Category:Atypical antipsychotic: Difference between revisions

Antipsychotic Drug

Drug class: Atypical antipsychotic

Brexpiprazole (Rexulti)（中文：銳思定）

Common Strengths of Brexpiprazole Tablet

Brexpiprazole tablets are available in the following strengths:

• 0.25 mg

• 0.5 mg

• 1 mg

• 2 mg

• 3 mg

• 4 mg

Drug Trade Names of BrexpiprazoleBrexpiprazole Tablet

Rexulti is the trade name for Brexpiprazole:

Drug Usage

Brexpiprazole is used for:

• Treatment of schizophrenia
• Adjunctive treatment of major depressive disorder (MDD)
• Treatment of agitation associated with dementia due to Alzheimer's disease

Mechanism of Action

Brexpiprazole acts as a partial agonist at dopamine D2 and serotonin 5-HT1A receptors and as an antagonist at serotonin 5-HT2A receptors. It modulates dopaminergic and

serotonergic activity to improve symptoms of schizophrenia and depression

Route of Administration

Brexpiprazole is administered orally in the form of tablets or liquid solution.

Dosages

• Schizophrenia (Adults): Initial dose of 1 mg once daily, titrated to 2 mg on Day 5 to 7, and up to 4 mg by Day 8. Target dose: 2 to 4 mg daily. Maximum dose: 4 mg/day.

• Depression (Adults): Initial dose of 0.5 mg or 1 mg once daily, titrated to 2 mg daily. Maximum dose: 3 mg/day.
• Pediatric Schizophrenia (13-17 years): Initial dose of 0.5 mg once daily, titrated to 1 mg on Day 5 to 7, and up to 2 mg by Day 8. Maximum dose: 4 mg/day.

For patients with moderate to severe renal impairment, the dosage of brexpiprazole should be reduced to a maximum of 3 mg per day for schizophrenia and 2 mg per day for MDD.

No adjustment is needed for mild renal impairment.

Side Effects

Pharmacokinetics

• Absorption
  • Bioavailability is 50-60%. Metformin reaches maximum plasma concentration in 1-3 hours after taking immediate-release tablets. For extended-release formulations, peak plasma levels are reached in 4-8 hours.
• Metabolism
  • Not metabolized by the liver.
• Excretion
  • Primarily excreted unchanged in urine.
• Half-life
  • 4 - 8.7 hours

Drug Precautions

Pregnancy

Generally considered safe, but should be used under medical supervision.

Breastfeeding

Metformin is excreted in breast milk, but the risk to the infant is considered low.

Children and Elderly

• Not recommended for children under 10 years.
• Use with caution in the elderly due to the potential for decreased renal function.

Renal Impairment

• Contraindicated in patients with eGFR < 30 mL/min/1.73 m².
• Dose adjustments required for eGFR 30-44 mL/min/1.73 m².

Monitoring Requirements

• Regularly monitor renal function, blood glucose, and vitamin B12 levels.
• Monitor for signs of lactic acidosis, especially in patients with renal impairment.

The key symptoms of metformin-associated lactic acidosis (MALA) include:

It is important to note that these symptoms can be nonspecific and may overlap with other conditions. MALA is a medical emergency that requires immediate treatment.

Drug Interaction

• Cimetidine: This antacid can increase metformin levels in the blood by inhibiting its elimination.
• Diuretics, especially loop diuretics eg Frusemide: Can increase the risk of lactic acidosis
• Corticosteroids: May increase blood glucose levels, potentially reducing metformin's effectiveness
• NSAIDs: Long-term use may increase the risk of lactic acidosis, especially in those with reduced kidney function

FAQ

How Should I Take the Tablet?

• Take with meals to reduce gastrointestinal side effects.
• Swallow whole; do not crush or chew extended-release tablets.

What Should I Avoid While Taking?

• Avoid excessive alcohol consumption due to increased risk of lactic acidosis.
• Avoid skipping meals to prevent hypoglycemia.

What Happens if I Miss a Dose?

• Take the missed dose as soon as you remember unless it is almost time for the next dose.
• Do not double the dose to make up for the missed one.