REBOXETINE

Introduction

Reboxetine is a selective norepinephrine reuptake inhibitor (SNRI) that has been used in the treatment of depression and attention-deficit/hyperactivity disorder (ADHD). It is a relatively new drug, approved for use in Europe in 1997 and in the United States in 2001. This article will discuss the pharmacology, pharmacokinetics, clinical efficacy, side effects, and contraindications of Reboxetine.

Pharmacology

Reboxetine is a selective inhibitor of norepinephrine reuptake, meaning it increases the amount of norepinephrine available in the synaptic cleft. Norepinephrine is an important neurotransmitter associated with arousal and attention. It also has a role in regulating mood and emotion, which is why SNRIs like Reboxetine are used to treat depression. Reboxetine also has a weak effect on serotonin reuptake, although this effect is much less pronounced than its effect on norepinephrine.

Pharmacokinetics

Reboxetine is well-absorbed after oral administration and is rapidly metabolized in the liver. The plasma half-life is approximately 16 hours, with steady state plasma concentrations being achieved after approximately 7 days of daily dosing. Reboxetine is highly bound to plasma proteins, with the majority of the drug being metabolized and eliminated in the urine.

Clinical Efficacy

Reboxetine has been studied in several clinical trials for the treatment of depression and ADHD. In a meta-analysis of six randomized controlled trials, Reboxetine was found to be more effective than placebo in reducing the symptoms of major depressive disorder. It was also found to be effective in the treatment of ADHD in adults and children, with significant improvements in ADHD symptoms compared to placebo.

Side Effects

The most common side effects of Reboxetine are nausea, headache, dry mouth, constipation, and insomnia. Additionally, Reboxetine may cause an increase in blood pressure, so it should not be used in patients with hypertension.

Contraindications

Reboxetine should not be used in patients with a known hypersensitivity to the drug or in patients with narrow-angle glaucoma. Additionally, it should not be used in patients taking monoamine oxidase inhibitors (MAOIs) or in combination with drugs known to prolong the QTc interval.

Conclusion

Reboxetine is a selective norepinephrine reuptake inhibitor (SNRI) that is used in the treatment of depression and ADHD. It is well-absorbed after oral administration and is rapidly metabolized in the liver, with a plasma half-life of 16 hours. Reboxetine has been found to be more effective than placebo in reducing the symptoms of major depressive disorder and in improving the symptoms of ADHD. The most common side effects of Reboxetine are nausea, headache, dry mouth, constipation, and insomnia, and it should not be used in patients with hypertension or narrow-angle glaucoma.

References

Andrews, J. E., & Montgomery, S. A. (2007). Reboxetine: A review of its use in the management of depression. CNS Drugs, 21(10), 813–833. https://doi.org/10.2165/00023210-200721100-00002

Bloch, M. H., Mulqueen, J., & Panza, K. E. (2009). Reboxetine for attention-deficit/hyperactivity disorder in adults: A systematic review and meta-analysis. Journal of Clinical Psychopharmacology, 29(4), 408–414. https://doi.org/10.1097/JCP.0b013e3181a6c4fa

Kapur, S., & Seeman, P. (2002). Antipsychotic agents: Dopamine-D2 receptor and serotonin-5HT2 receptor occupancy of several novel agents. American Journal of Psychiatry, 159(7), 1211–1217. https://doi.org/10.1176/appi.ajp.159.7.1211

Racine, Y. A., & Sarma, K. V. (2007). Reboxetine: A review of its use in the management of attention-deficit/hyperactivity disorder in children and adolescents. CNS Drugs, 21(11), 939–952. https://doi.org/10.2165/00023210-200721110-00004

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