inhibitor (SNRI).
Not approved in the United States?
Available as Norebox or Edronax in some international markets. It is one of the few purely noradrenergic antidepressants, which is why it retains interest despite limited availability.
Cardiovascular monitoring required?
Increased heart rate, hypertension, and palpitations follow directly from noradrenergic selectivity. Blood pressure and pulse should be checked at baseline and during titration.
Contraindicated in urinary retention and narrow-angle glaucoma?
Noradrenergic activity produces urinary hesitancy that becomes retention in men with prostatic hypertrophy. Also contraindicated in severe renal impairment and with MAOIs.
Low sexual dysfunction?
Rates are lower than with SSRIs and some patients report improvement. Weight gain is also minimal, which are the main reasons for choosing it.