Brofaromine

Overview of the antidepressant drug Brofaromine

Brofaromine
INN
Drug class
Routes of administration
Pregnancy category
Bioavailability
Metabolism
Elimination half-life
Excretion
Legal status
CAS Number
PubChem
DrugBank
ChemSpider
KEGG

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

• Monoamine oxidase inhibitor
• Antidepressant
• Anxiolytic
• Serotonin
• Norepinephrine
• Dopamine