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Risperidone
Class: Atypical Antipsychotics
VA Class: CN709
Chemical Name: 3-[2-[4-(6-Fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl]-6,7,8, 9-tetrahydro-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one
Molecular Formula: C23H27FN4O2

Introduction

 Its Benzisothiazol-derivative; atypical or second-generation antipsychotic agent.

Uses of Risperidone

Schizophrenia

Orally and IM (as extended-release injection) for the treatment of schizophrenia.
American Psychiatric Association (APA) considers most atypical antipsychotic agents first-line drugs for management of the acute phase of schizophrenia (including first psychotic episodes)

Bipolar Disorder

Orally for the treatment (alone or in combination with lithium or valproate) of acute manic or mixed episodes associated with bipolar I disorder (bipolar mania)

Autistic Disorder

Orally for the management of irritability associated with autistic disorder, including symptoms of aggression towards others, deliberate self-injuriousness, temper tantrums, and quickly changing moods

Risperidone Dosage and Administration

Administration

Administer orally or IM.1 103

Oral Administration

Administer orally once or twice (in equally divided doses) daily without regard to meals.1 14
Twice-daily administration may be helpful in pediatric patients with schizophrenia or bipolar mania who experience persistent somnolence.
Twice-daily administration also may minimize risk of orthostatic hypotension and syncope in geriatric patients and in patients with renal or hepatic impairment.
Do not remove orally disintegrating tablets from the blister until just prior to administration.1 With dry hands, peel back the blister foil backing to expose the tablet. Do not push the tablet through the foil, since this may damage the tablet.1 Gently remove the tablet and immediately place on tongue, where it rapidly disintegrates in saliva, and then swallow with or without liquid

Dosage

If risperidone is used concurrently with a CYP enzyme inducer or CYP2D6 inhibitor, dosage adjustment may be required.
If risperidone is reinitiated after a drug-free period, titrate oral dosage as with initial therapy.1

Pediatric Patients

Schizophrenia
Oral

Adolescents ≥13 years of age: Initially, 0.5 mg once daily in the morning or evening.
Adjust dosage, if indicated, in increments of 0.5–1 mg daily at intervals of ≥24 hours to target dosage of 3 mg daily.
Dosages >3 mg daily did not result in greater efficacy and were associated with increased adverse effects. Antipsychotic efficacy demonstrated in dosage range of 1–6 mg daily in clinical trials; dosages >6 mg daily not studied
Twice-daily administration may be helpful in pediatric patients experiencing persistent somnolence.
Efficacy maintained for up to 2 years in adults, but optimum duration of therapy currently not known. In responding patients, continue therapy at the effective dosage; periodically reassess need for continued therapy.

Bipolar Disorder
Oral

Children and adolescents 10–17 years of age: Initially, 0.5 mg once daily in the morning or evening.1
Adjust dosage, if indicated, in increments of 0.5–1 mg daily at intervals of ≥24 hours to target dosage of 1–2.5 mg daily.1
Dosages >2.5 mg daily did not result in greater efficacy, but were associated with increased adverse effects.1
Antimanic efficacy demonstrated in dosage range of 0.5–6 mg daily in clinical trials; dosages >6 mg daily not studied.1
Twice-daily administration may be helpful in pediatric patients experiencing persistent somnolence.1
If used for extended periods (i.e., >3 weeks), periodically reevaluate long-term risks and benefits for the individual patient

Irritability associated with Autistic Disorder
Oral

Children ≥5 years of age and adolescents weighing <20 kg: Initially, 0.25 mg daily; may administer once daily or in divided doses twice daily.1 31 105 May increase dosage to 0.5 mg daily after ≥4 days; maintain this dosage for ≥14 days.1 In patients not responding adequately, may increase dosage in increments of 0.25 mg daily in ≥2-week intervals.1 Individualize dosage based on clinical response and tolerability; once adequate clinical response achieved and maintained, consider gradually reducing dosage.1
Children ≥5 years of age and adolescents weighing ≥20 kg: Initially, 0.5 mg daily; may administer once daily or in divided doses twice daily. May increase dosage to 1 mg daily after ≥4 days; maintain this dosage for ≥14 days. In patients not responding adequately, may increase dosage in increments of 0.5 mg daily in ≥2-week intervals. Individualize dosage based on clinical response and tolerability; once adequate clinical response achieved and maintained, consider gradually reducing dosage.
Overall efficacy demonstrated in dosage range of 0.5–3 mg daily. In the main clinical trials, 90% of patients who responded to therapy received dosages from 0.5–2.5 mg daily.Maximum daily dosage (i.e., when therapeutic effect reached a plateau) in one trial was 1 mg in patients weighing <20 kg, 2.5 mg in patients weighing ≥20 kg, and 3 mg in patients weighing >45 kg.
Dosing data not available for children weighing <15 kg.
Patients experiencing persistent somnolence may benefit from a once-daily dosage administered at bedtime, administering half the daily dosage twice daily, or a reduction in dosage.
If used for extended periods, periodically reevaluate long-term risks and benefits for the individual patient

Adults

Schizophrenia
Oral

Initially, 2 mg daily (as 2 mg once daily or 1 mg twice daily), with increases in increments of 1–2 mg daily at intervals of ≥24 hours, as tolerated, to target dosage of 4–8 mg daily (once daily or in 2 equally divided doses) recommended by manufacturers.1 115 The manufacturers state that slower dosage titration may be appropriate in certain patients.1 115
Alternatively, an initial dosage of 1–2 mg daily, with increases in increments of 0.5–1 mg daily titrated over 6–7 days, as tolerated, to target dosage of 4 mg daily may be more appropriate in most otherwise healthy adults
Lower initial dosages (e.g., 1 mg daily) and slower dosage titrations to an initial target dosage of 2 mg daily may be appropriate for younger patients and those being treated for their first psychotic episode. Titrate dosage up to 4 mg daily depending on clinical response and adverse neurologic effects; 1–3 mg daily may be optimal
Efficacy generally observed in dosage range of 4–16 mg daily; dosages >6 mg daily (given twice daily) did not result in greater efficacy, but were associated with increased adverse effects (e.g., extrapyramidal symptoms) and are generally not recommended. In a study of once-daily dosing, efficacy of 8-mg dosage generally was better than for 4-mg dosage.
Efficacy maintained for up to 2 years in adults, but optimum duration of therapy currently not known. In responding patients, continue therapy at their effective dosage; periodically reassess need for continued therapy
In patients with remitted first or multiple episodes, APA recommends either indefinite maintenance therapy or gradual discontinuance of the antipsychotic with close follow-up and a plan to reinstitute treatment upon symptom recurrence. Consider antipsychotic therapy discontinuance only after ≥1 year of symptom remission or optimal response while receiving the drug. Indefinite maintenance treatment recommended if patient has experienced multiple previous psychotic episodes or 2 episodes within 5 years

Bipolar Disorder
Acute Manic or Mixed Episodes

Oral
As monotherapy or adjunctive therapy with lithium or valproate, initially 2–3 mg once daily.
Adjust dosage, if indicated, in increments or decrements of 1 mg daily at intervals of ≥24 hours.
Antimanic efficacy demonstrated in dosage range of 1–6 mg daily; dosages >6 mg daily not studied.
If used for extended periods (i.e., >3 weeks), periodically reevaluate long-term risks and benefits for the individual patient

Maintenance Treatment

IM
As monotherapy or adjunctive therapy with lithium or valproate, 25 mg IM every 2 weeks
Lower initial dosage of 12.5 mg IM every 2 weeks may be appropriate in certain patients (e.g., renal or hepatic impairment, concurrent use of drugs that can increase risperidone plasma concentrations); however, efficacy of this dosage not systematically evaluated in clinical trials
Administer oral risperidone (or another antipsychotic agent) with the first IM risperidone injection and continue oral therapy for 3 weeks thereafter to ensure adequate therapeutic plasma concentrations are maintained prior to main release of risperidone from injection site
Some patients not responding to 25 mg may benefit from dosages of 37.5 or 50 mg IM every 2 weeks, although dose response for efficacy not established.
Dosages >50 mg IM every 2 weeks not studied
Increase dosage at intervals of ≥4 weeks. Clinical effects of the increased dosage generally occur ≥3 weeks after the first injection at the higher dosage.
If reinitiating IM risperidone after a drug-free period, administration of oral risperidone (or another antipsychotic agent) initially for supplementation will be needed
If used for extended periods, periodically reevaluate long-term risks and benefits for the individual patient

Bipolar Disorder
Acute Manic or Mixed Episodes

Oral
As monotherapy or adjunctive therapy with lithium or valproate, initially 2–3 mg once daily.
Adjust dosage, if indicated, in increments or decrements of 1 mg daily at intervals of ≥24 hours
Antimanic efficacy demonstrated in dosage range of 1–6 mg daily; dosages >6 mg daily not studied.
If used for extended periods (i.e., >3 weeks), periodically reevaluate long-term risks and benefits for the individual patient.

Maintenance Treatment

IM
As monotherapy or adjunctive therapy with lithium or valproate, 25 mg IM every 2 weeks
Lower initial dosage of 12.5 mg IM every 2 weeks may be appropriate in certain patients (e.g., renal or hepatic impairment, concurrent use of drugs that can increase risperidone plasma concentrations); however, efficacy of this dosage not systematically evaluated in clinical trials. (See Hepatic Impairment and Renal Impairment under Dosage and Administration, and also see Interactions.)
Administer oral risperidone (or another antipsychotic agent) with the first IM risperidone injection and continue oral therapy for 3 weeks thereafter to ensure adequate therapeutic plasma concentrations are maintained prior to main release of risperidone from injection site. Some patients not responding to 25 mg may benefit from dosages of 37.5 or 50 mg IM every 2 weeks, although dose response for efficacy not established.
Dosages >50 mg IM every 2 weeks not studied.
Increase dosage at intervals of ≥4 weeks. Clinical effects of the increased dosage generally occur ≥3 weeks after the first injection at the higher dosage
If reinitiating IM risperidone after a drug-free period, administration of oral risperidone (or another antipsychotic agent) initially for supplementation will be needed.
If used for extended periods, periodically reevaluate long-term risks and benefits for the individual patient

Risperidone Pharmacokinetics

Absorption

Bioavailability

Well absorbed after oral administration, with peak plasma concentrations of risperidone attained in approximately 1 hour.1
Mean peak plasma concentrations of the major active metabolite, 9-hydroxyrisperidone, occur at about 3 and 17 hours in patients who are extensive and poor metabolizers of CYP2D6, respectively.1 Steady state of risperidone reached in 1 day in extensive metabolizers and expected in 5 days in poor metabolizers; 9-hydroxyrisperidone steady state reached in 5–6 days in extensive metabolizers.1
Absolute bioavailability is 70%; relative oral bioavailability from a tablet is 94% compared with a solution.1
Commercially available conventional and orally disintegrating tablets and oral solution are bioequivalent.

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