Brexpiprazole
Brexpiprazole Uses, Dosage, Side Effects, Mechanism of Action, How Long Does it Take to Work? Brexpiprazole is a brand name. Its generic name is Brexpiprazole.
Introduction
Brexpiprazole is an atypical antipsychotic drug used to treat certain mental conditions such as schizophrenia, acute treatment of bipolar disorder, and major depressive disorder. It is an active component of the brand name Rexulti. The drug is known to have effects similar to that of risperidone and aripiprazole, but with a wide range of effects.
Uses for
Brexpiprazole is used to treat mental or mood disorders such as schizophrenia, bipolar disorder, and major depressive disorder. It is also used to treat irritability associated with autistic disorder in children and adolescents aged 6–17 years. It is used in combination with an antidepressant for the treatment of major depressive disorder. It can also be used to treat symptoms of bipolar disorder such as agitation, aggression, and change in mood.
Mechanism of Action
Brexpiprazole is believed to exert its action in the central nervous system by acting as a dopamine partial agonist and a serotonin partial agonist. It binds to D2 and 5-HT1A receptors in the brain and modulates their activity. This action affects the dopamine and serotonin receptor availability and modulates their activity in the brain and is believed to be the mechanism of action of the drug.
How long does it take to work?
The effects of Brexpiprazole on symptoms may occur as early as the first week of treatment but usually take 4–6 weeks to be fully realized. The effects may take longer to fully manifest in elderly patients.
Absorption
Brexpiprazole is rapidly and completely absorbed from the gastrointestinal tract following oral administration. Peak plasma concentrations of the drug are reached in 1–2 hours.
Route of elimination
Brexpiprazole is extensively metabolized in the liver to less active metabolites which are then eliminated mainly via the kidney. Urinary excretion is the major route of elimination of the drug and its metabolites.
Dosage
Brexpiprazole is available in tablet form and should be taken orally with or without food. The recommended dose of the drug is:
- For schizophrenia, the recommended dose is 2-4 mg once daily or 1-2 mg twice daily.
- For treating acute manic or mixed episodes associated with bipolar disorder, the recommended dose is 2-4 mg once daily.
- For treating major depressive disorder, the recommended dose is 2-3 mg once daily.
- For treating irritability associated with autistic disorder in children and adolescents, the recommended dose is 0.5-2.5 mg once daily.
Administration
Brexpiprazole tablets should be taken orally with or without food. The dose of the drug may be increased or decreased based on the patient's response and tolerability. Tablet should be swallowed whole and not be crushed or split.
Side Effect
Common side effects of Brexpiprazole include: drowsiness, dizziness, vision changes, weight gain, nausea, vomiting, constipation, difficulty in sleeping, lower blood pressure, fever, restlessness, anxiety, and headache. Other less common side effects are tremor, increased cholesterol levels, restlessness, difficulty in concentrating, fast or irregular heartbeats, and increased risk of suicidal thinking.
Toxicity
Brexpiprazole has low potential of toxicity in humans. In rodents, it has low acute toxicity at high doses. Overdose can cause serious side effects.
Precautions
Brexpiprazole should be used with caution in patients with a history of cardiovascular disorders or those taking drugs that are known to interfere with heart rhythm. It should be used with caution in patients with estrogen-dependent conditions like breast cancer. The drug should also be used with caution in patients with liver impairment. It is not recommended to be used in pregnancy.
Interactions
Brexpiprazole may interact with certain drugs and reduce or increase the levels of the drug in the blood or cause drug toxicity. Some of the drugs that may cause interaction are sedatives, antihistamines, drugs used for treating depression, antifungal agents, drugs used for treating hypertension, and cholesterol lowering agents. It may also interact with herbs and dietary supplements.
Disease Interaction
Brexpiprazole is contraindicated in patients with lung disease, liver disease, cardiovascular disorders, and in patients taking drugs that cause abnormal heart rhythm. The drug should not be used if the patient has a known hypersensitivity to the drug. It should also not be used in patients with dementia.
Drug Interaction
Brexpiprazole may interact with certain drugs and reduce or increase the levels of the drug in the blood or cause drug toxicity. Some of the drugs that may cause interaction are sedatives, antihistamines, drugs used for treating depression, antifungal agents, drugs used for treating hypertension, and cholesterol lowering agents.
Food Interactions
Food does not appear to affect the absorption of brexpiprazole so patients can take the drug with or without meals. However, it is important to take the drug exactly as prescribed by the doctor.
Pregnancy Use
Brexpiprazole is a FDA-classified C which suggests that the use during pregnancy is not recommended. The drug may cause fetal harm and its use should be avoided during pregnancy unless absolutely necessary.
Lactation Use
Brexpiprazole is excreted in human milk and therefore should not be used during breastfeeding. Women taking Brexpiprazole should discontinue breastfeeding while taking the drug.
Acute Overdose
Overdose of Brexpiprazole may lead to serious effects such as sedation, rapid heart rate, muscle rigidity, and/or seizures. In case of an overdose, the patient should be taken to a hospital for medical attention.
Contraindication
Brexpiprazole is contraindicated in patients with lung disease, liver disease, cardiovascular disorders, and in patients taking drugs that cause abnormal heart rhythm. The drug should not be used if the patient has a known hypersensitivity to the drug. It should also not be used in patients with dementia.
Use Direction
Brexpiprazole should be taken as directed by the doctor. The dose of the drug may be increased or decreased based on the patient's response and tolerability. Tablet should be swallowed whole and not be crushed or split.
Storage Condition
Brexpiprazole tablets should be stored at room temperature, away from moisture and heat. Keep out of reach of children.
Volume of Distribution
The volume of distribution of brexpiprazole is approximately 333-625 L, indicating that the drug is widely distributed throughout the body.
Half Life
The effective half-life of Brexpiprazole is approximately 800 minutes (13.3 hours).
Clearance
The metabolic elimination of Brexpiprazole is mainly carried out by the liver. The mean total body clearance of the drug in healthy adults is 85.5 mL/min/1.73 m2.
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