Risperidone: Difference between revisions

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[[File:Risperidone orodispersible 2mg.mp3]]
[[File:Risperidone orodispersible 2mg.mp3]]


==Common Strengths of Brexpiprazole Tablet==
==Common Strengths of Risperidone Tablet==
Brexpiprazole tablets are available in the following strengths:
Brexpiprazole tablets are available in the following strengths:
*0.25 mg, 0.5 mg, 1 mg, 2 mg, 3 mg, 4 mg tablets; 1 mg/mL oral solution
*0.25 mg, 0.5 mg, 1 mg, 2 mg, 3 mg, 4 mg tablets; 1 mg/mL oral solution
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==Drug Usage==
==Drug Usage==
Brexpiprazole is used for:
Risperidone is used for:
* Treatment of schizophrenia
* Treatment of schizophrenia
* Adjunctive treatment of major depressive disorder (MDD)
* Acute treatment of manic or mixed episodes associated with bipolar disorder
* Treatment of agitation associated with dementia due to Alzheimer's disease
* Treatment of irritability associated with autistic disorder


==Mechanism of Action==
==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
Risperidone is a selective monoaminergic antagonist with high affinity for serotonin 5-HT2 and dopamine D2 receptors
 
serotonergic activity to improve symptoms of schizophrenia and depression


==Route of Administration==
==Route of Administration==
Brexpiprazole is administered orally in the form of tablets or liquid solution.
* Oral (tablets and oral solution)
* Intramuscular injection (long-acting injectable form)


==Dosages==
==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.
* Schizophrenia (adults): Initial dose 2 mg/day, target dose 4 to 8 mg/day
 
* Bipolar mania (adults): Initial dose 2 to 3 mg/day, target dose 1 to 6 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.  
For moderate to severe renal impairment (eGFR < 60 mL/min/1.73 m2):
* The maximum recommended dosage for schizophrenia is 3 mg per day.
* The maximum recommended dosage for major depressive disorder is 2 mg per day.


No adjustment is needed for mild renal impairment.
For patients with severe renal impairment (CrCl < 30 mL/min):
* Initial dose: 0.5 mg twice daily
* Titrate in increments of up to 0.5 mg twice daily
* Increases above 1.5 mg twice daily should occur at intervals of at least one week


==Side Effects==
==Side Effects==
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!Adverse reactions
!Adverse reactions
|-
|-
| rowspan="12" | '''Common
| rowspan="13" | '''Common
| Weight gain
| Drowsiness
|-
|-
| Akathisia (feeling of restlessness, constant urge to move)
| Dizziness:  which can increase the risk of falling
|-
|-
| Headache
| Weight Gain: Increased appetite leading to weight gain
|-
|-
| Drowsiness/sleepiness
| Nausea: Feeling sick to the stomach
|-
|-
| Dizziness
| Constipation
|-
|-
| Nausea
| Nausea
|-
|-
| Constipation
| Constipation
|-
| Dry Mouth: Reduced saliva production
|-
|-
| Indigestion/heartburn
| Increased Saliva: Excessive saliva production
|-
|-
| Increased appetite
| Anxiety: Feelings of nervousness or worry
|-
|-
| Fatigue/tiredness
| Agitation: Restlessness or irritability
|-
|-
| Tremor
| Difficulty Sleeping: Trouble falling or staying asleep
|-
|-
| Stuffy or runny nose
| Blurred Vision: Changes in vision clarity
|-
|-
| rowspan="13" | '''Uncommon
| Runny or Stuffy Nose: Cold-like symptoms
| Neuroleptic malignant syndrome (high fever, muscle stiffness, confusion)
|-
|-
| Tardive dyskinesia (uncontrolled muscle movements)
| Fatigue: General feeling of tiredness
|-
|-
| High blood sugar/diabetes
| rowspan="12" | '''Uncommon
| Neuroleptic Malignant Syndrome (NMS): Symptoms include high fever, muscle stiffness, and altered mental status
|-
|-
| Orthostatic hypotension (dizziness when standing up)
| Tardive Dyskinesia**: Involuntary, repetitive movements, particularly of the face and limbs, which may be irreversible
|-
|-
| Seizures
| Metabolic Changes: Increased blood sugar, cholesterol and triglycerides, and weight gain, which can lead to diabetes
|-
|-
| Low white blood cell count
| Cognitive Impairment: Difficulty thinking or concentrating
|-
|-
| Difficulty swallowing
| Heat Intolerance: Difficulty regulating body temperature, leading to overheating or hypothermia
|-
|-
| Suicidal thoughts or behaviors (especially in young adults)
| Increased Risk of Falls: Particularly in elderly patients due to dizziness and drowsiness
|-
|-
| Compulsive behaviors (gambling, sexual urges, binge eating)
| Orthostatic Hypotension: Sudden drop in blood pressure upon standing, leading to dizziness or fainting
|-
|-
| Cognitive impairment
| Seizures: Convulsions or fits
|-
|-
| Impaired body temperature regulation
| Low White Blood Cell Count: Increased risk of infections
|-
|-
| Stroke in elderly patients with dementia-related psychosis
| Allergic Reactions: Symptoms include rash, itching, and trouble breathing
|-
|-
| Allergic reactions (rash, itching, difficulty breathing)
| Stroke: Increased risk in elderly patients with dementia-related psychosis
|-
| Increased Prolactin Levels: This can lead to breast milk production, menstrual irregularities, and sexual dysfunction
|}
|}


==Pharmacokinetics==
==Pharmacokinetics==
*Absorption
*Absorption
**Peak plasma concentration within 4 hours.
**Peak plasma concentrations occurring within 1 to 2 hours
*Metabolism
*Metabolism
**Primarily metabolized by CYP3A4 and CYP2D6.
**Extensively metabolized in the liver by CYP2D6
*Excretion
*Elimination
**25% in urine and 46% in feces. Terminal elimination half-life is approximately 91 hours.
**Approximately 70% excreted in urine and 14% in feces. The half-life of the active moiety (risperidone plus 9-hydroxyrisperidone) is approximately 20 hours.


Initial effects: Some patients may begin to see improvements within 1 to 2 weeks of starting treatment.
Drug onset time and duration: Onset of action may be seen within 1 to 2 weeks, with full effects typically observed within 4-6 weeks.
 
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
 
dementia due to Alzheimer's disease, significant results may be seen in about 12 weeks.


==Drug Precautions==
==Drug Precautions==
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*May cause drowsiness, dizziness, and difficulty swallowing in elderly patients, increasing the risk of falls and choking
*May cause drowsiness, dizziness, and difficulty swallowing in elderly patients, increasing the risk of falls and choking


'''Suicidal thoughts in young people
''' Pregnancy
 
*May increase the risk of suicidal thoughts in young people under 24 years old, especially in the first few months of treatment or with dose changes
*Close monitoring is required for children/teens taking aripiprazole


'''Use cautiously in patients with a history of seizures or with conditions that lower the seizure threshold.
*Use with caution; potential risks to the fetus should be considered


'''Dysphagia
''' Breastfeeding


*Esophageal dysmotility and aspiration associated with antipsychotic drug use
*Not recommended; risperidone is excreted in human milk
*Use cautiously in patients at risk for aspiration pneumonia


'''Monitoring Requirements
'''Monitoring Requirements
*Regular monitoring of blood sugar levels, weight, and signs of extrapyramidal symptoms
*Weight, blood glucose, lipid profile, prolactin levels, signs of extrapyramidal symptoms
*Perform complete blood count (CBC) in patients with pre-existing low white blood cell count (WBC) or history of drug-induced leukopenia/neutropenia
*Monitor heart rate and blood pressure and warn patients with known cardiovascular or cerebrovascular disease, and risk of dehydration or syncope


'''Drug Interactions
'''Drug Interactions


*Avoid strong CYP3A4 inducers and inhibitors
*May enhance the effects of other CNS depressants; caution with drugs that prolong QT interval as risperidone may cause QT prolongation


==FAQ==
==FAQ==
'''How Should I Take the Tablet?
'''How Should I Take the Tablet?
* Take brexpiprazole once daily with or without food, at the same time each day.  
* Take risperidone exactly as prescribed by your doctor, usually once or twice daily with or without food.  


''What should I avoid while taking brexpiprazole?
''What should I avoid while taking?
*Avoid alcohol, and activities requiring alertness until you know how the medication affects you. Avoid overheating and dehydration
* Avoid alcohol and activities requiring mental alertness until you know how risperidone affects you.


'''What Happens if I Miss a Dose?
'''What Happens if I Miss a Dose?
*Take the missed dose as soon as you remember unless it is almost time for your next dose. Do not double doses.
* Take the missed dose as soon as you remember unless it is almost time for your next dose. Do not double doses

Revision as of 05:23, 8 July 2024


Antipsychotic Drug

Drug class: Atypical antipsychotic

Risperidone (RISPERDAL)(中文:利培酮

Pronunciation

Risperidone 1mg

Risperidone 2mg

Risperidone orodispersible 1mg

Risperidone orodispersible 2mg

Common Strengths of Risperidone Tablet

Brexpiprazole tablets are available in the following strengths:

  • 0.25 mg, 0.5 mg, 1 mg, 2 mg, 3 mg, 4 mg tablets; 1 mg/mL oral solution

Drug Trade Names of Risperidone Tablet

Risperdal, Risperdal Consta (long-acting injectable form)

Drug Usage

Risperidone is used for:

  • Treatment of schizophrenia
  • Acute treatment of manic or mixed episodes associated with bipolar disorder
  • Treatment of irritability associated with autistic disorder

Mechanism of Action

Risperidone is a selective monoaminergic antagonist with high affinity for serotonin 5-HT2 and dopamine D2 receptors

Route of Administration

  • Oral (tablets and oral solution)
  • Intramuscular injection (long-acting injectable form)

Dosages

  • Schizophrenia (adults): Initial dose 2 mg/day, target dose 4 to 8 mg/day
  • Bipolar mania (adults): Initial dose 2 to 3 mg/day, target dose 1 to 6 mg/day

For moderate to severe renal impairment (eGFR < 60 mL/min/1.73 m2):

  • The maximum recommended dosage for schizophrenia is 3 mg per day.
  • The maximum recommended dosage for major depressive disorder is 2 mg per day.

For patients with severe renal impairment (CrCl < 30 mL/min):

  • Initial dose: 0.5 mg twice daily
  • Titrate in increments of up to 0.5 mg twice daily
  • Increases above 1.5 mg twice daily should occur at intervals of at least one week

Side Effects

Frequency Adverse reactions
Common Drowsiness
Dizziness: which can increase the risk of falling
Weight Gain: Increased appetite leading to weight gain
Nausea: Feeling sick to the stomach
Constipation
Nausea
Constipation
Dry Mouth: Reduced saliva production
Increased Saliva: Excessive saliva production
Anxiety: Feelings of nervousness or worry
Agitation: Restlessness or irritability
Difficulty Sleeping: Trouble falling or staying asleep
Blurred Vision: Changes in vision clarity
Runny or Stuffy Nose: Cold-like symptoms
Fatigue: General feeling of tiredness
Uncommon Neuroleptic Malignant Syndrome (NMS): Symptoms include high fever, muscle stiffness, and altered mental status
Tardive Dyskinesia**: Involuntary, repetitive movements, particularly of the face and limbs, which may be irreversible
Metabolic Changes: Increased blood sugar, cholesterol and triglycerides, and weight gain, which can lead to diabetes
Cognitive Impairment: Difficulty thinking or concentrating
Heat Intolerance: Difficulty regulating body temperature, leading to overheating or hypothermia
Increased Risk of Falls: Particularly in elderly patients due to dizziness and drowsiness
Orthostatic Hypotension: Sudden drop in blood pressure upon standing, leading to dizziness or fainting
Seizures: Convulsions or fits
Low White Blood Cell Count: Increased risk of infections
Allergic Reactions: Symptoms include rash, itching, and trouble breathing
Stroke: Increased risk in elderly patients with dementia-related psychosis
Increased Prolactin Levels: This can lead to breast milk production, menstrual irregularities, and sexual dysfunction

Pharmacokinetics

  • Absorption
    • Peak plasma concentrations occurring within 1 to 2 hours
  • Metabolism
    • Extensively metabolized in the liver by CYP2D6
  • Elimination
    • Approximately 70% excreted in urine and 14% in feces. The half-life of the active moiety (risperidone plus 9-hydroxyrisperidone) is approximately 20 hours.

Drug onset time and duration: Onset of action may be seen within 1 to 2 weeks, with full effects typically observed within 4-6 weeks.

Drug Precautions

Increased risk in elderly patients

  • Should not be used to treat dementia-related psychosis in older adults due to increased risk of stroke and death
  • May cause drowsiness, dizziness, and difficulty swallowing in elderly patients, increasing the risk of falls and choking

Pregnancy

  • Use with caution; potential risks to the fetus should be considered

Breastfeeding

  • Not recommended; risperidone is excreted in human milk

Monitoring Requirements

  • Weight, blood glucose, lipid profile, prolactin levels, signs of extrapyramidal symptoms

Drug Interactions

  • May enhance the effects of other CNS depressants; caution with drugs that prolong QT interval as risperidone may cause QT prolongation

FAQ

How Should I Take the Tablet?

  • Take risperidone exactly as prescribed by your doctor, usually once or twice daily with or without food.

What should I avoid while taking?

  • Avoid alcohol and activities requiring mental alertness until you know how risperidone affects you.

What Happens if I Miss a Dose?

  • Take the missed dose as soon as you remember unless it is almost time for your next dose. Do not double doses