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| [[Category: Drugs]][[Category: Atypical antipsychotic ]] | | [[Category: Antipsychotic Drug]] |
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| [[:Category: Antipsychotic Drug | '''Antipsychotic Drug''']]
| | '''Atypical Antipsychotic'''（中文：[[:Category: 非典型抗精神病藥物 | 非典型抗精神病藥物]]） |
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| '''Drug class: [[:Category: Atypical antipsychotic | Atypical antipsychotic]]
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| '''Brexpiprazole (Rexulti)'''（中文：[[銳思定]]）
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| ==Common Strengths of Brexpiprazole Tablet==
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| Brexpiprazole tablets are available in the following strengths:
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| * 0.25 mg
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| * 0.5 mg
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| * 1 mg
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| * 2 mg
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| * 3 mg
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| * 4 mg
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| ==Drug Trade Names of BrexpiprazoleBrexpiprazole Tablet==
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| Rexulti is the trade name for Brexpiprazole:
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| ==Drug Usage==
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| Brexpiprazole is used for:
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| * Treatment of schizophrenia
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| * Adjunctive treatment of major depressive disorder (MDD)
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| * Treatment of agitation associated with dementia due to Alzheimer's disease
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| ==Mechanism of Action==
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| 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
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| serotonergic activity to improve symptoms of schizophrenia and depression
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| ==Route of Administration==
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| Brexpiprazole is administered orally in the form of tablets or liquid solution.
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| ==Dosages==
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| * 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.
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| * Depression (Adults): Initial dose of 0.5 mg or 1 mg once daily, titrated to 2 mg daily. Maximum dose: 3 mg/day.
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| * 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.
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| 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.
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| No adjustment is needed for mild renal impairment.
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| ==Side Effects==
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| {| class="wikitable"
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| !style="text-align: left"| Frequency
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| !Adverse reactions
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| |-
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| | rowspan="12" | '''Common
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| | Weight gain
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| | Akathisia (feeling of restlessness, constant urge to move)
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| | Headache
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| | Drowsiness/sleepiness
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| | Dizziness
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| | Nausea
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| | Constipation
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| |-
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| | Indigestion/heartburn
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| | Increased appetite
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| | Fatigue/tiredness
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| | Tremor
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| | Stuffy or runny nose
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| | rowspan="13" | '''Uncommon
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| | Neuroleptic malignant syndrome (high fever, muscle stiffness, confusion)
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| | Tardive dyskinesia (uncontrolled muscle movements)
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| | High blood sugar/diabetes
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| | Orthostatic hypotension (dizziness when standing up)
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| | Seizures
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| | Low white blood cell count
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| | Difficulty swallowing
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| | Suicidal thoughts or behaviors (especially in young adults)
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| | Compulsive behaviors (gambling, sexual urges, binge eating)
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| | Cognitive impairment
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| | Impaired body temperature regulation
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| | Stroke in elderly patients with dementia-related psychosis
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| | Allergic reactions (rash, itching, difficulty breathing)
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| |}
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| ==Pharmacokinetics==
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| *Absorption
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| **Peak plasma concentration within 4 hours.
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| *Metabolism
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| **Primarily metabolized by CYP3A4 and CYP2D6.
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| *Excretion
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| **25% in urine and 46% in feces. Terminal elimination half-life is approximately 91 hours.
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| Initial effects: Some patients may begin to see improvements within 1 to 2 weeks of starting treatment.
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| Full Therapeutic Effects: The best results are typically observed after 4 to 6 weeks for schizophrenia and major depressive disorder (MDD) For agitation associated with
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| dementia due to Alzheimer's disease, significant results may be seen in about 12 weeks.
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| ==Drug Precautions==
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| '''Increased risk in elderly patients
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| *Should not be used to treat dementia-related psychosis in older adults due to increased risk of stroke and death
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| *May cause drowsiness, dizziness, and difficulty swallowing in elderly patients, increasing the risk of falls and choking
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| '''Breastfeeding
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| Metformin is excreted in breast milk, but the risk to the infant is considered low.
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| '''Children and Elderly
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| *Not recommended for children under 10 years.
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| *Use with caution in the elderly due to the potential for decreased renal function.
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| '''Renal Impairment
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| *Contraindicated in patients with eGFR < 30 mL/min/1.73 m<sup>2</sup>.
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| *Dose adjustments required for eGFR 30-44 mL/min/1.73 m<sup>2</sup>.
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| '''Monitoring Requirements
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| *Regularly monitor renal function, blood glucose, and vitamin B12 levels.
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| *Monitor for signs of lactic acidosis, especially in patients with renal impairment.
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| The key symptoms of metformin-associated lactic acidosis (MALA) include:
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| {| class="wikitable"
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| | rowspan="3" | '''Gastrointestinal
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| | Nausea and vomiting
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| | Abdominal pain
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| | Diarrhoea
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| | rowspan="2" | '''Neurological
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| | Confusion
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| | Lethargy
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| | rowspan="2" | '''Resoiratory
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| | Rapid breathing
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| | Difficulty breathing
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| | rowspan="2" | '''Cardiovascular
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| | Hypotension
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| | Rapid heart rate
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| | rowspan="2" | '''General
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| | Extreme tiredness
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| | Feeling cold, especially in arms and legs
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| | rowspan="2" | '''Other
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| | Dizziness
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| | Lighteadedness
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| |}
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| 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.
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| '''Drug Interaction
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| *Cimetidine: This antacid can increase metformin levels in the blood by inhibiting its elimination.
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| *Diuretics, especially loop diuretics eg Frusemide: Can increase the risk of lactic acidosis
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| *Corticosteroids: May increase blood glucose levels, potentially reducing metformin's effectiveness
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| *NSAIDs: Long-term use may increase the risk of lactic acidosis, especially in those with reduced kidney function
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| ==FAQ==
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| '''How Should I Take the Tablet?
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| *Take with meals to reduce gastrointestinal side effects.
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| *Swallow whole; do not crush or chew extended-release tablets.
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| '''What Should I Avoid While Taking?
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| *Avoid excessive alcohol consumption due to increased risk of lactic acidosis.
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| *Avoid skipping meals to prevent hypoglycemia.
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| '''What Happens if I Miss a Dose?
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| *Take the missed dose as soon as you remember unless it is almost time for the next dose.
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| *Do not double the dose to make up for the missed one.
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