Brofaromine: Difference between revisions

Brofaromine
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Revision as of 03:56, 13 February 2025

Overview of the antidepressant drug Brofaromine

Brofaromine is a reversible inhibitor of monoamine oxidase A (RIMA) that was developed as an antidepressant and anxiolytic agent. It belongs to the class of monoamine oxidase inhibitors (MAOIs), which are used to treat depression by increasing the levels of neurotransmitters in the brain.

Mechanism of Action

Brofaromine works by selectively inhibiting the enzyme monoamine oxidase A (MAO-A). This enzyme is responsible for breaking down monoamines such as serotonin, norepinephrine, and dopamine. By inhibiting MAO-A, brofaromine increases the availability of these neurotransmitters, which can help alleviate symptoms of depression and anxiety.

Pharmacokinetics

Brofaromine is absorbed from the gastrointestinal tract and undergoes extensive first-pass metabolism. It has a relatively short half-life, which allows for reversible inhibition of MAO-A, reducing the risk of hypertensive crisis associated with traditional MAOIs.

Clinical Use

Brofaromine was investigated for the treatment of major depressive disorder and anxiety disorders. However, it was never marketed due to the development of newer antidepressants with more favorable side effect profiles.

Side Effects

Common side effects of brofaromine include nausea, headache, and insomnia. Unlike traditional MAOIs, brofaromine has a lower risk of causing tyramine-induced hypertensive crisis, allowing for a less restrictive diet.

Development and History

Brofaromine was developed in the 1980s and underwent clinical trials to assess its efficacy and safety. Despite promising results, it was not brought to market, partly due to the emergence of selective serotonin reuptake inhibitors (SSRIs) and other antidepressants that offered similar benefits with fewer dietary restrictions and side effects.

Related pages

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-'''Brofaromine''' is a [[reversible inhibitor of monoamine oxidase A]] (RIMA) and a [[5-HT reuptake inhibitor]] that was investigated for its potential use in the treatment of [[depression]] and [[anxiety disorders]]. Despite showing promise in clinical trials, brofaromine has not been widely marketed or approved for medical use in many countries. Its chemical structure and mechanism of action share similarities with other antidepressants, but its unique properties as a RIMA make it of particular interest in psychiatric pharmacology.
+{{Short description|Overview of the antidepressant drug Brofaromine}}
+{{Drugbox
+| image = Brofaromine.svg
+| image_size = 200px
+| image_alt = Chemical structure of Brofaromine
+}}
+'''Brofaromine''' is a [[reversible inhibitor of monoamine oxidase A]] (RIMA) that was developed as an [[antidepressant]] and [[anxiolytic]] agent. It belongs to the class of [[monoamine oxidase inhibitors]] (MAOIs), which are used to treat [[depression]] by increasing the levels of [[neurotransmitters]] in the brain.
 ==Mechanism of Action==
-Brofaromine acts primarily by inhibiting the enzyme [[monoamine oxidase A]] (MAO-A), which is responsible for the breakdown of monoamines such as [[serotonin]], [[norepinephrine]], and [[dopamine]]. By inhibiting this enzyme, brofaromine increases the levels of these neurotransmitters in the brain, which can help improve mood and alleviate symptoms of depression. Unlike non-selective monoamine oxidase inhibitors (MAOIs), brofaromine selectively targets MAO-A, reducing the risk of [[hypertensive crisis]] associated with dietary tyramine intake, a serious side effect of older MAOIs. Additionally, its ability to inhibit the reuptake of serotonin contributes to its antidepressant effects.
+Brofaromine works by selectively inhibiting the enzyme [[monoamine oxidase A]] (MAO-A). This enzyme is responsible for breaking down [[monoamines]] such as [[serotonin]], [[norepinephrine]], and [[dopamine]]. By inhibiting MAO-A, brofaromine increases the availability of these neurotransmitters, which can help alleviate symptoms of depression and anxiety.
-==Clinical Uses==
+==Pharmacokinetics==
-Brofaromine was primarily investigated for its potential in treating major depressive disorder (MDD) and various anxiety disorders. Clinical trials have demonstrated its efficacy in reducing depressive symptoms, with an advantage of having a more favorable side effect profile compared to traditional MAOIs and some tricyclic antidepressants (TCAs). Its anxiolytic effects also suggested potential use in treating social anxiety disorder and panic disorder, but further research was needed to fully establish its effectiveness and safety for these conditions.
+Brofaromine is absorbed from the [[gastrointestinal tract]] and undergoes extensive [[first-pass metabolism]]. It has a relatively short half-life, which allows for reversible inhibition of MAO-A, reducing the risk of [[hypertensive crisis]] associated with traditional MAOIs.
-==Pharmacokinetics==
+==Clinical Use==
-The pharmacokinetic profile of brofaromine includes oral administration with good absorption. It is metabolized in the liver and has a relatively short half-life, which necessitates daily dosing to maintain therapeutic levels. The drug's metabolism and excretion pathways suggest that dose adjustments may be necessary in patients with hepatic impairment, but its overall pharmacokinetics are considered favorable for an antidepressant.
+Brofaromine was investigated for the treatment of [[major depressive disorder]] and [[anxiety disorders]]. However, it was never marketed due to the development of newer antidepressants with more favorable side effect profiles.
-==Adverse Effects==
+==Side Effects==
-Brofaromine is generally well tolerated, with fewer dietary restrictions compared to non-selective MAOIs due to its selectivity for MAO-A. However, it can still cause some adverse effects, including insomnia, nausea, dizziness, and headaches. The risk of serotonin syndrome, a potentially life-threatening condition, may be increased if brofaromine is combined with other serotonergic drugs.
+Common side effects of brofaromine include [[nausea]], [[headache]], and [[insomnia]]. Unlike traditional MAOIs, brofaromine has a lower risk of causing [[tyramine]]-induced hypertensive crisis, allowing for a less restrictive diet.
-==Current Status==
+==Development and History==
-As of the last update, brofaromine has not been approved for clinical use in the United States, European Union, or many other regions. Its development was discontinued for reasons that are not entirely clear but may include commercial considerations or the emergence of other antidepressants with similar or better efficacy and safety profiles. Despite its limited availability, research on brofaromine contributes to the understanding of RIMAs and their potential role in treating mood and anxiety disorders.
+Brofaromine was developed in the 1980s and underwent clinical trials to assess its efficacy and safety. Despite promising results, it was not brought to market, partly due to the emergence of [[selective serotonin reuptake inhibitors]] (SSRIs) and other antidepressants that offered similar benefits with fewer dietary restrictions and side effects.
-==See Also==
+==Related pages==
 * [[Monoamine oxidase inhibitor]]
-* [[Depression]]
+* [[Antidepressant]]
-* [[Anxiety disorder]]
+* [[Anxiolytic]]
 * [[Serotonin]]
+* [[Norepinephrine]]
+* [[Dopamine]]
 [[Category:Antidepressants]]
 [[Category:Monoamine oxidase inhibitors]]
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