Brexpiprazole

Brexpiprazole, known by its trade name Rexulti, is classified as an atypical antipsychotic medication. Its primary applications include the treatment of schizophrenia and major depressive disorder, where it may be utilized as an adjunct to antidepressants. Additionally, it is indicated for managing agitation associated with Alzheimer’s disease. The compound demonstrates its effects primarily via partial agonism at the D₂ and D₃ dopamine receptors, as well as the 5-HT_1A serotonin receptors. Additionally, it exhibits antagonistic properties towards the 5-HT_2A, 5-HT_2B, 5-HT₇, H₁, and M₁ receptors. The primary metabolic pathways involve the CYP3A4 and CYP2D6 enzymes, with excretion occurring through both the liver and kidneys, and a half-life established at 96 hours. This treatment demonstrates clinical efficacy in addressing acute episodes of schizophrenia by mitigating psychotic symptoms and enhancing psychosocial functioning, as well as in maintenance therapy, prolonging the time to relapse in contrast to placebo. Research findings indicate that brexpiprazole may have the potential to address the social cognition deficits associated with autism spectrum disorder (ASD). This compound functions as a partial dopamine agonist and is currently under investigation for its potential role as an adjunctive therapy in individuals with ADHD who do not respond adequately to stimulant medications.

Brexpiprazole exerts its effects by modulating the levels of dopamine and serotonin, thereby impacting a range of brain functions. These include the regulation of mood, motivation, and cognitive processes such as attention, memory, and executive function. Research indicates that brexpiprazole may facilitate neurite outgrowth and provide neuroprotection, which could have implications for neuronal plasticity and overall brain health. The pharmacological profile indicates a potential enhancement in the release of dopamine and acetylcholine within the prefrontal cortex, which may contribute to the improvement of cognitive function, alleviation of depression, and reduction of negative psychotic symptoms. Certain patients may observe enhancements in cognitive function following brexpiprazole treatment, including heightened concentration, better memory retention, or diminished cognitive deficits, which may occur as a secondary outcome of alleviating the symptoms associated with their underlying psychiatric disorders.

Brexpiprazole demonstrates a favorable tolerance profile among patients during both acute and maintenance phases of treatment. Among various antipsychotic medications, it stands out due to its advantageous side effect profile, notably its minimal influence on prolactin levels and QTc interval, along with a limited effect on body weight and a reduced risk of akathisia.

Benefits of taking brexpiprazole

• attenuated symptoms of schizophrenia;

• alleviates depression;

• diminished anhedonia;

• reduced social cognition deficits;

• improved attention;

• better memory retention;

• possible neuroprotective properties;

• might enhance neuroplasticity.

Side effects

• tiredness;

• drowsiness;

• weight gain;

• constipation;

• headache;

• tremor;

• akathisia.

Dosage

Brexpiprazole is effective against acute episodes of schizophrenia at oral daily doses of 2-4 mg, while its maintenance doses range from 1 to 4 mg per day. While it is important to take it at the same time each day, it might be taken in the morning or in the evening.