Risperidone (Risperdal) is an atypical antipsychotic medicine that is used to treat schizophrenia, aggression, bipolar disorder, and behavioral problems associated with autism.

Risperidone (Risperdal) Uses:

• Injection:

  • Bipolar disorder (IM injection only):

    • Used alone or as additional therapy to lithium or valproate for maintenance treatment of bipolar I disorder

  • Schizophrenia:

    • Treatment of schizophrenia

• Oral:

  • Bipolar mania:

    • Monotherapy: For treating acute manic or mixed episodes associated with bipolar I disorder in adults, children, and adolescents 10 to 17 years of age
    • Adjunctive therapy: As add on therapy with lithium or valproate for the treatment of acute manic or mixed episodes associated with bipolar I disorder in adults

  • Irritability associated with autistic disorder:

    • For the treatment of irritability due to autistic disorder in children and adolescents 5 to 17 years of age, including symptoms of aggressive behavior, deliberate self-harm, temper tantrums, and mood swings.

  • Schizophrenia:

    • For treatment of schizophrenia in adults and adolescents of 13 to 17 years in age.

  • Off Label Use of Risperidone in Adults:

    • Delusional infestation (also called delusional parasitosis);
    • Major depressive disorder;
    • Posttraumatic stress disorder;
    • Psychosis/agitation associated with dementia;
    • Tourette syndrome

Risperidone (Risperdal) Dose in Adults

Note:    in case of restarting medication after stopping follow initial titration schedule. Limit starting oral dose to 2 mg daily (in 1 or 2 divided doses) to reduce risk of orthostatic hypotension.

Risperidone (Risperdal) Dose in the treatment of Bipolar mania (monotherapy or as an adjunct to lithium or Divalproex):

• Oral: Initial: 2 to 3 mg once daily;
• if needed, adjust dose by 1 mg daily in intervals ≥24 hours; dosing range: 1 to 6 mg daily.
• Maintenance:
  • No dosing recommendation available for treatment duration more than 3 weeks.

Risperidone (Risperdal) Dose in the maintenance treatment of Bipolar disorder (monotherapy or as an adjunct to lithium or divalproex):

• IM: 25 mg every 15 days;
• if unresponsive, some may require increased doses (37.5 to 50 mg);
• maximum dose: 50 mg every 2 weeks.
• Do not adjust doses more frequently than every 4 weeks.
• A lower initial dose of 12.5 mg may be appropriate in some patients (eg, hepatic or renal impairment, poor tolerability to other psychotropic medications).

Note: Establish tolerance to oral risperidone before initiating IM injections. Overlap oral risperidone (or other antipsychotic) with the initial injection of the intramuscular injection, and continued for 3 weeks (then discontinued) to maintain adequate therapeutic plasma concentrations prior to main release phase of risperidone from injection site.

Risperidone (Risperdal) Dose in the treatment of Delusional infestation (also called delusional parasitosis) (off-label):

• Oral: Initial: 0.5 mg before sleep; up titrate gradually based on response and tolerance up to 1 to 2 mg given before sleep or in 2 divided doses.
• Doses up to 8 mg/day have been evaluated.

Risperidone (Risperdal) Dose in the treatment of the major depressive disorder (as adjunct to antidepressants; off-label):

• Oral: Initial: 0.25 mg to 0.5 mg daily;
• gradually adjust dose based on response and tolerability up to 3 mg/day.
• Average doses in clinical trials were 1.2 to 1.6 mg/day.

Risperidone (Risperdal) Dose in the treatment of Posttraumatic stress disorder (PTSD) (off-label):

• Oral: Initial: 0.5 to 1 mg at bedtime or 0.5 mg two times daily;
• adjust dose based on response and tolerance to a maximum of 8 mg daily;
• The total daily dose may be given in 2 or 3 divided doses.
• Average dose in clinical trials: 1.25 to 3.75 mg daily.

Risperidone (Risperdal) Dose in the treatment of Schizophrenia:

• Oral:
  • Initial: 2 mg daily in 1 to 2 divided doses;
  • The dose may be up titrated 1 to 2 mg daily at intervals ≥24 hours to a recommended dosage range of 4 to 8 mg daily.
  • Daily dosages >6 mg have no additional benefit and have higher incidence of extrapyramidal symptoms.
  • Dose range studied in clinical trials: 4 to 16 mg daily.
  • Maintenance: Recommended dosage range: 2 to 8 mg daily
• IM:
  • Initial: 25 mg every 2 weeks;
  • if unresponsive, some may benefit from larger doses (37.5 to 50 mg);
  • maximum dose: 50 mg every 2 weeks.
  • No further benefit, only increased side effects were seen with doses >50 mg.
  • Do not adjust dose more frequently than every 4 weeks. A lower initial dose of 12.5 mg may be better in some patients (eg, demonstrated poor tolerability to other psychotropic medications).
  • Note:
    • The establishment of tolerability to oral risperidone is recommended before starting intramuscular injection.
    • Oral risperidone (or other antipsychotic) should be overlapped with the first injection of the intramuscular injection and continued for 3 weeks (then discontinued) to maintain adequate therapeutic plasma concentrations before main release phase of risperidone from injection site.
• SubQ:
  • Usual dose: 90 or 120 mg once monthly.
  • No more than one 90 or 120 mg injection per month.
  • Note: Establishment of tolerability to oral risperidone is recommended before initiating SubQ injection. Neither a loading dose nor oral overlap with risperidone is required.

• Conversion between oral risperidone to SubQ risperidone:

  • Oral dose of 3 mg/day is equal to a SubQ injection of 90 mg once monthly.
  • An Oral dose of 4 mg/day is equal to a SubQ injection of 120 once monthly.

Risperidone (Risperdal) Dose in the treatment of Tourette syndrome (off-label):

• Oral: Initial: 0.25 mg once daily;
• increase slowly according to response and tolerability up to a usual dosage of 0.25 to 6 mg daily.
• Dosage adjustments in clinical trials were often in increments of <0.5 mg twice daily and at intervals ≥3 days.

• ---

  Concomitant CYP2D6 inhibitors:

  • Addition of fluoxetine or paroxetine: SubQ:

    • In patients receiving 90 mg once monthly:
      • Continue treatment with 90 mg unless clinical judgment suggests otherwise.
    • In patients receiving 120 mg once monthly:
      • Decrease dose to 90 mg once monthly 2 to 4 weeks before the planned start of fluoxetine or paroxetine.

• Concomitant CYP3A4 inducers:

  • Addition of carbamazepine or other known hepatic enzyme inducer: SubQ:

Note: Monitor closely for the first 4 to 8 weeks:

• • In patients receiving 90 mg once monthly: Consider increasing risperidone to 120 mg once monthly.
  • In patients receiving 120 mg once monthly: Consider oral risperidone supplementation.

• Discontinuation of carbamazepine or other known hepatic enzyme inducer:

  • SubQ: Consider reducing dose of risperidone SubQ injection from 120 mg to 90 mg and/or decreasing oral supplementation dose.
  • In patients taking 90 mg risperidone injection once monthly, continue dose unchanged and monitor for worsening tolerability.

• Risperidone (Risperdal) Discontinuation of therapy:

  • American Psychiatric Association (APA), Canadian Psychiatric Association (CPA), and World Federation of Societies of Biological Psychiatry (WFSBP) guidelines recommend slowly tapering antipsychotics to avoid withdrawal symptoms and reduce risk of relapse.
  • The risk for withdrawal symptoms may be highest with highly anti-cholinergic or dopaminergic antipsychotics.
  • When stopping antipsychotic therapy in patients with schizophrenia, the CPA guidelines recommend a slow taper over 6 to 24 months, and the APA guidelines recommend reducing the dose by 10% each month.
  • Continuing anti-parkinsonism agents for a small period after discontinuation may prevent withdrawal symptoms.
  • When switching antipsychotics, 3 strategies have been suggested: Cross-titration (gradually discontinuing the first antipsychotic while gradually increasing the new antipsychotic).
  • overlap and taper (maintaining the dose of the first antipsychotic while gradually increasing the new antipsychotic, then tapering the first antipsychotic).
  • Sudden change (suddenly discontinuing the first antipsychotic and either increasing the new antipsychotic gradually or starting it at a treatment dose).
  • Evidence supporting ideal switch strategies and taper rates is limited, and results are conflicting.

Risperidone (Risperdal) Dose in Children

Risperidone (Risperdal) Dose in the treatment of Autism, associated irritability, including aggression, temper, tantrums, self-injurious behavior, and quickly changing moods:

• Children ≥5 years and Adolescents: Note:

• customize dose according to patient response and tolerability:
  • 15 to 20 kg:
    • Oral: Initial: 0.25 mg/day;
    • after ≥4 days, may increase the dose to 0.5 mg/day;
    • maintain this dose for ≥14 days.
    • In patients not achieving an adequate clinical response, may increase the dose in increments of 0.25 mg/day at ≥2-week intervals.
    • Doses ranging from 0.5 to 3 mg/day have been evaluated; however, the therapeutic effect reached a plateau at 1 mg/day in clinical trials.
    • Following the clinical response, consider slowly decreasing dose to the lowest effective dose.
    • May be administered once daily or in divided doses twice daily.
  • ≥20 kg:
    • Oral: Initial: 0.5 mg/day;
    • after ≥4 days, may increase dose to 1 mg/day;
    • maintain this dose for ≥14 days.
    • In patients not achieving sufficient clinical response, may increase dose in increments of 0.5 mg/day at ≥2-week intervals.
    • Doses ranging from 0.5 to 3 mg/day have been evaluated; however, therapeutic effect reached a plateau at 2.5 mg/day (3 mg/day in pediatric patients >45 kg) in clinical trials.
    • Following the clinical response, consider gradually decreasing to the lowest effective dose. May be administered once daily or in divided doses twice daily.

Risperidone (Risperdal) Dose in the treatment of Bipolar mania:

• Children and Adolescents 10 to 17 years:

  • Oral: Initial: 0.5 mg once daily;
  • The dose may be adjusted if needed, in increments of 0.5 to 1 mg/day at intervals ≥24 hours, as tolerated, to a dose of 2.5 mg/day.
  • Doses ranging from 0.5 to 6 mg/day have been evaluated; however, doses >2.5 mg/day do not confer additional benefit and are associated with increased adverse events; doses >6 mg/day have not been studied.
  • Note: May administer / the daily dose twice daily in patients who experience persistent somnolence.

Risperidone (Risperdal) Dose in the treatment of Delirium: 

• Children <5 years:

  • Oral: Initial: 0.1 to 0.2 mg once daily at bedtime;
  • dosing based on retrospective review of 10 pediatric patients (ages: 4 months to 16 years) which included three patients <5 years of age.

• Children ≥5 years and Adolescents:

  • Oral: Initial: 0.2 to 0.5 mg once daily at bedtime;
  • may titrate to lowest effective dose every 1 to 2 days;
  • usual range: 0.2 to 2.5 mg/day in divided doses 2 to 4 times daily;
  • maximum daily dose dependent upon patient weight:
    • <20 kg: 1 mg/day;
    • 20 to 45 kg: 2.5 mg/day,
    • >45 kg: 3 mg/day.

Risperidone (Risperdal) Dose in the treatment of Disruptive behavior disorders (eg, conduct disorder, oppositional defiant disorder):

• Children ≥4 years and Adolescents:

  • Oral: Initial: 0.01 mg/kg/dose once daily for 2 days, then 0.02 mg/kg/dose once daily, may further increase on weekly basis as tolerated to 0.06 mg/kg/dose once daily;
  • The usual maximum daily dose: 2 mg/day;
  • improvement in target symptoms typically within 1 to 4 weeks.
  • Note: May administer the daily dose twice daily if breakthrough symptoms occur in the afternoon or evening.

Risperidone (Risperdal) Dose in the treatment of Pervasive developmental disorders (PDD) (eg, disruptive behavior, aggression, irritability):

• Children ≥5 years and Adolescents:

  • Oral: Initial: 0.01 mg/kg/dose once daily for 2 days, then 0.02 mg/kg/dose once daily;
  • may further increase on weekly basis by ≤0.02 mg/kg/day increments as tolerated to 0.06 mg/kg/dose once daily;
  • reported mean dose: 0.05 mg/kg/day (1.48 mg/day);
  • other trials have reported similar optimal doses: 0.75 to 1.8 mg/day;
  • improvement in target symptoms typically within 2 to 4 weeks.
  • Note: May administer the daily dose twice daily if breakthrough symptoms occur in the afternoon or evening.

Risperidone (Risperdal) Dose in the treatment of Schizophrenia:

• Adolescents 13 to 17 years:

  • Oral: Initial: 0.5 mg once daily;
  • The dose may be adjusted if needed, in increments of 0.5 to 1 mg/day at intervals ≥24 hours, as tolerated, to a dose of 3 mg/day.
  • Doses ranging from 1 to 6 mg/day have been evaluated; however, doses >3 mg/day do not confer additional benefit and are associated with increased adverse events.
  • Note: May administer the daily dose twice daily in patients who experience persistent somnolence.

Risperidone (Risperdal) Dose in the treatment of Tourette syndrome, tics:

• Children ≥7 years and Adolescents:

  • Oral: Initial: 0.25 to 0.5 mg once daily at night;
  • May slowly titrate every 4 to 5 days in 0.25 to 0.5 mg increments to usual reported therapeutic range: 0.25 to 6 mg/day divided into twice-daily doses.

Risperidone (Risperdal) Discontinuation of therapy:

• Children and Adolescents:

  • American Academy of Child and Adolescent Psychiatry (AACAP), American Psychiatric Association (APA), Canadian Psychiatric Association (CPA), National Institute for Health and Care Excellence (NICE), and World Federation of Societies of Biological Psychiatry (WFSBP) guidelines recommend slowly tapering antipsychotics to avoid withdrawal symptoms and minimize the risk of relapse.
  • The risk for withdrawal symptoms may be highest with highly anticholinergic or dopaminergic antipsychotics.
  • When stopping antipsychotic therapy in patients with schizophrenia, the CPA guidelines recommend a gradual taper over 6 to 24 months and the APA guidelines recommend reducing the dose by 10% each month.
  • Continuing anti parkinsonism agents for a brief period after discontinuation may prevent withdrawal symptoms.
  • When switching antipsychotics, three strategies have been suggested:
    • Cross-titration (gradually discontinuing the first antipsychotic while slowly increasing the new antipsychotic),
    • overlap and taper (maintaining the dose of the first antipsychotic while gradually increasing the new antipsychotic, then tapering the first antipsychotic), and
    • sudden change.
  • Evidence supporting ideal switch strategies and taper rates is limited and results are conflicting.

Risperidone (Risperdal) Pregnancy Risk Category: C

• Risperidone crosses the placenta with its metabolite.
• One case report about an infant who was exposed to risperidone during pregnancy has reported agenesis of the corpus Callosum. The relationship to risperidone is not known.
• There is a possibility of withdrawal symptoms and extrapyramidal symptoms in the third trimester if antipsychotics are used during pregnancy.
• The newborn can experience agitation, feeding disorders, hypotonia and respiratory distress as well as somnolence and tremor.
• These effects can be self-limiting, allowing recovery in hours or days with no treatment or severe enough to require prolonged hospitalization.
• Patients should inform their health care providers if they become pregnant or plan to become pregnant while receiving the IM injection.
• ACOG recommends that treatment during pregnancy is individualized; treatment with psychiatric medication during pregnancy should include the clinical expertise of the mental healthcare clinician, primary care provider, and pediatrician.
• There are limited safety data regarding atypical antipsychotics during pregnancy.
• Routine use is therefore not recommended.
• If a woman is accidentally exposed to an antipsychotic atypical while pregnant, it may be preferable to continue therapy than switching to the agent. Consider risk: benefits
• It is preferable to use a different agent than risperidone if treatment is required for a woman who is pregnant or if the treatment is started during pregnancy.
• Risperidone can cause hyperprolactinemia in women, which could lead to a reversible decline in reproductive function.

Use of Risperidone (Risperdal), while breastfeeding

• Breast milk contains risperidone as well as its active metabolite 9-hydroxyrisperidone.
• The relative infant dose (RID), of risperidone, is 1.5%. The RID of 9-hydroxyrisperidone, on the other hand is 5.5%. This is calculated by using the highest breastmilk concentration and compared with a maternal weight-adjusted dose of 2 mg/day.
• According to the manufacturer, the RID of risperidone or the metabolite is between 2.3% and 4.7% weight-adjusted maternal dose.
• It is generally acceptable to breastfeed if the RID of the medication is less than 10% (Anderson 2016; Ito2000).
• Some sources mention that breastfeeding should be considered only if the RID for psychotropic drugs is less than 5% (Larsen 2015).
• The RID of Risperidone was calculated using a concentration of milk of 3 ng/mL. This gives an estimated daily infant dose of 0.45 mg/kg/day.
• The RID of 9hydroxyrisperidone was calculated with a milk concentration 11 ng/mL. This gives an estimated daily infant dose via breastmilk of 1.65 mg/kg/day.
• These milk concentrations were determined following the maternal administration of oral Risperidone 2 mg/day. Samples were taken 3 hours after the 6 day treatment. Treatment began 1 week after birth.
• Peak milk concentrations are seen within 2 to 4 hours of an oral maternal dose.
• For the first month after being exposed via breastmilk to second-generation antipsychotics, infants should be closely monitored for signs such as lethargy, appetite changes, insomnia or irritability.
• According to the manufacturer breastfeeding during therapy is a decision that should be made after considering the risks to infants, the benefits to the infant and the benefits to the mother.
• According to available information, it is preferable to use other agents than risperidone for breastfeeding women.

Risperidone (Risperdal) Dose in Kidney Disease:

Oral:

• The risk of orthostatic hypotension/syncope may be reduced by limiting the initial dose to 1mg daily in 2 divided doses.
• Clearance can be reduced by up to 60% for patients suffering from moderate or severe renal disease (CrCl 60mL/minute).
• Mild to moderate impairment (CrCl >=30mL/minute).
  • The manufacturer does not allow for dosage adjustments.
  • Reduce the dosage.
• Severe impairment (CrCl >30 mL/minute).
  • Initial: 0.5 mg twice daily
  • Slowly titrate in small increments, no more than 0.5 mg daily
  • Increases in dosages above 1.5 mg twice daily should be made at intervals of more than one week.

IM:

• Start oral dosing with 0.5 mg twice daily for one week, then 1 mg twice daily for the next week, or 2 mg once daily during the first week.
• If tolerated, start 25 mg IM every two weeks
• Continue oral dosing for three weeks following the second IM injection.
• A 12.5 mg initial IM dose may be considered.

SubQ

• Be careful.
• Begin with oral dosing (titrate to 3 mg/day).
• If tolerated and effective, 90 mg can be started once a month.

Risperidone (Risperdal) Dose in Liver disease:

Oral:Notice:

• The risk of orthostatic hypotension/syncope may be reduced by limiting initial doses to 1mg daily in 2 divided doses.
• Patients with severe hepatic impairment may have a 35% increase in the plasma mean free fraction of risperidone.
• Mild to moderate impairment (Child Puugh class A orB):
  • The manufacturer's labeling does not include any dosage adjustments. Reduce dosage.
• Severe impairment (Child Puugh class C).
  • Initial: 0.5 mg twice daily
  • Titration should be gradual and in increments of 0.5 mg daily
  • Increases in dosages above 1.5 mg twice daily should be made at intervals of more than one week.

IM:

• Start with oral dosing (0.5mg twice daily for one week, then 1mg twice daily or 2mg once daily for one week);
• If tolerated, start 25 mg IM every fifteen days
• Continue oral dosing for three weeks following the second IM injection.
• A 12.5 mg initial IM dose may be considered.

SubQ

• Be careful.
• Begin with oral dosing (titrate to 3 mg/day).
• If tolerated and effective, 90 mg can be started once a month.

Common Side Effects of Risperidone (Risperdal):

• Central Nervous System:

  • Sedation
  • Drowsiness
  • Drug-Induced Extrapyramidal Reaction
  • Insomnia
  • Fatigue
  • Parkinsonian-Like Syndrome
  • Headache
  • Anxiety
  • Dizziness
  • Drooling
  • Akathisia

• Endocrine & Metabolic:

  • Hyperprolactinemia
  • Weight Gain

• Gastrointestinal:

  • Increased Appetite
  • Vomiting
  • Constipation
  • Upper Abdominal Pain
  • Nausea

• Genitourinary:

  • Urinary Incontinence

• Neuromuscular & Skeletal:

  • Tremor

• Respiratory:

  • Nasopharyngitis
  • Cough
  • Rhinorrhea

• Miscellaneous:

  • Fever

Less Common Side Effects of Risperidone (Risperdal):

• Cardiovascular:

  • Bradycardia
  • Bundle Branch Block
  • Chest Discomfort
  • Chest Pain
  • ECG Changes
  • Facial Edema
  • First-Degree Atrioventricular Block
  • Hypotension
  • Orthostatic Hypotension
  • Palpitations
  • Prolonged Q-T Interval On ECG
  • Tachycardia
  • Hypertension
  • Peripheral Edema
  • Syncope

• Central Nervous System:

  • Dystonia
  • Abnormal Gait
  • Procedural Pain
  • Pain
  • Disturbance In Attention
  • Agitation
  • Ataxia
  • Depression
  • Dysarthria
  • Falling
  • Lethargy
  • Malaise
  • Nervousness
  • Orthostatic Dizziness
  • Paresthesia
  • Seizure
  • Sleep Disturbance
  • Tardive Dyskinesia
  • Vertigo
  • Hypoesthesia

• Dermatologic:

  • Skin Rash
  • Eczema
  • Pruritus
  • Xeroderma
  • Acne Vulgaris

• Endocrine & Metabolic:

  • Decrease In HDL Cholesterol
  • Increased Thirst
  • Increased Serum Cholesterol
  • Amenorrhea
  • Weight Loss
  • Decreased Libido
  • Delayed Ejaculation
  • Galactorrhea Not Associated With Childbirth
  • Glycosuria
  • Gynecomastia
  • Hyperglycemia
  • Increased Gamma-Glutamyl Transferase
  • Infrequent Uterine Bleeding
  • Menstrual Disease
  • Increased Serum Triglycerides

• Gastrointestinal:

  • Xerostomia
  • Dyspepsia
  • Sialorrhea
  • Diarrhea
  • Decreased Appetite
  • Stomach Discomfort
  • Abdominal Pain
  • Anorexia
  • Gastritis
  • Gastroenteritis
  • Abdominal Distress
  • Toothache

• Genitourinary:

  • Menstruation
  • Cystitis
  • Erectile Dysfunction
  • Irregular Menses
  • Mastalgia
  • Sexual Disorder
  • Urinary Tract Infection

• Hematologic & Oncologic:

  • Anemia
  • Neutropenia

• Hepatic:

  • Increased Liver Enzymes
  • Increased Serum Alanine Aminotransferase
  • Increased Serum Aspartate Aminotransferase

• Hypersensitivity:

  • Hypersensitivity Reaction

• Infection:

  • Abscess At Injection Site
  • Infection
  • Influenza
  • Localized Infection
  • Viral Infection

• Local:

  • Induration At Injection Site
  • Injection Site Reaction
  • Local Pain
  • Pain At Injection Site
  • Swelling At Injection Site

• Neuromuscular & Skeletal:

  • Limb Pain
  • Back Pain
  • Dyskinesia
  • Musculoskeletal Pain
  • Arthralgia
  • Abnormal Posture
  • Akinesia
  • Hypokinesia
  • Musculoskeletal Chest Pain
  • Myalgia
  • Myasthenia
  • Neck Pain
  • Muscle Spasm
  • Muscle Rigidity
  • Asthenia
  • Increased Creatine Phosphokinase

• Ophthalmic:

  • Blurred Vision
  • Conjunctivitis
  • Decreased Visual Acuity

• Otic:

  • Otalgia
  • Otic Infection

• Respiratory:

  • Nasal Congestion
  • Pharyngolaryngeal Pain
  • Rhinitis
  • Respiratory Tract Infection
  • Bronchitis
  • Dyspnea
  • Flu-Like Symptoms
  • Pharyngitis
  • Pneumonia
  • Sinusitis
  • Epistaxis
  • Paranasal Sinus Congestion

Contraindications to Risperidone (Risperdal):

Allergy to paliperidone, risperidone or any other component of the formulation

Warnings and precautions

• Modified cardiac conduction

  • QT prolongation may occur; life-threatening arrhythmias can be caused by therapeutic doses antipsychotics.
  • Concomitant medications can increase your risk of hypokalemia, bradycardia and/or bradycardia.
  • Patients with conduction abnormalities should be cautious.
  • Risperidone is less likely to cause arrhythmias than other neuroleptics.

• Anticholinergic effects

  • Anticholinergic effects may occur (confusion, agitation and constipation; blurred vision, urinary retention; xerostomia, xerostomia, xerostomia, and xerostomia).
  • Patients with decreased gastrointestinal motility, BPH, xerostomia, and/or visual impairments should be cautious.
  • Risperidone is less likely to cause a cholinergic blockade than other neuroleptics.

• Anti-emetic effects

  • Antiemetic effects may cause toxicities of other drugs and conditions to be hidden (e.g., intestinal obstruction, Reyes syndrome or brain tumor).

• Blood dyscrasias

  • Clinical trials have shown that neutropenia, leukopenia and agranulocytosis can sometimes be fatal. Antipsychotic use should also be accompanied by postmarketing reports.
  • Stop treatment at the first sign of blood dyscrasias, or if your absolute neutrophil count is 1,000/mm3.

• Effects on the cerebrovascular system:

  • In placebo-controlled trials of Risperidone's unapproved use in dementia-related psychosis patients aged over 60, there was an increase in cerebrovascular effects, including stroke, in some elderly patients.

• Depression in the CNS:

  • CNS depression can lead to impairment of mental or physical abilities. Patients should be cautious about driving, operating machinery, and other tasks that require mental alertness.
  • Low to moderate sedation may be experienced in comparison to antipsychotics. Dose-related effects have been documented.

• Dyslipidemia

  • This has been reported when taking atypical antipsychotics. The risk profile of each agent may be different.
  • Risperidone has a lower risk of metabolic side effects than other antipsychotics.

• Aspiration/Esophageal dysmotility

  • Aspiration and esophageal dysmotility have been linked to antipsychotic use.
  • Patients at high risk of aspiration pneumonia (eg Alzheimer disease) should be treated with caution, especially patients over 75 years old.

• Extrapyramidal symptoms

  • Extrapyramidal symptoms (EPS) may occur, including pseudo parkinsonism and acute dystonic reactions.
  • Higher doses of conventional antipsychotics, older age, and greater risk of dystonia (and other EPS) could increase the chance.
  • Tiltive dyskinesia is more common in older people, postmenopausal women and those with Parkinson's disease symptoms.
  • If you notice signs and symptoms of tardive dyskinesia, stop taking the therapy.

• Falls

  • Somniolence, orthostatic hypotension and motor or sensor instability increase the risk of falling.
  • Patients with comorbidities or taking medications that can increase fall risk should have their fall risk assessed at baseline and again periodically throughout treatment.

• Hyperglycemia

  • Hyperglycemia can be caused by antipsychotics that are not typical. In some cases, this may lead to hyperglycemia, hyperosmolar or even fatal complications.
  • Patients with diabetes and other disorders of glucose regulation should be cautious; you must monitor for any changes in glycemic control.
  • Risperidone has a low risk of metabolic side effects, especially hyperglycemia, compared to other antipsychotics.

• Hyperprolactinemia

  • Risperidone is associated more with higher levels of prolactin than other antipsychotic drugs. However, the clinical significance and prolactinemia in patients suffering from breast cancer or other prolactin dependent tumors is not known.
  • Patients taking risperidone are at higher risk for hyperprolactinemia if they have a female gender, a younger age when the illness begins, and higher scores on both the Positive and Negative Symptom Scales (PANSS).
  • Also, higher prolactin levels are associated with higher doses.

• Hypersensitivity

  • Angioedema and anaphylactic reactions have been reported as hypersensitivity reactions.

• Intraoperative floppy-iris syndrome:

  • Very few cases report intraoperative floppy iris (IFIS), in patients who have received risperidone or had cataract surgery.
  • Before cataract surgery, evaluate for risperidone use in the past or present.
  • It is not known whether interrupting risperidone prior to surgery has any benefits or risks. Therefore, it is important that you proceed with caution.

• Neuroleptic malignant Syndrome:

  • It may also be used in conjunction with neuroleptic malignant Syndrome (NMS).
  • Monitor for changes in mental status, fever, rigidity of the muscles, and/or signs of autonomic instability.

• Orthostatic hypotension

  • Orthostatic hypotension may occur; caution is advised for patients at high risk (eg, concurrent drug use that could predispose you to hypotension/bradycardia/presence of hypovolemia) and those who cannot tolerate transient hypotensive episodes.
  • Be cautious if you have a history of cerebrovascular disease or cardiovascular disease (MI or heart failure)

• Priapism

  • Rare cases of priapism were reported.

• Suicidal thoughts:

  • Patients at high risk should be treated with caution
  • Good patient care requires that prescriptions be limited to the minimum amount.

• Temperature regulation

  • It is possible to have impaired core body temperature regulation. Be careful with vigorous exercise, heatexposure, dehydration and coadministration of anticholinergic medications.

• Weight loss

  • Antipsychotic therapy has led to significant weight gain; incidences vary from product to product.
  • There is a moderate risk of weight gain with antipsychotics.
  • Check your waist circumference and your BMI.

• Cardiovascular disease

  • Patients with severe heart disease, hemodynamic instability, prior myocardial injury, or ischemic heart disease should be cautious.

• Dementia: [US Boxed Warning]

  • Antipsychotics have a higher death rate than placebo for dementia-related psychosis in the elderly.
  • The majority of deaths were either from cardiovascular disease (eg heart failure, sudden death) and infectious diseases (eg pneumonia).
  • Patients with Parkinson disease dementia or Lewy body dementia should be cautious about using this medication. There is a greater chance of adverse effects and increased sensitivity to extrapyramidal side effects. Also, there may be irreversible cognitive decline or death.
  • Risperidone has not been approved to treat dementia-related psychosis.
  • Before starting treatment, it is important to carefully assess your risk factors for stroke and other cardiovascular conditions.

• Hepatic impairment

  • Recommendations for adjustment:

• Renal impairment

  • Patients with impaired renal function should be cautious. You will need to adjust the dose.

• Seizures

  • Patients at high risk for seizures, patients with brain damage, history of seizures, and those who are receiving concurrent treatment with medication that may lower seizure threshold should be cautious.

Risperidone: Drug Interaction

Monitoring parameters:

• Mental state
• Vital signs (as indicated by a physician); blood pressure (baseline); repeat the process after 3 months, then every year.
• Weight, height, BMI and waist circumference (baseline); repeat at 4, 8 and 12 weeks after starting, changing or stopping therapy. Then, 3 times per month. If you gain more than 5%, consider switching to another antipsychotic.
• CBC (as indicated by the doctor; patients with pre-existing or past drug-induced leukopenia/neutropenia should be monitored frequently for the first few months.
• The serum electrolytes renal function and liver function (yearly or as clinically indicated).
• Personal and family history of cardiovascular disease, obesity, diabetes, dyslipidemia or hypertension (baseline; repeated annually);
• Fasting plasma glucose/HbA
• Fasting lipid panel (baseline); repeat 3 months after antipsychotics are started; if LDL levels are normal, repeat every 2 to 5 years or more if clinically indicated.
• Changes in menstruation, libido and development of galactorrhea (at each visit during the first 12 weeks following the antipsychotic's administration or until the dose becomes stable; thereafter, annually).
• Parkinsonian signs or abnormal involuntary movements (baseline; continue weekly until dose stabilization for at least 2 week after introduction, and 2 weeks after any significant dose rise);
• Tightening of the muscles (every 12 to 18 months; high-risk patients, every 6 months);
• Ocular examinations (yearly for patients over 40 years old; every 2 years for younger patients).

How to administer Risperidone (Risperdal)?

Oral:

• No association with food intake.
• Do not spit or chew.
• Remove tablet from foil and immediately place on tongue with dry hands, it will dissolve immediately.
• Do not push foil, peel it back.
• May be swallowed with or without water.
• Oral solution can be taken as is or mixed with juice or water, do not mix with cola or tea.

IM:

• Shake syringe vigorously.
• Administer IM into either the deltoid muscle or the upper outer quadrant of the gluteal area.
• For IM use only; do not administer IV.
• Rotate injection site between both arms and buttocks.
• Do not combine two different dosage strengths into one single administration.
• Do not substitute any components of the dose-pack; administer with the provided needle (1-inch needle for deltoid administration or 2-inch needle for gluteal administration).
• Administer entire contents of the vial to ensure the correct dose is provided.

SubQ:

• Administer SubQ into the abdomen only.
• Choose an injection site with adequate subcutaneous tissue without any skin conditions (eg, bruising, excessive pigment, infection, irritation, lesions, nodules, redness, or scarring).
• It is recommended that the patient be in the supine position.
• Keep rotating injection sites.
• Lump may form at injection site, which reduces in sizes over few weeks.
• Do not rub injection site; be careful of the placement of any belts or clothing waistbands.

Mechanism of action of Risperidone (Risperdal):

• Risperidone, a benzisoxazole antipsychotic atypical with potent 5-HT-2A activity and dopamine D2 receptor antagonist activity, is a benzisoxazole.
• High affinity can also be used to antagonize alpha-1, alpha-adrenergic and histaminergic receptors.
• Risperidone is low to moderately affine for 5-HT-1A, 5-HT-1C, and 5-HT-1D receptors. It also has weak affinity for D-1. There is no affinity for beta or muscarinic receptors.

Absorption:

• Oral:
  • Rapid and well absorbed; no association with food intake
• IM:
  • <1% absorbed initially; major release occurs at ~3 weeks and is maintained from 4 to 6 weeks; ends by 7 weeks
• SubQ:
  • Two absorption peaks; first release occurs immediately post-injection and second release occurs 10 to 14 days later; therapeutic levels maintained for 4 weeks post-injection.

Protein binding, plasma:

• Risperidone 90%; 9-hydroxyrisperidone: 77%;
• Note: Risperidone free fraction may be increased by ~35% in patients with hepatic impairment because of reduced concentrations of albumin and alpha-1 acid glycoprotein

Metabolism:

• Mostly hepatic via CYP2D6 to 9-hydroxyrisperidone (similar pharmacological activity as risperidone); N-dealkylation is another minor pathway;
• Note: 9-hydroxyrisperidone is the predominant circulating form and is approximately equal to risperidone in receptor binding activity;
• clinical effects are due to combined concentrations of risperidone and 9hydroxyrisperidone; no clinically important differences expected between CYP2D6 poor and extensive metabolizers.

Bioavailability:

• Oral: 70%;
  • Tablet (relative to solution): 94%;
  • orally-disintegrating tablets and oral solution are bioequivalent to tablets
• IM: Deltoid IM injection is bioequivalent to gluteal IM injection

Half-life elimination: Active moiety (risperidone and its active metabolite 9-hydroxyrisperidone): Oral: 20 hours (mean); prolonged in elderly patients

• Extensive metabolizers: Risperidone: 3 hours; 9-hydroxyrisperidone: 21 hours
• Poor metabolizers: Risperidone: 20 hours; 9-hydroxyrisperidone: 30 hours

IM: 3 to 6 days; related to microsphere erosion and subsequent absorption of risperidone Risperidone: SubQ: 9 to 11 days Time to peak, plasma:

• Oral: Risperidone: Within 1 hour; 9-hydroxyrisperidone: Extensive metabolizers: 3 hours; Poor metabolizers: 17 hours
• SubQ: Risperidone: First peak: 4 to 6 hours; Second peak: 10 to 14 days

Excretion:

• Urine (70%);
• feces (14%)

International Brand Names of Risperidone:

• Perseris
• RisperDAL
• RisperDAL Consta
• RisperDAL M-TAB
• risperiDONE M-TAB
• ACT Risperidone
• AG-Risperidone
• APO-Risperidone
• DOM-Risperidone
• JAMP-Risperidone
• JOI-Risperidone
• Mar-Risperidone
• MINT-Risperidon
• MYLAN-Risperidone ODT
• MYLAN-Risperidone
• PHL-Risperidone
• PMS-Risperidone
• PMS-Risperidone ODT
• PRO-Risperidone
• RAN-Risperidone
• RATIO-Risperidone
• RisperDAL
• RisperDAL Consta
• RisperDAL M-TAB
• RIVA-Risperidone
• SANDOZ Risperidone
• TEVA-Risperidone
• Aleptolan
• Anxilet
• Apexidone
• Arketin
• Aspidon
• Calmapride
• Diaforin
• Dyperidone
• Eperon
• Eridon
• Goval
• Ispidon
• Luvenil
• Mirabril
• Neirispin
• Neorisp
• Neripros
• Neuris
• Nodiril
• Noprenia
• Noprenia OS
• Ozidal
• Perdamel
• Persidal-2
• Prospera
• Psychodal
• Raxidone
• Renuvie
• Respal
• Resperiteg
• Revoc
• Riatul
• Ridal
• Ridkline
• Rileptid
• Riper
• Riperidon
• Riscord
• Risdin
• Risdon
• Risfree
• Risnia
• Rison
• Risoperin
• Rispa
• Rispaxol
• Rispefar
• Risperdal
• Risperdal Const
• Risperdal Consta
• Risperdal OD
• Risperdal Quicklet
• Risperdalconsta LP
• Risperidex
• Risperigamma
• Risperiteg
• Risperon
• Rispeva
• Rispid
• Rispolept
• Rispolet
• Rispond
• Rispone
• Rispons
• Risset
• Rixadone
• Rkdone
• Sequinan
• Spiron
• Steviso
• Torendo
• Xenoma
• Zofredal
• Zyresp
• Ñorispez

Risperidone Brand Names in Pakistan: