Active Substance: Aripiprazole.
Overview
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This medicine contains an important and useful components, as it consists of
Aripiprazoleis available in the market in concentration
Aripiprazole
- **Monitor for suicidal thoughts**: Patients, especially adolescents and young adults, should be closely monitored for worsening depression or suicidal thoughts during the initial treatment or dose adjustments. - **Elderly patients with dementia-related psychosis**: Aripiprazole is not approved for the treatment of dementia-related psychosis and may increase the risk of death in elderly patients with this condition. - **Extrapyramidal symptoms**: May cause movement disorders, such as tremors, stiffness, or restlessness. These symptoms may occur, especially during the initiation phase. Monitor patients for signs of tardive dyskinesia (involuntary movements) and Parkinsonism. - **Metabolic changes**: Aripiprazole may cause weight gain, changes in lipid levels, and increased blood glucose. Monitor for signs of hyperglycemia, especially in patients with a history of diabetes. - **Orthostatic hypotension**: Aripiprazole may cause a drop in blood pressure, particularly after the first dose, leading to dizziness, fainting, or falls. This is more common in elderly individuals or patients taking other medications that affect blood pressure. - **Caution in patients with a history of seizures**: Aripiprazole may lower the seizure threshold. Use with caution in patients with a history of epilepsy or other conditions that predispose them to seizures. - **Discontinuation syndrome**: Abruptly stopping aripiprazole can lead to withdrawal symptoms such as insomnia, nausea, headache, and dizziness. Taper the dosage gradually when discontinuing treatment. - **Pregnancy and breastfeeding**: Use during pregnancy only if clearly needed and under a healthcare provider's supervision, as the effects on the fetus are not fully established. Caution should also be exercised when breastfeeding. - **Monitor liver function**: Aripiprazole should be used cautiously in patients with liver impairment, as the drug is metabolized in the liver, and impaired liver function may lead to drug accumulation and toxicity.
- **Schizophrenia**: Aripiprazole is primarily indicated for the treatment of schizophrenia in adults and adolescents aged 13 years and older. It helps manage symptoms such as delusions, hallucinations, and disorganized thinking. - **Bipolar disorder**: It is used as a mood stabilizer for the treatment of manic and mixed episodes of bipolar I disorder, either alone or in combination with other mood stabilizers. - **Major depressive disorder (MDD)**: Aripiprazole is indicated as an adjunctive treatment for major depressive disorder in adults who have not responded adequately to antidepressant therapy. - **Tourette's syndrome**: It is also used for the treatment of Tourette’s syndrome in pediatric patients (ages 6-18) who have moderate to severe symptoms. - **Irritability associated with autistic disorder**: Aripiprazole is prescribed to treat irritability and aggression associated with autism spectrum disorders in children aged 6 years and older. - **Other off-label uses**: Occasionally used off-label for conditions like anxiety disorders or treatment-resistant depression, but such uses should be discussed with a healthcare provider.
- **Hypersensitivity**: Aripiprazole is contraindicated in patients who have a known hypersensitivity to aripiprazole or any of its components. - **Severe liver impairment**: Contraindicated in patients with severe hepatic impairment, as aripiprazole is metabolized by the liver, and impaired liver function can increase the risk of drug toxicity. - **Narrow-angle glaucoma**: Caution is recommended in patients with narrow-angle glaucoma as aripiprazole can potentially increase intraocular pressure. - **Severe CNS depression**: Contraindicated in patients with severe central nervous system depression, as the sedative effects of aripiprazole could exacerbate these conditions. - **Concurrent use with strong CYP3A4 and CYP2D6 inhibitors**: In patients taking potent inhibitors of CYP3A4 and CYP2D6, such as ketoconazole or fluoxetine, dose adjustments may be necessary. However, caution should still be taken in co-administration due to the increased risk of adverse effects.
- **Extrapyramidal symptoms**: Includes symptoms like tremors, stiffness, akathisia (restlessness), and tardive dyskinesia (involuntary movements), which may occur, especially with long-term use. - **Weight gain**: Aripiprazole may cause modest weight gain, although it is generally less likely to lead to significant weight changes compared to other atypical antipsychotics. - **Metabolic disturbances**: Can lead to changes in blood glucose levels, lipid levels (increased cholesterol, triglycerides), and weight gain. Regular monitoring of metabolic parameters is recommended. - **Sedation**: Some patients may experience sedation or drowsiness, particularly when starting treatment or increasing the dose. - **Orthostatic hypotension**: A drop in blood pressure upon standing, causing dizziness, lightheadedness, or fainting, especially during initial treatment or dose adjustments. - **Akathisia**: Restlessness, inner tension, and an inability to sit still. - **Increased prolactin levels**: Although aripiprazole is considered to have a lower risk of prolactin elevation compared to other antipsychotics, it may still occur in some patients, leading to symptoms like galactorrhea or sexual dysfunction. - **Seizures**: Aripiprazole may lower the seizure threshold, leading to an increased risk of seizures, especially in patients with a history of epilepsy or those using other medications that lower the threshold.
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- **Aripiprazole** is a partial agonist at both dopamine D2 and serotonin 5-HT1A receptors and an antagonist at serotonin 5-HT2A receptors. This dual action helps balance dopamine and serotonin activity in the brain, which is thought to contribute to its antipsychotic effects. - **Dopamine modulation**: By partially activating dopamine receptors, aripiprazole stabilizes dopamine activity, reducing symptoms of psychosis (e.g., hallucinations, delusions) without causing the motor side effects typically seen with full dopamine antagonists. - **Serotonin modulation**: The antagonism of serotonin 5-HT2A receptors helps reduce anxiety and improve mood, contributing to the treatment of depression and bipolar disorder. - Aripiprazole’s unique mechanism makes it an effective treatment for various psychiatric disorders, offering a favorable side effect profile compared to other antipsychotic medications.
- **CYP450 inducers/inhibitors**: Aripiprazole is metabolized by the CYP3A4 and CYP2D6 enzymes. Drugs that inhibit these enzymes (e.g., fluoxetine, paroxetine, ketoconazole) may increase aripiprazole levels, while inducers (e.g., carbamazepine, rifampin) may reduce its levels, potentially reducing its therapeutic effects. - **Antihypertensive agents**: Aripiprazole can enhance the blood pressure-lowering effects of antihypertensive medications, leading to an increased risk of hypotension. - **CNS depressants**: Combining aripiprazole with other central nervous system depressants, such as benzodiazepines, alcohol, or other sedatives, can increase the risk of sedation, respiratory depression, and cognitive impairment. - **Dopamine agonists**: Concurrent use with dopamine agonists, such as levodopa or pramipexole, may decrease the efficacy of aripiprazole in treating psychotic symptoms and increase the risk of movement disorders. - **Antidepressants**: When used with selective serotonin reuptake inhibitors (SSRIs) or serotonin-norepinephrine reuptake inhibitors (SNRIs), there is an increased risk of serotonin syndrome, a potentially life-threatening condition. - **Other antipsychotics**: Caution is needed when using aripiprazole with other antipsychotic medications as it may enhance the risk of extrapyramidal symptoms (movement disorders) and other side effects.
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- **Schizophrenia**: The usual starting dose is 10-15 mg/day, which may be increased based on clinical response, with a typical maintenance dose ranging from 10 mg to 30 mg/day. - **Bipolar I Disorder (manic or mixed episodes)**: The recommended starting dose is 15 mg/day, with the maintenance dose typically ranging from 15 mg to 30 mg/day. - **Major depressive disorder**: For adjunctive treatment of MDD, the usual starting dose is 2-5 mg/day, with a maintenance dose of 5-15 mg/day, depending on response. - **Tourette's Syndrome**: The recommended starting dose is 2 mg/day, with gradual increases based on clinical response and tolerance, up to 10 mg/day. - **Irritability in Autism**: The recommended dose is typically between 2 mg and 15 mg/day, depending on the severity of symptoms.
- **Schizophrenia (children 13-17 years)**: The recommended dose for adolescents is typically 10 mg/day, which may be adjusted based on response, with a target dose between 10 mg to 30 mg/day. - **Bipolar I Disorder (manic or mixed episodes, children 10-17 years)**: The usual starting dose is 10 mg/day, with dose adjustments made based on clinical response. - **Tourette's Syndrome (children 6-18 years)**: The starting dose is generally 2 mg/day, with a maximum recommended dose of 10 mg/day, depending on the patient's response and tolerance. - **Irritability associated with Autism (children 6-17 years)**: The starting dose is typically 2 mg/day, with the dose adjusted based on clinical response, with a maximum dose of 15 mg/day.
- **Renal impairment**: Aripiprazole requires no dose adjustment in patients with mild to moderate renal impairment. However, caution is advised in patients with severe renal impairment (e.g., creatinine clearance less than 30 mL/min). In such cases, dose adjustments and closer monitoring may be required. - **Dialysis patients**: Although the pharmacokinetics of aripiprazole in dialysis patients have not been well-studied, since the drug is extensively metabolized by the liver, dialysis is unlikely to significantly affect aripiprazole levels.
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