Reboxetine

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Substrate of
  • Inhibits
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Austria: Edronax; Belgium: Edronax; Bulgaria: Edronax; Denmark: Edronax; Estonia: Edronax; Finland: Edronax; Germany: Edronax, Solvex; Hungary: Edronax; Ireland: Edronax; Italy: Davedax, Edronax; Latvia: Edronax; Luxembourg: Edronax; Poland: Edronax; Portugal: Edronax; Slovenia: Edronax; Spain: Irenor, Norebox; Sweden: Edronax; UK: Edronax.

Latin America

Brazil: Prolift; Mexico: Edronax.

Drug combinations

Chemistry

Reboxetine Mesylate: C~19~H~23~NO~3~ CH~4~O~3~S. Mw: 409.50. (1)(±)-(R*,S*)-2-[(2-Ethoxyphenoxy)phenylmethyl]morpholine methanesulfonate; (2)(±)-(2R*)-2-[(αS*)-α-(o-Ethoxyphenoxy)benzyl]morpholine methanesulfonate. CAS-98769-84-7 (1997).

Pharmacologic Category

Antidepressants, Miscellaneous. (ATC-Code: N06AX18).

Mechanism of action

A highly selective and potent inhibitor of noradrenaline reuptake. Only has weak effect on 5-HT reuptake and does not affect uptake of dopamine. In vitro, studies have shown reboxetine has no significant affinity for adrenergic (α~1~-, α~2~-, β-) or muscarinic receptors. Devoid of in vitro binding to either α~1~- or α~2~-adrenoreceptors; however, functional interference with α-adrenoreceptors at high doses in vivo cannot be excluded. In healthy volunteers administration of reboxetine single doses of 1 and 3 mg was followed by dose-dependent CNS effects with EEG modifications (decreased power of θ- and fast β-waves in fronto-central derivative) and performance improvement (peg-board test).

Therapeutic use

Depressive illness.

Pregnancy and lactiation implications

Increased post-implantation loss, decreased mean fetal weight and increased incidence of skeletal anomalies, including delayed ossification, described in animals. Reboxetine should be used during pregnancy only if potential benefit justifies potential risk to fetus. Excreted in milk of lactating rats; reduces survival of offspring and retards postnatal growth and development. While no information is available on excretion of reboxetine in maternal milk in humans, reboxetine administration not recommended in breast-feeding women.

Unlabeled use

Contraindications

Hypersensitivity to reboxetine or any other components of the compound. Concomitant use in patients taking MAOIs. Narrow-angle glaucoma.

Warnings and precautions

Cases of seizures reported (discontinue if seizures develop). Switches to mania/hypomania occurred during clinical studies (caution in bipolar patients). Risk of suicidal attempt inherent in depression and may persist until significant remission occurs. Symptoms of anxiety, agitation, panic attacks, insomnia, irritability, hostility (aggressiveness), impulsivity, akathisia (psychomotor restlessness), hypomania, and mania, reported with antidepressants for major depressive disorder as well as for other indications, both psychiatric and nonpsychiatric. Close supervision should be applied in current evidence of urinary retention, prostatic hypertrophy and glaucoma. Patients (particularly aged >65 years) with history of cardiac disease, including hypertension, should be closely supervised. At doses higher than recommended maximum, orthostatic hypotension observed with greater frequency. Caution in known cardiovascular disease, cerebrovascular disease, and conditions that would predispose patients to hypotension. Caution indicated in treating patients whose underlying medical conditions might be compromised by increases in blood pressure, those with pre-existing hypertension, heart failure or recent MI. Use with caution in patients whose underlying medical conditions might be compromised by increases in heart rate, e.g. hyperthyroidism, heart failure, or recent MI. Should not be taken with, or within 2 weeks of stopping, an MAOI.

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